Balanced Pharmacokinetics and Metabolism of Bisoprolol

  title={Balanced Pharmacokinetics and Metabolism of Bisoprolol},
  author={G. Leopold},
  journal={Journal of Cardiovascular Pharmacology},
  • G. Leopold
  • Published 1 November 1985
  • Medicine, Biology
  • Journal of Cardiovascular Pharmacology
&NA; Bisoprolol exhibits a high absolute bioavailability (90%) because of its nearly complete absorption (> 90%) and small first‐pass effect (10%). Bioavailability is independent of food intake. A long plasma‐elimination half‐life (10‐11 h) allows a once‐a‐day dose regimen. Because of the low plasma protein‐binding (30%), kinetics are insensitive to protein‐binding interactions. The balanced clearance (equieffective hepatic and renal clearance) renders the kinetics virtually insensitive to… 
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.
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.
Variability of bioavailability and intestinal absorption mechanisms of metoprolol.
The findings indicate that residual variability of F is one of the causes of the interindividual pharmacokinetic variability of metoprolol, and that the inter individual variability of not only presystemic first-pass metabolism, but also intestinal absorption, may be responsible for the variable F of the drug.
Stereoselective pharmacokinetics of bisoprolol after intravenous and oral administration in beagle dogs.
It is concluded that the stereoselective difference in the metabolic clearance between S(-)- and R(+)-bisoprolol caused the difference inThe disposition of bisoproll enantiomers.
Variability of bioavailability and intestinal absorption characteristics of bisoprolol.
The findings suggest that the rate/extent of the intestinal absorption of bisoprolol is another cause of the interindividual variability of the pharmacokinetics, and that the uptake of bisOProlol in intestinal epithelial cells is highly pH-dependent and also variable.
Multimorbidity and polypharmacy: which betablocker to use in relation to the pharmacokinetic profile and interaction potential.
  • M. Wehling
  • Biology, Medicine
  • 2010
A favourable compound should be partially stable in regard to metabolism to depend less on drug-drug and gene-drug interactions, but also utilize more than one routes of excretion, meaning both the direct renal and the metabolic routes.
Pharmacokinetics and pharmacodynamics of bisoprolol in rats with bilateral ureter ligation-induced renal failure.
The results suggested that renal excretion and hepatic metabolism of bisoprolol were significantly reduced in BUL rats, but that pharmacodynamics of bisOProlol was not altered by acute renal failure.
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.
Pharmacokinetics of intravenous bisoprolol in obese and non-obese volunteers
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 bisopolol.
Population Pharmacokinetic Analysis of Bisoprolol in Patients With Acute Coronary Syndrome
It is suggested that possible autoinduction of drug metabolism by higher total daily doses and induction of cytochrome P450 isoform 3A4 (CYP3A4) by cigarette smoke in liver could be the potential causes of increased total clearance of bisoprolol in patients with ACS.