Metabolism of medroxyprogesterone acetate (MPA) via CYP enzymes in vitro and effect of MPA on bleeding time in female rats in dependence on CYP activity in vivo

Life Sciences

Volumn 73, Issue 25, 2003, Pages 3201-3212

  Mimura, Nobuhito ^a   Kobayashi, Kaoru ^a   Nakamura, Yoshika ^a   Shimada, Noriaki ^b   Hosokawa, Masakiyo ^a   Chiba, Kan ^a  

^a CHIBA UNIVERSITY   (Japan)

^b NONE

Author keywords

cDNA expression system; Hypercoagulation; MPA; P450; Rat liver microsomes

Indexed keywords

CYTOCHROME P450; CYTOCHROME P450 1A; CYTOCHROME P450 2A2; CYTOCHROME P450 2B; CYTOCHROME P450 2C; CYTOCHROME P450 3A; CYTOCHROME P450 3A1; CYTOCHROME P450 3A2; CYTOCHROME P450 INHIBITOR; ENZYME ACTIVATOR; FURAFYLLINE; ISOENZYME; KETOCONAZOLE; MEDROXYPROGESTERONE ACETATE; PHENOBARBITAL; PROADIFEN; RECOMBINANT ENZYME; SULFAPHENAZOLE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLEEDING TIME; CATALYSIS; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG CLEARANCE; DRUG EFFECT; DRUG METABOLISM; ENZYME ACTIVITY; ENZYME ASSAY; FEMALE; HYPERCOAGULABILITY; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; NONHUMAN; RAT; SEX DIFFERENCE;

EID: 0141886331     PISSN: 00243205     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.lfs.2003.05.004     Document Type: Article

References (17)

1. Daujat M., Peryt B., Lesca P., Fourtanier G., Domergue J., Maurel P. Omeprazole, an inducer of human CYP1A1 and 1A2, is not a ligand for the Ah receptor. Biochemical and Biophysical Research Communications. 188(2):1992;820-825.
2. Etienne M.C., Milano G., Frenay M., Renee N., Francois E., Thyss A., Schneider M., Namer M. Pharmacokinetics and pharmacodynamics of medroxyprogesterone acetate in advanced breast cancer patients. Journal of Clinical Oncology. 10(7):1992;1176-1182.
3. Guengerich F.P., Wang P., Davidson N.K. Estimation of isozymes of microsomal cytochrome P-450 in rats, rabbits, and humans using immunochemical staining coupled with sodium dodecylsulfate-polyacrylamide gel electrophoresis. Biochemistry. 21(5):1982;1698-1706.
4. Kobayashi K., Mimura N., Fujii H., Minami H., Sasaki Y., Shimada N., Chiba K. Role of human cytochrome P450 3A4 in metabolism of medroxyprogesterone acetate. Clinical Cancer Research. 6(8):2000;3297-3303.
5. Laemmli U.K. Cleavage of structural proteins during the assembly of the head of bacteriophage T4. Nature. 227(259):1970;680-685.
6. Morris D.L., Davila J.C. Analysis of rat cytochrome P450 isoenzyme expression using semi-quantitative reverse transcriptase-polymerase chain reaction (RT-PCR). Biochemical Pharmacology. 52(5):1996;781-792.
7. Newton D.J., Wang R.W., Lu A.Y.H. Cytochrome P450 inhibitors. Evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metabolism and Disposition. 23(1):1995;154-158.
8. Nobukata H., Katsuki Y., Ishikawa T., Inokuma M., Shibutani Y. Effect of dienogest on bleeding time, coagulation, fibrinolysis, and platelet aggregation in female rats. Toxicology Letters. 104(1-2):1999;93-101.
9. Ohtsu T., Fujii H., Wakita H., Igarashi T., Itoh K., Imoto S., Kohagura M., Sasaki Y. Pharmacokinetic study of low- versus high-dose medroxyprogesterone acetate (MPA) in women. Cancer Chemotherapy Pharmacology. 42(1):1998;1-8.
10. Pampori N.A., Shapiro B.H. Gender differences in the responsiveness of the sex-dependent isoforms of hepatic P450 to the feminine plasma growth hormone profile. Endocrinology. 140(3):1999;1245-1254.
11. Pichard L., Fabre I., Fabre G., Domergue J., Saint Aubert B., Mourad G., Maurel P. Cyclosporin A drug interactions. Screening for inducers and inhibitors of cytochrome P-450 (cyclosporin A oxidase) in primary cultures of human hepatocytes and in liver microsomes. Drug Metabolism and Disposition. 18(5):1990;595-606.
12. Rautio A., Saarni H.U., Arranto A.J., Stengard J.H., Karki N.T., Sotaniemi E.A. Metabolism of medroxyprogesterone acetate and hepatic drug metabolism activity. Research Communications in Chemical Pathology and Pharmacology. 47(2):1985;305-308.
13. Rosendaal F.R. Venous thrombosis: a multicausal disease. Lancet. 353(9159):1999;1167-1173.
14. Saarni H.U., Rautio A., Karki N.T., Sotaniemi E.A. Disposition of medroxyprogesterone acetate and drug metabolism. Research Communications in Chemical Pathology and Pharmacology. 39(2):1983;251-260.
15. Stockdale A.D., Rostom A.Y. Clinical significance of differences in bioavailability of medroxyprogesterone acetate preparations. Clinical Pharmacokinetics. 16(3):1989;129-133.
16. Waxman D.J., Azaroff L. Phenobarbital induction of cytochrome P-450 gene expression. Biochemical Journal. 281(3):1992;577-592.
17. Yoshinari K., Sueyoshi T., Moore R., Negishi M. Nuclear receptor CAR as a regulatory factor for the sexually dimorphic induction of CYP2B1 gene by phenobarbital in rat livers. Molecular Pharmacology. 59(2):2001;278-284.