Double-Blind Comparison of the β1-Selectivity of Single Doses of Bisoprolol and Atenolol

The pharmacokinetics of a single i.v. dose of dl-bisoprolol 0.16 mg.kg-1 ideal body weight has been studied in 8 obese women (mean weight 91 kg; 161% of ideal body weight) and 8 non-obese women (51 kg; 94% of ideal body weight). Compared to the controls, the obese subjects showed an increase in the total apparent volume of distribution (Vz) (182 vs 1351) and a decrease in Vz per kg body weight (2 vs 2.71.kg-1). There was a negative correlation between Vz l.kg-1 and the percentage of ideal body weight (r = -0.672). Total body clearance was increased, but t1/2 and renal clearance was unchanged. It is concluded that tissue diffusion of bisoprolol in obese subjects is limited, despite its lipophilicity, possibly because of alteration in the blood flow to adipose tissue produced by bisoprolol.

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Pharmacokinetics of intravenous bisoprolol in obese and non-obese volunteers

Jeunne

Poirier

Cheymol

et al. 1991

Eur J Clin Pharmacol

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A dose-ranging study to evaluate the β1-adrenoceptor selectivity of bisoprolol

Lipworth

Irvine

McDevitt

1991

Eur J Clin Pharmacol

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A randomized double-blind study of bisoprolol versus atenolol in mild to moderate essential hypertension

Dixon

Thomas

Sheridan

1990

Eur J Clin Pharmacol

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We have compared the efficacy and pharmacokinetics of bisoprolol, a new cardioselective beta-adrenoceptor antagonist, with atenolol in a randomized double-blind crossover study in 12 patients (mean age 53.5 y) with mild to moderate essential hypertension. After a two week placebo wash-out period without any antihypertensive therapy, the patients were given bisoprolol 10 mg daily or atenolol 50 mg daily, increasing to 20 mg or 100 mg respectively if the sitting diastolic blood pressure did not fall below 90 mm Hg after two weeks of therapy. Crossover occurred after six weeks of active therapy followed by two weeks of placebo wash-out. After 6 weeks of therapy both drugs significantly reduced sitting and standing diastolic blood pressures (bisoprolol by 15% and 16% respectively, atenolol by 11% in both cases). However, while sitting and standing systolic pressures were significantly reduced by bisoprolol (13% and 16% respectively), only standing systolic pressures were significantly reduced by atenolol (11%), and this reduction was significantly less than with bisoprolol (p less than 0.05). Both drugs similarly reduced mean sitting and standing heart rates. There were no significant differences between the single-dose and steady-state kinetics of either bisoprolol or atenolol. The mean plasma elimination half-life (t1/2) increased from 12.9 to 13.2 h during steady state on bisoprolol and from 7.2 to 11.5 h on atenolol. The apparent volume of distribution (Vz) was greater for bisoprolol than for atenolol after single dosing (235 1 vs 146 1) and at steady state (216 1 vs 137 1), but clearances were similar for both drugs.(ABSTRACT TRUNCATED AT 250 WORDS)

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Double-Blind Comparison of the β1-Selectivity of Single Doses of Bisoprolol and Atenolol

Cited by 4 publications

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Pharmacokinetics of intravenous bisoprolol in obese and non-obese volunteers

Pharmacokinetics of intravenous bisoprolol in obese and non-obese volunteers

A dose-ranging study to evaluate the β1-adrenoceptor selectivity of bisoprolol

A randomized double-blind study of bisoprolol versus atenolol in mild to moderate essential hypertension

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