Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension

Abstract

Betaxolol is a relatively cardioselective beta-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilising (local anaesthetic) activity. Its pharmacokinetic properties of most interest include high bioavailability after oral administration, and a long elimination half-life. It has a narrow dose-response range, which obviates the need for dose titration, with 10 to 20 mg once daily being the usual dosage. This dose reduces systolic and diastolic blood pressures by about 15 mm Hg in most patients with mild to moderate hypertension. In a few comparative studies betaxolol 20 mg daily was as effective as atenolol and moderate doses of propranolol, and more effective than acebutolol, in reducing blood pressure in such patients. Betaxolol has been well tolerated in most patients. Thus, betaxolol is an effective alternative to other beta-blocking drugs in patients with essential hypertension, with properties that may offer advantages in some patients.