Levamlodipine Maleate

Levamlodipine is used to treat hypertension, to lower blood pressure, in adults and in children aged 6 years and older. Amlodipine is a dihydropyridine calcium antagonist (also called a calcium ion antagonist or slow channel blocker). It stops calcium ions from moving across the cell membrane into vascular smooth muscle and cardiac muscle. This effect is selective, and it is greater on vascular smooth muscle cells than on cardiac muscle cells. Amlodipine is a 1:1 racemic mixture of levamlodipine and dextro amlodipine, and levamlodipine has been shown to be the pharmacologically active, anti-hypertensive isomer.

Absorption: Taken by mouth, levamlodipine has a Tmax of 6 to 12 h and a bioavailability of 64 to 90%. Food does not significantly affect its absorption.

Distribution: The volume of distribution of levamlodipine is similar to that of amlodipine, which is 21 L/kg.

Metabolism and Excretion: About 90% of levamlodipine is metabolized to inactive metabolites. Tests with liver microsomes showed that this metabolism is mainly mediated by CYP3A4. The derivative can be oxidatively deaminated or O-dealkylated further, but it doesn't seem to undergo O-demethylation the way racemic amlodipine does. Levamlodipine is 60% eliminated in urine, and 10% is eliminated as the unmetabolized drug.