Quantitative relationships between structure and pharmacokinetics of beta-adrenoceptor blocking agents in man
- 1 June 1984
- journal article
- research article
- Published by Springer Nature in Journal of Pharmacokinetics and Biopharmaceutics
- Vol. 12 (3) , 263-287
- https://doi.org/10.1007/bf01061721
Abstract
The structure and pharmacokinetics relationship of 14-beta-adrenoceptor antagonists was investigated in humans. Statistically significant linear and parabolic correlations were found to exist between standard and derived mean pharmacokinetic parameters and the apparent octanol/buffer (pH7.4) partition coefficient of the compounds. The lipophilic/hydrophilic properties were the primary determinants for the pharmacokinetic behavior of the compounds. Most of the pharmacokinetic parameters were also significantly correlated with the plasma protein/plasma water partition coefficient for the compounds. When the values of the pharmacokinetic parameters of the individual compounds were predicted from the regressions on the apparent partition coefficients in octanol/buffer (pH 7.4) and in plasma protein/plasma water, the error was on average 60%.Keywords
This publication has 53 references indexed in Scilit:
- Kinetics of Partitioning and Binding of Digoxin and Its Analogues in the Subcompartments of BloodJournal of Pharmaceutical Sciences, 1984
- Comparative pharmacokinetics of benzodiazepines in dog and manJournal of Pharmacokinetics and Biopharmaceutics, 1982
- The application of statistical moment theory to the evaluation ofin vivo dissolution time and absorption timeJournal of Pharmacokinetics and Biopharmaceutics, 1980
- Influence of renal failure on the hepatic clearance of bufuralol in manJournal of Pharmacokinetics and Biopharmaceutics, 1980
- Pharmacokinetic and Pharmacodynamic Properties of Metoprolol in Patients with Impaired Renal FunctionClinical Pharmacokinetics, 1980
- Importance of “first-pass elimination” for interindividual differences in steady-state concentrations of the adrenergicβ-receptor antagonist alprenololJournal of Pharmacokinetics and Biopharmaceutics, 1977
- Protein Binding of AntimicrobialsClinical Pharmacokinetics, 1977
- Human Pharmacokinetics of SotalolActa Pharmacologica et Toxicologica, 1976
- Absorption, Distribution and Excretion of Alprenolol in Man, Dog and RatActa Pharmacologica et Toxicologica, 1974
- Pharmacokinetic studies on the selectiveβ 1-receptor antagonist metoprolol in manJournal of Pharmacokinetics and Biopharmaceutics, 1974