Literature DB >> 7995326

Plasma concentrations of the enantiomers of halofantrine and its main metabolite in malaria patients.

F Gimenez1, C Gillotin, L K Basco, O Bouchaud, A F Aubry, I W Wainer, J Le Bras, R Farinotti.   

Abstract

The plasma concentrations of the enantiomers of halofantrine and its N-desbutyl metabolite in six patients with malaria were measured after oral administration of 3 x 750 mg doses of micronised, racemic halofantrine hydrochloride given at 6-hour intervals. Significant differences were observed between the plasma concentrations of the enantiomers both of halofantrine and its N-monodesbutyl metabolite. AUC(0)84h values were higher for (+)halofantrine (9917 micrograms.ml-1.h) than for (-)-halofantrine (6127 micrograms.ml-1.h). The clinical significance of these observations is not known. The isomers have equipotent activity in vitro but their relative toxicity has not yet been assessed.

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Year:  1994        PMID: 7995326     DOI: 10.1007/BF00196116

Source DB:  PubMed          Journal:  Eur J Clin Pharmacol        ISSN: 0031-6970            Impact factor:   2.953


  5 in total

1.  The determination of the enantiomers of halofantrine and monodesbutylhalofantrine in plasma and whole blood using sequential achiral/chiral high-performance liquid chromatography.

Authors:  F Gimenez; A F Aubry; R Farinotti; K Kirkland; I W Wainer
Journal:  J Pharm Biomed Anal       Date:  1992 Feb-Mar       Impact factor: 3.935

2.  In vitro activity of the enantiomers of mefloquine, halofantrine and enpiroline against Plasmodium falciparum.

Authors:  L K Basco; C Gillotin; F Gimenez; R Farinotti; J Le Bras
Journal:  Br J Clin Pharmacol       Date:  1992-05       Impact factor: 4.335

3.  Antimalarial activity in vitro of the N-desbutyl derivative of halofantrine.

Authors:  L K Basco; C Gillotin; F Gimenez; R Farinotti; J Le Bras
Journal:  Trans R Soc Trop Med Hyg       Date:  1992 Jan-Feb       Impact factor: 2.184

4.  Pharmacokinetics of halofantrine in healthy Thai volunteers.

Authors:  J Karbwang; S A Ward; K A Milton; K Na Bangchang; G Edwards
Journal:  Br J Clin Pharmacol       Date:  1991-11       Impact factor: 4.335

5.  Cardiac effect of halofantrine.

Authors:  J Karbwang; K Na Bangchang; D Bunnag; T Harinasuta; P Laothavorn
Journal:  Lancet       Date:  1993-08-21       Impact factor: 79.321

  5 in total
  6 in total

1.  The stereoselective distribution of halofantrine enantiomers within human, dog, and rat plasma lipoproteins.

Authors:  D R Brocks; M Ramaswamy; A I MacInnes; K M Wasan
Journal:  Pharm Res       Date:  2000-04       Impact factor: 4.200

2.  An investigation of the interaction between halofantrine, CYP2D6 and CYP3A4: studies with human liver microsomes and heterologous enzyme expression systems.

Authors:  R C Halliday; B C Jones; D A Smith; N R Kitteringham; B K Park
Journal:  Br J Clin Pharmacol       Date:  1995-10       Impact factor: 4.335

3.  Stereoselective halofantrine disposition and effect: concentration-related QTc prolongation.

Authors:  D R Abernethy; D L Wesche; J T Barbey; C Ohrt; S Mohanty; J C Pezzullo; B G Schuster
Journal:  Br J Clin Pharmacol       Date:  2001-03       Impact factor: 4.335

4.  X-ray crystal structure of the antimalarial agent (-)-halofantrine hydrochloride supports stereospecificity for cardiotoxicity.

Authors:  J M Karle
Journal:  Antimicrob Agents Chemother       Date:  1997-04       Impact factor: 5.191

5.  Effect of experimental hyperlipidaemia on the electrocardiographic effects of repeated doses of halofantrine in rats.

Authors:  Jigar P Patel; Dion R Brocks
Journal:  Br J Pharmacol       Date:  2010-11       Impact factor: 8.739

Review 6.  Stereoselectivity in the pharmacodynamics and pharmacokinetics of the chiral antimalarial drugs.

Authors:  Dion R Brocks; Reza Mehvar
Journal:  Clin Pharmacokinet       Date:  2003       Impact factor: 6.447

  6 in total

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