Amlopress 5: Each tablet contains amlodipine besylate equivalent to amlodipine 5 mg.
Amlopress 10: Each tablet contains Amlodipine besylate equivalent to amlodipine 10 mg.
Pharmacology: Pharmacodynamics: Mechanism of Action: Amlodipine is a calcium channel blockers (slow channel blockers, calcium antagonist), share the ability to inhibit movement of calcium ions across the cell membrane. The effects on the cardiovascular system include depression of mechanical contraction of myocardial and smooth muscle and depression of both impulse formation (automaticity) and conduction velocity.
Pharmacokinetics: Following oral administration of amlodipine besylate, peak plasma concentrations of the drug are attained within 6-12 hours. Absolute bioavailability ranges from 64-90%; food does not affect bioavailability of amlodipine. Amlodipine is approximately 93% bound to plasma proteins. The drug is extensively (approximately 90%) metabolized to inactive metabolites in the liver. Amlodipine is excreted in the urine as metabolites (60%) and unchanged drug (10%). The terminal elimination half-life is about 30-50 hours.
Hypertension: Amlodipine is indicated for the treatment of hypertension. Amlodipine may be used alone or in combination with other antihypertensive agents.
Coronary artery disease: Amlodipine is indicated to reduce the risk of coronary revascularization and the need for hospitalization due to angina in patient with coronary artery disease.
Chronic stable angina: Amlodipine is indicated for the first line treatment of myocardial ischemia, whether due to fixed obstruction (stable angina) and/or vasospasm/vasoconstriction (Prinzmetal's or variant angina) of coronary vasculature. Amlodipine may be used as monotherapy or in combination with other antianginal drugs.
Adult: Hypertension: The usual initial dose is 5 mg once daily which may be increased to a maximum dose of 10 mg once daily.
Coronary artery disease: 5-10 mg once daily.
Chronic stable angina: 5-10 mg once daily. Most patients will require 10 mg for adequate effect.
Children 6 - 17 years of age: Hypertension: 2.5-5 mg once daily.
Elderly: Hypertension: 2.5 mg once daily initially.
Chronic stable angina: 5 mg once daily.
Hepatic function impairment: Hypertension: 2.5 mg once daily initially. Titrate slowly in patients with severe hepatic impairment.
Chronic stable angina: 5 mg once daily.
Mode of Administration: Amlodipine besylate is administered orally. Amlodipine generally can be given without regard to meals.
Symptoms: Symptoms of overdosage include marked and prolonged hypotension and bradycardia, both of which may result in decreased cardiac output.
Treatment: If the patient is seen shortly after oral ingestion, employ lavage, activated charcoal, and cathartics. Treatment is supportive. Treat cardiac failure with inotropic agents (isoproterenol, dopamine, or dobutamine) and diuretics. In patients with hypertrophic cardiomyophathy, use alpha-adenergic agents (phenylephrine HCl or metaraminol bitartrate) to maintain blood pressure; avoid isoproterenol and norepinephine. Monitor cadiac and respiratory function; elevate the extremities. Because these agents are highly protein bound, dialysis is not likely to help.
Amlodipine is contraindicated in patients with known hypersensitivity to the drug or any ingredient in the formulation.
Symptomatic hypotension may occur in patients receiving amlodipine, particularly in individuals with severe aortic stenosis; however, acute hypotension is unlikely because of the gradual onset of action of the drug.
Worsening of angina or acute myocardial infarction can occur, particularly in patients with severe obstructive coronary artery disease, upon initiaton of amlodipine therapy or an increase in amlodipine dosage.
Use with caution in patients with hepatic impairment, amlodipine clearance is decreased and AUC is increased by about 40-60%. A reduced initial dosage of the drug is recommended, and subsequent dosage should be titrated slowly.
Use in Pregnancy: Pregnancy: Category C. Teratogenic and embryotoxic effects have been demonstrated in small animals, usually at doses higher than the usual human dosage. There are no well-controlled studies in pregnant women. Use during pregnancy only when clearly needed and when potential benefits outweigh potential hazards to the fetus.
Use in Lactation: It is not known if amlodipine is excreted in breast milk. Discontinue nursing while taking amlodipine.
Adverse effect reported in 1% or more of patients receiving amlodipine include edema, dizziness, flushing, palpitations, fatigue, nausea, abdominal pain, and somnolence. Edema, flushing, palpitations, and somnolence may occur more commonly in women than in men. Edema is dose related and may be less frequent with concomitant use of an angiotensin-converting enzyme (ACE) inhibitor or angiotensin II receptor antagonist.
Concomitant use of amlodipine with moderate (e.g., diltiazem) or potent (e.g., clarithromycin, itraconazole) inhibitors of cytochrome P-450 (CYP) 3A isoenzymes (CYP3A) results in increased systemic exposure to amlodipine. Reduction of amlodipine dosage may be necessary.
Concomitant administration of grapefruit juice with amlodipine did not alter systemic exposure to amlodipine.
Concomitant administration of amlodipine (multiple 10 mg) with simvastatin (80 mg) resulted in a 77% increase in simvastatin exposure compared with simvastatin alone. In patients receiving amlodipine, simvastatin dosage should not exceed 20 mg daily.
Concomitant use of CYP3A4 inducers (e.g., rifampicin, hypericum perforatum) may give a lower plasma concentration of amlodipine.
Concomitant use of alcohol with amlodipine did not alter systemic exposure to alcohol.
Concomitant administration of a magnesium- and aluminium antacid with amlodipine did not alter systemic exposure to amlodipine.
Concomitant administration of cimetidine with amlodipine did not alter systemic exposure to amlodipine.
Concomitant use of amlodipine with digoxin did not alter systemic exposure to digoxin.
Concomitant administration of amlodipine with atorvastatin did not alter systemic exposure to atorvastatin.
Concomitant administration of amlodipine with warfarin did not alter prothrombin time.
Store at temperature below 30°C.
C08CA01 - amlodipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
Amlopress 5: Tab 5 mg (octagon, flat, white, with one side has score and letter "LP" and "5" on each side and another side has letter "Rx") 10 x 10's, 50 x 10's.
Amlopress 10: Tab 10 mg (octagon, flat, white, with one side has score and letter "LP" and "10" on each side and another side has letter "Rx") 10 x 10's, 50 x 10's.