Beta-adrenoceptor blocking effects and pharmacokinetics of betaxolol (SL 75212) in man

British Journal of Clinical Pharmacology
J F GiudicelliP L Morselli

Abstract

1 The pharmacological effects and the pharmacokinetics of betaxolol (SL 75212), a new beta-adrenoceptor blocking agent, were compared with those of propranolol and a placebo in a double-blind trial involving six healthy volunteers. 2 Heart rate (HR), myocardial contractile force (MCF), systolic blood pressure (SBP) and peak expiratory flow rate (PEFR) were measured at rest and during vigorous exercise before and at intervals up to 25 h after oral administration of the drugs. In addition, plasma renin activity (PRA) at rest and blood levels of betaxolol and propranolol were determined. 3. Betaxolol proved to be a potent and long-lasting beta-adrenoceptor blocking drug, devoid of intrinsic beta-sympathomimetic activity. Its beta-adrenoceptor blocking action was shown to four-fold that of propranolol at the cardiac and renal levels and to last at least 25 h after drug intake. 4 The peak blood level of betaxolol was reached 2 to 4 hr after its administration, the first-pass loss is likely to be low and the half-life is 12.3 h. These pharmacokinetic data are perfectly consistent with the long duration of the pharmacological effects of betaxolol in man.

References

Feb 1, 1978·British Journal of Clinical Pharmacology·D G McDevitt
Jun 1, 1977·Journal of Pharmacokinetics and Biopharmaceutics·R GomeniP L Morselli
Feb 1, 1975·Clinical Pharmacology and Therapeutics·R GuglerH J Dengler
Oct 1, 1975·Clinical Pharmacology and Therapeutics·G R Wilkinson, D G Shand
Apr 1, 1975·British Journal of Clinical Pharmacology·G E MarlinP Turner
Sep 1, 1966·The American Journal of Cardiology·D A Chamberlain
May 1, 1972·The Journal of Clinical Pharmacology and New Drugs·D C HicksM Hills
Nov 23, 1974·British Medical Journal·C R KumanaD M Smith
Jan 1, 1970·Clinical Pharmacology and Therapeutics·D G ShandJ A Oates
Sep 1, 1971·Journal of Pharmaceutical Sciences·M GibaldiS Feldman
Feb 1, 1968·Circulation·A M WeisslerC D Schoenfeld
Apr 1, 1969·The American Journal of Cardiology·A M WeisslerC D Schoenfeld

❮ Previous
Next ❯

Citations

Aug 1, 1990·Journal of Clinical Pharmacology·W H FrishmanD Behrman
Apr 1, 1992·Journal of Clinical Pharmacology·R L WilliamsL B Hogan
Jan 1, 1991·European Journal of Clinical Pharmacology·B J LipworthD G McDevitt
Jan 1, 1985·European Journal of Clinical Pharmacology·M MauryJ F Giudicelli
Jan 1, 1986·European Journal of Clinical Pharmacology·G BianchettiJ P Thenot
Jan 1, 1983·European Journal of Clinical Pharmacology·R Palminteri, G Kaik
Jan 1, 1985·European Journal of Clinical Pharmacology·F Weber, M Anlauf
Jan 1, 1985·European Journal of Clinical Pharmacology·C ThuillezJ F Giudicelli
Jan 1, 1982·European Journal of Clinical Pharmacology·J T Salonen, R Palminteri
Jan 1, 1989·Pharmacology & Therapeutics·M F Sugrue
Jul 5, 2001·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·E Vainio-JylhäR Huupponen
Jul 1, 1990·British Journal of Clinical Pharmacology·N A IrvineD G McDevitt
Feb 1, 1991·British Journal of Clinical Pharmacology·B J LipworthD G McDevitt
Jan 1, 1984·American Journal of Ophthalmology·R B SchoeneC H Beasley
Feb 15, 1985·American Journal of Ophthalmology·J M AtkinsR M Timewell
Dec 15, 1985·American Journal of Ophthalmology·J G Feghali, P L Kaufman
Dec 1, 1987·Journal of Clinical Pharmacy and Therapeutics·J V Okopski
Nov 11, 2009·Current Eye Research·Igor KaisermanShlomo Vinker
Mar 8, 2017·Integrative Biology : Quantitative Biosciences From Nano to Macro·Christian MaassMurat Cirit
Feb 1, 1989·Australian and New Zealand Journal of Ophthalmology·I Goldberg
Jan 1, 1988·Fundamental & Clinical Pharmacology·A BerdeauxJ F Giudicelli
Apr 1, 1991·Postgraduate Medicine·A M ReyJ G Gums
Nov 1, 1990·Survey of Ophthalmology·S L GerberD C Brater

❮ 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.