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Chemical Compound Review

Halfan     3-(dibutylamino)-1-[1,3- dichloro-6...

Synonyms: Halofantrina, Halofantrine, Halofantrino, Halofantrinum, CHEMBL1107, ...
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Disease relevance of AIDS008015


Psychiatry related information on AIDS008015

  • A dose of 9.6 ng/chick halofantrine induced amnesia at the beginning of a protein synthesis-dependent long-term memory stage, the last of three stages of memory postulated to underly memory formation in the chick following passive avoidance learning [6].

High impact information on AIDS008015

  • Efficacy of low-dose halofantrine for second treatment of uncomplicated falciparum malaria [7].
  • We compared the following antimalarial drugs in relation to subsequent Plasmodium falciparum gametocyte carriage: mefloquine, halofantrine, quinine, and the artemisinin derivatives [8].
  • In-vitro chemosensitivity tests showed that most infections were due to chloroquine-resistant parasites, and that parasite maturation was inhibited by considerably lower concentrations of halofantrine than of chloroquine [9].
  • Concomitant with the increase in mefloquine resistance was a corresponding increase in the level of resistance to halofantrine and quinine, suggesting a true multidrug-resistance phenotype [10].
  • BACKGROUND: Halofantrine, an antimalarial drug that prolongs the QT interval, is metabolized into N-debutyl-halofantrine by cytochrome P450 (CYP) 3A4 [11].

Chemical compound and disease context of AIDS008015


Biological context of AIDS008015

  • Plasma pharmacokinetics of halofantrine and N-debutyl-halofantrine and QTc interval duration were studied during the following 168 hours [11].
  • Halofantrine peak plasma concentrations and bioavailability on the first day of treatment were significantly lower in patients with malaria than in healthy volunteers [17].
  • RESULTS: Compared with water, grapefruit juice increased halofantrine area under the plasma concentration versus time curve (AUC) and peak plasma concentration by 2.8-fold +/- 1.5-fold (P <.0001) and 3.2-fold +/- 1.3-fold (P <.0001), respectively [11].
  • Using a ventricular action potential voltage clamp protocol, halofantrine and N-desbutylhalofantrine block of HERG current was greatest during phases 2 and 3 of the action potential waveform [18].
  • The change in heart rate became significant after administration of 10 mg kg(-1) halofantrine (-23+/-9 beats min[-1]) whereas the increase in QTc was significant with only 1 mg kg(-1) halofantrine (22+/-10 ms) [19].

Anatomical context of AIDS008015

  • Halofantrine produced a stereoselective block of the delayed rectifier potassium channel in isolated feline myocytes [4].
  • Grapefruit juice increases the bioavailability of several orally administered CYP3A4 substrates by inhibiting CYP3A4 at the enterocyte level and could therefore increase the risk of halofantrine-induced QT interval prolongation [11].
  • We here report on the effect of various 4-aminoquinolines, as well as pyronaridine, halofantrine and some bis-quinolines, on glutathione-mediated destruction of FP in aqueous solution, when FP was bound non-specifically to a protein, and when it was dissolved in human erythrocyte ghost membranes [20].
  • 5. The results of these experiments suggest that any direct effects that halofantrine may have had on the effective refractory period of cardiac muscle cannot be separated from those of the vehicle [19].
  • 4 In guinea-pig left papillary muscles the effective refractory period was increased significantly 60 min after addition of halofantrine; from 161+/-4 to 173+/-6 ms with 10 microM, 156+/-8 to 174+/-6 ms with 30 microM and 165+/-6 to 179+/-5 ms with 100 microM halofantrine [19].

Associations of AIDS008015 with other chemical compounds


Gene context of AIDS008015


Analytical, diagnostic and therapeutic context of AIDS008015


  1. Halofantrine to prevent falciparum malaria on return from malarious areas. Baudon, D., Bernard, J., Moulia-Pelat, J.P., Martet, G., Sarrouy, J., Touze, J.E., Spiegel, A., Lantrade, P., Picq, J.J. Lancet (1990) [Pubmed]
  2. Halofantrine and pruritus. Hallwood, P.M., Horton, R.J., O'Sullivan, K.M., Parr, S.N. Lancet (1989) [Pubmed]
  3. Blackwater fever after halofantrine. Orlando, G., Isabella, L., Atzori, C., Cargnel, A. Lancet (1996) [Pubmed]
  4. Mechanism of cardiotoxicity of halofantrine. Wesche, D.L., Schuster, B.G., Wang, W.X., Woosley, R.L. Clin. Pharmacol. Ther. (2000) [Pubmed]
  5. Food-drug interactions. Schmidt, L.E., Dalhoff, K. Drugs (2002) [Pubmed]
  6. Inhibitors of cAMP-dependent protein kinase impair long-term memory formation in day-old chicks. Zhao, W.Q., Polya, G.M., Wang, B.H., Gibbs, M.E., Sedman, G.L., Ng, K.T. Neurobiology of learning and memory. (1995) [Pubmed]
  7. Efficacy of low-dose halofantrine for second treatment of uncomplicated falciparum malaria. Touze, J.E., Perret, J.L., Nicolas, X., Fourcade, L., Bernard, J., Keundjian, A., Soares, J.M., Doury, J.C. Lancet (1997) [Pubmed]
  8. Effects of artemisinin derivatives on malaria transmissibility. Price, R.N., Nosten, F., Luxemburger, C., ter Kuile, F.O., Paiphun, L., Chongsuphajaisiddhi, T., White, N.J. Lancet (1996) [Pubmed]
  9. Efficacy of multiple-dose halofantrine in treatment of chloroquine-resistant falciparum malaria in children in Kenya. Watkins, W.M., Oloo, J.A., Lury, J.D., Mosoba, M., Kariuki, D., Mjomba, M., Koech, D.K., Gilles, H.M. Lancet (1988) [Pubmed]
  10. Selection for mefloquine resistance in Plasmodium falciparum is linked to amplification of the pfmdr1 gene and cross-resistance to halofantrine and quinine. Cowman, A.F., Galatis, D., Thompson, J.K. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  11. Pharmacokinetic and pharmacodynamic interaction between grapefruit juice and halofantrine. Charbit, B., Becquemont, L., Lepère, B., Peytavin, G., Funck-Brentano, C. Clin. Pharmacol. Ther. (2002) [Pubmed]
  12. Cardiac effects of antimalarial treatment with halofantrine. Nosten, F., ter Kuile, F.O., Luxemburger, C., Woodrow, C., Kyle, D.E., Chongsuphajaisiddhi, T., White, N.J. Lancet (1993) [Pubmed]
  13. Efficacy and pharmacokinetics of intravenous nanocapsule formulations of halofantrine in Plasmodium berghei-infected mice. Mosqueira, V.C., Loiseau, P.M., Bories, C., Legrand, P., Devissaguet, J.P., Barratt, G. Antimicrob. Agents Chemother. (2004) [Pubmed]
  14. Halofantrine. A review of its antimalarial activity, pharmacokinetic properties and therapeutic potential. Bryson, H.M., Goa, K.L. Drugs (1992) [Pubmed]
  15. Postexposure administration of halofantrine for the prevention of malaria. Shanks, G.D., Edstein, M.D., Kereu, R.K., Spicer, P.E., Rieckmann, K.H. Clin. Infect. Dis. (1993) [Pubmed]
  16. Proarrhythmic potential of halofantrine, terfenadine and clofilium in a modified in vivo model of torsade de pointes. Batey, A.J., Coker, S.J. Br. J. Pharmacol. (2002) [Pubmed]
  17. Pharmacokinetics of an extended-dose halofantrine regimen in patients with malaria and in healthy volunteers. Ohrt, C., Watt, G., Teja-Isavadharm, P., Keeratithakul, D., Loesuttiviboon, L., Webster, H.K., Schuster, B., Fleckenstein, L. Clin. Pharmacol. Ther. (1995) [Pubmed]
  18. The anti-malarial drug halofantrine and its metabolite N-desbutylhalofantrine block HERG potassium channels. Mbai, M., Rajamani, S., January, C.T. Cardiovasc. Res. (2002) [Pubmed]
  19. Comparison of the acute cardiotoxicity of the antimalarial drug halofantrine in vitro and in vivo in anaesthetized guinea-pigs. Batey, A.J., Lightbown, I.D., Lambert, J.P., Edwards, G., Coker, S.J. Br. J. Pharmacol. (1997) [Pubmed]
  20. Kinetics of inhibition of glutathione-mediated degradation of ferriprotoporphyrin IX by antimalarial drugs. Famin, O., Krugliak, M., Ginsburg, H. Biochem. Pharmacol. (1999) [Pubmed]
  21. In vitro culture and drug sensitivity assay of Plasmodium falciparum with nonserum substitute and acute-phase sera. Ringwald, P., Meche, F.S., Bickii, J., Basco, L.K. J. Clin. Microbiol. (1999) [Pubmed]
  22. An improved high-performance liquid chromatographic method for the simultaneous measurement of halofantrine and desbutylhalofantrine in human serum. Keeratithakul, D., Teja-Isavadharm, P., Shanks, G.D., Webster, H.K., Edstein, M.D. Therapeutic drug monitoring. (1991) [Pubmed]
  23. Urban malaria in Dakar, Senegal: chemosusceptibility and genetic diversity of Plasmodium falciparum isolates. Henry, M., Diallo, I., Bordes, J., Ka, S., Pradines, B., Diatta, B., M'Baye, P.S., Sane, M., Thiam, M., Gueye, P.M., Wade, B., Touze, J.E., Debonne, J.M., Rogier, C., Fusai, T. Am. J. Trop. Med. Hyg. (2006) [Pubmed]
  24. Inhibition of hERG K+ currents by antimalarial drugs in stably transfected HEK293 cells. Traebert, M., Dumotier, B., Meister, L., Hoffmann, P., Dominguez-Estevez, M., Suter, W. Eur. J. Pharmacol. (2004) [Pubmed]
  25. In vitro susceptibility of African isolates of Plasmodium falciparum from Gabon to pyronaridine. Pradines, B., Mabika Mamfoumbi, M., Parzy, D., Owono Medang, M., Lebeau, C., Mourou Mbina, J.R., Doury, J.C., Kombila, M. Am. J. Trop. Med. Hyg. (1999) [Pubmed]
  26. An investigation of the interaction between halofantrine, CYP2D6 and CYP3A4: studies with human liver microsomes and heterologous enzyme expression systems. Halliday, R.C., Jones, B.C., Smith, D.A., Kitteringham, N.R., Park, B.K. British journal of clinical pharmacology. (1995) [Pubmed]
  27. Interactions of the antimalarial drug mefloquine with the human cardiac potassium channels KvLQT1/minK and HERG. Kang, J., Chen, X.L., Wang, L., Rampe, D. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  28. Effect of the antimalarial drug halofantrine in the long QT syndrome due to a mutation of the cardiac sodium channel gene SCN5A. Piippo, K., Holmström, S., Swan, H., Viitasalo, M., Raatikka, M., Toivonen, L., Kontula, K. Am. J. Cardiol. (2001) [Pubmed]
  29. Interference by antimalarial drugs with the in-vitro production of reactive nitrogen intermediates by murine macrophages. Kremsner, P.G., Neifer, S., Rasenack, T., Bienzle, U. J. Antimicrob. Chemother. (1993) [Pubmed]
  30. Clinical pharmacokinetics of halofantrine. Karbwang, J., Na Bangchang, K. Clinical pharmacokinetics. (1994) [Pubmed]
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