Lacidipine: a calcium antagonist with potent and long-lasting antihypertensive effects in animal studies.

摘要: Lacidipine, currently being evaluated as a once-daily antihypertensive agent, acted calcium entry blocker on rabbit ear artery (pA2 = 9.4) with markedly slower onset of action than that nitrendipine; this effect was not reversed after 9 h drug washout. Calcium activity also nonvascular smooth muscles: Lacidipine showed more pronounced vascular selectivity for both drugs, concentrations required to induce negative inotropic effects in guinea pig ventricular strip were approximately 100 times higher needed antagonize contraction muscle. In spontaneously hypertensive rats (SHR), by the tail-cuff method, lacidipine (ED25 0.35 mg/kg orally, p.o.) proved 30 potent, onset, and longer-acting nitrendipine reducing blood pressure. These features confirmed chronically implanted SHR oral intravenous (i.v.) administration 0.19 p.o. 0.006 i.v.). A short-lasting tachycardia detected drugs. No evidence acquired tolerance emerged repeated administrations over 3-week period. induced natriuretic saline-loaded at doses. renal dogs, potent (three seven times), longer-lasting 0.22 mg/kg) i.v. 0.004 administrations.