✦ LIBER ✦

PHARMACOKINETICS OF THE ENANTIOMERS OF VERAPAMIL AFTER INTRAVENOUS AND ORAL ADMINISTRATION OF RACEMIC VERAPAMIL IN A RAT MODEL

✍ Scribed by M. MASOOD BHATTI; ROBERT T. FOSTER

Publisher: John Wiley and Sons
Year: 1997
Tongue: English
Weight: 111 KB
Volume: 18
Category: Article
ISSN: 0142-2782
DOI: 10.1002/(sici)1099-081x(199707)18:5<387::aid-bdd26>3.0.co;2-x

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✦ Synopsis

Verapamil is a chiral calcium channel blocking drug which is useful clinically as the racemate in treating hypertension and arrhythmia. The published pharmacokinetic data for verapamil enantiomers in the rat model are limited. Utilizing a stereospeci®c highperformance liquid chromatographic (HPLC) assay, the enantiomeric disposition of verapamil is reported after intravenous (1´0 mg kg 71 ) and oral (10 mg kg 71 ) administration of racemic verapamil to the rat model. After intravenous administration the systemic clearance of R-verapamil was signi®cantly greater than that of S-verapamil; 34´97 against 23´73´7 mL min 71 kg 71 (meanSD), respectively. After oral administration, the clearance of R-verapamil was signi®cantly greater than that of Sverapamil, 889294 against 351109 mL min 71 kg 71 , respectively. The apparent oral bioavailability of S-verapamil was greater than that of R-verapamil, 0´0740´031 against 0´0410´011, respectively. These data suggest that the disposition of verapamil in the rat is stereoselective; verapamil undergoes extensive stereoselective ®rst-pass clearance after oral administration and the direction of stereoselectivity in plasma is opposite to that observed in the human. &1997 by John Wiley & Sons, Ltd.

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