Pharmacodynamics of antimalarial chemotherapy

Expert Review of Clinical Pharmacology

Volumn 2, Issue 5, 2009, Pages 491-515

  Na Bangchang, Kesara ^a  

^a THAMMASAT UNIVERSITY   (Thailand)

Author keywords

Antimalarial drug; Chemoprophylaxis; Chemotherapy; Malaria drug resistance

Indexed keywords

AMODIAQUINE; AMODIAQUINE PLUS ARTESUNATE; ARTEMETHER; ARTEMETHER PLUS BENFLUMETOL; ARTEMISININ; ARTESUNATE; ATOVAQUONE; ATOVAQUONE PLUS PROGUANIL; AZITHROMYCIN; BENFLUMETOL; CHLOROQUINE; CHLOROQUINE PLUS PROGUANIL; CLINDAMYCIN; DIHYDROARTEMISININ; DIHYDROARTEMISININ PLUS PIPERAQUINE; DOXYCYCLINE; FANSIDAR; HALOFANTRINE; MACROLIDE; MEFLOQUINE; PRIMAQUINE; PYRIMETHAMINE; QUINIDINE; QUININE; QUININE SULFATE; QUINOLINE DERIVATIVE; SULFADOXINE; SULFADOXINE PLUS TRIMETHOPRIM; TETRACYCLINE; UNINDEXED DRUG;

ABDOMINAL PAIN; ABORTION; AGRANULOCYTOSIS; ANAPHYLAXIS; ANEMIA; ANTIMALARIAL DRUG RESISTANCE; BLOOD DISEASE; BLURRED VISION; CARDIOTOXICITY; CARDIOVASCULAR DISEASE; CHEMOPROPHYLAXIS; CLINICAL TRIAL; COMBINATION CHEMOTHERAPY; CONGENITAL DISORDER; CONVULSION; DISEASE TRANSMISSION; DIZZINESS; DRUG EFFICACY; DRUG INDUCED HEADACHE; DRUG TOLERABILITY; DYSPHORIA; EMBRYOTOXICITY; ENDEMIC DISEASE; GAMETOCYTE; HEARING IMPAIRMENT; HEMOLYTIC ANEMIA; HEPATITIS; HUMAN; HYPOGLYCEMIA; HYPOTENSION; LEUKOCYTE; LOADING DRUG DOSE; MALARIA; MALARIA CONTROL; MALARIA FALCIPARUM; MENTAL DISEASE; METHEMOGLOBINEMIA; MONOTHERAPY; MORTALITY; NAUSEA; NEUROLOGIC DISEASE; NEUROTOXICITY; NEUTROPENIA; ORTHOSTATIC HYPOTENSION; PHOTOSENSITIVITY; PLASMODIUM (LIFE CYCLE STAGE); PLASMODIUM VIVAX; PRURITUS; PSORIASIS; QRS COMPLEX; QT PROLONGATION; RECOMMENDED DRUG DOSE; REVIEW; SIDE EFFECT; SINGLE DRUG DOSE; SLEEP; STILLBIRTH; SUDDEN DEATH; THROMBOCYTE COUNT; TINNITUS; VOMITING;

EID: 70549104643     PISSN: 17512433     EISSN: None     Source Type: Journal    
DOI: 10.1586/ecp.09.27     Document Type: Review

References (297)

1. Guerra CA, Snow RW, Hay SI. Mapping the global extent of malaria in 2005. Trends Parasitol. 22, 353-358 (2006).
2. Breman JG, Alilio MS, Mills A. Conquering the intolerable burden of malaria: what's new, what's needed: a summary. Am. J. Trop. Med. Hyg. 71(Suppl. 2), 1-15 (2004). (Pubitemid 39127486)
3. Chin W, Coatney GR. Relapse activity in sporozoite-induced infections with a West African strain of Plasmodium ovale. Am. J. Trop. Med. Hyg. 20(6), 825-827 (1971).
4. Pukrittayakamee S, Chotivanich K, Chantra A, Clemens R, Looareesuwan S, White NJ. Activities of artesunate and primaquine against asexual- and sexualstage parasites in falciparum malaria. Antimicrob. Agents Chemother. 8(4), 1329-1334 (2004). (Pubitemid 38405489)
5. Mueller I, Zimmerman PA, Reeder JC. Plasmodium malariae and Plasmodium ovale - the "bashful" malaria parasites. Trends Parasitol. 23(6), 278-283 (2007).
6. Cox-Singh J, Davis TM, Lee KS et al. Plasmodium knowlesi malaria in humans is widely distributed and potentially life threatening. Clin. Infect. Dis. 46(2), 165-171 (2008). (Pubitemid 351269152)
7. Marsh MB, Forster D, Waruiru C et al. Indicators of life-threatening malaria in African children. N. Engl. J. Med. 332 (21), 1399-1404 (1995).
8. World Health Organization. Severe falciparum malaria. Trans. R. Soc. Trop. Med. Hyg. 94(Suppl. 1), S1-S90 (2000).
9. Artavanis-Tsakonas K, Tongren JE, Riley EM. The war between the malaria parasite and the immune system: immunity, immunoregulation and immunopathology. Clin. Exp. Immunol. 133, 145-152 (2003). (Pubitemid 36918587)
10. Trape JF. The public health impact of chloroquine resistance in Africa. Am. J. Trop. Med. Hyg. 64(Suppl. 1-2), 12-17 (2001).
11. White NJ. The management of severe falciparum malaria. Am. J. Respir. Crit. Care Med. 167(5), 673-674 (2003).
12. Menendez C, Ordi J, Ismail MR et al. The impact of placental malaria on gestational age and birth weight. J. Infect. Dis. 181(5), 1740-1745 (2000). (Pubitemid 30387768)
13. Stevens RD. Anaemia - the scourge of the Third World. Health Millions 26(2), 21-23 (2000).
14. Brabin BJ, Premji Z, Verhoeff F. An analysis of anemia and child mortality. J. Nutr. 131(2S-2), 636S-645S (2001).
15. Steketee RW, Nahlen BL, Parise ME, Menendez C. The burden of malaria in pregnancy in malaria-endemic areas. Am. J. Trop. Med. Hyg. 64(Suppl. 1-2), 28-35 (2001). (Pubitemid 32552569)
16. Binka F, Akweongo P. Prevention of malaria using ITNs: potential for achieving the millennium development goals. Curr. Mol. Med. 6(2), 261-267 (2006).
17. Snow RW, Guerra CA, Noor AM, Myint HY, Hay SI. The global distribution of clinical episodes of Plasmodium falciparum malaria. Nature 434, 214-217 (2005).
18. Harinasuta T, Suntharasamai P, Viravan C. Chloroquine-resistant falciparum malaria in Thailand. Lancet 2(7414), 657-660 (1965).
19. Mehlotra RK, Mattera G, Bockarie MJ et al. Discordant patterns of genetic variation at two chloroquine resistance loci in worldwide populations of the malaria parasite Plasmodium falciparum. Antimicrob. Agents Chemother. 6, 2212-2222 (2008). (Pubitemid 351758561)
20. Plowe CV, Cortese JF, Djimde A et al. Mutations in Plasmodium falciparum dihydrofolate reductase and dihydropteroate synthase and epidemiologic patterns of pyrimethaminesulfadoxine use and resistance. J. Infect. Dis. 176(6), 1590-1596 (2007).
21. Alker AP, Lim P, Sem R et al. Pfmdr1 and in vivo resistance to artesunate-mefloquine in falciparum malaria on the Cambodian- Thai border. Am. J. Trop. Med. Hyg. 76(4), 641-647 (2007). (Pubitemid 351627700)
22. Na-Bangchang K, Congpuong K. Current malaria status and distribution of drug resistance in East and Southeast Asia with special focus to Thailand. Tohoku J. Exp. Med. 211(2), 99-113 (2007). (Pubitemid 46268067)
23. Wongsrichanalai C and Meshnick SR. Declining artesunate-mefloquine efficacy against falciparum malaria on the Cambodia-Thailand border. Emerg. Infect. Dis. 5, 716-719 (2008). (Pubitemid 351838633)
24. Rieckmann KH, Davis DR, Hutton DC. Plasmodium vivax resistant to chloroquine? Lancet 2, 1183-1184 (1989).
25. Baird JK, Basri H, Purnomo et al. Resistance to chloroquine by Plasmodium vivax in Irian Jaya, Indonesia. Am. J. Trop. Med. Hyg. 44, 547-552 (1991).
26. Myat-Phone-Kyaw, Myint-Oo, Myint- Lwin, Thaw-Zin, Kyin-Hla-Aye, Nwe- Nwe-Yin. Emergence of chloroquineresistant Plasmodium vivax in Myanmar (Burma). Trans. R. Soc. Trop. Med. Hyg. 87(6), 687-692 (1993).
27. Marlar T, Myat PK, Aye YS, Khaing KG, Ma S, Mind O. Development of resistance to chloroquine by Plasmodium vivax in Myanmar. Trans. R. Soc. Trop. Med. Hyg. 89, 307-308 (1995).
28. Dua VK, Kar PK, Sharma VP. Chloroquine resistant Plasmodium vivax malaria in India. Trop. Med. Int. Health 1, 816-819 (1996).
29. Kurcer MA, Simsek Z, Zeyrek FY et al. Efficacy of chloroquine in the treatment of Plasmodium vivax malaria in Turkey. Ann. Trop. Med. Parasitol. 98, 447-451 (2004). (Pubitemid 38951677)
30. Fryauff DJ, Tuti S, Mardi A et al. Chloroquine-resistant Plasmodium vivax in transmigration settlements of West Kalimantan, Indonesia. Am. J. Trop. Med. Hyg. 59, 513-518 (1998). (Pubitemid 28480701)
31. Phillips EJ, Keystone JS, Kain KC. Failure of combined chloroquine and high-dose primaquine therapy for Plasmodium vivax malaria acquired in Guyana, South America. Clin. Infect. Dis. 23, 1171-1173 (1996).
32. Alecrim MG, Alecrim W, Macedo V. Plasmodium vivax resistance to chloroquine (R2) and mefloquine (R3) in Brazilian Amazon region. Rev. Soc. Bras. Med. Trop. 32, 67-68 (1999). (Pubitemid 29006271)
33. Villalobos-Salcedo JM, Tada MS, Kimura E, Menezes MJ, Pereira da Silva LH. In-vivo sensitivity of Plasmodium vivax isolates from Rond nia (western Amazon region, Brazil) to regimens including chloroquine and primaquine. Ann. Trop. Med. Parasitol. 94(8), 749-758 (2000). (Pubitemid 32102485)
34. de Santana Filho FS, Arcanjo AR, Chehuan YM et al. Chloroquine-resistant Plasmodium vivax, Brazilian Amazon. Emerg. Infect. Dis. 13, 1125-1126 (2007).
35. Soto J, Toledo J, Gutierrez P et al. Plasmodium vivax clinically resistant to chloroquine in Colombia. Am. J. Trop. Med. Hyg. 65, 90-93 (2001). (Pubitemid 32744210)
36. Ruebush TK, Zegarra J, Cairo J et al. Chloroquine resistant Plasmodium vivax malaria in Peru. Am. J. Trop. Med. Hyg. 69, 548-552 (2003). (Pubitemid 38248258)
37. Phan GT, de Vries PJ, Tran BQ et al. Artemisinin or chloroquine for blood stage Plasmodium vivax malaria in Vietnam. Trop. Med. Int. Health 7, 858-864 (2002).
38. Teka H, Petros B, Yamuah L et al. Chloroquine-resistant Plasmodium vivax malaria in Debre Zeit, Ethiopia. Malar. J. 7, 220 (2008).
39. Sumawinata IW, Bernadeta BL, Awalludin S et al. Very high risk of therapeutic failure with chloroquine for uncomplicated Plasmodium falciparum and P. vivax malaria in Indonesian Papua. Am. J. Trop. Med. Hyg. 68, 416-420 (2003).
40. Tjitra E, Baker J, Suprianto S, Cheng Q, Anstey NM. Therapeutic efficacies of artesunate-sulfadoxine-pyrimethamine and chloroquine-sulfadoxine- pyrimethamine in vivax malaria pilot studies: relationship to Plasmodium vivax dhfr mutations. Antimicrob. Agents Chemother. 46(12), 3947-3953 (2002). (Pubitemid 35403273)
41. Barnes KI, Watkins WM, White NJ. Antimalarial dosing regimens and drug resistance. Trends Parasitol. 24(3), 127-134 (2008).
42. Golenser J, Waknine JH, Krugliak M, Hunt NH, Grau GE. Current perspectives on the mechanism of action of artemisinins. Int. J. Parasitol. 36(14), 1427-1441 (2006). (Pubitemid 44751746)
43. Wilson CM, Volkman SK, Thaithong S et al. Amplification of pfmdr 1 associated with mefloquine and halofantrine resistance in Plasmodium falciparum from Thailand. Mol. Biochem. Parasitol. 57(1), 151-160 (1993). (Pubitemid 23020712)
44. Cowman AF, Galatis D, Thompson JK. Selection for mefloquine resistance in Plasmodium falciparum is linked to amplification of the pfmdr1 gene and cross-resistance to halofantrine and quinine. Proc. Natl Acad. Sci. USA 91(3), 1143-1147 (1994). (Pubitemid 24048525)
45. Sidhu AB, Uhlemann AC, Valderramos SG, Valderramos JC, Krishna S, Fidock DA. Decreasing pfmdr1 copy number in plasmodium falciparum malaria heightens susceptibility to mefloquine, lumefantrine, halofantrine, quinine, and artemisinin. J. Infect. Dis. 194(4), 528-535 (2006). (Pubitemid 44162666)
46. Uhlemann AC, McGready R, Ashley EA et al. Intrahost selection of Plasmodium falciparum pfmdr1 alleles after antimalarial treatment on the northwestern border of Thailand. J. Infect. Dis. 195(1), 134-141 (2007). (Pubitemid 44958235)
47. Price RN, Uhlemann AC, van Vugt M et al. Molecular and pharmacological determinants of the therapeutic response to artemether-lumefantrine in multidrugresistant Plasmodium falciparum malaria. Clin. Infect. Dis. 42(11), 1570-1577 (2006).
48. Rungsihirunrat K, Chaijareonkul W, Seugorn A, Na-Bangchang K, Thaithong S. Association between chloroquine resistance phenotypes and point mutations in pfcrt and pfmdr1 in Plasmodium falciparum isolates from Thailand. Acta Trop. 109(1), 37-40 (2009).
49. Fidock DA, Nomura T, Cooper RA, Su X, Talley AK, Wellems TE. Allelic modifications of the cg2 and cg1 genes do not alter the chloroquine response of drug-resistant Plasmodium falciparum. Mol. Biochem. Parasitol. 110(1), 1-10 (2000).
50. Bray PG, Ward SA, O'Neill PM. Quinolines and artemisinin: chemistry, biology and history. Curr. Top. Microbiol. Immunol. 295, 3-38 (2005).
51. Eckstein-Ludwig U, Webb RJ, Van Goethem ID et al. Artemisinins target the SERCA of Plasmodium falciparum. Nature 424(6951), 957-961 (2003).
52. Ferreira ID, Martinelli A, Rodrigues LA et al. Plasmodium falciparum from Pará state (Brazil) shows satisfactory in vitro response to artemisinin derivatives and absence of the S769N mutation in the SERCA-type PfATPase6. Trop. Med. Int. Health. 13(2), 199-207 (2008). (Pubitemid 351316971)
53. Price RN, Uhlemann AC, Brockman A et al. Mefloquine resistance in Plasmodium falciparum and increased pfmdr1 gene copy number. Lancet 364, 438-447 (2007). (Pubitemid 39036891)
54. Bell DJ, Molyneux ME. Treatment of childhood Plasmodium falciparum malaria: current challenges. Expert Rev. Anti. Infect. Ther. 5(1), 141-152 (2007).
55. Na-Bangchang K, Karbwang J. Current status of malaria chemotherapy and the role of pharmacology in antimalarial drug research and development. Fund Clin. Pharmacol. 23(4), 387-409(2009).
56. Trampuz A, Jereb M, Muzlovic I, Prabhu RM. Clinical review: Severe malaria. Crit. Care 7(4), 315-323 (2003).
57. Pengsaa K, Sirivichayakul C, Na-Bangchang K et al. Life-saving rectal artesunate for complicated malaria in children. Southeast Asian J. Trop. Med. Public Health 36(3), 597-601 (2005). (Pubitemid 41316779)
58. Karunajeewa HA, Manning L, Mueller I, Ilett KF, Davis TM. Rectal administration of artemisinin derivatives for the treatment of malaria. JAMA 297(21), 2381-2390 (2007). (Pubitemid 46883751)
59. Gomes M, Ribeiro I, Warsame M, Karunajeewa H, Petzold M. Rectal artemisinins for malaria: a review of efficacy and safety from individual patient data in clinical studies. BMC Infect Dis. 8, 39 (2008). (Pubitemid 351634257)
60. World Health Organization. Antimalarial drug combination therapy. Report of a WHO Technical Consultation. (WHO/ CDS/RBM/2001.35) Geneva, 4-5 April 2001.
61. Kuhn S, Gill MJ, Kain KC. Emergence of atovaquone-proguanil resistance during treatment of Plasmodium falciparum malaria acquired by a non-immune north American traveller to west Africa. Am. J. Trop. Med. Hyg. 72(4), 407-409 (2005). (Pubitemid 41278848)
62. Krudsood S, Patel SN, Tangpukdee N et al. Efficacy of atovaquone-proguanil for treatment of acute multidrug-resistant Plasmodium falciparum malaria in Thailand. Am. J. Trop. Med. Hyg. 76(4), 655-658 (2007). (Pubitemid 351627702)
63. Klayman DL. Qinghaosu (artemisinin): an antimalarial drug from China. Science 228, 1049-1055 (1985).
64. Nosten F, White NJ. Artemisinin-based combination treatment of falciparum malaria. Am. J. Trop. Med. Hyg. 77(6 Suppl.), 181-192 (2007).
65. Hien TT, White NJ. Qinghaosu. Lancet 341(8845), 603-608 (1993).
66. De Vries PJ, Dien TK. Clinical pharmacology and therapeutic potential of artemisinin and its derivatives in the treatment of malaria. Drugs 52, 818-836 (1996).
67. Price RN, Nosten F, Luxemburger C et al. Effects of artemisinin derivatives on malaria transmissibility. Lancet 347(9016), 1654-1658 (1996). (Pubitemid 26177386)
68. Dutta GP, Bajpai R, Vishwakarma RA. Artemisinin (qinghaosu) - a new gametocytocidal drug for malaria. Chemotherapy 35(3), 200-207 (1989). (Pubitemid 19161234)
69. Bousema JT, Schneider P, Gouagna LC et al. Moderate effect of artemisinin-based combination therapy on transmission of Plasmodium falciparum. J. Infect. Dis. 193(8), 1151-1159 (2006).
70. Hien TT. An overview of the clinical use of artemisinin and its derivatives in the treatment of falciparum malaria in Viet Nam. Trans. R. Soc. Trop. Med. Hyg. 88 (Suppl. 1), S7-S8 (1994).
71. McIntosh HM, Olliaro P. Artemisinin derivatives for treating severe malaria. Cochrane Database Syst Rev 2, CD000527 (2000).
72. Duffy PE, Sibley CH. Are we losing artemisinin combination therapy already? Lancet 66 (9501), 1908-1909 (2005).
73. Krishna S, Bustamante L, Haynes RK, Staines HM. Artemisinins: their growing importance in medicine. Trends Pharmacol. Sci. 29(10), 520-572 (2008).
74. White N. Antimalarial drug resistance and combination chemotherapy. Philos. Trans. R. Soc. Lond. B. Biol. Sci. 354(1384), 739-749 (1999). (Pubitemid 29365622)
75. Davis TM, Karunajeewa HA, Ilett KF. Artemisinin-based combination therapies for uncomplicated malaria. Med. J. Aust. 182(4), 181-185 (2005) .
76. World Health Organization Guidelines for the treatment of malaria. WHO/HTM/ MAL 2006.1108 [cited 2008 Mar 5]. Geneva (2006)
77. Ogbonna A, Uneke CJ. Artemisinin-based combination therapy for uncomplicated malaria in sub-Saharan Africa: the efficacy, safety, resistance and policy implementation since Abuja 2000. Trans. R. Soc. Trop. Med. Hyg. 102(7), 621-627 (2008).
78. Tangpukdee N, Krudsood S, Thanachartwet V et al. Efficacy of Artequick versus artesunate-mefloquine in the treatment of acute uncomplicated falciparum malaria in Thailand. Southeast Asian J. Trop. Med. Public Health 39(1), 1-8 (2008).
79. World Health Organization. Drug resistance in malaria. Report of a WHO Technical Consultation (WHO/CDS/ RBM/2001.4) Geneva, Switzerland (2001).
80. Davis TME, Hung TY, Sim IK et al. Piperaquine: a resurgent antimalarial drug. Drugs 65, 75-87 (2005).
81. Nosten F, Luxemburger C, ter Kuile FO et al.Treatment of multidrug-resistant Plasmodium falciparum malaria with 3-day artesunate-mefloquine combination. J. Infect. Dis. 170(4), 971-977 (1994). (Pubitemid 24296580)
82. Nosten F, van Vugt M, Price R et al. Effects of artesunate-mefloquine combination on incidence of Plasmodium falciparum malaria and mefloquine resistance in estern Thailand: a prospective study. Lancet 356, 297-302 (2000). (Pubitemid 30459588)
83. Muheki C, McIntyre D, Barnes KI. Artemisinin-based combination therapy reduces expenditure on malaria treatment in KwaZulu natal, south Africa. Trop. Med. Int. Health 9(9), 959-966 (2004). (Pubitemid 39278996)
84. Barnes KI, Durrheim DN, Little F et al. Effect of artemether-lumefantrine policy and improved vector control on malaria burden in KwaZulu-Natal, South Africa. PLoS Med. 2(11), 330 (2005).
85. Nkhoma S, Nair S, Mukaka M, Molyneux ME, Ward SA, Anderson TJ. Parasites bearing a single copy of the multi-drug resistance gene (pfmdr-1) with wild-type SNPs predominate amongst Plasmodium falciparum isolates from Malawi. Acta Trop. 111(1), 78-81 (2009).
86. Abacassamo F, Enosse S, Aponte JJ et al. Efficacy of chloroquine, amodiaquine, sulphadoxine-pyrimethamine and combination therapy with artesunate in Mozambican children with noncomplicated malaria. Trop. Med. Int. Health 9(2), 200-208 (2004). (Pubitemid 38250806)
87. Nguyen MH, Davis TM, Cox-Singh J et al. Treatment of uncomplicated falciparum malaria in southern Vietnam: can chloroquine or sulfadoxine- pyrimethamine be reintroduced in combination with artesunate? Clin. Infect. Dis. 37, 1461-1466 (2003). (Pubitemid 37494673)
88. Mita T, Kaneko A, Lum JK et al. Recovery of chloroquine sensitivity and low prevalence of the Plasmodium falciparum chloroquine resistance transporter gene mutation K76T following the discontinuance of chloroquine use in Malawi. Am. J. Trop. Med. Hyg. 68(4), 413-415 (2003). (Pubitemid 38230640)
89. Mita T, Kaneko A, Lum JK et al. Recovery of chloroquine sensitivity and low prevalence of the Plasmodium falciparum chloroquine resistance transporter gene mutation K76T following the discontinuance of chloroquine use in Malawi. Am. J. Trop. Med. Hyg. 68(4), 413-415 (2003). (Pubitemid 38230640)
90. Thimasarn K, Sirichaisinthop J, Chanyakhun P, Palananth C, Rooney W A. Comparative study of artesunate and artemether in combination with mefloquine on multidrug resistant falciparum malaria in eastern Thailand. Southeast Asian J. Trop. Med. Public Health 28, 465-471 (1997). (Pubitemid 127523373)
91. Wongsrichanalai C, Prajakwong S, Meshnick SR, Shanks GD, Thimasarn K. Mefloquine - its 20 years in the Thai Malaria Control Program. Southeast Asian J. Trop. Med. Public Health 35(2), 300-308 (2004). (Pubitemid 39248705)
92. Abdulla S, Sagara I, Borrmann S et al. Efficacy and safety of artemetherlumefantrine dispersible tablets compared with crushed commercial tablets in African infants and children with uncomplicated malaria: a randomised, single-blind, multicentre trial. Lancet 372(9652), 1819-1827 (2008).
93. Hatz C, Soto J, Nothdurft HD et al. Treatment of acute uncomplicated Falciparum malaria with artemetherlumefantrine in non-immune populations: a safety, efficacy, and pharmacokinetic study. Am. J. Trop. Med. Hyg. 2, 241-247 (2008). (Pubitemid 351844558)
94. Teklehaimanot A, Teklehaimanot HD. Alternative form of artemetherlumefantrine for infants. Lancet 372(9652), 1786-1787 (2008).
95. Thapa S, Hollander J, Linehan M et al. Comparison of artemether- lumefantrine with sulfadoxine-pyrimethamine for the treatment of uncomplicated falciparum malaria in Eastern Nepal. Am. J. Trop. Med. Hyg. 3, 423-430 (2007). (Pubitemid 351844313)
96. Sowunmi, GO Gbotosho, CT Happi et al. Therapeitic efficacy and effects of artemether-lumefantrine and amodiaquine-sulfalene-pyrimethamine on gametocyte carriage in children with uncomplicated Plasmodium falciparum malaria in Southwestern Nigeria. Am. J. Trop. Med. Hyg. 2, 235-241 (2007).
97. Zurovac D, Tibenderana JK, Nankabirwa J et al. Malaria case-management under artemether-lumefantrine treatment policy in Uganda. Malar. J. 7, 181 (2008).
98. Gitonga CW, Amin AA, Ajanga A, Kangwana BB, Noor AM, Snow RW. The use of artemether-lumefantrine by febrile children following national implementation of a revised drug policy in Kenya. Trop. Med. Int. Health 13(4), 487-494 (2008).
99. Ashley EA, Stepniewska K, Lindegårdh N et al. How much fat is necessary to optimize lumefantrine oral bioavailability? Trop. Med. Int. Health 12(2), 195-200 (2007). (Pubitemid 46244168)
100. Kobbe R, Klein P, Adjei S et al. A randomized trial on effectiveness of artemether-lumefantrine versus artesunate plus amodiaquine for unsupervised treatment of uncomplicated Plasmodium falciparum malaria in Ghanaian children. Malar. J. 7, 261 (2008).
101. Odura AR, Anyorigiya T, Anto F et al. A randomized, comparative study of supervised and unsupervised artesunateamodiaquine, for the treatment of uncomplicated malaria in Ghana. Ann. Trop. Med. Parasitol. 102(7), 565-576 (2008).
102. Sarrassat S, Senghor P, Le Hesran JY. Trends in malaria morbidity following the introduction of artesunate plus amodiaquine combination in M'lomp village dispensary, south-western Senegal. Malar. J. 7, 215 (2008).
103. Sowunmi A, Balogun ST, Gbotosho GO, Happi CT. Effects of amodiaquine, artesunate, and artesunate-amodiaquine on Plasmodium falciparum malaria-associated anaemia in children. Acta Trop 109(1), 55-60 (2009).
104. Adjuik M, Agnamey P, Babiker A et al. Amodiaquine-artesunate versus amodiaquine for uncomplicated Plasmodium falciparum malaria in African children: a randomised, multicentre trial. Lancet 359, 1365-1372 (2002). (Pubitemid 34442375)
105. Neftel KA, Woodtly W, Schmid M, Frick PG, Fehr J. Amodiaquine induced agranulocytosis and liver damage. BMJ 292, 721-723 (1986). (Pubitemid 16167398)
106. Phillips-Howard PA, Bjorkman AB. Ascertainment of risk of serious adverse reactions associated with chemoprophylactic antimalarial drugs. Bull World Health Organ. 68, 493-504 (1990).
107. Hatton CS, Peto TE, Bunch C et al. Frequency of severe neutropenia associated with amodiaquine prophylaxis against malaria. Lancet 1, 411-414 (1986). (Pubitemid 16166282)
108. Tall A, Rabarijaona LP, Robert V, Bedja SA, Ariey F, Randrianarivelojosia M. Efficacy of artesunate plus amodiaquine, artesunate plus sulfadoxine- pyrimethamine, and chloroquine plus sulfadoxine-pyrimethamine in patients with uncomplicated Plasmodium falciparum in the Comoros Union. Acta Trop. 102(3), 176-181 (2007). (Pubitemid 47017199)
109. Ibrahium AM, Kheir MM, Osman ME et al. Efficacies of artesunate plus either sulfadoxine-pyrimethamine or amodiaquine, for the treatment of uncomplicated, Plasmodium falciparum malaria in eastern Sudan. Ann. Trop. Med. Parasitol. 101(1), 15-21 (2007).
110. Mohamed AO, Eltaib EH, Ahmed OA, Elamin SB, Malik EM. The efficacies of artesunate-sulfadoxine-pyrimethamine and artemether-lumefantrine in the treatment of uncomplicated, Plasmodium falciparum malaria, in an area of low transmission in central Sudan. Ann. Trop. Med. Parasitol. 100(1), 5-10 (2006).
111. Tall A, Rabarijaona LP, Robert V, Bedja SA, Ariey F, Randrianarivelojosia M. Efficacy of artesunate plus amodiaquine, artesunate plus sulfadoxine- pyrimethamine, and chloroquine plus sulfadoxine-pyrimethamine in patients with uncomplicated Plasmodium falciparum in the Comoros Union. Acta Trop. 102(3), 176-181 (2007). (Pubitemid 47017199)
112. Price RN, Hasugian AR, Ratcliff A et al. Clinical and pharmacological determinants of the therapeutic response to dihydroartemisinin-piperaquine for drug-resistant malaria. Antimicrob. Agents Chemother. 51(11), 4090-4097 (2007). (Pubitemid 350057809)
113. Vennerstrom JL, Ellis WY, Ager AL Jr, Andersen SL, Gerena L, Milhous WK. Bisquinolines. 1. N,N-bis(7- chloroquinolin-4-yl)alkanediamines with potential against chloroquine-resistant malaria. J. Med. Chem. 35(11), 2129-2134 (1992).
114. Ashley EA, R McGready, R Hutagalung et al. A randomized, controlled study of a simple, once-daily regimen of dihydroartemisinin-piperaquine for the treatment of uncomplicated, multidrugresistant falciparum malaria. Clin. Infect. Dis. 41, 425-432 (2005).
115. Denis MB, Davis TME, Hewitt S et al. Efficacy and safety of dihydroartemisininpiperaquine (Artekin) in Cambodian children and adults with uncomplicated falciparum malaria. Clin. Infect. Dis. 35, 1469-1476 (2002). (Pubitemid 36020689)
116. Karunajeewa H, Lim C, Hung T et al. Safety evaluation of fixed combination piperaquine plus dihydroartemisinin (Artekin®) in Cambodian children and adults with malaria. Br. J. Clin. Pharmacol. 57, 93-99 (2004). (Pubitemid 38067955)
117. Ashley EA, Krudsood S, Phaiphun L et al. Randomized, controlled dose-optimization studies of dihydroartemisinin-piperaquine for the treatment of uncomplicated multidrug-resistant falciparum malaria in Thailand. J. Infect. Dis. 190, 1773-1782 (2004). (Pubitemid 39487822)
118. Smithuis F, Kyaw MK, Phe O et al. Efficacy and effectiveness of dihydroartemisininpiperaquine versus artesunate-mefloquine in falciparum malaria: an open-label randomised comparison. Lancet 367(9528), 2075-2085 (2006). (Pubitemid 43949291)
119. Ratcliff A, Siswantoro H, Kenangalem E et al. Two fixed-dose artemisinin combinations for drug-resistant falciparum and vivax malaria in Papua, Indonesia: an open-label randomised comparison. Lancet 369(9563), 757-765 (2007). (Pubitemid 46335820)
120. Hasugian AR, Purba HL, Kenangalem E et al. Dihydroartemisinin-piperaquine versus artesunate-amodiaquine: superior efficacy and posttreatment prophylaxis against multidrug-resistant Plasmodium falciparum and Plasmodium vivax malaria. Clin. Infect. Dis. 44(8), 1067-1074 (2007). (Pubitemid 46580274)
121. Hastings IM, Watkins WM, White NJ. The evolution of drug resistant malaria: the role of drug elimination half-life. Phil. Trans. R. Soc. Lond. B 357, 505-519 (2002).
122. Nwaka S, Riopel L, Ubben D, Craft JC. Medicines for malaria menture new developments in antimalarials. Travel Med. Infect. Dis. 2(3-4), 161-170 (2004). (Pubitemid 39236770)
123. Alloueche A, Bailey W, Barton S et al. Comparison of chlorproguanil- dapsone with sulfadoxine-pyrimethamine for the treatment of uncomplicated falciparum malaria in young African children: double-blind randomised controlled trial. Lancet 363, 1843-1848 (2004).
124. van Vugt M, Leonardi E, Phaipun L et al. Treatment of uncomplicated multidrugresistant falciparum malaria with artesunate-atovaquone-proguanil. Clin. Infect. Dis. 5(12), 1498-1504 (2002). (Pubitemid 36020693)
125. Noedl H, Krudsood S, Chalermratana K et al. Azithromycin combination therapy with artesunate or quinine for the treatment of uncomplicated Plasmodium falciparum malaria in adults: a randomized, Phase 2 clinical trial in Thailand. Clin. Infect. Dis. 43(10), 1264-1271 (2006). (Pubitemid 44706451)
126. Jambou R, Legrand E, Niang M et al. Resistance of Plasmodium falciparum field isolates to in-vitro artemether and point mutations of the SERCA-type PfATPase6. Lancet 366, 1960-1963 (2005).
127. Vijaykadga S, Rojanawatsirivej C, Cholpol S, Phoungmanee D, Nakavej A, Wongsrichanalai C. In vivo sensitivity monitoring of mefloquine monotherapy and artesunate-mefloquine combinations for the treatment of uncomplicated falciparum malaria in Thailand in 2003. Trop. Med. Int. Health 11, 211-219 (2006).
128. Noedl H, Se Y, Schaecher K, Smith BL, Socheat D, Fukuda MM. Artemisinin Resistance in Cambodia 1 (ARC1) Study Consortium. Evidence of artemisininresistant malaria in western Cambodia. N. Engl. J. Med. 359(24), 2619-2620 (2008).
129. ter Kuile F, White NJ, Holloway P, Pasvol G, Krishna S. Plasmodium falciparum: in vitro studies of the pharmacodynamic properties of drugs used for the treatment of severe malaria. Exp. Parasitol. 76(1), 85-95 (1993).
130. Dondorp A, Nosten F, Stepniewska K, Day N, White N. South East Asian Quinine Artesunate Malaria Trial (SEAQUAMAT) group. Artesunate versus quinine for treatment of severe falciparum malaria: a randomised trial. Lancet 366 (9487), 717-725 (2005).
131. White NJ, Looareesuwan S, Warrell DA, Warrell MJ, Bunnag D, Harinasuta T. Quinine pharmacokinetics and toxicity in cerebral and uncomplicated falciparum malaria. Am. J. Med. 73(4), 564-572 (1982).
132. Winstanley PA, Pasvol G, and Marsh K. Quinine dose recommendations in childhood malaria - a reply. Trans. R. Soc. Trop. Med. Hyg. 89 (4), 463-464 (1995).
133. Huda SN, Shahab T, Ali SM, Afzal K, Khan HM. A comparative clinical trial of artemether and quinine in children with severe malaria. Indian Pediatr. 40(10), 939-945 (2003). (Pubitemid 37295893)
134. Schapira A, Solomon T, Julien M et al. Comparison of intramuscular and intravenous quinine for the treatment of severe and complicated malaria in children. Trans. R. Soc. Trop. Med. Hyg. 87(3), 299-302 (1993). (Pubitemid 23212364)
135. Taylor TE, Wills BA, Kazembe P et al. Rapid coma resolution with artemether in Malawian children with cerebral malaria. Lancet 341(8846), 661-662 (1993). (Pubitemid 23083249)
136. Wongsrichanalai C, Pickard AL, Wernsdorfer WH, Meshnick SR. Epidemiology of drug-resistant malaria. Lancet Infect. Dis. 2(4), 209-218 (2002).
137. Nour BY, Faragalla IA, Saeed OK, Mohamadani AA. In vitro study assessing the response of Plasmodium falciparum malaria to chloroquine, sulfadoxine/ pyrimethamine, quinine and mefloquine in Wad Medani District, Sudan. Saudi Med. J. 27(6), 808-812 (2006).
138. Pradines B, Hovette P, Fusai T et al. Prevalence of in vitro resistance to eleven standard or new antimalarial drugs among Plasmodium falciparum isolates from Pointe-Noire, Republic of the Congo. J. Clin. Microbiol. 44(7), 2404-2408 (2006). (Pubitemid 44092404)
139. Al-Shamahy H, Al-Harazy AH, Harmal NS, Al-Kabsi AM. The prevalence and degree of resistance of Plasmodium falciparum to first-line antimalarial drugs: an in vitro study from a malaria endemic region in Yemen. Ann. Saudi. Med. 27(6), 432-436 (2007). (Pubitemid 351234119)
140. Nealon C, Dzeing A, Müller-Römer U et al. Intramuscular bioavailability and clinical efficacy of artesunate in gabonese children with severe malaria. Antimicrob. Agents Chemother. 46(12), 3933-3939 (2002). (Pubitemid 35403271)
141. Hien TT, Davis TM, Chuong LV et al. Comparative pharmacokinetics of intramuscular artesunate and artemether in patients with severe falciparum malaria. Antimicrob. Agents Chemother. 48(11), 4234-4239 (2004).
142. Barnes KI, Mwenechanya J, Tembo M et al. Efficacy of rectal artesunate compared with parenteral quinine in initial treatment of moderately severe malaria in African children and adults: a randomised study. Lancet 363(9421), 1598-1605 (2004). (Pubitemid 38625662)
143. Barradell LB, Fitton A. Artesunate. A review of its pharmacology and therapeutic efficacy in the treatment of malaria. Drugs 50(4), 714-741 (1995).
144. Jones KL, Donegan S, Lalloo DG. Artesunate versus quinine for treating severe malaria. Cochrane Database Syst. Rev. 17(4), CD005967 (2007). (Pubitemid 351805160)
145. Karbwang J, Laothavorn P, Sukontason K et al. Effect of artemether on electrocardiogram in severe falciparum malaria. Southeast Asian J. Trop. Med. Public Health 28(3), 472-475 (1997). (Pubitemid 127523374)
146. Murphy SA, Mberu E, Muhia D et al. The disposition of intramuscular artemether in children with cerebral malaria; a preliminary study. Trans. R. Soc. Trop. Med. Hyg. 91(3), 331-334 (1997). (Pubitemid 27261178)
147. Checkley AM, Whitty CJ. Artesunate, artemether or quinine in severe Plasmodium falciparum malaria? Expert Rev. Anti Infect. Ther. 5(2), 199-204 (2007).
148. Praygod G, de Frey A, Eisenhut M. Artemisinin derivatives versus quinine in treating severe malaria in children: a systematic review. Malar. J. 7, 210 (2008).
149. Tran TH, Day NP, Nguyen HP et al. A controlled trial of artemether or quinine in Vietnamese adults with severe falciparum malaria. N. Engl. J. Med. 335(2), 76-83 (1996).
150. Mithwani S, Aarons L, Kokwaro GO et al. Population pharmacokinetics of artemether and dihydroartemisinin following single intramuscular dosing of artemether in African children with severe falciparum malaria. Br. J. Clin. Pharmacol. 57(2) 146-152 (2004). (Pubitemid 38223526)
151. Karunajeewa HA, Reeder J, Lorry K et al. Artesunate suppositories versus intramuscular artemether for treatment of severe malaria in children in Papua New Guinea. Antimicrob. Agents Chemother. 50(3), 968-974 (2006). (Pubitemid 43327802)
152. Gomes MF, Faiz MA, Gyapong JO et al. Study 13 research group: pre-referral rectal artesunate to prevent death and disability in severe malaria: a placebo-controlled trial. Lancet 373(9663), 557-566 (2009).
153. von Seidlein L, Deen JL. Pre-referral rectal artesunate in severe malaria. Lancet 373 (9663), 522-523 (2009).
154. Awad MI, E ltayeb IB, Baraka OZ, Behrens RH, Alkadru AM. Pharmacokinetics of artesunate following oral and rectal administration in healthy Sudanese volunteers. Trop. Doct. 34(3), 132-135 (2004).
155. Simpson JA, Agbenyega T, Barnes KI et al. Population pharmacokinetics of artesunate and dihydroartemisinin following intra-rectal dosing of artesunate in malaria patients. PLoS Med. 3(11), e444 (2006).
156. Benakis A, Binh TQ, Keundjian A, Scheiwe MW. Pharmacokinetics/ Pharmacodynamics findings after repeated administration of ARTESUNATE thermostable suppositories (RECTOCAPS) in Vietnamese patients with uncomplicated malaria. Eur. J. Drug Metab. Pharmacokinet. 31(1), 41-45 (2006). (Pubitemid 43736055)
157. Sirivichayakul C, Sabchareon A, Pengsaa K et al. Comparative study of the effectiveness and pharmacokinetics of two rectal artesunate/oral mefloquine combination regimens for the treatment of uncomplicated childhood falciparum malaria. Ann. Trop. Paediatr. 27(1), 17-24 (2007). (Pubitemid 47628957)
158. van Hensbroek MB, Palmer A, Onyiorah E et al. The effect of a monoclonal antibody to tumor necrosis factor on survival from childhood cerebral malaria. J. Infect. Dis. 174, 1091-1097 (1996). (Pubitemid 26357475)
159. Warrell DA, Looareesuwan S, Warrell MJ et al. Dexamethasone proves deleterious in cerebral malaria: a double-blind trial in 100 comatose patients. N. Engl. J. Med. 306, 313-319 (1982). (Pubitemid 12169111)
160. Hoffman SL, Rustama D, Punjabi NH et al. High-dose dexamethasone in quinine-treated patients with cerebral malaria: a doubleblind, placebocontrolled trial. J. Infect. Dis. 158, 325-331 (1988). (Pubitemid 18223247)
161. Di Perri G, Di Perri IG, Monteiro GB et al. Pentoxifylline as a supportive agent in the treatment of cerebral malaria in children. J. Infect. Dis. 171, 1317-1322 (1995).
162. Hemmer CJ, Hort G, Chiwakata CB et al. Supportive pentoxifylline in falciparum malaria: no effect on tumor necrosis factor alpha levels or clinical outcome: a prospective, randomized, placebocontrolled study. Am. J. Trop. Med. Hyg. 56, 397-403 (1997).
163. Bunnag D, Karbwang J, Thanavibul A et al. High dose of primaquine in primaquine resistant vivax malaria. Trans. R. Soc. Trop. Med. Hyg. 88(2), 218-219 (1994). (Pubitemid 24139695)
164. Looareesuwan S, Wilairatana P, Krudsood S et al. Chloroquine sensitivity of Plasmodium vivax in Thailand. Ann. Trop. Med. Parasitol. 93(3), 225-230 (1999). (Pubitemid 29355870)
165. Goller JL, Jolley D, Ringwald P, Biggs BA. Regional differences in the response of Plasmodium vivax malaria to primaquine as anti-relapse therapy. Am. J. Trop. Med. Hyg. 2, 203-207 (2007). (Pubitemid 351627764)
166. Baird JK. A rare glimpse at the efficacy of primaquine. Am. J. Trop. Med. Hyg. 2, 201-202 (2007).
167. Vinety JM. Editorial commentary: emerging chloroquine-resistant Plasmodium vivax (benign tertian) malaria: the need for alternative drug treatment. CID 42, 1073-1074 (2006).
168. Imwong M, Snounou G, Pukrittayakamee S et al. Relapses of Plasmodium vivax infection usually result from activation of heterologous hypnoyoites. JID 195, 927-933 (2007). (Pubitemid 46452096)
169. Krudsood S, Tangpukdee N, Wilairatana P et al. High-dose primaquine regimens against relapse of Plasmodium vivax malaria. Am. J. Trop. Med. Hyg. 5, 736-740 (2008). (Pubitemid 351845129)
170. Kitchener S, Nasveld P, Edstein MD. Short report: tafenoquine for the treatment of recurrent Plasmodium vivax malaria. Am. J. Trop. Med. Hyg. 3, 494-496 (2007). (Pubitemid 351627742)
171. Shanks GD, Oloo AJ, Aleman GM et al. A new primaquine analogue, tafenoquine (WR 238605), for prophylaxis against Plasmodium falciparum malaria. Clin. Infect. Dis. 33(12), 1968-1974 (2001).
172. Crockett M, Kain KC. Tafenoquine: a promising new antimalarial agent. Expert Opin. Investig. Drugs 16(5) 705-715 (2007). (Pubitemid 46723273)
173. Mehrotra N, Lal J, Puri SK, Madhusudanan KP, Gupta RC. in vitro and in vivo pharmacokinetic studies of bulaquine (analogue of primaquine), a novel antirelapse antimalarial, in rat, rabbit and monkey - highlighting species similarities and differences. Biopharm. Drug Dispos. 28(5), 209-227 (2007). (Pubitemid 47180171)
174. Puri SK, Srivastava R, Pandey VC, Sethi N, Dutta GP. Methemoglobin toxicity and hematological studies on malaria anti-relapse compound CDRI 80/53 in dogs. Am. J. Trop. Med. Hyg. 41(6), 638-642 (1998).
175. Puri SK, Dutta GP. Quinoline esters as potential antimalarial drugs: effect on relapses of Plasmodium cynomolgi infections in monkeys. Trans. R. Soc. Trop. Med. Hyg. 84(6), 759-760 (1990).
176. Gogtay NJ, Kamtekar KD, Dalvi SS, Chogle AR, Aigal U, Kshirsagar NA. Preliminary report of the evaluation of the gametocytocidal action of bulaquine, in adult patients with acute, Plasmodium falciparum malaria. Ann. Trop. Med. Parasitol. 98(5), 525-528 (2004). (Pubitemid 38951686)
177. Gogtay NJ, Kamtekar KD, Dalvi SS et al. A randomized, parallel study of the safety and efficacy of 45 mg primaquine versus 75 mg bulaquine as gametocytocidal agents in adults with blood schizonticide-responsive uncomplicated falciparum malaria [ISCRTN50134587]. BMC Infect. Dis. 6, 16-21 (2006)
178. Adak T, Valecha N, Sharma VP. Plasmodium vivax polymorphism in a clinical drug trial. Clin. Diagn. Lab. Immunol. 8(5), 891-894 (2001). (Pubitemid 32868302)
179. Tekwani BL, Walker LA. 8-Aminoquinolines: future role as antiprotozoal drugs. Curr. Opin. Infect. Dis. 19(6), 623-631 (2006).
180. Hoffman SL. Diagnosis, treatment, and prevention of malaria. Med. Clin. North. Am. 76(6), 1327-1355 (1992).
181. Garner P, Gülmezoglu AM. Drugs for preventing malaria in pregnant women. Cochrane Database Syst. Rev. 18(4), CD000169 (2006).
182. Brabin BJ, Wasame M, Uddenfeldt-Wort U, Dellicour S, Hill J, Gies S. Monitoring and evaluation of malaria in pregnancy - developing a rational basis for control. Malar. J. 11, (7 Suppl. 1), S6 (2008).
183. Ward SA, Sevene EJ, Hastings IM, Nosten F, McGready R. Antimalarial drugs and pregnancy: safety, pharmacokinetics, and pharmacovigilance. Lancet Infect. Dis. 7(2), 136-144 (2007). (Pubitemid 46123134)
184. Nosten F, McGready R, d'Alessandro U et al. Antimalarial drugs in pregnancy: a review. Curr. Drug Saf. 1(1), 1-15 (2006).
185. World Health Organization. Containment of malaria multi-drug resistance on the Cambodia-Thailand border. Report of an informal consultation, Phnom Penh, Cambodia. 29-30 January 2007, Report no. SEA-MAL-246.
186. World Health Organization. Assessment of the Safety of Artemisinins in Pregnancy: Report of Two Informal Consultations Convened by WHO in 2002. (WHO/CDS/ MAL/ 2003.1094, WHO/RBM/TDR/ Artemisinin/03.1). WHO, Geneva, Switzerland 1-14 (2003)
187. Nosten F, ter Kuile FO, Luxemburger C et al. Cardiac effects of antimalarial treatment with halofantrine. Lancet 341(8852), 1054-1056 (1993).
188. Taylor WR, White NJ. Anti malarial drug toxicity: a review. Drug Saf. 27(1), 25-61 (2004).
189. Clyde DF. Clinical problems associated with the use of primaquine as a tissue schizontocidal and gametocytocidal drug. Bull World Health Organ. 59(3), 391-395 (1981).
190. Nosten F, Vincenti M, Simpson J et al. The effects of mefloquine treatment in pregnancy. Clin. Infect. Dis. 28(4), 808-815 (1999).
191. Nosten F, McGready R, d'Alessandro U et al. Antimalarial drugs in pregnancy: a review. Curr. Drug Saf. 1(1), 1-15 (2006).
192. Phillips-Howard PA, Wood D. The safety of antimalarial drugs in pregnancy. Drug Safety 14, 131-145 (1996).
193. Checkley AM, Hill DR. Prevention of malaria in long-term travelers. Trends Parasitol. 23(10), 462-465 (2007).
194. Touze JE, Debonne JM, Boutin JP. Current situation and future perspectives for malaria prophylaxis among travelers and military personnel. Bull. Acad. Natl Med. 191(7), 1293-1302 (2007).
195. Lalloo DG, Hill DR. Preventing malaria in travelers. BMJ 336(7657), 1362-1366 (2008).
196. White NJ.. How antimalarial drug resistance affects post-treatment prophylaxis. Malar. J. 7, 1-7 (2008).
197. White NJ. Intermittent presumptive treatment for malaria. PLoS Med. 2, 1-3 (2005).
198. Tukur IU, Thacher TD, Sagay AS, Madaki JKA. A comparison of sulfadoxine-pyrimethamine with chloroquine and pyrimethamine for prevention of malaria in pregnant Nigerian women. Am. J. Trop. Med. Hyg. 6, 1019-1023 (2007).
199. Ramharter M, Schuster K, Bouyou-Akotet MK et al. Malaria in pregnancy before and after the implementation of a national IPTp program in Gabon. Am. J. Trop. Med. Hyg. 3, 418-422 (2007). (Pubitemid 351844312)
200. Ntab B, Cissé B, Boulanger D et al. Impact of intermittent preventive antimalarial treatment on the growth and Nutritional status of preschool children in rural Senegal (West Africa). Am. J. Trop. Med. Hyg. 3, 411-417 (2007). (Pubitemid 351844311)
201. Kobbe R, C Kreuzberg, S Adjei et al. A randomized controlled trial of extended intermittent preventive antimalarial treatment in infants, Clin. Infect. Dis. 45, 16-25 (2007). (Pubitemid 46984610)
202. Dicko A, Sagara I, Sissoko MS et al. Impact of intermittent preventive treatment with sulphadoxine-pyrimethamine targeting the transmission season on the incidence of clinical malaria in children in Mali. Malar. J. 7, 123 (2008).
203. Marsh K. Malaria disaster in Africa. Lancet 352(9132), 924 (1998).
204. Jones KD. Malarial chemoprophylaxis. BMJ 1, 337 (2008).
205. Bojang KA. Novel therapies for the prevention of malaria. Expert Opin. Investig. Drugs 17(12), 1839-1847 (2008).
206. Sicard S, Simon F, Soula G, Gazin P. Efficacy of antimalarial chemoprophylaxis for travelers. J. Travel Med. 16(1), 66-67 (2009)
207. Senn N, D'Acremont V, Landry P, Genton B. Malaria chemoprophylaxis: what do the travelers choose, and how does pretravel consultation influence their final decision. Am. J. Trop. Med. Hyg. 6, 1010-1014 (2007). (Pubitemid 351837784)
208. Polhemus ME, Remich S, Ogutu B et al. Malaria treatment with atovaquono- proguanil in malaria-immune adults: implications for malaria intervention trials and for pre-exposure prophylaxis of malaria. Antimicrob. Agents Chemother. 4, 1493-1495 (2008).
209. Thapar MM, Gupta S, Spindler C, Wernsdorfer WH, Björkman A. Pharmacodynamic interactions among atovaquone, proguanil and cycloguanil against Plasmodium falciparum in vitro. Trans. R. Soc. Trop. Med. Hyg. 97(3), 331-337 (2003).
210. Hill DR, Baird JK, Parise ME, Lewis LS, Ryan ET, Magill AJV. Primaquine: report from CDC expert meeting on malaria chemoprophylaxis I. Am. J. Trop. Med. Hyg. 75(3), 402-415 (2006).
211. Milhous W. Development of new drugs for chemoprophylaxis of malaria. Bull. Soc. Pathol. Exot. 94(2), 149-151 (2001).
212. Shanks GD, Oloo AJ, Aleman GM et al. A new primaquine analogue, tafenoquine (WR 238605), for prophylaxis against Plasmodium falciparum malaria. Clin. Infect. Dis. 33(12), 1968-1974 (2001).
213. Edstein MD, Kocisko DA, Walsh DS, Eamsila C, Charles BG, Rieckmann KH. Plasma concentrations of tafenoquine, a new long-acting antimalarial agent, in Thai soldiers receiving monthly prophylaxis. Clin. Infect. Dis. 37(12), 1654-1658 (2003). (Pubitemid 37549953)
214. Albright TA, Binns HJ, Katz BZ. Side effects of and compliance with malaria prophylaxis in children. J. Trav. Med. 9 (6), 289-292 (2006).
215. White NJ, Chanthavanich P, Krishna S, Bunch C, Silamut K. Quinine disposition kinetics. Br. J. Clin. Pharmacol. 16(4), 399-403 (1983).
216. AlKadi HO. Antimalarial drug toxicity: a review. Chemotherapy 53(6), 385-391 (2007).
217. German PI, Aweeka FT. Clinical pharmacology of artemisinin-based combination therapies. Clin. Pharmacokinet. 47(2), 91-102 (2008).
218. Mohapara MK, Srinivas D, Kar AK. Anaphylactic reaction to intravenous artesunate. JAPI 57, 182-183 (2009).
219. White NJ. Cardiotoxicity of antimalarial drugs. Lancet Infect. Dis. 7(8), 549-558 (2007).
220. AlKadi HO. Antimalarial drug toxicity: a review. Chemotherapy 53(6), 385-391 (2007).
221. Karbwang J, Na-Bangchang K. Clinical pharmacokinetics of halofantrine. Clin. Pharmacokinet. 27(2), 104-119 (1994).
222. Wesche DL, Schuster BG, Wang WX, Woosley RL. Mechanism of cardiotoxicity of halofantrine. Clin. Pharmacol. Ther. 67(5), 521-529 (2000).
223. Lefèvre G, Carpenter P, Souppart C et al. Interaction trial between artemetherlumefantrine (Riamet) and quinine in healthy subjects. J. Clin. Pharmacol. 42(10),1147-1158 (2002). (Pubitemid 35056439)
224. van Vugt M, Ezzet F, Nosten F, Gathmann I, Wilairatana P, Looareesuwan S, White NJ. No evidence of cardiotoxicity during antimalarial treatment with artemether-lumefantrine. Am. J. Trop. Med. Hyg. 61(6), 964-967 (1999).
225. Davidson DE Jr. Role of arteether in the treatment of malaria and plans for further development. Trans. R. Soc. Trop. Med. Hyg. 88(Suppl. 1), S51-S52 (1994).
226. Soni CL, Kumhar MR, Gupta BK et al. Prognostic implication of hypocalcemia and QTc interval in malaria. Indian J. Malariol. 37(3-4), 61-67 (2000).
227. Traebert M, Dumotier B. Antimalarial drugs: QT prolongation and cardiac arrhythmias. Expert Opin. Drug Saf. 4(3), 421-431 (2005). (Pubitemid 40723717)
228. Brewer TG, Grate SJ, Peggins JO et al. Fatal neurotoxicity of arteether and artemether. Am. J. Trop. Med. Hyg. 51(3), 251-259 (1994).
229. Maude RJ, Plewes K, Faiz MA et al. Does artesunate prolong the electrocardiograph QT interval in patients with severe malaria? Am. J. Trop. Med. Hyg. 80(1), 126-132 (2009).
230. Nontprasert A, Nosten-Bertrand M, Pukrittayakamee S, Vanijanonta S, Angus BJ, White NJ. Assessment of the neurotoxicity of parenteral artemisinin derivatives in mice. Am. J. Trop. Med. Hyg. 59(4), 519-522 (1998). (Pubitemid 28480702)
231. Genovese RF, Newman DB, Brewer TG. Behavioural and neural toxicity of the artemisinin antimalarial, arteether, but not artesunate and artelinate, in rats. Pharmacol. Biochem. Behav. 67, 37-44 (2000).
232. Nontprasert A, Pukrittayakamee S, Nosten-Bertrand M, Vanijanonta S, White NJ. Studies of the neurotoxicity of oral artemisinin derivatives in mice. Am. J. Trop. Med. Hyg. 62(3), 409-412 (2000). (Pubitemid 30774747)
233. Nontprasert A, Pukrittayakamee S, Prakongpan S, Supanaranond W, Looareesuwan S, White NJ. Assessment of the neurotoxicity of oral dihydroartemisinin in mice. Trans. R. Soc. Trop. Med. Hyg. 96(1), 99-101 (2002). (Pubitemid 34846544)
234. Ribeiro IR, Olliaro P. Safety of artemisinin and its derivatives. A review of published and unpublished clinical trials. Med. Trop. (Mars) 58(3 Suppl.), 50-53 (1998). (Pubitemid 128707818)
235. Kissinger E, Hien TT, Hung NT et al. Clinical and neurophysiological study of the effects of multiple doses of artemisinin on brain-stem function in Vietnamese patients. Am. J. Trop. Med. Hyg. 63, 48-65 (2000). (Pubitemid 32423094)
236. Toovey S, Jamieson A. Audiometric changes associated with the treatment of uncomplicated falciparum malaria with co-artemether. Trans. R. Soc. Trop. Med. Hyg. 98(5), 261-367 (2004). (Pubitemid 38950400)
237. Chen LJ, Wang MY, Sun WK, Liu MZ. Embryotoxicity and teratogenicity studies on artemether in mice, rats and rabbits. Zhongguo Yao Li Xue Bao 5(2), 118-122 (1984).
238. Dellicour S, Hall S, Chandramohan D, Greenwood B. The safety of artemisinins during pregnancy: a pressing question. Malar. J. 6, 15 (2007). (Pubitemid 46321435)
239. Kalilani L, Mofolo I, Chaponda M et al. A randomized controlled pilot trial of azithromycin or artesunate added to sulfadoxine-pyrimethamine as treatment for malaria in pregnant women. PLoS ONE 2(11), e116 (2007). (Pubitemid 351637964)
240. Rijken MJ, McGready R, Boel ME et al. Dihydroartemisinin-piperaquine rescue treatment of multidrug-resistant Plasmodium falciparum malaria in pregnancy: a preliminary report. Am. J. Trop. Med. Hyg. 78(4), 543-545 (2008). (Pubitemid 351845153)
241. Pukrittayakamee S, Viravan C, Charoenlarp P, Yeamput C, Wilson RJ, White NJ. Antimalarial effects of rifampin in Plasmodium vivax malaria. Antimicrob. Agents Chemother. 38(3), 511-514 (1994). (Pubitemid 24072240)
242. Sousa M, Pozniak A, Boffito M. Pharmacokinetics and pharmacodynamics of drug interactions involving rifampicin, rifabutin and antimalarial drugs. J. Antimicrob. Chemother. 18, 1-7 (2008).
243. Wanwimolruk S, Kang W, Coville PF, Viriyayudhakorn S, Thitiarchakul S. Marked enhancement by rifampicin and lack of effect of isoniazid on the elimination of quinine in man. Br. J. Clin. Pharmacol. 40(1), 87-91 (1995).
244. Pukrittayakamee S, Prakongpan S, Wanwimolruk S, Clemens R, Looareesuwan S, White NJ. Adverse effect of rifampin on quinine efficacy in uncomplicated falciparum malaria. Antimicrob. Agents Chemother. 47(5) 1509-1513 (2003). (Pubitemid 36548530)
245. Biagini G, O'Neill PM, Bray PG, Ward SA. Current drug development portfolio for antimalarial therapies. Curr. Opin. Pharmacol. 5, 473-478 (2005). (Pubitemid 41258563)
246. Gardner MJ. The genome of the malaria parasite. Curr. Opin. Genet. Dev. 9(6), 704-708 (1999).
247. Sakata T, Winzeler EA. Genomics, systems biology and drug development for infectious diseases. Mol. Biosyst. 3, 841-848 (2007). (Pubitemid 350115411)
248. Meissner M, Agop-Nersesian C, Sullivan WJ Jr. Molecular tools for analysis of gene function in parasitic microorganisms. Appl. Microbiol. Drug Discov. 3, 509-520 (2007).
249. Ekland EH, Fidock, DA. Advances in understanding the genetic basis of antimalarial drug resistance. Curr. Opin. Microbiol. 10, 363-370 (2007).
250. Fidock DA, Rosenthal PJ, Croft SL, Brun R, Nwaka S. Antimalarial drug discovery: efficacy models for compound screening. Nat. Rev. Drug Discov. 3, 509-520 (2004) (Pubitemid 38807533)
251. Singh N, Misra K. Computational screening of molecular targets in Plasmodium for novel non resistant anti-malarial drugs. Bioinformation 3(6), 255-262 (2009).
252. Cameron A, Read J, Tranter R et al. Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity. J. Biol. Chem. 279(30), 31429-31439 (2004). (Pubitemid 39037810)
253. Jomaa H, Wiesner J, Sanderbrand S et al. Inhibitors of the nonmevalonate pathway of isoprenoid biosynthesis as antimalarial drugs. Science 285, 1573-1576 (1999). (Pubitemid 29420582)
254. Udeinya IJ, Brown N, Shu EN, Udeinya FI, Quakeyie I. Fractions of an antimalarial neem-leaf extract have activities superior to chloroquine, and are gametocytocidal. Ann. Trop. Med. Parasitol. 100(1), 17-22 (2006). (Pubitemid 43139628)
255. Baird JK. Effectiveness of antimalarial drugs. N. Engl. J. Med. 352, 1565-1577 (2005).
256. Tarun AS, Baer K, Dumpit RF et al. Quantitative isolation and in vivo imaging of malaria parasite liver stages. Int. J. Parasitol. 36, 1283-1293 (2006). (Pubitemid 44353485)
257. Sturm A, Sturm A, Amino R et al. Manipulation of host hepatocytes by the malaria parasite for delivery into liver sinusoids. Science 313, 1287-1290 (2006). (Pubitemid 44330952)
258. Amino R, Thiberge S, Shorte S, Frischknecht F, Ménard R. Quantitative imaging of Plasmodium transmission from mosquito to mammal. Nat. Med. 12, 220-224 (2006). (Pubitemid 43214749)
259. Gemma S, Campiani G, Butini S et al. Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials. J. Med. Chem. 52(2), 502-513 (2009).
260. Yeates CL, Batchelor JF, Capon EC et al. Synthesis and structure-activity relationships of 4-pyridones as potential antimalarials. J. Med. Chem. 3, 449-457 (2008).
261. Haynes RK, Fugmann B, Stetter J et al. Artemisone - a highly active antimalarial drug of the artemisinin class. Angew. Chem. Int. Ed. Engl. 45, 2082-2088 (2006). (Pubitemid 44105182)
262. 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. 43, 690-692 (1999). (Pubitemid 29109543)
263. Kotecka BM, Edstein MD, Rieckmann KH. Chloroquine bioassay of plasma specimens obtained from soldiers on chloroquine plus doxycycline for malaria prophylaxis. Int. J. Parasitol. 26, 1325-1329 (1996).
264. Watkins WM, Sixsmith DG, Spencer HC et al. Effectiveness of amodiaquine as treatment for chloroquine-resistant Plasmodium falciparum infections in Kenya. Lancet 1, 357-359 (1984).
265. Missinou MA, Borrmann S, Schindier A et al. Fosmidomycin for malaria. Lancet 360, 1941-1942 (2002).
266. Wiesner J, Henschker D, Hutchinson DB, Beck E, Jomaa H. In vitro and in vivo synergy of fosmidomycin, a novel antimalarial drug, with clindamycin. Antimicrob. Agents Chemother. 46, 1889-1894 (2002).
267. Neu HC, Kamimura T. Synergy of fosmidomycin (FR-31564) and other antimicrobial agents. Antimicrob. Agents Chemother. 22, 560-563 (1982). (Pubitemid 13206532)
268. Borrmann S, Adegnika AA, Matsiegui PB et al. Fosmidomycin-clindamycin for Plasmodium falciparum infections in African children. JID 189, 901-908 (2004). (Pubitemid 38328192)
269. Borrmann S, Lundgren I, Oyakhirome S et al. Fosmidomycin plus clindamycin for treatment of pediatric patients aged 1 to 14 years with Plasmodium falciparum malaria. Antimicrob. Agents Chemother. 50, 2713-2718 (2006). (Pubitemid 44198692)
270. Creek DJ, Charman WN, Chiu FCK et al. Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-troxolane antimalarials. Antimicrob. Agents Chemother. 4, 1291-1296 (2008).
271. Kreidenweiss A, Kremsner PG, Dietz K, Mordmüller B. In vitro activity of ferroquine (SAR97193) is independent of chloroquine resistance in Plasmodium falciparum. Am. J. Trop. Med. Hyg. 6, 1178-1181 (2006). (Pubitemid 351627504)
272. Kitjaroentham A, Suthiphongchai T, Wilairat P. Effect of metalloprotease inhibitors on invasion of red blood cell by Plasmodium falciparum. Acta Trop. 97(1), 5-9 (2006).
273. Dietmann A, Helbok R, Lackner P et al. Matrix metalloproteinases and their tissue inhibitors (TIMPs) in Plasmodium falciparum malaria: serum levels of TIMP-1 are associated with disease severity. JID 197, 1614-1620 (2008). (Pubitemid 351706493)
274. Andrews KT, Tran TN, Lucke AJ et al. Potent antimalarial activity of histone deacetylase inhibitor analogues. Antimicrob. Agents Chemother. 4, 1454-1461 (2008).
275. Mahmoudi N, Garcia-Domenech R, Galvezv J et al. New active drugs against liver stages of Plasmodium predicted by molecular topology. Antimicrob. Agents Chemother. 4, 1215-1220 (2008).
276. Bustos MD, Gay F, Diquet B. In vitro tests on Philippine isolates of Plasmodium falciparum against four standard antimalarials and four qinghaosu derivatives. Bull World Health Org. 72, 729-735 (1994). (Pubitemid 24344096)
277. Li Q, Xie LH, Johnson TO et al. Toxicity exaluation of artesunate and artelinate in Plasmodium berghei-infected and uninfected rats. Trans. R. Soc. Trop. Med. Hyg. Z 101(2), 104-112 (2007). (Pubitemid 44835337)
278. Kuzuyama T, Shizimu T, Takashi S, Seto H. Fosmidomycin, a specific inhibitor of 1-deoxy-d-xylulose 5-phosphate reductoisomerase in the nonmevalonate pathway of isoprenoid biosynthesis. Tetrahaedron Lett. 39, 7913-7916 (1998). (Pubitemid 28475040)
279. Rohmer M, Knani M, Simonin P, Sutter B, Sahm H. Isoprenoid biosynthesis in bacteria: a novel pathway for the early steps leading to isopentenyl diphosphate. Biochem. J. 295, 517-523 (1993). (Pubitemid 23315192)
280. Zeidler J, Schwender J, Mûller C et al. Inhibition of the non-mevalonate 1-deoxy-d- xylulose-5-phosphate pathway of plant isoprenoid biosynthesis by fosmidomycin. Z. Naturforsch. C53, 980-986 (1998). (Pubitemid 29064476)
281. Arribas J, Coodly L, Vollmer P, Kishimoto TK, Rose-John S, Massagué J. Diverse cell surface protein ectodomains are shed by a system sensitive to metalloprotease inhibitors. J. Biol. Chem. 271(19), 11376-11382 (1996) (Pubitemid 26155976)
282. Cary C, Lamont D, Dalton JP, Doerig C. Plasmodium falciparum chromatin: nucleosomal organisation and histone-like proteins. Parasitol. Res. 80, 255-258 (1994). (Pubitemid 24127031)
283. Cui L, Cui QFL, Miao J. Histone lysine methyltransferases and demethylases in the malaria parasite Plasmodium falciparum. Int. J. Parasitol. 38, 1083-1097 (2008).
284. Felsenfeld G, Groudine M. Controlling the double helix. Nature 421, 448-453 (2003).
285. Cui L, Miao J, Furuya T et al. Histone acetyltransferase inhibitor anacardic acid causes changes in global gene expression during in vitro Plasmodium falciparum development. Eukaryotic Cell 7(7), 1200-1210 (2008). (Pubitemid 351969334)
286. Vennerstrom JL, Arbe-Barnes S, Brun R et al. Identification of an antimalarial synthetic trioxolane drug development candidate. Nature 430, 900-904 (2004). (Pubitemid 39119218)
287. Haynes RK, Ho WY, Chan HW et al. Highly antimalaria-active artemisinin derivatives: biological activity does not correlate wit h chemical reactivity. Angew. Chem. Int. Ed. Engl. 43, 1381-1385 (2004).
288. Lambros C, Vanderberg JP. Synchronization of Plasmodium falciparum erythrocytic stages in culture. J. Parasitol. 65, 418-420 (1979). (Pubitemid 10222999)
289. Looareesuwan S, Viravan C, Webster HK, Kyle DE, Hutchinson DB, Canfield. CJ Clinical studies of atovaquone, alone or in combination with other antimalarial drugs, for treatment of acute uncomplicated malaria in Thailand. Am. J. Trop. Med. Hyg. 54, 62-66 (1996). (Pubitemid 26045736)
290. Fishwick J, McLean WG, Edwards G, Ward SA. The toxicity of artemisinin and related compounds on neuronal and glial cells in culture. Chem. Biol. Interact. 96, 263-271 (1995).
291. McLean WG, Ward SA. In vitro neurotoxicity of artemisinin derivatives. Med. Trop. 58(Suppl. 3), 28-31 (1998).
292. Wesche DL, DeCoster MA, Tortella FC, Brewer TG. Neurotoxicity of artemisinin analogs in vitro. Antimicrob. Agents Chemother. 38, 1813-1819 (1994).
293. Kamchonwongpaisan S, McKeever P, Hossler P, Ziffer H, Meshnick SR. Artemisinin neurotoxicity: neuropathology in rats and mechanistic studies in vitro. Am. J. Trop. Med. Hyg. 56(1), 7-12 (1997). (Pubitemid 27097951)
294. Hawkins VN, Joshi H, Rungsihirunrat K et al. Antifolates can have a role in the treatment of Plasmodium vivax. Trends Parasitol. 23, 213-222 (2007). (Pubitemid 46621225)
295. Rungsihirunrat K, Na-Bangchang K, Hawkins VN et al. Sensitivity to antifolates and genetic analysis of Plasmodium vivax isolates from Thailand. Am. J. Trop. Med. Hyg. 76, 1057-1065 (2007) (Pubitemid 351837866)
296. Hastings MD, Sibley CH. Pyrimethamine and WR99210 exert opposing selection on dihydrofolate reductase from Plasmodium vivax. Proc. Natl Acad. Sci. USA 99, 13-20 (2002).
297. Development project: Dihydroartemisinin (DHA)-piperaquine (Artekin® ). Medicines for Malaria Venture (MMV) www.mmv.org/pages/content-frame.asp