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Selected Publication:
Stoschitzky, K; Koshucharova, G; Zweiker, R; Lercher, P; Maier, R; Klein, W; Zitta, S; Gruber, L; Lamprecht, G; Lindner, W.
Exercise does not affect plasma concentrations of (R)- and (S)-carvedilol.
Cardiovasc Drugs Ther. 2002; 16(2):133-140
Doi: 10.1023%2FA%3A1015705516496
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- Leading authors Med Uni Graz
- Stoschitzky Kurt
- Co-authors Med Uni Graz
- Lercher Peter
- Maier Robert
- Zitta Sabine
- Zweiker Robert
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- Abstract:
- 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.
- Find related publications in this database (using NLM MeSH Indexing)
- Administration, Oral -
- Adrenergic beta-Antagonists - blood
- Adult - blood
- Analysis of Variance - blood
- Carbazoles - blood
- Double-Blind Method - blood
- Exercise - blood
- Humans - blood
- Hypertension - drug therapy
- Male - drug therapy
- Middle Aged - drug therapy
- Propanolamines - blood
- Stereoisomerism - blood
- Find related publications in this database (Keywords)
- beta-blockers
- carvedilol
- exercise
- plasma concentrations
- pharmacokinetics