Key result
Pharmacokinetic analysis of carvedilol in a hypertensive elderly female patient demonstrated higher plasma levels for R(+)-carvedilol than S(-)-carvedilol (AUC 75.64 vs 37.29 ng/ml).
Case Report (n=1)
An enantioselective HPLC method was successfully developed and demonstrated stereoselective pharmacokinetics of carvedilol in a hypertensive patient, with higher plasma levels of the R(+) enantiomer.
Single-case PK data warrant no change in carvedilol dosing; leaves open stereoselective effects in larger elderly cohorts.
An enantioselective high-performance liquid chromatographic method for the analysis of carvedilol in plasma and urine was developed and validated using (-)-menthyl chloroformate (MCF) as a derivatizing reagent. Chloroform was used for extraction, and analysis was performed by HPLC on a C18 column with a fluorescence detector. The quantitation limit was 0.25 ng/ml for S(-)-carvedilol in plasma and 0.5 ng/ml for R(+)-carvedilol in plasma and for both enantiomers in urine. The method was applied to the study of enantioselectivity in the pharmacokinetics of carvedilol administered in a multiple dose regimen (25 mg/12 h) to a hypertensive elderly female patient. The data obtained demonstrated highest plasma levels for the R(+)-carvedilol (AUC(SS) (0-12) 75.64 vs 37.29 ng/ml). The enantiomeric ratio R(+)/S(-) was 2.03 for plasma and 1.49 for urine (Ae(0-12) 17.4 vs 11.7 microg).
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Peccinini et al. (2008) conducted a case report in Hypertension (n=1). Carvedilol was evaluated on Enantioselectivity in the pharmacokinetics of carvedilol. Pharmacokinetic analysis of carvedilol in a hypertensive elderly female patient demonstrated higher plasma levels for R(+)-carvedilol than S(-)-carvedilol (AUC 75.64 vs 37.29 ng/ml).
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