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Tenovir
Atenolol
Tenovir
Atenolol
Indications
Tachycardia
Indication detailsView
Atenolol is indicated-
- In the management of hypertension. It may be used alone or concomitantly with other antihypertensive agents, particularly with a thiazide-type diuretic.
- For the long-term management of patients with angina pectoris.
- In the management of hemodynamically stable patients with defnite or suspected acute myocardial infarction to reduce cardiovascular mortality.
Therapeutic classView
Beta-adrenoceptor blocking drugs, Beta-blockers
PharmacologyView
The synthesis of atenolol resulted from attempts to produce a β-adrenoceptor antagonist that would competitively block β1 (cardiac) receptors but have no effect on β2-receptors. It is classified as a β1 selective (cardioselective) β-adrenergic receptor antagonist with no membranestability activity and no partial agonist activity. It is markedly the most hydrophilic of the currently available β- blockers and thus penetrates the lipid of cell membranes poorly
DosageView
Hypertension: The initial dose of Atenolol is 50 mg given as one tablet a day either alone or added to diuretic therapy. The full effect of this dose will usually be seen within one to two weeks. If an optimal response is not achieved, the dosage should be increased to Atenolol 100 mg given as one tablet a day. Increasing the dosage beyond 100 mg a day is unlikely to produce any further benefit.
Angina Pectoris: The initial dose of Atenolol is 50 mg given as one tablet a day. If an optimal response is not achieved within one week, the dosage should be increased to Atenolol 100 mg given as one tablet a day. Some patients may require a dosage of 200 mg once a day for optimal effect. Twenty-four hour control with once daily dosing is achieved by giving doses larger than necessary to achieve an immediate maximum effect. The maximum early effect on exercise tolerance occurs with doses of 50 to 100 mg, but at these doses the effect at 24 hours is attenuated, averaging about 50% to 75% of that observed with once a day oral doses of 200 mg.
Acute Myocardial Infarction: In patients with definite or suspected acute myocardial infarction, treatment with Atenolol I.V. Injection should be initiated as soon as possible after the patient's arrival in the hospital and after eligibility is established. Treatment should begin with the intravenous administration of 5 mg Atenolol over 5 minutes followed by another 5 mg intravenous injection 10 minutes later. In patients who tolerate the full intravenous dose (10 mg), Atenolol Tablets 50 mg should be initiated 10 minutes after the last intravenous dose followed by another 50 mg oral dose 12 hours later. Thereafter, Atenolol can be given orally either 100 mg once daily or 50 mg twice a day for a further 6-9 days or until discharge from the hospital. If bradycardia or hypotension requiring treatment or any other untoward effects occur, Atenolol should be discontinued.
Angina Pectoris: The initial dose of Atenolol is 50 mg given as one tablet a day. If an optimal response is not achieved within one week, the dosage should be increased to Atenolol 100 mg given as one tablet a day. Some patients may require a dosage of 200 mg once a day for optimal effect. Twenty-four hour control with once daily dosing is achieved by giving doses larger than necessary to achieve an immediate maximum effect. The maximum early effect on exercise tolerance occurs with doses of 50 to 100 mg, but at these doses the effect at 24 hours is attenuated, averaging about 50% to 75% of that observed with once a day oral doses of 200 mg.
Acute Myocardial Infarction: In patients with definite or suspected acute myocardial infarction, treatment with Atenolol I.V. Injection should be initiated as soon as possible after the patient's arrival in the hospital and after eligibility is established. Treatment should begin with the intravenous administration of 5 mg Atenolol over 5 minutes followed by another 5 mg intravenous injection 10 minutes later. In patients who tolerate the full intravenous dose (10 mg), Atenolol Tablets 50 mg should be initiated 10 minutes after the last intravenous dose followed by another 50 mg oral dose 12 hours later. Thereafter, Atenolol can be given orally either 100 mg once daily or 50 mg twice a day for a further 6-9 days or until discharge from the hospital. If bradycardia or hypotension requiring treatment or any other untoward effects occur, Atenolol should be discontinued.
Side effectsView
In a series of investigations in the treatment of acute myocardial infarction, bradycardia and hypotension occurred more commonly, as expected for any beta blocker. In addition, a variety of adverse efects has been reported with other beta-adrenergic blocking agents, and may be considered potential adverse efects of Atenolol.
- Hematologic: Agranulocytosis.
- Allergic: Fever, combined with aching and sore throat, laryngospasm, and respiratory distress.
- Central Nervous System: Reversible mental depression progressing to catatonia; an acute reversible syndrome characterized by disorientation of time and place; short term memory loss; emotional lability with slightly clouded sensorium; and, decreased performance on neuropsychometrics.
- Gastrointestinal: Mesenteric arterial thrombosis, ischemic colitis.
- Miscellaneous: There have been reports of skin rashes and/or dry eyes associated with the use of beta-adrenergic blocking drugs. Discontinuance of the drug should be considered if any such reaction is not otherwise explicable. Patients should be closely monitored following cessation of therapy.
- Other: Erythematous rash
ContraindicationsView
Atenolol is contraindicated in-
- Sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure.
- Those patients with a history of hypersensitivity to the atenolol or any of the drug product’s components.
PrecautionsView
General: Patients already on a beta blocker must be evaluated carefully before Atenolol is administered. Initial and subsequent Atenolol dosages can be adjusted downward depending on clinical observations including pulse and blood pressure. Atenolol may aggravate peripheral arterial circulatory disorders.
Impaired Renal Function: The drug should be used with caution in patients with impaired renal function.
Geriatric Use:
Impaired Renal Function: The drug should be used with caution in patients with impaired renal function.
Geriatric Use:
- Hypertension and Angina Pectoris: Due to Coronary Atherosclerosis: Dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
- Acute Myocardial Infarction: Dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. Evaluation of patients with hypertension or myocardial infarction should always include assessment of renal function.
InteractionsView
- Catecholamine-depleting drugs (eg, reserpine) may have an additive effect when given with beta-blocking agents. Patients treated with Atenolol plus a catecholamine depletor should therefore be closely observed for evidence of hypotension and/or marked bradycardia which may produce vertigo, syncope, or postural hypotension.
- Calcium channel blockers may also have an additive effect when given with Atenolol.
- Disopyramide is a Type I antiarrhythmic drug with potent negative inotropic and chronotropic effects. Disopyramide has been associated with severe bradycardia, asystole and heart failure when administered with beta blockers.
- Amiodarone is an antiarrhythmic agent with negative chronotropic properties that may be additive to those seen with beta blockers.
- Beta blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. If the two drugs are coadministered, the beta blocker should be withdrawn several days before the gradual withdrawal of clonidine. If replacing clonidine by beta-blocker therapy, the introduction of beta blockers should be delayed for several days after clonidine administration has stopped.
- Concomitant use of prostaglandin synthase inhibiting drugs, eg, indomethacin, may decrease the hypotensive effects of beta blockers.
- While taking beta blockers, patients with a history of anaphylactic reaction to a variety of allergens may have a more severe reaction on repeated challenge, either accidental, diagnostic or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat the allergic reaction.
- Both digitalis glycosides and beta-blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase the risk of bradycardia.
Pregnancy & lactationView
Pregnancy Category D. Caution should be exercised when Atenolol is administered to a nursing woman. Clinically significant bradycardia has been reported in breast-fed infants. Premature infants, or infants with impaired renal function, may be more likely to develop adverse effects.
Pediatric usageView
Elderly Patients or Patients with Renal Impairment: Atenolol is excreted by the kidneys; consequently dosage should be adjusted in cases of severe impairment of renal function. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, refecting greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. The following maximum oral dosages are recommended for elderly, renal impaired patients and for patients with renal impairment due to other causes:
- Creatinine clearance 15-35 ml/min/1.73 m2: Maximum dosage 50 mg daily
- Creatinine clearance <15 mL/min/1.73 m2: Maximum dosage 25 mg daily
Overdose effectsView
Overdosage with Atenolol has been reported with patients surviving acute doses as high as 5 g. One death was reported in a man who may have taken as much as 10 g acutely. The predominant symptoms reported following Atenolol overdose are lethargy, disorder of respiratory drive, wheezing, sinus pause and bradycardia. Additionally, common efects associated with overdosage of any beta-adrenergic blocking agent and which might also be expected in Atenolol overdose are congestive heart failure, hypotension, bronchospasm and/or hypoglycemia. Treatment of overdose should be directed to the removal of any unabsorbed drug by induced emesis, gastric lavage, or administration of activated charcoal. Atenolol can be removed from the general circulation by hemodialysis. Based on the severity of symptoms, management may require intensive support care and facilities for applying cardiac and respiratory support.
StorageView
Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician.
Tenoviral
Tenofovir Disoproxil Fumarate
Tenoviral
Tenofovir Disoproxil Fumarate
Indications
HIV infection
Indication detailsView
This is indicated for the treatment of:
- Chronic hepatitis B virus infection in adults
- HIV infected adults in combination with other anti retroviral agents
Therapeutic classView
Drugs for HIV / Anti-retroviral drugs, Hepatic viral infections (Hepatitis B)
PharmacologyView
Tenofovir Disoproxil Fumarate, an acyclic nucleotide analogue of adenosine monophosphate, is a pro-drug of Tenofovir. It shows activity against hepatitis B virus polymerase and HIV reverse transcriptase after phosphorylation to the active diphosphate form. Tenofovir diphosphate inhibits viral polymerase (reverse transcriptase) by directly competing with the natural substrate deoxyribonucleotide and by causing DNA chain termination after its incorporation into viral DNA.
DosageView
The recommended dose of Tenofovir in chronic hepatitis B virus infection in adults 18 years of age and older with adequate renal function is 300 mg once daily with or without food.
Side effectsView
The most common side effects are nausea, vomiting, diarrhea and flatulence.
ContraindicationsView
Tenofovir is contraindicated in patients with known hypersensitivity to Tenofovir or any component of the product.
PrecautionsView
Co-administration with other drugs: Tenofovir should not be administered concurrently with Emtricitabine & Tenofovir combination or Adefovir Dipivoxil.
Lactic Acidosis & Severe Hepatomegaly with Steatosis: Though the risk of occurrence of lactic acidosis is low for Tenofovir, treatment should be suspended in any patient who develops lactic acidosis or hepatotoxicity.
Exacerbation of hepatitis after discontinuation of treatment: Discontinuation of Tenofovir
therapy may be associated with severe acute exacerbation of hepatitis.
Lactic Acidosis & Severe Hepatomegaly with Steatosis: Though the risk of occurrence of lactic acidosis is low for Tenofovir, treatment should be suspended in any patient who develops lactic acidosis or hepatotoxicity.
Exacerbation of hepatitis after discontinuation of treatment: Discontinuation of Tenofovir
therapy may be associated with severe acute exacerbation of hepatitis.
InteractionsView
Co-administration of Tenofovir with anti-retroviral, entecavir, lamivudine, methadone, oral contraceptives, ribavirin and tacrolimus did not result in significant drug interactions. The effects of co-administration of Tenofovir with other drugs that are renally eliminated or are known to affect renal function have not been evaluated.
Pregnancy & lactationView
Pregnancy: Pregnancy category B. It should be used during pregnancy only if clearly needed.
Lactation: It is not known whether it is excreted in human milk. Mothers should be instructed not to breast feed if they are taking Tenofovir.
Lactation: It is not known whether it is excreted in human milk. Mothers should be instructed not to breast feed if they are taking Tenofovir.
Pediatric usageView
Pediatric use: Safety and effectiveness of Tenofovir in pediatric patients below the age of 18 years have not been established.
Geriatrics use: Clinical studies of Tenofovir did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects. But care should be taken in dose selection, and it may be useful to monitor renal function.
Renal Impairment: Haemodialysis patients: 300 mg once every 7 days or after a cumulative total of 12 hr of dialysis.
Geriatrics use: Clinical studies of Tenofovir did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects. But care should be taken in dose selection, and it may be useful to monitor renal function.
Renal Impairment: Haemodialysis patients: 300 mg once every 7 days or after a cumulative total of 12 hr of dialysis.
- CrCl (10-29 mL/min): 300 mg 72-96 hrly.
- CrCl (30-49 mL/min): 300 mg 48 hrly.
Overdose effectsView
There is no experience of Tenofovir overdose reported in patients
StorageView
Store in a cool and dry place, protected from light and moisture. Keep the medicine out of the reach of children.
Tenoxim
Tenoxicam
Tenoxim
Tenoxicam
Indications
Pain and inflammation associated with musculoskeletal and joint disorders
Indication detailsView
Tenoxicam is indicated for the symptomatic treatment of the following painful inflammatory and degenerative disorders of the musculoskeletal system:
- Rheumatoid arthritis.
- Osteoarthritis.
- Arthrosis.
- Ankylosing spondylitis.
- Extra-articular disorders, e.g. tendinitis, bursitis, periarthritis of the shoulders (shoulder-hand syndrome) or hips, strains, and sprains.
- Acute gout.
Therapeutic classView
Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
PharmacologyView
Tenoxicam is a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic properties and it also inhibits platelet aggregation. Tenoxicam inhibits prostaglandin biosynthesis. In-vitro tests of leukocyte peroxidase suggest that tenoxicam may act as a scavenger for active oxygen at the site of inflammation. Tenoxicam is a potent in-vitro inhibitor of human metalloproteinases (stromelysin and collagenase), which induce cartilage breakdown. These pharmacological effects explain, at least in part, the therapeutic benefit of Tenoxicam in the treatment of painful inflammatory and degenerative disorders of the musculoskeletal system. Tenoxicam showed no mutagenic, carcinogenic or teratogenic effects in animals. As with other prostaglandin inhibitors, renal and gastrointestinal effects, increased incidence of dystocia and delayed parturition were observed in animal safety studies.
DosageView
Standard dosage: For all indications except acute gout, a daily dosage of 20 mg should be given at the same time of day.
In acute attacks of gout: The recommended dose for acute attacks of gout is 40 mg once daily for two days followed by 20 mg once daily for a further five days.
In the treatment of chronic disorders: The therapeutic effect of tenoxicam is evident early in treatment but there is a progressive increase in response over time. In chronic disorders, daily doses higher than 20 mg should be avoided since this would increase the frequency and intensity of unwanted reactions without significantly increasing efficacy. For patients needing long-term treatment, a reduction to a daily oral dose of 10 mg may be tried for maintenance.
Special dosage instructions: In principle, the above dosage recommendations also apply to elderly patients and to patients suffering from kidney or liver disease. Because of lack of clinical experience, no dosage recommendations have so far been established for children and adolescents.
In acute attacks of gout: The recommended dose for acute attacks of gout is 40 mg once daily for two days followed by 20 mg once daily for a further five days.
In the treatment of chronic disorders: The therapeutic effect of tenoxicam is evident early in treatment but there is a progressive increase in response over time. In chronic disorders, daily doses higher than 20 mg should be avoided since this would increase the frequency and intensity of unwanted reactions without significantly increasing efficacy. For patients needing long-term treatment, a reduction to a daily oral dose of 10 mg may be tried for maintenance.
Special dosage instructions: In principle, the above dosage recommendations also apply to elderly patients and to patients suffering from kidney or liver disease. Because of lack of clinical experience, no dosage recommendations have so far been established for children and adolescents.
AdministrationView
The tablets should be taken with a glass of water. It is preferable to take this medicine during or immediately after a meal.
Side effectsView
Based on clinical trials including large numbers of patients, Tenoxicam proved to be well tolerated in the recommended dose. Usually, the undesirable effects reported were mild and transient. In a small proportion of patients, the interruption of treatment due to undesirable effects was necessary. Local tolerance of Tenoxicam given parenterally was good. The following undesirable effects have been reported:
Frequency is greater than 1%-
Frequency is greater than 1%-
- Gastrointestinal tract: gastric, epigastric and abdominal discomfort, dyspepsia, heartburn, nausea.
- Central nervous system: dizziness, headache.
- Gastrointestinal tract: constipation, diarrhea, stomatitis, gastritis, vomiting, ulcers, Gl-bleeding including hematemesis and melena.
- Central nervous system: fatigue, sleep disturbances, appetite loss, dry mouth, vertigo.
- Skin: itching (also in the anal region after rectal administration), erythema, exanthema, rash, urticaria.
- Urinary tract and kidneys: increase in BUN or creatinine, edema.
- Liver and biliary tract: increased liver enzyme activity.
- Cardiovascular system: palpitations.
- Gastrointestinal tract: Gl-perforation.
- Central nervous system: visual disturbances.
- Skin: Stevens-Johnson and Lyell's syndrome, photosensitivity reaction, vasculitis.
- Blood: anemia, agranulocytosis, leukopenia, thrombocytopenia.
- Hypersensitivity reactions: dyspnea, asthma, anaphylaxis, angioedema.
- Cardiovascular system: elevated blood pressure, mainly in patients treated with cardiovascular drugs.
- Liver/Biliary tract: hepatitis.
ContraindicationsView
Tenoxicam must not be administered to patients:
- known to be hypersensitive to the drug;
- in whom salicylates or other non-steroidal anti-inflammatory drugs (NSAIDs) induce symptoms of asthma, rhinitis, or urticaria;
- suffering or having suffered from the disease of the upper gastrointestinal tract, such as gastritis, gastric and duodenal ulcer.
PrecautionsView
NSAIDs inhibit renal prostaglandin synthesis and consequently may have an undesirable effect on renal hemodynamics and on salt and water balance. It is necessary to adequately monitor the patient with a special emphasis on cardiac and renal function (BUN, creatinine, development of edema, weight gain, etc.) when giving Tenoxicam to patients with conditions that could increase their risk of developing renal failure, such as pre-existing renal disease, impaired renal function in diabetics, hepatic cirrhosis, congestive heart failure, volume depletion or concomitant treatment with potentially nephrotoxic drugs, diuretics and corticosteroids. Tenoxicam inhibits platelet aggregation and may affect hemostasis. Tenoxicam has no significant influence on blood coagulation factors, coagulation time, prothrombin time or activated thromboplastin time. Patients having coagulation disorders or receiving drug therapy that interferes with hemostasis should, however, be carefully observed when Tenoxicam is administered. Any patient being treated with Tenoxicam who presents with symptoms of gastrointestinal disease should be closely monitored. If peptic ulceration or gastrointestinal bleeding occurs, Tenoxicam should be immediately withdrawn. If severe skin reactions (e.g. Lyell's or Stevens-Johnson syndrome) occur, the treatment should be discontinued immediately. Adverse eye findings have been reported with Tenoxicam. Thus ophthalmic evaluation is recommended for patients who develop visual disturbances. Because of the high plasma protein binding of tenoxicam, caution is required when plasma albumin levels are markedly reduced. In common with anti-inflammatory drugs, Tenoxicam may mask the usual signs of infection. Tenoxicam Tablets should not be given to patients who either dislike or do not tolerate milk products.
InteractionsView
As in the case of other NSAIDs, salicylate displaces tenoxicam from protein-binding sites and increases clearance and volume of distribution of tenoxicam. Concurrent treatment with salicylate or other NSAIDs should be avoided because of increased risk of gastrointestinal undesirable reactions. The co-administration of some NSAIDs and methotrexate has been associated with reduced renal tubular secretion of methotrexate, higher plasma concentrations of methotrexate, and severe methotrexate toxicity. Therefore, caution should be exercised when Tenoxicam is administered concurrently with methotrexate. No clinically relevant interaction was found in the small number of patients receiving concomitant treatment with gold, penicillamine or probenecid. As Tenoxicam may decrease the renal clearance of lithium, their concomitant administration may lead to increased plasma levels and toxicity of lithium. The plasma levels of lithium should be closely monitored. As with NSAIDs in general, Tenoxicam should not be administered concurrently with K-sparing diuretics. There is a known interaction between these two classes of compounds, which may cause hyperkalemia and renal failure. No clinically significant interaction between Tenoxicam and furosemide was noted, but Tenoxicam attenuates the blood pressure-lowering effect of hydrochlorothiazide. As known from other NSAIDs, Tenoxicam might attenuate the antihypertensive effects of alpha-adrenergic blockers and ACE-inhibitors. No interactions have been reported between NSAIDs and centrally-acting alpha agonists or calcium channel blockers. There was no clinically relevant interaction when Tenoxicam was administered together with atenolol. During clinical trials no interaction was reported for patients treated concomitantly with digitalis products. Thus concurrent dosing of Tenoxicam and digoxin appears to be without major risk. No interaction has been found with concomitantly administered antacids, cimetidine, warfarin and phenprocoumon at the recommended dosages. The clinical effect of oral antidiabetic drugs (glibornuride, glibenclamide, tolbutamide) was likewise not modified by Tenoxicam. Nevertheless, careful monitoring is recommended when patients concomitantly receive anticoagulants or oral antidiabetic drugs. No clinically relevant interaction has been found between Tenoxicam and low molecular weight heparin.
Pregnancy & lactationView
NSAIDs have an inhibitory effect on prostaglandin synthesis and, when given during late pregnancy, may cause the closure of the fetal ductus arteriosus, prolong labor and delay parturition. Treatment during the third trimester of pregnancy should be avoided. Based on findings from single-dose administration, a very small amount (approximately 0.2%) of tenoxicam passes into breast milk. There is no evidence of adverse reactions in breast-fed infants of mothers taking Tenoxicam. Nevertheless, infants should be weaned or the drug discontinued.
Pediatric usageView
Use in Children & adolescent: Tenoxicam is not recommended for use in patients under 16 years of age, as the dose and indications in this population have not been established.
Effects on ability to drive and use machines: Patients experiencing adverse events that might affect driving or using machines, such as vertigo, dizziness or visual disturbances should refrain from driving a car or using machines.
Effects on ability to drive and use machines: Patients experiencing adverse events that might affect driving or using machines, such as vertigo, dizziness or visual disturbances should refrain from driving a car or using machines.
Overdose effectsView
Although there is no experience of acute overdosage with Tenoxicam, it may be expected that the signs and symptoms mentioned under Undesirable effects would be more pronounced. Overdose should be countered by conventional measures to reduce absorption (e.g. gastrolavage and charcoal) and speed up elimination (e.g. cholestyramine).
StorageView
Do not store above 30°C, protect from light & moisture. Keep out of the reach of children.
Tensa
Flupentixol + Melitracen
Tensa
Flupentixol + Melitracen
Indications
Psychosis
Indication detailsView
Flupentixol and Melitracen tablet is indicated in-
- Anxiety
- Depression
- Apathy
- Psychogenic depression.
- Depressive neurosses.
- Masked depression.
- Psychosomatic affections accompanied by anxiety and apathy.
- Menopausal depressions.
- Dysphoria and depression in alcoholics and drug addicts.
Therapeutic classView
Combined anxiolytics & anti-depressant drugs
PharmacologyView
This consists of two well known and well proven compounds: flupentixol-a neuroleptic with anxiolytic and antidepressant properties of its own when given in small doses, and melitracen-a bipolar thymoleptic with activating properties in low doses. In combination the compounds render a preparation with antidepressant, anxiolytic and activating properties. Maximal serum concentration is reached in about 4 hours after oral administration of flupentixol and in about 4 hours after oral administration of melitracen. The biological half-life of flupentixol is about 35 hours and that of melitracen is about 19 hours. The combination of flupentixol and melitracen does not seem to influence the pharmacokinetic properties of the individual compounds.
DosageView
Adults: Usually 2 tablets orally daily in the morning and noon. In severe cases, the morning dose may be increased to 2 tablets.
Elderly patients: 1 tablet in the morning.
Maintenance dose: Usually 1 tablet orally in the morning. In cases of insomnia or severe restlessness, additional treatment with a sedative in the acute phase is recommended.
Elderly patients: 1 tablet in the morning.
Maintenance dose: Usually 1 tablet orally in the morning. In cases of insomnia or severe restlessness, additional treatment with a sedative in the acute phase is recommended.
Side effectsView
In the recommended doses side effects are rare. These could be transient restlessness and insomnia.
ContraindicationsView
- The immediate recovery phase after myocardial infarction.
- Defects in bundle-branch conduction.
- Untreated narrow-angle glaucoma.
- Acute alcohol, barbiturate and opiate intoxications.
- This tablet should not be given to patients who have received an MAO-inhibitor within two weeks.
- Not recommended for excitable or overactive patients since its activating effect may lead to exaggeration of these characteristics.
PrecautionsView
If previously the patient has been treated with tranquillizers with sedative effect these should be withdrawn gradually.
InteractionsView
This tablet may enhance the response to alcohol, barbiturates and other CNS depressants. Simultaneous administration of MAO-inhibitors may cause hypertensive crises. Neuroleptics and thymoleptics reduce the antihypertensive effect of guanethidine and similar acting compounds and thymoleptics enhance the effects of adrenaline and noradrenaline.
Pregnancy & lactationView
This tablet should preferably not be given during pregnancy and lactation.
Overdose effectsView
In cases of overdosage the symptoms of intoxications by melitracen, especially of anticholinergic nature, dominate. More rarely extrapyramidal symptoms due to flupentixol occur. Symptomatic and Supportive. Gastric lavage should be carried out as soon as possible and activated charcoal may be administered. Measures aimed at supporting the respiratory and cardiovascular systems should be instituted. Epinephrine (adrenaline) must not be used for such patients. Convulsions may be treated with diazepam and extrapyramidal symptoms with biperiden.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light. Keep out of reach of children.
Tensareal
Diazepam
Tensareal
Diazepam
Indications
Severe anxiety disorders
Indication detailsView
Diazepam is indicated for the short-term treatment of mild to moderate anxiety, excitation, agitation, fear, aggressiveness, etc. Anxiety reactions caused by stressed conditions, anxiety states with somatic expression, acute alcohol withdrawal, status epilepticus, premedication for surgical procedures, febrile convulsions, insomnia of hospitalized patients.
Therapeutic classView
Benzodiazepine sedatives, Centrally acting Skeletal Muscle Relaxants, Primary anti-epileptic drugs
PharmacologyView
Diazepam attaches to the specific site on the GABA receptor and potentiates the effect of GABA, which acts by opening chloride ion channels into cells.
Diazepam is absorbed rapidly and completely after oral administration. Peak Plasma concentration reaches within 15-90 minutes. Mean plasma half-life is 30 hours. Plasma protein binding is 98-99%. Diazepam is metabolized in the liver with only traces of the unchanged drug excreted in urine. A very small proportion of the metabolites is excreted through the bile into the intestine and eliminated with the feces. After rectal administration in suppository form diazepam is significantly absorbed and peak concentration reaches within 1.5-2 hours.
Diazepam is absorbed rapidly and completely after oral administration. Peak Plasma concentration reaches within 15-90 minutes. Mean plasma half-life is 30 hours. Plasma protein binding is 98-99%. Diazepam is metabolized in the liver with only traces of the unchanged drug excreted in urine. A very small proportion of the metabolites is excreted through the bile into the intestine and eliminated with the feces. After rectal administration in suppository form diazepam is significantly absorbed and peak concentration reaches within 1.5-2 hours.
DosageView
Oral:
- Anxiety: 2 mg thrice daily, increased if necessary to 15-30 mg daily in divided doses. Elderly (or debilitated), half of the adult dose.
- Insomnia associated with anxiety: 5-15 mg at bedtime.
- Night terrors and somnambulism in Child: 1-5 mg at bedtime.
- For severe acute anxiety, control of acute panic attacks, and acute alcohol withdrawal: 10 mg repeated if necessary after not less than 4 hours.
- Febrile convulsion in children: Slow IV in a dose of 250 mcg/kg.
- In case of children- A dose of 500 mcg/kg (maximum 10 mg), repeated if necessary.
Side effectsView
Diazepam is generally well tolerated. Higher doses may cause somnolence, dizziness, light headedness, confusion and ataxia.
ContraindicationsView
Diazepam is contraindicated in myasthenia gravis, pulmonary insufficiency, respiratory depression and hypersensitivity to bezodiazepine.
PrecautionsView
Prolonged use and abrupt withdrawal should be avoided. Diazepam should be used with caution in respiratory disease, muscle weakness, history of drug or alcohol abuse, in hepatic or renal impairment.
InteractionsView
Concomitant intake with alcohol is not recommended. Sedation may be increased due to concomitant use of neuroleptics (antipsychotics), hypnotics, sedative antihistamines and CNS depressants e.g., general anesthetics, narcotic analgesics or antidepressants. Diazepam clearance is increased by concomitant administration of phonobarbitone and is decreased by administration of cimetidine. Omeprazole and isoniazide inhibit diazepam metabolism.
Pregnancy & lactationView
Diazepam and its active metabolites cross the placental barrier and also pass into breast milk. So, it should be avoided if possible during pregnancy and lactation. US FDA pregnancy category D.
Overdose effectsView
Sedation, muscle weakness, profound sleep or paradoxical excitation. In more severe cases symptoms may include ataxia, hypotonia, hypotension, respiratory depression and rarely coma and death.
StorageView
Store in a cool (below 25˚C temperature) and dry place protected from light.
Tensfree
Bromazepam
Tensfree
Bromazepam
Indications
Panic attack
Indication detailsView
Bromazepam is indicated in-
- Emotional disturbances, i.e. acute tension and anxiety states. Difficulties in interpersonal contact. Agitation, insomnia, anxious and agitated depressive reactions.
- Functional disturbances in the cardiovascular and respiratory systems, i.e. pseudoangina pectoris, pericardial anxiety, tachycardia, emotiogenic hypertension, dyspnea and hyperventilation.
- Disturbances in the gastrointestinal tract, i.e. irritable bowel syndrome, epigastric pain, spasm, bloating diarrhea etc.
- Disturbances in the urinary tract, i.e. frequency, irritable bladder and dysmenorrhea.
- Psychosomatic disorder, i.e. psychogenic headache, asthma, gastric and duodenal ulcer.
- It is also indicated in emotional reactions to chronic organic disease.
Therapeutic classView
Benzodiazepine sedatives
PharmacologyView
Bromazepam is a powerful psychotropic agent. In lower dosage, it selectively reduces tension and anxiety. In higher dosage, it shows sedative and muscle-relaxant properties. Bromazepam binds to the GABA-A receptor producing a conformational change and potentiating its inhibitory effects. Other neurotransmitters are not influenced.
DosageView
Standard dosage: Average dosage for outpatient therapy is 1.5-3 mg up to three times daily. Treatment of outpatients should begin with low doses, gradually increasing to the optimum level.
In severe cases, especially in hospital: 6-12 mg 2 or 3 times daily. The overall treatment generally should not be more than 8-12 weeks. In certain cases extension beyond the maximum treatment period may be necessary; if so, it should be taken with re-evaluation of the patient's status with special expertise.
Elderly and debilitated patients: Elderly patients and those with impaired hepatic functions require lower doses.
Children: Bromazepam is usually not indicated in children, but if the physician feels bromazepam treatment is appropriate, then the dose should be adjusted to their low bodyweight (about 0.1-0.3 mg/kg bodyweight)
In severe cases, especially in hospital: 6-12 mg 2 or 3 times daily. The overall treatment generally should not be more than 8-12 weeks. In certain cases extension beyond the maximum treatment period may be necessary; if so, it should be taken with re-evaluation of the patient's status with special expertise.
Elderly and debilitated patients: Elderly patients and those with impaired hepatic functions require lower doses.
Children: Bromazepam is usually not indicated in children, but if the physician feels bromazepam treatment is appropriate, then the dose should be adjusted to their low bodyweight (about 0.1-0.3 mg/kg bodyweight)
AdministrationView
Bromazepam tablets are for oral administration
Side effectsView
Common side-effects include fatigue, drowsiness, muscle weakness, numbed muscle, reduced alertness, confusion, headache, ataxia etc. These phenomena occur predominantly at the start of therapy and usually disappear with prolonged administration. Anterograde amnesia may occur using therapeutic doses.
ContraindicationsView
Bromazepam is contraindicated in patients with known hypersensitivity to bromazepam, severe respiratory insufficiency, severe hepatic insufficiency or sleep apnea syndrome.
PrecautionsView
The use of benzodiazepines and benzodiazepine like agents may lead to the development of physical and psychological dependence upon these products. This dependence depends on the dose and duration of treatment; it is also greater in predisposed patients with a history of alcohol. Once physical dependence has developed, termination of the treatment will be accompanied by withdrawal symptoms. These may consist of headache, muscle pain, extreme anxiety, tension, confusion and irritability. Since the risk of withdrawal phenomena and rebound phenomena is greater after abrupt discontinuation of the treatment, it is recommended that the dosage be decreased gradually. Bromazepam is not recommended for the primary treatment of sleeplessness caused by psychotic illness. Caution should be exercised while driving cars or using machineries.
InteractionsView
If bromazepam is combined with other centrally active drugs, its sedative effects may be enhanced. These drugs are antidepressants, hypnotics, narcotics, antipsychotics, sedatives, antiepileptic drugs, sedative antihistamines and anesthetics. Co-administration of cimetidine may prolong the eliminiation half-life of bromazepam. Concomitant intake of bromazepam with alcohol should be avoided, because the sedative effect of bromazepam may be intensified by alcohol.
Pregnancy & lactationView
The safety of bromazepam during pregnancy has not been established. As bromazepam is excreted in breast milk, use should be avoided during lactation.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.
Tensicon
Flupentixol + Melitracen
Tensicon
Flupentixol + Melitracen
Indications
Psychosis
Indication detailsView
Flupentixol and Melitracen tablet is indicated in-
- Anxiety
- Depression
- Apathy
- Psychogenic depression.
- Depressive neurosses.
- Masked depression.
- Psychosomatic affections accompanied by anxiety and apathy.
- Menopausal depressions.
- Dysphoria and depression in alcoholics and drug addicts.
Therapeutic classView
Combined anxiolytics & anti-depressant drugs
PharmacologyView
This consists of two well known and well proven compounds: flupentixol-a neuroleptic with anxiolytic and antidepressant properties of its own when given in small doses, and melitracen-a bipolar thymoleptic with activating properties in low doses. In combination the compounds render a preparation with antidepressant, anxiolytic and activating properties. Maximal serum concentration is reached in about 4 hours after oral administration of flupentixol and in about 4 hours after oral administration of melitracen. The biological half-life of flupentixol is about 35 hours and that of melitracen is about 19 hours. The combination of flupentixol and melitracen does not seem to influence the pharmacokinetic properties of the individual compounds.
DosageView
Adults: Usually 2 tablets orally daily in the morning and noon. In severe cases, the morning dose may be increased to 2 tablets.
Elderly patients: 1 tablet in the morning.
Maintenance dose: Usually 1 tablet orally in the morning. In cases of insomnia or severe restlessness, additional treatment with a sedative in the acute phase is recommended.
Elderly patients: 1 tablet in the morning.
Maintenance dose: Usually 1 tablet orally in the morning. In cases of insomnia or severe restlessness, additional treatment with a sedative in the acute phase is recommended.
Side effectsView
In the recommended doses side effects are rare. These could be transient restlessness and insomnia.
ContraindicationsView
- The immediate recovery phase after myocardial infarction.
- Defects in bundle-branch conduction.
- Untreated narrow-angle glaucoma.
- Acute alcohol, barbiturate and opiate intoxications.
- This tablet should not be given to patients who have received an MAO-inhibitor within two weeks.
- Not recommended for excitable or overactive patients since its activating effect may lead to exaggeration of these characteristics.
PrecautionsView
If previously the patient has been treated with tranquillizers with sedative effect these should be withdrawn gradually.
InteractionsView
This tablet may enhance the response to alcohol, barbiturates and other CNS depressants. Simultaneous administration of MAO-inhibitors may cause hypertensive crises. Neuroleptics and thymoleptics reduce the antihypertensive effect of guanethidine and similar acting compounds and thymoleptics enhance the effects of adrenaline and noradrenaline.
Pregnancy & lactationView
This tablet should preferably not be given during pregnancy and lactation.
Overdose effectsView
In cases of overdosage the symptoms of intoxications by melitracen, especially of anticholinergic nature, dominate. More rarely extrapyramidal symptoms due to flupentixol occur. Symptomatic and Supportive. Gastric lavage should be carried out as soon as possible and activated charcoal may be administered. Measures aimed at supporting the respiratory and cardiovascular systems should be instituted. Epinephrine (adrenaline) must not be used for such patients. Convulsions may be treated with diazepam and extrapyramidal symptoms with biperiden.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light. Keep out of reach of children.
Tensnil
Clobazam
Tensnil
Clobazam
Indications
Tension
Indication detailsView
Acute and chronic anxiety states which may produce the following symptoms in particular: anxiety, tension, restlessness, excitement, irritability, sleep disturbances from emotional causes, psychovegetative and psychosomatic disorders (for example, in the cardiovascular or gastrointestinal area), and emotional instability.
In patients with depression or anxiety associated with depression, Clobazam must be used only in conjunction with adequate concomitant treatment. Use of benzodiazepines alone, can precipitate suicide in such patients. Before treatment of anxiety states associated with emotional instability, it must first be determined whether the patient suffers from a depressive disorder requiring adjunctive or different treatment.
In patients with schizophrenic or other psychotic illnesses, use of benzodiazepines is recommended only for adjunctive, i.e. not for primary treatment.
As adjunctive therapy in patients with epilepsy who are not adequately stabilized with their anticonvulsant monotherapy.
In patients with depression or anxiety associated with depression, Clobazam must be used only in conjunction with adequate concomitant treatment. Use of benzodiazepines alone, can precipitate suicide in such patients. Before treatment of anxiety states associated with emotional instability, it must first be determined whether the patient suffers from a depressive disorder requiring adjunctive or different treatment.
In patients with schizophrenic or other psychotic illnesses, use of benzodiazepines is recommended only for adjunctive, i.e. not for primary treatment.
As adjunctive therapy in patients with epilepsy who are not adequately stabilized with their anticonvulsant monotherapy.
Therapeutic classView
Benzodiazepine hypnotics
PharmacologyView
Clobazam binds at distinct binding sites associated with the chloride ionopore at the post-synaptic GABA receptor. These GABA receptors are in various locations in the CNS (limbic, reticular formation) and clobazam increases the duration of time for which the chloride ionopore is open. As a result, hyper polarization and stabilization of the membrane occur as the post-synaptic inhibitory effect of GABA is enhanced.
DosageView
General Dosage: Dosage and duration of treatment must be adjusted to the indication, the severity of the condition and the individual clinical response. Due regard must be paid to the possibility of interference with alertness and reaction time. The fundamental principle is to keep the dose as low as possible.
Elderly: Increased responsiveness and higher susceptibility to adverse effects may be present in elderly patients and require low initial doses and gradual dose increments under careful observation. A maintenance dose of 10 to 15 mg clobazam daily is frequently sufficient.
Children from 3 to 15 years of age: Increased responsiveness and higher susceptibility to adverse effects may be present in children and require low initial doses and gradual dose increments under careful observation. A daily dose of 5 to 10 mg clobazam is frequently sufficient. Benzodiazepines must not be given to children without careful assessment of the need for their use.
Secondary dosage adjustment: After the improvement of the symptoms, the dose may be reduced.
Timing of doses: If the dose is to be spread throughout the day, it is recommended that the larger portion be taken in the evening.
Duration of treatment: The duration of treatment must be as short as possible. The patient must be reassessed after a period not exceeding 4 weeks and regularly thereafter in order to evaluate the need for continued treatment, especially where the patient is free of symptoms. Generally, the overall duration of treatment (i.e. including tapering-of process) must not exceed 8 to 12 weeks. In certain cases, extension beyond the maximum treatment period may be necessary; treatment must not be extended without a re-evaluation of the patient's status using special expertise. It is strongly recommended that prolonged periods of uninterrupted treatment be avoided, since they may lead to dependence.
Discontinuation of treatment: It is strongly recommended that after prolonged treatment clobazam is not withdrawn suddenly but rather that the dose is reduced gradually under medical supervision; otherwise, withdrawal symptoms may occur.
Children from 3 to 15 years of age: It is recommended that normally treatment be started at 5 mg daily. A maintenance dose of 0.3 to 1.0 mg/kg body weight daily is usually sufficient. Higher susceptibility to adverse effects may be present in children and require gradual dose increments under careful observation; Benzodiazepines must not be given to children without careful assessment of the need for their use.
Elderly: Higher susceptibility to adverse effects may be present in elderly patients and require low initial doses and gradual dose increments under careful observation.
Timing of doses: If the dose is spread throughout the day, it is recommended that the larger portion be taken in the evening. Doses of up to 30 mg clobazam can also be administered as a single evening dose.
Duration of treatment: The patient must be re-assessed after a period not exceeding 4 weeks and regularly thereafter in order to evaluate the need for continued treatment.
Discontinuation of treatment: At the end of treatment- to include cases in which response to therapy has been poor- it is strongly recommended that clobazam is not withdrawn suddenly but rather that the dose is reduced gradually; otherwise an increased susceptibility to seizures as well as other withdrawal symptoms may occur.
Treatment of anxiety states-
Adults and adolescents over 15 years of age: The initial dose is usually 20 mg clobazam daily. If necessary, the daily dose may be increased. Generally, it is recommended that a total daily dose of 30 mg is not exceeded.Elderly: Increased responsiveness and higher susceptibility to adverse effects may be present in elderly patients and require low initial doses and gradual dose increments under careful observation. A maintenance dose of 10 to 15 mg clobazam daily is frequently sufficient.
Children from 3 to 15 years of age: Increased responsiveness and higher susceptibility to adverse effects may be present in children and require low initial doses and gradual dose increments under careful observation. A daily dose of 5 to 10 mg clobazam is frequently sufficient. Benzodiazepines must not be given to children without careful assessment of the need for their use.
Secondary dosage adjustment: After the improvement of the symptoms, the dose may be reduced.
Timing of doses: If the dose is to be spread throughout the day, it is recommended that the larger portion be taken in the evening.
Duration of treatment: The duration of treatment must be as short as possible. The patient must be reassessed after a period not exceeding 4 weeks and regularly thereafter in order to evaluate the need for continued treatment, especially where the patient is free of symptoms. Generally, the overall duration of treatment (i.e. including tapering-of process) must not exceed 8 to 12 weeks. In certain cases, extension beyond the maximum treatment period may be necessary; treatment must not be extended without a re-evaluation of the patient's status using special expertise. It is strongly recommended that prolonged periods of uninterrupted treatment be avoided, since they may lead to dependence.
Discontinuation of treatment: It is strongly recommended that after prolonged treatment clobazam is not withdrawn suddenly but rather that the dose is reduced gradually under medical supervision; otherwise, withdrawal symptoms may occur.
Treatment of epilepsy in combination with one or more other anticonvulsants-
Adults and adolescents over 15 years of age: It is recommended that administration be started at small doses (5 to 15 mg daily), if necessary, increasing the dose gradually to a maximum daily dose of about 80 mg.Children from 3 to 15 years of age: It is recommended that normally treatment be started at 5 mg daily. A maintenance dose of 0.3 to 1.0 mg/kg body weight daily is usually sufficient. Higher susceptibility to adverse effects may be present in children and require gradual dose increments under careful observation; Benzodiazepines must not be given to children without careful assessment of the need for their use.
Elderly: Higher susceptibility to adverse effects may be present in elderly patients and require low initial doses and gradual dose increments under careful observation.
Timing of doses: If the dose is spread throughout the day, it is recommended that the larger portion be taken in the evening. Doses of up to 30 mg clobazam can also be administered as a single evening dose.
Duration of treatment: The patient must be re-assessed after a period not exceeding 4 weeks and regularly thereafter in order to evaluate the need for continued treatment.
Discontinuation of treatment: At the end of treatment- to include cases in which response to therapy has been poor- it is strongly recommended that clobazam is not withdrawn suddenly but rather that the dose is reduced gradually; otherwise an increased susceptibility to seizures as well as other withdrawal symptoms may occur.
AdministrationView
The tablets can be administered whole, or crushed and mixed in applesauce. The 10 mg tablets can be divided into equal halves of 5 mg. Clobazam can be given with or without food.
Side effectsView
Metabolism and nutrition disorders: Common: decreased appetite
Psychiatric disorders: Common: irritability, aggression, restlessness, depression (pre-existing depression may be unmasked), drug tolerance (especially during prolonged use), agitation.
Nervous system disorders: Very common: somnolence, especially at the beginning of treatment and when higher doses are used; Common: sedation, dizziness, disturbance in attention, slow speech/dysarthria/ speech disorder (particularly with high doses or in long-term treatment, and are reversible), headache, tremor, ataxia.
Eye Disorders: Uncommon: diplopia (particularly with high doses or in long-term treatment and is reversible)
Respiratory, thoracic and mediastinal disorders: Not known: respiratory depression respiratory failure (particularly in patients with pre-existing compromised respiratory function e.g. in patients with bronchial asthma or brain damage)
Gastrointestinal disorders: Common: dry mouth, nausea, constipation
Skin and subcutaneous disorders: Uncommon: rash; Not known: photosensitivity reaction urticaria; Steven Johnson syndrome, toxic epidermal necrolysis (including some cases with fatal outcome);
Musculoskeleteal and connective tissue disorders: Not known: muscle spasms, muscle weakness
General disorders and administration site conditions: Very common: fatigue, especially at the beginning of treatment and when higher doses are used. Not known: slow response to stimuli, hypothermia
Investigations: Uncommon: weight increased (particularly with high doses or in long-term treatment).
Psychiatric disorders: Common: irritability, aggression, restlessness, depression (pre-existing depression may be unmasked), drug tolerance (especially during prolonged use), agitation.
Nervous system disorders: Very common: somnolence, especially at the beginning of treatment and when higher doses are used; Common: sedation, dizziness, disturbance in attention, slow speech/dysarthria/ speech disorder (particularly with high doses or in long-term treatment, and are reversible), headache, tremor, ataxia.
Eye Disorders: Uncommon: diplopia (particularly with high doses or in long-term treatment and is reversible)
Respiratory, thoracic and mediastinal disorders: Not known: respiratory depression respiratory failure (particularly in patients with pre-existing compromised respiratory function e.g. in patients with bronchial asthma or brain damage)
Gastrointestinal disorders: Common: dry mouth, nausea, constipation
Skin and subcutaneous disorders: Uncommon: rash; Not known: photosensitivity reaction urticaria; Steven Johnson syndrome, toxic epidermal necrolysis (including some cases with fatal outcome);
Musculoskeleteal and connective tissue disorders: Not known: muscle spasms, muscle weakness
General disorders and administration site conditions: Very common: fatigue, especially at the beginning of treatment and when higher doses are used. Not known: slow response to stimuli, hypothermia
Investigations: Uncommon: weight increased (particularly with high doses or in long-term treatment).
ContraindicationsView
Clobazam must not be used-
- In patients with hypersensitivity to clobazam or any of the excipients of Clobazam.
- In patients with myasthenia gravis (risk of aggravation of muscle weakness).
- In patients with severe respiratory insufciency (risk of deterioration).
- In patients with sleep apnoea syndrome (risk of deterioration).
- In patients with severe impairment of liver function (risk of precipitating encephalopathy).
- In breast-feeding women Benzodiazepines must not be given to children without careful assessment of the need for their use.
- Clobazam must not be used in children between the ages of 6 months and 3 years, other than in exceptional cases for anticonvulsant treatment where there is a compelling indication.
PrecautionsView
Serious Skin Reactions: Serious skin reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), have been reported with clobazam in both children and adults during the post-marketing experience. A majority of the reported cases involved the concomitant use of other drugs, including antiepileptic drugs that are associated with serious skin reactions. SJS/TEN could be associated with a fatal outcome. Patients should be closely monitored for signs or symptoms of SJS/TEN, especially during the first 8 weeks of treatment. Clobazam should be immediately discontinued when SJS/TEN is suspected. If signs or symptoms suggest SJS/TEN, use of this drug should not be resumed and alternative therapy should be considered.
Respiratory depression: Clobazam can cause respiratory depression, especially if administered in high doses. Therefore in patients with chronic or acute respiratory insufficiency, respiratory function must be monitored and a dose reduction may be necessary. Clobazam is contraindicated in patients with severe respiratory insufficiency.
Muscle weakness: Clobazam can cause muscle weakness. Clobazam is contraindicated in patients with myasthenia gravis.
Renal and hepatic impairment: In patients with impairment of renal or hepatic function, responsiveness to clobazam and susceptibility to adverse effects are increased, and a dose reduction may be necessary. In long-term treatment, renal and hepatic function must be checked regularly.
Elderly patients: In the elderly, due to the increased sensitivity to adverse reactions such as drowsiness, dizziness, muscle weakness, there is an increased risk of fall that may result in serious injury. A dose reduction is recommended.
Tolerance in epilepsy: In the treatment of epilepsy with benzodiazepines- including Clobazam, consideration must be given to the possibility of a decrease in anticonvulsant efficacy (development of tolerance) in the course of treatment.
CYP2C19 poor metabolizers: In patients who are CYP2C19 poor metabolizers, levels of the active metabolite N-desmethylclobazam are expected to be increased as compared to extensive metabolizers. Dosage adjustment of clobazam may be necessary (e.g. low starting dose with careful dose titration).
Suicidality: Several epidemiological studies show an increased incidence of suicide and suicide attempt in patients with or without depression, treated with other benzodiazepines and hypnotics. There are very limited data available for clobazam in these studies. Cases of suicidal behavior have been reported with clobazam in post-marketing surveillance. All of these cases had confounding factors.
Concomitant use of CYP2C19 inhibitors: The concomitant use of clobazam with CYP2C19 inhibitors, including cannabidiol containing medicinal products, dietary supplements and recreational products may result in increased exposure to N-desmethylclobazam (NCLB). Such increases might lead to increased adverse effects, such as somnolence and sedation. When used with medicinal products that are CYP2C19 inhibitors dosage adjustment of clobazam may be necessary. Dietary supplements and recreational products containing cannabidiol must not be taken in combination with clobazam as they contain unknown quantities of cannabidiol and are of variable quality
Respiratory depression: Clobazam can cause respiratory depression, especially if administered in high doses. Therefore in patients with chronic or acute respiratory insufficiency, respiratory function must be monitored and a dose reduction may be necessary. Clobazam is contraindicated in patients with severe respiratory insufficiency.
Muscle weakness: Clobazam can cause muscle weakness. Clobazam is contraindicated in patients with myasthenia gravis.
Renal and hepatic impairment: In patients with impairment of renal or hepatic function, responsiveness to clobazam and susceptibility to adverse effects are increased, and a dose reduction may be necessary. In long-term treatment, renal and hepatic function must be checked regularly.
Elderly patients: In the elderly, due to the increased sensitivity to adverse reactions such as drowsiness, dizziness, muscle weakness, there is an increased risk of fall that may result in serious injury. A dose reduction is recommended.
Tolerance in epilepsy: In the treatment of epilepsy with benzodiazepines- including Clobazam, consideration must be given to the possibility of a decrease in anticonvulsant efficacy (development of tolerance) in the course of treatment.
CYP2C19 poor metabolizers: In patients who are CYP2C19 poor metabolizers, levels of the active metabolite N-desmethylclobazam are expected to be increased as compared to extensive metabolizers. Dosage adjustment of clobazam may be necessary (e.g. low starting dose with careful dose titration).
Suicidality: Several epidemiological studies show an increased incidence of suicide and suicide attempt in patients with or without depression, treated with other benzodiazepines and hypnotics. There are very limited data available for clobazam in these studies. Cases of suicidal behavior have been reported with clobazam in post-marketing surveillance. All of these cases had confounding factors.
Concomitant use of CYP2C19 inhibitors: The concomitant use of clobazam with CYP2C19 inhibitors, including cannabidiol containing medicinal products, dietary supplements and recreational products may result in increased exposure to N-desmethylclobazam (NCLB). Such increases might lead to increased adverse effects, such as somnolence and sedation. When used with medicinal products that are CYP2C19 inhibitors dosage adjustment of clobazam may be necessary. Dietary supplements and recreational products containing cannabidiol must not be taken in combination with clobazam as they contain unknown quantities of cannabidiol and are of variable quality
InteractionsView
Alcohol: Concomitant consumption of alcohol can increase the bioavailability of clobazam by 50% and therefore lead to increased clobazam effects.
Central nervous system depressant drugs: Especially when clobazam is administered in higher doses, a mutually potentiating effect is to be expected if other central nervous system depressant drugs (such as antipsychotics, anxiolytics, certain antidepressant agents, anticonvulsant drugs, sedative antihistamines, anaesthetics, hypnotics or narcotic analgesics, or other sedatives) are taken at the same time. Special caution is also necessary when clobazam is administered in cases of intoxication with such substances or with lithium.
Opioids: The concomitant use of benzodiazepines, including clobazam, and opioids increases the risk of sedation, respiratory depression, coma, and death because of the additive CNS depressant effect. Limit dosage and duration of concomitant use of benzodiazepines and opioids.
Anticonvulsants: If clobazam is administered simultaneously with anticonvulsants in the treatment of epilepsy, the dosage must be adjusted under regular medical supervision (EEG monitoring), as there may be interactions with the patient's basic anticonvulsant medication. In patients receiving concomitant treatment with valproic acid, there may be a slight to moderate rise in plasma valproic acid concentration. Phenytoin plasma levels may rise if patients receive concomitant treatment with clobazam. Where possible, it is recommended that blood levels of concomitantly administered valproic acid or phenytoin be monitored. Carbamazepine and phenytoin may cause an increase in the metabolic conversion of clobazam to the active metabolite N-desmethyl clobazam. Stiripentol increases plasma levels of clobazam and its active metabolite N-desmethylclobazam, through inhibition of CYP3A and CYP2C19. Monitoring of blood levels is recommended, prior to initiation of stiripentol, and then once new steady-state concentration has been reached, i.e. after 2 weeks approximately.
Narcotic analgesics: If clobazam is used concomitantly with narcotic analgesics, possible euphoria may be enhanced; this may lead to increased psychological dependence.
Muscle relaxants: The effects of muscle relaxants and nitrous oxide may be enhanced.
CYP 2C19 inhibitors: Strong and moderate inhibitors of CYP2C19 may result in increased exposure to N-desmethylclobazam (N-CLB), the active metabolite of clobazam. Dosage adjustment of clobazam may be necessary when co-administered with strong CYP2C19 inhibitors (e.g., cannabidiol containing medicinal products, fuconazole, fuvoxamine, ticlopidine) or moderate CYP2C19 inhibitors (e.g. omeprazole).
CYP 2D6 substrates: Clobazam is a weak CYP2D6 inhibitor. Dose adjustment of drugs metabolized by CYP2D6 (e.g. dextromethorphan, pimozide, paroxetine, nebivolol) may be necessary.
Central nervous system depressant drugs: Especially when clobazam is administered in higher doses, a mutually potentiating effect is to be expected if other central nervous system depressant drugs (such as antipsychotics, anxiolytics, certain antidepressant agents, anticonvulsant drugs, sedative antihistamines, anaesthetics, hypnotics or narcotic analgesics, or other sedatives) are taken at the same time. Special caution is also necessary when clobazam is administered in cases of intoxication with such substances or with lithium.
Opioids: The concomitant use of benzodiazepines, including clobazam, and opioids increases the risk of sedation, respiratory depression, coma, and death because of the additive CNS depressant effect. Limit dosage and duration of concomitant use of benzodiazepines and opioids.
Anticonvulsants: If clobazam is administered simultaneously with anticonvulsants in the treatment of epilepsy, the dosage must be adjusted under regular medical supervision (EEG monitoring), as there may be interactions with the patient's basic anticonvulsant medication. In patients receiving concomitant treatment with valproic acid, there may be a slight to moderate rise in plasma valproic acid concentration. Phenytoin plasma levels may rise if patients receive concomitant treatment with clobazam. Where possible, it is recommended that blood levels of concomitantly administered valproic acid or phenytoin be monitored. Carbamazepine and phenytoin may cause an increase in the metabolic conversion of clobazam to the active metabolite N-desmethyl clobazam. Stiripentol increases plasma levels of clobazam and its active metabolite N-desmethylclobazam, through inhibition of CYP3A and CYP2C19. Monitoring of blood levels is recommended, prior to initiation of stiripentol, and then once new steady-state concentration has been reached, i.e. after 2 weeks approximately.
Narcotic analgesics: If clobazam is used concomitantly with narcotic analgesics, possible euphoria may be enhanced; this may lead to increased psychological dependence.
Muscle relaxants: The effects of muscle relaxants and nitrous oxide may be enhanced.
CYP 2C19 inhibitors: Strong and moderate inhibitors of CYP2C19 may result in increased exposure to N-desmethylclobazam (N-CLB), the active metabolite of clobazam. Dosage adjustment of clobazam may be necessary when co-administered with strong CYP2C19 inhibitors (e.g., cannabidiol containing medicinal products, fuconazole, fuvoxamine, ticlopidine) or moderate CYP2C19 inhibitors (e.g. omeprazole).
CYP 2D6 substrates: Clobazam is a weak CYP2D6 inhibitor. Dose adjustment of drugs metabolized by CYP2D6 (e.g. dextromethorphan, pimozide, paroxetine, nebivolol) may be necessary.
Pregnancy & lactationView
Pregnancy: Clobazam is not recommended during the first trimester of pregnancy and in women of childbearing potential not using contraception. Clobazam should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have demonstrated reproductive toxicity. Clobazam crosses the placenta. In the post-marketing safety database, limited data on exposed pregnancies are available with clobazam. A large amount of data collected from cohort studies has not demonstrated evidence of the occurrence of malformations following exposure to benzodiazepines during the first trimester of pregnancy. However, in certain epidemiological case-control studies, an increased incidence of cleft lip and palate was observed with benzodiazepines. Cases of reduced fetal movement and fetal heart rate variability have been described after administration of benzodiazepines during the second and/or third trimester of pregnancy. Administration of clobazam during the late phase of pregnancy or during childbirth can result in the occurrence of neonatal respiratory depression (including respiratory distress and apnea), which may be associated with other disorders such as sedation signs, hypothermia, hypotonia, and feeding difficulties (which may result in poor weight gain) in the newborn (signs and symptoms of the so-called "floppy infant syndrome"). Moreover, infants born to mothers who have taken benzodiazepines over longer periods during the later stages of pregnancy may have developed physical dependence and may be at risk of developing a withdrawal syndrome in the postnatal period. Appropriate monitoring of the newborn in the postnatal period is recommended. Women of childbearing potential should be informed of the risks and benefits of the use of Clobazam during pregnancy. If a woman plans a pregnancy or becomes pregnant, carefully evaluate the risks and benefits and whether treatment with Clobazam should be discontinued. If Clobazam treatment is to be continued, use Clobazam at the lowest effective dose.
Lactation: Clobazam must not be used in breastfeeding women, since clobazam passes into breast milk.
Lactation: Clobazam must not be used in breastfeeding women, since clobazam passes into breast milk.
StorageView
Do not use the medicine later than the date of expiry. Store below 30° and protect from light. Keep out of the reach of children.
Tenvira
Tenofovir Disoproxil Fumarate
Tenvira
Tenofovir Disoproxil Fumarate
Indications
HIV infection
Indication detailsView
This is indicated for the treatment of:
- Chronic hepatitis B virus infection in adults
- HIV infected adults in combination with other anti retroviral agents
Therapeutic classView
Drugs for HIV / Anti-retroviral drugs, Hepatic viral infections (Hepatitis B)
PharmacologyView
Tenofovir Disoproxil Fumarate, an acyclic nucleotide analogue of adenosine monophosphate, is a pro-drug of Tenofovir. It shows activity against hepatitis B virus polymerase and HIV reverse transcriptase after phosphorylation to the active diphosphate form. Tenofovir diphosphate inhibits viral polymerase (reverse transcriptase) by directly competing with the natural substrate deoxyribonucleotide and by causing DNA chain termination after its incorporation into viral DNA.
DosageView
The recommended dose of Tenofovir in chronic hepatitis B virus infection in adults 18 years of age and older with adequate renal function is 300 mg once daily with or without food.
Side effectsView
The most common side effects are nausea, vomiting, diarrhea and flatulence.
ContraindicationsView
Tenofovir is contraindicated in patients with known hypersensitivity to Tenofovir or any component of the product.
PrecautionsView
Co-administration with other drugs: Tenofovir should not be administered concurrently with Emtricitabine & Tenofovir combination or Adefovir Dipivoxil.
Lactic Acidosis & Severe Hepatomegaly with Steatosis: Though the risk of occurrence of lactic acidosis is low for Tenofovir, treatment should be suspended in any patient who develops lactic acidosis or hepatotoxicity.
Exacerbation of hepatitis after discontinuation of treatment: Discontinuation of Tenofovir
therapy may be associated with severe acute exacerbation of hepatitis.
Lactic Acidosis & Severe Hepatomegaly with Steatosis: Though the risk of occurrence of lactic acidosis is low for Tenofovir, treatment should be suspended in any patient who develops lactic acidosis or hepatotoxicity.
Exacerbation of hepatitis after discontinuation of treatment: Discontinuation of Tenofovir
therapy may be associated with severe acute exacerbation of hepatitis.
InteractionsView
Co-administration of Tenofovir with anti-retroviral, entecavir, lamivudine, methadone, oral contraceptives, ribavirin and tacrolimus did not result in significant drug interactions. The effects of co-administration of Tenofovir with other drugs that are renally eliminated or are known to affect renal function have not been evaluated.
Pregnancy & lactationView
Pregnancy: Pregnancy category B. It should be used during pregnancy only if clearly needed.
Lactation: It is not known whether it is excreted in human milk. Mothers should be instructed not to breast feed if they are taking Tenofovir.
Lactation: It is not known whether it is excreted in human milk. Mothers should be instructed not to breast feed if they are taking Tenofovir.
Pediatric usageView
Pediatric use: Safety and effectiveness of Tenofovir in pediatric patients below the age of 18 years have not been established.
Geriatrics use: Clinical studies of Tenofovir did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects. But care should be taken in dose selection, and it may be useful to monitor renal function.
Renal Impairment: Haemodialysis patients: 300 mg once every 7 days or after a cumulative total of 12 hr of dialysis.
Geriatrics use: Clinical studies of Tenofovir did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects. But care should be taken in dose selection, and it may be useful to monitor renal function.
Renal Impairment: Haemodialysis patients: 300 mg once every 7 days or after a cumulative total of 12 hr of dialysis.
- CrCl (10-29 mL/min): 300 mg 72-96 hrly.
- CrCl (30-49 mL/min): 300 mg 48 hrly.
Overdose effectsView
There is no experience of Tenofovir overdose reported in patients
StorageView
Store in a cool and dry place, protected from light and moisture. Keep the medicine out of the reach of children.
Teolex SR
Theophylline
Teolex SR
Theophylline
Indications
Status asthmaticus
Indication detailsView
Theophylline is indicated for the-
- Control of acute asthma.
- Management of chronic asthma (For both Symptomatic and prophylactic treatment).
- For controlling nocturnal asthma and early morning wheezing.
- Management of chronic obstructive lung disease (Chronic bronchitis and emphysema) and acute exacerbation of chronic obstructive lung disease.
- Control of apnea of pre-maturity.
Therapeutic classView
Bronchodilator, Theophylline & related drugs
PharmacologyView
Theophylline is a bronchodilator, structurally classified as a Methylxanthine. Theophylline has two distinct actions in the airways of patients with reversible obstruction; smooth muscle relaxation and suppression of the response of the airways to stimuli. Theophylline also increases the force of contraction of diaphragmatic muscles. The half-life of Theophylline is influenced by a number of known variables. In adult nonsmokers with uncomplicated asthma the half-life ranges from 3 to 9 hours
DosageView
The dose of theophylline must be individualized on the basis of peak serum theophylline concentration measurements in order to achieve a dose that will provide maximum potential benefit with minimal risk of adverse effects. Most of the sustained release preparations may be administered every 12 hours in adults while administration every 8 hours may be necessary in some children with markedly rapid hepatic
metabolism of theophylline. The recommended maintenance dose within accepted therapeutic range is as follows :
metabolism of theophylline. The recommended maintenance dose within accepted therapeutic range is as follows :
- 16 years or older: 10 mg/Kg/day (Do not exceed 900 mg/day)
- 12 years-15 years: 13 mg/Kg/day
- 9-11 years: 16 mg/Kg/day
- 1 year-8 years: 24-24 mg/Kg/day
- 6 months-1 year: 12-18 mg/Kg/day
- 1-6 months: 10 mg/Kg/day.
Side effectsView
Generally side effects are rare at normal dosage. It may include gastrointestinal discomfort, headache, nausea, insomnia and hypotension. CNS stimulation and diuresis may also occur, especially in children.
ContraindicationsView
Theophylline is contraindicated in patients with hypersensitivity to Theophylline or any other component of the product.
PrecautionsView
Careful consideration is needed for various interacting drugs and physiologic conditions that can alter Theophylline clearance. Dosage adjustment is required prior to initiation of Theophylline therapy, prior to increases in Theophylline dose, and during follow up. The dose of Theophylline selected for initiation of therapy should be low and, if tolerated, increased slowly over a period of time.
InteractionsView
Theophylline should not be used concurrently with other preparations containing xanthine derivatives. The clearance of theophylline is increased by barbiturates, carbamazepine, lithium, phenytoin, rifampicin and sulphinpyrazone and it may therefore be necessary to increase dosage. On the other hand, the clearance of the drug is reduced by allopurinol, cimetidine, ciprofloxacin, corticosteroids, erythromycin, frusemide, isoprenaline, oral contraceptive and thiabendazole and a reduced dosage may therefore be needed to avoid side effects. Theophylline can potentiate hypokalemia resulting from beta-2-agonist therapy, steroids, diuretics and hypoxia, so serum potassium levels should be monitored in such instances.
Pregnancy & lactationView
It is not known whether Theophylline can cause foetal harm when administered to pregnant woman. Xanthines should be given to a pregnant woman only if clearly needed. Theophylline is excreted into breast milk and may cause irritability or other signs of mild toxicity in nursing human infants. Serious adverse effects in the infant are unlikely unless the mother has toxic serum Theophylline concentrations.
Pediatric usageView
Pediatrics use: The clearance of Theophylline is very low in neonates. Careful attention to dosage selection and monitoring of serum Theophylline concentrations are required in pediatric patients.
StorageView
Keep all medicines out of reach of children. Store in a cool and dry place, protected from light.
Tepadina
Thiotepa
Tepadina
Thiotepa
Indications
Allogeneic or autologous haematopoietic progenitor cell transplantation (HPCT)
Indication detailsView
Thiotepa is indicated, in combination with other chemotherapy medicinal products:
- With or without total body irradiation (TBI), as conditioning treatment prior to allogeneic or autologous haematopoietic progenitor cell transplantation (HPCT) in haematological diseases in adult and paediatric patients;
- When high dose chemotherapy with HPCT support is appropriate for the treatment of solid tumours in adult and paediatric patients.
Therapeutic classView
Haematopoietic Agents
PharmacologyView
Thiotepa is a polyfunctional cytotoxic agent related chemically and pharmacologically to the nitrogen mustard. The radiomimetic action of thiotepa is believed to occur through the release of ethylene imine radicals that, as in the case of irradiation therapy, disrupt the bonds of DNA, e.g. by alkylation of guanine at the N-7, breaking the linkage between the purine base and the sugar and liberating alkylated guanine.
DosageView
Adults-
Autologous HPCT:
Autologous HPCT:
- Haematological diseases: The recommended dose in haematological diseases ranges from 125 mg/m2/day (3.38 mg/kg/day) to 300 mg/m2/day (8.10 mg/kg/day) as a single daily infusion, administered from2up to 4 consecutive days before autologous HPCT depending on the combination with other chemotherapeutic medicinal products, without exceeding the total maximum cumulative dose of 900 mg/m2(24.32 mg/kg), during the time of the entire conditioning treatment.
- Lymphoma: The recommended dose ranges from 125 mg/m2/day (3.38 mg/kg/day) to 300 mg/m2/day (8.10 mg/kg/day) as a single daily infusion, administered from2up to 4 consecutive days before autologous HPCT depending on the combination with other chemotherapeutic medicinal products, without exceeding the total maximum cumulative dose of 900 mg/m2(24.32 mg/kg), during the time of the entire conditioning treatment.
- Central nervous system lymphoma: The recommended dose is 185 mg/m2/day (5 mg/kg/day) as a single daily infusion, administered for 2 consecutive days before autologous HPCT, without exceeding the total maximum cumulative dose of 370 mg/m2(10 mg/kg), during the time of the entire conditioning treatment.
- Multiple myeloma: The recommended dose ranges from 150 mg/m2/day (4.05 mg/kg/day) to 250 mg/m2/day (6.76 mg/kg/day) as a single daily infusion, administered for 3 consecutive days before autologous HPCT depending on the combination with other chemotherapeutic medicinal products, without exceeding the total maximum cumulative dose of 750 mg/m2(20.27 mg/kg), during the time of the entire conditioning treatment.
- Breast cancer: The recommended dose ranges from 120 mg/m2/day (3.24 mg/kg/day) to 250 mg/m2/day (6.76 mg/kg/day) as a single daily infusion, administered from 3 up to 5 consecutive days before autologous HPCT depending on the combination with other chemotherapeutic medicinal products, without exceeding the total maximum cumulative dose of 800 mg/m2(21.62 mg/kg), during the time of the entire conditioning treatment.
- CNS tumours: The recommended dose ranges from 125 mg/m2/day (3.38 mg/kg/day) to 250 mg/m2/day (6.76 mg/kg/day) divided in one or two daily infusions, administered from 3 up to 4 consecutive days before autologous HPCT depending on the combination with other chemotherapeutic medicinal products, without exceeding the total maximum cumulative dose of 750 mg/m2(20.27 mg/kg), during the time of the entire conditioning treatment.
- Ovarian cancer: The recommended dose is 250 mg/m2/day (6.76 mg/kg/day) as a single daily infusion, administered in 2 consecutive days before autologous HPCT, without exceeding the total maximum cumulative dose of 500 mg/m2(13.51 mg/kg), during the time of the entire conditioning treatment.
- Germ cell tumours: The recommended dose ranges from 150 mg/m2/day (4.05 mg/kg/day) to 250 mg/m2/day (6.76 mg/kg/day) as a single daily infusion, administered for 3 consecutive days before autologous HPCT depending on the combination with other chemotherapeutic medicinal products, without exceeding the total maximum cumulative dose of 750 mg/m2(20.27 mg/kg), during the time of the entire conditioning treatment.
- Haematological diseases: The recommended dose in haematological diseases ranges from 185 mg/m2/day (5 mg/kg/day) to 481 mg/m2/day (13 mg/kg/day) divided in one or two daily infusions, administered from 1 up to 3 consecutive days before allogeneic HPCT depending on the combination with other chemotherapeutic medicinal products, without exceeding the total maximum cumulative dose of 555 mg/m2(15 mg/kg), during the time of the entire conditioning treatment.
- Lymphoma: The recommended dose in lymphoma is 370 mg/m2/day (10 mg/kg/day) divided in two daily infusions before allogeneic HPCT, without exceeding the total maximum cumulative dose of 370 mg/m2(10 mg/kg), during the time of the entire conditioning treatment.
- Multiple myeloma: The recommended dose is 185 mg/m2/day (5 mg/kg/day) as a single daily infusion before allogeneic HPCT, without exceeding the total maximum cumulative dose of 185 mg/m2(5 mg/kg), during the time of the entire conditioning treatment.
- Leukaemia: The recommended dose ranges from 185 mg/m2/day (5 mg/kg/day) to 481 mg/m2/day (13 mg/kg/day) divided in one or two daily infusions, administered from 1 up to 2 consecutive days before allogeneic HPCT depending on the combination with other chemotherapeutic medicinal products, without exceeding the total maximum cumulative dose of 555 mg/m2(15 mg/kg), during the time of the entire conditioning treatment.
- Thalassemia: The recommended dose is 370 mg/m2/day (10 mg/kg/day) divided in two daily infusions, administered before allogeneic HPCT, without exceeding the total maximum cumulative dose of 370 mg/m2(10 mg/kg), during the time of the entire conditioning treatment.
ContraindicationsView
Hypersensitivity to the active substance. Pregnancy and lactation. Concomitant use with yellow fever vaccine and with live virus and bacterial vaccines.
PrecautionsView
The consequence of treatment with thiotepa at the recommended dose and schedule is profound myelosuppression, occurring in all patients. Severe granulocytopenia, thrombocytopenia, anaemia or any combination thereof may develop. Frequent complete blood counts, including differential white blood cell counts, and platelet counts need to be performed during the treatment and until recovery is achieved. Platelet and red blood cell support, as well as the use of growth factors such as Granulocyte- colony stimulating factor (G-CSF), should be employed as medically indicated. Daily white blood cell counts and platelet counts are recommended during therapy with thiotepa and after transplant for at least 30 days.
InteractionsView
Live virus and bacterial vaccines must not be administered to a patient receiving an immunosuppressive chemotherapeutic agent and at least three months must elapse between discontinuation of therapy and vaccination.
Thiotepa appears to be metabolised via CYP2B6 and CYP3A4. Co-administration with inhibitors of CYP2B6 (for example clopidogrel and ticlopidine) or CYP3A4 (for example azole antifungals, macrolides like erythromycin, clarithromycin, telithromycin, and protease inhibitors) may increase the plasma concentrations of thiotepa and potentially decrease the concentrations of the active metabolite TEPA. Co-administration of inducers of cytochrome P450 (such as rifampicin, carbamazepine, phenobarbital) may increase the metabolism of thiotepa leading to increased plasma concentrations of the active metabolite. Therefore, during the concomitant use of thiotepa and these medicinal products, patients should be carefully monitored clinically.
Thiotepa is a weak inhibitor for CYP2B6, and may thereby potentially increase plasma concentrations of substances metabolised via CYP2B6, such as ifosfamide, tamoxifen, bupropion, efavirenz and cyclophosphamide. CYP2B6 catalyzes the metabolic conversion of cyclophosphamide to its active form 4-hydroxycyclophosphamide (4-OHCP) and co-administration of thiotepa may therefore lead to decreased concentrations of the active 4 OHCP. Therefore, a clinical monitoring should be exercised during the concomitant use of thiotepa and these medicinal products.
Thiotepa appears to be metabolised via CYP2B6 and CYP3A4. Co-administration with inhibitors of CYP2B6 (for example clopidogrel and ticlopidine) or CYP3A4 (for example azole antifungals, macrolides like erythromycin, clarithromycin, telithromycin, and protease inhibitors) may increase the plasma concentrations of thiotepa and potentially decrease the concentrations of the active metabolite TEPA. Co-administration of inducers of cytochrome P450 (such as rifampicin, carbamazepine, phenobarbital) may increase the metabolism of thiotepa leading to increased plasma concentrations of the active metabolite. Therefore, during the concomitant use of thiotepa and these medicinal products, patients should be carefully monitored clinically.
Thiotepa is a weak inhibitor for CYP2B6, and may thereby potentially increase plasma concentrations of substances metabolised via CYP2B6, such as ifosfamide, tamoxifen, bupropion, efavirenz and cyclophosphamide. CYP2B6 catalyzes the metabolic conversion of cyclophosphamide to its active form 4-hydroxycyclophosphamide (4-OHCP) and co-administration of thiotepa may therefore lead to decreased concentrations of the active 4 OHCP. Therefore, a clinical monitoring should be exercised during the concomitant use of thiotepa and these medicinal products.
Pregnancy & lactationView
There are no data on the use of thiotepa during pregnancy. In pre-clinical studies thiotepa, as most alkylating agents, has been shown to cause embryofoetal lethality and teratogenicity. Therefore, thiotepa is contraindicated during pregnancy. It is unknown whether thiotepa is excreted in human milk. Due to its pharmacological properties and its potential toxicity for breast-fed newborns/infants, breastfeeding is contraindicated during treatment with thiotepa.
Pediatric usageView
Renal impairment: Studies in renally impaired patients have not been conducted. As thiotepa and its metabolites are poorly excreted in the urine, dose modification is not recommended in patients with mild or moderate renal insufficiency. However, caution is recommended.
Hepatic impairment: Thiotepa has not been studied in patients with hepatic impairment. Since thiotepa is mainly metabolized through the liver, caution needs to be exercised when thiotepa is used in patients with pre-existing impairment of liver function, especially in those with severe hepatic impairment. Dose modification is not recommended for transient alterations of hepatic parameters.
Elderly: The administration of thiotepa has not been specifically investigated in elderly patients. However, in clinical studies, a proportion of patients over the age of 65 received the same cumulative dose as the other patients. No dose adjustment was deemed necessary.
Hepatic impairment: Thiotepa has not been studied in patients with hepatic impairment. Since thiotepa is mainly metabolized through the liver, caution needs to be exercised when thiotepa is used in patients with pre-existing impairment of liver function, especially in those with severe hepatic impairment. Dose modification is not recommended for transient alterations of hepatic parameters.
Elderly: The administration of thiotepa has not been specifically investigated in elderly patients. However, in clinical studies, a proportion of patients over the age of 65 received the same cumulative dose as the other patients. No dose adjustment was deemed necessary.
Overdose effectsView
There is no experience with overdoses of thiotepa. The most important adverse reactions expected in case of overdose is myeloablation and pancytopenia. There is no known antidote for thiotepa. The haematological status needs to be closely monitored and vigorous supportive measures instituted as medically indicated.
StorageView
Store and transport refrigerated (2°C-8°C). Do not freeze.
Teracin
Oxytetracycline
Teracin
Oxytetracycline
Indications
Uncomplicated gonorrhoea
Indication detailsView
Oxytetracycline is indicated in-
- Respiratory tract infections
- Mycoplasma pneumonia
- Urinary tract infections
- Sexually transmitted diseases: Infections due to Chlamydia trachomatis including uncom-plicated urethral, endocervical or rectal infections, non gonococcal urethritis, chancroid, granuloma inguinale, lymphogranuloma venereum, gonorrhoea, syphilis
- Skin infections: Acne and rosacea
- Ophthalmic infections: Trachoma
- Rickettsial infections
- Other infections: Psittacosis, brucellosis, cholera, acute
- intestinal amoebiasis etc.
Therapeutic classView
Eye Anti-Infectives & Antiseptics, Tetracycline group of drugs, Topical antibiotics for Acne
PharmacologyView
Oxytetracycline inhibits cell growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. The binding is reversible in nature. Oxytetracycline is lipophilic and can easily pass through the cell membrane or passively diffuses through porin channels in the bacterial membrane.
DosageView
Adults: 250-500 mg every 6 hours. Food, milk and some dairy products interfere with the absorption of Tetracyclines. So Tetracyclines should be given one hour before or two hours after meals.
Side effectsView
Side effects of Oxytetracycline, which have been reported in some patients, are anorexia, nausea, vomiting, diarrhoea, glossitis, skin rashes and urticaria.
ContraindicationsView
Oxytetracycline should not be used with patients who are hypersensitive to Tetracyclines. It should not be used in children under 12 years of age. It is contraindicated in pregnant women because of tooth staining in the fetus and possible growth retardation effects.
PrecautionsView
Oxytetracycline should be used with caution in renal impairment.
InteractionsView
Antacids containing Aluminium, Calcium, Magnesium, Zinc or Iron salts may impair the absorption of Oxytetracycline. In long term therapy, Tetracyclines depress plasma prothrombin activity and reduced doses of concomitant anticoagulants may be necessary. A few cases of pregnancy or breakthrough bleeding have been attributed to the concurrent use of Tetracyclines or Oxytetracyclines with oral contraceptives.
Pregnancy & lactationView
Results of animal studies indicate that tetracyclines cross the placenta, are found in fetal tissues and can have toxic effects on the developing fetus. Evidence of embryotoxicity has also been noted in animals treated early in pregnancy. Tetracyclines are present in the milk of lactating women who are taking a drug in this class.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Terazon
Terazosin Hydrochloride
Terazon
Terazosin Hydrochloride
Indications
Hypertension
Indication detailsView
Terazosin Hydrochloride is indicated in-
- Single therapy is used to relieve from signs and symptoms of benign prostatic hyperplasia (BPH).
- For the treatment of hypertension.
Therapeutic classView
Alpha adrenoceptor blocking drugs, BPH/ Urinary retention/ Urinary incontinence
PharmacologyView
Terazosin is selective for alpha-1-adrenoceptors but not their individual subtypes. Inhibition of these alpha-1-adrenoceptors results in relaxation of smooth muscle in blood vessels and the prostate, lowering blood pressure and improving urinary flow. Smooth muscle cells accounts for roughly 40% of the volume of the prostate and so their relaxation reduces pressure on the urethra.
It has also been shown that catecholamines induce factors responsible for mitogenesis and alpha-1-adrenergic receptor blockers inhibit this effect. A final long term mechanism of terazosin and other alpha-1-adrenergic receptor blockers is the induction of apoptosis of prostate cells. Treatment with terazosin enhances the expression of transforming growth factor beta-1 (TGF-beta1), which upregulates p27kip1, and the caspase cascade
It has also been shown that catecholamines induce factors responsible for mitogenesis and alpha-1-adrenergic receptor blockers inhibit this effect. A final long term mechanism of terazosin and other alpha-1-adrenergic receptor blockers is the induction of apoptosis of prostate cells. Treatment with terazosin enhances the expression of transforming growth factor beta-1 (TGF-beta1), which upregulates p27kip1, and the caspase cascade
DosageView
Benign Prostatic Hyperplasia-
- Initial dose: 1 mg at bedtime is starting dose of all patients and this dose should not be exceeded.
- Subsequent dose: The dose slowly increases to achieve the desired response. The usual recommended dose range is 5-10 mg administered once a day.
- Initial dose: 1 mg at bedtime is starting dose of all patients and this dose should not be exceeded.
- Subsequent dose: The dose slowly increases to achieve the desired response. The usual recommended dose range is 2-10 mg administered once a day.
Side effectsView
Postural hypotension is more commonly reported side effect. Dizziness, lack of energy, peripheral oedema; urinary frequency and priapism reported.
ContraindicationsView
Terazosin is contraindicated in patients known to be hypersensitive to Terazosin or its analogues.
PrecautionsView
- First dose may cause hypotension (within 30-90 minutes). Therefore should be taken on retiring to bed.
- Caution should be observed when Terazosin is administered with other antihypertensive agents, avoid the possibility of significant hypotension. When adding Terazosin to a diuretic or other antihypertensive agent, dosage reduction and retitration may be necessary.
- The patients should be cautioned to avoid situation such as driving and hazardous tasks where injury could result due to syncope after initiation of Terazosin therapy.
InteractionsView
- In patients receiving Terazosin plus ACE inhibitors or diuretics the proportion reporting dizziness or related side effects was greater than in the total population of Terazosin treated patients from clinical trials.
- Terazosin has been given without interaction with analgesics/anti-inflammatory, cardiac glycosides, hypoglycemic, antiarrhythmic, anxiolytics/sedatives, antibacterial, hormones/steroids and drugs used for gout.
Pregnancy & lactationView
The safety of Terazosin during pregnancy has not been established. So Terazosin is not recommended during pregnancy unless the potential benefit justifies the potential risk to mother and fetus. It is not known whether Terazosin is excreted in breast milk. As many drugs are excreted in breast milk, caution should be exercised when Terazosin is administered to a nursing mother.
Overdose effectsView
Acute overdose may lead to acute hypotension, cardiovascular support is of first importance. Restoration of blood pressure and normalization of heart rate may be accomplished by keeping the patient in a supine position. At the same time expansion of plasma volume and noradrenergic vasopressor may also be needed.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Terazon
Terazosin Hydrochloride
Terazon
Terazosin Hydrochloride
Indications
Hypertension
Indication detailsView
Terazosin Hydrochloride is indicated in-
- Single therapy is used to relieve from signs and symptoms of benign prostatic hyperplasia (BPH).
- For the treatment of hypertension.
Therapeutic classView
Alpha adrenoceptor blocking drugs, BPH/ Urinary retention/ Urinary incontinence
PharmacologyView
Terazosin is selective for alpha-1-adrenoceptors but not their individual subtypes. Inhibition of these alpha-1-adrenoceptors results in relaxation of smooth muscle in blood vessels and the prostate, lowering blood pressure and improving urinary flow. Smooth muscle cells accounts for roughly 40% of the volume of the prostate and so their relaxation reduces pressure on the urethra.
It has also been shown that catecholamines induce factors responsible for mitogenesis and alpha-1-adrenergic receptor blockers inhibit this effect. A final long term mechanism of terazosin and other alpha-1-adrenergic receptor blockers is the induction of apoptosis of prostate cells. Treatment with terazosin enhances the expression of transforming growth factor beta-1 (TGF-beta1), which upregulates p27kip1, and the caspase cascade
It has also been shown that catecholamines induce factors responsible for mitogenesis and alpha-1-adrenergic receptor blockers inhibit this effect. A final long term mechanism of terazosin and other alpha-1-adrenergic receptor blockers is the induction of apoptosis of prostate cells. Treatment with terazosin enhances the expression of transforming growth factor beta-1 (TGF-beta1), which upregulates p27kip1, and the caspase cascade
DosageView
Benign Prostatic Hyperplasia-
- Initial dose: 1 mg at bedtime is starting dose of all patients and this dose should not be exceeded.
- Subsequent dose: The dose slowly increases to achieve the desired response. The usual recommended dose range is 5-10 mg administered once a day.
- Initial dose: 1 mg at bedtime is starting dose of all patients and this dose should not be exceeded.
- Subsequent dose: The dose slowly increases to achieve the desired response. The usual recommended dose range is 2-10 mg administered once a day.
Side effectsView
Postural hypotension is more commonly reported side effect. Dizziness, lack of energy, peripheral oedema; urinary frequency and priapism reported.
ContraindicationsView
Terazosin is contraindicated in patients known to be hypersensitive to Terazosin or its analogues.
PrecautionsView
- First dose may cause hypotension (within 30-90 minutes). Therefore should be taken on retiring to bed.
- Caution should be observed when Terazosin is administered with other antihypertensive agents, avoid the possibility of significant hypotension. When adding Terazosin to a diuretic or other antihypertensive agent, dosage reduction and retitration may be necessary.
- The patients should be cautioned to avoid situation such as driving and hazardous tasks where injury could result due to syncope after initiation of Terazosin therapy.
InteractionsView
- In patients receiving Terazosin plus ACE inhibitors or diuretics the proportion reporting dizziness or related side effects was greater than in the total population of Terazosin treated patients from clinical trials.
- Terazosin has been given without interaction with analgesics/anti-inflammatory, cardiac glycosides, hypoglycemic, antiarrhythmic, anxiolytics/sedatives, antibacterial, hormones/steroids and drugs used for gout.
Pregnancy & lactationView
The safety of Terazosin during pregnancy has not been established. So Terazosin is not recommended during pregnancy unless the potential benefit justifies the potential risk to mother and fetus. It is not known whether Terazosin is excreted in breast milk. As many drugs are excreted in breast milk, caution should be exercised when Terazosin is administered to a nursing mother.
Overdose effectsView
Acute overdose may lead to acute hypotension, cardiovascular support is of first importance. Restoration of blood pressure and normalization of heart rate may be accomplished by keeping the patient in a supine position. At the same time expansion of plasma volume and noradrenergic vasopressor may also be needed.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Terbex
Terbinafine Hydrochloride
Terbex
Terbinafine Hydrochloride
Indication detailsView
Terbinafine tablet: This tablet is indicated for the treatment of onychomycosis of the toenail or fingernail due to dermatophytes (tinea unguium).
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Therapeutic classView
Other Antifungal preparations, Topical Antifungal preparations
PharmacologyView
Terbinafine, an Allylamine antifungal, inhibits biosynthesis of Ergosterol (an essential component of fungai cell membrane) via inhibition of Squalene Epoxidase enzyme. This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of Squalene but not due to Ergosterol deficiency. Depending on the concentration of the drug and the fungal species test in vitro, Terbinafine hydrochloride may be fungicidal. However, the clinical significance of in vitro data is unknown. Terbinafine has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections: Tricophyton Mentagrophyte, Trichophyton Rubrum.
DosageView
Terbinafine tablet:
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- For the treatment of fingernail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 6 weeks.
- For the treatment of toenail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 12 weeks.
- The optimal clinical effect is seen some months after mycological cure and cessation of treatment. This is related to the period required for the outgrowth of healthy nail.
- Body Weight: <25 kg: 125 mg/day up to 6 weeks
- Body Weight: 25-35 kg: 187.5 mg/day up to 6 weeks
- Body Weight: >35 kg: 250 mg/day up to 6 weeks
- Tinea corporis, cruris: 1 to 2 weeks
- Tinea pedis: 1 week
- Cutaneous candidiasis: 2 weeks
- Pityriasis versicolor: 2 weeks
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- Tinea pedis: once a day,1 week
- Tinea corporis/cruris: once a day,1 week
- Pityriasis versicolor: twice a day, 1 week
Side effectsView
The adverse events reported encompass gastrointestinal symptoms (including diarrhea, dyspepsia and abdominal pain), liver test abnormalities, rashes, urticaria, pruritus, and taste disturbances. In general, the adverse events were mild, transient, and did not lead to discontinuation. Adverse events, based on worldwide experience with terbinafine use, include: idiosyncratic and symptomatic hepatic injury and more rarely, cases of liver failure, some leading to death or liver transplant, serious skin reactions, severe neutropenia, thrombocytopenia, angioedema and allergic reactions (including anaphylaxis). Other adverse reactions that have been reported include malaise, fatigue, vomiting, arthralgia, myalgia, and hair loss.
ContraindicationsView
Terbinafine tablet and cream are contra-indicated in individuals with hypersensitive to terbinafine.
PrecautionsView
Warnings-
- Terbinafine tablets: Rare cases of liver failure, some leading to death or liver transplant, have occurred with the use of terbinafine tablets for the treatment of onychomycosis in individuals with and without preexisting liver disease. In the majority of liver cases reported in association with terbinafine use, the patients had serious underlying systemic conditions and an uncertain causal association with terbinafine. The severity of hepatic events and/or their outcome may be worse in patients with active or chronic liver disease. Treatment with terbinafine tablets should be discontinued if there is biochemical or clinical evidence of liver injury. There have been isolated reports of serious skin reaction (e.g., Stevens-Johnson Syndrome and toxic epidermal necrolysis). If progressive skin rash occurs, treatment with terbinafine should be discontinued.
- Terbinafine cream: Terbinafine cream is for external use only. Contact with the eyes should be avoided.
InteractionsView
In vivo studies have shown that terbinafine is an inhibitor of the CYP450 2D6 isozyme. Drugs predominantly metabolized by the CYP450 2D6 isozyme include the following drug classes: tricyclic antidepressants, selective serotonin reuptake inhibitors, beta-blockers, antiarrhythmics class 1C (e.g., flecainide and propafenone) and monoamine oxidase inhibitors Type B. Co-administration of terbinafine should be done with careful monitoring and may require a reduction in dose of the 2D6-metabolized drug.
Pregnancy & lactationView
Terbinafine tablet: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, and because treatment of onychomycosis can be postponed until after pregnancy is completed, it is recommended that terbinafine not be initiated during pregnancy. After oral administration, terbinafine is present in the breast milk of nursing mothers. Treatment with terbinafine is not recommended in nursing mothers.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Pediatric usageView
Pediatric use: The safety and efficacy of terbinafine have not been established in pediatric patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Overdose effectsView
Clinical experience regarding overdose with terbinafine tablets is limited. Doses up to 5 gm (20 times the therapeutic daily dose) have been taken without inducing serious adverse reactions. The symptoms of overdose included nausea, vomiting, abdominal pain, dizziness, rash, frequent urination, and headache.
StorageView
Store in a cool and dry place, below 30°C, protect from light.
Terbex
Terbinafine Hydrochloride
Terbex
Terbinafine Hydrochloride
Indication detailsView
Terbinafine tablet: This tablet is indicated for the treatment of onychomycosis of the toenail or fingernail due to dermatophytes (tinea unguium).
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Therapeutic classView
Other Antifungal preparations, Topical Antifungal preparations
PharmacologyView
Terbinafine, an Allylamine antifungal, inhibits biosynthesis of Ergosterol (an essential component of fungai cell membrane) via inhibition of Squalene Epoxidase enzyme. This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of Squalene but not due to Ergosterol deficiency. Depending on the concentration of the drug and the fungal species test in vitro, Terbinafine hydrochloride may be fungicidal. However, the clinical significance of in vitro data is unknown. Terbinafine has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections: Tricophyton Mentagrophyte, Trichophyton Rubrum.
DosageView
Terbinafine tablet:
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- For the treatment of fingernail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 6 weeks.
- For the treatment of toenail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 12 weeks.
- The optimal clinical effect is seen some months after mycological cure and cessation of treatment. This is related to the period required for the outgrowth of healthy nail.
- Body Weight: <25 kg: 125 mg/day up to 6 weeks
- Body Weight: 25-35 kg: 187.5 mg/day up to 6 weeks
- Body Weight: >35 kg: 250 mg/day up to 6 weeks
- Tinea corporis, cruris: 1 to 2 weeks
- Tinea pedis: 1 week
- Cutaneous candidiasis: 2 weeks
- Pityriasis versicolor: 2 weeks
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- Tinea pedis: once a day,1 week
- Tinea corporis/cruris: once a day,1 week
- Pityriasis versicolor: twice a day, 1 week
Side effectsView
The adverse events reported encompass gastrointestinal symptoms (including diarrhea, dyspepsia and abdominal pain), liver test abnormalities, rashes, urticaria, pruritus, and taste disturbances. In general, the adverse events were mild, transient, and did not lead to discontinuation. Adverse events, based on worldwide experience with terbinafine use, include: idiosyncratic and symptomatic hepatic injury and more rarely, cases of liver failure, some leading to death or liver transplant, serious skin reactions, severe neutropenia, thrombocytopenia, angioedema and allergic reactions (including anaphylaxis). Other adverse reactions that have been reported include malaise, fatigue, vomiting, arthralgia, myalgia, and hair loss.
ContraindicationsView
Terbinafine tablet and cream are contra-indicated in individuals with hypersensitive to terbinafine.
PrecautionsView
Warnings-
- Terbinafine tablets: Rare cases of liver failure, some leading to death or liver transplant, have occurred with the use of terbinafine tablets for the treatment of onychomycosis in individuals with and without preexisting liver disease. In the majority of liver cases reported in association with terbinafine use, the patients had serious underlying systemic conditions and an uncertain causal association with terbinafine. The severity of hepatic events and/or their outcome may be worse in patients with active or chronic liver disease. Treatment with terbinafine tablets should be discontinued if there is biochemical or clinical evidence of liver injury. There have been isolated reports of serious skin reaction (e.g., Stevens-Johnson Syndrome and toxic epidermal necrolysis). If progressive skin rash occurs, treatment with terbinafine should be discontinued.
- Terbinafine cream: Terbinafine cream is for external use only. Contact with the eyes should be avoided.
InteractionsView
In vivo studies have shown that terbinafine is an inhibitor of the CYP450 2D6 isozyme. Drugs predominantly metabolized by the CYP450 2D6 isozyme include the following drug classes: tricyclic antidepressants, selective serotonin reuptake inhibitors, beta-blockers, antiarrhythmics class 1C (e.g., flecainide and propafenone) and monoamine oxidase inhibitors Type B. Co-administration of terbinafine should be done with careful monitoring and may require a reduction in dose of the 2D6-metabolized drug.
Pregnancy & lactationView
Terbinafine tablet: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, and because treatment of onychomycosis can be postponed until after pregnancy is completed, it is recommended that terbinafine not be initiated during pregnancy. After oral administration, terbinafine is present in the breast milk of nursing mothers. Treatment with terbinafine is not recommended in nursing mothers.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Pediatric usageView
Pediatric use: The safety and efficacy of terbinafine have not been established in pediatric patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Overdose effectsView
Clinical experience regarding overdose with terbinafine tablets is limited. Doses up to 5 gm (20 times the therapeutic daily dose) have been taken without inducing serious adverse reactions. The symptoms of overdose included nausea, vomiting, abdominal pain, dizziness, rash, frequent urination, and headache.
StorageView
Store in a cool and dry place, below 30°C, protect from light.
Terbicon
Terbinafine Hydrochloride
Terbicon
Terbinafine Hydrochloride
Indication detailsView
Terbinafine tablet: This tablet is indicated for the treatment of onychomycosis of the toenail or fingernail due to dermatophytes (tinea unguium).
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Therapeutic classView
Other Antifungal preparations, Topical Antifungal preparations
PharmacologyView
Terbinafine, an Allylamine antifungal, inhibits biosynthesis of Ergosterol (an essential component of fungai cell membrane) via inhibition of Squalene Epoxidase enzyme. This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of Squalene but not due to Ergosterol deficiency. Depending on the concentration of the drug and the fungal species test in vitro, Terbinafine hydrochloride may be fungicidal. However, the clinical significance of in vitro data is unknown. Terbinafine has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections: Tricophyton Mentagrophyte, Trichophyton Rubrum.
DosageView
Terbinafine tablet:
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- For the treatment of fingernail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 6 weeks.
- For the treatment of toenail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 12 weeks.
- The optimal clinical effect is seen some months after mycological cure and cessation of treatment. This is related to the period required for the outgrowth of healthy nail.
- Body Weight: <25 kg: 125 mg/day up to 6 weeks
- Body Weight: 25-35 kg: 187.5 mg/day up to 6 weeks
- Body Weight: >35 kg: 250 mg/day up to 6 weeks
- Tinea corporis, cruris: 1 to 2 weeks
- Tinea pedis: 1 week
- Cutaneous candidiasis: 2 weeks
- Pityriasis versicolor: 2 weeks
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- Tinea pedis: once a day,1 week
- Tinea corporis/cruris: once a day,1 week
- Pityriasis versicolor: twice a day, 1 week
Side effectsView
The adverse events reported encompass gastrointestinal symptoms (including diarrhea, dyspepsia and abdominal pain), liver test abnormalities, rashes, urticaria, pruritus, and taste disturbances. In general, the adverse events were mild, transient, and did not lead to discontinuation. Adverse events, based on worldwide experience with terbinafine use, include: idiosyncratic and symptomatic hepatic injury and more rarely, cases of liver failure, some leading to death or liver transplant, serious skin reactions, severe neutropenia, thrombocytopenia, angioedema and allergic reactions (including anaphylaxis). Other adverse reactions that have been reported include malaise, fatigue, vomiting, arthralgia, myalgia, and hair loss.
ContraindicationsView
Terbinafine tablet and cream are contra-indicated in individuals with hypersensitive to terbinafine.
PrecautionsView
Warnings-
- Terbinafine tablets: Rare cases of liver failure, some leading to death or liver transplant, have occurred with the use of terbinafine tablets for the treatment of onychomycosis in individuals with and without preexisting liver disease. In the majority of liver cases reported in association with terbinafine use, the patients had serious underlying systemic conditions and an uncertain causal association with terbinafine. The severity of hepatic events and/or their outcome may be worse in patients with active or chronic liver disease. Treatment with terbinafine tablets should be discontinued if there is biochemical or clinical evidence of liver injury. There have been isolated reports of serious skin reaction (e.g., Stevens-Johnson Syndrome and toxic epidermal necrolysis). If progressive skin rash occurs, treatment with terbinafine should be discontinued.
- Terbinafine cream: Terbinafine cream is for external use only. Contact with the eyes should be avoided.
InteractionsView
In vivo studies have shown that terbinafine is an inhibitor of the CYP450 2D6 isozyme. Drugs predominantly metabolized by the CYP450 2D6 isozyme include the following drug classes: tricyclic antidepressants, selective serotonin reuptake inhibitors, beta-blockers, antiarrhythmics class 1C (e.g., flecainide and propafenone) and monoamine oxidase inhibitors Type B. Co-administration of terbinafine should be done with careful monitoring and may require a reduction in dose of the 2D6-metabolized drug.
Pregnancy & lactationView
Terbinafine tablet: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, and because treatment of onychomycosis can be postponed until after pregnancy is completed, it is recommended that terbinafine not be initiated during pregnancy. After oral administration, terbinafine is present in the breast milk of nursing mothers. Treatment with terbinafine is not recommended in nursing mothers.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Pediatric usageView
Pediatric use: The safety and efficacy of terbinafine have not been established in pediatric patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Overdose effectsView
Clinical experience regarding overdose with terbinafine tablets is limited. Doses up to 5 gm (20 times the therapeutic daily dose) have been taken without inducing serious adverse reactions. The symptoms of overdose included nausea, vomiting, abdominal pain, dizziness, rash, frequent urination, and headache.
StorageView
Store in a cool and dry place, below 30°C, protect from light.
Terbiderm
Terbinafine Hydrochloride
Terbiderm
Terbinafine Hydrochloride
Indication detailsView
Terbinafine tablet: This tablet is indicated for the treatment of onychomycosis of the toenail or fingernail due to dermatophytes (tinea unguium).
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Therapeutic classView
Other Antifungal preparations, Topical Antifungal preparations
PharmacologyView
Terbinafine, an Allylamine antifungal, inhibits biosynthesis of Ergosterol (an essential component of fungai cell membrane) via inhibition of Squalene Epoxidase enzyme. This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of Squalene but not due to Ergosterol deficiency. Depending on the concentration of the drug and the fungal species test in vitro, Terbinafine hydrochloride may be fungicidal. However, the clinical significance of in vitro data is unknown. Terbinafine has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections: Tricophyton Mentagrophyte, Trichophyton Rubrum.
DosageView
Terbinafine tablet:
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- For the treatment of fingernail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 6 weeks.
- For the treatment of toenail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 12 weeks.
- The optimal clinical effect is seen some months after mycological cure and cessation of treatment. This is related to the period required for the outgrowth of healthy nail.
- Body Weight: <25 kg: 125 mg/day up to 6 weeks
- Body Weight: 25-35 kg: 187.5 mg/day up to 6 weeks
- Body Weight: >35 kg: 250 mg/day up to 6 weeks
- Tinea corporis, cruris: 1 to 2 weeks
- Tinea pedis: 1 week
- Cutaneous candidiasis: 2 weeks
- Pityriasis versicolor: 2 weeks
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- Tinea pedis: once a day,1 week
- Tinea corporis/cruris: once a day,1 week
- Pityriasis versicolor: twice a day, 1 week
Side effectsView
The adverse events reported encompass gastrointestinal symptoms (including diarrhea, dyspepsia and abdominal pain), liver test abnormalities, rashes, urticaria, pruritus, and taste disturbances. In general, the adverse events were mild, transient, and did not lead to discontinuation. Adverse events, based on worldwide experience with terbinafine use, include: idiosyncratic and symptomatic hepatic injury and more rarely, cases of liver failure, some leading to death or liver transplant, serious skin reactions, severe neutropenia, thrombocytopenia, angioedema and allergic reactions (including anaphylaxis). Other adverse reactions that have been reported include malaise, fatigue, vomiting, arthralgia, myalgia, and hair loss.
ContraindicationsView
Terbinafine tablet and cream are contra-indicated in individuals with hypersensitive to terbinafine.
PrecautionsView
Warnings-
- Terbinafine tablets: Rare cases of liver failure, some leading to death or liver transplant, have occurred with the use of terbinafine tablets for the treatment of onychomycosis in individuals with and without preexisting liver disease. In the majority of liver cases reported in association with terbinafine use, the patients had serious underlying systemic conditions and an uncertain causal association with terbinafine. The severity of hepatic events and/or their outcome may be worse in patients with active or chronic liver disease. Treatment with terbinafine tablets should be discontinued if there is biochemical or clinical evidence of liver injury. There have been isolated reports of serious skin reaction (e.g., Stevens-Johnson Syndrome and toxic epidermal necrolysis). If progressive skin rash occurs, treatment with terbinafine should be discontinued.
- Terbinafine cream: Terbinafine cream is for external use only. Contact with the eyes should be avoided.
InteractionsView
In vivo studies have shown that terbinafine is an inhibitor of the CYP450 2D6 isozyme. Drugs predominantly metabolized by the CYP450 2D6 isozyme include the following drug classes: tricyclic antidepressants, selective serotonin reuptake inhibitors, beta-blockers, antiarrhythmics class 1C (e.g., flecainide and propafenone) and monoamine oxidase inhibitors Type B. Co-administration of terbinafine should be done with careful monitoring and may require a reduction in dose of the 2D6-metabolized drug.
Pregnancy & lactationView
Terbinafine tablet: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, and because treatment of onychomycosis can be postponed until after pregnancy is completed, it is recommended that terbinafine not be initiated during pregnancy. After oral administration, terbinafine is present in the breast milk of nursing mothers. Treatment with terbinafine is not recommended in nursing mothers.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Pediatric usageView
Pediatric use: The safety and efficacy of terbinafine have not been established in pediatric patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Overdose effectsView
Clinical experience regarding overdose with terbinafine tablets is limited. Doses up to 5 gm (20 times the therapeutic daily dose) have been taken without inducing serious adverse reactions. The symptoms of overdose included nausea, vomiting, abdominal pain, dizziness, rash, frequent urination, and headache.
StorageView
Store in a cool and dry place, below 30°C, protect from light.
Terbifin
Terbinafine Hydrochloride
Terbifin
Terbinafine Hydrochloride
Indication detailsView
Terbinafine tablet: This tablet is indicated for the treatment of onychomycosis of the toenail or fingernail due to dermatophytes (tinea unguium).
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Therapeutic classView
Other Antifungal preparations, Topical Antifungal preparations
PharmacologyView
Terbinafine, an Allylamine antifungal, inhibits biosynthesis of Ergosterol (an essential component of fungai cell membrane) via inhibition of Squalene Epoxidase enzyme. This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of Squalene but not due to Ergosterol deficiency. Depending on the concentration of the drug and the fungal species test in vitro, Terbinafine hydrochloride may be fungicidal. However, the clinical significance of in vitro data is unknown. Terbinafine has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections: Tricophyton Mentagrophyte, Trichophyton Rubrum.
DosageView
Terbinafine tablet:
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- For the treatment of fingernail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 6 weeks.
- For the treatment of toenail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 12 weeks.
- The optimal clinical effect is seen some months after mycological cure and cessation of treatment. This is related to the period required for the outgrowth of healthy nail.
- Body Weight: <25 kg: 125 mg/day up to 6 weeks
- Body Weight: 25-35 kg: 187.5 mg/day up to 6 weeks
- Body Weight: >35 kg: 250 mg/day up to 6 weeks
- Tinea corporis, cruris: 1 to 2 weeks
- Tinea pedis: 1 week
- Cutaneous candidiasis: 2 weeks
- Pityriasis versicolor: 2 weeks
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- Tinea pedis: once a day,1 week
- Tinea corporis/cruris: once a day,1 week
- Pityriasis versicolor: twice a day, 1 week
Side effectsView
The adverse events reported encompass gastrointestinal symptoms (including diarrhea, dyspepsia and abdominal pain), liver test abnormalities, rashes, urticaria, pruritus, and taste disturbances. In general, the adverse events were mild, transient, and did not lead to discontinuation. Adverse events, based on worldwide experience with terbinafine use, include: idiosyncratic and symptomatic hepatic injury and more rarely, cases of liver failure, some leading to death or liver transplant, serious skin reactions, severe neutropenia, thrombocytopenia, angioedema and allergic reactions (including anaphylaxis). Other adverse reactions that have been reported include malaise, fatigue, vomiting, arthralgia, myalgia, and hair loss.
ContraindicationsView
Terbinafine tablet and cream are contra-indicated in individuals with hypersensitive to terbinafine.
PrecautionsView
Warnings-
- Terbinafine tablets: Rare cases of liver failure, some leading to death or liver transplant, have occurred with the use of terbinafine tablets for the treatment of onychomycosis in individuals with and without preexisting liver disease. In the majority of liver cases reported in association with terbinafine use, the patients had serious underlying systemic conditions and an uncertain causal association with terbinafine. The severity of hepatic events and/or their outcome may be worse in patients with active or chronic liver disease. Treatment with terbinafine tablets should be discontinued if there is biochemical or clinical evidence of liver injury. There have been isolated reports of serious skin reaction (e.g., Stevens-Johnson Syndrome and toxic epidermal necrolysis). If progressive skin rash occurs, treatment with terbinafine should be discontinued.
- Terbinafine cream: Terbinafine cream is for external use only. Contact with the eyes should be avoided.
InteractionsView
In vivo studies have shown that terbinafine is an inhibitor of the CYP450 2D6 isozyme. Drugs predominantly metabolized by the CYP450 2D6 isozyme include the following drug classes: tricyclic antidepressants, selective serotonin reuptake inhibitors, beta-blockers, antiarrhythmics class 1C (e.g., flecainide and propafenone) and monoamine oxidase inhibitors Type B. Co-administration of terbinafine should be done with careful monitoring and may require a reduction in dose of the 2D6-metabolized drug.
Pregnancy & lactationView
Terbinafine tablet: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, and because treatment of onychomycosis can be postponed until after pregnancy is completed, it is recommended that terbinafine not be initiated during pregnancy. After oral administration, terbinafine is present in the breast milk of nursing mothers. Treatment with terbinafine is not recommended in nursing mothers.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Pediatric usageView
Pediatric use: The safety and efficacy of terbinafine have not been established in pediatric patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Overdose effectsView
Clinical experience regarding overdose with terbinafine tablets is limited. Doses up to 5 gm (20 times the therapeutic daily dose) have been taken without inducing serious adverse reactions. The symptoms of overdose included nausea, vomiting, abdominal pain, dizziness, rash, frequent urination, and headache.
StorageView
Store in a cool and dry place, below 30°C, protect from light.
Terbifin
Terbinafine Hydrochloride
Terbifin
Terbinafine Hydrochloride
Indication detailsView
Terbinafine tablet: This tablet is indicated for the treatment of onychomycosis of the toenail or fingernail due to dermatophytes (tinea unguium).
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Terbinafine granules: This is indicated in Tinea Capitis.
Terbinafine cream: Fungal infection of the skin caused by Trichophyton (e.g. T. rubrum, T. mentagrophytes, T. verrucosum, T. violaceum), Microsporum canis and Epidermophyton floccosum. Yeast infections of the skin, principally those caused by the genus Candida (e.g. C. albicans). Pityriasis (tinea) versicolor due to Pityrosporum orbicular (also known as Malassezia furfur).
Terbinafine 1% Spray: This spray is indicated in the treatment of tinea infections of the skin. This spray is also indicated in the treatment of pityriasis (tinea) versicolor due to Malassezia furfur.
Therapeutic classView
Other Antifungal preparations, Topical Antifungal preparations
PharmacologyView
Terbinafine, an Allylamine antifungal, inhibits biosynthesis of Ergosterol (an essential component of fungai cell membrane) via inhibition of Squalene Epoxidase enzyme. This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of Squalene but not due to Ergosterol deficiency. Depending on the concentration of the drug and the fungal species test in vitro, Terbinafine hydrochloride may be fungicidal. However, the clinical significance of in vitro data is unknown. Terbinafine has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections: Tricophyton Mentagrophyte, Trichophyton Rubrum.
DosageView
Terbinafine tablet:
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- For the treatment of fingernail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 6 weeks.
- For the treatment of toenail onychomycosis: Terbinafine 250 mg (one tablet), once daily for 12 weeks.
- The optimal clinical effect is seen some months after mycological cure and cessation of treatment. This is related to the period required for the outgrowth of healthy nail.
- Body Weight: <25 kg: 125 mg/day up to 6 weeks
- Body Weight: 25-35 kg: 187.5 mg/day up to 6 weeks
- Body Weight: >35 kg: 250 mg/day up to 6 weeks
- Tinea corporis, cruris: 1 to 2 weeks
- Tinea pedis: 1 week
- Cutaneous candidiasis: 2 weeks
- Pityriasis versicolor: 2 weeks
Terbinafine 1% Spray: This spray is applied once or twice daily, depending on the indication. The affected areas should be cleansed and dried thoroughly before application of this spray. A sufficient amount of solution should be applied to wet the treatment area(s) thoroughly.
- Tinea pedis: once a day,1 week
- Tinea corporis/cruris: once a day,1 week
- Pityriasis versicolor: twice a day, 1 week
Side effectsView
The adverse events reported encompass gastrointestinal symptoms (including diarrhea, dyspepsia and abdominal pain), liver test abnormalities, rashes, urticaria, pruritus, and taste disturbances. In general, the adverse events were mild, transient, and did not lead to discontinuation. Adverse events, based on worldwide experience with terbinafine use, include: idiosyncratic and symptomatic hepatic injury and more rarely, cases of liver failure, some leading to death or liver transplant, serious skin reactions, severe neutropenia, thrombocytopenia, angioedema and allergic reactions (including anaphylaxis). Other adverse reactions that have been reported include malaise, fatigue, vomiting, arthralgia, myalgia, and hair loss.
ContraindicationsView
Terbinafine tablet and cream are contra-indicated in individuals with hypersensitive to terbinafine.
PrecautionsView
Warnings-
- Terbinafine tablets: Rare cases of liver failure, some leading to death or liver transplant, have occurred with the use of terbinafine tablets for the treatment of onychomycosis in individuals with and without preexisting liver disease. In the majority of liver cases reported in association with terbinafine use, the patients had serious underlying systemic conditions and an uncertain causal association with terbinafine. The severity of hepatic events and/or their outcome may be worse in patients with active or chronic liver disease. Treatment with terbinafine tablets should be discontinued if there is biochemical or clinical evidence of liver injury. There have been isolated reports of serious skin reaction (e.g., Stevens-Johnson Syndrome and toxic epidermal necrolysis). If progressive skin rash occurs, treatment with terbinafine should be discontinued.
- Terbinafine cream: Terbinafine cream is for external use only. Contact with the eyes should be avoided.
InteractionsView
In vivo studies have shown that terbinafine is an inhibitor of the CYP450 2D6 isozyme. Drugs predominantly metabolized by the CYP450 2D6 isozyme include the following drug classes: tricyclic antidepressants, selective serotonin reuptake inhibitors, beta-blockers, antiarrhythmics class 1C (e.g., flecainide and propafenone) and monoamine oxidase inhibitors Type B. Co-administration of terbinafine should be done with careful monitoring and may require a reduction in dose of the 2D6-metabolized drug.
Pregnancy & lactationView
Terbinafine tablet: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, and because treatment of onychomycosis can be postponed until after pregnancy is completed, it is recommended that terbinafine not be initiated during pregnancy. After oral administration, terbinafine is present in the breast milk of nursing mothers. Treatment with terbinafine is not recommended in nursing mothers.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Terbinafine cream: Foetal toxicity and fertility studies in animals suggest no adverse effects. There is no clinical experience with terbinafine in pregnant women; therefore, unless the potential benefits outweigh any potential risk, terbinafine should not be administered. Terbinafine is excreted in breast milk and therefore mothers should not receive terbinafine treatment whilst breast-feeding.
Pediatric usageView
Pediatric use: The safety and efficacy of terbinafine have not been established in pediatric patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Use in the elderly: There is no evidence to suggest that elderly patients require different dosages or experience side-effects different to those of younger patients.
Overdose effectsView
Clinical experience regarding overdose with terbinafine tablets is limited. Doses up to 5 gm (20 times the therapeutic daily dose) have been taken without inducing serious adverse reactions. The symptoms of overdose included nausea, vomiting, abdominal pain, dizziness, rash, frequent urination, and headache.
StorageView
Store in a cool and dry place, below 30°C, protect from light.