Lacidipine

(BAN, USAN, rINN)
Lacidipine Chemical formula
Synonyms: GR-43659X; GX-1048; Lacidipin; Lacidipino; Lacidipinum; Lasidipiini; Lasidipin. Diethyl 4-{2-[(tert-butoxycarbonyl)vinyl]phenyl}-1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate.
Cyrillic synonym: Лацидипин.

💊 Chemical information

Chemical formula: C26H33NO6 = 455.5.
CAS — 103890-78-4.
ATC — C08CA09.
ATC Vet — QC08CA09.

Pharmacopoeias.

In Br.

BP 2008

(Lacidipine). A white to pale yellow crystalline powder. Practically insoluble in water; sparingly soluble in dehydrated alcohol; freely soluble in acetone and in dichloromethane.

💊 Adverse Effects, Treatment, and Precautions

As for dihydropyridine calcium-channel blockers.

💊 Interactions

As for dihydropyridine calcium-channel blockers.

💊 Pharmacokinetics

Lacidipine is rapidly but poorly absorbed from the gastrointestinal tract after oral doses and undergoes extensive first-pass metabolism; the bioavailability has been reported to be 2 to 9%, or 18.5% (range 4 to 52%) using a more sensitive assay method. It is more than 95% bound to plasma proteins. Lacidipine is eliminated by metabolism in the liver and metabolites are excreted mainly by the biliary route. About 70% of an oral dose is eliminated in the faeces, the remainder in the urine. The average steady-state terminal elimination half-life of lacidipine is 13 to 19 hours.

💊 Uses and Administration

Lacidipine is a dihydropyridine calcium-channel blocker with actions similar to those of nifedipine. It is used in the treatment of hypertension. The usual initial dose of lacidipine is 2 mg once daily by mouth increased if necessary after 3 to 4 weeks or more to 4 mg daily; a further increase in dose to 6 mg daily may be necessary in some patients.
1. Lee CR, Bryson HM. Lacidipine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the treatment of hypertension. Drugs 1994; 48: 274–96
2. Zanchetti A, ed. Cardiovascular advantages of a third generation calcium antagonist: symposium on lacidipine. Drugs 1999; 57 (suppl 1): 1–29
3. McCormack PL, Wagstaff AJ. Lacidipine: a review of its use in the management of hypertension. Drugs 2003; 63: 2327–56.

💊 Preparations

BP 2008: Lacidipine Tablets.

Proprietary Preparations

Arg.: Lacipil†; Midotens†; Belg.: Motens; Braz.: Lacipil; Midotens; Cz.: Lacipil; Denm.: Midotens; Fr.: Caldine; Ger.: Motens; Gr.: Balnox; Lacipil; Lacitens; Motens; Hong Kong: Lacipil; Hung.: Lacipil; India: Sinopil; Indon.: Lacipil; Ital.: Aponil; Lacipil; Lacirex; Ladip; Viapres; Malaysia: Lacipil; Mex.: Lacipil; Midotens; Neth.: Motens; Philipp.: Lacipil; Pol.: Lacipil; Port.: Lacipil; Tens; Rus.: Lacipil (Лаципил); Singapore: Lacipil; Spain: Lacimen; Lacipil; Motens; Switz.: Motens; Thai.: Motens; Turk.: Lacipil; UK: Motens; Venez.: Lacipil; Tens†.
Published May 06, 2019.