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Studies on concentration–time profiles of nimodipine enantiomers following intravenous and oral administration of nimodipine in patients with subarachnoid hemorrhage
Author(s) -
WannerOlsen Henrik,
Gaarskær Frank B.,
Mikkelsen Erich O.,
Jakobsen Preben,
Voldby Bo
Publication year - 2000
Publication title -
chirality
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.43
H-Index - 77
eISSN - 1520-636X
pISSN - 0899-0042
DOI - 10.1002/1520-636x(2000)12:9<660::aid-chir3>3.0.co;2-1
Subject(s) - nimodipine , chemistry , subarachnoid hemorrhage , enantiomer , oral administration , anesthesia , pharmacology , stereoselectivity , pharmacokinetics , medicine , stereochemistry , organic chemistry , calcium , catalysis
After i.v. and oral administration of nimodipine the concentration–time profiles of the drug and its enantiomers were studied in seven patients with subarachnoid hemorrhage. Concentrations of nimodipine, (+)‐(R)‐, and (‐)‐(S)‐nimodipine were analyzed using a new stereoselective high‐performance liquid chromatographic method. During the first 3 h after oral administration the concentrations of (+)‐(R)‐ and (‐)‐(S)‐nimodipine were significantly different, the (‐)‐(S)‐enantiomer being found in much lesser concentrations compared to the (+)‐(R)‐enantiomer. The results indicate that if uptake from the gastrointestinal system is equal for the two enantiomers, then (‐)‐(S)‐nimodipine is metabolized at a much faster rate compared to (+)‐(R)‐nimodipine after oral administration of the drug in patients with subarachnoid bleeding. After i.v. administration; no significant differences between the concentrations of the (‐)‐(S) and the (+)‐(R) isomers were demonstrated. Chirality 12:660–664, 2000. © 2000 Wiley‐Liss, Inc.