Summary
The pharmacokinetics of a single oral dose of 20 mg (+)-, (-)- and racemic homochlorcyclizine (HCZ) have been studied in humans. The formation of the quarternary ammonium-linked glucuronide was an important metabolic pathway, and the metabolic process was enantioselective as a result of differing urinary excretion rates of (+)-, (-)- and racemic glucuronide.
There were significant differences between (+)-, (-) and racemic HCZ in AUC (0-14 h) and plasma protein binding, but all HCZ enantiomers were slowly absorbed and eliminated (elimination half-lives about 11 h).
The results shows help to establish a more efficient dosage regimen for HCZ therapy.
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Nishikata, M., Nomura, A., Iseki, K. et al. Enantioselective pharmacokinetics of homochlorcyclizine II: disposition and metabolism of (+)-, (−)- and racemic homochlorcyclizine after oral administration to man. Eur J Clin Pharmacol 43, 533–538 (1992). https://doi.org/10.1007/BF02285097
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DOI: https://doi.org/10.1007/BF02285097