Bisoprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and angina pectoris.

Bisoprolol is a beta 1-adrenoceptor antagonist with no partial agonist (intrinsic sympathomimetic) activity or membrane stabilising (local anaesthetic) activity. The oral bioavailability of bisoprolol is high (90%) and the drug has a long elimination half-life which allows once-daily administration; in addition, it is hepatically and renally cleared in equal proportions. In non-comparative studies, and comparative trials, bisoprolol proved effective, and as efficacious as atenolol, low doses of metoprolol, diuretics and nifedipine SR in hypertension, and atenolol and verapamil in stable angina pectoris. Bisoprolol has been well tolerated in most patients. Thus, bisoprolol is an effective alternative to other beta-adrenoceptor antagonists in patients with mild to moderate essential hypertension or stable angina pectoris. Furthermore, its unique pharmacokinetic properties may offer advantages in selected patients. However, the results of further comparative studies with established agents in the treatment of hypertension and angina pectoris are still awaited so that a final assessment of the relative place in therapy of bisoprolol in these disease states may be made.

[1]  A. Somogyi,et al.  Pharmacokinetic Interactions of Cimetidine 1987 , 1987, Clinical pharmacokinetics.

[2]  A. Tattersfield,et al.  Assessment of beta-adrenoceptor selectivity of a new beta-adrenoceptor antagonist, bisoprolol, in man. , 1984, British journal of clinical pharmacology.

[3]  R. Beresford,et al.  Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension. , 1986, Drugs.

[4]  H. R. Besch Characterization of [3H](±)Carazolol Binding to β‐Adrenergic Receptors: Application to Study of β‐Adrenergic Receptor Subtypes in Canine Ventricular Myocardium and Lung , 1981, Circulation research.

[5]  J. Cruickshank The clinical importance of cardioselectivity and lipophilicity in beta blockers. , 1980, American heart journal.

[6]  A. Garbe,et al.  Determination of the new β-blocker bisoprolol and of metoprolol, atenolol and propranolol in plasma and urine by high-performance liquid chromatography , 1986 .

[7]  W. Kirch,et al.  Pharmacokinetics of Bisoprolol During Repeated Oral Administration to Healthy Volunteers and Patients with Kidney or Liver Disease , 1987, Clinical pharmacokinetics.

[8]  J. Harting,et al.  Antagonistic effects of bisoprolol on several beta-adrenoceptor-mediated actions in anaesthetized cats. , 1986, European journal of pharmacology.

[9]  A. Kaumann,et al.  Direct labelling of myocardial beta 1-adrenoceptors. Comparison of binding affinity of 3H-(-)-bisoprolol with its blocking potency. , 1985, Naunyn-Schmiedeberg's archives of pharmacology.

[10]  H. Wiemann,et al.  Pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist. , 1986, British journal of clinical pharmacology.

[11]  O. Brodde,et al.  Selective labelling of beta 1-adrenoceptors in rabbit lung membranes by (-)[3H]bisoprolol. , 1985, European journal of pharmacology.

[12]  R. Pugh,et al.  Transection of the oesophagus for bleeding oesophageal varices , 1973, The British journal of surgery.