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Aminopyrine demethylation kinetics. Use of metabolite exhalation rates as an index of enhanced mixed-function oxidase activity in vivo

Journal Article · · Drug Metab. Dispos.; (United States)
OSTI ID:5387298
; ;

The usefulness of determining aminopyrine demethylation kinetics via monitoring of metabolite exhalation rates had been assessed. In rats receiving (N-dimethyl-14C)aminopyrine, a biexponential decline in the 14CO2 exhalation rate is apparent when monitoring is continued over a 5 to 6-hr period. Both the fast phase (representing the first demethylation) and the slower phase (representing the second demethylation) are markedly influenced by phenobarbital and promethazine pretreatment. These changes are consistent with enhanced mixed-function oxidase activity. Examination of the urinary excretion products of aminopyrine obtained in these studies support this claim. The sensitivity of the above index of mixed-function oxidase activity is increased considerably by the use of crossover experimental designs. Considerable interanimal variation is observed in the metabolite production in both exhaled air and urine from rats administered aminopyrine.

Research Organization:
Department of Pharmacy, University of Manchester, UK
OSTI ID:
5387298
Journal Information:
Drug Metab. Dispos.; (United States), Journal Name: Drug Metab. Dispos.; (United States) Vol. 9:5; ISSN DMDSA
Country of Publication:
United States
Language:
English

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Related Subjects

550201 -- Biochemistry-- Tracer Techniques
560305* -- Chemicals Metabolism & Toxicology-- Vertebrates-- (-1987)
59 BASIC BIOLOGICAL SCIENCES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMALS
AZOLES
BIOCHEMICAL REACTION KINETICS
CARBON 14 COMPOUNDS
CARBON COMPOUNDS
CARBON DIOXIDE
CARBON OXIDES
CHALCOGENIDES
CLEARANCE
ENZYME ACTIVITY
ENZYMES
EXCRETION
EXHALATION
HETEROCYCLIC COMPOUNDS
IN VIVO
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
METABOLISM
METABOLITES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
OXIDES
OXIDOREDUCTASES
OXYGEN COMPOUNDS
PYRAZOLES
PYRAZOLINES
RATS
REACTION KINETICS
RODENTS
VERTEBRATES