The antihypertensive effects of the new cardioselective beta-blocker celiprolol and acebutolol have been compared. Thirty patients with arterial hypertension WHO Grade I-II were treated in a double-blind fashion with celiprolol or acebutolol. Before starting the treatment and on Days 15 and 29, before the morning dose, blood samples were taken for measurement of the plasma level of celiprolol. At the same times physical examinations, and clinical and urine chemistry analyses were performed. At the 99% probability level both drugs had significantly lowered the systolic and diastolic blood pressures to normal values at the end of the second and fourth weeks. There was no significant difference between their antihypertensive efficacy. The decrease in diastolic blood pressure at the end of the second week was significantly correlated with the reciprocal of the plasma celiprolol concentration at steady-state at the end of the dosage interval.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1007/BF00614547 | DOI Listing |
Arch Pharm (Weinheim)
September 2016
Faculty of Pharmacy, Department of Chemical Theory of Drugs, Comenius University in Bratislava, Bratislava, Slovakia.
The structure-activity relationships of 13 analogs of aryloxyaminopropanol type derived from 2-hydroxyphenylethanone as potential β-blockers are described. The synthesized compounds possess an isopropyl or a tert-butyl group in the hydrophilic part of the molecule and an alkoxymethyl substitution in the lipophilic moiety. The target compounds were prepared by an established four-step method and their structures were confirmed by interpretation of their UV, IR, (1) H NMR and (13) C NMR spectra, and by elemental analysis.
View Article and Find Full Text PDFCochrane Database Syst Rev
November 2014
Department of Anesthesiology, Pharmacology and Therapeutics, University of British Columbia, 2176 Health Sciences Mall, Vancouver, BC, Canada, V6T 1Z3.
Background: Partial agonists are a subclass of beta blockers used to treat hypertension in many countries. Partial agonist act by stimulating beta receptors when they are quiescent and blocking beta receptors when they are active. The blood pressure (BP) lowering effect of partial agonist beta blockers has not been quantified.
View Article and Find Full Text PDFJ Chromatogr B Analyt Technol Biomed Life Sci
September 2012
Department of Clinical Pharmacology and Therapeutics, Oita University Faculty of Medicine, Hasama-machi, Yufu-shi, Oita 879-5593, Japan.
A new method of analysis has been developed and validated for the determination of plasma celiprolol concentration. Plasma samples (1 ml) were pre-purified by solid-phase extraction with Bond Elut C18. The separation was achieved with XBridge C18 column (150 mm × 3.
View Article and Find Full Text PDFBr J Clin Pharmacol
November 2010
Department of Medicine and Lawson Health Research Institute, London Health Sciences Centre Department of Physiology & Pharmacology, University of Western Ontario, London, Ontario, Canada.
A new type of interaction in which fruit juices diminish oral drug bioavailability through inhibition of uptake transport is the focus of this review. The discovery was based on an opposite to anticipated finding when assessing the possibility of grapefruit juice increasing oral fexofenadine bioavailability in humans through inhibition of intestinal MDR1-mediated efflux transport. In follow-up investigations, grapefruit or orange juice at low concentrations potentially and selectively inhibited in vitro OATP1A2-mediated uptake compared with MDR1-caused efflux substrate transport.
View Article and Find Full Text PDFEnviron Sci Technol
February 2010
Federal Institute of Hydrology, D-56068 Koblenz, Am Mainzer Tor 1, Germany.
The fate of beta blockers (atenolol, acebutolol, bisoprolol, celiprolol, metoprolol, nadolol, pindolol, propranolol, and sotalol) was studied in surface water-sediment systems. A new analytical method was developed to determine the beta blockers in sediments by LC-ESI-tandem MS detection. The relative recoveries in sediments ranged from 89 +/- 7% (acebutolol) to 102 +/- 3% (nadolol) using deuterated surrogate standards.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!