Celiprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in cardiovascular disease.
Celiprolol is a hydrophilic, beta 1-selective adrenoceptor antagonist with mild selective beta 2-agonist as well as weak vasodilator properties. Celiprolol 200 to 400mg once daily by mouth is similar in antihypertensive efficacy to usual doses of propranolol, atenolol, metoprolol and pindolol in patients with mild to moderate systemic hypertension. Similar doses of celiprolol are as efficacious as propranolol and atenolol in improving exercise tolerance and reducing the frequency of anginal attacks in patients with angina pectoris. Further clinical experience suggests that celiprolol does not produce bronchoconstriction and may have mild bronchodilating activity in asthmatic patients; it may also enhance the effects of bronchodilator drugs. Celiprolol has a slightly beneficial effect on serum lipid profiles, and does not appear to exert adverse effects on carbohydrate metabolism. If the apparent pharmacodynamic advantages of celiprolol translate into clinical benefits and are confirmed in well designed long term clinical trials, then celiprolol should represent a definite advance in beta-blocker therapy.
Milne
R J
RJ
Adis Drug Information Services, Auckland, New Zealand.
Buckley
M M
MM
D000319:Adrenergic beta-Antagonists / Q000627:therapeutic use; D000787:Angina Pectoris / Q000188:drug therapy*; D000818:Animals; D000959:Antihypertensive Agents / Q000627:therapeutic use; D017272:Celiprolol; D004285:Dogs; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D008055:Lipids / Q000097:blood; D011412:Propanolamines / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use
D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D008055:Lipids; D011412:Propanolamines; D017272:Celiprolol