Celiprolol

Celiprolol is a vasoactive beta-l selective adrenoceptor antagonist with partial beta-2 agonist activity indicated in mild to moderate hypertension. The beta-2 agonist activity is thought to account for its mild vasodilating properties. It lowers blood pressure in hypertensive patients at rest and on exercise. The effects on heart rate and cardiac output are dependant on the pre-existing background level of sympathetic tone.

Under conditions of stress such as exercise celiprolol attenuates chronotropic and inotropic responses to sympathetic stimulation. However, at rest minimal impairment of cardiac function is seen.

Celiprolol therapy has not been shown to adversely effect plasma lipid profiles.

Celiprolol is a hydrophilic compound that is incompletely absorbed from the gastrointestinal tract. Bioavailability of orally administered celiprolol ranges from 30 to 70% depending upon the dose administered. Plasma half-life is approximately 5-6 hours and pharmacodynamic effects are present for at least 24 hours. At plasma concentrations of 0.11 to 0.86 μmol/L, celiprolol is about 25% bound to human plasma proteins. After once daily administration, celiprolol is only slightly metabolised before excretion in the bile and urine in almost equal quantities.

It has been shown that the bioavailability of celiprolol is impaired when it is given with food. Co-administration of chlorthalidone, hydrochlorothiazide and theophylline also reduces the bioavailability of celiprolol.

Preclinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential and reproductive toxicity.