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  • 1
    Electronic Resource
    Electronic Resource
    Early stage autoinduction of carbamazepine metabolism in humans (1994)
    Springer
    European journal of clinical pharmacology 47 (1994), S. 355-360 
    Details
    ISSN: 1432-1041
    Keywords: Carbamazepine ; metabolism ; autoinduction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Six healthy young adult male volunteers were given two 600 mg (2540 μ 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− (difference 0.26 l·h−, 95% confidence interval 0.11 to 0.41 l·h−) 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.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00191168
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  • 2
    Electronic Resource
    Electronic Resource
    Phenytoin metabolism during pregnancy (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 389-392 
    Details
    ISSN: 1432-1041
    Keywords: Phenytoin, Pregnancy ; metabolism, p-HPPH pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The steady-state 72 h urinary excretion of various phenytoin metabolites has been measured in 10 epileptic women, whose plasma phenytoin concentrations relative to the phenytoin dose fell during pregnancy and rose again post-partum. In later pregnancy and post parturn, a mean of 61.3 % and 48.9 %, respectively, of the total daily phenytoin dose was eliminated as 5-(4-hydroxyphenyl)-5-phenylhydantoin (p-HPPH). Even thoughp-HPPH accounts for not much more than half the total daily phenytoin dose, increased excretion of this metabolite sufficed to account for the elimination of the entire increase in the dose of phenytoin required during pregnancy. There was no definite increase in the excretion of any other (minor) metabolite measured. Thus pregnancy seems not to enhance uniformly the capacity of the various metabolic pathways of phenytoin.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02220614
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Urinary excretion of phenobarbitone and its metabolites in chronically treated patients (1994)
    Springer
    European journal of clinical pharmacology 46 (1994), S. 473-475 
    Details
    ISSN: 1432-1041
    Keywords: Phenobarbitone ; phenobarbitone-N-glucoside ; urine ; metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The elimination of phenobarbitone (PB) was studied in 14 chronically treated epileptic patients under steady state conditions. PB, [S]-PB-N-glucoside ([S]-PB-N-G) and p-hydroxy-PB (p-OH-PB) were assayed in urine by a HPLC method. Some 57 % of the daily dose was recovered in urine, 14 % as [S]-PB-N-G, 16 % as p-OH-PB (conjugated plus non-conjugated) and 27 % as unaltered PB. Thus PB-N-G formation contributed significantly to the elimination of PB during long-term administration of the drug, and there was reason to suspect that some of the PB-N-G formed may have already been degraded to untraced products before excretion from the body.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00191914
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    Paper (German National Licenses)
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