Semi-mechanistic pharmacokinetic/pharmacodynamic modelling of the antimalarial effect of artemisinin

British Journal of Clinical Pharmacology

Volumn 60, Issue 6, 2005, Pages 594-604

  Gordi, Toufigh ^a,c   Xie, Rujia ^b   Jusko, William J ^a  

^a UNIVERSITY AT BUFFALO   (United States)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^c CV THERAPEUTICS INC   (United States)

Author keywords

Artemisinin; Mechanism based model; Pharmacodynamics; Pharmacokinetics

Indexed keywords

ARTEMISININ;

ANTIMALARIAL ACTIVITY; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG CLEARANCE; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG SALIVA LEVEL; ENZYME INDUCTION; FEMALE; HALF LIFE TIME; HUMAN; IN VIVO STUDY; LIFE CYCLE; MAJOR CLINICAL STUDY; MALARIA; MALE; PARASITE DEVELOPMENT; PARASITE IDENTIFICATION; PHYSICAL MODEL; PRIORITY JOURNAL; PROCESS MODEL; RANDOMIZED CONTROLLED TRIAL; VIET NAM;

ANTIMALARIALS; ARTEMISININS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; DRUG ADMINISTRATION SCHEDULE; FEMALE; HALF-LIFE; HUMANS; MALARIA, FALCIPARUM; MALE; MODELS, BIOLOGICAL; PARASITEMIA; SALIVA; SESQUITERPENES;

EID: 28244491463     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2005.02508.x     Document Type: Article

References (32)

1. Price RN. Artemisinin drugs: novel antimalarial agents. Expert Opin Invest Drugs 2000; 9: 1815-27.
2. Ashton M, Hai TN, Sy ND, Huong DX, Huong NV, Nieu Nt Cong LD. Artemisinin pharmacokinetics is time-dependent during repeated oral administration in healthy male adults. Drug Metab Dispos 1998; 26: 25-7.
3. 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.
4. Ashton M, Sy ND, Huong NV, Gordi T, Hai TN, Huong DX, Niêu NT, Công LD. Artemisinin kinetics and dynamics during oral and rectal treatment of uncomplicated malaria. Clin Pharmacol Ther 1998; 63: 482-93.
5. Gordi T, Xie R, Huong NV, Huong DX, Karlsson M, Ashton M. A semi-physiological pharmacokinetic model for artemisinin in healthy subjects incorporating autoinduction of metabolism and saturable first-pass hepatic extraction. Br J Clin Pharmacol 2005; 59: 189-98.
6. 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.
7. van Agtmael MA, Eggelte TA, van Boxtel CJ. Artemisinin drugs in the treatment of malaria: from medicinal herb to registered medication. Trends Pharmacol Sci 1999; 20: 199-205.
8. Dhingra V, Vishweshwar RK, Lakshmi NM. Current status of artemisinin and its derivatives as antimalarial drugs. Life Sci 2000; 66: 279-300.
9. Hoshen MB, Na-Bangchang K, Stein WD, Ginsburg H. Mathematical modelling of the chemotherapy of Plasmodium falciparum malaria with artesunate: postulation of 'dormancy', a partial cytostatic effect of the drug, and its implication for treatment regimens. Parasitol 2000; 12: 237-46.
10. Svensson US, Alin H, Karlsson MO, Bergqvist Y, Ashton M. Population pharmacokinetic and pharmacodynamic modelling of artemisinin and mefloquine enantiomers in patients with falciparum malaria. Eur J Clin Pharmacol 2002; 58: 339-51.
11. Gordi T, Nielsen E, Yu Z, 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.
12. Beal SL, Sheiner LB. NONMEM Users Guide. Introductory Guide. San Francisco: NONMEM Project Group, 1998.
13. 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.
14. 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.
15. Dayneka NL, Garg V, Jusko WJ. Comparison of four basic models of indirect pharmacodynamic responses. J Pharmacokinet Biopharm 1993; 21: 457-78.
16. White NJ. Clinical pharmacokinetics and pharmacodynamics of artemisinin and derivatives. Trans R Soc Trop Med Hyg 1994; 88(Suppl 1): S41-3.
17. Gordi T, Lepist EI. Artemisinin derivatives: toxic for laboratory animals, safe for humans? Toxicol Lett 2004; 147: 99-107.
18. Ashton M, Gordi T, Trinh NH, Nguyen VH, Nguyen DS, Nguyen TN, Dinh XH, Johansson M, Le DC. Artemisinin pharmacokinetics in healthy adults after 250, 500 and 1000 mg single oral doses. Biopharm Drug Disp 1998; 19: 245-250.
19. Svensson US, Ashton M, Trinh NH, Bertilsson L, Dinh XH, Nguyen VH, Nguyen TN, Nguyen DS, Lykkesfeldt J, Le DC. Artemisinin induces omeprazole metabolism in human beings. Clin Pharmacol Ther 1998; 64: 160-7.
20. Hassan Alin M, Ashton M, Kihamia CM, Mtey GJ, Bjorkman 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.
21. Angus BJ, Thaiaporn I, Chanthapadith K, Suputtamongkol Y, White NJ. Oral artesunate dose-response relationship in acute falciparum malaria. Antimicrob Agents Chemother 2002; 46: 778-82.
22. Hoshen MB, Heinrich R, Stein WD, Ginsburg H. Mathematical modelling of the within-host dynamics of Plasmodium falciparum. Parasitology 2000; 121: 227-35.
23. Hoshen MB, Stein WD, Ginsburg H. Modelling the chloroquine chemotherapy of falciparum malaria: the value of spacing a split dose. Parasitology 1998; 116: 407-16.
24. Hoshen MB, Stein WD, Ginsburg HD. Pharmacokinetic-pharmacodynamic modelling of the antimalarial activity of mefloquine. Parasitology 2001; 123: 337-46.
25. Hoshen MB, Stein WD, Ginsburg H. Mathematical modelling of malaria chemotherapy: combining artesunate and mefloquine. Parasitology 2002; 124: 9-15.
26. Gravenor MB, van Hensbroek MB, Kwiatkowski D. Estimating sequestered parasite population dynamics in cerebral malaria. Proc Natl Acad Sci USA 1998; 95: 7620-4.
27. de Vries PJ, Bich NN, Van Thien H, Hung LN, Anh TK, Kager PA, Heisterkamp SH. Combinations of artemisinin and quinine for uncomplicated falciparum malaria: efficacy and pharmacodynamics. Antimicrob Agents Chemother 2000; 44: 1302-8.
28. White NJ. Assessment of the pharmacodynamic properties of antimalarial drugs in vivo. Antimicrob Agents Chemother 1997; 41: 1413-22.
29. Silachamroon U, Phumratanaprapin W, Krudsood S, Treeprasertsuk S, Budsaratid V, Pornpininworakij K, Wilairatan P, Looareesuwan S. Frequency of early rising parasitemia in falciparum malaria treated with artemisinin derivatives. Southeast Asian J Trop Med Public Health 2001; 32: 50-6.
30. Bakhshi HB, Gordi T, Ashton M. In vitro interaction of artemisinin with intact human erythrocytes, erythrocyte ghosts, haemoglobin and carbonic anhydrase. J Pharm Pharmacol 1997; 49: 223-6.
31. Meshnick SR. Artemisinin mechanisms of action, resistance and toxicity. Int J Parasitol 2002; 32: 1655-60.
32. Parapini S, Basilico N, Mondani M, Olliaro P, Taramelli D, Monti D. Evidence that haem iron in the malaria parasite is not needed for the antimalarial effects of artemisinin. FEBS Lett 2004; 575: 91-4.