Rifampin induces the in vitro oxidative metabolism, but not the in vivo clearance of diclofenac in rhesus monkeys

Drug Metabolism and Disposition

Volumn 34, Issue 11, 2006, Pages 1806-1810

  Prueksaritanont, Thomayant ^a   Li, Chunze ^a   Tang, Cuyue ^a   Kuo, Yuhsin ^a   Strong Basalyga, Kristie ^a   Carr, Brian ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4' HYDROXYLASE; CYTOCHROME P450 2C9; DICLOFENAC; MIDAZOLAM; OXYGENASE; RIFAMPICIN; UNCLASSIFIED DRUG;

AEROBIC METABOLISM; ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG GLUCURONIDATION; DRUG HALF LIFE; DRUG INHIBITION; DRUG OXIDATION; ENZYME ACTIVITY; HYDROXYLATION; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; MALE; MAXIMUM ALLOWABLE CONCENTRATION; NONHUMAN; PRIORITY JOURNAL; RHESUS MONKEY;

ANIMALS; CYTOCHROME P-450 ENZYME SYSTEM; DICLOFENAC; ENZYME INDUCTION; HEPATOCYTES; HYDROLASES; MACACA MULATTA; MALE; METABOLIC CLEARANCE RATE; METABOLIC DETOXICATION, PHASE I; MICROSOMES, LIVER; RIFAMPIN; SUBSTRATE SPECIFICITY;

ANIMALIA; MACACA MULATTA;

EID: 33751093804     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.106.011643     Document Type: Article

References (20)

1. Bjornsson TD, Callaghan JT, Einolf HJ, Fisher V, Gan L, Grimm S, Kao J, King SP, Miwa G, Ni L, et al. (2003) The conduct of in vitro and in vivo drug-drug interaction studies: a PhRMA perspective. J Clin Pharmacol 43:443-469.
2. Kumar S, Samuel K, Subramanian R, Braun MP, Stearns RA, Chiu SL, Evans DC, and Baillie TA (2002) Extrapolation of diclofenac clearance from in vitro microsomal metabolism data: role of acyl glucuronidation and sequential oxidative metabolism of the acyl glucuronide. J Pharmacol Exp Ther 303:969-978.
3. LeCluyse EL (2001) Human hepatocyte culture systems for the in vitro evaluation of cytochrome P450 expression and regulation. Eur J Pharm Sci 13:343-368.
4. Leemann T, Transon C, and Dayer P (1993) Cytochrome P450TB (CYP2C): a major monooxygenase catalyzing diclofenac 4′-hydroxylation in human liver. Life Sci 52:29-34.
5. Moldeús P, Hogberg J, and Orrenius S (1978) The isolation and use of liver cells. Methods Enzymol 52:60-71.
6. Niemi M, Backman JT, Fromm MF, Neuvonen J, and Kivistö KT (2003) Pharmacokinetic interactions with rifampin: clinical relevance. Clin Pharmacokinet 42:819-850.
7. Parkinson A, Mudra DR, Johnson C, Dwyer A, and Carroll KM (2004) The effects of gender, age, ethnicity, and liver cirrhosis on cytochrome P450 enzyme activity in human liver microsomes and inducibility in cultured human hepatocytes. Toxicol Appl Pharmacol 199:193-209.
8. Prueksaritanont T, Kuo Y, Tang C, Li C, Qiu Y, Lu B, Strong-Basalyga K, Richards K, Carr B, and Lin JH (2006) In vitro and in vivo CYP3A64 induction and inhibition studies in rhesus monkeys: a preclinical approach for CYP3A-mediated drug interaction studies. Drug Metab Dispos 34:1546-1555.
9. Prueksaritanont T, Richards KM, Qiu Y, Strong-Basalyga K, Miller A, Li C, Eisenhandler R, and Carlini EJ (2005) Comparative effects of fibrates on drug metabolizing enzymes in human hepatocytes. Pharm Res (NY) 22:71-78.
10. Sanofi-Aventis (2003) Prescribing information on Rafadin (Rifampin). Physicians' Desk Reference, pp 759-762, Medical Economics Co., Montvale, NJ.
11. Shen S, Marchick MR, Davis MR, Doss GA, and Pohl LR (1999) Metabolic activation of diclofenac by human cytochrome P450 3A4: role of 5-hydroxydiclofenac. Chem Res Toxicol 12:214-222.
12. Stierlin H and Faigle JW (1979) Biotransformation of diclofenac sodium (Voltaren) in animals and man. II. Quantitative determination of the unchanged drug and principal phenolic metabolites, in urine and bile. Xenobiotica 9:611-621.
13. Stierlin H, Faigle JW, Sallman A, Küng W, Richter WJ, Kriemler H-P, Alt KO, and Winkler T (1979) Biotransformation of diclofenac sodium in animals and man. I. Isolation and identification of principal metabolites. Xenobiotica 9:601-610.
14. Tang C, Booth-Genthe C, Kuo Y, Fang Y, and Carr B (2005) Evaluation of diclofenac and tolbutamide as in vitro probe substrates for monkey CYP2C activities. Drug Metab Rev 37(Suppl 2):317.
15. Tang W, Stearns RA, Kwei GY, Iliff SA, Miller RR, Egan MA, Yu NX, Dean DC, Kumar S, Shou M, et al. (1999) Interaction of diclofenac and quinidine in monkeys: stimulation of diclofenac metabolism. J Pharmacol Exp Ther 291:1068-1074.
16. Thummel KE and Wilkinson GR (1998) In vitro and in vivo drug interactions involving human CYP3A. Annu Rev Pharmacol Toxicol 38:389-430.
17. Tucker GT, Houston JB, and Huang S-M (2001) Optimizing drug development: strategies to assess drug metabolism/transporter interaction potential - towards a consensus. Br J Clin Pharmacol 52:107-117.
18. Weaver RJ (2001) Assessment of drug-drug interactions: concepts and approaches. Xenobiotica 31:499-538.
19. Wilkinson GR (1987) Clearance approaches in pharmacology. Pharmacol Rev 39:1-47.
20. Worboys PD and Carlile DJ (2001) Implications and consequences of enzyme induction on preclinical and clinical drug development. Xenobiotica 31:539-556.