Metabolism and elimination of quinine in healthy volunteers

European Journal of Clinical Pharmacology

Volumn 59, Issue 5-6, 2003, Pages 423-427

  Mirghani, Rajaa A ^a   Hellgren, Urban ^a   Bertilsson, Leif ^a   Gustafsson, Lars L ^a   Ericsson, Örjan ^b  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

^b NATIONAL BOARD OF HEALTH AND WELFARE   (Sweden)

Author keywords

CYP3A4; Metabolism; Quinine

Indexed keywords

11 DIHYDROXYDIHYDROQUININE; 2' QUININONE; 3 HYDROXYQUININE; BETA GLUCURONIDASE; CYTOCHROME P450 1A2; CYTOCHROME P450 2C19; CYTOCHROME P450 3A4; DRUG METABOLITE; FLUVOXAMINE; KETOCONAZOLE; QUININE; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CLINICAL TRIAL; CONFIDENCE INTERVAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG METABOLISM; DRUG STRUCTURE; DRUG URINE LEVEL; GEOMETRY; HEALTH STATUS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; HYDROLYSIS; IN VIVO STUDY; KIDNEY CLEARANCE; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; STATISTICAL SIGNIFICANCE; SWEDEN; URINALYSIS; VOLUNTEER;

ANTIMALARIALS; AREA UNDER CURVE; ARYL HYDROCARBON HYDROXYLASES; BENZOQUINONES; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CROSS-OVER STUDIES; CYTOCHROME P-450 CYP1A2; CYTOCHROME P-450 ENZYME SYSTEM; DRUG INTERACTIONS; FLUVOXAMINE; HUMANS; KETOCONAZOLE; MIXED FUNCTION OXYGENASES; QUINIDINE; QUININE; QUINONES; TIME FACTORS;

EID: 0141706460     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00228-003-0637-8     Document Type: Article

References (20)

1. World Health Organization (2000) Management of severe malaria: a practical handbook. WHO, Geneva
2. Liddle C, Graham GG, Christopher RK, Bhuwapathanapun S, Duffield AM (1981) Identification of new urinary metabolites in man of quinine using methane chemical ionization gas chromatography-mass spectrometry. Xenobiotica 11:81-87
3. Zhao XJ, Yokoyama H, Chiba K, Wanwimolruk S, Ishizaki T (1996) Identification of human cytochrome P450 isoforms involved in the 3-hydroxylation of quinine by human liver microsomes and nine recombinant human cytochromes P450. J Pharmacol Exp Ther 279:1327-1334
4. Zhang H, Coville PF, Walker RJ, Miners JO, Birkett DJ, Wanwimolruk S (1997) Evidence for involvement of human CYP3A in the 3-hydroxylation of quinine. Br J Clin Pharmacol 43:245-252
5. Zhao XJ, Ishizaki T (1997) The in vitro hepatic metabolism of quinine in mice, rats and dogs: comparison with human liver microsomes. J Pharmacol Exp Ther 283:1168-1176
6. Mirghani RA, Yasar U, Zheng T, Cook JM, Gustafsson LL, Tybring G, Ericsson O (2002) Enzyme kinetics for the formation of 3-hydroxyquinine and three new metabolites of quinine in vitro; 3-hydroxylation by CYP3A4 is indeed the major metabolic pathway. Drug Metab Dispos 30:1368-1371
7. Morel F, Beaune PH, Ratanasavanh D, Flinois JP, Yang CS, Guengerich FP, Guillouzo A (1990) Expression of cytochrome P-450 enzymes in cultured human hepatocytes. Eur J Biochem 191:437-444
8. Oesch F, Arand M, Benedetti MS, Castelli MG, Dostert P (1996) Inducing properties of rifampicin and rifabutin for selected enzyme activities of the cytochrome P-450 and UDP-glucuronosyltransferase superfamilies in female rat liver. J Antimicrob Chemother 37:1111-1119
9. Wanwimolruk S, Kang W, Coville PF, Viriyayudhakorn S, Thitiarchakul S (1995) Marked enhancement by rifampicin and lack of effect of isoniazid on the elimination of quinine in man. Br J Clin Pharmacol 40:87-91
10. Sai Y, Dai R, Yang TJ, Krausz KW, Gonzalez FJ, Gelboin HV, Shou M (2000) Assessment of specificity of eight chemical inhibitors using cDNA-expressed cytochromes P450. Xenobiotica 30:327-343
11. Mirghani RA, Hellgren U, Westerberg PA, Ericsson O, Bertilsson L, Gustafsson LL (1999) The roles of cytochrome P450 3A4 and 1A2 in the 3-hydroxylation of quinine in vivo. Clin Pharmacol Ther 66:45-460
12. Brosen K, Skjelbo E, Rasmussen BB, Poulsen HE, Loft S (1993) Fluvoxamine is a potent inhibitor of cytochrome P4501A2. Biochem Pharmacol 45:1211-1214
13. Jeppesen U, Rasmussen BB, Brosen K (1997) Fluvoxamine inhibits the CYP2C19-catalyzed bioactivation of chloroguanide. Clin Pharmacol Ther 62:279-286
14. Christensen M, Tybring G, Mihara K, Yasui-Furokori N, Carrillo JA, Ramos SI, Andersson K, Dahl ML, Bertilsson L (2002) Low daily 10-mg and 20-mg doses of fluvoxamine inhibit the metabolism of both caffeine (cytochrome P4501A2) and omeprazole (cytochrome P4502C19). Clin Pharmacol Ther 71:141-152
15. Paintaud G, Alvan G, Ericsson O (1993) The reproducibility of quinine bioavailability. Br J Clin Pharmacol 35:305-307
16. Mirghani RA, Ericsson O, Cook J, Yu P, Gustafsson LL (2001) Simultaneous determination of quinine and four metabolites in plasma and urine by high-performance liquid chromatography. J Chromatogr B Biomed Sci Appl 754:57-64
17. Ono S, Hatanaka T, Hotta H, Satoh T, Gonzalez FJ, Tsutsui M (1996) Specificity of substrate and inhibitor probes for cytochrome P450s: evaluation of in vitro metabolism using cDNA-expressed human P450s and human liver microsomes. Xenobiotica 26:681-693
18. Newton DJ, Wang RW, Lu AY (1995) Cytochrome P450 inhibitors. Evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metab Dispos 23:154-158
19. Gibbs MA, Thummel KE, Shen DD, Kunze KL (1999) Inhibition of cytochrome P-450 3A (CYP3A) in human intestinal and liver microsomes: comparison of Ki values and impact of CYP3A5 expression. Drug Metab Dispos 27:180-187
20. Jeppesen U, Gram LF, Vistisen K, Loft S, Poulsen HE, Brosen K (1996) Dose-dependent inhibition of CYP1A2, CYP2C19 and CYP2D6 by citalopram, fluoxetine, fluvoxamine and paroxetine. Eur J Clin Pharmacol 51:73-78