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 α
1- and α
2-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)
Uses
Antihypertensive compound; calcium channel blocker.
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).
