Lacidipine

Description

Lacidipine is a new second-generation dihydropyridine calcium antagonist introduced as a once a day treatment for mild to moderate hypertension. It is reported to have high selectivity for vascular smooth muscle and also a long duration of action. The use of lacidipine as an antiatherosclerotic agent is currently under investigation.

Description

Lacidipine is a dihydropyridine L-type calcium channel blocker. It induces relaxation of isolated rat aorta and inhibits calcium-induced contraction of rabbit ear artery (pA₂ = 9.4). It also induces relaxation of calcium-induced contractions in isolated rat colon and bladder and guinea pig trachea (IC₅₀s = 6.7, 6, and 7.8 nM, respectively). Lacidipine induces negative inotropy in isolated guinea pig ventricular strips (IC₅₀ = 110 nM). It reduces mean blood pressure in spontaneously hypertensive rats (ED₂₅ = 0.35 mg/kg) and in renal hypertensive dogs (ED₂₅ = 0.22 mg/kg) with a transient increase in heart rate. Lacidipine inhibits copper-induced oxidation of isolated human LDL when used at concentrations of 1 and 5 μM. It reduces the extension of aortic atheromatous lesions and decreases renal injury in ApoE^-/- mice in a model of Western diet-induced atherosclerosis.

Chemical Properties

White-to-Off-White Crystalline Solid

Originator

Glaxo (United Kingdom)

Uses

A dihydropyridine calcium channel blocker. Antihypertensive.

Uses

antihypertensive;dihydropyridinr calcium channel blocker

Definition

ChEBI: Lacidipine is a cinnamate ester and a tert-butyl ester.

brand name

Lacipil; Lacirex; Viapres

Biochem/physiol Actions

Lacidipine is a long-acting calcium antagonist that is used in the management of hypertension. Lacidipine is a L-type Ca(2+) channel blocker belonging to 1,4-dihydropyridine class. Also, Lacidipine inhibits ryanodine receptors on the ER membrane that enhances folding, trafficking and lysosomal activity of ERAD (ER-associated degradation) misfolded lysosomal glucocerebrosidase (GS).