Interindividual variation of beta-adrenoceptor blocking drugs, plasma concentration and effect: influence of genetic status on behaviour of atenolol, bopindolol and metoprolol

Ten healthy subjects whose genetic oxidative phenotype had been determined (6 extensive and 4 poor metabolizers of the debrisoquine-sparteine type of polymorphism) received single oral doses of 3 beta-blockers: atenolol, bopindolol and metoprolol. The plasma concentrations and the extent of the decr...

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Bibliographic Details
Published in:European journal of clinical pharmacology 1985-01, Vol.28 (2), p.149-153
Main Authors: DAYER, P, LEEMANN, T, MARMY, A, ROSENTHALER, J
Format: Article
Language:English
Subjects:
Adrenergic beta-Antagonists - blood
Adrenergic beta-Antagonists - pharmacology
Adult
Atenolol - blood
Atenolol - pharmacology
Biological and medical sciences
Cardiovascular system
Humans
Individuality
Medical sciences
Metoprolol - blood
Metoprolol - pharmacology
Miscellaneous
Oxidation-Reduction
Pharmacology. Drug treatments
Pindolol - analogs & derivatives
Pindolol - blood
Pindolol - pharmacology
Polymorphism, Genetic
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Summary:Ten healthy subjects whose genetic oxidative phenotype had been determined (6 extensive and 4 poor metabolizers of the debrisoquine-sparteine type of polymorphism) received single oral doses of 3 beta-blockers: atenolol, bopindolol and metoprolol. The plasma concentrations and the extent of the decrease in exercise-induced tachycardia were determined. The oxidative polymorphism was only significant for substances that had a high hepatic first pass metabolism, such as metoprolol. The metabolic pathway under genetic control was highly stereoselective. This observation must be taken into account when assessing the relation between the plasma concentration and effect of these drugs, which are often administered as racemic mixtures.
ISSN:0031-6970
1432-1041
DOI:10.1007/BF00609683