高血壓 (CCB) Hypertension.

Lercanidipine is a dihydropyridine calcium antagonist. It lowers blood pressure by relaxing arteriolar smooth muscle, which decreases peripheral vascular resistance. Lercanidipine produces no negative cardiac inotropism and only mild reflex tachycardia. Prolonged antihypertensive effects are due to its high membrane partition coefficient.

Duration: 24 hours; Time to peak: ~1.5 to 3 hours; Protein binding: >98%; Metabolism: Extensively metabolized by CYP3A4, predominantly to inactive metabolites; Bioavailability: ~10% (large first-pass metabolism); Excretion: Urine (~50%; as metabolites); Half-life elimination: ~8 to 10 hours.

Hypersensitivity to lercanidipine, any other dihydropyridine, or to any component of the formulation; severe renal impairment or patients on dialysis; severe hepatic impairment; concomitant use with strong CYP3A4 inhibitors, cyclosporine, or grapefruit juice; women who are pregnant or may become pregnant (unless effective contraception is used); breast-feeding. Left ventricular outflow obstruction (aortic stenosis), untreated congestive heart failure, unstable angina; previous myocardial infarction (within 1 month).

contraindicated

contraindicated

Headache (>4%), Flushing (>3%), cardiac arrhythmia (<2%; palpitations, tachycardia).

Oral: Initial: 10 mg once daily; may increase to 20 mg once daily if needed.
May take up to 2 weeks after initiation or titration for full antihypertensive response.
Administer at least 15 minutes before meals.