Human pharmacokinetic and pharmacodynamic studies on the atenolo (ICI 66,082), a new cardioselective beta-adrenoceptor blocking drug

British Journal of Clinical Pharmacology
F J ConwayW T Simpson

Abstract

The beta-adrenoceptor blocking effects of orally administered atenolol on tachycardia induced by intravenous isoprenaline or by exercise have been studied in normal volunteers, and compared with the effects of similar doses of propranolol. The blood levels of atenolol at various times after oral administration were determined by g.l.c. and correlated with the degree of inhibition of tachycardia. Atenolol was shown to be a beta-adrenoceptor blocker in man, as in animals, in that it antagonized the chronotropic effects of isoprenaline and of exercise. The inhibitory effect of atenolol on exercise-induced tachycardia was evident at a concentration in blood of 0.2 mug/ml and virtually complete at 0.5 mug/ml. Higher concentrations than this did not produce significantly greater blockade. The effects of atenolol on exercise-induced tachycardia were similar to those of propranolol but it was less effective in blocking the rise in heart rate and fall in diastolic blood-pressure induced by intravenous infusion of isoprenaline. This separation of effects is considered characteristic of drugs causing preferential blockade of cardiac beta-adrenoreceptors. The half-life of atenolol in blood was calculated to ablut 9 hours.

References

Jun 1, 1975·The Journal of Pharmacy and Pharmacology·B Scales, P B Copsey

Citations

Jan 1, 1981·European Journal of Clinical Pharmacology·W KirchM Schäfer
May 1, 1980·European Journal of Clinical Pharmacology·E RivaJ McAinsh
Feb 1, 1981·European Journal of Clinical Pharmacology·J B FourtillanJ Girault
Jan 1, 1977·European Journal of Clinical Pharmacology·D L ClementR Pannier
May 17, 1978·European Journal of Clinical Pharmacology·J D FitzgeraldJ McAinsh
Nov 14, 1977·European Journal of Clinical Pharmacology·J SassardP Zech
Jan 1, 1981·European Journal of Clinical Pharmacology·M E EllisS H Ellis
Dec 1, 1991·Clinical Autonomic Research : Official Journal of the Clinical Autonomic Research Society·C Nyarko-Adomfeh
Jan 1, 1982·European Journal of Drug Metabolism and Pharmacokinetics·W Kirch, K G Görg
Aug 30, 2005·Journal of Pharmacological and Toxicological Methods·Christian HöchtCarlos A Taira
Apr 6, 2002·Reproductive Toxicology·Sonia A Tabacova, Carole A Kimmel
Oct 1, 1977·British Journal of Clinical Pharmacology·T A JeffersN P Barker
Jun 1, 1979·British Journal of Clinical Pharmacology·S H WanR F Maronde
Jan 1, 1994·British Journal of Clinical Pharmacology·D LyonsJ C Petrie
Dec 25, 2004·International Journal of Clinical Practice. Supplement·L AlcocerR Dominguez-Henkel
Aug 21, 1976·British Medical Journal·J S Vilsvik, J Schaanning
Jan 1, 1977·British Heart Journal·D A RichardsE J Knight
Feb 1, 1978·British Heart Journal·P B DecalmerG M Sterling
Oct 1, 1979·Journal of Neurology, Neurosurgery, and Psychiatry·D JeffersonC D Marsden
Nov 1, 1977·Postgraduate Medical Journal·C M CastledenC F George
Jan 1, 1980·Pharmacology & Therapeutics·S D Seth
Jan 1, 1983·Current Medical Research and Opinion·O De DivitiisV Ligouri
Jan 1, 1977·Current Medical Research and Opinion·N K GostickN P Barmer
Jul 1, 1990·Journal of Neurosurgery·M G YaşargilP Roth
Mar 1, 1994·International Journal of Cardiology·G RufH Roskamm
Jan 1, 1976·The Journal of International Medical Research·A M HarrisJ A Tweed
Apr 1, 1977·Journal of Clinical Pharmacology·J J VallnerI L Honigberg
Jan 1, 1978·British Heart Journal·C RobinsonD Jewitt
Jul 1, 1981·British Journal of Clinical Pharmacology·H R GribbinA E Tattersfield
Nov 1, 1981·British Journal of Clinical Pharmacology·K J ThorleyJ M Cruickshank
Sep 1, 1984·British Journal of Clinical Pharmacology·H J WharradJ M Roland
May 1, 1978·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·P R ReevesM J Winrow
Mar 1, 1989·Journal of Clinical Pharmacology·F GallettiM Mancini
Jan 1, 1993·The American Journal of Physiology·E E BlaakW H Saris

Related Concepts

Tenormin
Dose-Response Relationship, Drug
Drug Evaluation
Pulse Rate
Novodrin
Propanolamines
Rexigen

Related Feeds

Antiarrhythmic Agents: Mechanisms of Action

Understanding the mechanism of action of antiarrhythmic agents is essential in developing new medications as treatment of cardiac arrhythmias is currently limited by the reduced availability of safe and effective drugs. Discover the latest research on Antiarrhythmic Agents: Mechanism of Action here.

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.