Bisoprolol is a selective inhibitor of beta1-adrenergic receptors; competitively blocks beta1-receptors, with little or no effect on beta2-receptors at doses ?20 mg.
藥動學
Onset of action: 1-2 hrs; Bioavailability: about 80%; Plasma protein binding: 30%; Metabolism: Extensively hepatic; significant first-pass effect (~20%); Elimination half-life: normal renal function: 9-12 hrs; Clcr <40 ml/min: 27-36 hrs; Hepatic cirrhosis: 8-22 hrs; Excretion: Urine (50% as unchanged drug, remainder as inactive metabolites); feces (<2%)
禁忌症
Cardiogenic shock; overt cardiac failure; marked sinus bradycardia; heart block greater than first-degree (except in patients with a functioning artificial pacemaker)
Angina pectoris, chronic: 5-20 mg ORALLY once daily; Congestive heart failure: initial, 1.25 mg once daily, titrate to maximum dose of 10 mg once daily; Hypertension: initial, 2.5-5 mg once daily, maximum dose, 40 mg once daily.