Basic Pharmacokinetics of Bisoprolol, a New Highly Beta1‐selective Adrenoceptor Antagonist

  title={Basic Pharmacokinetics of Bisoprolol, a New Highly Beta1‐selective Adrenoceptor Antagonist},
  author={G. Leopold and Joachim Pabst and W. Ungeth{\"u}m and K. U. B{\"u}hring},
  journal={The Journal of Clinical Pharmacology},
The basic pharmacokinetics of bisoprolol were investigated in three independent studies involving 23 healthy volunteers. After administering 20 mg of 14C‐bisoprolol orally, mean elimination half‐lives of 11 hours for the unchanged drug and 12 hours for total radioactivity were observed. The enteral absorption of bisoprolol was nearly complete. Fifty percent of the dose was eliminated renally as unchanged bisoprolol and the other 50% metabolically, with subsequent renal excretion of the… 
Pharmacokinetics of Bisoprolol During Repeated Oral Administration to Healthy Volunteers and Patients with Kidney or Liver Disease
The present study indicates that in patients with impairment of kidney or liver function accumulation of bisoprolol above a factor of 2 did not occur, however, in the terminal stages of insufficiency of kidney and liver function bisopolol dosage should not exceed 10mg.
Metabolic Fate of the New β-Adrenoceptor Antagonist, Bisoprolol, in Animals (1) : Absorption, Distribution and Excretion of 14C-Bisoprolol in Rats
The absorption, distribution and excretion of bisoprolol were studied in rats after oral or intravenous administration of 14C-bisoproll and whole body autoradiograms obtained with pigmented rats demonstrated that specific binding of radioactivity to melanin containing tissues was noticed.
Interaction of bisoprolol with cimetidine and rifampicin
B bisoprolol showed a statistically significant but probably clinically not important interaction with the enzyme-inducing drug rifampicin, but not with the enzymes inhibitor cimetidine.
Pharmacokinetics and metabolism of bisoprolol enantiomers in humans.
It is suggested that the small differences in the pharmacokinetics between (S)-(-)- and (R)-(+)-bisoprolol are mainly due to the stereoselectivity in the intrinsic metabolic clearance by CYP2D6 and renal tubular secretion.
Population Pharmacokinetic Analysis of Bisoprolol
The technique of population pharmacokinetic analysis was employed to study the variability in the dose concentration relationship of bisoprolol during its clinical development, predicting that progressive increases in serum creatinine or aspartate transaminase activity will result in only a 50% reduction of clearance.
Pharmacokinetic variability of routinely administered bisoprolol in middle-aged and elderly Japanese patients.
The pharmacokinetic variability of bisoprolol is small even in routinely treated Japanese patients, provided that both body weight and renal function are taken into account for the prediction of oral clearance of the drug.
Population Pharmacokinetics of Bisoprolol in Hemodialysis Patients with Hypertension
It is suggested that the routine measuring of serum creatinine level may be used to facilitate administration of bisoprolol in patients on hemodialysis.
Pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist.
The dose-response relationship using individual maximal reduction of ET showed that bisoprolol is about 5, 7 and 10 times more effective than propranolol, atenolol and metoproleol, respectively, on a molar basis.
Effects of Acute Febrile Infectious Diseases on the Oral Pharmacokinetics and Effects of Nitrendipine Enantiomers and of Bisoprolol
SummaryIn 2 longitudinal studies with 10 patients each, the stereoselective pharmacokinetics of nitrendipine and the pharmacokinetics of racemic (rac) bisoprolol (both 20mg orally) were investigated
Population pharmacokinetics of bisoprolol in patients with chronic heart failure
The derived PK model describes the clearance of bisoprolol in patients with CHF, showing that the total daily dose of bisiprolol is the most important covariate.


Clinical Pharmacokinetics of Metoprolol
The β-blocking effect of metoprolol is linearly related to the logarithm of the dose and the plasma concentration of the drug, and the antihypertensive effect increases with increasing dosage up to 200 to 300mg daily.
Clinical Pharmacokinetics of Propranolol
Hepatic, renal, thyroid and some gastrointestinal diseases as well as hypertension, malnutrition and hypothermia may be associated with alterations in propranolol disposition, all of which are consistent with the pathophysiology of these diseases.
Beta 1-selectivity of bisoprolol, a new beta-adrenoceptor antagonist, in anesthetized dogs and guinea pigs.
In anesthetized, bivagotomized dogs and guinea pigs, isoprenaline dose-response relations for increase in heart rate and decrease in diastolic blood pressure were established, and it is indicated that bisoprolol possesses a pronounced beta 1-selectivity, which seems to be superior to that of known beta 2-selective antagonists.
Characterization of [3H](±)Carazolol Binding to β‐Adrenergic Receptors: Application to Study of β‐Adrenergic Receptor Subtypes in Canine Ventricular Myocardium and Lung
The results demonstrate that the state of guanine nucleotide regulation of receptors should be defined when examining agonist selectivities for β-adrenergic receptor subtypes in vitro.
Clinical pharmacokinetics of propran - 1 - exp ( - 1 n 2 X r / ti , , ) olol
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