DESCRIPTION
Levamlodipine (INN), also known as levoamlodipine or S-amlodipine is a pharmacologically active enantiomer of amlodipine.
CATEGORIES
Amlodipine belongs to the dihydropyridine group of calcium channel blocker s.
CHEMICAL FORMULA
C20H25ClN2O5.
COMPOSITION
Amlodipine 2.5mg
INDICATION
it is used as an antihypertensive and antianginal agent.
MECHANISM
Amlodipine blocks the transmembrane influx of calcium into the vascular and cardiac smooth muscles resulting in vasodilation and hence a fall in blood pressure. Levamlodipine is an allosteric modulator and acts on the L-type of calcium channels.[4][5] Receptor binding studies have shown that out of the two forms only the (S)-enantiomer of amlodipine binds to and blocks L-type calcium channels whereas the (R)-enantiomer has no activity on these channels. The precise mechanisms by which levamlodipine relieves angina have not been fully explored, but are thought to include the following: Decreases peripheral resistance by arteriolar vasodilatation leading to the reduction in oxygen requirement and energy consumption of cardiac smooth muscles. Decreases coronary vascular resistance and can lead to an increase in coronary blood flow.
VOLUME DISTRIBUTION
8.3 to 9.3 ng/mL.
METABOLISM
It is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine.
HALF LIFE
31±13 hrs