Summary
The inducing effect of feprazone, a pyrazolone anti-inflammatory agent, on hepatic drug-metabolizing enzymes has been studied in healthy volunteers. The ratio of 6β-hydroxycortisol (6β-OHF) to 17-hydroxycorticosteroids (17-OHCS) in urine, used as an indicator of oxidative drug-metabolizing enzyme activity, was increased up to 1.6-times the original level after 5 days of oral treatment with feprazone 300 mg/day. This indicates that feprazone induces hepatic drug-metabolising enzymes in man as does phenylbutazone.
References
Bianchi C, Lumachi B, Marazzi-Uberti E (1972) Pharmacological investigations of 4-prenyl-1, 2-diphenyl-3, 5-pyrazolidinedione (DA2370). Part 1: Anti-inflammatory, analgesic and antipyretic properties. Arzneimittelforsch 22: 183–190
Marazzi-Uberti E, Bianchi C, Gaetani M, Pozzi L (1972) Pharmacological investigations of 4-prenyl-1, 2-diphenyl-3, 5-pyrazolidinedione (DA2370). Part 2: Ulcerogenic effects in rats and dogs. Arzneimittelforsch 22: 191–196
Kuntzman R, Jacobson M, Conney AH (1966) Effect of phenylbutazone on cortisol metabolism in man. Pharmacologist 8: 195
Conney AH (1967) Pharmacological implications of microsomal enzyme inductionl. Pharmacol Revs 19: 317–366
Morita K, Hayashi Y, Ono T, Shimakawa H (1986) Comparison of the effects of feprazone and phenylbutazone on testosterone hydroxylations in mouse hepatic microsomes. Chem Pharm Bull (Tokyo) 34: 214–220
Ono T, Tanida K, Shibata H, Konishi H, Shimakawa H (1986) High-performance liquid chromatographic determination of 6β-hydroxycortisol in urine. Chem Pharm Bull (Tokyo) 34: 2522–2527
Nishikaze O, Furuya E (1969) A new method for the determination of 17-OHCS (Porter-Silver chromagen) in urine. I. the effect of sodium sulfate on the β-glucuronidase catalyzed reduction. Rinshobyori (in Japanese) 17: 634–638
Silver RH, Porter CC (1954) The determination of 17, 21-dihydroxy-20-ketosteroids in urine and plasma. J Biol Chem 210: 923–932
Ohnhaus EE, Park BK (1979) Measurement of urinary 6β-hydroxycortisol excretion as an in vivo parameter in the clinical assessment of the microsomal enzyme-inducing capacity of antipyrine, phenobarbitone and rifampicin. Eur J Clin Pharmacol 15: 139–145
Saenger P, Forster E, Kream J (1981) 6β-hydroxycortisol: A noninvasive indicator of enzyme induction. J Clin Endocrinol Metab 52: 381–384
Kuntzman R, Jacobson M, Levin W, Conney AH (1968) Stimulatory effect of N-phenylbarbital (phetharbital) on cortisol hydroxylation in man. Biochem Pharmacol 17: 565–571
Solomon HM, Reich S, Spirt N, Abrams WB (1971) Interaction between digitoxin and other drugs in vitro and in vivo. Ann NY Acad Sci 179: 362–368
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Morita, K., Shibata, H., Ono, T. et al. Inducing effect of feprazone on hepatic drug-metabolizing enzymes in man. Eur J Clin Pharmacol 31, 117–118 (1986). https://doi.org/10.1007/BF00870999
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00870999