| Exercise does not affect plasma concentrations of (R)- and (S)-carvedilol. | |
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MedLine Citation:
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PMID: 12090906 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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PURPOSE: In vitro studies have shown that beta-blockers are taken up into and released from adrenergic cells. As a consequence, plasma concentrations of beta-blockers increase during exercise together with those of epinephrine and norepinephrine. However, effects of exercise on plasma concentrations of (R)- and (S)-carvedilol are unknown. METHODS: Twelve healthy males received oral single doses of 12.5 mg (R)-carvedilol, 12.5 mg (S)-carvedilol and 25 mg (R,S)-carvedilol in a cross-over fashion; 11 patients with essential arterial hypertension were given 25 mg (R,S)-carvedilol. Exercise was performed 3 hours following drug intake, and blood samples were taken at rest, at the end of exercise, and after 15 min of recovery. Plasma concentrations of (R)- and (S)-carvedilol were determined by HPLC. RESULTS: Plasma concentrations of (R)-carvedilol were 2- to 3-fold higher than those of (S)-carvedilol (p < 0.05 in all cases). Plasma concentrations of both (R)- and (S)-carvedilol remained unaffected during exercise and recovery. CONCLUSIONS: Contrary to all other beta-blockers so far investigated, exercise had no effect on plasma concentrations of (R)- and (S)-carvedilol. We conclude that neither (R)- nor (S)-carvedilol is released from adrenergic cells during exercise, a feature that clearly distinguishes carvedilol from other beta-blockers. Thus, the human organism appears to handle (R)- and (S)-carvedilol differently than other beta-adrenoceptor antagonists. This finding deserves further investigation on a molecular and cellular level in order to clarify these differences between the pharmacokinetics of carvedilol and other beta-blockers. |
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Authors:
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Kurt Stoschitzky; Gergana Koshucharova; Robert Zweiker; Peter Lercher; Robert Maier; Werner Klein; Sabine Zitta; Leonhard Gruber; Günther Lamprecht; Wolfgang Lindner |
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Publication Detail:
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Type: Clinical Trial; Comparative Study; Journal Article; Randomized Controlled Trial |
Journal Detail:
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Title: Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy Volume: 16 ISSN: 0920-3206 ISO Abbreviation: Cardiovasc Drugs Ther Publication Date: 2002 Mar |
Date Detail:
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Created Date: 2002-07-01 Completed Date: 2003-03-28 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8712220 Medline TA: Cardiovasc Drugs Ther Country: United States |
Other Details:
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Languages: eng Pagination: 133-40 Citation Subset: IM |
Affiliation:
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Division of Cardiology, Karl Franzens University, Graz, Austria. kurt.stoschitzky@uni-graz.at |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Adrenergic beta-Antagonists / blood*, chemistry, pharmacokinetics Adult Analysis of Variance Carbazoles / blood*, chemistry, pharmacokinetics Double-Blind Method Exercise* Humans Hypertension / drug therapy, metabolism Male Middle Aged Propanolamines / blood*, chemistry, pharmacokinetics Stereoisomerism |
| Chemical | |
Reg. No./Substance:
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0/Adrenergic beta-Antagonists; 0/Carbazoles; 0/Propanolamines; 72956-09-3/carvedilol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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