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  • metabolism  (3)
  • Bioavailability  (1)
  • 1
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 46 (1994), S. 473-475 
    ISSN: 1432-1041
    Schlagwort(e): Phenobarbitone ; phenobarbitone-N-glucoside ; urine ; metabolism
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: 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.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 12 (1977), S. 451-456 
    ISSN: 1432-1041
    Schlagwort(e): Bioavailability ; carbamazepine ; elimination ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The time-courses of plasma carbamazepine concentrations were followed in six apparently healthy adult subjects who, at different times, took single oral drug doses of 200, 400, 500, 600, 700, 800 and 900 mg. There were some suggestions of impaired bioavailability of the drug when given in tablet form. The following values were obtained for various pharmacokinetic parameters:k abs =0.176±0.209 h−1;k=0.0203±0.0055 h−1; T1/2=37.5±13.1 h; VD=0.825±0.1041 · kg−1; Clearance=0.0163±0.0061 l · kg−1. The elimination rate constant showed a statistically significant increase with increasing drug dose. This may help explain the clinical observation that the rate of rise of steady state plasma carbamazepine concentrations tends to decrease with dose increase in patients taking carbamazepine alone.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 3
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 24 (1983), S. 727-732 
    ISSN: 1432-1041
    Schlagwort(e): propranolol ; foetus ; placenta ; metabolism ; pregnancy ; plasma levels ; plasma protein binding ; delivery
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary Propranolol (P) and all of its major known metabolites were found in maternal plasma, cord plasma and neonatal plasma in 10 women at term, irrespective of the P doses administered and the time elapsed (up to 15 h) between administration of the last P dose and delivery. The ratios of cord plasma to simultaneous maternal plasma levels for propranolol and its major metabolites (mean±SD) were: propranolol 0.32±0.17, propranolol glucuronide 0.86±0.36, 4-hydroxypropranolol 1.4±1.0, 4-hydroxypropranolol glucuronide 0.71±0.45 and naphthoxylactic acid 3.0±1.6. P binding in cord plasma at delivery was 67.2±3.9% (mean±SD) which was significantly less (‘t’=13.4,df=13,p〈0.001) than the P binding in maternal plasma at delivery (87.5±1.6%, mean±SD). The plasma protein binding (mean±SD) of naphthoxylactic acid in cord plasma (98.6±0.2%) was significantly greater (‘t’=3.808,df=4,p〈0.02) than the naphthoxylactic acid binding in maternal plasma at delivery (97.6±0.4%). When the simultaneous concentrations of P and naphthoxylactic acid in maternal and cord plasma are compared in conjunction with protein binding and ionic effects, it would seem that metabolism of P does occur in the placental/foetal unit.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 4
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 47 (1994), S. 355-360 
    ISSN: 1432-1041
    Schlagwort(e): Carbamazepine ; metabolism ; autoinduction
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: 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.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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