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  • 1
    ISSN: 1432-1041
    Keywords: Phenylbutazone ; 14C-label ; oxyphenbutazone ; gas chromatography ; disposition ; oxidative metabolism ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The absorption and elimination of orally administered14C-phenylbutazone and the role of oxidation in its metabolism have been studied. The main routes of excretion of14C-phenylbutazone and its metabolites were investigated in 3 patients with rheumatoid arthritis, and in 1 patient with a T-tube in the common bile duct. Up to 9 days after an oral dose of14C-phenylbutazone 600 mg (30 µCi) 63% of the radioactivity was found in the urine and 14% had appeared in the faeces. The cumulative excretion of radioactivity in bile amounted to 9.5% of the dose in 4 days. Only 1% of the radioactivity in the urine and bile was due to unchanged phenylbutazone. The role of oxidative metabolism of phenylbutazone in healthy human subjects was studied by gas chromatography. In 3 subjects given a single dose of phenylbutazone 600 mg, only 8.3% of the dose was excreted in urine as oxidized metabolites after 5 days. However, in 5 patients who had taken phenylbutazone for more than 5 weeks, these metabolites accounted for 23.4% of the dose. These results suggest that oxidative metabolism becomes more important after continued administration of the drug. After a single dose of phenylbutazone, the side-chain oxidized metabolite (II) was the major free derivative excreted in urine, but the ring oxidized metabolite, oxyphenbutazone (I), was much more important than the former in plasma. However, after prolonged treatment there was little difference between the concentration of the two metabolites in plasma. This finding suggests that side-chain oxidation is increased relative to ring oxidation on prolonged treatment with phenylbutazone. A third derivative containing hydroxyl groups both in the phenyl ring and in the side-chain (metabolite III) was found in urine in experiments with phenylbutazone, but in only one out of 3 volunteers given repeated doses of oxyphenbutazone.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: thiopental ; diazepam ; placental transfer ; Caesarean section ; neonatal depression
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Drug concentrations were measured in whole blood obtained from mother and child after induction of general anaesthesia with thiopental or diazepam and delivery by Caesarean section. In 27 cases given thiopental 3 mg/kg intravenously the 5-min child/mother concentration ratio rose with increasing injection-delivery (I-D) interval up to 8–10 min. The concentration in the newborn at 2 h showed a similar trend. In 30 cases given diazepam 0.3 mg/kg for sleep induction, there were some low values in cases delivered within 4 min after the injection. However, higher neonatal concentrations and child/mother ratios were observed when the operation lasted 4–5 min, and there was no further increase in cases with longer I-D intervals. There is evidence to suggest that net transfer to the fetus proceeds at a slower rate with thiopental than with diazepam. However, in the present series of low risk elective Caesarean sections, there was no appreciable difference between the induction agents with regard to their effect on the newborn infant.
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  • 3
    ISSN: 1432-1041
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Zusammenfassung In keimfrei aufgezogenen Mäusen werden fast keine einfachen Phenole mit dem Urin ausgeschieden, was auf den Mangel an Darmbakterien zurückzuführen ist.
    Type of Medium: Electronic Resource
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