ISSN:
1432-1041
Keywords:
aminopyrine
;
breath test
;
metabolites
;
plasma levels
;
drug metabolism
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00542049
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