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Restrict the search for
carvedilol
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Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
(R)-carvedilol, an enantiomer of the drug carvedilol, which is used in the treatment of mild to moderate congestive heart failure. (R)-carvedilol is an alpha adrenergic receptor blocker. It was shown, that (R)-carvedilol increased sympathetic tone, presumably as a physiological reaction to the decrease in blood pressure caused by alpha-blockade. The weak clinical net effect of beta-blockade of (R, S)-carvedilol at rest might be one reason why this drug causes fewer side effects than other beta-blockers, such as a reduction of nocturnal melatonin release.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
(S)-carvedilol, an enantiomer of the drug carvedilol, which is used in the treatment of mild to moderate congestive heart failure. (S)-carvedilol is an alpha- and beta-adrenergic receptor blocker. It was shown, that only (S)-carvedilol caused beta-blockade. It was suggested, that the weak clinical net effect of beta-blockade of (R, S)-carvedilol at rest could be one reason why this drug causes fewer side effects than other beta-blockers, such as a reduction of nocturnal melatonin release.
4'-Hydroxycarvedilol is a metabolite of Carvedilol. Incubation of R (+) - and S(-)-carvedilol with rat liver microsomes showed the formation of four oxidative metabolites: 1-hydroxycarvedilol (1-OHC), 8-hydroxycarvedilol (8-OHC), 4'-hydroxycarvedilol (4'-OHC), and O-desmethylcarvedilol (DesC). From in vivo metabolism studies were obtained, that 1-OHC and 8-OHC were the major products for both enantiomers used as a substrate. Also was invented, that 4'-hydroxycarvedilol slightly more effective than carvedilol in suppressing of store overload-induced calcium release (SOICR) through the cardiac ryanodine receptor (RyR2), which can trigger ventricular arrhythmias.
