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Abstract
Halofantrine is a phenanthrene methanol antimalarial agent that possesses high activity against sensitive and resistant strains of Plasmodium falciparum. It is slowly and variably absorbed following oral administration and is thus usually administered by multiple oral dosing, given over 12 hours, in order to achieve therapeutic blood levels the feasibility of performing pharmacokinetic and bioavailability studies of halofantrine via the intramuscular (IM) route was investigated using a parenteral formulation under development.
Muscle damage following IM administration of halofantrine HCl formulated as a co-solvent system (dimetylacetamide and polyethylene glycol 400) was assessed in studies of the M. vastus lateralis of the rabbit.
Intramuscular injection of the co-solvent system produced little or no muscle damage; while the IM injection of the co-solvent fomulation of halofantrine produced a dose-related myotoxicity, including necrosis.
The severity of the myotoxic reaction observed in the rabbit muscle precludes the IM administration of this parenteral formulation of halofantrine-HCl.