Lercanidipine

Description

Lerdip was launched in the Netherlands for hypertension. It is prepared in four steps, the last of which is a Hantsch reaction of 1-[(3,3-diphenyl)-N-methylpropylamino]- 2-methyl-2-propyl-2-(3-nitrobenzylidene)acetoacetate with methyl 3-aminocrotonate. This compound was designed to be very lipophilic which imparts the drug with a gradual onset and a long duration of action as a result of prolonged exposure to receptors by partitioning into membranes. It is an antagonist of L-type calcium channels with no activity in smooth muscle cells, is tissue selective, lacks any myocardial contractility impairment, has no neuroendocrine activation, and has negligible affinity for neurotransmitter receptors such as α₁- and α₂-adrenergic receptors. While sold as a racemate, the calcium channel activity is found in the (S)- isomer with the (R)-isomer being 2-orders of magnitude less active. It has an increased cardiac contractility index which is much more than Nitrendipine or nifedipine. The good selectivity causes a reduction in blood pressure with no negative inotropic effects.

Originator

Recordati (Italy)

The Uses of Lercanidipine

Antihypertensive compound; calcium channel blocker.

Background

Lercanidipine is a calcium channel blocker of the dihydropyridine class. It is sold under various commercial names including Zanidip.

Indications

For the treatment of Hypertension, management of angina pectoris and Raynaud's syndrome

Definition

ChEBI: Lercanidipine is a diarylmethane.

brand name

Cardiovasc (Recor dati, Italy); Carmen (Recordati, Italy); Corifeo (Recordati, Italy); Lercadip (Recordati, Italy); Lercan (Recordati, Italy); Lercapin (Recordati, Italy); Lercaton (Recordati, Italy); Lerkamen (Recordati, Italy); Lerzam (Recordati, Italy); Renovia (Recordati, Italy); Vasodip (Recordati, Italy); Zandip (Recordati, Italy); Zanicor (Recordati, Italy).

Pharmacokinetics

Lercanidipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Lercanidipine is similar to other peripheral vasodilators. Lercanidipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Metabolism

Not Available