Comparative pharmacodynamics and plasma levels of beta-adrenoceptor blocking drugs

British Journal of Clinical Pharmacology
R GuglerG Bodem

Abstract

1. Metoprolol (ME), pindolol (PI) and propranolol (PR) were studied in nine subjects at different doses and at 'maximum beta-adrenoceptor blockade' at a defined exercise load. Exercise tests were performed after each dosing period; isoprenaline stimulation was studied at the highest dose level. 2. ME and PR reduced heart rate at rest with most doses tested, while PI had no effect on resting heart rate. 3. Exercise heart rate was reduced with the smallest daily doses (ME 75 mg; PI 7.5 mg; PR 60 mg), and maximum reduction was from 163 to 116 beats/min (ME), 124 (PT) and 115 (PR) beats/min with daily doses of 242, 23 and 233 mg, respectively. 4. Resting blood pressure was not significantly affected by any beta-adrenoceptor blocker dose, but exercise induced blood pressure decreased from 166 to 130 (ME), 138 (PI) and 131 (PR) mm Hg, respectively. 5. Mean plasma concentrations at 'maximum beta-adrenoceptor blockade' were 158 (ME), 24 (PI) and 159 (PR) ng/ml without significant differences in the plasma level variation between beta-adrenoceptor blockers. 6. Isoprenaline doses required to increase heart rate by 30 beats/min were 3.8 microgram (control), 22 microgram (ME), 458 microgram (PI) and 200 microgram (PR), respectively. The di...Continue Reading

References

Dec 1, 1976·Drugs·H J Waal-Manning
Jan 1, 1976·Clinical Pharmacokinetics·G Johnsson, C G Regàrdh
May 1, 1977·Clinical Pharmacology and Therapeutics·D G McDevittR G Shanks
Feb 1, 1975·Thorax·E SowtonI Baker
Mar 17, 1978·European Journal of Clinical Pharmacology·R Gugler, G Bodem
Feb 1, 1975·Clinical Pharmacology and Therapeutics·R GuglerH J Dengler
Apr 1, 1973·The Journal of Clinical Investigation·G BodemC A Chidsey
May 1, 1973·British Medical Bulletin·J W Black, B N Prichard
Sep 26, 1973·Journal of Chromatography·E Di SalleP L Morselli
Jul 1, 1969·Progress in Cardiovascular Diseases·D Gibson, E Sowton

❮ Previous
Next ❯

Citations

Dec 1, 1985·British Journal of Clinical Pharmacology·P C O'ConnorR G Shanks
Jan 1, 1985·Acta Medica Scandinavica. Supplementum·U Thadani
Jan 1, 1986·European Journal of Clinical Pharmacology·P H Held, C G Regårdh
Mar 1, 1985·British Journal of Clinical Pharmacology·P C O'ConnorR G Shanks
Jan 1, 1988·European Journal of Clinical Pharmacology·R KoopmansC J van Boxtel
Jan 1, 1988·European Journal of Clinical Pharmacology·S LindebergB Sandström
Jan 1, 1983·European Journal of Clinical Pharmacology·M T SmithE J Triggs
Dec 1, 1991·Clinical Autonomic Research : Official Journal of the Clinical Autonomic Research Society·C Nyarko-Adomfeh
Jul 1, 1983·Klinische Wochenschrift·U Klotz, I Reimann

❮ Previous
Next ❯

Related Concepts

Related Feeds

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.