Plasma and urinary metabolites of efonidipine hydrochloride in man.
1. The plasma and urinary metabolite profiles of efonidipine hydrochloride, a new dihydropyridine calcium antagonist, have been examined in six healthy male volunteers after oral dosing. 2. Unchanged drug in plasma was determined by hplc-ms. Five metabolites in plasma and five metabolites and unchanged drug in urine were identified by hplc. 3. The main plasma metabolites were N-dephenylated-efonidipine and deaminated-efonidipine. 4. No significant amount of unchanged drug was excreted in urine. In the urine collected for 24 h after a oral dosing, 1.1% of the dose was excreted as deaminated-efonidipine, and 0.5% as a pyridine analogue of deaminated-efonidipine.
Nakabeppu
H
H
Shiraoka Research Station of Biological Science, Nissan Chemical Industries, Ltd, Saitama, Japan.
Asada
M
M
Oda
T
T
Shinozaki
Y
Y
Yajima
T
T
D000328:Adult; D000818:Animals; D001711:Biotransformation; D002121:Calcium Channel Blockers / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D002851:Chromatography, High Pressure Liquid; D004095:Dihydropyridines / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D004285:Dogs; D006801:Humans; D008297:Male; D013058:Mass Spectrometry; D009596:Nitrophenols; D009943:Organophosphorus Compounds / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D051381:Rats; D013045:Species Specificity
D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D009596:Nitrophenols; D009943:Organophosphorus Compounds; C066425:efonidipine