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Angiotensin-ll receptor blocker

Losartan Potassium is the first non-peptide orally active angiotensin II receptor blocker. It binds to the AT1 receptor found in many tissues (e.g. vascular smooth muscle, adrenal gland, kidneys and the heart) and reduces several important biological actions including vasoconstriction and the release of aldosterone responsible for hypertension.

The usual starting and maintenance dose is 50 mg once daily for most patients. If the antihypertensive effect using 50 mg once daily is inadequate, 25 mg twice daily is recommended prior to increasing the dose. For patients with intravascular volume-depletion (e.g., those treated with high-dose diuretics), a starting dose of 25 mg once daily should be considered. Losartan Potassium can be administered once or twice daily. The total daily dose ranges from 25 mg to 100 mg.

The side effects with the use of Losartan Potassium are mild and transient in nature. The most common side effects are dizziness, diarrhea, nasal congestion, cough, upper respiratory infection. Other side effects are fatigue, oedema, abdominal pain, chest pain, nausea, headache & pharyngitis.

Losartan Potassium is contraindicated in pregnant women and in patients who are hypersensitive to any component of this product. Losartan Potassium should not be administered with Aliskiren in patients with diabetes.

Use of Losartan Potassium during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. In patients who are intravascularly volume-depleted (e.g., those treated with high-dose diuretics), symptomatic hypotension may occur. Plasma concentration of Losartan Potassium is significantly increased in cirrhotic patients. Changes in renal function including renal failure have been reported in renal impaired patient.

Rifampicin and fluconazole reduce levels of active metabolite of Losartan Potassium. Concomitant use of Losartan Potassium and hydrochlorothiazide may lead to potentiation of the antihypertensive effects. Concomitant use of potassium-sparing diuretics (eg, spironolactone, triamterene, amiloride), potassium supplements or salt substitutes containing potassium may lead to increases in serum potassium. The antihypertensive effect of losartan may be attenuated by the non-steroidal anti-inflammatory drug indomethacin. The use of ACE-inhibitor, angiotensin receptor antagonist, an anti-inflammatory drug and a thiazide diuretic at the same time increases the risk of renal impairment.

Pregnancy Category D. The risk to the fetus increases if Losartan Potassium is administered during the second or third trimesters of pregnancy. It is not known whether Losartan Potassium is excreted in human milk, as many drugs are excreted in human milk and because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

keep in a dry place away from light and heat. Keep out of the reach of children.

This is indicated for the treatment of hypertension. It is also indicated to reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy.

Combined antihypertensive preparations

Angiotensin II formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE), is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT₁ receptor found in many tissues, (e.g. vascular smooth muscle, adrenal gland). In vitro binding studies indicate that losartan is a reversible, competitive inhibitor of the AT₁ receptor. Neither Losartan nor its active metabolite inhibits ACE (kinase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin); nor do they bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

Hydrochlorothiazide is a thiazide diuretic. Thiazides affect the renal tubular mechanisms of electrolyte reabsorption, directly increasing excretion of Sodium and Chloride in approximately equivalent amounts. Indirectly, the diuretic action of Hydrochlorothiazide reduces plasma volume, with consequent increases in plasma renin activity, increases in Aldosterone secretion, increases in urinary Potassium loss, and decreases in serum Potassium. The renin-aldosterone link is mediated by angiotensin II, so co-administration of an angiotensin II receptor antagonist tends to reverse the Potassium loss associated with these diuretics.

Hypertension-

• The usual starting dose of 50/12.5 is one tablet once daily.
• For patients who do not respond adequately to one tablet the dosage may be increased to 100/25 once daily.
• A patient whose blood pressure is not adequately controlled with Losartan 100 mg monotherapy may be switched to this combination 100/12.5 once daily.
• In hypertensive patients with left ventricular hypertrophy initial dose is 50/12.5, if additional blood pressure reduction is needed, 100/12.5 may be given, followed by 100/25 if required. The maximum dose is 100/25 once daily.
• In general, the antihypertensive effect is attained within three weeks after initiation of therapy.
• No initial dosage adjustment of 50/12.5 is necessary for elderly patients. But maximum dose of 100/25 once daily dose should not be used as initial therapy in elderly patients.

Severe Hypertension:

• The starting dose for initial treatment of severe hypertension is one tablet of 50/12.5 once daily.
• For patients who do not respond adequately to this dose after 2 to 4 weeks of therapy, the dosage may be increased to 100/25 once daily. The maximum dose is one tablet of 100/25 once daily.

This preparation may be administered with other antihypertensive agents. This may be administered with or without food.

Side-effects are usually mild. Symptomatic hypotension including dizziness may occur, particularly in patients with intravascular volume depletion (e.g. those taking high-dose diuretics). Hyperkalaemia occurs occasionally; angioedema has also been reported with some angiotensin-II receptor antagonists. Vertigo; less commonly gastro-intestinal disturbances, angina, palpitation, oedema, dyspnoea, headache, sleep disorders, malaise, urticaria, pruritus, rash; rarely hepatitis, atrial fibrillation, cerebrovascular accident, syncope, paraesthesia; also reported pancreatitis, anaphylaxis, cough, depression, erectile dysfunction, anaemia, thrombocytopenia, hyponatraemia, arthralgia, myalgia, renal impairment, rhabdomyolysis, tinnitus, photosensitivity, and vasculitis (including Henoch-Schonlein purpura)

The combination of Losartan and Hydrochlorothiazide is contraindicated in patients who are hypersensitive to any component of this product. Because of the Hydrochlorothiazide component, this product is contraindicated in patients with anuria or hypersensitivity to other sulfonamide-derived drugs.

Losartan Potassium: No significant drug-drug pharmacokinetic interactions have been found in interaction studies with Hydrochlorothiazide, Digoxin, Warfarin, Cimetidine and Phenobarbital. As with other drugs that block angiotensin II or its effects, concomitant use of potassium-sparing diuretics (e.g. Spironolactone, Triamterene, Amiloride), potassium supplements, or salt substitutes containing potassium may lead to increase in serum potassium. As with other antihypertensive agents, the antihypertensive effect of Losartan may be blunted by the non-steroidal anti-inflammatory drug Indomethacin.

Hydrochlorothiazide: When administered concurrently, the following drugs may interact with Thiazide diuretics: alcohol, barbiturates, or narcotics-potentiation of orthostatic hypotension may occur.

Antidiabetic drugs (oral agents and Insulin): dosage adjustment of the antidiabetic drug may be required.

Other antihypertensive drugs: additive effect or potentiation.

Cholestyramine and colestipol resins: absorption of Hydrochlorothiazide is impaired in the presence of anionic exchange resins

Angiotensin-II receptor antagonists should be avoided in pregnancy unless essential. They may adversely affect fetal and neonatal blood pressure control and renal function; skull defects and oligohy dramnios have also been reported. Information on the use of angiotensin-II receptor antagonists in breastfeeding is limited. They are not recommended in breastfeeding and alternative treatment options, with better-established safety information during breastfeeding, are available.

Use in Patients with Renal Impairment: The usual regimens of therapy with 50/12.5 may be followed as long as the patient's creatinine clearance is >30 ml/min. In patients with more severe renal impairment, loop diuretics are preferred to thiazides. In that case, hydrochlorothiazide is not recommended.

Use in Patients with Hepatic Impairment: The combination of Losartan and Hydrochlorothiazide is not recommended for titration in patients with hepatic impairment because the appropriate 25 mg starting dose of Losartan cannot be given.

Use in pediatric patients: The safety and effectiveness in pediatric patients have not been established.

Losartan Potassium: Limited data are available in regard to overdosage in humans. The most likely manifestation of overdosage would be hypotension and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted. Neither losartan nor its metabolite can be removed by hemodialysis.

Hydrochlorothiazide: The most common signs and symptoms observed are those caused by electrolyte depletion (hypokalemia, hypochloremia, and dehydration resulting from excessive diuresis. If digitalis has also been administered, hypokalemia, may accentuate cardiac arrhythmias. The degree to which Hydrochlorothiazide is removed by hemodialysis has not been established.

Do not store above 30°C. Keep out of the reach of children.

This is indicated for the treatment of hypertension. It is also indicated to reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy.

Combined antihypertensive preparations

Angiotensin II formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE), is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT₁ receptor found in many tissues, (e.g. vascular smooth muscle, adrenal gland). In vitro binding studies indicate that losartan is a reversible, competitive inhibitor of the AT₁ receptor. Neither Losartan nor its active metabolite inhibits ACE (kinase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin); nor do they bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.

Hydrochlorothiazide is a thiazide diuretic. Thiazides affect the renal tubular mechanisms of electrolyte reabsorption, directly increasing excretion of Sodium and Chloride in approximately equivalent amounts. Indirectly, the diuretic action of Hydrochlorothiazide reduces plasma volume, with consequent increases in plasma renin activity, increases in Aldosterone secretion, increases in urinary Potassium loss, and decreases in serum Potassium. The renin-aldosterone link is mediated by angiotensin II, so co-administration of an angiotensin II receptor antagonist tends to reverse the Potassium loss associated with these diuretics.

Hypertension-

• The usual starting dose of 50/12.5 is one tablet once daily.
• For patients who do not respond adequately to one tablet the dosage may be increased to 100/25 once daily.
• A patient whose blood pressure is not adequately controlled with Losartan 100 mg monotherapy may be switched to this combination 100/12.5 once daily.
• In hypertensive patients with left ventricular hypertrophy initial dose is 50/12.5, if additional blood pressure reduction is needed, 100/12.5 may be given, followed by 100/25 if required. The maximum dose is 100/25 once daily.
• In general, the antihypertensive effect is attained within three weeks after initiation of therapy.
• No initial dosage adjustment of 50/12.5 is necessary for elderly patients. But maximum dose of 100/25 once daily dose should not be used as initial therapy in elderly patients.

Severe Hypertension:

• The starting dose for initial treatment of severe hypertension is one tablet of 50/12.5 once daily.
• For patients who do not respond adequately to this dose after 2 to 4 weeks of therapy, the dosage may be increased to 100/25 once daily. The maximum dose is one tablet of 100/25 once daily.

This preparation may be administered with other antihypertensive agents. This may be administered with or without food.

Side-effects are usually mild. Symptomatic hypotension including dizziness may occur, particularly in patients with intravascular volume depletion (e.g. those taking high-dose diuretics). Hyperkalaemia occurs occasionally; angioedema has also been reported with some angiotensin-II receptor antagonists. Vertigo; less commonly gastro-intestinal disturbances, angina, palpitation, oedema, dyspnoea, headache, sleep disorders, malaise, urticaria, pruritus, rash; rarely hepatitis, atrial fibrillation, cerebrovascular accident, syncope, paraesthesia; also reported pancreatitis, anaphylaxis, cough, depression, erectile dysfunction, anaemia, thrombocytopenia, hyponatraemia, arthralgia, myalgia, renal impairment, rhabdomyolysis, tinnitus, photosensitivity, and vasculitis (including Henoch-Schonlein purpura)

The combination of Losartan and Hydrochlorothiazide is contraindicated in patients who are hypersensitive to any component of this product. Because of the Hydrochlorothiazide component, this product is contraindicated in patients with anuria or hypersensitivity to other sulfonamide-derived drugs.

Losartan Potassium: No significant drug-drug pharmacokinetic interactions have been found in interaction studies with Hydrochlorothiazide, Digoxin, Warfarin, Cimetidine and Phenobarbital. As with other drugs that block angiotensin II or its effects, concomitant use of potassium-sparing diuretics (e.g. Spironolactone, Triamterene, Amiloride), potassium supplements, or salt substitutes containing potassium may lead to increase in serum potassium. As with other antihypertensive agents, the antihypertensive effect of Losartan may be blunted by the non-steroidal anti-inflammatory drug Indomethacin.

Hydrochlorothiazide: When administered concurrently, the following drugs may interact with Thiazide diuretics: alcohol, barbiturates, or narcotics-potentiation of orthostatic hypotension may occur.

Antidiabetic drugs (oral agents and Insulin): dosage adjustment of the antidiabetic drug may be required.

Other antihypertensive drugs: additive effect or potentiation.

Cholestyramine and colestipol resins: absorption of Hydrochlorothiazide is impaired in the presence of anionic exchange resins

Angiotensin-II receptor antagonists should be avoided in pregnancy unless essential. They may adversely affect fetal and neonatal blood pressure control and renal function; skull defects and oligohy dramnios have also been reported. Information on the use of angiotensin-II receptor antagonists in breastfeeding is limited. They are not recommended in breastfeeding and alternative treatment options, with better-established safety information during breastfeeding, are available.

Use in Patients with Renal Impairment: The usual regimens of therapy with 50/12.5 may be followed as long as the patient's creatinine clearance is >30 ml/min. In patients with more severe renal impairment, loop diuretics are preferred to thiazides. In that case, hydrochlorothiazide is not recommended.

Use in Patients with Hepatic Impairment: The combination of Losartan and Hydrochlorothiazide is not recommended for titration in patients with hepatic impairment because the appropriate 25 mg starting dose of Losartan cannot be given.

Use in pediatric patients: The safety and effectiveness in pediatric patients have not been established.

Losartan Potassium: Limited data are available in regard to overdosage in humans. The most likely manifestation of overdosage would be hypotension and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted. Neither losartan nor its metabolite can be removed by hemodialysis.

Hydrochlorothiazide: The most common signs and symptoms observed are those caused by electrolyte depletion (hypokalemia, hypochloremia, and dehydration resulting from excessive diuresis. If digitalis has also been administered, hypokalemia, may accentuate cardiac arrhythmias. The degree to which Hydrochlorothiazide is removed by hemodialysis has not been established.

Do not store above 30°C. Keep out of the reach of children.

Ophthalmic Steroid preparations

Loteprednol is a corticosteroid which is thought to act by the induction of phospholipase A2 inhibitory proteins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid.

Loteprednol ophthalmic gel: Instill one to two drops of Ophthalmic Gel into the conjunctival sac of the affected eye four times daily beginning the day after surgery and continuing throughout the first 2 weeks of the postoperative period.

Loteprednol ophthalmic suspension:

• For steroid-responsive ocular inflammation: Instill 1 drop of Ophthalmic Suspension into the conjunctival sac of the eye(s) four times a day.
• For inflammation after surgery: Instill 1 drop of Ophthalmic Suspension into the conjunctival sac of the operated eye(s) four times a day beginning 24 hours after surgery and continuing throughout the first two weeks after surgery.

Use in children: Safety and effectiveness in pediatric patients have not been established.

Glaucoma with optic nerve damage, visual acuity and field defects; cataract formation; secondary ocular infection following suppression of host response; and perforation of the globe may occur.

It is contraindicated in most viral diseases of the cornea and conjunctiva. It is also contraindicated in individuals with known or suspected hypersensitivity to any of the ingredients of this preparation and to other corticosteroids.

For ophthalmic use only. If this product is used for 10 days or longer, intraocular pressure should be monitored. Fungal infections of the cornea are particularly prone to develop coincidentally with long-term use of steroid topically. Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and visual field, and in posterior subcapsular cataract formation. Use of a corticosteroid medication in the treatment of patients with a history of herpes simplex requires great caution.

No clinical data available for use in pregnancy. It is not known whether Loteprednol Etabonate passes into breast milk.

Protect from light. Store in cool & dry place. Keep out of the reach of children.

Atenolol is indicated-

• In the management of hypertension. It may be used alone or concomitantly with other antihypertensive agents, particularly with a thiazide-type diuretic.
• For the long-term management of patients with angina pectoris.
• In the management of hemodynamically stable patients with defnite or suspected acute myocardial infarction to reduce cardiovascular mortality.

Beta-adrenoceptor blocking drugs, Beta-blockers

The synthesis of atenolol resulted from attempts to produce a β-adrenoceptor antagonist that would competitively block β1 (cardiac) receptors but have no effect on β2-receptors. It is classified as a β1 selective (cardioselective) β-adrenergic receptor antagonist with no membranestability activity and no partial agonist activity. It is markedly the most hydrophilic of the currently available β- blockers and thus penetrates the lipid of cell membranes poorly

Hypertension: The initial dose of Atenolol is 50 mg given as one tablet a day either alone or added to diuretic therapy. The full effect of this dose will usually be seen within one to two weeks. If an optimal response is not achieved, the dosage should be increased to Atenolol 100 mg given as one tablet a day. Increasing the dosage beyond 100 mg a day is unlikely to produce any further benefit.

Angina Pectoris: The initial dose of Atenolol is 50 mg given as one tablet a day. If an optimal response is not achieved within one week, the dosage should be increased to Atenolol 100 mg given as one tablet a day. Some patients may require a dosage of 200 mg once a day for optimal effect. Twenty-four hour control with once daily dosing is achieved by giving doses larger than necessary to achieve an immediate maximum effect. The maximum early effect on exercise tolerance occurs with doses of 50 to 100 mg, but at these doses the effect at 24 hours is attenuated, averaging about 50% to 75% of that observed with once a day oral doses of 200 mg.

Acute Myocardial Infarction: In patients with definite or suspected acute myocardial infarction, treatment with Atenolol I.V. Injection should be initiated as soon as possible after the patient's arrival in the hospital and after eligibility is established. Treatment should begin with the intravenous administration of 5 mg Atenolol over 5 minutes followed by another 5 mg intravenous injection 10 minutes later. In patients who tolerate the full intravenous dose (10 mg), Atenolol Tablets 50 mg should be initiated 10 minutes after the last intravenous dose followed by another 50 mg oral dose 12 hours later. Thereafter, Atenolol can be given orally either 100 mg once daily or 50 mg twice a day for a further 6-9 days or until discharge from the hospital. If bradycardia or hypotension requiring treatment or any other untoward effects occur, Atenolol should be discontinued.

In a series of investigations in the treatment of acute myocardial infarction, bradycardia and hypotension occurred more commonly, as expected for any beta blocker. In addition, a variety of adverse efects has been reported with other beta-adrenergic blocking agents, and may be considered potential adverse efects of Atenolol.

• Hematologic: Agranulocytosis.
• Allergic: Fever, combined with aching and sore throat, laryngospasm, and respiratory distress.
• Central Nervous System: Reversible mental depression progressing to catatonia; an acute reversible syndrome characterized by disorientation of time and place; short term memory loss; emotional lability with slightly clouded sensorium; and, decreased performance on neuropsychometrics.
• Gastrointestinal: Mesenteric arterial thrombosis, ischemic colitis.
• Miscellaneous: There have been reports of skin rashes and/or dry eyes associated with the use of beta-adrenergic blocking drugs. Discontinuance of the drug should be considered if any such reaction is not otherwise explicable. Patients should be closely monitored following cessation of therapy.
• Other: Erythematous rash

Atenolol is contraindicated in-

• Sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure.
• Those patients with a history of hypersensitivity to the atenolol or any of the drug product’s components.

General: Patients already on a beta blocker must be evaluated carefully before Atenolol is administered. Initial and subsequent Atenolol dosages can be adjusted downward depending on clinical observations including pulse and blood pressure. Atenolol may aggravate peripheral arterial circulatory disorders.

Impaired Renal Function: The drug should be used with caution in patients with impaired renal function.

Geriatric Use:

• Hypertension and Angina Pectoris: Due to Coronary Atherosclerosis: Dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
• Acute Myocardial Infarction: Dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. Evaluation of patients with hypertension or myocardial infarction should always include assessment of renal function.

Pregnancy Category D. Caution should be exercised when Atenolol is administered to a nursing woman. Clinically significant bradycardia has been reported in breast-fed infants. Premature infants, or infants with impaired renal function, may be more likely to develop adverse effects.

Elderly Patients or Patients with Renal Impairment: Atenolol is excreted by the kidneys; consequently dosage should be adjusted in cases of severe impairment of renal function. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, refecting greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. The following maximum oral dosages are recommended for elderly, renal impaired patients and for patients with renal impairment due to other causes:

• Creatinine clearance 15-35 ml/min/1.73 m²: Maximum dosage 50 mg daily
• Creatinine clearance <15 mL/min/1.73 m²: Maximum dosage 25 mg daily

Some renal impaired or elderly patients being treated for hypertension may require a lower starting dose of Atenolol: 25 mg given as one tablet a day. Patients on hemodialysis should be given 25 mg or 50 mg after each dialysis; this should be done under hospital supervision as marked falls in blood pressure can occur.

Overdosage with Atenolol has been reported with patients surviving acute doses as high as 5 g. One death was reported in a man who may have taken as much as 10 g acutely. The predominant symptoms reported following Atenolol overdose are lethargy, disorder of respiratory drive, wheezing, sinus pause and bradycardia. Additionally, common efects associated with overdosage of any beta-adrenergic blocking agent and which might also be expected in Atenolol overdose are congestive heart failure, hypotension, bronchospasm and/or hypoglycemia. Treatment of overdose should be directed to the removal of any unabsorbed drug by induced emesis, gastric lavage, or administration of activated charcoal. Atenolol can be removed from the general circulation by hemodialysis. Based on the severity of symptoms, management may require intensive support care and facilities for applying cardiac and respiratory support.

Do not use later than the date of expiry. Keep all medicines out of the reach of children. To be dispensed only on the prescription of a registered physician.

Metoprolol is a selective beta1-blocker. Metoprolol reduces or inhibits the agonistic effect on the heart of catecholamines (which are released during physical and mental stress). This means that the usual increase in heart rate, cardiac output, cardiac contractility and blood pressure, produced by the acute increase in catecholamines, is reduced by Metoprolol. Metoprolol interferes less with Insulin release and carbohydrate metabolism than do non-selective beta-blockers. Metoprolol interferes much less with the cardiovascular response to hypoglycaemia than do non-selective beta-blockers.

Film-coated tablet-

• Hypertension: Total daily dosage Metoprolol 100-400 mg to be given as a single or twice-daily dose. The starting dose is 100 mg (two Metoprolol-50 tablets) per day. This may be increased by 100 mg per day at weekly intervals. lf full control is not achieved using a single daily dose, a b.i.d. regimen should be initiated. Combination therapy with a diuretic or other antihypertensive agents may also be considered.
• Angina: Usually Metoprolol 50 mg (one Metoprolol-50 tablet) to 100 mg (two Metoprolol-50 tablets) twice or three times daily.
• Cardiac arrhythmias: Metoprolol 50 mg (one Metoprolol-50 tablet) b.i.d or t.i.d should usually control the condition. It is necessary the dose can be increased up to 300 mg per day in divided doses. Following the treatment of an acute arrhythmia with Metoprolol injection, continuation therapy with Metoprolol tablets should be initiated 4-6 hours later. The initial oral dose should not exceed 50 mg t.i.d.
• Hyperthyroidism: Metoprolol 50 mg (one Metoprolol-50 tablet) four times a day. The dose should be reduced as the euthyroid state is achieved.
• Myocardial infarction: Orally, therapy should commence 15 minutes after the last injection with 50 mg every 6 hours for 48 hours. Patients who fail to tolerate the full intravenous dose should be given half the suggested oral dose. Maintenance- The usual maintenance dose is 200 mg daily given in divided doses. Elderly’ There are no special dosage requirements in otherwise healthy elderly patients. Significant hepatic dysfunction: A reduction in dosage may be necessary.

Extended-release tablet-

• Hypertension: The usual initial dosage is 25 to 100 mg daily in a single dose, whether used alone or added to a diuretic.
• Angina Pectoris: The dosage of extended-release Metoprolol Succinate should be individualized. The usual initial dosage is 100 mg daily, in a single dose.
• Heart Failure: The recommended starting dose of sustained-release Metoprolol Succinate is 25 mg once daily for two weeks in patients with NYHA class II heart failure and 12.5 mg once daily in patients with more severe heart failure. The dosage may be increased at weekly (or longer) intervals until optimum blood pressure reduction is achieved. If treatment is to be discontinued, the dosage should be reduced gradually over a period of 1-2 weeks.

IV Injection-

• Arrhythmias: By intravenous injection, up to 5 mg at a rate of 1-2 mg/minute, repeated after 5 minutes if necessary, total dose 10-15 mg.
• In surgery: By slow intravenous injection 2-4 mg at induction or to control arrhythmias developing during anaesthesia; 2 mg doses may be repeated to a maximum of 10 mg.
• Myocardial Infarction: Early intervention within 12 hours of infarction, by intravenous injection 5 mg every 2 minutes to a maximum of 15 mg, followed after 15 minutes by 50 mg by mouth every 6 hours for 48 hours; maintenance 200 mg daily in divided doses.

Tiredness, dizziness, depression, diarrhea, itching or rash, shortness of breath, slow heart rate, mental confusion, headache, somnolence, nightmares, insomnia, dyspnea, Nausea, dry mouth, gastric pain, constipation, flatulence, digestive tract disorders, heartburn, pruritus, musculoskeletal pain, blurred vision, decreased libido, and tinnitus have also been reported, intensification of AV block.

AV block, Uncontrolled heart failure, severe bradycardia, sick-sinus syndrome, cardiogenic shock and severe peripheral arterial disease. Known hypersensitivity to Metoprolol or other B-blockers. Metoprolol is also contra-indicated when myocardial infarction is complicated by significant bradycardia, first-degree heart block, systolic hypotension (<100mmHg) and/or severe heart failure.

Bronchospastic Diseases: Because of its relative beta 1 ‐selectivity, however, Metoprolol may be used with caution in patients with bronchospastic disease who do not respond to, or cannot tolerate other antihypertensive treatment.

Major Surgery: The necessity or desirability of withdrawing beta‐blocking therapy prior to major surgery is controversial; the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures.

Diabetes and Hypoglycemia: Beta‐blockers may mask tachycardia occurring with hypoglycemia, but other manifestations such as dizziness and sweating may not be significantly affected. Peripheral Vascular Disease: Beta‐blockers can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease. Calcium Channel Blockers: Because of significant inotropic and chronotropic effects in patients, caution should be exercised in patients treated with these agents concomitantly.

Catecholamine‐depleting drugs (e.g. Reserpine, Monoamine Oxidase (MAO) inhibitors) may have an additive effect when given with beta‐blocking agents. Drugs that inhibit CYP2D6 such as quinidine, fluoxetine, paroxetine and propafenone are likely to increase Metoprolol concentration. These increases in plasma concentration would decrease the cardioselectivity of Metoprolol. Concomitant use of digitalis glycosides and beta‐blockers can increase the risk of bradycardia. Beta‐blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine.

Pregnancy Category C. There are no adequate and well‐controlled studies in pregnant women. This drug should be used during pregnancy only if clearly needed. Metoprolol is excreted in breast milk in very small quantities. Caution should be exercised when Metoprolol is administered to a nursing woman.

Hepatic impaired patient: Metoprolol should be used with caution in patients with impaired hepatic function.

Pediatric Use: No clinically relevant differences in the adverse event profile were observed for pediatric patients aged 6 to 16 years as compared with adult patients. Safety and effectiveness of Metoprolol have not been established in patients <6 years of age.

Geriatric Use: There were no notable differences in efficacy or the rate of adverse events between older and younger patients.

Poisoning due to an overdose of metoprolol may lead to severe hypotension, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, impairment of consciousness, coma, nausea, vomiting, cyanosis, hypoglycaemia and, occasionally, hyperkalaemia. The first manifestations usually appear 20 minutes to 2 hours after drug ingestion. Treatment: Treatment should include close monitoring of cardiovascular, respiratory and renal function, and blood glucose and electrolytes. Further absorption may be prevented by induction of vomiting, gastric lavage or administration of activated-charcoal if ingestion is recent. Cardiovascular complications should be treated symptomatically, which may require the use of sympathomimetic agents (e.g. noradrenaline, metaramionl), atropine or inotropic agents (e.g. dopamine, dobutamine). Temporary pacing may be required for AV block. Glucagon can reverse the effects of excessive B-blockade, given in a dose of 1-10 mg intravenously. Intravenous B2-stimulants e.g. terbutaline may be required to relieve bronchospasm. Metoprolol cannot be effectively removed by haemodialysis.

Store in a cool and dry place, protected from light.

Non-sedating antihistamines

This tablet is a preparation of Loratadine. Loratadine is a non-sedative histamine Hr receptor antagonist with antiallergic properties. Loratadine is a long-acting tricyclic antihistamine with selective peripheral Hi-receptor antagonistic activity and no central sedative or anticholinergic effect. It is rapidly effective and long-lasting, allowing once-a-day administration.

Adults and children over 12 years of age: One Loratadine tablet once daily. It is usually administered in the morning or when symptoms require treatment.

Children 2-12 years: Body weight over 30 kg: one Loratadine tablet once daily, below 30 kg: half Loratadine tablet once daily.

Below 2 years of age: Loratadine tablet is not recommended for use below 2 years of age since safety and efficacy has not been established.

During controlled clinical studies the incidence of adverse events, including sedation and anticholinergic effects observed with 10 mg Loratadine was comparable to that observed with placebo. Studies on the effect of Loratadine on actual driving performance, and on tests of cognitive and psychomotor functioning have shown it to be comparable to placebo.

Loratadine is contraindicated in patients who have shown hypersensitivity or idiosyncrasy to their components.

Caution should be taken in patients with liver impairment or renal insufficiency (eGFR <30 ml/min).

There are no reports of potentially hazardous interactions with other drugs. In contrast to many other histamine H1 receptor antagonists, Loratadine has no potentiating effects when administered concurrently with alcohol, as measured by psychomotor performance studies. Concomitant therapy with drugs that inhibit or are metabolized by hepatic cytochromes P450 3A4 and 2D6 may elevate plasma concentrations of either drug and this mayifesult in adverse effects. Cimetidine inhibits both enzymes while erythromycin or ketoconazole inhibits P450 3A4. These drugs increase loratadine serum concentrations but no adverse effects are reported.

There is no experience of the use of Loratadine in human pregnancy. Therefore its use during pregnancy is not advisable. Loratadine is excreted in breast milk in a very small amount. So nursing mothers are advised not to take the drug.

In adults somnolence, tachycardia and headache have been reported with overdose greater than 10 mg. Extrapyramidal signs and palpitations have been reported in children with overdoses of greater than 10 mg. In the event of overdosage, general symptomatic and supportive measures should be instituted promptly and maintained for as long as necessary. It would seem reasonable to treat patients presenting early after large overdoses with oral activated charcoal. The conscious patients may be induced to vomit or gastric lavage may be performed.

Keep in a dry place away from light and heat. Keep out of the reach of children.

Non-sedating antihistamines

This tablet is a preparation of Loratadine. Loratadine is a non-sedative histamine Hr receptor antagonist with antiallergic properties. Loratadine is a long-acting tricyclic antihistamine with selective peripheral Hi-receptor antagonistic activity and no central sedative or anticholinergic effect. It is rapidly effective and long-lasting, allowing once-a-day administration.

Adults and children over 12 years of age: One Loratadine tablet once daily. It is usually administered in the morning or when symptoms require treatment.

Children 2-12 years: Body weight over 30 kg: one Loratadine tablet once daily, below 30 kg: half Loratadine tablet once daily.

Below 2 years of age: Loratadine tablet is not recommended for use below 2 years of age since safety and efficacy has not been established.

During controlled clinical studies the incidence of adverse events, including sedation and anticholinergic effects observed with 10 mg Loratadine was comparable to that observed with placebo. Studies on the effect of Loratadine on actual driving performance, and on tests of cognitive and psychomotor functioning have shown it to be comparable to placebo.

Loratadine is contraindicated in patients who have shown hypersensitivity or idiosyncrasy to their components.

Caution should be taken in patients with liver impairment or renal insufficiency (eGFR <30 ml/min).

There are no reports of potentially hazardous interactions with other drugs. In contrast to many other histamine H1 receptor antagonists, Loratadine has no potentiating effects when administered concurrently with alcohol, as measured by psychomotor performance studies. Concomitant therapy with drugs that inhibit or are metabolized by hepatic cytochromes P450 3A4 and 2D6 may elevate plasma concentrations of either drug and this mayifesult in adverse effects. Cimetidine inhibits both enzymes while erythromycin or ketoconazole inhibits P450 3A4. These drugs increase loratadine serum concentrations but no adverse effects are reported.

There is no experience of the use of Loratadine in human pregnancy. Therefore its use during pregnancy is not advisable. Loratadine is excreted in breast milk in a very small amount. So nursing mothers are advised not to take the drug.

In adults somnolence, tachycardia and headache have been reported with overdose greater than 10 mg. Extrapyramidal signs and palpitations have been reported in children with overdoses of greater than 10 mg. In the event of overdosage, general symptomatic and supportive measures should be instituted promptly and maintained for as long as necessary. It would seem reasonable to treat patients presenting early after large overdoses with oral activated charcoal. The conscious patients may be induced to vomit or gastric lavage may be performed.

Keep in a dry place away from light and heat. Keep out of the reach of children.

Cefaclor is indicated in the treatment of the following infections: Otitis media, Lower respiratory tract infections, including pneumonia, bronchitis and acute exacerbation of chronic bronchitis, Upper respiratory tract infections, including pharyngitis and tonsillitis, Urinary tract infections, including pyelonephritis and cystitis, Skin and soft tissue infections, Sinusitis

Second generation Cephalosporins

Cefaclor is a second generation cephalosporin antibiotic which has stability against b-lactamase inactivation and possesses a broad spectrum of activity. Cefaclor is active against the following organisms in vitro: Alpha and beta haemolytic Streptococci, Staphylococci; including coagulase-positive, coagulase negative and penicillinase-producing strains, Streptococcus pneumoniae, Streptococcus pyogenes (Group A b-haemolytic Streptococci), Branhamella catarrhalis, Escherichia coli, Proteus mirabilis, Klebsiella species Haemophilus influenzae, including ampicillin-resistant strains. Cefaclor is generally effective in the eradication of Streptococci from the nasopharynx.

Adult-

• Usual dose: 250 mg 8 hrly.
• Bronchitis & pneumonia: 250 mg tid.
• Sinusitis: 500 mg tid for 10 days.
• Pneumonia & other more severe infections: Max: 4 gm/day for 28 days.
• Acute gonococcal urethritis: 3 gm as a single dose combined with probenecid 1 gm.

Children- 

• Recommended dose: 20 mg/kg/day in divided doses 8 hrly.
• Bronchitis & pneumonia: 20 mg/kg/day in divided doses tid.
• Serious infections, sinusitis, otitis media & infections: caused by less susceptible organisms 40 mg/kg/day in divided doses. Max: 1 gm/day.

May be taken with or without food.

Gastro-intestinal: Diarrhoea, nausea and vomiting have been reported. Hypersensitivity: Allergic reactions such as eruptions, pruritis and urticaria have been observed. These reactions usually subside upon discontinuation of therapy. Serum sickness like reactions have been reported.

Haematological: Eosinophilia, thrombocytopenia, transient lymphocytosis and leucopenia may occur rarely. Hepatic: Transient hepatitis and cholestatic jaundice, slight elevation in AST, ALT or alkaline phosphate values have been reported rarely.

Renal: Reversible interstitial nephritis has occurred rarely, also slight elevations in blood urea or serum creatinine or abnormal urinalysis.

Central Nervous System: Reversible hyperactivity, nervousness, confusion, hypertonia, dizziness, hallucinations and somnolence have been reported rarely.

Cefaclor is contraindicated in patients with known allergy to the Cephalosporin group of antibiotics.

Cefaclor should be administered with caution in the presence of markedly impaired renal function. Dosage adjustments for patients with moderate or severe renal impairment are not usually required.

The nephrotoxicity of aminoglycoside antibiotics such as gentamicin and tobramicin may be enhanced by any cephalosporin. Therefore, one should be cautious in concomitant use of these categories of drugs.

There are no adequate and well-controlled studies in pregnant women. This drug should be used during pregnancy only if clearly needed. Small amounts of Cefaclor have been detected in mother's milk. The effect on nursing infants is not known. Caution should be exercised when Cefaclor is administered to a nursing woman.

Symptoms: Nausea, vomiting, epigastric distress and diarrhoea would be anticipated.

Treatment: Unless 5 times the normal total daily dose has been ingested, gastrointestinal decontamination will not be necessary. General management may consist of supportive therapy.

Store in a cool and dry place. Protect from light.

Cefaclor is indicated in the treatment of the following infections: Otitis media, Lower respiratory tract infections, including pneumonia, bronchitis and acute exacerbation of chronic bronchitis, Upper respiratory tract infections, including pharyngitis and tonsillitis, Urinary tract infections, including pyelonephritis and cystitis, Skin and soft tissue infections, Sinusitis

Second generation Cephalosporins

Cefaclor is a second generation cephalosporin antibiotic which has stability against b-lactamase inactivation and possesses a broad spectrum of activity. Cefaclor is active against the following organisms in vitro: Alpha and beta haemolytic Streptococci, Staphylococci; including coagulase-positive, coagulase negative and penicillinase-producing strains, Streptococcus pneumoniae, Streptococcus pyogenes (Group A b-haemolytic Streptococci), Branhamella catarrhalis, Escherichia coli, Proteus mirabilis, Klebsiella species Haemophilus influenzae, including ampicillin-resistant strains. Cefaclor is generally effective in the eradication of Streptococci from the nasopharynx.

Adult-

• Usual dose: 250 mg 8 hrly.
• Bronchitis & pneumonia: 250 mg tid.
• Sinusitis: 500 mg tid for 10 days.
• Pneumonia & other more severe infections: Max: 4 gm/day for 28 days.
• Acute gonococcal urethritis: 3 gm as a single dose combined with probenecid 1 gm.

Children- 

• Recommended dose: 20 mg/kg/day in divided doses 8 hrly.
• Bronchitis & pneumonia: 20 mg/kg/day in divided doses tid.
• Serious infections, sinusitis, otitis media & infections: caused by less susceptible organisms 40 mg/kg/day in divided doses. Max: 1 gm/day.

May be taken with or without food.

Gastro-intestinal: Diarrhoea, nausea and vomiting have been reported. Hypersensitivity: Allergic reactions such as eruptions, pruritis and urticaria have been observed. These reactions usually subside upon discontinuation of therapy. Serum sickness like reactions have been reported.

Haematological: Eosinophilia, thrombocytopenia, transient lymphocytosis and leucopenia may occur rarely. Hepatic: Transient hepatitis and cholestatic jaundice, slight elevation in AST, ALT or alkaline phosphate values have been reported rarely.

Renal: Reversible interstitial nephritis has occurred rarely, also slight elevations in blood urea or serum creatinine or abnormal urinalysis.

Central Nervous System: Reversible hyperactivity, nervousness, confusion, hypertonia, dizziness, hallucinations and somnolence have been reported rarely.

Cefaclor is contraindicated in patients with known allergy to the Cephalosporin group of antibiotics.

Cefaclor should be administered with caution in the presence of markedly impaired renal function. Dosage adjustments for patients with moderate or severe renal impairment are not usually required.

The nephrotoxicity of aminoglycoside antibiotics such as gentamicin and tobramicin may be enhanced by any cephalosporin. Therefore, one should be cautious in concomitant use of these categories of drugs.

There are no adequate and well-controlled studies in pregnant women. This drug should be used during pregnancy only if clearly needed. Small amounts of Cefaclor have been detected in mother's milk. The effect on nursing infants is not known. Caution should be exercised when Cefaclor is administered to a nursing woman.

Symptoms: Nausea, vomiting, epigastric distress and diarrhoea would be anticipated.

Treatment: Unless 5 times the normal total daily dose has been ingested, gastrointestinal decontamination will not be necessary. General management may consist of supportive therapy.

Store in a cool and dry place. Protect from light.

Anti-histamine & decongestant

Loratadine is a non-sedative histamine H1-receptor antagonist with anti-allergic properties. Loratadine is a long acting tricyclic anti-histamine with selective peripheral H1-receptor antagonistic activity and no central sedative or anti-cholinergic effect.

Pseudoephedrine is an orally active sympathomimetic amine and exerts a decongestant action on the nasal mucosa. This is recognized as an effective agent for the relief of nasal congestion due to allergic rhinitis. It has nasal and bronchial decongestant activity. Pseudoephedrine is both an α-and β-adrenergic receptor agonist. It causes vasoconstriction via direct stimulation of α-adrenergic receptors of the respiratory mucosa. It also directly stimulates β-adrenergic receptors causing bronchial relaxation, increased heart rate and contractility.

Adults and children over 12 years:

• 5/120 tablet: One tablet twice daily (every 12 hours)
• 10/240 tablet: One tablet once daily and to be taken in the morning instead of night.

Patients with renal insufficiency (GFR<30 ml/min) should be given a lower initial dose (one 5/120 tablet per day, or one 10/240 tablet every alternate day) because they have reduced clearance of Loratadine and Pseudoephedrine.

Patients who have a history of difficulty in swallowing tablets or who have known upper gastrointestinal narrowing or abnormal esophageal peristalsis should not use 10/240 tablet.

Paediatric use: Safety and effectiveness in children below the age of 12 years have not been established.

Use in patients approximately 60 years of age and older: The safety and efficacy of this tablet in patients greater than 60 years old have not been investigated in placebo-controlled clinical trials. The elderly is more likely to have adverse reactions to sympathomimetic amines.

Loratadine & Pseudoephedrine tablet should be administered when both the antihistaminic properties of Loratadine and the nasal decongestant activity of Pseudoephedrine Sulfate are desired in patients 12 years of age and older.

In general it is well tolerated. Clinical trial suggests a very low of adverse effects commonly reported is dry mouth, somnolence, insomnia, pharyngitis, dizziness, coughing, fatigue, nausea, nervousness, anorexia, dysmenorrheal and headache. Other less common side effects may include; increased sweating, thirst, back pain, chest pain, malaise, palpitations, hypertension, tachycardia, abdominal distension, altered taste, flatulence, myalgia, dry throat, agitation, micturation frequency etc.

This tablet is contraindicated in patients who are hypersensitive to any component of this product.

This tablet should generally be avoided in patients with hepatic insufficiency. Patients with renal insufficiency should be given a lower initial dose because they have reduced clearance of Loratadine and Pseudoephedrine. As because the doses of this fixed combination product cannot be individually titrated and hepatic insufficiency results in a reduced clearance of Loratadine to a much greater extent than Pseudoephedrine.

This tablet should be used with caution in patients with hypertension, diabetes mellitus, ischemic heart disease, increased intraocular pressure, hyperthyroidism, renal impairment, or with accompanying hypotension may be produced by sympathomimetic amines.

This tablet is contraindicated in patients taking monoamino oxidase (MAO) inhibitors and for 2 weeks after stopping use of an MAO inhibitor. The antihypertensive effects of beta-adrenergic blocking agents, methyldopa, reserpine and veaturm alkaloids may be reduced by sympathomimetics. Increased ectopic pacemaker activity can occur when Pseudoephedrine is used concomitantly with digitalis. Concomitantly administration of Erythromycin, Ketoconazole and Cimetidine increases plasma concentration of both Loratadine and Decarboethoxyloratadine. But there were no clinically relevant changes in the safety profile of Loratadine.

Pregnancy category B: no evidence of risk in human is reported. It is not known if this combination product is excreted in human milk. However, both Loratadine and Pseudoephedrine when administered alone passed into breast milk, so it should not be administered to lactating mothers.

In the event of overdosage, general symptomatic and supportive measure should be instituted promptly and maintained for as long as necessary. Treatment of overdose would reasonably consist of emesis (ipecac syrup), except in patients with impaired consciousness, followed by the administration of activated charcoal to absorb any remaining drug. If vomiting is unsuccessful or contraindicated, gastric lavage should be performed with normal saline.

Store at a cool and dry place, away from light. Keep out of the reach of children.

Non-sedating antihistamines

Desloratadine, the major active metabolite of Loratadine, is a non-sedating; long acting tricyclic histamine antagonist with selective H1-receptor histamine antagonist activity. Desloratadine also inhibits histamine release from human mast cell.

Pediatric drops:

• Child 6-11 months of age: 2 ml drops once daily.
• Child 1-2 years of age: 2.5 ml drops once daily.

Syrup:

• Child 6-11 months of age: 2 ml once daily.
• Child 1-5 years of age: 2.5 ml once daily.
• Child 6-11 years of age: 5 ml once daily.
• Adults & >12 years of age: 10 ml once daily.

Tablet:

• Adults and children 12 years of age and over: 1 tablet daily

Less common side effects may include headache, nausea, fatigue, dizziness, pharyngitis, dyspepsia and myalgia.

Desloratadine is contraindicated in patients having hypersensitivity to this medication or to any of its ingredients or Loratadine.

In adult patients with liver or renal impairment: A starting dose of one 5 mg tablet every other day is recommended based on pharmacokinetic data. If the patient has medical or familial history of seizures.

No clinically relevant drug interactions have been reported.

Pregnancy Category C. The safe use of Desloratadine during pregnancy has not been established. Therefore, Desloratadine is not to be used during pregnancy unless clearly indicated. Desloratadine passes into breast milk, therefore a decision should be made whether to discontinue nursing or to discontinue Desloratadine taking into account the importance of the drug to the mother.

Recommended in the use in children & adolescents.

No clinically relevant adverse effects have been reported.

Store in a cool & dry place, protected from light. Store below 30°C. Keep all medicines out of the reach of children.

Non-sedating antihistamines

Desloratadine, the major active metabolite of Loratadine, is a non-sedating; long acting tricyclic histamine antagonist with selective H1-receptor histamine antagonist activity. Desloratadine also inhibits histamine release from human mast cell.

Pediatric drops:

• Child 6-11 months of age: 2 ml drops once daily.
• Child 1-2 years of age: 2.5 ml drops once daily.

Syrup:

• Child 6-11 months of age: 2 ml once daily.
• Child 1-5 years of age: 2.5 ml once daily.
• Child 6-11 years of age: 5 ml once daily.
• Adults & >12 years of age: 10 ml once daily.

Tablet:

• Adults and children 12 years of age and over: 1 tablet daily

Less common side effects may include headache, nausea, fatigue, dizziness, pharyngitis, dyspepsia and myalgia.

Desloratadine is contraindicated in patients having hypersensitivity to this medication or to any of its ingredients or Loratadine.

In adult patients with liver or renal impairment: A starting dose of one 5 mg tablet every other day is recommended based on pharmacokinetic data. If the patient has medical or familial history of seizures.

No clinically relevant drug interactions have been reported.

Pregnancy Category C. The safe use of Desloratadine during pregnancy has not been established. Therefore, Desloratadine is not to be used during pregnancy unless clearly indicated. Desloratadine passes into breast milk, therefore a decision should be made whether to discontinue nursing or to discontinue Desloratadine taking into account the importance of the drug to the mother.

Recommended in the use in children & adolescents.

No clinically relevant adverse effects have been reported.

Store in a cool & dry place, protected from light. Store below 30°C. Keep all medicines out of the reach of children.

Loperamide Hydrochloride is indicated in-

• Acute diarrhea
• Chronic diarrhea
• Abdominal cramps associated with diarrhea
• Crohn's disease
• Postgastric surgery
• Ulcerative colitis.

Anti-diarrhoeal, Anti-motility drugs

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.

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.

Chronic diarrhea-

• Adults: 2-4 capsules daily in divided doses, depending on severity.
• Children: 1-2 capsules daily, depending on severity. Or directed by physician.

Abdominal pain and other gastrointestinal disturbances including dry mouth, dizziness, fatigue and skin rashes etc. have been reported.

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.

Loperamide Hydrochloride must be used with caution in cases of severe hepatic disturbance.

There are no data available.

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.

Overdosage of Loperamide may result in constipation, CNS depression, and nausea.

Keep all medicines out of reach of children. Store in a cool and dry place protected from light.

Benzodiazepine hypnotics, Benzodiazepine sedatives

Lorazepam is a short-acting tranquilizer of the benzodiazepine group. It is an agonist at benzodiazepine receptors in the CNS. It exerts a depressant action on the CNS, which may be mediated by potentiating the inhibitory actions of GABA (gamma amino butyric acid) in the CNS. This will result in diminution of the ascending activating systems, particularly the serotonergic and noradrenergic pathway from brain stem or the mid-brain to the cerebral cortex.

Lorazepam is administered orally. For optimal results; dose, frequency of administration and duration of therapy should be individualized according to patient's response.

• The usual range is 2 to 6 mg/day given in divided doses, the largest dose being taken before bedtime, but the largest dosage may vary from 1 to 10 mg/day.
• For anxiety, most patients require an initial dose of 2 to 3 mg/day given b.i.d. or t.i.d.
• For elderly or debilitated patients, an initial dosage of 1 to 2 mg/day in divided doses is recommended, to be adjusted as needed and tolerated.
• For insomnia 1 to 2 mg before bedtime and as premedicant 1 to 2 mg the night before surgery and 1 to 2 hour before surgery.

Lorazepam injection can be given intravenously or intramuscularly. Premedication (Adults): 0.05 mg/kg (3.5 mg for average 70 kg person) (For IV 30-45 minutes before & IM 60-90 minutes before); Acute anxiety (Adults): 0.025-0.03 mg/kg (1.75-2.1 mg for an average 70 kg person), Repeat 6 hourly; Status epilepticus (Adults): 4 mg intravenously; Status epilepticus (Children): 2 mg intravenously.

For IM use, undiluted Lorazepam injection should be administered. For IV use, it must be diluted with an equal volume of compatible solutions e.g. Sterile Water for Injection, Sodium Chloride Injection, 5% Dextrose Injection. The rate of injection should not exceed 2 mg per minute.

Adverse reactions are usually observed at the beginning of therapy and generally disappeared on continued medication or upon decreasing the dose. The most frequent adverse reactions of Lorazepam are sedation followed by dizziness, weakness and unsteadiness. Less frequent adverse reactions are disorientation, depression, nausea, change in appetite, headache, sleep disturbance, agitation, dermatological symptoms, eye-function disturbance, together with various gastrointestinal symptoms and autonomic manifestations.

Lorazepam should not be given to patients with a previous sensitivity to benzodiazepines or with acute narrow-angle glaucoma and myasthenia gravis.

In patients with depression accompanying anxiety, a possibility for suicide should be borne in mind. For elderly or debilitated patients, the initial daily dosage should not exceed 2 mg in order to avoid over sedation. The usual precautions for treating patients with impaired renal or hepatic function and with acute and chronic pulmonary insufficiency should be observed. Use of Lorazepam for prolonged period and gastric patients requires caution and there should be frequent monitoring for symptoms of upper gastrointestinal disease. Machineries should be avoided during taking Lorazepam.

Lorazepam may potentiate the central depressant effect when combined with other drugs with central depressant action. Such drugs include alcohol, general anesthetics, tricyclic antidepressants and monoamine oxidase inhibitors.

Safety of Lorazepam in pregnancy has not been established. Because the use of this drug is rarely a matter of urgency, the use of Lorazepam during this period should almost always be avoided.

It is not known whether oral Lorazepam is excreted in human milk like other benzodiazepine tranquilizers. As a general rule, nursing should not be undertaken while a patient is on a drug since many drugs are excreted in human milk.

Overdosage of Lorazepam is usually manifested by varying degrees of central nervous system depression ranging from drowsiness to coma. In mild cases, symptoms include drowsiness, mental confusion and lethargy. In more serious cases and especially when other drugs or alcohol were ingested, symptoms may include ataxia, hypotonia, hypotension, hypnotic states (stages I to III), coma.

Store between 20-25°C

Non-sedating antihistamines

This tablet is a preparation of Loratadine. Loratadine is a non-sedative histamine Hr receptor antagonist with antiallergic properties. Loratadine is a long-acting tricyclic antihistamine with selective peripheral Hi-receptor antagonistic activity and no central sedative or anticholinergic effect. It is rapidly effective and long-lasting, allowing once-a-day administration.

Adults and children over 12 years of age: One Loratadine tablet once daily. It is usually administered in the morning or when symptoms require treatment.

Children 2-12 years: Body weight over 30 kg: one Loratadine tablet once daily, below 30 kg: half Loratadine tablet once daily.

Below 2 years of age: Loratadine tablet is not recommended for use below 2 years of age since safety and efficacy has not been established.

During controlled clinical studies the incidence of adverse events, including sedation and anticholinergic effects observed with 10 mg Loratadine was comparable to that observed with placebo. Studies on the effect of Loratadine on actual driving performance, and on tests of cognitive and psychomotor functioning have shown it to be comparable to placebo.

Loratadine is contraindicated in patients who have shown hypersensitivity or idiosyncrasy to their components.

Caution should be taken in patients with liver impairment or renal insufficiency (eGFR <30 ml/min).

There are no reports of potentially hazardous interactions with other drugs. In contrast to many other histamine H1 receptor antagonists, Loratadine has no potentiating effects when administered concurrently with alcohol, as measured by psychomotor performance studies. Concomitant therapy with drugs that inhibit or are metabolized by hepatic cytochromes P450 3A4 and 2D6 may elevate plasma concentrations of either drug and this mayifesult in adverse effects. Cimetidine inhibits both enzymes while erythromycin or ketoconazole inhibits P450 3A4. These drugs increase loratadine serum concentrations but no adverse effects are reported.

There is no experience of the use of Loratadine in human pregnancy. Therefore its use during pregnancy is not advisable. Loratadine is excreted in breast milk in a very small amount. So nursing mothers are advised not to take the drug.

In adults somnolence, tachycardia and headache have been reported with overdose greater than 10 mg. Extrapyramidal signs and palpitations have been reported in children with overdoses of greater than 10 mg. In the event of overdosage, general symptomatic and supportive measures should be instituted promptly and maintained for as long as necessary. It would seem reasonable to treat patients presenting early after large overdoses with oral activated charcoal. The conscious patients may be induced to vomit or gastric lavage may be performed.

Keep in a dry place away from light and heat. Keep out of the reach of children.

Non-sedating antihistamines

This tablet is a preparation of Loratadine. Loratadine is a non-sedative histamine Hr receptor antagonist with antiallergic properties. Loratadine is a long-acting tricyclic antihistamine with selective peripheral Hi-receptor antagonistic activity and no central sedative or anticholinergic effect. It is rapidly effective and long-lasting, allowing once-a-day administration.

Adults and children over 12 years of age: One Loratadine tablet once daily. It is usually administered in the morning or when symptoms require treatment.

Children 2-12 years: Body weight over 30 kg: one Loratadine tablet once daily, below 30 kg: half Loratadine tablet once daily.

Below 2 years of age: Loratadine tablet is not recommended for use below 2 years of age since safety and efficacy has not been established.

During controlled clinical studies the incidence of adverse events, including sedation and anticholinergic effects observed with 10 mg Loratadine was comparable to that observed with placebo. Studies on the effect of Loratadine on actual driving performance, and on tests of cognitive and psychomotor functioning have shown it to be comparable to placebo.

Loratadine is contraindicated in patients who have shown hypersensitivity or idiosyncrasy to their components.

Caution should be taken in patients with liver impairment or renal insufficiency (eGFR <30 ml/min).

There are no reports of potentially hazardous interactions with other drugs. In contrast to many other histamine H1 receptor antagonists, Loratadine has no potentiating effects when administered concurrently with alcohol, as measured by psychomotor performance studies. Concomitant therapy with drugs that inhibit or are metabolized by hepatic cytochromes P450 3A4 and 2D6 may elevate plasma concentrations of either drug and this mayifesult in adverse effects. Cimetidine inhibits both enzymes while erythromycin or ketoconazole inhibits P450 3A4. These drugs increase loratadine serum concentrations but no adverse effects are reported.

There is no experience of the use of Loratadine in human pregnancy. Therefore its use during pregnancy is not advisable. Loratadine is excreted in breast milk in a very small amount. So nursing mothers are advised not to take the drug.

In adults somnolence, tachycardia and headache have been reported with overdose greater than 10 mg. Extrapyramidal signs and palpitations have been reported in children with overdoses of greater than 10 mg. In the event of overdosage, general symptomatic and supportive measures should be instituted promptly and maintained for as long as necessary. It would seem reasonable to treat patients presenting early after large overdoses with oral activated charcoal. The conscious patients may be induced to vomit or gastric lavage may be performed.

Keep in a dry place away from light and heat. Keep out of the reach of children.

Non-sedating antihistamines

This tablet is a preparation of Loratadine. Loratadine is a non-sedative histamine Hr receptor antagonist with antiallergic properties. Loratadine is a long-acting tricyclic antihistamine with selective peripheral Hi-receptor antagonistic activity and no central sedative or anticholinergic effect. It is rapidly effective and long-lasting, allowing once-a-day administration.

Adults and children over 12 years of age: One Loratadine tablet once daily. It is usually administered in the morning or when symptoms require treatment.

Children 2-12 years: Body weight over 30 kg: one Loratadine tablet once daily, below 30 kg: half Loratadine tablet once daily.

Below 2 years of age: Loratadine tablet is not recommended for use below 2 years of age since safety and efficacy has not been established.

During controlled clinical studies the incidence of adverse events, including sedation and anticholinergic effects observed with 10 mg Loratadine was comparable to that observed with placebo. Studies on the effect of Loratadine on actual driving performance, and on tests of cognitive and psychomotor functioning have shown it to be comparable to placebo.

Loratadine is contraindicated in patients who have shown hypersensitivity or idiosyncrasy to their components.

Caution should be taken in patients with liver impairment or renal insufficiency (eGFR <30 ml/min).

There are no reports of potentially hazardous interactions with other drugs. In contrast to many other histamine H1 receptor antagonists, Loratadine has no potentiating effects when administered concurrently with alcohol, as measured by psychomotor performance studies. Concomitant therapy with drugs that inhibit or are metabolized by hepatic cytochromes P450 3A4 and 2D6 may elevate plasma concentrations of either drug and this mayifesult in adverse effects. Cimetidine inhibits both enzymes while erythromycin or ketoconazole inhibits P450 3A4. These drugs increase loratadine serum concentrations but no adverse effects are reported.

There is no experience of the use of Loratadine in human pregnancy. Therefore its use during pregnancy is not advisable. Loratadine is excreted in breast milk in a very small amount. So nursing mothers are advised not to take the drug.

In adults somnolence, tachycardia and headache have been reported with overdose greater than 10 mg. Extrapyramidal signs and palpitations have been reported in children with overdoses of greater than 10 mg. In the event of overdosage, general symptomatic and supportive measures should be instituted promptly and maintained for as long as necessary. It would seem reasonable to treat patients presenting early after large overdoses with oral activated charcoal. The conscious patients may be induced to vomit or gastric lavage may be performed.

Keep in a dry place away from light and heat. Keep out of the reach of children.

Non-sedating antihistamines

This tablet is a preparation of Loratadine. Loratadine is a non-sedative histamine Hr receptor antagonist with antiallergic properties. Loratadine is a long-acting tricyclic antihistamine with selective peripheral Hi-receptor antagonistic activity and no central sedative or anticholinergic effect. It is rapidly effective and long-lasting, allowing once-a-day administration.

Adults and children over 12 years of age: One Loratadine tablet once daily. It is usually administered in the morning or when symptoms require treatment.

Children 2-12 years: Body weight over 30 kg: one Loratadine tablet once daily, below 30 kg: half Loratadine tablet once daily.

Below 2 years of age: Loratadine tablet is not recommended for use below 2 years of age since safety and efficacy has not been established.

During controlled clinical studies the incidence of adverse events, including sedation and anticholinergic effects observed with 10 mg Loratadine was comparable to that observed with placebo. Studies on the effect of Loratadine on actual driving performance, and on tests of cognitive and psychomotor functioning have shown it to be comparable to placebo.

Loratadine is contraindicated in patients who have shown hypersensitivity or idiosyncrasy to their components.

Caution should be taken in patients with liver impairment or renal insufficiency (eGFR <30 ml/min).

There are no reports of potentially hazardous interactions with other drugs. In contrast to many other histamine H1 receptor antagonists, Loratadine has no potentiating effects when administered concurrently with alcohol, as measured by psychomotor performance studies. Concomitant therapy with drugs that inhibit or are metabolized by hepatic cytochromes P450 3A4 and 2D6 may elevate plasma concentrations of either drug and this mayifesult in adverse effects. Cimetidine inhibits both enzymes while erythromycin or ketoconazole inhibits P450 3A4. These drugs increase loratadine serum concentrations but no adverse effects are reported.

There is no experience of the use of Loratadine in human pregnancy. Therefore its use during pregnancy is not advisable. Loratadine is excreted in breast milk in a very small amount. So nursing mothers are advised not to take the drug.

In adults somnolence, tachycardia and headache have been reported with overdose greater than 10 mg. Extrapyramidal signs and palpitations have been reported in children with overdoses of greater than 10 mg. In the event of overdosage, general symptomatic and supportive measures should be instituted promptly and maintained for as long as necessary. It would seem reasonable to treat patients presenting early after large overdoses with oral activated charcoal. The conscious patients may be induced to vomit or gastric lavage may be performed.

Keep in a dry place away from light and heat. Keep out of the reach of children.

Non-sedating antihistamines

This tablet is a preparation of Loratadine. Loratadine is a non-sedative histamine Hr receptor antagonist with antiallergic properties. Loratadine is a long-acting tricyclic antihistamine with selective peripheral Hi-receptor antagonistic activity and no central sedative or anticholinergic effect. It is rapidly effective and long-lasting, allowing once-a-day administration.

Adults and children over 12 years of age: One Loratadine tablet once daily. It is usually administered in the morning or when symptoms require treatment.

Children 2-12 years: Body weight over 30 kg: one Loratadine tablet once daily, below 30 kg: half Loratadine tablet once daily.

Below 2 years of age: Loratadine tablet is not recommended for use below 2 years of age since safety and efficacy has not been established.

During controlled clinical studies the incidence of adverse events, including sedation and anticholinergic effects observed with 10 mg Loratadine was comparable to that observed with placebo. Studies on the effect of Loratadine on actual driving performance, and on tests of cognitive and psychomotor functioning have shown it to be comparable to placebo.

Loratadine is contraindicated in patients who have shown hypersensitivity or idiosyncrasy to their components.

Caution should be taken in patients with liver impairment or renal insufficiency (eGFR <30 ml/min).

There are no reports of potentially hazardous interactions with other drugs. In contrast to many other histamine H1 receptor antagonists, Loratadine has no potentiating effects when administered concurrently with alcohol, as measured by psychomotor performance studies. Concomitant therapy with drugs that inhibit or are metabolized by hepatic cytochromes P450 3A4 and 2D6 may elevate plasma concentrations of either drug and this mayifesult in adverse effects. Cimetidine inhibits both enzymes while erythromycin or ketoconazole inhibits P450 3A4. These drugs increase loratadine serum concentrations but no adverse effects are reported.

There is no experience of the use of Loratadine in human pregnancy. Therefore its use during pregnancy is not advisable. Loratadine is excreted in breast milk in a very small amount. So nursing mothers are advised not to take the drug.

In adults somnolence, tachycardia and headache have been reported with overdose greater than 10 mg. Extrapyramidal signs and palpitations have been reported in children with overdoses of greater than 10 mg. In the event of overdosage, general symptomatic and supportive measures should be instituted promptly and maintained for as long as necessary. It would seem reasonable to treat patients presenting early after large overdoses with oral activated charcoal. The conscious patients may be induced to vomit or gastric lavage may be performed.

Keep in a dry place away from light and heat. Keep out of the reach of children.