A semiphysiological pharmacokinetic model for artemisinin in healthy subjects incorporating autoinduction of metabolism and saturable first-pass hepatic extraction

British Journal of Clinical Pharmacology

Volumn 59, Issue 2, 2005, Pages 189-198

  Gordi, Toufigh ^b,c   Xie, Rujia ^a   Huong, Nguyen V ^a   Huong, Dinh X ^a   Karlsson, Mats O ^a   Ashton, Michael ^a  

^a UPPSALA UNIVERSITY   (Sweden)

^b CV THERAPEUTICS INC   (United States)

^c UNIVERSITY AT BUFFALO   (United States)

Author keywords

Antoinduction; Artemisinin; Pharmacokinetic model

Indexed keywords

ANTIMALARIAL AGENT; ARTEMISININ;

ADULT; AREA UNDER THE CURVE; ARTICLE; BIOAVAILABILITY; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DATA ANALYSIS; DRUG CLEARANCE; DRUG DOSE REGIMEN; ENZYME INDUCTION; ENZYME METABOLISM; FIRST PASS EFFECT; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; MALARIA; MALE; METABOLISM; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SALIVA; TIMED DRUG RELEASE;

ADMINISTRATION, ORAL; ADOLESCENT; ADULT; ANTIMALARIALS; ARTEMISININS; BIOLOGICAL AVAILABILITY; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; LIVER; MALE; MIDDLE AGED; SALIVA; SENSITIVITY AND SPECIFICITY; SESQUITERPENES;

EID: 13444304087     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2004.02321.x     Document Type: Article

References (28)

1. van Agtmael MA, Eggelte TA, van Boxtel O. Artemisinin drugs in the treatment of malaria: from medicinal herb to registered medication. Trends Pharmacol Sci 1999; 20: 199-205.
2. Alin MH, Ashton M, Kihamia CM, Mtey GJ, Björkman A. Clinical efficacy and pharmacokinetics of artemisinin monotherapy and in combination with mefloquine in patients with falciparum malaria. Br J Clin Pharmacol 1996; 41: 587-92.
3. Augustijns P, D'Hulst A, Van Daele J, Kinget R. Transport of artemisinin and sodium artesunate in Caco-2 intestinal epithelial cells. J Pharm Sci 1996; 85: 577-9.
4. Svensson USH, Sandstrom R, Carlborg O, Lennernas H, Ashton M. High in situ rat intestinal permeability of artemisinin unaffected by multiple dosing and with no evidence of P-glycoprotein involvement. Drug Metab Dispos 1999; 27: 227-32.
5. Ashton M, Sy ND, Gordi T, Hai TN, Thach DC, Farah MH, et al. Evidence for time-dependent artemisinin kinetics in adults with uncomplicated malaria. Pharm Pharmacol Lett 1996; 6: 127-30.
6. Ashton M, Hai TN, Sy ND, Huong DX, Huong NV, Nieu NT, et al. Artemisinin pharmacokinetics is time-dependent during repeated oral administration in healthy male adults. Drug Metab Dispos 1998; 26: 25-7.
7. Svensson US, Ashton M, Hai TN, Bertilsson L, Huong DX, Huong NV, et al. Artemisinin induces omeprazole metabolism in human beings. Clin Pharmacol Ther 1998; 64: 160-7.
8. Alin MH, Ashton M, Kihamia CM, Mtey GJ, Björkman A. Multiple dose pharmacokinetics of oral artemisinin and comparison of its efficacy with that of oral artesunate in falciparum malaria patients. Trans R Soc Trop Med Hyg 1996; 90: 61-5.
9. Ashton M, Sy ND, Huong NV, Gordi T, Hai TN, Huong DX, et al. Artemisinin kinetics and dynamics during oral and rectal treatment of uncomplicated malaria. Clin Pharmacol Ther 1998; 63: 482-93.
10. Gordi T, Huong DX, Hai TN, Nieu NT, Ashton M. Artemisinin pharmacokinetics and efficacy in uncomplicated-malaria patients treated with two different dosage regimens. Antimicrob Agent Chemother 2002; 46: 1026-31.
11. Ashton M, Gordi T, Hai TN, Huong NV, Sy ND, Nieu NT, et al. Artemisinin pharmacokinetics in healthy adults after 250, 500 and 1000 mg single oral doses. Biopharm Drug Dispos 1998; 19: 245-50.
12. Zhang SQ, Hai TN, Ilett KF, Huong DX, Davis TM, Ashton M. Multiple dose study of interactions between artesunate and artemisinin in healthy volunteers. Br J Clin Pharmacol 2001; 52: 377-85.
13. van Agtmael MA, Cheng-Qi S, Qing JX, Mull R, van Boxtel JC. Multiple dose pharmacokinetics of artemether in Chinese patients with uncomplicated falciparum malaria. Int J Antimicrob Agents 1999; 12: 151-8.
14. Ezzet F, Mull R, Karbwang J. Population pharmacokinetics and therapeutic response of CGP 56697 (artemether + benflumetol) in malaria patients. Br J Clin Pharmacol 1998; 46: 553-61.
15. Khanh NX, de Vries PJ, Ha LD, van Boxtel CJ, Koopmans R, Kager PA. Declining concentrations of dihydroartemisinin in plasma during 5-day oral treatment with artesunate for falciparum malaria. Antimicrob Agents Chemother 1999; 43: 690-2.
16. Svensson US, Ashton M. Identification of the human cytochrome P450 enzymes involved in the in vitro metabolism of artemisinin. Br J Clin Pharmacol 1999; 48: 528-35.
17. Sidhu JS, Ashton M. Single-dose, comparative study of venous, capillary and salivary artemisinin concentrations in healthy, male adults. Am J Trop Med Hyg 1997; 56: 13-6.
18. Gordi T, Hai TN, Hoai NM, Thyberg M, Ashton M. Use of saliva and capillary blood samples as substitutes for venous blood sampling in pharmacokinetic investigations of artemisinin. Eur J Clin Pharmacol 2000; 56: 561-6.
19. Gordi T, Nielsen EYuZ, Westerlund D, Ashton M. Direct analysis of artemisinin in plasma and saliva using coupled- column high-performance liquid chromatography with a restricted-access material pre-column. J Chromatogr B Biomed Sci Appl 2000; 742: 155-62.
20. Beal SL, Sheiner LB. NONMEM users guide. Introductory guide. San Francisco: NONMEM Project Group, 1998.
21. Jonsson EN, Karlsson MO. Xpose- an S-PLUS based population pharmacokinetic/pharmacodynamic model building aid for NONMEM. Comp Meth Prog Biomed 1999; 58: 51-64.
22. Mandema JW, Verotta D, Sheiner LB. Building population pharmacokinetic/pharmacodynamic models. I. Models for covariate effects. J Pharmacokinet Biopharm 1992; 20: 511-28.
23. Bock KW, Lipp HP, Bock-Hennig BS. Induction of drug-metabolizing enzymes by xenobiotics. Xenobiotica 1990; 20: 1101-11.
24. Whitlock JP. The regulation of cytochrome P-450 gene expression. Ann Rev Pharmacol Toxicol 1986; 26: 333-69.
25. Levy RH, Dumain MS, Cook JL. Time-dependent kinetics. V. Time course of drug levels during enzyme induction (one-compartment model). J Pharmacokinet Biopharm 1979; 7: 557-78.
26. Hassan M, Svensson US, Ljungman P, Bjorkstrand B, Olsson H, Bielenstein M, et al. A mechanism-based pharmacokinetic-enzyme model for cyclophosphamide autoinduction in breast cancer patients. Br J Clin Pharmacol 1999; 48: 669-77.
27. Rostami-Hodjegan A, Wolff K, Hay AW, Raistrick D, Calvert RR, Tucker GT. Population pharmacokinetics of methadone in opiate users: characterization of time-dependent changes. Br J Clin Pharmacol 1999; 48: 43-52.
28. Body AV, Cole M, Pearson AD, Idle JR. The kinetics of the autoinduction of ifosfamide metabolism during continuous infusion. Cancer Chemother Pharmacol 1995; 36: 53-60.