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Celiprolol

A Preliminary Review of its Pharmacodynamic and Pharmacokinetic Properties and its Therapeutic Use in Hypertension and Angina Pectoris

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Summary

Synopsis

Celiprolol1 is a new ‘cardioselective’ β-adrenoceptor blocking drug with intrinsic sympathomimetic (partial agonist) activity and a weak vasodilating effect. Celiprolol appears not to cause bronchoconstriction or inhibit the effect of bronchodilating drugs in asthmatic patients and there is some evidence that it may have mild bronchodilating activity in such patients. Some studies suggest that celiprolol, because of vasodilation, may be less likely to reduce blood flow to the peripheries than other β- adrenoceptor blocking drugs and hence cause fewer peripheral vascular side effects. Significant inhibition of exercise tachycardia occurs 24 hours after a single oral dose of celiprolol. In preliminary therapeutic trials celiprolol 200 to 600mg once daily was similar in efficacy to propranolol 40mg to 80mg twice daily or atenolol 100mg once daily in patients with mild to moderate hypertension or angina pectoris. If the apparent pharmacodynamic advantages of celiprolol are confirmed in well designed therapeutic trials then celiprolol should represent a definite advance in β-adrenoceptor blocking therapy.

Pharmacodynamic Studies

In animals, the β-adrenoceptor blocking activity of celiprolol is more potent than that of sotalol and practolol, and about equipotent with that of propranolol but in man it is about 4 times less potent than atenolol. However, dose-ranging studies employing a range of doses in the same subjects have not been reported and it is possible that celiprolol’s potency has been underestimated. β-Blockade following a single oral dose of 400mg in man can be detected at 24 hours and once-daily dosing is effective in hypertension and angina.

Using the standard animal models celiprolol is more selective for the β1- than the β2-adrenoceptor, and in patients with angina the reduction in blood pressure following exercise was larger after treatment with celiprolol than propranolol, suggesting a degree of cardioselectivity. Studies in guinea-pig atria show that celiprolol has a small degree of partial agonist activity and one report suggests that it has no membrane stabilising activity.

Celiprolol has weak α-adrenoceptor antagonist activity which in early studies was thought responsible for the bronchodilating and vasodilating effects of the drug in animals, but these effects are now considered to be due to β2-adrenoceptor agonist activity and/or a direct (papaverine-like) smooth muscle relaxing effect.

In animals celiprolol caused a smaller reduction in the maximum rate of change of left ventricular pressure than metoprolol, acebutolol, atenolol and propranolol and actually increased stroke volume and femoral artery flow. After experimental coronary artery occlusion in dogs celiprolol had little effect on heart rate, stroke volume, left ventricular output and total peripheral resistance, while atenolol and propranolol had the expected depressant effects. Similar effects have been observed in patients with coronary artery disease in studies comparing celiprolol with atenolol, metoprolol, propranolol and pindolol.

Studies in animals have shown celiprolol to have a bronchodilator action unaffected by propranolol. Single-dose studies in man indicate that, while propranolol and atenolol reduce FEV1 and FVC in asthmatic patients, celiprolol is not significantly different from placebo and may increase lung function in some patients. The apparent effects of celiprolol on respiratory function have been confirmed in a 12-week study in hypertensive patients with reversible bronchial obstruction, although further well designed trials in large numbers of asthmatic patients are required to determine its long term effects in patients with asthma.

Only limited data are available on the effects of celiprolol on carbohydrate and lipid metabolism. Using the glucose clamp technique there was no difference in insulin requirements in 10 Type I diabetic patients who were treated with either celiprolol or placebo but in Type II patients celiprolol 300mg caused significantly reduced blood glucose concentrations in the middle of the afternoon compared with placebo. In patients with Fredrickson Type II or IV hyperlipidaemia 4 weeks’ treatment with celiprolol increased high density lipoprotein concentrations but not the concentrations of other lipids, while there were no changes after metoprolol or placebo.

Pharmacokinetic Studies

Published data on the pharmacokinetics of celiprolol in man are limited. Absorption is dose-dependent, increasing with higher doses. The drug is eliminated from the plasma with a half-life of about 4 to 5 hours. Half of an intravenously administered dose and 10 to 15% of an oral dose appear in the urine within 3 days, the rest being excreted in the faeces. In patients with renal dysfunction, systemic clearance was reduced and may necessitate a reduction in dosage. Preliminary data suggest that bioavailability is decreased and renal clearance increased in patients with cirrhosis.

Therapeutic Trials

Much of the published clinical experience with celiprolol is in relatively small numbers of patients which makes evaluation of its efficacy relative to other drugs difficult. Nevertheless, celiprolol has been shown to be more effective than placebo in the treatment of hypertension (WHO type I or II) and of angina pectoris. Celiprolol 200 to 600mg administered once daily appears similar in efficacy to propranolol 80 to 160mg daily (in 2 divided doses) or atenolol 100mg once daily in patients with mild to moderate hypertension. Trials usually involving small numbers of patients with angina pectoris suggest that celiprolol 300 to 600mg once daily or in divided doses is at least as effective as propranolol 80 to 160mg or atenolol 50 to 100mg daily in improving exercise performance, and in reducing the number of anginal attacks and glyceryl trinitrate (nitroglycerin) requirements.

Side Effects

In a double-blind placebo-controlled study of celiprolol in hypertension there was little difference in the incidence of side effects between the celiprolol and placebo groups. A much larger open post-marketing surveillance study also suggested that the incidence of adverse effects after treatment with celiprolol is low. However, well controlled comparative studies are required to establish the relative incidence of side effects with celiprolol and other β-adrenoceptor blocking drugs.

Dosage

The usual initial dose of celiprolol used to treat mild to moderate essential hypertension is 200mg once daily. If response to this dose is inadequate the daily dosage may be increased to 400mg. In the treatment of angina pectoris the usual average dosage is 200 to 400mg given once daily.

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Authors and Affiliations

  1. Belfast, The Queen’s University of Belfast, USA

    J. G. Riddell, R. G. Shanks & Rex N. Brogden

  2. ADIS Drug Information Services, 41 Centorian Drive, Private Bag, Mairangi Bay, Auckland 10, New Zealand

    J. G. Riddell, R. G. Shanks & Rex N. Brogden

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Various sections of the manuscript reviewed by: W.E. Harston, Cardiology Department, Graves Gilbert Clinic, P.S.C. Bowling Green, USA; G. Hitzenberger, I. Medizinische Universitätsklinik, Wein, Lazarettgasse, Austria; N.C. Jackson, The General Infirmary at Leeds, Leeds, England; B.N.C. Prichard, Department of Clinical Pharmacology, University College London and The Middlesex Hospital Medical School, London, England; F.D. Rosenthal, Leicester Royal Infirmary, Leicester, England; R.R. Rosenthal, Clinical Immunology Division, School of Medicine, Johns Hopkins University, The Good Samaritan Hospital, Baltimore, Maryland, USA; A.E. Tattersfield, Respiratory Medicine Unit, City Hospital, Nottingham, England.

‘Selectol’, ‘Celectol’ (Chemie Linz AG; Revlon Health Care; Rorer Pharmaceutical Corp.).

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Riddell, J.G., Shanks, R.G. & Brogden, R.N. Celiprolol. Drugs 34, 438–458 (1987). https://doi.org/10.2165/00003495-198734040-00002

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