Population pharmacokinetics of artesunate and dihydroartemisinin following single-and multiple-dosing of oral artesunate in healthy subjects

Malaria Journal

Volumn 8, Issue 1, 2009, Pages

  Tan, Beesan ^a   Naik, Himanshu ^a   Jang, In Jin ^b   Yu, Kyung Sang ^b   Kirsch, Lee E ^a   Shin, Chang Sik ^c   Craft, J Carl ^d   Fleckenstein, Lawrence ^a  

^a UNIVERSITY OF IOWA   (United States)

^b Seoul National University   (South Korea)

^c Shin Poong Pharmaceutical Company   (South Korea)

^d Medicines for Malaria Venture   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMALARIAL AGENT; ARTESUNATE; ARTESUNATE PLUS PYRONARIDINE PHOSPHATE; DIHYDROARTEMISININ; PLACEBO; PYRONARIDINE; UNCLASSIFIED DRUG; ARTEMISININ DERIVATIVE; DIHYDROQUINGHAOSU; NAPHTHYRIDINE DERIVATIVE;

ADULT; ARTICLE; CALORIC INTAKE; CLINICAL TRIAL; COMPARTMENT MODEL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DISTRIBUTION VOLUME; DOUBLE BLIND PROCEDURE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE INCREASE; FEMALE; HUMAN; HUMAN EXPERIMENT; KOREA; LIPID DIET; MALE; MONOTHERAPY; NONLINEAR SYSTEM; NORMAL HUMAN; PHASE 1 CLINICAL TRIAL; RANDOMIZED CONTROLLED TRIAL; STOICHIOMETRY; WEIGHT CHANGE; CHEMISTRY; EATING; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; METHODOLOGY; ORAL DRUG ADMINISTRATION; PLASMA; SOUTH KOREA; STATISTICAL MODEL;

ADMINISTRATION, ORAL; ADULT; ANTIMALARIALS; ARTEMISININS; CHROMATOGRAPHY, LIQUID; EATING; FEMALE; HUMANS; MALE; MASS SPECTROMETRY; MODELS, STATISTICAL; NAPHTHYRIDINES; PLASMA; REPUBLIC OF KOREA; YOUNG ADULT;

EID: 74849104255     PISSN: None     EISSN: 14752875     Source Type: Journal    
DOI: 10.1186/1475-2875-8-304     Document Type: Article

References (42)

1. World Health Organization, World Malaria Report 2008 World Health Organization, Geneva, Switzerland 2008
2. Pharmacokinetic determinants of the window of selection for antimalarial drug resistance. K Stepniewska NJ White, Antimicrob Agents Chemother 2008 52 1589 1596 10.1128/AAC.00903-07 18299409
3. Artesunate combinations for treatment of malaria: meta-analysis. International Artemisinin Study Group, Lancet 2004 363 9 17 10.1016/S0140- 6736(03)15162-8 14723987
4. Reduction of transmission from malaria patients by artemisinin combination therapies: a pooled analysis of six randomized trials. LC Okell CJ Drakeley AC Ghani T Bousema CJ Sutherland, Malar J 2008 7 125 10.1186/1475-2875-7-125 18613962
5. Effects of artemisinin derivatives on malaria transmissibility. RN Price F Nosten C Luxemburger FO ter Kuile L Paiphun T Chongsuphajaisiddhi NJ White, Lancet 1996 347 1654 1658 10.1016/S0140-6736(96)91488-9 8642959
6. Artemisinin-based combination therapies for uncomplicated malaria. TM Davis HA Karunajeewa KF Ilett, Med J Aust 2005 182 181 185 15720175
7. Artesunate and dihydroartemisinin (DHA): unusual decomposition products formed under mild conditions and comments on the fitness of DHA as an antimalarial drug. RK Haynes HW Chan CM Lung NC Ng HN Wong LY Shek ID Williams A Cartwright MF Gomes, ChemMedChem 2007 2 1448 1463 10.1002/cmdc.200700064 17694524
8. In vitro activity of artemisinin, its derivatives, and pyronaridine against different strains of Plasmodium falciparum. MH Alin A Bjorkman M Ashton, Trans R Soc Trop Med Hyg 1990 84 635 637 10.1016/0035-9203(90)90129-3 2278058
9. In vitro activities of pyronaridine, alone and in combination with other antimalarial drugs, against Plasmodium falciparum. P Ringwald EC Eboumbou J Bickii LK Basco, Antimicrob Agents Chemother 1999 43 1525 1527 10348789
10. In vitro activity of pyronaridine against Plasmodium falciparum and comparative evaluation of anti-malarial drug susceptibility assays. F Kurth P Pongratz S Belard B Mordmuller PG Kremsner M Ramharter, Malar J 2009 8 79 10.1186/1475-2875-8-79 19389221
11. Randomised trial of pyronaridine versus chloroquine for acute uncomplicated falciparum malaria in Africa. P Ringwald J Bickii L Basco, Lancet 1996 347 24 28 10.1016/S0140-6736(96)91558-5 8531545
12. Clinical study of pyronaridine for the treatment of acute uncomplicated falciparum malaria in Thailand. S Looareesuwan DE Kyle C Viravan S Vanijanonta P Wilairatana WH Wernsdorfer, Am J Trop Med Hyg 1996 54 205 209 8619449 (Pubitemid 26084442)
13. Efficacy of oral pyronaridine for the treatment of acute uncomplicated falciparum malaria in African children. P Ringwald J Bickii LK Basco, Clin Infect Dis 1998 26 946 953 10.1086/513942 9564481
14. Disposition of artesunate and dihydroartemisinin after administration of artesunate suppositories in children from Papua New Guinea with uncomplicated malaria. HA Karunajeewa KF Ilett K Dufall A Kemiki M Bockarie MP Alpers PH Barrett P Vicini TM Davis, Antimicrob Agents Chemother 2004 48 2966 2972 10.1128/AAC.48.8.2966-2972.2004 15273107
15. Pharmacokinetics of dihydroartemisinin following oral artesunate treatment of pregnant women with acute uncomplicated falciparum malaria. R McGready K Stepniewska SA Ward T Cho G Gilveray S Looareesuwan NJ White F Nosten, Eur J Clinical Pharmacol 2006 62 367 371 10.1007/s00228-006-0118-y
16. Population pharmacokinetics of artesunate and dihydroartemisinin following intra-rectal dosing of artesunate in malaria patients. JA Simpson T Agbenyega KI Barnes G Di Perri P Folb M Gomes S Krishna S Krudsood S Looareesuwan S Mansor H McIlleron R Miller M Molyneux J Mwenechanya V Navaratnam F Nosten P Olliaro L Pang I Ribeiro M Tembo M van Vugt S Ward K Weerasuriya K Win NJ White, PLoS Medicine 2006 3 444 10.1371/journal.pmed.0030444 17132053
17. Population pharmacokinetics of artesunate and amodiaquine in African children. K Stepniewska W Taylor SB Sirima EB Ouedraogo A Ouedraogo A Gansane JA Simpson CC Morgan NJ White JR Kiechel, Malar J 2009 8 200 10.1186/1475-2875-8- 200 19691851
18. Development and validation of a high-performance liquid chromatography-mass spectroscopy assay for determination of artesunate and dihydroartemisinin in human plasma. H Naik DJ Murry LE Kirsch L Fleckenstein, J Chromatogr B Analyt Technol Biomed Life Sci 2005 816 233 242 10.1016/j.jchromb.2004.11.042 15664355
19. SL Beal LB Sheiner, NONMEM users' guides NONMEM Project Group, University of San Francisco, CA 1998
20. Xpose-an S-PLUS based population pharmacokinetic/pharmacodynamic model building aid for NONMEM. EN Jonsson MO Karlsson, Comput Methods Programs Biomed 1999 58 51 64 10.1016/S0169-2607(98)00067-4 10195646
21. Glucuronidation of dihydroartemisinin in vivo and by human liver microsomes and expressed UDP-glucuronosyltransferases. KF Ilett BT Ethell JL Maggs TM Davis KT Batty B Burchell TQ Binh TA Thu le NC Hung M Pirmohamed BK Park G Edwards, Drug Metab Dispos 2002 30 1005 1012 10.1124/dmd.30.9.1005 12167566
22. Building population pharmacokinetic-pharmacodynamic models. I. Models for covariate effects. JW Mandema D Verotta LB Sheiner, J Pharmacokinet Biopharm 1992 20 511 528 10.1007/BF01061469 1287200
23. Pharmacokinetics of artemisinin and artesunate after oral administration in healthy volunteers. A Benakis M Paris L Loutan CT Plessas ST Plessas, Am J Trop Med Hyg 1997 56 17 23 9063354
24. Comparative pharmacokinetic study of oral and rectal formulations of artesunic acid in healthy volunteers. V Navaratnam SM Mansor MN Mordi A Akbar MN Abdullah, Eur J Clin Pharmacol 1998 54 411 414 10.1007/s002280050484 9754985
25. Comparative pharmacokinetics and effect kinetics of orally administered artesunate in healthy volunteers and patients with uncomplicated falciparum malaria. P Teja-Isavadharm G Watt C Eamsila K Jongsakul Q Li G Keeratithakul N Sirisopana L Luesutthiviboon TG Brewer DE Kyle, Am J Trop Med Hyg 2001 65 717 721 11791963
26. The pharmacokinetics of oral dihydroartemisinin and artesunate in healthy Thai volunteers. K Na-Bangchang S Krudsood U Silachamroon P Molunto O Tasanor K Chalermrut N Tangpukdee O Matangkasombut S Kano S Looareesuwan, Southeast Asian J Trop Med Public Health 2004 35 575 582 15689069
27. Pharmacokinetics of oral artesunate in children with moderately severe Plasmodium falciparum malaria. DB Bethell P Teja-Isavadharm XT Cao TT Pham TT Ta TN Tran TT Nguyen TP Pham D Kyle NP Day NJ White, Trans R Soc Trop Med Hyg 1997 91 195 198 10.1016/S0035-9203(97)90222-4 9196768
28. A pharmacokinetic and pharmacodynamic study of intravenous vs oral artesunate in uncomplicated falciparum malaria. KT Batty LT Thu TM Davis KF Ilett TX Mai NC Hung NP Tien SM Powell HV Thien TQ Binh NV Kim, Br J Clin Pharmacol 1998 45 123 129 10.1046/j.1365-2125.1998.00655.x 9491824
29. Antimalarial bioavailability and disposition of artesunate in acute falciparum malaria. P Newton Y Suputtamongkol P Teja-Isavadharm S Pukrittayakamee V Navaratnam I Bates N White, Antimicrob Agents Chemother 2000 44 972 977 10.1128/AAC.44.4.972-977.2000 10722499
30. Pharmacokinetics of artesunate following oral and rectal administration in healthy Sudanese volunteers. MI Awad IB Eltayeb OZ Baraka RH Behrens AM Alkadru, Trop Doct 2004 34 132 135 15267037
31. Glucuronidation in humans. Pharmacogenetic and developmental aspects. SN de Wildt GL Kearns JS Leeder JN van den Anker, Clin Pharmacokinet 1999 36 439 452 10.2165/00003088-199936060-00005 10427468
32. Clinical efficacy and pharmacokinetics of artemisinin monotherapy and in combination with mefloquine in patients with falciparum malaria. MH Alin M Ashton CM Kihamia GJ Mtey A Bjorkman, Br J Clin Pharmacol 1996 41 587 592 10.1046/j.1365-2125.1996.35116.x 8799526 (Pubitemid 26184681)
33. Artemisinin pharmacokinetics in healthy adults after 250, 500 and 1000 mg single oral doses. M Ashton T Gordi NH Trinh VH Nguyen DS Nguyen TN Nguyen XH Dinh M Johansson DC Le, Biopharm Drug Dispos 1998 19 245 250 10.1002/(SICI)1099-081X(199805)19:4<245:AID-BDD99>3.0.CO;2-Z 9604124
34. Artemisinin pharmacokinetics is time-dependent during repeated oral administration in healthy male adults. M Ashton TN Hai ND Sy DX Huong N Van Huong NT Nieu LD Cong, Drug Metab Dispos 1998 26 25 27 9443848 (Pubitemid 28071320)
35. Artemisinin kinetics and dynamics during oral and rectal treatment of uncomplicated malaria. M Ashton DS Nguyen VH Nguyen T Gordi NH Trinh XH Dinh TN Nguyen DC Le, Clin Pharmacol Ther 1998 63 482 493 10.1016/S0009-9236(98)90044-3 9585803
36. Artemisinin autoinduction is caused by involvement of cytochrome P450 2B6 but not 2C9. US Simonsson B Jansson TN Hai DX Huong G Tybring M Ashton, Clin Pharmacol Ther 2003 74 32 43 10.1016/S0009-9236(03)00092-4 12844133
37. Artemisinin antimalarials moderately affect cytochrome P450 enzyme activity in healthy subjects. S Asimus D Elsherbiny TN Hai B Jansson NV Huong MG Petzold US Simonsson M Ashton, Fundam Clin Pharmacol 2007 21 307 316 10.1111/j.1472-8206.2007.00471.x 17521300
38. A model based assessment of the CYP2B6 and CYP2C19 inductive properties by artemisinin antimalarials: implications for combination regimens. DA Elsherbiny SA Asimus MO Karlsson M Ashton USH Simonsson, J Pharmacokinet Pharmacodyn 2008 35 203 217 10.1007/s10928-008-9084-6 18350255
39. A semiphysiological pharmacokinetic model for artemisinin in healthy subjects incorporating autoinduction of metabolism and saturable first-pass hepatic extraction. T Gordi R Xie NV Huong DX Huong MO Karlsson M Ashton, Br J Clin Pharmacol 2005 59 189 198 10.1111/j.1365-2125.2004.02321.x 15676041
40. Declining concentrations of dihydroartemisinin in plasma during 5-day oral treatment with artesunate for falciparum malaria. NX Khanh PJ de Vries LD Ha CJ van Boxtel R Koopmans PA Kager, Antimicrob Agents Chemother 1999 43 690 692 10049291
41. Multiple dose study of interactions between artesunate and artemisinin in healthy volunteers. SQ Zhang TN Hai KF Ilett DX Huong TM Davis M Ashton, Br J Clin Pharmacol 2001 52 377 385 10.1046/j.0306-5251.2001.01461.x 11678781
42. Absence of time-dependent artesunate pharmacokinetics in healthy subjects during 5-day oral administration. LT Diem Thuy L Ngoc Hung PT Danh K Na-Bangchang, Eur J Clin Pharmacol 2008 64 993 998 10.1007/s00228-008-0506-6 18600318