PMID: 22454938Dec 1, 1974

The effects of oral AH 5158, a combined α and β-adrenoceptor antagonist, in healthy volunteers

British Journal of Clinical Pharmacology
D A RichardsJ G Maconochie

Abstract

1 In healthy male volunteers after single oral doses, AH 5158 produced inhibition of exercise induced tachycardia, falls in systolic and diastolic pressure at rest and in response to exercise, which are probably related to combined β- and α-adrenoceptor antagonism. 2 At increasing doses from 100 mg to 400 mg there exists a dose related antagonistic effect, though the dominant effect of β-adrenoceptor antagonism is more easily demonstrable than is α antagonism. 3 As indicated by the pattern of pharmacological effects, absorption of the oral drug is good and the duration of action of a 400 mg dose is approximately 8 hours. 4 Despite being administered in β-adrenoceptor blocking doses, AH 5158 had no adverse effects upon peak expiratory flow at rest or in response to exercise. 5 It is concluded that the pharmacological profile of this combined α- and β-adrenoceptor antagonism suggests a potential therapeutic role as an antihypertensive drug.

References

May 6, 1972·Lancet·L Beilin, B E Juel-Jensen
Feb 1, 1972·British Journal of Pharmacology·J G CollierB F Robinson
Aug 1, 1972·British Journal of Pharmacology·J B FarmerR J Marshall
Aug 1, 1974·British Journal of Clinical Pharmacology·G M BerlyneC Yoran

Citations

Jan 3, 1977·European Journal of Clinical Pharmacology·D A RichardsL E Martin
Jan 1, 1978·General Pharmacology·A G Blakeley, R J Summers
Jan 1, 1981·General Pharmacology·D E Potter, J M Rowland
Oct 1, 1976·British Journal of Clinical Pharmacology·D A RichardsB N Prichard
Feb 1, 1977·British Journal of Clinical Pharmacology·D A RichardsJ G Maconochie
Apr 1, 1977·British Journal of Clinical Pharmacology·J G MaconochieD A Richards
Sep 1, 1979·Postgraduate Medical Journal·M A Frais, T J Bayley
Jan 1, 1980·Current Medical Research and Opinion·J TuomilehtoJ Elo
Aug 1, 1984·British Journal of Clinical Pharmacology·D P NichollsR G Shanks
Dec 1, 1985·British Journal of Clinical Pharmacology·P C O'ConnorR G Shanks
Jun 1, 1980·British Journal of Clinical Pharmacology·O ThulesiusE Berlin
Sep 1, 1981·British Journal of Clinical Pharmacology·A J Riley, E J Riley
Aug 1, 1976·Australian and New Zealand Journal of Medicine·E A RoseiP M Trust
Oct 1, 1979·Scottish Medical Journal·D G Lambie
Jun 1, 1982·British Journal of Clinical Pharmacology·T TakedaR Shigiya
Apr 5, 1980·The Medical Journal of Australia·I MacdonaldP Kincaid-Smith
Apr 1, 1979·British Journal of Clinical Pharmacology·B N Prichard, D A Richards

Related Concepts

Antihypertensive Agents
Human Volunteers
Hydrocarbons, Aromatic
Alpha-adrenergic receptor
Beta-adrenergic receptor
Tachycardia
Oral Cavity
Antagonists
Diastolic Blood Pressure
Patterns

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