Skip to main content
NCBI home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1976 Oct;3(5):849–855. doi: 10.1111/j.1365-2125.1976.tb00637.x

Assessment of alpha- and beta-adrenoceptor blocking actions of labetalol.

D A Richards, J Tuckman, B N Prichard
PMCID: PMC1428931  PMID: 9968

Abstract

Isoprenaline dose-response curves plotting increases in heart rate before and after labetalol are suggestive of competitive antagonism at beta-adrenoceptor sites. Phenylephrine dose-response curves using increases in systolic pressure before and after labetalol are suggestive of competitive antagonism at alpha-adrenoceptor sites. The ratio of alpha:beta-adrenoceptor antagonism induced by labetalol is approximately 1:3. Peak pharmacological responses after a single oral dose of labetalol (400 mg) occurred between 90-120 min after administration.

Full text

PDF
849

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Boakes A. J., Knight E. J., Prichard B. N. Preliminary studies of the pharmacological effects of 5-[1-hydroxy-2-((1-methyl-3-phenylpropyl)amino)-ethyl] salicylamide (AH 5158) in man. Clin Sci. 1971 Apr;40(4):18P–19P. doi: 10.1042/cs040018pa. [DOI] [PubMed] [Google Scholar]
  2. Brick I., Hutchison K. J., McDevitt D. G., Roddie I. C., Shanks R. G. Comparison of the effects of I.C.I. 50172 and propranolol on the cardiovascular responses to adrenaline, isoprenaline and exercise. Br J Pharmacol. 1968 Sep;34(1):127–140. doi: 10.1111/j.1476-5381.1968.tb07956.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Bühler F. R., Burkart F., Lütold B. E., Küng M., Marbet G., Pfisterer M. Antihypertensive beta blocking action as related to renin and age: a pharmacologic tool to identify pathogenetic mechanisms in essential hypertension. Am J Cardiol. 1975 Oct 31;36(5):653–669. doi: 10.1016/0002-9149(75)90168-x. [DOI] [PubMed] [Google Scholar]
  4. Collier J. G., Dawnay N. A., Nachev C., Robinson B. F. Clinical investigation of an antagonist at alpha- and beta-adrenoceptors-AH5158A. Br J Pharmacol. 1972 Feb;44(2):286–293. doi: 10.1111/j.1476-5381.1972.tb07265.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Cuthbert A. W., Pic P. Adrenoceptors and adenyl cyclase in gills. Br J Pharmacol. 1973 Sep;49(1):134–137. doi: 10.1111/j.1476-5381.1973.tb08277.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. DORNHORST A. C., ROBINSON B. F. Clinical pharmacology of a beta-adrenergic-blocking agent (Nethalide). Lancet. 1962 Aug 18;2(7251):314–316. doi: 10.1016/s0140-6736(62)90104-6. [DOI] [PubMed] [Google Scholar]
  7. ECKSTEIN J. W., ABBOUD F. M. Circulatory effects of sympathomimetic amines. Am Heart J. 1962 Jan;63:119–135. doi: 10.1016/0002-8703(62)90230-2. [DOI] [PubMed] [Google Scholar]
  8. Farmer J. B., Kennedy I., Levy G. P., Marshall R. J. Pharmacology of AH 5158; a drug which blocks both - and -adrenoceptors. Br J Pharmacol. 1972 Aug;45(4):660–675. doi: 10.1111/j.1476-5381.1972.tb08125.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Kennedy I., Levy G. P. Combined alpha- and beta-adrenoceptor blocking drug AH 5158: further studies on alpha-adrenoceptor blockade in anaesthetized animals. Br J Pharmacol. 1975 Apr;53(4):585–592. doi: 10.1111/j.1476-5381.1975.tb07398.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Majid P. A., Meeran M. K., Benaim M. E., Sharma B., Taylor S. H. Alpha- and beta-adrenergic receptor blockade in the treatment of hypertension. Br Heart J. 1974 Jun;36(6):588–596. doi: 10.1136/hrt.36.6.588. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Prichard B. N., Thompson F. O., Boakes A. J., Joekes A. M. Some haemodynamic effects of compound AH 5158 compared with propranolol, propranolol plus hydrallazine, and diazoxide: the use of AH 5158 in the treatment of hypertension. Clin Sci Mol Med Suppl. 1975 Jun;2:97s–100s. doi: 10.1042/cs048097s. [DOI] [PubMed] [Google Scholar]
  12. ROSE G. A., HOLLAND W. W., CROWLEY E. A. A SPHYGMOMANOMETER FOR EPIDEMIOLOGISTS. Lancet. 1964 Feb 8;1(7328):296–300. doi: 10.1016/s0140-6736(64)92408-0. [DOI] [PubMed] [Google Scholar]
  13. White C. B., Udwadia B. P. Beta-adrenoceptors in the human dorsal hand vein, and the effects of propranolol and practolol on venous sensitivity to noradrenaline. Br J Clin Pharmacol. 1975 Apr;2(2):99–105. doi: 10.1111/j.1365-2125.1975.tb01564.x. [DOI] [PMC free article] [PubMed] [Google Scholar]

Articles from British Journal of Clinical Pharmacology are provided here courtesy of British Pharmacological Society

RESOURCES