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Bisoprolol

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

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Summary

Synopsis

Bisoprolol is a β: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 β-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.

Pharmacodynamic Studies

Bisoprolol is a β1-adrenoceptor antagonist which has been shown to be devoid of partial agonist or membrane-stabilising activity. Animal studies have shown that bisoprolol is a more potent antagonist of β1-adrenoceptors than atenolol or metoprolol, but the drug appears to be less potent than propranolol and betaxolol in this regard. Bisoprolol possesses a long duration of action, with significant reductions in exercise tachycardia (about 20%) being observed in subjects with stable angina pectoris 24 hours after oral administration of 5 and 10mg. Both systolic and diastolic blood pressures are reduced by bisoprolol (by up to about 20%, respectively, in healthy subjects and in patients with mild to moderate essential hypertension) as well as myocardial oxygen demand (by up to 34%).

Respiratory function in healthy subjects was not affected by bisoprolol 20 and 40mg orally, but in asthmatic patients oral bisoprolol 10 and 20mg and metoprolol 100mg significantly reduced peak expiratory flow rate (p<0.01 vs placebo), while bisoprolol 10mg also significantly decreased vital capacity and forced expiratory volume in 1 second (p<0.01 vs placebo). The patients remained asymptomatic and all of these changes in ventilatory parameters were rapidly reversed by inhaled terbutaline.

In non-diabetic healthy subjects bisoprolol did not significantly affect insulin-induced hypoglycaemia or the compensatory rise in serum lactate concentration after insulin. In hypertensive non-insulin-dependent diabetics bisoprolol had no effect on carbohydrate metabolism.

Statistically significant increases in serum triglycerides (p<0.05) and reductions in high density lipoprotein (HDL)-cholesterol (bisoprolol, p<0.01; atenolol, p<0.05) were reported in a 3-month comparison of oral bisoprolol 10 and 20 mg/day and atenolol 50 and 100 mg/day in patients with mild to moderate essential hypertension. However, the overall effects of bisoprolol on lipid metabolism are as yet still unclear and further studies in this area are required.

Pharmacokinetic Studies

Bisoprolol, possessing both lipophilic and hydrophilic properties, has been shown to have a bioavailability ⩾ 90% after oral administration. Peak plasma concentrations are reached within 3 hours of a single 10mg dose in healthy subjects, with maximum plasma concentrations of between 36 and 78 μg/L being achieved after the same dose in healthy subjects and patients with varying degrees of renal and hepatic insufficiency. Animal studies indicate that bisoprolol is rapidly and widely distributed, but little placental transfer occurs and the drug only penetrates the blood-brain barrier to a small degree in comparison to metoprolol and propranolol. Bisoprolol binds to human plasma proteins to the extent of about 30%. Approximately 50% of a dose of bisoprolol is hepatically metabolised to 3 inactive metabolites while the rest is renally excreted unchanged; in addition,⩽ 10% of the drug undergoes ‘first-pass’ metabolism. The elimination half-life of unchanged bisoprolol in healthy subjects is 9 to 12 hours and is increased to about 18 hours in patients with renal impairment or to about 13 hours in patients with hepatic cirrhosis.

Therapeutic Trials

Several short and long term non-comparative studies have indicated that the optimum oral dose range of bisoprolol in patients with mild to moderate essential hypertension is 5 to 20mg once daily. Systolic and diastolic blood pressures were well controlled with a single daily dose of bisoprolol ( 15 to 20% reductions from baseline), and in long term non-comparative studies reductions in diastolic blood pressure to⩽ 90mm Hg were achieved in 70 to 95% of patients. In comparative studies bisoprolol 5 to 20mg once daily was as effective as atenolol 50 to 100 mg/day, metoprolol 100 mg/day and nifedipine SR 40 to 80 mg/day, and more effective than daily treatment with hydrochlorothiazide 50mg plus amiloride 5mg in reducing blood pressure in patients with mild to moderate essential hypertension.

Non-comparative clinical trials in patients with stable angina pectoris have confirmed the efficacy of bisoprolol in short term studies. During a 12-month study approximately 50% of the patients were completely free from anginal attacks, with 27%, 55% and 18% of the patients receiving bisoprolol 5mg, 10mg and 20mg daily, respectively. In comparative studies bisoprolol 5 to 10mg once daily and atenolol 100mg once daily produced similar increases in exercise duration, time to onset of exercise-induced ischaemia and reductions in the frequency of anginal attacks, glyceryl trinitrate (nitroglycerin) consumption and myocardial oxygen demand. In addition, in combination therapy with isosorbide dinitrate 20mg twice daily, bisoprolol 10 to 20mg once daily or verapamil 240 to 360 mg/day produced comparable improvements in exercise duration, myocardial ischaemia and oxygen demand, frequency of anginal attacks and glyceryl trinitrate consumption. However, these comparative studies involved only small numbers of patients, and further comparative studies in larger patient groups are required to confirm their findings.

Side Effects

Bisoprolol has been well tolerated by most patients in long term trials (6 to 24 months duration). ‘Giddiness’, headache and tiredness were the most commonly reported adverse reactions. In long term trials, side effects necessitated discontinuation of treatment in about 2.7% of patients. In comparative trials the tolerability of bisoprolol 5 to 20 mg/day appeared to be comparable to atenolol 50 to 100 mg/day, metoprolol 100 mg/day and verapamil 240 to 360 mg/day, and superior to nifedipine SR 40 to 80 mg/day or hydrochlorothiazide 50 mg/day plus amiloride 5 mg/day. Adverse reactions tend to occur more frequently during the first few weeks of bisoprolol treatment and then subside with continued therapy.

Dosage and Administration

The usual oral dose of bisoprolol in mild to moderate essential hypertension or stable angina pectoris is 10mg once daily with a maximum recommended dose of 20 mg/day. In some patients 5 mg/day may be adequate. However, in end-stage renal or hepatic insufficiency, dosage should not exceed 10mg once daily.

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Various sections of the manuscript reviewed by: F. Burkart, Division of Cardiology, University Hospital, Basel, Switzerland; S.S. Chatterjee, Department of Respiratory Physiology, Wythenshawe Hospital, Manchester, England; D.C. Harrison, University of Cincinnati Medical Center, Cincinnati, Ohio, USA; N.M. Kaplan, Department of Internal Medicine, University of Texas Health Science Center, Dallas, Texas, USA; W. Kirch, Medizinische Klinik, Christian-Albrechts Universität, Kiel, Federal Republic of Germany; B. Krämer, Medizinische Klinik, Ruprecht-Karls Universität, Heidelberg, Federal Republic of Germany; J.C. Petrie, Department of Medicine and Therapeutics, University of Abderdeen, Aberdeen, Scotland; B.N.C. Prichard, Department of Clinical Pharmacology, University College, London, and the Middlesex Hospital Medical School, London, England; E.B. Raftery, Northwick Park Hospital and Clinical Research Centre, Harrow, England; T. Sugimoto, Second Department of Internal Medicine, University of Tokyo, Tokyo, Japan.

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Lancaster, S.G., Sorkin, E.M. Bisoprolol. Drugs 36, 256–285 (1988). https://doi.org/10.2165/00003495-198836030-00002

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