The efficacy of antifolate antimalarial combinations in Africa: A predictive model based on pharmacodynamic and pharmacokinetic analyses

Parasitology Today

Volumn 13, Issue 12, 1997, Pages 459-464

  Watkins, W M ^a,b   Mberu, Eddy K ^a,b   Winstanley, Peter A ^d   Plowe, Chris V ^c  

^a KENYA MEDICAL RESEARCH INSTITUTE   (Kenya)

^b KEMRI WELLCOME TRUST RESEARCH PROGRAMME   (Kenya)

^c UNIVERSITY OF MARYLAND SCHOOL OF MEDICINE   (United States)

^d NONE

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMALARIAL AGENT; CHLOROQUINE; CHLORPROGUANIL; DAPSONE; DIHYDROFOLATE REDUCTASE; FANSIDAR; FOLIC ACID ANTAGONIST; PYRIMETHAMINE; SULFADOXINE;

AFRICA; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG PROTEIN BINDING; DRUG RESISTANCE; HYPOTHESIS; MALARIA CONTROL; PHARMACODYNAMICS; PHARMACOKINETICS; PLASMODIUM FALCIPARUM; REVIEW;

PLASMODIUM FALCIPARUM;

EID: 0030813699     PISSN: 01694758     EISSN: None     Source Type: Journal    
DOI: 10.1016/s0169-4758(97)01124-1     Document Type: Review

References (54)

1. Peters, W. (1970) Chemotherapy and Drug Resistance in Malaria, Academic Press
2. World Health Organization (1973) Chemotherapy of malaria and resistance to antimalarials. Tech. Rep. Series 529, 48-49
3. Ferone, R. (1977) Folate metabolism in malaria. Bull. WHO 55, 291-298
4. Sherman, I.W. (1979) Biochemistry of Plasmodium (malarial parasites). Microbiol. Rev. 43, 453-495
5. Krungkrai, J., Webster, J.K. and Yuthavong, Y. (1989) De novo and salvage biosynthesis of pteroylpentaglutamates in the human malaria parasite Plasmodium falciparum. Mol. Biochem. Parasitol. 32, 25-38
6. Watkins, W.M. et al. (1985) Antagonism of sulfadoxine and pyrimethamine antimalarial activity in vitro by p-aminobenzoic acid, p-aminobenzoylglutamic acid and folic acid. Mol. Biochem. Parasitol. 14, 55-61
7. Chulay, J.D., Watkins, W.M. and Sixsmith, D.G. (1984) Synergistic antimalarial activity of pyrimethamine and sulfadoxine against Plasmodium falciparum in vitro. Am. J. Trop. Med. Hyg. 33, 325-330
8. Milhous, W.K. et al. (1985) In vitro activities of and mechanisms of resistance to antifolate antimalarial drugs. Antimicrob. Agents Chemother. 27, 525-530
9. Hewlett, P.S. (1969) Measurement of the potencies of drug mixtures. Biometrics 25, 477-487
10. Chou, T.C. and Talalay, P. (1977) A simple generalised equation for the analysis of multiple inhibitions of Michaelis-Menten kinetic systems. J. Biol. Chem. 252, 6438-6442
11. Berenbaum, M.C. (1978) A method for testing synergy with any number of agents. J. Infect. Dis. 137, 122-130
12. Dieckmann, A. and Jung, A. (1986) Stage-specific sensitivity of Plasmodium falciparum to antifolates. Z. Parasitenkd. 72, 591-594
13. Watkins, W.M., Woodrow, C. and Marsh, K. (1993) Falciparum malaria: differential effects of antimalarial drugs on ex vivo parasite viability during the critical early phase of therapy. Am. J. Trop. Med. Hyg. 49, 106-112
14. White, N.J. and Krishna, S. (1989) Treatment of malaria: some considerations and limitations of the current methods of assessment. Trans. R. Soc. Trop. Med. Hyg. 83, 767-777
15. Wernsdorfer, W.H. (1984) Drug resistant malaria. Endeavour 8, 166-171
16. Watkins, W.M. and Mosobo, M. (1993) Treatment of Plasmodium falciparum malaria with pyrimethamine-sulfadoxine: selective pressure for resistance is a function of long elimination half life. Trans. R. Soc. Trop. Med. Hyg. 87, 75-78
17. Peterson, D.S., Milhous, W.K. and Wellems, T.E. (1990) Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria. Proc. Natl. Acad. Sci. U. S. A. 87, 3018-3022
18. Peterson, D.S. et al. (1991) Prevalence of the dihydrofolate reductase Asn-108 mutation as the basis for pyrimethamine-resistant falciparum malaria in the Brazilian Amazon. Am. J. Trop. Med. Hyg. 45, 492-497
19. Hyde, J.E. (1989) Point mutations and pyrimethamine resistance in Plasmodium falciparum. Parasitol. Today 5, 252-255
20. Peterson, D.S., Walliker, D. and Wellems, T.E. (1988) Evidence that a point mutation in dihydrofolate reductase-thymidylate synthase confers resistance to pyrimethamine in falciparum malaria. Proc. Natl. Acad. Sci. U. S. A. 85, 9114-9118
21. Zolg, J.W. et al. (1989) Point mutations in the dihydrofolate reductase-thymidylate synthase gene as the molecular basis for pyrimethamine resistance in Plasmodium falciparum. Mol. Biochem. Parasitol. 36, 253-262
22. Cowman, A.F. et al. (1988) Amino acid changes linked to pyrimethamine resistance in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum. Proc. Natl. Acad. Sci. U. S. A. 85, 9109-9113
23. Foote, S.J., Galatis, D. and Cowman, A.F. (1990) 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. U. S. A. 87, 3014-3017
24. Wu, Y., Kirkman, L.A. and Wellems, T.E. (1996) Transformation of Plasmodium falciparum malaria parasites by homologous integration of plasmids that confer resistance to pyrimethamine. Proc. Natl. Acad. Sci. U. S. A. 93, 1130-1134
25. Brooks, R. et al. (1994) Sequence variation of the hydroxymethyldihydropterin pyrophosphokinase: dihydropteroate synthase gene in lines of the human malaria parasite Plasmodium falciparum with differing resistance to sulfadoxine. Eur. J. Biochem. 224, 397-405
26. Desjardins, R.E. et al. (1979) Quantitative assessment of antimalarial activity by a semi-automated microdilution technique. Antimicrob. Agents Chemother. 16, 710-718
27. Winstanley, P.A. et al. (1992) The disposition of oral and intramuscular pyrimethamine/sulfadoxine in Kenyan children with high parasitaemia but clinically non-severe falciparum malaria. Br. J. Clin. Pharmacol. 33, 143-148
28. Winstanley, P.A. et al. (1995) In vitro activities of novel antifolate drug combinations against Plasmodium falciparum and human granulocyte CFUs. Antimicrob. Agents Chemother. 39, 948-952
29. Sixsmith, D.G. et al. (1984) In vitro antimalarial activity of tetrahydrofolate dehydrogenase inhibitors. Am. J. Trop. Med. Hyg. 33, 772-776
30. Watkins, W.M. et al. (1987) In vitro susceptibility of Plasmodium falciparum isolates from Jilore, Kenya, to antimalarial drugs. Am. J. Trop. Med. Hyg. 37, 445-451
31. Winstanley, P.A. and Watkins, W.M. (1992) Pharmacology and parasitology: integrating experimental methods and approaches to falciparum malaria. Br. J. Clin. Pharmacol. 33, 575-581
32. World Health Organization (1984) Advances in malaria chemotherapy. Tech. Rep. Series 711, 99
33. Martindale, (1978) The Extra Pharmacopoeia (27th edn), Pharmaceutical Press
34. Lamont, G. and Darlow, B. (1982) Comparison of in vitro pyrimethamine assays and in vivo response to sulfadoxine-pyrimethamine in Plasmodium falciparum from Papua New Guinea. Trans. R. Soc. Trop. Med. Hyg. 76, 797-799
35. Spencer, H.C. et al. (1984) A new in vitro test for pyrimethamine/sulfadoxine susceptibility of Plasmodium falciparum and its correlation with in vivo resistance in Kenya. Bull. WHO 62, 615-621
36. Schapira, A. et al. (1986) The susceptibility of Plasmodium falciparum to sulfadoxine and pyrimethamine: correlation of in vivo and in vitro results. Am. J. Trop. Med. Hyg. 35, 239-245
37. Spencer, H.C. et al. (1986) Response of Plasmodium falciparum to dihydrofolate reductase inhibitors in Malindi, Kenya. Trans. R. Soc. Trop. Med. Hyg. 80, 201-203
38. Schapira, A. and Schwalbach, J. (1988) Evaluation of four therapeutic regimens for falciparum malaria in Mozambique. Bull. WHO 66, 219-226
39. Nguyen-Dinh, P. et al. (1982) Susceptibility of Plasmodium falciparum to pyrimethamine and sulfadoxine/pyrimethamine in Kisumu, Kenya. Lancet i, 823-825
40. Watkins, W.M. et al. (1988) The changing response of Plasmodium falciparum to antimalarial drugs in East Africa. Trans. R. Soc. Trop. Med. Hyg. 82, 21-26
41. Winstanley, P.A. et al. (1997) Chlorproguanil-dapsone for uncomplicated falciparum malaria in young children: pharmacokinetics and therapeutic range. Trans. R. Soc. Trop. Med. Hyg. 91, 322-327
42. Wilairatana, P. et al. (1997) Poor efficacy of antimalarial biguanide-dapsone combinations in the treatment of acute, uncomplicated, falciparum malaria in Thailand. Ann. Trop. Med. Parasitol. 91, 125-132
43. Trigg, J.K. et al. (1997) Resistance to pyrimethamine-sulfadoxine in Plasmodium falciparum in 12 villages in North East Tanzania and a test of chlorproguanil-dapsone. Acta Trop. 63, 185-189
44. Bjorkman, A. and Phillips-Howard, P.A. (1991) Adverse reactions to sulfa drugs: implications for malaria chemotherapy. Bull. WHO 69, 297-304
45. Gordin, F.M. et al. (1984) Adverse reactions to trimethoprim-sulfamethoxazole in patients with the acquired immunodeficiency syndrome. Ann. Intern. Med. 100, 495-499
46. Snewin, V.A. et al. (1991) Polymorphism of the alleles of the merozoite surface antigens MSA1 and MSA2 in Plasmodium falciparum wild isolates from Colombia. Biochem. Parasitol. 49, 265-275
47. Paul, R.E. et al. (1995) Mating patterns in malaria parasite populations of Papua New Guinea. Science 269, 1709-1711
48. Thaithong, S. et al. (1984) Clonal diversity in a single isolate of the malaria parasite Plasmodium falciparum. Trans. R. Soc. Trop. Med. Hyg. 78, 242-245
49. Plowe, C.V. et al. (1995) Pyrimethamine and proguanil resistance-conferring mutations in Plasmodium falciparum dihydrofolate reductase: polymerase chain reaction methods for surveillance in Africa. Am. J. Trop. Med. Hyg. 52, 565-568
50. Centers for Disease Control (1985) Revised recommendations for preventing malaria in travellers to areas with chloroquine-resistant Plasmodium falciparum. Morb. Mortal. Wkly Rep. 34, 185-195
51. Brandling-Bennett, A.D. et al. (1988) Chloroquine treatment of falciparum malaria in an area of Kenya of intermediate chloroquine resistance. Trans. R. Soc. Trop. Med. Hyg. 82, 833-837
52. Pasvol, G. et al. (1991) Quinine treatment of severe falciparum malaria in African children: a randomised comparison of three regimens. Am. J. Trop. Med. Hyg. 45, 702-713
53. Hurwitz, E.S., Johnson, D. and Campbell, C. (1981) Resistance of Plasmodium falciparum to sulfadoxine-pyrimethamine (Fansidar) in a refugee camp in Thailand. Lancet i, 1068-1070
54. Johnson, D.E., Roendej, P. and Williams, R.G. (1982) Falciparum malaria acquired in the area of the Thai-Khmer border resistant to treatment with Fansidar. Am. J. Trop. Med. Hyg. 31, 907-912