Document Detail

Early stage autoinduction of carbamazepine metabolism in humans.
MedLine Citation:
PMID:  7875188     Owner:  NLM     Status:  MEDLINE    
Six healthy young adult male volunteers were given two 600 mg (2540 mu moles) oral doses of carbamazepine (CBZ) 5 days apart. Serial concentrations of CBZ and its 10,11-epoxy (CBZ-epoxide) and 10,11-dihydro-10,11-trans-dihydroxy (CBZ-diol) metabolites in plasma, and daily excretions of these substances and the 2-hydroxy (2-OH-CBZ), 3-hydroxy (3-OH-CBZ) and 9-hydroxymethyl-10-carbamoylacridan (acridan) metabolites in urine were followed for 5 days after each dose. Pharmacokinetic analysis showed that autoinduction of CBZ metabolism was present within 6-10 days of the initial drug dose. The mean oral clearance of CBZ increased from 1.48 to 1.74 l.h-1 (difference 0.26 l.h-1, 95% confidence interval 0.11 to 0.41 l.h-1) and the mean percentage urinary recovery of the amount of CBZ eliminated increased from 41.8% to 44.6% (difference 2.8%, 95% confidence interval 0.5 to 5%) between the two studies 5 days apart. The data for daily clearance to metabolite and the time-courses of the plasma CBZ-epoxide to CBZ and CBZ-diol to CBZ concentration ratios suggested that autoinduction had begun by the second day after CBZ intake, and involved not only the epoxide-diol pathway but, to a lesser extent, the oxidations to phenolic derivatives.
I Bernus; R G Dickinson; W D Hooper; M J Eadie
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of clinical pharmacology     Volume:  47     ISSN:  0031-6970     ISO Abbreviation:  Eur. J. Clin. Pharmacol.     Publication Date:  1994  
Date Detail:
Created Date:  1995-04-06     Completed Date:  1995-04-06     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1256165     Medline TA:  Eur J Clin Pharmacol     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  355-60     Citation Subset:  IM    
Department of Medicine, Royal Brisbane Hospital, Queensland, Australia.
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MeSH Terms
Acridines / metabolism
Carbamazepine / analogs & derivatives,  blood,  metabolism*,  pharmacokinetics,  urine
Confidence Intervals
Reg. No./Substance:
0/Acridines; 298-46-4/Carbamazepine; 35079-97-1/10,11-dihydro-10,11-dihydroxy-5H-dibenzazepine-5-carboxamide; 36507-30-9/carbamazepine epoxide; 92-81-9/acridan

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