Atovaquone/proguanil: A review of its use for the prophylaxis of Plasmodium falciparum malaria

Drugs

Volumn 63, Issue 6, 2003, Pages 597-623

  McKeage, Kate ^a   Scott, Lesley J ^a   Borrmann, S ^b   De Vries, P J ^c   Hutchinson, D B A ^h   Looareesuwan, S ^d   Nosten, F ^e   Price, R ^f   Shanks, G D ^g  

^a ADIS INTERNATIONAL LIMITED   (New Zealand)

^b Institute of Tropical Medicine   (Germany)

^c Division of Infectious Diseases   (Netherlands)

^d MAHIDOL UNIVERSITY   (Thailand)

^e SHOKLO MALARIA RESEARCH UNIT   (Thailand)

^f MENZIES SCHOOL OF HEALTH RESEARCH   (Australia)

^g ARMED FORCES RESEARCH INSTITUTE OF MEDICAL SCIENCES   (Thailand)

^h NONE

Author keywords

[No Author keywords available]

Indexed keywords

ATOVAQUONE; ATOVAQUONE PLUS PROGUANIL; CHLOROQUINE; CYCLOGUANIL; CYTOCHROME P450; DOXYCYCLINE; MEFLOQUINE; METOCLOPRAMIDE; PLACEBO; PROGUANIL; RIFABUTIN; RIFAMPICIN; TETRACYCLINE;

ABDOMINAL PAIN; ANTIBIOTIC RESISTANCE; ANXIETY; BODY WEIGHT; BREAST FEEDING; CLINICAL TRIAL; COMPARATIVE STUDY; CROSS RESISTANCE; DEPRESSION; DIARRHEA; DISEASE SEVERITY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CONTRAINDICATION; DRUG EFFECT; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENTIATION; DRUG PROTEIN BINDING; DRUG SOLUBILITY; DRUG TOLERABILITY; ELECTRON TRANSPORT; ENDEMIC DISEASE; GASTROINTESTINAL SYMPTOM; HEADACHE; HUMAN; IC 50; INSOMNIA; KIDNEY DYSFUNCTION; MALARIA FALCIPARUM; MEGALOBLASTIC ANEMIA; MITOCHONDRION; MOTHER; MOUTH ULCER; NAUSEA; NEUROPSYCHIATRY; NONHUMAN; PANCYTOPENIA; PARASITE DEVELOPMENT; PARASITEMIA; PLASMODIUM FALCIPARUM; PREGNANCY; PROPHYLAXIS; PRURITUS; REVIEW; RISK; SIDE EFFECT; TABLET FORMULATION; VERTIGO; VISUAL IMPAIRMENT; VIVID DREAM; VOMITING;

ANIMALS; ANTIMALARIALS; ATOVAQUONE; CHLOROGUANIDE; CLINICAL TRIALS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG COMBINATIONS; HUMANS; MALARIA, FALCIPARUM; NAPHTHOQUINONES; TRAVEL;

PLASMODIUM FALCIPARUM; PROTOZOA;

EID: 0037243541     PISSN: 00126667     EISSN: None     Source Type: Journal    
DOI: 10.2165/00003495-200363060-00006     Document Type: Review

References (71)

1. Kain KC. Prophylactic drugs for malaria: why do we need another one? J Travel Med 1999; 6 Suppl. 1: S2-7
2. Bradley DJ, Bannister B. Guidelines for malaria prevention in travellers from the United Kingdom for 2001. Advisory Committee on Malaria Prevention for UK Travellers. Commun Dis Public Health 2001; 4 (2): 84-101
3. Goodyear L. Malaria. Pharm J 2000; 264: 405-10
4. Kain KC, Shanks GD, Keystone JS. Malaria chemoprophylaxis in the age of drug resistance. I. Currently recommended drug regimens. Clin Infect Dis 2001; 33 (2): 226-34
5. Palmer KJ, Holliday SM, Brogden RN. Mefloquine: a review of its antimalarial activity, pharmacokinetic properties and therapeutic efficacy. Drugs 1993; 45 (3): 430-75
6. Baird JK, Hoffman L. Prevention of malaria in travelers. Travel Medicine 1999; 83 (4): 923-44
7. Fry M, Pudney M. Site of action of the antimalarial hydroxynaphthoquinone, 2-[trans-4-(4′-chlorophenyl) cyclohexyl]-3-hydroxy-1, 4-naphthoquinone (566C80). Biochem Pharmacol 1992; 43 (7): 1545-53
8. Spencer CM, Goa KL. Atavaquone: a review of its pharmacological properties and therapeutic efficacy in opportunistic infections. Drugs 1995; 50 (1): 176-96
9. Hudson AT, Dickins M, Ginger CD, et al. 566C80: a potent broad spectrum anti-infective agent with activity against malaria and opportunistic infections in AIDS patients. Drugs Exptl Clin Res 1991; 17 (9): 427-35
10. Basco LK, Ramiliarisoa O, Le Bras J. In vitro activity of atovaquone against the African isolates and clones of Plasmodium falciparum Am J Trop Med Hyg 1995; 53 (4): 388-91
11. Gay F, Bustos D, Traore B, et al. In vitro response of Plasmodium falciparum to atovaquone and correlation with other antimalarials: comparison between African and Asian strains. Am J Trop Med Hyg 1997; 56 (3): 315-7
12. Davies CS, Suhrbier AS, Winger L.A., et al. Improved techniques for the culture of the liver stages of Plasmodium berghei and their relevance to the study of causal prophylactic drugs. Acta Leiden 1989; 58 (2): 97-113
13. Davies CS, Pudney M, Matthews PJ, et al. The causal prophylactic activity of the novel hydroxynaphthoquinone 566C80 against Plasmodium berghei infections in rats. Acta Leiden 1989: 58 (2): 115-28
14. Shapiro TA, Ranasinha CD, Kumar N, et al. Prophylactic activity of atovaquone against Plasmodium falciparum in humans. Am J Trop Med Hyg 1999: 60 (5): 831-6
15. Watkins WM, Sixsmith DG, Chulay JD. The activity of proguanil and its metabolites, cycloguanil and p-chlorophenylbiguanide, against Plasmodium falciparum in vitro. Ann Trop Med Parasitol 1984; 78 (3): 273-8
16. Srivastava IK, Vaidya AB. A mechanism for the synergistic antimalarial action of atovaquone and proguanil. Antimicrob Agents Chemother 1999 Jun: 43 (6): 1334-9
17. Canfield CJ, Pudney M, Gutteridge WE. Interactions of atovaquone with other antimalarial drugs against Plasmodium falciparum in vitro. Exp Parasitol 1995 May; 80: 373-81
18. Enosse S, Butcher GA, Margos G, et al. The mosquito transmission of malaria: the effects of atovaquone-proguanil (Malarone) and chloroquine. Trans R Soc Trop Med Hyg 2000 Jan; 94 (1): 77-82
19. Berman JD, Nielsen R, Chulay JD, et al. Causal prophylactic efficacy of atovaquone-proguanil (Malarone) in a human challenge model. Trans R Soc Trop Med Hyg 2001 Jul; 95 (4): 429-32
20. GlaxoSmithKline. Malarone: US Prescribing Information [online]. Available from URL: http://www.gsk.com [Accessed 2002 Oct 10]
21. Winstanley PA, Ward SA, Snow RW. Clinical status and implications of antimalarial drug resistance. Microbes Infect 2002 Feb; 4 (2): 157-64
22. White NJ. Drug resistance in malaria. Br Med Bull 1998; 54 (3): 703-15
23. Vaidya AB, Mather MW. Atovaquone resistance in malaria parasites. Drug Resist Update 2000; 3 (5): 283-7
24. Korsinczky M, Chen N, Kotecka B, et al. Mutations in Plasmodium falciparum cytochrome b that are associated with atovaquone resistance are located at a putative drug-binding site. Antimicrob Agents Chemother 2000 Aug: 44 (8): 2100-8
25. Looareesuwan S, Viravan C, Webster HK, et al. 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 1996; 54 (1): 62-6
26. Foote SJ, Galatis D, Cowman AF. Amino acids in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum involved in cycloguanil resistance differ from those involved in pyrimethamine resistance. Proc Natl Acad Sci USA 1990; 87: 3014-7
27. Khan B, Omar S, Kanyara JN, et al. Antifolate drug resistance and point mutations in Plasmodium falciparum in Kenya. Trans R Soc Trop Med Hyg 1997; 91: 456-60
28. Peterson DS, Walliker D, Wellems TE. Evidence that a point mutation in dihydrofolate reductase-thymidylate synthase confers resistance to pyrimethamine in falciparum malaria. Proc Natl Acad Sci USA 1988; 85: 9114-8
29. Fidock DA, Wellems TE. Transformation with human dihydrofolate reductase renders malaria parasites insensitive to WR99210 but does not affect the intrinsic activity of proguanil. Proc Natl Acad Sci USA 1997; 94: 10931-6
30. Shanks GD, Gordon DM, Klotz FW, et al. Efficacy and safety of atovaquone/proguanil as suppressive prophylaxis for Plasmodium falciparum malaria. Clin Infect Dis 1998 Sep; 27 (3): 494-9
31. Fivelman QL, Butcher GA, Adagu IS, et al. Malarone treatment failure and in vitro confirmation of resistance of Plasmodium falciparum isolate from Lagos, Nigeria. Malaria J 2002; 1 (1): 1-3
32. Thapar MM, Ashton M, Lindegardh N, et al. Time-dependent pharmacokinetics and drug metabolism of atovaquone plus proguanil (Malarone) when taken as chemoprophylaxis. Eur J Clin Pharmacol 2002 Apr; 58 (1): 19-27
33. Beerahee M, Clarke P, Overbosch D, et al. Prophylaxis with Malarone (atovaquone and proguanil hydrochloride) in non-immune subjects 65 years of age and older [poster]. Proceedings of Third European Conference on Travel Medicine; 2002 May 15-18; Florence
34. Sabchareon A, Attanath P, Phanuaksook P, et al. Efficacy and pharmacokinetics of atovaquone and proguanil in children with multidrug-resistant Plasmodium falciparum malaria. Trans R Soc Trop Med Hyg 1998; 92: 201-6
35. Hussein Z, Eaves J, Hutchinson DB, et al. Population pharmacokinetics of atovaquone in patients with acute malaria caused by Plasmodium falciparum. Clin Pharmacol Ther 1997; 61 (5): 518-30
36. Rolan PE, Mercer AJ, Weatherley BC. et al. Examination of some factors responsible for a food-induced increase in absorption of atovaquone. Br J Clin Pharmac 1994; 37: 13-20
37. Beerahee M. Clinical pharmacology of atovaquone and proguanil hydrochloride. J Travel Med 1999; 6 Suppl. 1: S13-7
38. GlaxoSmithKline. Malarone: atovaquone/proguanil hydrochloride [product monograph]. United Kingdom: GlaxoSmithKline. 2001 Jul
39. Hughes WT, Kennedy W, Shenep JL, et al. Safety and pharmacokinetics of 566C80, a hydroxynaphthoquinone with anti-Pneumocystis carinii activity: a phase I study in human immunodeficieny virus (HIV)-infected men. J Infect Dis 1991; 163 (4): 843-8
40. Hussein Z, Eaves CJ, Hutchinson DB, et al. Population pharmacokinetics of proguanil in patients with acute P. falciparum malaria after combined therapy with atovaquone. Br J Clin Pharmacol 1996 Nov; 42: 589-97
41. Wattanagoon Y, Taylor RB, Moody RR, et al. Single dose pharmacokinetics of proguanil and its metabolites in healthy subjects. Br J Clin Pharmacol 1987; 24: 775-80
42. Gillotin C, Mamet JP, Veronese L. Lack of a pharmacokinetic interaction between atovaquone and proguanil. Eur J Clin Pharmacol 1999 Jun; 55 (4): 311-5
43. Helsby NA, Edwards G, Breckenridge A.M., et al. The multiple dose pharmacokinetics of proguanil. Br J Clin Pharmacol 1993; 35: 653-6
44. Funck-Brentano C, Becquemont L, Leneveu A, et al. Inhibition by omeprazole of proguanil metabolism: mechanism of the interaction in vitro and prediction of in vivo results from the in vitro experiments. J Pharmacol Exp Ther 1997; 280 (2): 730-8
45. Birkett DJ, Rees D, Andersson T, et al. In vitro proguanil activation to cycloguanil by human liver microsomes is mediated by CYP3A isoforms as well as by S-mephenytoin hydroxylase. Br J Clin Pharmac 1994; 37:413-20
46. Helsby NA, Ward SA, Edwards G, et al. The pharmacokinetics and activation of proguanil in man: consequences of variability in drug metabolism. Br J Clin Pharmacol 1990; 30 (4): 593-8
47. Edstein MD, Yeo AET, Kyle DE, et al. Proguanil polymorphism does not affect the antimalarial activity of proguanil combined with atovaquone in vitro. Trans R Soc Trop Med Hyg 1996 Jul; 90: 418-21
48. Looareesuwan S, Chulay JD, Canfield CJ, et al. Malarone (atovaquone and proguanil hydrochloride): a review of its clinical development for treatment of malaria. Am J Trop Med Hyg 1999; 60 (4): 533-41
49. van Vugt M, Edstein MD, Proux S, et al. Absence of an interaction between artesunate and atovaquone - proguanil. Eur J Clin Pharmacol 1999 Aug; 55 (6): 469-74
50. Høgh B, Clarke PD, Camus D, et al. Atovaquone-proguanil versus chloroquine-proguanil for malaria prophylaxis in non-immune travellers: a randomised, double-blind study. Malarone International Study Team. Lancet 2000 Dec 2; (9245): 1888-94
51. Overbosch D, Schilthuis H, Bienzle U, et al. Atovaquone-proguanil versus mefloquine for malaria prophylaxis in nonimmune travelers: results from a randomized, double-blind study. Clin Infect Dis 2001 Oct 1; 33 (7): 1015-21
52. Camus D, Malvy D, Schilthuis H, et al. Atovaquone/proguanil versus chloroquine/proguanil or mefloquine in clinical trials of non-immune paediatric travellers 11-40kg [poster]. Proceedings of Third European Conference on Travel Medicine; 2002 May 15-18; Florence
53. Nasveld PE, Edstein MD, Kitchener SJ, et al. Comparison of the effectiveness of atovaquone/proguanil combination and doxycycline in the chemoprophylaxis of malaria in Australian Defence Force personnel [abstract no. 16]. Am J Trop Med Hyg 2000; 62 (3): 139
54. van der Berg JD, Duvenage CSJ, Roskell NS, et al. Safety and efficacy of atovaquone and proguanil hydrochloride for the prophylaxis of Plasmodium falciparum malaria in South Africa. Clin Ther 1999; 21 (4): 741-9
55. Ling J, Baird JK, Fryauff DJ, et al. Randomized, placebo-controlled trial of atovaquone/proguanil for the prevention of Plasmodium falciparum or Plasmodium vivax malaria among migrants to Papua, Indonesia. Clin Infect Dis 2002 Oct 1; 35 (7): 825-33
56. Sukwa TY, Mulenga M, Chisdaka N, et al. A randomized, double-blind, placebo-controlled field trial to determine the efficacy and safety of Malarone (atovaquone/proguanil) for the prophylaxis of malaria in Zambia. Am J Trop Med Hyg 1999 Apr; 60 (4): 521-5
57. Lell B, Luckner D, Ndjave M, et al. Randomised placebo-controlled study of atovaquone plus proguanil for malaria prophylaxis in children. Lancet 1998; 351 (9104): 709-13
58. White NJ. The development of immunity to malaria (a clinical view). Asian Pac J Allergy Immunol 1993; 11: 1-3
59. Nosten F. Prophylactic effect of Malarone against malaria: all good news? Lancet 2000 Dec 2; 356 (9245): 1864-5
60. Boots M, Phillips M, Curtis JR. Megaloblastic anemia and pancytopenia due to proguanil in patients with chronic renal failure. Clin Nephrol 1982; 18 (2): 106-8
61. Sirsat RA, Dasgupta A. Haematological complications of proguanil in a patient with chronic renal failure. Nephron 1997; 75: 108
62. van Riemsdijk MM, Sturkenboom MCJM, Ditters JM, et al. Atovaquone plus chloroguanide versus mefloquine for malaria prophylaxis: a focus on neuropsychiatric adverse events. Clin Pharmacol Ther 2002; 72 (3): 294-301
63. GlaxoSmithKline. Malarone: UK Prescribing Information [online]. Available from URL: http://www.gsk.com [Accessed 2002 Apr 5]
64. Vidal. Malarone [online]. Available from URL: http://www.vidalpro.net [Accessed 2003 Feb 20]
65. World Health Organization. International travel and health [online]. Available from URL: http://www.who/ith [Accessed 2002 Jun 19]
66. Olukayode Oyediran ABO, Heisler MH. Malarone™ donation program. J Travel Med 1999; 6 Suppl. 1: S28-30
67. Nosten F, Brasseur P. Combination therapy for malaria: the way forward? Drugs 2002; 62 (9): 1315-29
68. Ryan ET, Kain KC. Primary care: health advice and immunizations for travelers. N Engl J Med 2000; 342 (23): 1716-25
69. Luxemburger C, Nosten F, Ter Kuiile F, et al. Mefloquine for multidrug-resistant malaria [letter]. Lancet 1991; 338: 1268
70. The Cheshire Medical Center. Doxycycline (Vibramycin) [online]. Available from URL: www.cheshire-med.com/services/pharm [Accessed 2002 Sep 2]
71. Centers for Disease Control and Prevention. Travellers Health [online]. Available from URL: http://www.cdc.gov [Accessed 2002 Sep 2]