Products
Halofantrine was approved in 1988 and is now no longer available as a finished drug in many countries and many more. Halfan tablets (GlaxoSmithKline AG, 250 mg) are off the market.
Structure and properties
Halofantrine (C26H30Cl2F3NO, Mr = 500.4 g/mol) is a racemate and a halogenated phenanthrene derivative. It is also known as phenanthrene methanol. In pharmaceuticals, the active ingredient is present as halofantrine hydrochloride, a white powder that is practically insoluble in water.
Effects
Halofantrine (ATC P01BX01) has antiparasitic (blood schizontocidal) properties. It has a long half-life of up to ten days. The active metabolite -desbutylhalofantrine is involved in the effects.
Indications
For the treatment of mild to moderate malaria (, ).
Dosage
According to the SmPC. The drug is administered fasting.
Contraindications
Halofantrine is contraindicated in hypersensitivity, in congenital prolongation of the QT interval, and in combination with drugs that prolong the QT interval. For complete precautions, see the drug label.
Interactions
Drug-drug interactions have been described with drugs that prolong the QT interval. Halofantrine is a CYP substrate should not be combined with CYP3A inhibitors.
Adverse effects
The most common possible adverse effects include abdominal pain, diarrhea, dizziness, nausea, vomiting, cough, headache, pruritus, and muscle pain. Halofantrine may prolong the QT interval and rarely cause life-threatening cardiac arrhythmias. Deaths have been reported.