Lacibloc Mechanism of Action

Calcium Channel Blocker (Dihydropyridine derivative).
Pharmacology: Pharmacodynamics: Lacidipine is a specific and potent calcium antagonist, with a predominantly selectivity for calcium channels in the vascular smooth muscle.
Its main action is to dilate peripheral arterioles, reducing peripheral vascular resistance and lowering blood pressure.
Pharmacokinetics: 4 mg: Absorption: Lacidipine is rapidly but poorly absorbed from the gastrointestinal tract following oral dosing and undergoes extensive first-pass metabolism in the liver. Absolute bioavailability averages about 10%. Peak plasma concentrations are reached between 30 and 150 min.
Metabolism: There are four principal metabolites which possess little, if any pharmacodynamic activity. The drug is eliminated primarily by hepatic metabolism (involving P450 CYP3A4). There is no evidence that Lacidipine causes either induction or inhibition of hepatic enzymes.
Elimination: Approximately 70% of the administered dose is eliminated as metabolites in the faeces and the remainder as metabolites in the urine.
The average terminal half-life of lacidipine ranges from between 13 and 19 h at steady state.
6 mg: Lacidipine is rapidly but poorly absorbed from the gastrointestinal tract following oral administration 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.