(S)-Amlodipine

Absorption

Oral levamlodipine has a Tmax of 6-12h and a bioavailability of 64-90%. Absorption of levamlodipine is not significantly affected by food.
20mg or oral s-amlodipine besylate reaches a Cmax of 6.13±1.29ng/mL with a Tmax of 8.4±3.6h and an AUC of 351±72h*ng/mL. 20mg or oral s-amlodipine maleate reaches a Cmax of 5.07±1.09ng/mL with a Tmax of 10.7±3.4h and an AUC of 330±88h*ng/mL.

Toxicity

Patients experiencing an overdose may present with hypotension and reflex tachycardia. Treat overdose with cardiac and respiratory monitoring, frequent blood pressure measurement, elevation of extremities to treat hypotension, and possible administration of vasopressors. Hemodialysis is not expected to be useful as levamlodipine is highly protein bound.

The Uses of (S)-Amlodipine

(S)-Enantiomer of Amlodipine. A dihydropyridine calcium channel blocker; activity resides mainly in the (-)-isomer.

Indications

Levamlodipine is indicated alone or in combination to treat hypertension in adults and children.

Background

Levamlodipine, also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive medication. Levamlodipine belongs to the dihydropyridine group of calcium channel blockers. This medication was first marketed in Russia and India before being granted FDA approval. The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however. As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.
Levamlodipine was granted FDA approval on 19 December 2019.

What are the applications of Application

(S)-Amlodipine is a (S)-Enantiomer of Amlodipine

Pharmacokinetics

Levamlodipine inhibits L-type calcium channels in vascular smooth muscle, reducing peripheral vascular resistance and blood pressure. It is given once daily in doses of 1.25-2.5mg in children and 2.5-5mg in adults. Patients should be counselled regarding the risk of symptomatic hypotension, worsening angina, and myocardial infarction.

Metabolism

Levamlodipine is 90% metabolized to inactive metabolites. Incubation with liver microsomes has shown that this metabolism is primarily mediated by CYP3A4. Levamlodipine's dehydrogenation to a pyridine metabolite (M9) is the most important metabolic pathway in human liver microsomes. This derivative can be further oxidatively deaminated or O-dealkylated, but does not appear to undergo O-demethylation like racemic amlodipine.