Drug metabolism in rats with arthritis induced by 6-sulfanilamidoindazole (6-SAI).

Abstract

Hexobarbital sleeping time was prolonged and ethylmorphine N-demethylation was inhibited after a single dosage or seven administration of 6-SAI to old rats. These effects were independent of the development of arthritis. Changes in cytochrome P-450 concentration after 6-SAI treatment were insignificant and thus not responsible for the decrease in drug metabolism. In vitro 6-SAI inhibited ethylmorphine N-demethylation; the inhibition was of a mixed type. 6-SAI bound to cytochrome P-450 and induced a type II spectrum. The magnitude of hexobarbital-induced type I spectral changes was diminished by 6-SAI. It is concluded that 6-SAI inhibits cytochrome P-450-dependent drug metabolism by binding to cytochrome P-450.

• Authors: D Müller, R Hirschelmann
• Journal: Agents and actions (Agents Actions) Vol. 11 Issue 6-7 Pg. 736-40 (Dec 1981) ISSN: 0065-4299 [Print] Switzerland
• PMID: 7340465 (Publication Type: Journal Article)

Chemical References

• Indazoles
• Pharmaceutical Preparations
• Sulfanilamides
• 6-sulfanilamidoindazole
• Cytochrome P-450 Enzyme System
• Hexobarbital
• Mixed Function Oxygenases

Topics

• Animals
• Arthritis (chemically induced, metabolism)
• Biotransformation
• Cytochrome P-450 Enzyme System (metabolism)
• Hexobarbital (pharmacology)
• Indazoles (pharmacology)
• Kinetics
• Male
• Mixed Function Oxygenases (metabolism)
• Pharmaceutical Preparations (metabolism)
• Rats
• Rats, Inbred Strains
• Sleep (drug effects)
• Sulfanilamides (pharmacology)