The effect of norethynodrel, norethindrone and ethynodiol diacetate on hepatic microsomal drug metabolism
| Autor: | Monroe E. Wall, J Martin, E Amerson, RI Freudenthal |
|---|---|
| Rok vydání: | 1974 |
| Předmět: |
Pentobarbital
medicine.medical_specialty Time Factors Absorption (skin) In Vitro Techniques Reductase Pharmacology Mixed Function Oxygenases Ethynodiol Diacetate Cytochrome P-450 Enzyme System Internal medicine medicine Animals Cytochrome Reductases Progesterone Aniline Compounds Chemistry Body Weight Metabolism Norethynodrel Rats Endocrinology Microsomes Liver Microsome Norethindrone Sleep Drug metabolism Aminopyrine N-Demethylase medicine.drug |
| Zdroj: | Pharmacological Research Communications. 6:457-468 |
| ISSN: | 0031-6989 |
| Popis: | The effects of ethynodiol diacetate norethindtone and norethynodrel on the hepatic microsomal drug metabolizing enzyme system of rat were studied. 10 or 50 mg norethynodren/kg or 50 mg norethindrone/kg markedly increased the duration of pentobarital-induced sleep. When the rats were pretreated with 10 or 50 ethynodiol diacetate/kg or 10 mg norethindrone/kg the duration of pentobarbital-induced sleep was not altered. These steroids had no effect on sodium barbital induced sleep which suggested an inhibitory action of the metabolism of pentobarbital. The steroids markedly inhibited the N-dimethylation of aminopyrine the p-hydroxylation of aniline and the side-chain oxidation of pentobarbital during in vitro incubations. Spectral studies revealed that the 3 progestins are Type 1 substrates with an absorption maximum at 390 mM and a minimum at 424 mM. Chronic pretreatment did not cause a change in the amount of microsomal protein/gm liver the concentration of cytochrom P-450 the rate of reduction of P-450 by P-450 reductase or on the duration of pentobarbital-induced sleep. However a significant decrease in the rate of daily body weight gain in rats pretreated with the synthetic progestins was seen (p less than .01). |
| Databáze: | OpenAIRE |
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