Drug intelligence / Profile preview

r-amlodipine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

R-amlodipine is the pharmacologically active (levorotatory, or "R") enantiomer of amlodipine, a long-acting dihydropyridine calcium channel blocker. Unlike standard amlodipine formulations, which are racemic mixtures of both R- and S-enantiomers, r-amlodipine contains only the R-enantiomer, which is responsible for the majority of the drug's therapeutic vasodilatory effects. Its mechanism of action involves inhibition of L-type calcium channels in vascular smooth muscle, leading to decreased peripheral vascular resistance, reduced blood pressure, and relief of cardiac workload. The clinical aim of r-amlodipine (versus racemic amlodipine) is to achieve the same or greater antihypertensive and antianginal effects at lower doses, possibly with fewer side effects such as peripheral edema. It is primarily used for the management of hypertension and chronic stable angina.

Brand names
r-amlodipine
Other names
r-amlodipinelevo-amlodipine
02

Targets

CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)CACNA1B (Voltage-dependent N-type calcium channel subunit alpha-1B)

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