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  • 1
    ISSN: 1432-1041
    Schlagwort(e): cyclobarbital ; aminopyrine ; liver disease ; 14CO2 breath test ; barbiturate ; pharmacokinetics ; hepatic drug metabolism ; cirrhosis ; alcoholic liver disease ; viral hepatitis
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The exhalation of 14CO2 derived from an i.v. tracer dose of [dimethylamine-14C]aminopyrine has been investigated in normal controls and patients. They subsequently ingested 200 mg cyclobarbital calcium in the evening and the decline in the plasma drug level over the following 2 days was measured by thin-layer chromatography. The peak specific activity of exhaled 14CO2 occurred 0.5–2 h after 14C-aminopyrine injection in the absence of liver disease and in non-cirrhotic liver disorders. It was delayed in certain patients with cirrhosis. Compared to 8 medically healthy subjects, 10 patients with acute viral hepatitis, 8 with cirrhosis and 10 with fatty liver exhibited a significantly increased half-life of 14CO2 exhalation. Normal mean values were found in 12 patients with non-cirrhotic alcoholic liver disease and in 14 patients with non-hepatic diseases. The cyclobarbital (CB) half-life was prolonged and the clearance reduced in patients with viral hepatitis, cirrhosis, or alcoholic liver damage as compared to data from 17 control subjects. Due to a larger apparent volume of distribution, patients with fatty liver disease had an increased CB half-life, although its clearance was normal. A close negative correlation was detected between the clearance and the logarithm of the CB level measured 36 h after drug ingestion. The oral CB test evaluated from a single blood sample taken about 36 h after drug administration appears to be a useful indicator of human drug metabolising capacity. Discrimination between patients with and without disordered liver function was similar in the two drug elimination tests.
    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 21 (1982), S. 521-528 
    ISSN: 1432-1041
    Schlagwort(e): aminopyrine ; breath test ; metabolites ; plasma levels ; drug metabolism
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary [Dimethylamine-14C]-aminopyrine was given i.v. to 5 healthy volunteers and 5 medical patients in a dose of 1.67 mg/kg, containing 0.02 µCi/kg 14C. In 4 volunteers the experiment was repeated using oral administration of aminopyrine. Exhalation of 14CO2 was followed for 6–10 h and plasma levels of the drug and of its metabolites 4-methylamino-antipyrine, 4-amino-antipyrine, 4-acetylamino-antipyrine and 4-formylamino-antipyrine, were measured by thin-layer chromatography. The concentration-time profiles of the metabolites mostly failed to conform to a Bateman function. Areas under the curves from 1 to 6 h after dosing indicated distinct interindividual differences in metabolite patterns even in the absence of disturbed liver function, whereas the intraindividual data were closely reproducible. In most subjects, the area of 4-formylamino-antipyrine exceeded that of the acetyl analogue. The metabolite patterns did not exhibit a consistent relationship to the ratios between 14CO2 half-life in breath and aminopyrine half-life in plasma, which varied from 1.4 to 3.2.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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