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Iminod
Imiquimod
Iminod
Imiquimod
Indications
Basal cell carcinoma
Indication detailsView
Imiquimod cream is indicated for the topical treatment of-
- External genital and perianal warts in adults.
- Small superficial basal cell carcinomas in adults.
- Clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses on the face or scalp in immunocompetent adult patients when size or number of lesions limit the efficacy and/or acceptability of cryotherapy and other topical treatment options are contraindicated or less appropriate.
Therapeutic classView
Immunosuppressant, Miscellaneous topical agents
PharmacologyView
Imiquimod is a toll-like receptor-7 agonist enhancing both the innate and acquired immune response. It activates the production of numerous compounds, including IFN-α, IL-1, -6, -8, -10, -12, and TNF-α, stimulates natural killer cells and the proliferation of B-cells. It also activates Langerhans cells and promotes their migration to the regional lymph nodes. Imiquimod stimulates TH-1 cells to produce IFN-g, which in turn can activate cytotoxic T lymphocytes. These cells provide long-term immune memory, which can offer future protection against the previously encountered virus or tumor.
DosageView
External genital warts in adults: Imiquimod cream should be applied 3 times per week (example: Monday, Wednesday, and Friday; or Tuesday, Thursday, and Saturday) prior to normal sleeping hours, and should remain on the skin for 6 to 10 hours. Imiquimod cream treatment should continue until the clearance of visible genital or perianal warts or for a maximum of 16 weeks per episode of warts.
Imiquimod cream should be applied in a thin layer and rubbed on the clean wart area until the cream vanishes. Only apply to affected areas and avoid any application on internal surfaces. Imiquimod cream should be applied prior to normal sleeping hours. During the 6 to 10 hour treatment period, showering or bathing should be avoided. After this period it is essential that Imiquimod cream is removed with mild soap and water. Application of an excess of cream or prolonged contact with the skin may result in a severe application site reaction. A single use sachet is sufficient to cover a wart area of 20 cm2 (approx. 3 inches2). Sachets should not be re-used once opened. Hands should be washed carefully before and after application of cream. Uncircumcised males treating warts under the foreskin should retract the foreskin and wash the area daily.
Superficial basal cell carcinoma in adults: Apply Imiquimod cream for 6 weeks, 5 times per week (example: Monday to Friday) prior to normal sleeping hours, and leave on the skin for approximately 8 hours. Before applying Imiquimod cream, patients should wash the treatment area with mild soap and water and dry thoroughly. Sufficient cream should be applied to cover the treatment area, including one centimetre of skin surrounding the tumour. The cream should be rubbed into the treatment area until the cream vanishes. The cream should be applied prior to normal sleeping hours and remain on the skin for approximately 8 hours. During this period, showering and bathing should be avoided. After this period it is essential that Imiquimod cream is removed with mild soap and water. Sachets should not be re-used once opened. Hands should be washed carefully before and after application of cream. Response of the treated tumour to Imiquimod cream should be assessed 12 weeks after the end of treatment. If the treated tumour shows an incomplete response, a different therapy should be used. A rest period of several days may be taken if the local skin reaction to Imiquimod cream causes excessive discomfort to the patient, or if infection is observed at the treatment site. In this latter case, appropriate other measures should be taken.
Actinic keratosis in adults: Treatment should be initiated and monitored by a physician. Imiquimod cream should be applied 3 times per week (example: Monday, Wednesday and Friday) for four weeks prior to normal sleeping hours, and left on the skin for approximately 8 hours. Sufficient cream should be applied to cover the treatment area. After a 4-week treatment-free period, clearance of Actinic Keratosis should be assessed. If any lesions persist, treatment should be repeated for another four weeks. An interruption of dosing should be considered if intense local inflammatory reactions occur or if infection is observed at the treatment site. In this latter case, appropriate other measures should be taken. Each treatment period should not be extended beyond 4 weeks due to missed doses or rest periods. If the treated area does not show complete clearance at a follow-up examination about 8 weeks after the last 4-weeks course of treatment, an additional 4-weeks course of Imiquimod treatment may be considered. A different therapy is recommended if the treated lesion(s) shows insufficient response to Imiquimod. Actinic keratosis lesions that have cleared after one or two courses of treatment and subsequently recur can be re-treated with one or two further courses of Imiquimod cream following an at least 12 weeks treatment pause. Before applying Imiquimod cream, patients should wash the treatment area with mild soap and water and dry thoroughly. Sufficient cream should be applied to cover the treatment area, including one centimetre of skin surrounding the tumour. The cream should be rubbed into the treatment area until the cream vanishes. The cream should be applied prior to normal sleeping hours and remain on the skin for approximately 8 hours. During this period, showering and bathing should be avoided. After this period it is essential that Imiquimod cream is removed with mild soap and water. Sachets should not be re-used once opened. Hands should be washed carefully before and after application of cream.
Information applicable to all indications: If a dose is missed, the patient should apply the cream as soon as he/she remember and then he/she should continue with the regular schedule. However the cream should not be applied more than once a day.
Imiquimod cream should be applied in a thin layer and rubbed on the clean wart area until the cream vanishes. Only apply to affected areas and avoid any application on internal surfaces. Imiquimod cream should be applied prior to normal sleeping hours. During the 6 to 10 hour treatment period, showering or bathing should be avoided. After this period it is essential that Imiquimod cream is removed with mild soap and water. Application of an excess of cream or prolonged contact with the skin may result in a severe application site reaction. A single use sachet is sufficient to cover a wart area of 20 cm2 (approx. 3 inches2). Sachets should not be re-used once opened. Hands should be washed carefully before and after application of cream. Uncircumcised males treating warts under the foreskin should retract the foreskin and wash the area daily.
Superficial basal cell carcinoma in adults: Apply Imiquimod cream for 6 weeks, 5 times per week (example: Monday to Friday) prior to normal sleeping hours, and leave on the skin for approximately 8 hours. Before applying Imiquimod cream, patients should wash the treatment area with mild soap and water and dry thoroughly. Sufficient cream should be applied to cover the treatment area, including one centimetre of skin surrounding the tumour. The cream should be rubbed into the treatment area until the cream vanishes. The cream should be applied prior to normal sleeping hours and remain on the skin for approximately 8 hours. During this period, showering and bathing should be avoided. After this period it is essential that Imiquimod cream is removed with mild soap and water. Sachets should not be re-used once opened. Hands should be washed carefully before and after application of cream. Response of the treated tumour to Imiquimod cream should be assessed 12 weeks after the end of treatment. If the treated tumour shows an incomplete response, a different therapy should be used. A rest period of several days may be taken if the local skin reaction to Imiquimod cream causes excessive discomfort to the patient, or if infection is observed at the treatment site. In this latter case, appropriate other measures should be taken.
Actinic keratosis in adults: Treatment should be initiated and monitored by a physician. Imiquimod cream should be applied 3 times per week (example: Monday, Wednesday and Friday) for four weeks prior to normal sleeping hours, and left on the skin for approximately 8 hours. Sufficient cream should be applied to cover the treatment area. After a 4-week treatment-free period, clearance of Actinic Keratosis should be assessed. If any lesions persist, treatment should be repeated for another four weeks. An interruption of dosing should be considered if intense local inflammatory reactions occur or if infection is observed at the treatment site. In this latter case, appropriate other measures should be taken. Each treatment period should not be extended beyond 4 weeks due to missed doses or rest periods. If the treated area does not show complete clearance at a follow-up examination about 8 weeks after the last 4-weeks course of treatment, an additional 4-weeks course of Imiquimod treatment may be considered. A different therapy is recommended if the treated lesion(s) shows insufficient response to Imiquimod. Actinic keratosis lesions that have cleared after one or two courses of treatment and subsequently recur can be re-treated with one or two further courses of Imiquimod cream following an at least 12 weeks treatment pause. Before applying Imiquimod cream, patients should wash the treatment area with mild soap and water and dry thoroughly. Sufficient cream should be applied to cover the treatment area, including one centimetre of skin surrounding the tumour. The cream should be rubbed into the treatment area until the cream vanishes. The cream should be applied prior to normal sleeping hours and remain on the skin for approximately 8 hours. During this period, showering and bathing should be avoided. After this period it is essential that Imiquimod cream is removed with mild soap and water. Sachets should not be re-used once opened. Hands should be washed carefully before and after application of cream.
Information applicable to all indications: If a dose is missed, the patient should apply the cream as soon as he/she remember and then he/she should continue with the regular schedule. However the cream should not be applied more than once a day.
Side effectsView
Reported side effects are pustules, genital candidiasis, vaginitis, bacterial infection, fungal infection, upper respiratory tract infection, vulvitis, rhinitis, influenza, lymphadenopathy, anorexia, insomnia, depression, irritability, headache, paraesthesia, dizziness, migraine, somnolence, conjunctival irritation, eyelid oedema, tinnitus, flushing, pharyngitis, nasal congestion, pharyngo laryngeal pain, nausea, abdominal pain, diarrhoea, vomitting, rectal disorder, rectal tenesmus, dry mouth, pruritus, folliculitis, rash erythematous, eczema, rash, increased sweating, urticaria, erythema, face oedema, skin ulcer, myalgia, arthralgia, back pain, pain in extremity, dysuria, genital pain in male, penile disorder, dyspareunia, erectile dysfunction, uterovaginal prolapse, vaginal pain, vaginitis atrophic, vulval disorder, and general disorders and administration site disorders such as pruritus, pain, burning, irritation, erythema, reaction, bleeding, papules, rash, inflammation asthenia, malaise, rigors, lethargy, discomfort, fatigue, discharge, oedema, scar, ulcer, vesicle, warmth, pyrexia etc. Reports have been received of localised hypopigmentation and hyperpigmentation following Imiquimod cream use. Clinical studies investigating the use of Imiquimod for the treatment of actinic keratosis have detected a 0.4% frequency of alopecia at the treatment site or surrounding area. Reductions in haemoglobin, white blood cell count, absolute neutrophils and platelets have been observed in clinical trials.
ContraindicationsView
Imiquimod cream is contraindicated in patients with hypersensitivity to imiquimod or cream excipients.
PrecautionsView
Hypersensitivity to the active substance or to any of the excipients.
InteractionsView
No interaction studies have been performed. This includes studies with immunosuppressive drugs. Interactions with systemic drugs would be limited by the minimal percutaneous absorption of Imiquimod cream. Due to its immunostimulating properties, Imiquimod cream should be used with caution in patients who are receiving immunosuppressive medication.
Pregnancy & lactationView
Use in Pregnancy B1. No human study is available. Imiquimod cream should only be used during pregnancy, if the potential benefit justifies the potential risk of fetus. No human study is available. Imiquimod cream should only be used during lactation if the potential benefit justifies the potential risk to the new-born baby.
Pediatric usageView
Use in Children: Imiquimod cream is not recommended below the age of 12 years.
Use in Elderly: Imiquimod cream is recommended in elderly patient.
Effect on ability to drive and use machineries: Imiquimod cream is unlikely to produce any effect.
Use in Elderly: Imiquimod cream is recommended in elderly patient.
Effect on ability to drive and use machineries: Imiquimod cream is unlikely to produce any effect.
Overdose effectsView
When applied topically, systemic overdosage with Imiquimod cream is unlikely due to minimal percutaneous absorption. Persistent dermal overdosing of Imiquimod cream could result in severe local skin reactions. Following accidental ingestion, nausea, emesis, headache, myalgia and fever could occur after a single dose of 200 mg Imiquimod which corresponds to the content of approximately 16 sachets. The most clinically serious adverse event reported following multiple oral doses of ≥ 200 mg was hypotension which resolved following oral or intravenous fluid administration.
StorageView
Store in a cool & dry place, protected from light. Store at 4°-25°C.
Imipen
Imipenem + Cilastatin
Imipen
Imipenem + Cilastatin
Indications
Urinary tract infection
Indication detailsView
The activity of Cilastatin & Imipenem against an unusually broad spectrum of pathogens makes it particularly useful in the treatment of polymicrobic mixed aerobic/anaerobic infections as well as initial therapy prior to the identification of the causative organisms. Cilastatin & Imipenem is indicated for the treatment of the following infections due to susceptible organisms:
- Intra-abdominal infections
- Lower respiratory tract infections
- Gynaecological infections
- Septicaemia
- Genitourinary tract infections
- Bone and joint infections
- Skin and soft tissue infections
- Endocarditis
Therapeutic classView
Other beta-lactam Antibiotics
PharmacologyView
Imipenem acts as an antimicrobial through the inhibition of cell wall synthesis of various gram-positive and gram-negative bacteria. This inhibition of cell wall synthesis in gram-negative bateria is attained by binding to pencillin binding proteins (PBPs). In E. coli and selected strains of P. aeruginosa, imipenem has shown to have the highest affinity to PBP-2, PBP-1a, and PBP-1b. This preferential binding to PBP-2 and PBP-1b results in the direct conversion of the individual cell to a spheroblast, which leads to rapid cell lysis and death without filament formation.
Cilastatin is a specific and reversible renal dehydropeptidase-I inhibitor. Since the antibiotic, imipenem, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to block the metabolism and thus the inactivation of imipenem so that antibacterial levels of imipenem can be attained in the urine. The drug also prevents the metabolism of leukotriene D4 to leukotriene E4 through the inhibition of leukotriene D4 dipeptidase.
Cilastatin is a specific and reversible renal dehydropeptidase-I inhibitor. Since the antibiotic, imipenem, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to block the metabolism and thus the inactivation of imipenem so that antibacterial levels of imipenem can be attained in the urine. The drug also prevents the metabolism of leukotriene D4 to leukotriene E4 through the inhibition of leukotriene D4 dipeptidase.
DosageView
The total daily dosage of Imipenem should be based on the type or severity of infection and given in equally divided doses based on consideration of degree of susceptibility of the pathogens, renal function and body-weight.
Imipenem & Cilastatin IV: Up to 500 mg dose should be given over 20 to 30 minutes; > 500 mg dose should be infused over 40 to 60 minutes. In patients who develop nausea during the infusion, the rate of infusion may be slowed.
Adult: Normal daily dose is 1-2 g administered in 3-4 divided doses. For the treatment of moderate infection, a 1 g b.i.d. dosage regimen may also be used. In infections due to less susceptible organisms, the daily dosage may be increased to a maximum of 4 g/day or 50 mg/kg/day, whichever is lower.
Imipenem & Cilastatin IV: Up to 500 mg dose should be given over 20 to 30 minutes; > 500 mg dose should be infused over 40 to 60 minutes. In patients who develop nausea during the infusion, the rate of infusion may be slowed.
Adult: Normal daily dose is 1-2 g administered in 3-4 divided doses. For the treatment of moderate infection, a 1 g b.i.d. dosage regimen may also be used. In infections due to less susceptible organisms, the daily dosage may be increased to a maximum of 4 g/day or 50 mg/kg/day, whichever is lower.
- Mild infection: 250 mg 6 hourly (1 gm/day)
- Moderate infection: 500 mg 8 hourly or 1 gm 12 hourly (1.5-2 gm/day)
- Severe infection with fully susceptible microorganism: 500 mg 6 hourly (2gm/day)
- Severe infection with less susceptible organisms (primarily some strains of P. aeruginosa): 1 gm 3-4 times daily (3-4 gm/day)
- ≥ 3 months of age: the recommended dose for non-CNS infections is 15-25 mg/kg/dose administered every six hours. The maximum daily dose for treatment of infections with fully susceptible organisms is 2.0 g per day, and of infections with moderately susceptible organisms is 4.0 g/day. Higher doses (up to 90 mg/kg/day in older children) have been used in patients with cystic fibrosis.
- ≤3 months of age: Following dosage schedule is recommended for non-CNS infections:
- <1 week of age: 25 mg/kg every 12 hrs
- 1-4 weeks of age: 25 mg/kg every 8 hrs
- 4 weeks-3 months of age: 25 mg/kg every 6 hrs.
Side effectsView
Most common side effects with imipenem are nausea and vomiting. Other side effects reported with this drug are diarrhea, rash, thrombophlebitis, thrombocytosis, neutro-penia, eosinophilia and derangements of liver and renal functions. Use of imipenem is not recommended for patient with history of anaphylactic reaction with penicillin.
ContraindicationsView
Contraindicated in patients who have demonstrated hypersensitivity to this product.
PrecautionsView
Caution when used in patients with known hypersensitivity to other β-lactams due to possibility of cross-sensitivity. CNS disorders such as epilepsy; renal, hepatic impairment; pregnancy, lactation.
InteractionsView
Concurrent admin with probenecid may increase the half-life of cilastatin. Increased risk of generalised seizures when used concurrently with ganciclovir.
Pregnancy & lactationView
Pregnancy: Category C. There are no adequate and well controlled studies in pregnant women. Cispenam should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation: Imipenem has been detected in human milk. If the use of Cispenam is deemed essential, the patient should stop nursing.
Lactation: Imipenem has been detected in human milk. If the use of Cispenam is deemed essential, the patient should stop nursing.
Pediatric usageView
Dosage adjustment in renal impairment:
- CrCl >71: No changes.
- CrCl 41-70: Max 37.5 mg/kg/day or 3 g/day. (Range: 9.4 - 37.5 mg/kg/day) divided q6-8h.
- CrCl 21-40: Max 25 mg/kg/day or 2 g/day. (Range: 6.25 - 25 mg/kg/day) divided q6-12h.
- CrCl 6-20: Max 12.5 mg/kg/day (max dose 1 g/day). Range: 6.25 - 12.5 mg/kg/day) divided q12h. (Usual: 250mg q12h)
- Dialysis Hemodialysis: 125 - 500 mg q12h. (Max 12.5 mg/kg/day). Give dose after dialysis.
- Peritonial Dialysis: 125 - 250 mg q12h
Overdose effectsView
In the case of overdosage, discontinue Imipenem/Cilastatin, treat symptomatically, and institute supportive measures as required. Imipenem/Cilastatin Sodium is hemodialyzable.
Imiro
Iohexol
Imiro
Iohexol
Indications
Radiographic contrast medium for diagnostic procedures
Indication detailsView
Iohexol is an X-ray contrast medium for use in adults and children for cardioangiography, arteriography, urography, phlebography and CT-enhancement. Lumbar, thoracic, cervical myelography and computed tomography of the basal cisterns, following subarachnoid injection. It is also indicated for arthrography, endoscopic retrograde pancreatography (ERP), endoscopic retrograde cholangiopancreatography (ERCP), herniography, hysterosalpingography, sialography and studies of the gastrointestinal tract when the use of barium sulphate is unsatisfactory, undesirable or contraindicated.
The dosage varies depending on the type of examination, age, weight, cardiac output and general condition of the patient and the technique used. Usually the same iodine concentration and volume is used as with other iodinated X-ray contrast media in current use. Adequate hydration should be assured before and after administration as for other contrast media.
The dosage varies depending on the type of examination, age, weight, cardiac output and general condition of the patient and the technique used. Usually the same iodine concentration and volume is used as with other iodinated X-ray contrast media in current use. Adequate hydration should be assured before and after administration as for other contrast media.
Therapeutic classView
Contrast medium for diagnostic procedures
PharmacologyView
Iohexol provides opacification of blood vessels and permits radiographic visualisation until sufficient haemodilution occurs or sufficient contrast medium has left the site of injection. Being a non-ionic compound, Iohexol yields solutions of lower osmolality than the conventional ionic contrast media. Intravenous or intra-arterial injection of Iohexol causes less pain and sensation of heat than conventional ionic media with similar iodine content. Iohexol solutions cause less cardiac and vascular disturbances on intravascular injection. The transit time of Iohexol through the coronary vascular system is slightly increased compared with conventional ionic contrast media, probably due to the increased viscosity of Iohexol at comparable iodine concentrations. The period of maximal opacification of the renal vessels may begin as early as 30 seconds after IV injection. Urograms become apparent in about 1 to 3 minutes with optimal contrast occurring between 5 to 15 minutes. In nephropathic conditions, particularly when excretory capacity has been altered, the rate of excretion may vary unpredictably, and opacification may be delayed after injection. Severe renal impairment may result in a lack of diagnostic opacification of the collecting system. The initial concentration and volume of the medium, in conjunction with appropriate patient manipulation and the volume of CSF into which the medium is placed, will determine the extent of diagnostic contrast that can be achieved. Following subarachnoid injection, Iohexol will continue to provide good diagnostic contrast by conventional radiography for at least 30 minutes. Slow diffusion of Iohexol takes place throughout the CSF as well as transfer into the circulation. At approximately 1 hour, contrast of diagnostic quality will not usually be available for conventional myelography. However, sufficient contrast for CT myelography will be available for several hours. If CT myelography is to follow, it should be deferred for several hours to allow the degree of contrast to decrease. Following lumbar subarachnoid placement, irrespective of the position in which the patient is later maintained, slow upward diffusion of Iohexol takes place throughout the CSF. CSF contrast enhancement for CT scanning may be expected in the thoracic region in about 1 hour, in the cervical region in about 2 hours and in the basal cisterns in 3 to 4 hours after administration into the lumbar subarachnoid space.
DosageView
Injection As iohexol soln containing 6-350 mg iodine/mL: Dose and strength used depends on the procedure and route of administration.
Peripheral arteriography:
Contrast-enhanced computerized tomography:
Contrast-enhanced computerized tomography of the abdomen:
Injection-
Angiocardiography:- Adult: Ventriculography: 350 mg iodine/ml: 30-60 ml, usual: 40 ml, may be repeated as necessary. If with selective coronary arteriography: max 250 ml. Selective coronary arteriography: 350 mg iodine/ml: 3-14 ml per inj, usual: 5 ml. Aortic root and arch study when used alone: 350 mg iodine/ml: 20-75 ml, usual 50 ml. Multiple procedures: 350 mg iodine/ml: max 250 ml.
- Child: Ventriculography: 350 mg iodine/ml: 1-1.5 ml/kg, usual: 1.25 ml/kg; 300 mg iodine/ml: 1.5-2 ml/kg, usual 1.75 ml/kg. Max: 5 ml/kg; 350 mg iodine/ml: 250 ml; 300 mg iodine/ml: 291 ml. Pulmonary angiography: 350 mg iodine/ml: 1 ml/kg. Multiple procedures: Max: 5 ml/kg; 350 mg iodine/ml: 250 ml; 300 mg iodine/ml: 291 ml.
- Adult: Use 300 or 350 mg iodine/ml solution, single inj. Aorta: 50-80 ml; major branches: 30-60 ml; renal arteries: 5-15 ml. Repeat as necessary. Max: 300 mg iodine/ml: 291 ml; 350 mg iodine/ml: 250 ml.
- Child: Use 350 mg iodine/ml solution: 1 ml/kg, single dose. Max: 5 ml/kg up to 250 ml.
- Adult: Use diluted solutions using sterile water for inj to concentrations of 50-100 mg iodine/ml. Usual volume: 50 mg iodine/ml solution: 50-600 ml; 100 mg iodine/ml: 50-300 ml.
- Child: Children: Use diluted solutions using sterile water for inj to concentrations of 50-100 mg iodine/ml: 50-300 ml.
- Adult: 240 mg iodine/ml: 15-20 ml; 300 mg iodine/ml: 15-20 ml.
- Adult: Knee: 240 mg iodine/ml: 5-15 ml; 300 mg iodine/ml: 5-15 ml; 350 mg iodine/ml: 5-10 ml. Shoulder: 240 mg iodine/ml: 3 ml; 300 mg iodine/ml: 10 ml. Temporomandibular: 300 mg iodine/ml: 0.5-1 ml. Lower volumes are recommended for double-contrast examinations; higher volumes are recommended fro single-contrast examinations.
- Adult: 240 mg iodine/ml: 50 ml.
- Adult: Use 300 or 350 mg iodine/ml solution: 200-350 mg iodine/kg.
- Child: Use 300 mg iodine/ml solution: 0.5-3 ml/kg, usual: 1-1.5 ml/kg; max: 3 ml/kg.
- Adult: Use 240 mg iodine/ml: 10-50 ml.
Intra-arterial-
Peripheral arteriography:- Adult: Aortofemoral runoffs: 350 mg iodine/ml: 20-70 ml; 300 mg iodine/ml: 30-90 ml. Selective arteriograms (femoral/iliac): 350 mg iodine/ml: 10-30 ml; 300 mg iodine/ml: 10-60 ml. Venography (per leg): 240 mg iodine/ml: 20-150 ml; 300 mg iodine/ml: 40-100 ml.
- Adult: Use 300 mg iodine/ml solution: Common carotid artery: 6-12 ml; internal carotid artery: 8-10 ml; external carotid artery: 6-9 ml; vertebral artery: 6-10 ml.
- Adult: Use 140 mg iodine/ml solution: Aorta: 20-45 ml at 8-20 ml/sec; carotid: 5-10 ml at 3-6 ml/sec; femoral: 9-20 ml at 3-6 ml/sec; vertebral: 4-10 ml at 2-8 ml/sec; renal: 6-12 ml at 3-6 ml/sec; other branches of the aorta (includes subclavian, axillary, innominate and iliac): 8-25 ml at 3-10 ml/sec.
Intrathecal-
Contrast-enhanced computerized tomography:- Adult: Lumbar (via lumbar inj): 180 mg iodine/ml: 10-17 ml; 240 mg iodine/ml: 7-12.5 ml. Thoracic (via lumbar or cervical inj): 240 mg iodine/ml: 6-12.5 ml; 300 mg iodine/ml: 6-10 ml. Cervical (via lumbar inj): 240 mg iodine/ml: 6-12.5 ml; 300 mg iodine/ml solution: 6-10 ml. Cervical (via C1-2 inj): 180 mg iodine/ml: 7-10 ml; 240 mg iodine/ml: 6-12.5 ml; 300 mg iodine/ml: 4-10 ml. Total columnar (via lumbar inj): 240 mg iodine/ml: 6-12.5 ml; 300 mg iodine/ml: 6-10 ml.
- Child: Use 180 mg iodine/ml solution. 0-<3 mth: 240 ml; 3-<36 mth: 4-8 ml; 3-<7 yr: 5-10 ml; 7-<13 yr: 5-12 ml; 13-18 yr: 6-15 ml.
Intravenous-
Contrast-enhanced computerized tomography of the abdomen:- Adult: In conjunction with dilute oral admin, use 300 mg iodine/ml solution: 100-150 ml. The oral dose is administered 20-40 min prior to IV dose and image acquisition.
- Child: In conjunction with dilute oral admin, use 240 or 300 mg iodine/ml solution: 1-2 ml/kg; max 3 ml/kg. The oral dose is administered 30-60 min prior to IV dose and image acquisition.
- Adult: 350 mg iodine/ml: 30-50 ml, as a bolus at 7.5-30 ml/second using a pressure injector, usually for 3 or more inj; max: 250 ml.
- Adult: Head imaging by inj: 300 mg iodine/ml: 70-150 ml; 350 mg iodine/ml: 80 ml. Head imaging by infusion: 240 mg iodine/ml: 120-250 ml. Body imaging by inj: 300 mg iodine/ml: 50-200 ml; 350 mg iodine/ml: 60-100 ml.
- Child: Head imaging: 240 or 300 mg iodine/ml: 1-2 ml/kg. Max: 28 g iodine with 240 mg iodine/ml solution or 35 g iodine with 300 mg iodine/ml solution.
AdministrationView
Dose and strength used depends on the procedure and route of administration.
Side effectsView
Flushing or a sensation of heat; pain, extravasation, thrombophlebitis at the inj site; nausea, vomiting, headache, and dizziness; urticaria, pruritus, pallor, sweating, metallic taste, weakness, coughing, rhinitis, sneezing, lachrymation, visual disturbances; hypotension, tachycardia, bradycardia, transient ECG abnormalities, haemodynamic disturbances; dyspnoea, bronchospasm, angioedema, severe urticaria; convulsions, paraesthesia, paralysis; acute renal failure; thromboembolism, disseminated intravascular coagulation, thrombocytopenia; hyperthyroidism, thyroid storm thyrotoxicosis.
ContraindicationsView
Manifest thyrotoxicosis. History of serious reaction to Iohexol.
PrecautionsView
A positive history of allergy, asthma, or untoward reactions to iodinated contrast media indicates a need for special caution. Premedication with corticosteroids or histamine H1 and H2 antagonists might be considered in these cases. The risk of serious reactions in connection with use of Iohexol is regarded as minor. However, iodinated contrast media may provoke anaphylactoid reactions or other manifestations of hypersensitivity. A course of action should therefore be planned in advance, with necessary drugs and equipment available for immediate treatment, should a serious reaction occur. It is advisable always to use an indwelling cannula or catheter for quick intravenous access throughout the entire X-ray procedure. Non-ionic contrast media have less effect on the coagulation system in vitro, compared to ionic contrast media. When performing vascular catheterisation procedures one should pay meticulous attention to the angiographic technique and flush the catheter frequently (e.g.: with heparinised saline) so as to minimise the risk of procedure-related thrombosis and embolism. Adequate hydration should be assured before and after contrast media administration. This applies especially to patients with multiple myeloma, diabetes mellitus, renal dysfunction, as well as to infants, small children and elderly patients. Young infants (age < 1 year) and especially neonates are susceptible to electrolyte disturbance and haemodynamic alterations. Care should also be taken in patients with serious cardiac disease and pulmonary hypertension as they may develop haemodynamic changes or arrhythmias. Patients with acute cerebral pathology, tumours or a history of epilepsy are predisposed for seizures and merit particular care. Also alcoholics and drug addicts have an increased risk for seizures and neurological reactions. A few patients have experienced a temporary hearing loss or even deafness after myelography, which is believed to be due to a drop in spinal fluid pressure by the lumbar puncture per se. To prevent acute renal failure following contrast media administration, special care should be exercised in patients with pre-existing renal impairment and diabetes mellitus as they are at risk. Patients with paraproteinemias (myelomatosis and Waldenström's macroglobulinemia) are also at risk
InteractionsView
Use of contrast media may result in a transient impairment of renal function and this may precipitate lactic acidosis in diabetics who are taking metformin (see Warnings and Precautions). Patients treated with interleukin-2 less than two weeks previously have been associated with an increased risk for delayed reactions (flu-like symptoms or skin reactions). All iodinated contrast media may interfere with tests on thyroid function, thus the iodine binding capacity of the thyroid may be reduced for up to several weeks. High concentrations of contrast media in serum and urine can interfere with laboratory tests for bilirubin, proteins or inorganic substances (e.g. iron, copper, calcium and phosphate). These substances should therefore not be assayed on the day of examination.
Pregnancy & lactationView
Use in Pregnancy: The safety of Iohexol for use in human pregnancy has not been established. An evaluation of experimental animal studies does not indicate direct or indirect harmful effects with respect to reproduction, development of the embryo or foetus, the course of gestation and peri- and postnatal development. Since whenever possible, radiation exposure should be avoided during pregnancy, the benefits of an X-ray examination, with or without contrast media, should be carefully weighed against the possible risk. Iohexol should not be used in pregnancy unless the benefit outweighs the risk and it is considered essential by the physician.
Use during Lactation: Breast feeding may be continued normally when iodinated contrast media are given to the mother.
Use during Lactation: Breast feeding may be continued normally when iodinated contrast media are given to the mother.
Overdose effectsView
Preclinical data indicate a high safety margin for Iohexol and no fixed upper dose level has been established for routine intravascular use. Symptomatic overdosing is unlikely in patients with normal renal function unless the patient has received an excess of 2000 mg I/kg body-weight over a limited period of time. The duration of the procedure is important for the renal tolerability of high doses of contrast media (t½ ~ 2 hours). Accidental overdosing is most likely following complex angiographic procedures in children, particularly when multiple injections of contrast medium with high-concentration are given. In cases of overdose, any resulting water or electrolyte imbalance must be corrected. Renal function should be monitored for the next 3 days. If needed, haemodialysis may be used for clearance of excessive contrast medium. There is no specific antidote.
ReconstitutionView
Like all parenteral products, Iohexol should be inspected visually for particulate matter, discoloration and the integrity of the container prior to use. The product should be drawn into the syringe immediately before use. Vials are intended for single use only, any unused portions must be discarded. The 500 ml contrast medium bottles should only be used in connection with auto injectors/pumps approved for this volume. A single piercing procedure should be used. The line running from the auto injector/pump to the patient must be exchanged after each patient. Any unused portions of the contrast medium remaining in the bottle and all connecting tubes must be discarded at the end of the day. When convenient, smaller bottles can also be used. Instructions from the manufacturer of the auto injector/pump must be followed.
StorageView
Store at room temperature below 30° C and protect from light and secondary X-rays. The product in glass vials and bottles may be stored at 37° C for up to 3 months prior to use.Do not freeze.
Imitab
Imatinib Mesylate
Imitab
Imatinib Mesylate
Indication detailsView
- Newly diagnosed adult and pediatric patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+CML) in chronic phase.
- Patients with Philadelphia chromosome positive chronic myeloid leukemia in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy.
- Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL).
- Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy
- Adult patients with myelodysplastic/myeloproliferative diseases associated with platelet-derived growth factor receptor (PDGFR) gene re-arrangements.
- Adult patients with aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown.
- Adult patients with hypereosinophilic syndrome and/or chronic eosinophilic leukemia who have the FIP1L1-PDGFR a fusion kinase (mutational analysis or fluorescence in situ hybridization [FISH] demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRa fusion kinase negative or unknown.
- Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans.
- Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors.
- Adjuvant treatment of adult patients following complete gross resection of Kit (CD117) positive GIST.
Therapeutic classView
Targeted Cancer Therapy, Tyrosine Kinase Inhibitor
PharmacologyView
Imatinib is a small molecule protein-tyrosine kinase inhibitor that potently inhibits the activity of the Bcr-Abl tyrosine kinase (TK), as well as several receptor TKs: Kit, the receptor for stem cell factor (SCF) coded for by the c-Kit proto-oncogene, the discoidin domain receptors (DDR1 and DDR2), the colony stimulating factor receptor (CSF-1R) and the platelet-derived growth factor receptors alpha and beta (PDGFR-alpha and PDGFR beta). Imatinib can also inhibit cellular events mediated by activation of these receptor kinases.
Absorption and Distribution: Imatinib is well absorbed after oral administration with Cmax achieved within 2 4 hours post-dose. Mean absolute bioavailability is 98%. Mean Imatinib AUC increases proportionally with increasing doses ranging from 25 mg to 1,000 mg. There is no significant change in the pharmacokinetics of Imatinib on repeated dosing, and accumulation is 1.5- to 2.5- fold at a steady state when Imatinib is dosed once daily. At clinically relevant concentrations of Imatinib, binding to plasma proteins in in vitro experiments is approximately 95%, mostly to albumin and 1-acid glycoprotein.
Metabolism: CYP3A4 is the major enzyme responsible for metabolism of Imatinib. Other cytochrome P450 enzymes, such as CYP1A2, CYP2D6, CYP2C9, and CYP2C19, play a minor role in its metabolism. The main circulating active metabolite in humans is the N-demethylated piperazine derivative, formed predominantly by CYP3A4. It shows in vitro potency similar to the parent Imatinib. The plasma AUC for this metabolite is about 15% of the AUC for Imatinib. The plasma protein binding of N-demethylated metabolite CGP74588 is similar to that of the parent compound.
Excretion: Imatinib elimination is predominately in the feces, mostly as metabolites. Based on the recovery of compound(s) after an oral 14C-labeled dose of Imatinib, approximately 81% of the dose was eliminated within 7 days, in feces (68% of dose) and urine (13% of dose). Unchanged Imatinib accounted for 25% of the dose (5% urine, 20% feces), the remainder being metabolites. Following oral administration in healthy volunteers, the elimination half-lives of Imatinib and its major active metabolite, the N-demethyl derivative (CGP74588), are approximately 18 and 40 hours, respectively.
Absorption and Distribution: Imatinib is well absorbed after oral administration with Cmax achieved within 2 4 hours post-dose. Mean absolute bioavailability is 98%. Mean Imatinib AUC increases proportionally with increasing doses ranging from 25 mg to 1,000 mg. There is no significant change in the pharmacokinetics of Imatinib on repeated dosing, and accumulation is 1.5- to 2.5- fold at a steady state when Imatinib is dosed once daily. At clinically relevant concentrations of Imatinib, binding to plasma proteins in in vitro experiments is approximately 95%, mostly to albumin and 1-acid glycoprotein.
Metabolism: CYP3A4 is the major enzyme responsible for metabolism of Imatinib. Other cytochrome P450 enzymes, such as CYP1A2, CYP2D6, CYP2C9, and CYP2C19, play a minor role in its metabolism. The main circulating active metabolite in humans is the N-demethylated piperazine derivative, formed predominantly by CYP3A4. It shows in vitro potency similar to the parent Imatinib. The plasma AUC for this metabolite is about 15% of the AUC for Imatinib. The plasma protein binding of N-demethylated metabolite CGP74588 is similar to that of the parent compound.
Excretion: Imatinib elimination is predominately in the feces, mostly as metabolites. Based on the recovery of compound(s) after an oral 14C-labeled dose of Imatinib, approximately 81% of the dose was eliminated within 7 days, in feces (68% of dose) and urine (13% of dose). Unchanged Imatinib accounted for 25% of the dose (5% urine, 20% feces), the remainder being metabolites. Following oral administration in healthy volunteers, the elimination half-lives of Imatinib and its major active metabolite, the N-demethyl derivative (CGP74588), are approximately 18 and 40 hours, respectively.
DosageView
Adults with Ph+ CML CP: 400 mg/day
Adults with Ph+ CML AP or BC: 600 mg/day
Pediatrics with Ph+ CML CP: 340 mg/m2/day
Adults with Ph+ ALL: 600 mg/day
Pediatrics with Ph+ ALL: 340 mg/m2/day
Adults with MDS/MPD: 400 mg/day
Adults with ASM: 100 mg/day or 400 mg/day
Adults with HES/CEL: 100 mg/day or 400 mg/day
Adults with DFSP: 800 mg/day
Adults with metastatic and/or unresectable GIST: 400 mg/day
Adjuvant treatment of adults with GIST: 400 mg/day
Patients with mild to moderate hepatic impairment: 400 mg/day
Patients with severe hepatic impairment: 300 mg/day
All doses of Imatinib should be taken with a meal and a large glass of water. Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day. Imatinib can be dissolved in water or apple juice for patients having difficulty swallowing. Daily dosing of 800 mg and above should be accomplished using the 400-mg tablet to reduce exposure to iron.
Adults with Ph+ CML AP or BC: 600 mg/day
Pediatrics with Ph+ CML CP: 340 mg/m2/day
Adults with Ph+ ALL: 600 mg/day
Pediatrics with Ph+ ALL: 340 mg/m2/day
Adults with MDS/MPD: 400 mg/day
Adults with ASM: 100 mg/day or 400 mg/day
Adults with HES/CEL: 100 mg/day or 400 mg/day
Adults with DFSP: 800 mg/day
Adults with metastatic and/or unresectable GIST: 400 mg/day
Adjuvant treatment of adults with GIST: 400 mg/day
Patients with mild to moderate hepatic impairment: 400 mg/day
Patients with severe hepatic impairment: 300 mg/day
All doses of Imatinib should be taken with a meal and a large glass of water. Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day. Imatinib can be dissolved in water or apple juice for patients having difficulty swallowing. Daily dosing of 800 mg and above should be accomplished using the 400-mg tablet to reduce exposure to iron.
Side effectsView
The following serious adverse reactions are described elsewhere in the labeling:
- Fluid Retention and Edema
- Hematologic Toxicity
- Congestive Heart Failure and Left Ventricular Dysfunction
- Hepatotoxicity
- Hemorrhage
- Gastrointestinal Disorders
- Hypereosinophilic Cardiac Toxicity
- Dermatologic Toxicities
- Hypothyroidism
- Growth Retardation in Children and Adolescents
- Tumor Lysis Syndrome
- Impairments Related to Driving and Using Machinery
- Renal Toxicity
PrecautionsView
- Edema and severe fluid retention have occurred. Weigh patients regularly and manage unexpected rapid weight gain by drug interruption and diuretics.
- Cytopenias, particularly anemia, neutropenia, and thrombocytopenia, have occurred. Manage with dose reduction, dose interruption, or discontinuation of treatment. Perform complete blood counts weekly for the first month, biweekly for the second month, and periodically thereafter.
- Severe congestive heart failure and left ventricular dysfunction have been reported, particularly in patients with comorbidities and risk factors. Monitor and treat patients with cardiac disease or risk factors for cardiac failure.
- Severe hepatotoxicity, including fatalities may occur. Assess liver function before initiation of treatment and monthly thereafter or as clinically indicated. Monitor liver function when combined with chemotherapy known to be associated with liver dysfunction.
- Grade 3/4 hemorrhage has been reported in clinical studies in patients with newly diagnosed CML and with GIST. Gl tumor sites may be the source of Gl bleeds in GIST. Gastrointestinal (Gl) perforations, some fatal, have been reported.
- Cardiogenic shock/left ventricular dysfunction has been associated with the initiation of Imatinib in patients with conditions associated with high eosinophil levels (e.g., HES, MDS/MPD, and ASM).
- Bullous dermatologic reactions (e.g., erythema multiforme and Stevens-Johnson syndrome) have been reported with the use of Imatinib.
- Hypothyroidism has been reported in thyroidectomy ZyvaxatX patients undergoing levothyroxine replacement. Closely monitor TSH levels in such patients.
- Fetal harm can occur when administered to a pregnant woman. Apprise women of the potential harm to the fetus, and to avoid pregnancy when taking Imatinib.
- Growth retardation occurring in children and pre-adolescents receiving Imatinib has been reported. Close monitoring of growth in children under Imatinib treatment is recommended.
- Tumor Lysis Syndrome. Close monitoring is recommended.
- Reports of motor vehicle accidents have been received in patients receiving Imatinib. Caution patients about driving a car or operating machinery.
- Renal Toxicity. A decline in renal function may occur in patients receiving Imatinib. Evaluate renal function at baseline and during therapy, with attention to risk factors for renal dysfunction.
InteractionsView
Agents Inducing CYP3A Metabolism: Concomitant administration of Imatinib and strong CYP3A4 inducers may reduce total exposure of imatinib; consider alternative agents.
Agents Inhibiting CYP3A Metabolism: Concomitant administration of Imatinib and strong CYP3A4 inhibitors may result in a significant imatinib exposure increase. Grapefruit juice may also increase plasma concentrations of imatinib; avoid grapefruit juice).
Interactions with Drugs Metabolized by CYP3A4: Imatinib will increase plasma concentration of CYP3A4 metabolized drugs (e.g., triazolo-benzodiazepines, dihydropyridine calcium channel blockers, certain HMG-CoA reductase inhibitors, etc.). Use caution when administering Imatinib with CYP3A4 substrates that have a narrow therapeutic window. Because warfarin is metabolized by CYP2C9 and CYP3A4, use low-molecular weight or standard heparin instead of warfarin in patients who require anticoagulation.
Interactions with Drugs Metabolized by CYP2D6: Use caution when administering Imatinib with CYP2D6 substrates that have a narrow therapeutic window.
Agents Inhibiting CYP3A Metabolism: Concomitant administration of Imatinib and strong CYP3A4 inhibitors may result in a significant imatinib exposure increase. Grapefruit juice may also increase plasma concentrations of imatinib; avoid grapefruit juice).
Interactions with Drugs Metabolized by CYP3A4: Imatinib will increase plasma concentration of CYP3A4 metabolized drugs (e.g., triazolo-benzodiazepines, dihydropyridine calcium channel blockers, certain HMG-CoA reductase inhibitors, etc.). Use caution when administering Imatinib with CYP3A4 substrates that have a narrow therapeutic window. Because warfarin is metabolized by CYP2C9 and CYP3A4, use low-molecular weight or standard heparin instead of warfarin in patients who require anticoagulation.
Interactions with Drugs Metabolized by CYP2D6: Use caution when administering Imatinib with CYP2D6 substrates that have a narrow therapeutic window.
Pregnancy & lactationView
Women of childbearing potential: Women of childbearing potential must be advised to use effective contraception during treatment and for at least 15 days after stopping treatment with Imatinib.
Pregnancy: There are limited data on the use of imatinib in pregnant women. There have been post-marketing reports of spontaneous abortions and infant congenital anomalies from women who have taken Imatinib. Studies in animals have however shown reproductive toxicity and the potential risk for the foetus is unknown. Imatinib should not be used during pregnancy unless clearly necessary. If it is used during pregnancy, the patient must be informed of the potential risk to the foetus.
Breast-feeding: There is limited information on imatinib distribution on human milk. Studies in two breast feeding women revealed that both imatinib and its active metabolite can be distributed into human milk. The milk plasma ratio studied in a single patient was determined to be 0.5 for imatinib and 0.9 for the metabolite, suggesting greater distribution of the metabolite into the milk. Considering the combined concentration of imatinib and the metabolite and the maximum daily milk intake by infants, the total exposure would be expected to be low (-10% of a therapeutic dose). However, since the effects of low-dose exposure of the infant to imatinib are unknown, women should not breast-feed during treatment and for at least 15 days after stopping treatment with Imatinib.
Fertility: In non-clinical studies, the fertility of male and female rats was not affected, although effects on reproductive parameters were observed. Studies on patients receiving Imatinib and its effect on fertility and gametogenesis have not been performed. Patients concerned about their fertility on Imatinib treatment should consult with their physician.
Pregnancy: There are limited data on the use of imatinib in pregnant women. There have been post-marketing reports of spontaneous abortions and infant congenital anomalies from women who have taken Imatinib. Studies in animals have however shown reproductive toxicity and the potential risk for the foetus is unknown. Imatinib should not be used during pregnancy unless clearly necessary. If it is used during pregnancy, the patient must be informed of the potential risk to the foetus.
Breast-feeding: There is limited information on imatinib distribution on human milk. Studies in two breast feeding women revealed that both imatinib and its active metabolite can be distributed into human milk. The milk plasma ratio studied in a single patient was determined to be 0.5 for imatinib and 0.9 for the metabolite, suggesting greater distribution of the metabolite into the milk. Considering the combined concentration of imatinib and the metabolite and the maximum daily milk intake by infants, the total exposure would be expected to be low (-10% of a therapeutic dose). However, since the effects of low-dose exposure of the infant to imatinib are unknown, women should not breast-feed during treatment and for at least 15 days after stopping treatment with Imatinib.
Fertility: In non-clinical studies, the fertility of male and female rats was not affected, although effects on reproductive parameters were observed. Studies on patients receiving Imatinib and its effect on fertility and gametogenesis have not been performed. Patients concerned about their fertility on Imatinib treatment should consult with their physician.
Overdose effectsView
Experience with doses higher than the recommended therapeutic dose is limited. In the event of overdose the patient should be observed and an appropriate symptomatic treatment given. Generally, the reported outcome in these cases was "improved" or "recovered". Events that have been reported at different dose ranges are as follows:
Adult Population:
Adult Population:
- 1200 to 1600 mg (duration varying between 1 to 10 days): Nausea, vomiting, diarrhoea, rash, erythema, oedema, swelling, fatigue, muscle spasms, thrombocytopenia, pancytopenia, abdominal pain, headache, decreased appetite.
- 1800 to 3200 mg (as high as 3200 mg daily for 6 days): Weakness, myalgia, increased creatine phosphokinase,
- increased bilirubin, gastrointestinal pain.
- 6400 mg (single dose): One case reported in the literature of one patient who experienced nausea, vomiting, abdominal pain, pyrexia, facial swelling, decreased neutrophil count, and increased transaminases.
- 8 to 10 g (single dose): Vomiting and gastrointestinal pain have been reported.
StorageView
Store below 30°C, in a cool and dry place. Keep away from light. Keep out of the reach of children.
Imitab
Imatinib Mesylate
Imitab
Imatinib Mesylate
Indication detailsView
- Newly diagnosed adult and pediatric patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+CML) in chronic phase.
- Patients with Philadelphia chromosome positive chronic myeloid leukemia in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy.
- Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL).
- Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy
- Adult patients with myelodysplastic/myeloproliferative diseases associated with platelet-derived growth factor receptor (PDGFR) gene re-arrangements.
- Adult patients with aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown.
- Adult patients with hypereosinophilic syndrome and/or chronic eosinophilic leukemia who have the FIP1L1-PDGFR a fusion kinase (mutational analysis or fluorescence in situ hybridization [FISH] demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRa fusion kinase negative or unknown.
- Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans.
- Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors.
- Adjuvant treatment of adult patients following complete gross resection of Kit (CD117) positive GIST.
Therapeutic classView
Targeted Cancer Therapy, Tyrosine Kinase Inhibitor
PharmacologyView
Imatinib is a small molecule protein-tyrosine kinase inhibitor that potently inhibits the activity of the Bcr-Abl tyrosine kinase (TK), as well as several receptor TKs: Kit, the receptor for stem cell factor (SCF) coded for by the c-Kit proto-oncogene, the discoidin domain receptors (DDR1 and DDR2), the colony stimulating factor receptor (CSF-1R) and the platelet-derived growth factor receptors alpha and beta (PDGFR-alpha and PDGFR beta). Imatinib can also inhibit cellular events mediated by activation of these receptor kinases.
Absorption and Distribution: Imatinib is well absorbed after oral administration with Cmax achieved within 2 4 hours post-dose. Mean absolute bioavailability is 98%. Mean Imatinib AUC increases proportionally with increasing doses ranging from 25 mg to 1,000 mg. There is no significant change in the pharmacokinetics of Imatinib on repeated dosing, and accumulation is 1.5- to 2.5- fold at a steady state when Imatinib is dosed once daily. At clinically relevant concentrations of Imatinib, binding to plasma proteins in in vitro experiments is approximately 95%, mostly to albumin and 1-acid glycoprotein.
Metabolism: CYP3A4 is the major enzyme responsible for metabolism of Imatinib. Other cytochrome P450 enzymes, such as CYP1A2, CYP2D6, CYP2C9, and CYP2C19, play a minor role in its metabolism. The main circulating active metabolite in humans is the N-demethylated piperazine derivative, formed predominantly by CYP3A4. It shows in vitro potency similar to the parent Imatinib. The plasma AUC for this metabolite is about 15% of the AUC for Imatinib. The plasma protein binding of N-demethylated metabolite CGP74588 is similar to that of the parent compound.
Excretion: Imatinib elimination is predominately in the feces, mostly as metabolites. Based on the recovery of compound(s) after an oral 14C-labeled dose of Imatinib, approximately 81% of the dose was eliminated within 7 days, in feces (68% of dose) and urine (13% of dose). Unchanged Imatinib accounted for 25% of the dose (5% urine, 20% feces), the remainder being metabolites. Following oral administration in healthy volunteers, the elimination half-lives of Imatinib and its major active metabolite, the N-demethyl derivative (CGP74588), are approximately 18 and 40 hours, respectively.
Absorption and Distribution: Imatinib is well absorbed after oral administration with Cmax achieved within 2 4 hours post-dose. Mean absolute bioavailability is 98%. Mean Imatinib AUC increases proportionally with increasing doses ranging from 25 mg to 1,000 mg. There is no significant change in the pharmacokinetics of Imatinib on repeated dosing, and accumulation is 1.5- to 2.5- fold at a steady state when Imatinib is dosed once daily. At clinically relevant concentrations of Imatinib, binding to plasma proteins in in vitro experiments is approximately 95%, mostly to albumin and 1-acid glycoprotein.
Metabolism: CYP3A4 is the major enzyme responsible for metabolism of Imatinib. Other cytochrome P450 enzymes, such as CYP1A2, CYP2D6, CYP2C9, and CYP2C19, play a minor role in its metabolism. The main circulating active metabolite in humans is the N-demethylated piperazine derivative, formed predominantly by CYP3A4. It shows in vitro potency similar to the parent Imatinib. The plasma AUC for this metabolite is about 15% of the AUC for Imatinib. The plasma protein binding of N-demethylated metabolite CGP74588 is similar to that of the parent compound.
Excretion: Imatinib elimination is predominately in the feces, mostly as metabolites. Based on the recovery of compound(s) after an oral 14C-labeled dose of Imatinib, approximately 81% of the dose was eliminated within 7 days, in feces (68% of dose) and urine (13% of dose). Unchanged Imatinib accounted for 25% of the dose (5% urine, 20% feces), the remainder being metabolites. Following oral administration in healthy volunteers, the elimination half-lives of Imatinib and its major active metabolite, the N-demethyl derivative (CGP74588), are approximately 18 and 40 hours, respectively.
DosageView
Adults with Ph+ CML CP: 400 mg/day
Adults with Ph+ CML AP or BC: 600 mg/day
Pediatrics with Ph+ CML CP: 340 mg/m2/day
Adults with Ph+ ALL: 600 mg/day
Pediatrics with Ph+ ALL: 340 mg/m2/day
Adults with MDS/MPD: 400 mg/day
Adults with ASM: 100 mg/day or 400 mg/day
Adults with HES/CEL: 100 mg/day or 400 mg/day
Adults with DFSP: 800 mg/day
Adults with metastatic and/or unresectable GIST: 400 mg/day
Adjuvant treatment of adults with GIST: 400 mg/day
Patients with mild to moderate hepatic impairment: 400 mg/day
Patients with severe hepatic impairment: 300 mg/day
All doses of Imatinib should be taken with a meal and a large glass of water. Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day. Imatinib can be dissolved in water or apple juice for patients having difficulty swallowing. Daily dosing of 800 mg and above should be accomplished using the 400-mg tablet to reduce exposure to iron.
Adults with Ph+ CML AP or BC: 600 mg/day
Pediatrics with Ph+ CML CP: 340 mg/m2/day
Adults with Ph+ ALL: 600 mg/day
Pediatrics with Ph+ ALL: 340 mg/m2/day
Adults with MDS/MPD: 400 mg/day
Adults with ASM: 100 mg/day or 400 mg/day
Adults with HES/CEL: 100 mg/day or 400 mg/day
Adults with DFSP: 800 mg/day
Adults with metastatic and/or unresectable GIST: 400 mg/day
Adjuvant treatment of adults with GIST: 400 mg/day
Patients with mild to moderate hepatic impairment: 400 mg/day
Patients with severe hepatic impairment: 300 mg/day
All doses of Imatinib should be taken with a meal and a large glass of water. Doses of 400 mg or 600 mg should be administered once daily, whereas a dose of 800 mg should be administered as 400 mg twice a day. Imatinib can be dissolved in water or apple juice for patients having difficulty swallowing. Daily dosing of 800 mg and above should be accomplished using the 400-mg tablet to reduce exposure to iron.
Side effectsView
The following serious adverse reactions are described elsewhere in the labeling:
- Fluid Retention and Edema
- Hematologic Toxicity
- Congestive Heart Failure and Left Ventricular Dysfunction
- Hepatotoxicity
- Hemorrhage
- Gastrointestinal Disorders
- Hypereosinophilic Cardiac Toxicity
- Dermatologic Toxicities
- Hypothyroidism
- Growth Retardation in Children and Adolescents
- Tumor Lysis Syndrome
- Impairments Related to Driving and Using Machinery
- Renal Toxicity
PrecautionsView
- Edema and severe fluid retention have occurred. Weigh patients regularly and manage unexpected rapid weight gain by drug interruption and diuretics.
- Cytopenias, particularly anemia, neutropenia, and thrombocytopenia, have occurred. Manage with dose reduction, dose interruption, or discontinuation of treatment. Perform complete blood counts weekly for the first month, biweekly for the second month, and periodically thereafter.
- Severe congestive heart failure and left ventricular dysfunction have been reported, particularly in patients with comorbidities and risk factors. Monitor and treat patients with cardiac disease or risk factors for cardiac failure.
- Severe hepatotoxicity, including fatalities may occur. Assess liver function before initiation of treatment and monthly thereafter or as clinically indicated. Monitor liver function when combined with chemotherapy known to be associated with liver dysfunction.
- Grade 3/4 hemorrhage has been reported in clinical studies in patients with newly diagnosed CML and with GIST. Gl tumor sites may be the source of Gl bleeds in GIST. Gastrointestinal (Gl) perforations, some fatal, have been reported.
- Cardiogenic shock/left ventricular dysfunction has been associated with the initiation of Imatinib in patients with conditions associated with high eosinophil levels (e.g., HES, MDS/MPD, and ASM).
- Bullous dermatologic reactions (e.g., erythema multiforme and Stevens-Johnson syndrome) have been reported with the use of Imatinib.
- Hypothyroidism has been reported in thyroidectomy ZyvaxatX patients undergoing levothyroxine replacement. Closely monitor TSH levels in such patients.
- Fetal harm can occur when administered to a pregnant woman. Apprise women of the potential harm to the fetus, and to avoid pregnancy when taking Imatinib.
- Growth retardation occurring in children and pre-adolescents receiving Imatinib has been reported. Close monitoring of growth in children under Imatinib treatment is recommended.
- Tumor Lysis Syndrome. Close monitoring is recommended.
- Reports of motor vehicle accidents have been received in patients receiving Imatinib. Caution patients about driving a car or operating machinery.
- Renal Toxicity. A decline in renal function may occur in patients receiving Imatinib. Evaluate renal function at baseline and during therapy, with attention to risk factors for renal dysfunction.
InteractionsView
Agents Inducing CYP3A Metabolism: Concomitant administration of Imatinib and strong CYP3A4 inducers may reduce total exposure of imatinib; consider alternative agents.
Agents Inhibiting CYP3A Metabolism: Concomitant administration of Imatinib and strong CYP3A4 inhibitors may result in a significant imatinib exposure increase. Grapefruit juice may also increase plasma concentrations of imatinib; avoid grapefruit juice).
Interactions with Drugs Metabolized by CYP3A4: Imatinib will increase plasma concentration of CYP3A4 metabolized drugs (e.g., triazolo-benzodiazepines, dihydropyridine calcium channel blockers, certain HMG-CoA reductase inhibitors, etc.). Use caution when administering Imatinib with CYP3A4 substrates that have a narrow therapeutic window. Because warfarin is metabolized by CYP2C9 and CYP3A4, use low-molecular weight or standard heparin instead of warfarin in patients who require anticoagulation.
Interactions with Drugs Metabolized by CYP2D6: Use caution when administering Imatinib with CYP2D6 substrates that have a narrow therapeutic window.
Agents Inhibiting CYP3A Metabolism: Concomitant administration of Imatinib and strong CYP3A4 inhibitors may result in a significant imatinib exposure increase. Grapefruit juice may also increase plasma concentrations of imatinib; avoid grapefruit juice).
Interactions with Drugs Metabolized by CYP3A4: Imatinib will increase plasma concentration of CYP3A4 metabolized drugs (e.g., triazolo-benzodiazepines, dihydropyridine calcium channel blockers, certain HMG-CoA reductase inhibitors, etc.). Use caution when administering Imatinib with CYP3A4 substrates that have a narrow therapeutic window. Because warfarin is metabolized by CYP2C9 and CYP3A4, use low-molecular weight or standard heparin instead of warfarin in patients who require anticoagulation.
Interactions with Drugs Metabolized by CYP2D6: Use caution when administering Imatinib with CYP2D6 substrates that have a narrow therapeutic window.
Pregnancy & lactationView
Women of childbearing potential: Women of childbearing potential must be advised to use effective contraception during treatment and for at least 15 days after stopping treatment with Imatinib.
Pregnancy: There are limited data on the use of imatinib in pregnant women. There have been post-marketing reports of spontaneous abortions and infant congenital anomalies from women who have taken Imatinib. Studies in animals have however shown reproductive toxicity and the potential risk for the foetus is unknown. Imatinib should not be used during pregnancy unless clearly necessary. If it is used during pregnancy, the patient must be informed of the potential risk to the foetus.
Breast-feeding: There is limited information on imatinib distribution on human milk. Studies in two breast feeding women revealed that both imatinib and its active metabolite can be distributed into human milk. The milk plasma ratio studied in a single patient was determined to be 0.5 for imatinib and 0.9 for the metabolite, suggesting greater distribution of the metabolite into the milk. Considering the combined concentration of imatinib and the metabolite and the maximum daily milk intake by infants, the total exposure would be expected to be low (-10% of a therapeutic dose). However, since the effects of low-dose exposure of the infant to imatinib are unknown, women should not breast-feed during treatment and for at least 15 days after stopping treatment with Imatinib.
Fertility: In non-clinical studies, the fertility of male and female rats was not affected, although effects on reproductive parameters were observed. Studies on patients receiving Imatinib and its effect on fertility and gametogenesis have not been performed. Patients concerned about their fertility on Imatinib treatment should consult with their physician.
Pregnancy: There are limited data on the use of imatinib in pregnant women. There have been post-marketing reports of spontaneous abortions and infant congenital anomalies from women who have taken Imatinib. Studies in animals have however shown reproductive toxicity and the potential risk for the foetus is unknown. Imatinib should not be used during pregnancy unless clearly necessary. If it is used during pregnancy, the patient must be informed of the potential risk to the foetus.
Breast-feeding: There is limited information on imatinib distribution on human milk. Studies in two breast feeding women revealed that both imatinib and its active metabolite can be distributed into human milk. The milk plasma ratio studied in a single patient was determined to be 0.5 for imatinib and 0.9 for the metabolite, suggesting greater distribution of the metabolite into the milk. Considering the combined concentration of imatinib and the metabolite and the maximum daily milk intake by infants, the total exposure would be expected to be low (-10% of a therapeutic dose). However, since the effects of low-dose exposure of the infant to imatinib are unknown, women should not breast-feed during treatment and for at least 15 days after stopping treatment with Imatinib.
Fertility: In non-clinical studies, the fertility of male and female rats was not affected, although effects on reproductive parameters were observed. Studies on patients receiving Imatinib and its effect on fertility and gametogenesis have not been performed. Patients concerned about their fertility on Imatinib treatment should consult with their physician.
Overdose effectsView
Experience with doses higher than the recommended therapeutic dose is limited. In the event of overdose the patient should be observed and an appropriate symptomatic treatment given. Generally, the reported outcome in these cases was "improved" or "recovered". Events that have been reported at different dose ranges are as follows:
Adult Population:
Adult Population:
- 1200 to 1600 mg (duration varying between 1 to 10 days): Nausea, vomiting, diarrhoea, rash, erythema, oedema, swelling, fatigue, muscle spasms, thrombocytopenia, pancytopenia, abdominal pain, headache, decreased appetite.
- 1800 to 3200 mg (as high as 3200 mg daily for 6 days): Weakness, myalgia, increased creatine phosphokinase,
- increased bilirubin, gastrointestinal pain.
- 6400 mg (single dose): One case reported in the literature of one patient who experienced nausea, vomiting, abdominal pain, pyrexia, facial swelling, decreased neutrophil count, and increased transaminases.
- 8 to 10 g (single dose): Vomiting and gastrointestinal pain have been reported.
StorageView
Store below 30°C, in a cool and dry place. Keep away from light. Keep out of the reach of children.
Immense
Sildenafil Citrate
Immense
Sildenafil Citrate
Indications
Pulmonary arterial hypertension
Indication detailsView
Sildenafil is indicated for the treatment of erectile dysfunction.
Therapeutic classView
Drugs for Erectile Dysfunction
PharmacologyView
Sildenafil is a selective inhibitor of cyclic Guanosine Monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) used for treatment of erectile dysfunction. Danafil (Sildenafil) enhances the effect of nitric oxide (NO) by inhibiting phosphodiesterase type 5 (PDE5), which is responsible for degradation of cGMP in the corpus cavernosum that results in smooth muscle relaxation and inflow of blood to the corpus cavernosum.
DosageView
The recommended dose of Sildenafil is 50 mg taken approximately 1 hour before sexual activity. However, Sildenafil may be taken anywhere from half an hour to 4 hours before sexual activity. Based on effectiveness and toleration, the dose may be increased to a maximum 100 mg or decreased to 25 mg. The maximum recommended dosing frequency is once per day.
AdministrationView
Sildenafil may takes longer time to work if you take it with a heavy meal.
Side effectsView
The adverse effects treated with Sildenafil are headache, flushing, dyspepsia, nasal congestion, urinary tract infection, abnormal vision, diarrhea, dizziness and rash.
ContraindicationsView
Sildenafil is contraindicated in patient with hypersensitivity to any component of this medication. Sildenafil potentiates the hypotensive effects of nitrates, so it is contraindicated in patients who are using organic nitrates, either regularly or intermittently.
PrecautionsView
Caution should be exercised if patients have any allergies to any other medicines or any other substances such as foods, preservatives or dyes, heart or blood vessel problems, sudden loss of eyesight in one or both eyes. Caution should be taken if patients have any of the following medical conditions such as diabetes, kidney or liver problems, leukaemia, multiple myeloma, any disease or deformity of penis, any bleeding disorder such as haemophilia, stomach ulcer, sickle cell anaemia, color vision problems, sudden decrease or loss of hearing or receiving any other treatment for impotence.
InteractionsView
Concomitant use of Sildenafil with organic nitrates for angina may cause hypotension. Cimetidine, a medicine used to treat gastric ulcers, some antibiotics including Erythromycin and Rifampicin, some protease inhibitors such as Ritonavir and Saquinavir for the treatment of HIV infection may increase the plasma concentration of Sildenafil. Some medicines used to treat fungal infections including Ketoconazole and Itraconazole may reduce the clearance of Sildenafil.
Pregnancy & lactationView
Pregnancy category B. There are no adequate and well-controlled studies of Sildenafil in pregnant women. Sildenafil is not indicated for use by women. In animal study shows that Sildenafil has no evidence of teratogenicity or embryotoxicity.
StorageView
Keep in a dry place, away from light and heat. Keep out of the reach of children.
Immuna
Spirulina
Immuna
Spirulina
Indications
Runny nose
Indication detailsView
Spirulina is used for the treatment and prevention of malnutrition, diabetes, arthritis, asthma, hyperglycemia, anemia, allergic rhinitis and to enhance immunity. Spirulina helps to maintain healthy eyes and skin.
Therapeutic classView
Herbal and Nutraceuticals
PharmacologyView
Spirulina has such positive TTutritionafcontent that it is called the world's richest whole-food which can be found naturally. It is very high in protein with low calorie content (only coming in at 2.9 calories per gram) using this as a supplement for protein specifically this is less than % the amount of calories in protein per gram, Spirulina is the highest source of B-12, essential for healthy nerves and tissue, especially for vegetarians. Due to large amount of iron in spirulina, it helps to promote the creation of new red blood cells too. Not only does spirulina contain high protein content within it, but it also has nutrients in it which increase the body's ability to absorb protein, This means that it even makes any other protein being consumed by the person more effective than if they had just consumed the protein alone. ln this way, spirulina may even be a better source of protein than most meal. Spirulina contains a concentration of very single amino acid as well. These are amino acids that the body cannot survive without, but we cannot produce ourselves which means we have to get them through other dietary means. Spirulina contains approximately 100 nutrients and minerals. Furthermore it has fatty acids that help reduce bad cholesterol in our body and antioxidants that help strengthen our immune system, fight free radicals and slow down the aging process. It is recommended to people whose intake of nutritious food is anadequate.
How does it work-
How does it work-
- About 60% of spirulina dry weight is protein which is essential for growth and cell regeneration. Besides this it had sufficient vitamins and minerals within, With its high digestibility, spirulina has proven to fight malnutrition in impoverished communities by helping the body absorb nutrients when it has lost its ability to absorb normal forms of food.
- Every 10 grams of spirulina can supply up to 70% of the minimum daily requirements for iron. Being rich in iron, magnesium and trace minerals spirulina is easier to absorb than iron supplements to fight anemia effectively.
- Spirulina is rich in gamma-linolenic acid or GLA, a compound found in breast milk that helps develop healthier babies.
- Another health benefit of spirulina is that it stimulates beneficial flora like lactobacillus and bifidobacterial in our digestive tract to promote healthy digestion and proper bowel function. It acts as a natural cleanser by eliminating mercury and other deadly toxins commonly ingested by the body.
DosageView
2 to 4 capsules daily or as advised by the physician.
Side effectsView
Spirulina is generally well tolerated. Occasional diarrhea, gastrointestinal discomfort, such as nausea have been reported. Also there are few reports of allergic reactions to spirulina containing supplements.
ContraindicationsView
Spirulina is contraindicated in those who are hypersensitive to any component of this product.
PrecautionsView
Before taking spirulina pregnant or breast-feeding women should talk to the physician.
InteractionsView
There are no reports suggesting that spirulina interacts with any conventional medication.
Pregnancy & lactationView
Before taking spirulina pregnant or breast-feeding women should talk to the physician.
StorageView
Store in a cool and dry place. Keep away from direct sunlight. Keep out of reach of the children.
Imnoc
Imipramine Hydrochloride
Imnoc
Imipramine Hydrochloride
Indications
Urinary incontinence
Indication detailsView
Imipramine Hydrochloride is indicated in-
- Depressive illness
- Nocturnal enuresis in children.
Therapeutic classView
Tricyclic & related anti-depressant drugs, Tricyclic Anti-depressant
PharmacologyView
Imipramine works by inhibiting the neuronal reuptake of the neurotransmitters norepinephrine and serotonin. It binds the sodium-dependent serotonin transporter and sodium-dependent norepinephrine transporter reducing the reuptake of norepinephrine and serotonin by neurons. Depression has been linked to a lack of stimulation of the post-synaptic neuron by norepinephrine and serotonin. Slowing the reuptake of these neurotransmitters increases their concentration in the synaptic cleft, producing knock-on effects in protein kinase signaling which is thought to contribute to changes in neurotransmission and brain physiology which relieves symptoms of depression.
DosageView
Depression:
- Initially up to 75 mg daily in divided doses increased gradually to 150-200 mg (up to 300 mg in hospital patients)
- Up to 150 mg may be given as a single dose at bedtime
- Elderly initially 10 mg daily, increased gradually to 30-50 mg daily
- Child not recommended for depression
- Child 7-8 years: 25 mg
- 8-11 years: 25-50 mg
- Over 11 years: 50-75 mg at bedtime; max
Side effectsView
The most frequent of side effects are dry mouth, constipation, urinary retention, increased heart rate, sedation, irritability, dizziness, and decreased coordination. Dry mouth, if severe to the point of causing difficulty speaking or swallowing, may be managed by dosage reduction or temporary discontinuation of the drug. Imipramine usage has been linked to both increases and decreases in blood pressure and heart rate. Heart attacks, congestive heart failure, and strokes have been reported. Confusion, disorientation, delusions, insomnia, and anxiety have also been reported as side effects in a small percentage of people taking imipramine. Problems associated with the skin (loss of sensation, numbness and tingling, rashes, spots, itching and puffiness), seizures, and ringing in the ears have also been reported. Nausea, vomiting, loss of appetite, diarrhea, and abdominal cramping are all side effects associated with imipramine usage in a small number of people.
ContraindicationsView
Imipramine should not be given in conjunction with, or within 14 days of treatment with a MAO inhibitor. The combined therapy of this type could lead to the appearance of serious interactions such as hypertensive crises, hyperactivity, hyperpyrexia, spasticity, severe convulsions or coma and death may occur. Imipramine is contraindicated in patients with existing severe hepatic or renal damage, and those with a history of blood dyscrasias. Imipramine is contraindicated in patients who have shown hypersensitivity to the drug or hypersensitivity to tricyclic antidepressants belonging to the dibenzazepine group. Imipramine is contraindicated for use during the acute recovery phase following myocardial infarction. It should not be used in patients with convulsive disorders or glaucoma.
PrecautionsView
Imipramine should be used cautiously and with close physician supervision in people, especially the elderly, who have benign prostatic hypertrophy, urinary retention, and glaucoma, especially angle-closure glaucoma. The sedative effect is increased when imipramine is taken with other central nervous system depressants, such as alcoholic beverages, sleeping medications, other sedatives, or antihistamines. Imipramine may increase heart rate and stress on the heart. It may be dangerous for people with cardiovascular disease, especially those who have recently had a heart attack, to take this drug or other antidepressants in the same pharmacological class. Older people and persons with a history of heart disease may develop heart arrhythmias, heart conduction abnormalities, congestive heart failure, heart attack, abnormally rapid heart rates and strokes. Until a therapeutic dosage has been determined, people starting imipramine should be closely watched for signs of suicide. The risk of suicide is increased when imipramine is taken in overdose or combined with alcohol. Manic episodes and the emergence of symptoms of pre-existing psychotic states have been reported when imipramine therapy is started.
InteractionsView
Methylphenidate may increase the effects of imipramine. This is usually avoided by reducing the dosage of imipramine. Imipramine may increase the depressant action of alcohol. Dangerously high blood pressure has resulted from the combination of imipramine, and members of monoamine oxidase (MAO) inhibitors. Because of this, imipramine should never be taken in combination with MAO inhibitors. Patients taking any MAO inhibitors, for example phenelzine sulfate or tranylcypromine sulfate, should stop the MAO inhibitor then wait at least 14 days before starting imipramine or any other tricyclic antidepressant. The same holds true when discontinuing imipramine and starting an MAO inhibitor. The anticholinergic (drying out) effects of imipramine are additive with other anticholinergic drugs such as benztropine, biperiden, trihexyphenidyl, and antihistamines.
Pregnancy & lactationView
Pregnancy category D. Limited data suggest that imipramine is likely to be excreted in human breast milk. Known risk of damage to fetus.
Overdose effectsView
Children have been reported to be more sensitive than adults to an acute overdosage of imipramine. An acute overdose in infants or young children must be considered serious and potentially fatal.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Imojev
Encephalitis Vaccine
Imojev
Encephalitis Vaccine
Indications
Encephalitis virus vaccine
Indication detailsView
Encephalitis Vaccine is indicated for active immunisation against Japanese encephalitis in adults, adolescents, children and infants aged 2 months and older. Encephalitis Vaccine should be considered for use in individuals at risk of exposure through travel or in the course of their occupation.
Therapeutic classView
Vaccines, Anti-sera & Immunoglobulin
PharmacologyView
The mechanism of action of Japanese encephalitis (JE) vaccines is not well understood. Studies in animals have shown that the vaccine triggers the immune system to produce antibodies against Japanese encephalitis virus that are most often protective. Challenge studies were performed in mice that were treated with human Encephalitis Vaccine antisera. These studies showed that almost all mice that had a Plaque Reduction Neutralization Test titre of at least 1:10 were protected from a lethal Japanese encephalitis virus challenge.
DosageView
Adults (18 to ≤ 65 years of age): The primary vaccination series consists of two separate doses of 0.5 ml each, according to the following conventional schedule:
Booster dose: A booster dose (third dose) should be given within the second year (i.e. 12-24 months) after primary immunization, prior to potential re-exposure to JEV. Persons at continuous risk for acquiring Japanese encephalitis (laboratory personnel or persons residing in endemic areas) should receive a booster dose at month 12 after primary immunization. Long-term seroprotection data following a first booster dose administered 12-24 months after primary immunization suggest that a second booster should be given 10 years after the first booster dose, prior to potential exposure to JEV.
Elderly (>65 years of age): The primary vaccination series consists of two separate doses of 0.5 ml each, according to the following conventional schedule:
Children and adolescents from 3 years to <18 years of age: The primary vaccination series consists of two separate doses of 0.5 ml according to the following schedule:
- First dose: Day 0.
- Second dose: 28 days after first dose.
- First dose: Day 0.
- Second dose: 7 days after first dose.
Booster dose: A booster dose (third dose) should be given within the second year (i.e. 12-24 months) after primary immunization, prior to potential re-exposure to JEV. Persons at continuous risk for acquiring Japanese encephalitis (laboratory personnel or persons residing in endemic areas) should receive a booster dose at month 12 after primary immunization. Long-term seroprotection data following a first booster dose administered 12-24 months after primary immunization suggest that a second booster should be given 10 years after the first booster dose, prior to potential exposure to JEV.
Elderly (>65 years of age): The primary vaccination series consists of two separate doses of 0.5 ml each, according to the following conventional schedule:
- First dose: Day 0.
- Second dose: 28 days after first dose.
Children and adolescents from 3 years to <18 years of age: The primary vaccination series consists of two separate doses of 0.5 ml according to the following schedule:
- First dose: Day 0.
- Second dose: 28 days after first dose.
- First dose: Day 0.
- Second dose: 28 days after first dose.
AdministrationView
The vaccine should be administered by intramuscular injection into the deltoid muscle. In infants, the anterolateral aspect of the thigh may be used as injection site. Encephalitis Vaccine should never be injected intravascularly. When Encephalitis Vaccine is administered concomitantly with injectable vaccines, they should be given with separate syringes at opposite sites. Exceptionally, Encephalitis Vaccine can also be administered subcutaneously to patients with thrombocytopenia or bleeding disorders since bleeding may occur following an intramuscular administration. Subcutaneous administration could lead to a suboptimal response to the vaccine. However, it should be noted that there are no clinical efficacy data to support administration by the subcutaneous route.
Side effectsView
Very common: headache, muscle pain, injection site pain, injection site tenderness, tiredness.
Common: Nausea, influenza like illness, fever, other injection site reactions (e.g. redness, hardening, swelling, itching).
Uncommon: vomiting, skin rash, changes in the lymph-nodes, migraine (throbbing headache, often accompanied by nausea and vomiting and sensitivity to light), dizziness, vertigo (spinning sensation), diarrhoea, belly pain, excessive sweating, itching, chills, general condition of feeling unwell, musculoskeletal stiffness, joint pain, weakness, abnormal laboratory liver test results (hepatic enzymes increased).
Common: Nausea, influenza like illness, fever, other injection site reactions (e.g. redness, hardening, swelling, itching).
Uncommon: vomiting, skin rash, changes in the lymph-nodes, migraine (throbbing headache, often accompanied by nausea and vomiting and sensitivity to light), dizziness, vertigo (spinning sensation), diarrhoea, belly pain, excessive sweating, itching, chills, general condition of feeling unwell, musculoskeletal stiffness, joint pain, weakness, abnormal laboratory liver test results (hepatic enzymes increased).
ContraindicationsView
Hypersensitivity to the active substance or to any of the excipients or to the residues protamine sulphate, formaldehyde, bovine serum albumin, host cell DNA, sodium metabisulphite, host cell protein. Individuals who show hypersensitivity reactions after receiving the first dose of the vaccine should not be given the second dose. Administration must be postponed in persons with acute severe febrile conditions.
Pregnancy & lactationView
Pregnancy: There are limited amount of data from the use of Encephalitis Vaccine in pregnant women. In animal studies findings of unclear clinical relevance have been identified. As a precautionary measure, the use of Encephalitis Vaccine during pregnancy should be avoided.
Breast-feeding: It is unknown whether Encephalitis Vaccine is excreted in human milk. No effects on the breastfed newborn/infant are anticipated since the systemic exposure of the breast-feeding woman to Encephalitis Vaccine is negligible. However, in the absence of data and as a precautionary measure the use of Encephalitis Vaccine during lactation should be avoided.
Fertility: A study in rats did not indicate vaccine-related effects on female reproduction, foetal weight, survival and development of the off-spring.
Breast-feeding: It is unknown whether Encephalitis Vaccine is excreted in human milk. No effects on the breastfed newborn/infant are anticipated since the systemic exposure of the breast-feeding woman to Encephalitis Vaccine is negligible. However, in the absence of data and as a precautionary measure the use of Encephalitis Vaccine during lactation should be avoided.
Fertility: A study in rats did not indicate vaccine-related effects on female reproduction, foetal weight, survival and development of the off-spring.
Pediatric usageView
Children below 2 months of age: The safety and efficacy of Encephalitis Vaccine in children younger than 2 months has not been established. No data are available.
StorageView
Store in a refrigerator (2°C-8°C). Do not freeze. Store in the original package in order to protect from light.
Imotil
Loperamide Hydrochloride
Imotil
Loperamide Hydrochloride
Indications
Ulcerative colitis
Indication detailsView
Loperamide Hydrochloride is indicated in-
- Acute diarrhea
- Chronic diarrhea
- Abdominal cramps associated with diarrhea
- Crohn's disease
- Postgastric surgery
- Ulcerative colitis.
Therapeutic classView
Anti-diarrhoeal, Anti-motility drugs
PharmacologyView
Loperamide Hydrochloride inhibits the peristaltic activity of the longitudinal and circular smooth muscle in the intestine by interacting with cholinergic and noncholinergic neuronal mechanisms responsible for producing the peristaltic reflex. Loperamide Hydrochloride binds to the opiate receptor in the gut wall, reducing propulsive peristalsis and increasing intestinal transit time. Loperamide Hydrochloride increases the tone of the anal sphincter. This also inhibits electrolyte and fluid secretion in the intestine.
Loperamide Hydrochloride is an orally administered capsule. After administration absorption is more than 65% which occurs at a modest rate, with peak serum levels of 2-3 µgm/litre occurring at about 4 hours later after oral administration. The rest 35% is excreted unchanged in the faeces. Loperamide Hydrochloride undergoes an extensive presystemic first-pass metabolism in the gut wall and in the liver. Loperamide does not act centrally due to its high affinity for the gut wall and its presystemic metabolism. This is why it reaches the systemic circulation in a very minute amount. The route of elimination is 0.63-1.4% in urine as an unchanged drug, 58% is excreted in the bile and 15-23% appears in the faeces.
Loperamide Hydrochloride is an orally administered capsule. After administration absorption is more than 65% which occurs at a modest rate, with peak serum levels of 2-3 µgm/litre occurring at about 4 hours later after oral administration. The rest 35% is excreted unchanged in the faeces. Loperamide Hydrochloride undergoes an extensive presystemic first-pass metabolism in the gut wall and in the liver. Loperamide does not act centrally due to its high affinity for the gut wall and its presystemic metabolism. This is why it reaches the systemic circulation in a very minute amount. The route of elimination is 0.63-1.4% in urine as an unchanged drug, 58% is excreted in the bile and 15-23% appears in the faeces.
DosageView
Acute diarrhea-
- Adults: 2 capsules initially followed by 1 capsule after every loose stool.
- Usual dosage: 3-4 capsules/day. The maximum daily dose should not exceed 8 capsules.
- Children (9-12 years): 1 capsule after each loose stool until diarrhea is controlled. But not more than 6 capsules daily.
- Children (5-9 years): 1 capsule 4 times daily until diarrhea is controlled. But not more than 4 capsules daily.
- Adults: 2-4 capsules daily in divided doses, depending on severity.
- Children: 1-2 capsules daily, depending on severity. Or directed by physician.
Side effectsView
Abdominal pain and other gastrointestinal disturbances including dry mouth, dizziness, fatigue and skin rashes etc. have been reported.
ContraindicationsView
Hypersensitivity to the drug and in patients who must avoid constipation. Loperamide Hydrochloride should not be used alone in acute dysentery, which is characterized by blood in the stool and elevated body temperature.
PrecautionsView
Loperamide Hydrochloride must be used with caution in cases of severe hepatic disturbance.
InteractionsView
There are no data available.
Pregnancy & lactationView
Safety in human pregnancy has not been established. As with other drugs, it is not advisable to administer Loperamide in pregnancy. Although the fraction of Loperamide Hydrochloride secreted in human breast milk is extremely low, caution is advised if Loperamide Hydrochloride is to be administered to a nursing mother.
Overdose effectsView
Overdosage of Loperamide may result in constipation, CNS depression, and nausea.
StorageView
Keep all medicines out of reach of children. Store in a cool and dry place protected from light.
Imovane
Zopiclone
Imovane
Zopiclone
Indications
Insomnia and sleep disturbances
Indication detailsView
Zopiclone is indicated for the short-term treatment and symptomatic relief of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings and/or early morning awakenings.
Therapeutic classView
Miscellaneous sedatives & hypnotics
PharmacologyView
Zopiclone, a cyclopyrrolone derivative, is a short-acting hypnotic agent. This is structurally unrelated to existing hypnotics. However, the pharmacological profile of Zopiclone is similar to that of the benzodiazepines. Zopiclone pharmacological properties are: hypnotic, sedative, anxiolytic, anti-convulsant, muscle-relaxant. These effects are related to a specific agonist action at central receptors belonging to the GABAA macromolecular complex, modulating the opening of the chloride ion channel.
DosageView
The recommended initial dose is 3.75 mg (one-half of a 7.5 mg tablet). The dose can be increased to 5 mg and further to 7.5 mg if clinically indicated. In some patients, the higher doses result in zopiclone blood levels in the morning high enough to produce impairment of driving and other activities that require full alertness. The 7.5 mg dose should not be exceeded.
AdministrationView
Treatment with Zopiclone should usually not exceed 7-10 consecutive days. Use for more than 2-3 consecutive weeks requires complete re-evaluation of the patient. Prescriptions for Zopiclone should be written for short-term use (7-10 days) and it should not be prescribed in quantities exceeding a 1-month supply. The use of hypnotics should be restricted for insomnia where disturbed sleep results in impaired daytime functioning.
Side effectsView
Common side effects are somnolence, dizziness, confusion, anterograde amnesia or memory impairment, feeling of drunkenness, euphoria, nightmares, agitation, anxiety or nervousness, hostility, depression, decreased libido, libido disorder, coordination abnormality, headache, hypotonia, tremor, muscle spasms, paresthesia, and speech disorder, palpitations, dysgeusia (bitter taste), dry mouth, coated tongue, bad breath, nausea, vomiting, diarrhea, constipation, anorexia or increased appetite.
ContraindicationsView
Zopiclone is contraindicated in patients with severe hepatic insufficiency, contraindicated in patients with severe impairment of respiratory function.
PrecautionsView
- Do not take more Zopiclone than prescribed.
- Do not use for longer than recommended by your physician. Treatment should be as short as possible, because the risk of dependence increases with the duration of treatment.
- Do not take Zopiclone if you drink alcohol.
- Talk to your doctor if you have had episodes of sleepwalking in the past, or if there is a history of sleepwalking in your family.
- Talk to your doctor if you have a condition that affects your sleep, such as Periodic Limb Movement Disorder (involuntary movement of limbs during sleep) or Restless Legs Syndrome (urge to move legs, usually accompanied by uncomfortable and unpleasant sensations, that begins or worsens during periods of inactivity, typically in the evening and night).
InteractionsView
Zopiclone may produce more pronounced side effects when co- administered with:
- Alcohol
- Other tranquilizers or sleeping pills
- Sedative antihistamines
- Anticonvulsants (medicines used to control or prevent convulsions)
- Narcotic analgesics (opioids)
- Antipsychotics, antidepressants and other psychotropic medications (mood altering drugs) which themselves can make you sleepy.
Pregnancy & lactationView
Do no take Zopiclone at anytime during pregnancy, it may affect the developing baby. Zopiclone passes into breast milk. Therefore, if you are breast feeding, this medicine should be avoided. Your doctor will discuss this with you
Pediatric usageView
Zopiclone is not indicated for patients under 18 years of age.
Overdose effectsView
Overdose is usually manifested by varying degrees of central nervous system depression ranging from drowsiness to coma according to the quantity ingested. In mild cases, symptoms include drowsiness, confusion, and lethargy; in more severe cases, symptoms may include ataxia, hypotonia, hypotension, methaemoglobinaemia, respiratory depression, and coma. Overdose should not be life threatening unless combined with other CNS depressants, including alcohol. Other risk factors, such as the presence of concomitant illness and the debilitated state of the patient, may contribute to the severity of symptoms and very rarely can result in fatal outcome. Symptomatic and supportive treatment in adequate clinical environment is recommended, attention should be paid to respiratory and cardiovascular functions. Gastric lavage or activated charcoal is only useful when performed soon after ingestion.
StorageView
Store in a dry place, at room temperature (15°C to 30°C). Protect from light. Keep in a safe place out of reach of children.
Imped
Amlodipine Besilate
Imped
Amlodipine Besilate
Indications
Stroke
Indication detailsView
Essential hypertension: Amlodipine is efficacious as monotherapy in the treatment of hypertension. It may be used in combination with other antihypertensive agents.
Angina pectoris: Amlodipine is indicated for the treatment of chronic stable angina pectoris and is efficacious as monotherapy. It may be used in combination with other antianginal agents.
Vasospastic angina: Amlodipine is indicated for the treatment of confirmed or suspected vasospastic angina. It may be used as monotherapy or in combination with other antianginal drugs.
Angina pectoris: Amlodipine is indicated for the treatment of chronic stable angina pectoris and is efficacious as monotherapy. It may be used in combination with other antianginal agents.
Vasospastic angina: Amlodipine is indicated for the treatment of confirmed or suspected vasospastic angina. It may be used as monotherapy or in combination with other antianginal drugs.
Therapeutic classView
Calcium-channel blockers
PharmacologyView
Amlodipine is a dihydropyridine calcium-channel blocker, with a long duration of action, used for the treatment of hypertension and angina pectoris. Amlodipine influences the myocardial cells, the cells within the specialized conducting system of the heart, and the cells of vascular smooth muscle. Administration of Amlodipine results primarily in vasodilation, with reduced peripheral resistance, blood pressure and afterload, increased coronary blood flow and a reflex increase in coronary heart rate. This in turn results in an increase in myocardial oxygen supply and cardiac output.
DosageView
Hypertension: Usual dose is 5 mg once daily. The maximum dose is 10 mg once daily. Elderly patients with hepatic insufficiency may be started on 2.5 mg once daily; this dose may also be used when adding Amlodipine to other antihypertensive therapy.
Angina (Chronic stable or Vasospastic): 5 to 10 mg, using the lower dose for elderly and in patients with hepatic insufficiency. Most patients require 10 mg.
Administrations: May be taken without regard to meals.
Angina (Chronic stable or Vasospastic): 5 to 10 mg, using the lower dose for elderly and in patients with hepatic insufficiency. Most patients require 10 mg.
Administrations: May be taken without regard to meals.
Side effectsView
The most common adverse effects of amlodipine are associated with vasodilatory action, such as dizziness, flushing, headache, hypotension and peripheral edema. Gastrointestinal disturbances, increased micturition frequency, lethargy, eye pain and mental depression may also occur. A paradoxical increase in ischaemic chest pain may occur at the start of the treatment and in a few patients excessive fall in blood pressure has led to cerebral or myocardial ischaemia or transient blindness. Rashes, fever and abnormalities in liver function due to hypersensitivity reaction of Amlodipine may occur.
ContraindicationsView
Hypersensitivity to dihydropyridine derivatives. Pregnant woman.
PrecautionsView
Precaution should be taken in patients with hepatic impairment and during pregnancy and breast feeding.
InteractionsView
Drug Interactions-
- Potentially hazardous interactions: Little or no data are available in patients with markedly impaired cardiac left ventricular function; however, as with other calcium antagonist drugs, the combination of Amlodipine and p-blockers should be avoided in such patients.
- Digoxin: Absence of any interaction between Amlodipine and Digoxin in healthy volunteers has been documented in a controlled clinical study.
- Cimetidine: An unpublished clinical study indicated no interaction between, Amlodipine and Cimetidine in healthy volunteers.
- Warfarin: An unpublished clinical study in healthy volunteers indicates that Amlodipine did not significantly alter the effect of Warfarin on prothrombin time.
- Food: Food does not alter the rate or extent of absorption of Amlodipine.
Pregnancy & lactationView
Pregnancy Category C. There are no adequate and well-controlled studies of Amlodipine in pregnant women. Amlodipine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether Amlodipine is excreted in human milk. In the absence of this information, it is recommended that nursing be discontinued while Amlodipine is administered.
Pediatric usageView
Children with hypertension from 6 years to 17 years of age: 2.5 mg once daily as a starting dose, up-titrated to 5 mg once daily if blood pressure goal is not achieved after 4 weeks. Doses in excess of 5 mg daily have not been studied in pediatric patients.
Children under 6 years old: The effect of amlodipine on blood pressure in patients less than 6 years of age is not known.
Elderly: Amlodipine used at similar doses in elderly or younger patients is equally well tolerated. Normal dosage regimens are recommended in the elderly, but increase of the dosage should take place with care.
Renal impairment: Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment, therefore the normal dosage is recommended. Amlodipine is not dialysable.
Hepatic impairment: Dosage recommendations have not been established in patients with mild to moderate hepatic impairment; therefore dose selection should be cautions and should start at the lower end of the dosing range. The pharmacokinetics of Amlodipine have not been studied in severe hepatic impairment. Amlodipine should be initiated at the lowest dose (2.5 mg once daily) and titrated slowly in patients with severe hepatic impairment.
Children under 6 years old: The effect of amlodipine on blood pressure in patients less than 6 years of age is not known.
Elderly: Amlodipine used at similar doses in elderly or younger patients is equally well tolerated. Normal dosage regimens are recommended in the elderly, but increase of the dosage should take place with care.
Renal impairment: Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment, therefore the normal dosage is recommended. Amlodipine is not dialysable.
Hepatic impairment: Dosage recommendations have not been established in patients with mild to moderate hepatic impairment; therefore dose selection should be cautions and should start at the lower end of the dosing range. The pharmacokinetics of Amlodipine have not been studied in severe hepatic impairment. Amlodipine should be initiated at the lowest dose (2.5 mg once daily) and titrated slowly in patients with severe hepatic impairment.
Overdose effectsView
Symptoms: Available data suggest that large overdosage could result in excessive peripheral vasodilatation and possibly reflex tachycardia. Marked and probably prolonged systemic hypotension up to and including shock with fatal outcome have been reported.
Management: Clinically significant hypotension due to amlodipine overdosage calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities, and attention to circulating fluid volume and urine output.
A vasoconstrictor may be helpful in restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockade. Gastric lavage may be worthwhile in some cases. In healthy volunteers the use of charcoal up to 2 hours after administration of amlodipine 10 mg has been shown to reduce the absorption rate of amlodipine. Since amlodipine is highly protein-bound, dialysis is not likely to be of benefit.
Management: Clinically significant hypotension due to amlodipine overdosage calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities, and attention to circulating fluid volume and urine output.
A vasoconstrictor may be helpful in restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockade. Gastric lavage may be worthwhile in some cases. In healthy volunteers the use of charcoal up to 2 hours after administration of amlodipine 10 mg has been shown to reduce the absorption rate of amlodipine. Since amlodipine is highly protein-bound, dialysis is not likely to be of benefit.
StorageView
Keep all medicines out of reach of children. Store in a cool & dry place, protected from light.
Imped Plus
Amlodipine Besilate + Atenolol
Imped Plus
Amlodipine Besilate + Atenolol
Indications
Refractory angina pectoris where nitrate therapy has failed
Indication detailsView
This is indicated in-
- Patients with essential hypertension
- Patients with angina pectoris & hypertension as co-existing diseases
- ln post Ml patients
- ln patients with refractory angina pectoris where nitrate therapy has failed.
Therapeutic classView
Combined antihypertensive preparations
PharmacologyView
This is a fixed-dose combination of Amlodipine and Atenolol. Amlodipine is a dihydropyridine calcium antagonist that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle; it has a greater effect on vascular smooth muscle than on cardiac muscle. Amlodipine is a peripheral vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. Amlodipine reduces tone, decreases coronary vasoreactivity and lowers cardiac demand by reducing afterload.
Atenolol is a cardioselective beta-blocker. The cardio-selectivity is dose-related. Atenolol causes a reduction in blood pressure by lowering cardiac output, decreasing the plasma renin activity and sympathetic outflow from CNS. Atenolol also causes a reduction in myocardial oxygen demand by virtue of its negative inotropic and negative chronotropic effects.
Atenolol is a cardioselective beta-blocker. The cardio-selectivity is dose-related. Atenolol causes a reduction in blood pressure by lowering cardiac output, decreasing the plasma renin activity and sympathetic outflow from CNS. Atenolol also causes a reduction in myocardial oxygen demand by virtue of its negative inotropic and negative chronotropic effects.
DosageView
The recommended dosage is Amlodipine and Atenolol 5/25 mg tablet once daily. If necessary, the dosage may be increased to 5/25 mg two tablets daily or as advised by the physicians. The dosage however should be individualized.
Side effectsView
The combination of Amlodipine and Atenolol is well tolerated. Overall side-effects include
fatigue, headache, edema, nausea, drowsiness, anxiety and depression.
fatigue, headache, edema, nausea, drowsiness, anxiety and depression.
ContraindicationsView
Hypersensitivity to either component, sinus bradycardia, second and higher degrees of heart block, cardiogenic shock, hypotension, congestive heart failure, poor left ventricular function.
PrecautionsView
Bronchospasm: The combination should be used with caution in patients with airway obstruction.
Renal impairment: The combination can be used in patients with renal impairment. However, caution may be necessary if the creatinine clearance is less than 30 ml/min because of possible reduction in the excretion of unchanged Atenolol.
Hepatic impairment: Caution may be necessary in the use of the combination in patients with severe liver damage because of prolongation of the elimination half-life of Amlodipine.
Drug withdrawal: Since coronary heart disease may exist without being recognized, patients should be warned against stopping the drug suddenly. Any discontinuation should be gradual and under observation.
Renal impairment: The combination can be used in patients with renal impairment. However, caution may be necessary if the creatinine clearance is less than 30 ml/min because of possible reduction in the excretion of unchanged Atenolol.
Hepatic impairment: Caution may be necessary in the use of the combination in patients with severe liver damage because of prolongation of the elimination half-life of Amlodipine.
Drug withdrawal: Since coronary heart disease may exist without being recognized, patients should be warned against stopping the drug suddenly. Any discontinuation should be gradual and under observation.
InteractionsView
Disopyramide: Atenolol reduces the clearance of disopyramide by 20%. Additive negative inotropic effects on the heart may be produced.
Ampicillin: at doses of 1 gm and above may reduce Atenolol levels.
Oral antidiabetics and insulin: Beta-blockers may decrease tissue sensitivity to insulin and inhibit insulin secretion e.g. in response to oral antidiabetics. Atenolol has less potential for these actions.
Ampicillin: at doses of 1 gm and above may reduce Atenolol levels.
Oral antidiabetics and insulin: Beta-blockers may decrease tissue sensitivity to insulin and inhibit insulin secretion e.g. in response to oral antidiabetics. Atenolol has less potential for these actions.
Pregnancy & lactationView
The combination should be used during pregnancy only if the expected benefit outweighs the potential fetal risk. The combination should not be used by nursing mothers. If its use is considered necessary, breast-feeding should be stopped.
Overdose effectsView
Though not documented, hypotension and less frequently congestive cardiac failure may occur in cases of overdosage. Unabsorbed drugs may be removed by gastric lavage or administration of activated charcoal. Symptomatic treatment is suggested.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Imped Plus
Amlodipine Besilate + Atenolol
Imped Plus
Amlodipine Besilate + Atenolol
Indications
Refractory angina pectoris where nitrate therapy has failed
Indication detailsView
This is indicated in-
- Patients with essential hypertension
- Patients with angina pectoris & hypertension as co-existing diseases
- ln post Ml patients
- ln patients with refractory angina pectoris where nitrate therapy has failed.
Therapeutic classView
Combined antihypertensive preparations
PharmacologyView
This is a fixed-dose combination of Amlodipine and Atenolol. Amlodipine is a dihydropyridine calcium antagonist that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle; it has a greater effect on vascular smooth muscle than on cardiac muscle. Amlodipine is a peripheral vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. Amlodipine reduces tone, decreases coronary vasoreactivity and lowers cardiac demand by reducing afterload.
Atenolol is a cardioselective beta-blocker. The cardio-selectivity is dose-related. Atenolol causes a reduction in blood pressure by lowering cardiac output, decreasing the plasma renin activity and sympathetic outflow from CNS. Atenolol also causes a reduction in myocardial oxygen demand by virtue of its negative inotropic and negative chronotropic effects.
Atenolol is a cardioselective beta-blocker. The cardio-selectivity is dose-related. Atenolol causes a reduction in blood pressure by lowering cardiac output, decreasing the plasma renin activity and sympathetic outflow from CNS. Atenolol also causes a reduction in myocardial oxygen demand by virtue of its negative inotropic and negative chronotropic effects.
DosageView
The recommended dosage is Amlodipine and Atenolol 5/25 mg tablet once daily. If necessary, the dosage may be increased to 5/25 mg two tablets daily or as advised by the physicians. The dosage however should be individualized.
Side effectsView
The combination of Amlodipine and Atenolol is well tolerated. Overall side-effects include
fatigue, headache, edema, nausea, drowsiness, anxiety and depression.
fatigue, headache, edema, nausea, drowsiness, anxiety and depression.
ContraindicationsView
Hypersensitivity to either component, sinus bradycardia, second and higher degrees of heart block, cardiogenic shock, hypotension, congestive heart failure, poor left ventricular function.
PrecautionsView
Bronchospasm: The combination should be used with caution in patients with airway obstruction.
Renal impairment: The combination can be used in patients with renal impairment. However, caution may be necessary if the creatinine clearance is less than 30 ml/min because of possible reduction in the excretion of unchanged Atenolol.
Hepatic impairment: Caution may be necessary in the use of the combination in patients with severe liver damage because of prolongation of the elimination half-life of Amlodipine.
Drug withdrawal: Since coronary heart disease may exist without being recognized, patients should be warned against stopping the drug suddenly. Any discontinuation should be gradual and under observation.
Renal impairment: The combination can be used in patients with renal impairment. However, caution may be necessary if the creatinine clearance is less than 30 ml/min because of possible reduction in the excretion of unchanged Atenolol.
Hepatic impairment: Caution may be necessary in the use of the combination in patients with severe liver damage because of prolongation of the elimination half-life of Amlodipine.
Drug withdrawal: Since coronary heart disease may exist without being recognized, patients should be warned against stopping the drug suddenly. Any discontinuation should be gradual and under observation.
InteractionsView
Disopyramide: Atenolol reduces the clearance of disopyramide by 20%. Additive negative inotropic effects on the heart may be produced.
Ampicillin: at doses of 1 gm and above may reduce Atenolol levels.
Oral antidiabetics and insulin: Beta-blockers may decrease tissue sensitivity to insulin and inhibit insulin secretion e.g. in response to oral antidiabetics. Atenolol has less potential for these actions.
Ampicillin: at doses of 1 gm and above may reduce Atenolol levels.
Oral antidiabetics and insulin: Beta-blockers may decrease tissue sensitivity to insulin and inhibit insulin secretion e.g. in response to oral antidiabetics. Atenolol has less potential for these actions.
Pregnancy & lactationView
The combination should be used during pregnancy only if the expected benefit outweighs the potential fetal risk. The combination should not be used by nursing mothers. If its use is considered necessary, breast-feeding should be stopped.
Overdose effectsView
Though not documented, hypotension and less frequently congestive cardiac failure may occur in cases of overdosage. Unabsorbed drugs may be removed by gastric lavage or administration of activated charcoal. Symptomatic treatment is suggested.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Impedox
Doxycycline Hydrochloride
Impedox
Doxycycline Hydrochloride
Indications
Uncomplicated gonorrhoea
Indication detailsView
Doxycycline Hydrochloride is indicated in the following infections caused by susceptible microorganisms:
- Respiratory tract infections: Pneumonia, influenza, sinusitis, bronchitis, tonsillitis, tracheitis.
- Gastrointestinal tract infections: Cholera, traveler's diarrhea, shigella dysentery, acute intestinal amebiasis.
- Chlamydial infections: Lympho-granuloma venereum, psittacosis, trachoma.
- Sexually transmitted diseases: Non gonococcal urethritis, acute pelvic inflammatory disease, uncomplicated urethral and endocervical or rectal infections, gonorrhoea, syphilis, pyelonephritis, cystitis.
- Other infections: Impetigo, furunculosis, inclusion conjunctivitis, brucellosis, tularemia, cellulitis, acne and Q-fever.
Therapeutic classView
Tetracycline group of drugs
PharmacologyView
Doxycycline Hydrochloride is a semisynthetic tetracycline antibiotic with broad spectrum activity. It is primarily a bacteriostatic antibiotic. It has a similar spectrum of activity to other tetracyclines but in particular is more active against Staphylococcus aureus and Nocardia. The drug is often active against penicillin-resistant strains of Staphylococcus aureus and against strains of those organisms that are resistant to other Tetracyclines. Certain Gram-negative strains of E. coli, Proteus mirabilis and Klebsiella, which are often resistant to Tetracycline, may be sensitive to Doxycycline. In addition, 70-90% of the various anaerobes are sensitive to Doxycycline and Bacteroides fragilis is more likely to be sensitive to Doxycycline than to other tetracyclines.
Doxycycline is active against most strains of Haemophilus influenzaeand is particularly useful for infections with H. ducreyi, Actinomyces, Brucella and Vibrio cholerae. It is also active against Nocardia, Chlamydia, Mycoplasma and a wide range of Rickettsiae. Doxycycline is active against spirochetes such as Borellia recurrentis, Treponema pallidum and Treponema pertenue. It is also active against Plasmodium falciparum.
Doxycycline is active against most strains of Haemophilus influenzaeand is particularly useful for infections with H. ducreyi, Actinomyces, Brucella and Vibrio cholerae. It is also active against Nocardia, Chlamydia, Mycoplasma and a wide range of Rickettsiae. Doxycycline is active against spirochetes such as Borellia recurrentis, Treponema pallidum and Treponema pertenue. It is also active against Plasmodium falciparum.
DosageView
Usual dose: 200 mg on first day, then 100 mg daily for 7-10 days.
Severe infections (including refractory urinary tract infections): 200 mg daily for 10 days.
Acne: 100 mg daily.
Uncomplicated genital chlamydia, non-gonococcal urethritis: 100 mg twice daily for 7-21 days (14-21 days in pelvic inflammatory disease).
Severe infections (including refractory urinary tract infections): 200 mg daily for 10 days.
Acne: 100 mg daily.
Uncomplicated genital chlamydia, non-gonococcal urethritis: 100 mg twice daily for 7-21 days (14-21 days in pelvic inflammatory disease).
AdministrationView
Capsules should be swallowed whole with plenty of fluid during meals while sitting or standing.
Side effectsView
Nausea, vomiting, diarrhoea, skin rashes, hemolytic anaemia, eosinophilia may be reported.
ContraindicationsView
Doxycycline is contraindicated to the patients who have shown hypersensitivity to any of the tetracyclines. Doxycycline is contraindicated to the children under 8 years of age. It is also contraindicated to pregnant women and to the lactating mothers.
PrecautionsView
The use of drugs of the tetracycline class during tooth development (last half of pregnancy, infancy and childhood to the age of 8 years) may cause permanent discoloration of teeth. Tetracyclines drugs, therefore should not be used in this age group.
InteractionsView
Absorption of tetracyclines is impaired by antacid containing aluminium, calcium or magnesium, and iron containing preparation. Absorption of tetracyclines is also impaired by bismuth salicylate. Barbiturates, carbamazepine and phenytoin decrease half-life of doxycycline. Concurrent use of tetracyclines may render oral contraceptive less effective. Patients who are on anticoagulant therapy may require downward adjustment of their anticoagulant dosages. It is advisable to avoid giving tetracyclines in conjunction with penicillin.
Pregnancy & lactationView
Doxycycline should be avoided in pregnant women, because of the risk of both staining and effect on bone growth in the foetus. Doxycyclines enter breast milk, and mothers taking these drugs should not breastfeed their child.
StorageView
Keep all medicines out of reach of children. Store in a cool and dry place, protected from light.
Impreja
Dapoxetine Hydrochloride
Impreja
Dapoxetine Hydrochloride
Indications
Premature ejaculation
Indication detailsView
Indicated for the treatment of premature ejaculation (PE) in men 18 to 64 years of age, who have all of the following:
- Persistent or recurrent ejaculation with minimal sexual stimulation before, on or shortly after penetration and before the patient wishes.
- Marked personal distress or interpersonal difficulty as a consequence of PE and poor control over ejaculation.
Therapeutic classView
Drugs for Erectile Dysfunction
PharmacologyView
The mechanism of action is thought to be related to inhibition of neuronal reuptake of serotonin and subsequent potentiation of serotonin activity. The central ejaculatory neural circuit comprises spinal and cerebral areas that form a highly interconnected network. The sympathetic, parasympathetic, and somatic spinal centers, under the influence of sensory genital and cerebral stimuli integrated and processed at the spinal cord level, act in synergy to command physiologic events occurring during ejaculation. Experimental evidence indicates that serotonin (5-HT), throughout brain descending pathways, exerts an inhibitory role on ejaculation. To date, three 5-HT receptor subtypes 5-HT(1A), 5-HT(1B), and 5-HT(2C) have been postulated to mediate 5-HT's modulating activity on ejaculation.
DosageView
Adult (18 to 64 years of age): The recommended starting dose for all patients is 30 mg, taken as needed approximately 1 to 3 hours prior to sexual activity. If the effect of 30 mg is insufficient and the side effects are acceptable, the dose may be increased to the maximum recommended dose of 60 mg. The maximum recommended dosing frequency is one dose every 24 hours.
Side effectsView
Dizziness, Headache, Somnolence, Tremor, Blurred vision, Tinnitus, Sinus congestion, Nausea, Diarrhea, Abdominal pain, Dry mouth, Fatigue, Insomnia, Hypertension.
ContraindicationsView
- Patients with known hypersensitivity to Dapoxetine Hydrochloride.
- Patients with significant pathological cardiac conditions such as heart failure (NYHA class II-IV), conduction abnormalities (second or third degree AV block or sick sinus syndrome) not treated with a permanent pacemaker, significant ischemic heart disease of significant valvular disease.
- Concomitant treatment with monoamine oxidase inhibitors (MAOIs), thioridazine. Similarly, MAOIs or thioridazine should not be administered within 7 days after Dapoxetine has been discontinued.
- Concomitant treatment with serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs) or other medicinal/herbal products with serotonergic effects or within 14 days of discontinuing treatment with these medicinal/herbal products.
PrecautionsView
Patient with bleeding disorders, epilepsy, susceptibility to angle-closure glaucoma or raised intraocular pressure. Not intended for use in women. Known CYP2D6 poor metabolisers.
InteractionsView
CNS active medicinal products: The use of Dapoxetine in combination with CNS active medicinal products has not been systematically evaluated in patients with premature ejaculation. Consequently, caution is advised if the concomitant administration of Dapoxetine and such medicinal products is required.
PDE5 inhibitors: Tadalafil did not affect the pharmacokinetics of Dapoxetine. Sildenafil caused slight changes in Dapoxetine pharmacokinetics, which are not expected to be clinically significant. However, Dapoxetine should be prescribed with caution in patients who use PDE5 inhibitors due to possible reduced orthostatic tolerance.
Tamsulosin: Concomitant administration of single or multiple doses of 30 mg or 60 mg Dapoxetine to patients receiving daily doses of Tamsulosin did not result in changes in the pharmacokinetics of Tamsulosin. However, Dapoxetine should be prescribed with caution in patients who use alpha adrenergic receptor antagonists due to possible reduced orthostatic tolerance.
Warfarin: There are no data evaluating the effect of chronic use of Warfarin with Dapoxetine; therefore, caution is advised when Dapoxetine is used in patients taking Warfarin chronically.
Ethanol: Concomitant use of alcohol and Dapoxetine could increase the chance or severity of adverse reactions such as dizziness, drowsiness, slow reflexes, or altered judgment. Combining alcohol with Dapoxetine may increase these alcohol-related effects and may also enhance neurocardiogenic adverse events such as syncope, thereby increasing the risk of accidental injury; therefore, patients should be advised to avoid alcohol while taking Dapoxetine.
PDE5 inhibitors: Tadalafil did not affect the pharmacokinetics of Dapoxetine. Sildenafil caused slight changes in Dapoxetine pharmacokinetics, which are not expected to be clinically significant. However, Dapoxetine should be prescribed with caution in patients who use PDE5 inhibitors due to possible reduced orthostatic tolerance.
Tamsulosin: Concomitant administration of single or multiple doses of 30 mg or 60 mg Dapoxetine to patients receiving daily doses of Tamsulosin did not result in changes in the pharmacokinetics of Tamsulosin. However, Dapoxetine should be prescribed with caution in patients who use alpha adrenergic receptor antagonists due to possible reduced orthostatic tolerance.
Warfarin: There are no data evaluating the effect of chronic use of Warfarin with Dapoxetine; therefore, caution is advised when Dapoxetine is used in patients taking Warfarin chronically.
Ethanol: Concomitant use of alcohol and Dapoxetine could increase the chance or severity of adverse reactions such as dizziness, drowsiness, slow reflexes, or altered judgment. Combining alcohol with Dapoxetine may increase these alcohol-related effects and may also enhance neurocardiogenic adverse events such as syncope, thereby increasing the risk of accidental injury; therefore, patients should be advised to avoid alcohol while taking Dapoxetine.
Pregnancy & lactationView
Dapoxetine is not indicated for use by women. It is not known either dapoxetine or its metabolites are excreted through human breast milk.
Overdose effectsView
There were no unexpected adverse events in a clinical pharmacology study of Dapoxetine with daily doses up to 240 mg. In general, symptoms of overdose with SSRIs include serotonin-mediated adverse reactions such as somnolence, gastrointestinal disturbances such as nausea and vomiting, tachycardia, tremor, agitation and dizziness. In cases of overdose, standard supportive measures should be adopted as required.
StorageView
Store below 30°C. Protect from light and moisture. Keep out of reach of children
Improcal
Calcitriol
Improcal
Calcitriol
Indications
Secondary hyperparathyroidism
Indication detailsView
Calcitriol is indicated in-
- Post-menopausal osteoporosis
- Renal osteodystrophy
- Postsurgical hypoparathyroidism
- Idiopathic hypoparathyroidism
- Pseudohypoparathyroidism
- Secondary hyperparathyroidism in patients with moderate to severe chronic renal failure (pre-dialysis)
- Vitamin D dependent rickets
Therapeutic classView
Vitamin in bone formation, Vitamin-D preparations
PharmacologyView
Calcitriol is one of the most important active metabolites of vitamin D3. It is normally formed in the kidneys from its precursor, 25-hydroxycholecalciferol. Calcitriol promotes intestinal absorption of calcium and regulates bone mineralization. The key role of Calcitriol is the regulation of calcium homeostasis, which includes stimulation effects on osteoblastic activity in the skeleton.
DosageView
The optimal daily dose of Calcitriol capsule must be carefully determined for each patient on the basis of serum calcium level.
In Post-menopausal Osteoporosis: The recommended dose of Calcitriol capsule is 0.25 mcg twice daily.
In Renal Osteodystrophy (dialysis patients): The initial daily dose is 0.25 mcg of Calcitriol capsule. In patients with normal or only slightly reduced calcium levels, doses of 0.25 mcg every other day are sufficient.
In Hypoparathyroidism and Rickets: The recommended initial dosage of Calcitriol capsule is 0.25 mcg/day which given in the morning. If within 2-4 weeks satisfactory response is not observed by usual dose then dose may be increased at 2-4 weeks intervals.
The recommended intravenous initial dose of Calcitriol injection, depending on the severity of the hypocalcemia and/or secondary hyperparathyroidism, is 1 mcg (0.02 mcg/kg) to 2 mcg administered three times weekly, approximately every other day. Doses as small as 0.5 mcg and as large as 4 mcg three times weekly have been used as an initial dose. If a satisfactory response is not observed, the dose may be increased by 0.5 to 1 mcg at two to four week intervals.
In Post-menopausal Osteoporosis: The recommended dose of Calcitriol capsule is 0.25 mcg twice daily.
In Renal Osteodystrophy (dialysis patients): The initial daily dose is 0.25 mcg of Calcitriol capsule. In patients with normal or only slightly reduced calcium levels, doses of 0.25 mcg every other day are sufficient.
In Hypoparathyroidism and Rickets: The recommended initial dosage of Calcitriol capsule is 0.25 mcg/day which given in the morning. If within 2-4 weeks satisfactory response is not observed by usual dose then dose may be increased at 2-4 weeks intervals.
The recommended intravenous initial dose of Calcitriol injection, depending on the severity of the hypocalcemia and/or secondary hyperparathyroidism, is 1 mcg (0.02 mcg/kg) to 2 mcg administered three times weekly, approximately every other day. Doses as small as 0.5 mcg and as large as 4 mcg three times weekly have been used as an initial dose. If a satisfactory response is not observed, the dose may be increased by 0.5 to 1 mcg at two to four week intervals.
Side effectsView
Occasional symptoms include anorexia, headache, vomiting and constipation. Chronic effects may include dystrophy, fever, polyuria, dehydration, apathy and urinary tract infection.
ContraindicationsView
Calcitriol is contraindicated in patients with known hypersensitivity to any of its ingredients. Calcitriol is also contraindicated in all diseases associated with hypercalcemia.
PrecautionsView
During Calcitriol therapy if the serum calcium levels rise to 1 mg/100 ml above normal or serum creatinine rises to >120 µmol/l, the dosage of Calcitriol should be substantially reduced or treatment stopped.
InteractionsView
Concomitant treatment with a thiazide diuretics increases the risk of hypercalcemia. Calcitriol dosage must be determined with care in patients undergoing treatment with digitalis as hypercalcemia in such patients may precipitate cardiac arrhythmias. Magnesium containing drugs (e.g.,antacids) may cause hypermagnesemia.
Pregnancy & lactationView
There is no evidence that vitamin D is teratogenic in humans. Calcitriol may be used during pregnancy only if the benefits outweigh the potential risk to the fetus. Mothers may breast feed while taking Calcitriol but serum calcium levels of the mother and infant should be monitored.
Pediatric usageView
Secondary hyperparathyroidism in patients with moderate to severe chronic renal failure (pre-dialysis)-
- The recommended initial dosage of Calcitriol is 0.25 mcg/day in adults and pediatric patients 3 years of age or older. This dosage may be increased if necessary to 0.5 mcg/day.
- For pediatric patients less than 3 years of age, the recommended initial dosage of Calcitriol is 10 to 15 ng/kg/day.
- In Elderly: No dosage adjustment are required.
StorageView
keep in a dry place away from light and heat. Keep out of the reach of children.
Improliv
Silymarin [Milk thistle]
Improliv
Silymarin [Milk thistle]
Indications
Jaundice
Indication detailsView
Silymarin (Milk thistle) is indicated for the treatment and prevention of-
- Liver disease, (non-alcoholic & alcoholic)
- Liver cirrhosis, (non-alcoholic & alcoholic)
- Infectious hepatitis
- Drug-induced hepatitis
- Liver disease secondary to diabetes mellitus
- Toxicity of narcotics
- Fatty liver
- Jaundice
Therapeutic classView
Cholagogues, Cholelitholytics & Hepatic Protectors, Herbal and Nutraceuticals
PharmacologyView
Silymarin, a flavonoid complex of Silybum marianum or Milk thistle, is the biologically active component. It provides hepatocellular protection through toxin blockade at the membrane level, enhances protein synthesis, antioxidant activity, anti-fibrotic activity and possible anti-inflammatory or immunomodulating effects.
DosageView
1 capsule 2 to 3 times daily or as directed by a physician.
Side effectsView
Well tolerated in the recommended dose. Occasionally a mild laxative effect may observe.
ContraindicationsView
Contraindicated in patient with a known hypersensitivity to silymarin.
InteractionsView
Concomitant use of silymarin and butyrophenones or phenothiazines has resulted in the reduction of lipid peroxidation.
Pregnancy & lactationView
No experience is available about the use of Silymarin 70 mg or 140 mg during pregnancy and lactation. Therefore, if needed Silymarin 70 mg or 140 mg should be taken with caution according to the physician’s advice.
StorageView
Store in a cool & dry place, away from light & moisture. Keep out of reach of children.
Imucort
Deflazacort
Imucort
Deflazacort
Indications
Allergic and inflammatory disorders
Indication detailsView
Deflazacort is indicated in-
- Anaphylaxis, asthma, severe hypersensitivity reactions
- Rheumatoid arthritis, juvenile chronic arthritis, polymyalgia rheumatica
- Systemic lupus erythematosus, dermatomyositis, mixed connective tissue disease (other than systemic sclerosis), polyartritis nodosa, sarcoidosis
- Pemphigus,bullous pemphigoid, pyoderma gangrenosum
- Minimal change nephrotic syndrome, acute interstitial nephritis
- Rheumatic carditis
- Ulcerative colitis, Crohn's disease
- Uveitis, optic neuritis
- Autoimmune haemolytic anaemia, idiopathic thrombocytopenic purpura
- Acute and lymphatic leukaemia, malignant lymphoma, multiple myeloma
- Immune suppression in transplantation
Therapeutic classView
Glucocorticoids
PharmacologyView
Deflazacort provides anti-inflammatory action by inhibiting Phospholipase A2 enzyme which is responsible for prostaglandin synthesis. Besides Deflazacort decreases the release of certain chemicals that are important in the immune system. By decreasing the release of these chemicals Deflazacort provides immunosuppressive action.
DosageView
Adults-
The following ranges provide general guidance:
- For acute disorders: Up to 120 mg/day Deflazacort may need to be given initially. Maintenance doses in most conditions are within the range of 3-18 mg/day.
- Rheumatoid arthritis: The maintenance dose is usually within the range of 3-18 mg/day. The smallest effective dose should be used and increased if necessary.
- Bronchial asthma: In the treatment of an acute attack, high doses of 48-72 mg/day may be needed depending on severity and gradually reduced once the attack has been controlled. For maintenance in chronic asthma, doses should be titrated to the lowest dose that controls symptoms.
- Other conditions: The dose of Deflazacort depends on clinical need titrated to the lowest effective dose for maintenance. Starting doses may be estimated on the basis of ratio of 5 mg prednisone or prednisolone to 6 mg.
The following ranges provide general guidance:
- Juvenile chronic arthritis: The usual maintenance dose is between 0.25-1.0 mg/kg/day.
- Nephrotic syndrome: Initial dose of usually 1.5 mg/kg/day followed by down titration according to clinical need.
- Bronchial asthma: On the basis of the potency ratio, the initial dose should be between 0.25-1.0 mg/kg on alternate days.
Side effectsView
GI disturbances, musculoskeletal, endocrine, neuropsychiatric, ophthalmic, fluid and electrolyte disturbances; susceptible to infection, impaired healing, hypersensitivity, skin atrophy, striae, telangiectasia, acne, myocardial rupture following recent Ml, thromboembolism.
ContraindicationsView
Hypersensitivity to or any of the ingredients. Patients receiving live virus immunization.
PrecautionsView
The following clinical conditions require special caution and frequent patient monitoring is necessary-
- Cardiac disease or congestive heart failure (except in the presence of active rheumatic carditis), hypertension, thromboembolic disorders. Glucocorticoids can cause salt and water retention and increased excretion of potassium. Dietary salt restriction and potassium supplementation may be necessary.
- Gastritis or oesophagitis, diverticulitis, ulcerative colitis if there is the probability of impending perforation, abscess or pyogenic infections, fresh intestinal anastomosis, active or latent peptic ulcer.
- Diabetes mellitus or family history, osteoporosis, myasthenia gravis, renal insufficiency.
- Emotional instability or psychotic tendency, epilepsy.
- Previous corticosteroid-induced myopathy.
- Liver failure.
- Hypothyroidism and cirrhosis, which may increase the glucocorticoid effect.
- Ocular herpes simplex because of possible corneal perforation.
InteractionsView
Deflazacort is metabolized in the liver. It is recommended to increase the maintenance dose of Deflazacort if drugs which are liver enzyme inducers are co-administered, e.g. rifampicin, rifabutin, carbamazepine, phenobarbitone, phenytoin, primidone and aminoglutethimide. For drugs which inhibit liver enzymes, (e.g. ketoconazole) it may be possible to reduce the maintenance dose of Deflazacort.
Pregnancy & lactationView
Pregnancy: Deflazacort does cross the placenta. However, when administered for prolonged periods or repeatedly during pregnancy, corticosteroids may increase the risk of intrauterine growth retardation. As with all drugs, corticosteroids should only be prescribed when the benefits to the mother and child outweigh the risks.
Nursing Mother: Corticosteroids are excreted in breast milk, although no data are available for Deflazacort. Doses of up to 50 mg daily of Deflazacort are unlikely to cause systemic effects in the infant. Infants of mothers taking higher doses than this may have a degree of adrenal suppression but the benefits of breastfeeding are likely to outweigh any theoretical risk.
Nursing Mother: Corticosteroids are excreted in breast milk, although no data are available for Deflazacort. Doses of up to 50 mg daily of Deflazacort are unlikely to cause systemic effects in the infant. Infants of mothers taking higher doses than this may have a degree of adrenal suppression but the benefits of breastfeeding are likely to outweigh any theoretical risk.
Pediatric usageView
Hepatic Impairment: In patients with hepatic impairment, blood levels of may be increased. Therefore the dose of Deflazacort should be carefully monitored and adjusted to the minimum effective dose.
Renal Impairment: In renally impaired patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary.
Elderly: In elderly patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary. The common adverse effects of systemic corticosteroids may be associated with more serious consequences in old age.
Renal Impairment: In renally impaired patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary.
Elderly: In elderly patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary. The common adverse effects of systemic corticosteroids may be associated with more serious consequences in old age.
StorageView
Store in a cool (below 25°C) and dry place, protected from light & moisture. Keep out of the reach of children.
Imucort
Deflazacort
Imucort
Deflazacort
Indications
Allergic and inflammatory disorders
Indication detailsView
Deflazacort is indicated in-
- Anaphylaxis, asthma, severe hypersensitivity reactions
- Rheumatoid arthritis, juvenile chronic arthritis, polymyalgia rheumatica
- Systemic lupus erythematosus, dermatomyositis, mixed connective tissue disease (other than systemic sclerosis), polyartritis nodosa, sarcoidosis
- Pemphigus,bullous pemphigoid, pyoderma gangrenosum
- Minimal change nephrotic syndrome, acute interstitial nephritis
- Rheumatic carditis
- Ulcerative colitis, Crohn's disease
- Uveitis, optic neuritis
- Autoimmune haemolytic anaemia, idiopathic thrombocytopenic purpura
- Acute and lymphatic leukaemia, malignant lymphoma, multiple myeloma
- Immune suppression in transplantation
Therapeutic classView
Glucocorticoids
PharmacologyView
Deflazacort provides anti-inflammatory action by inhibiting Phospholipase A2 enzyme which is responsible for prostaglandin synthesis. Besides Deflazacort decreases the release of certain chemicals that are important in the immune system. By decreasing the release of these chemicals Deflazacort provides immunosuppressive action.
DosageView
Adults-
The following ranges provide general guidance:
- For acute disorders: Up to 120 mg/day Deflazacort may need to be given initially. Maintenance doses in most conditions are within the range of 3-18 mg/day.
- Rheumatoid arthritis: The maintenance dose is usually within the range of 3-18 mg/day. The smallest effective dose should be used and increased if necessary.
- Bronchial asthma: In the treatment of an acute attack, high doses of 48-72 mg/day may be needed depending on severity and gradually reduced once the attack has been controlled. For maintenance in chronic asthma, doses should be titrated to the lowest dose that controls symptoms.
- Other conditions: The dose of Deflazacort depends on clinical need titrated to the lowest effective dose for maintenance. Starting doses may be estimated on the basis of ratio of 5 mg prednisone or prednisolone to 6 mg.
The following ranges provide general guidance:
- Juvenile chronic arthritis: The usual maintenance dose is between 0.25-1.0 mg/kg/day.
- Nephrotic syndrome: Initial dose of usually 1.5 mg/kg/day followed by down titration according to clinical need.
- Bronchial asthma: On the basis of the potency ratio, the initial dose should be between 0.25-1.0 mg/kg on alternate days.
Side effectsView
GI disturbances, musculoskeletal, endocrine, neuropsychiatric, ophthalmic, fluid and electrolyte disturbances; susceptible to infection, impaired healing, hypersensitivity, skin atrophy, striae, telangiectasia, acne, myocardial rupture following recent Ml, thromboembolism.
ContraindicationsView
Hypersensitivity to or any of the ingredients. Patients receiving live virus immunization.
PrecautionsView
The following clinical conditions require special caution and frequent patient monitoring is necessary-
- Cardiac disease or congestive heart failure (except in the presence of active rheumatic carditis), hypertension, thromboembolic disorders. Glucocorticoids can cause salt and water retention and increased excretion of potassium. Dietary salt restriction and potassium supplementation may be necessary.
- Gastritis or oesophagitis, diverticulitis, ulcerative colitis if there is the probability of impending perforation, abscess or pyogenic infections, fresh intestinal anastomosis, active or latent peptic ulcer.
- Diabetes mellitus or family history, osteoporosis, myasthenia gravis, renal insufficiency.
- Emotional instability or psychotic tendency, epilepsy.
- Previous corticosteroid-induced myopathy.
- Liver failure.
- Hypothyroidism and cirrhosis, which may increase the glucocorticoid effect.
- Ocular herpes simplex because of possible corneal perforation.
InteractionsView
Deflazacort is metabolized in the liver. It is recommended to increase the maintenance dose of Deflazacort if drugs which are liver enzyme inducers are co-administered, e.g. rifampicin, rifabutin, carbamazepine, phenobarbitone, phenytoin, primidone and aminoglutethimide. For drugs which inhibit liver enzymes, (e.g. ketoconazole) it may be possible to reduce the maintenance dose of Deflazacort.
Pregnancy & lactationView
Pregnancy: Deflazacort does cross the placenta. However, when administered for prolonged periods or repeatedly during pregnancy, corticosteroids may increase the risk of intrauterine growth retardation. As with all drugs, corticosteroids should only be prescribed when the benefits to the mother and child outweigh the risks.
Nursing Mother: Corticosteroids are excreted in breast milk, although no data are available for Deflazacort. Doses of up to 50 mg daily of Deflazacort are unlikely to cause systemic effects in the infant. Infants of mothers taking higher doses than this may have a degree of adrenal suppression but the benefits of breastfeeding are likely to outweigh any theoretical risk.
Nursing Mother: Corticosteroids are excreted in breast milk, although no data are available for Deflazacort. Doses of up to 50 mg daily of Deflazacort are unlikely to cause systemic effects in the infant. Infants of mothers taking higher doses than this may have a degree of adrenal suppression but the benefits of breastfeeding are likely to outweigh any theoretical risk.
Pediatric usageView
Hepatic Impairment: In patients with hepatic impairment, blood levels of may be increased. Therefore the dose of Deflazacort should be carefully monitored and adjusted to the minimum effective dose.
Renal Impairment: In renally impaired patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary.
Elderly: In elderly patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary. The common adverse effects of systemic corticosteroids may be associated with more serious consequences in old age.
Renal Impairment: In renally impaired patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary.
Elderly: In elderly patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary. The common adverse effects of systemic corticosteroids may be associated with more serious consequences in old age.
StorageView
Store in a cool (below 25°C) and dry place, protected from light & moisture. Keep out of the reach of children.