Prozart Advance Mechanism of Action

Pharmacotherapeutic Group: Vasodilators, hypotensive medicines.
Pharmacology: Pharmacokinetics: Absorption: Amlodipine: Plasma levels peak 6-12 hr after oral administration; 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. Losartan is metabolised to an active carboxylic acid metabolite E-3174 (EXP-3174), which has greater pharmacological activity than Losartan; some inactive metabolites are also formed.
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 hrs. Losartan and its active metabolites: Biliary excretion; terminal half-life: About 2 hr (Losartan) and 6-9 hr (metabolites).