Halofantrine

Halofantrine

File:Halofantrine.svg
Clinical data
Routes of administration	Oral
ATC code	P01BX01 (WHO)
Pharmacokinetic data
Protein binding	60 to 70%
Metabolism	Hepatic (CYP3A4-mediated)
Elimination half-life	6 to 10 days
Identifiers
IUPAC name 3-dibutylamino-1-[1,3-dichloro-6-(trifluoromethyl) phenanthren-9-yl]-propan-1-ol
CAS Number	69756-53-2
PubChem CID	37393
DrugBank	APRD00419
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C26H30Cl2F3NO
Molar mass	500.423 g/mol

Halofantrine is a drug used to treat malaria. It belongs to the phenanthrene class of compounds that includes quinine and lumefantrine. It is never used to prevent malaria. Its mode of action is unknown.

Adverse reactions

Halofantrine can cause abdominal pain, diarrhoea, vomiting, rash, headache, itching and elevated liver enzymes. The most dangerous side effect is cardiac arrhythmias: halofantrine causes significant QT prolongation, and this effect is seen even at standard doses. The drug should therefore not be given to patients with cardiac conduction defects and should not be combined with mefloquine.

Pharmacology

The mechanism of action of halofantrine is unknown. The absorption of halofantrine is erratic, but is increased when taken with fatty food. Because of fears of toxicity due to increased halofantrine blood levels, halofantrine should be taken on an empty stomach.

Plasma levels peak at 16 hours and the half-life of the drug is about 4 days.

Uses

Halofantrine is only used to treat malaria. It is not used to prevent malaria (prophylaxis) because of the risk of toxicity and unreliable absorption.

Dosing

• Adult dose: Three doses of 500 mg six hours apart.

Halofantrine should be taken on an empty stomach.

Manufacturing information and availability

• Halfan (GlaxoSmithKline) is available as 250 mg tablets. A full treatment cost (6 tablets) costs US$1.40 in the developing world. Halofantrine is not available in the UK or U.S.

References

• Rosenthal, Philip J. (2004). "Antiprotozoal drugs". In Katzung BG. Basic & Clinical Pharmacology (9 ed.). New York: Lange Medical Books. pp. 874&ndash, 5. ISBN 0-07-141092-9.