Amlosar

Each film coated tablet contains: Losartan potassium USP 50 mg, amlodipine besilate BP eq to amlodipine 5 mg.

Pharmacological classification: Angiotensin II receptor blocker/calcium channel blocker.
Pharmacology: Amlodipine inhibits the movement of Ca ions across the cell membrane into vascular smooth muscles and myocytes. Action is greater in the arterial resistant vessels causing peripheral vasodilatation and reduction in afterload. Losartan is an angiotensin II receptor (type At1) antagonists antihypertensive which acts by blocking the actions of angiotensin II of renin-angiotensin-aldosterone system. The drug and its active metabolite selectively block the vasoconstrictor and aldosterone secreting effects of angiotensin II by selectively antagonising the binding of angiotensin II to At1 receptors.
Pharmacokinetics: Absorption: Amlodipine: Plasma levels peak 6-12 hr after oral admin; absolute bioavailability is estimated to be 64-90%. Losartan: Well absorbed; undergoes substantial 1st pass metabolism by CYP450 enzymes; systemic bioavailability is about 33%; about 14% of an oral dose is converted to active metabolites.
Distribution: Amlodipine: 93% bound to plasma proteins.
Losartan and its active metabolites: Highly bound to plasma proteins, mainly albumin.
Metabolism: Amlodipine: About 90% converted to inactive metabolites hepatically.
Excretion: Amlodipine: 10% of parent compound and 60% of the metabolites are removed in the urine; elimination from the plasma is biphasic with terminal half-life of about 30-50 hr.
Losartan and its active metabolites: Biliary excretion; terminal half-life: About 2 hr (losartan) and 6-9 hr (metabolites).

Treatment of mild to moderate hypertension. It is also indicated in hypertension not responding to monotherapy.

The recommended initial dose is 1 tab/day; it may be increased up to 2 tab/day.

Known hypersensitivity. Avoid concomitant K supplements. Pregnancy.

Caution should be exercised in patients with history of impaired liver or kidney function, heart failure, poor blood circulation, sick-sinus syndrome, severe ventricular dysfunction, elderly, children, during pregnancy and lactation.
It may cause dizziness, do not drive a car or operate machinery while taking this medication.
Monitor serum potassium concentration.
Avoid excess dosage.

Heart: Low blood pressure.
Central nervous System: Headache, dizziness, weakness, fatigue.
Musculoskeletal: Back pain, muscle pain.
Gastrointestinal: GI disturbances, transient elevation of liver enzymes; taste disturbances.
Miscellaneous: Respiratory tract disorders, cough, rash, allergic reactions.

Amlodipine: Increased metabolism with rifampin. Reduced hypotensive effect with calcium. Potentiates effects of thiazide diuretics and ACE inhibitors. Avoid combination with β-blockers in patients with markedly impaired left ventricular function.
Losartan: Concurrent use with NSAIDs may further worsen renal function.
Cimetidine may increase the AUC of losartan by about 18%. Phenobarbital and other enzyme inducers may decrease levels of losartan and its active metabolite.
Ketoconazole inhibits the conversion of losartan to its active metabolite. Concurrent use with potassium-sparing diuretics or potassium supplements or salt substitutes containing potassium may increase serum potassium levels.
Reduces lithium excretion; monitor lithium levels if used together.

Store at temperatures not exceeding 30°C.

Angiotensin II Antagonists / Calcium Antagonists

C09DB06 - losartan and amlodipine ; Belongs to the class of angiotensin II receptor blockers (ARBs) and calcium channel blockers. Used in the treatment of cardiovascular disease.

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