Halofantrine
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Halofantrine
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| Systematic (IUPAC) name | |
| 3-dibutylamino-1-[1,3-dichloro-6-(trifluoromethyl) phenanthren-9-yl]-propan-1-ol |
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| Identifiers | |
| CAS number | |
| ATC code | P01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C26H30Cl2F3NO |
| Mol. mass | 500.423 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 60 to 70% |
| Metabolism | Hepatic (CYP3A4-mediated) |
| Half life | 6 to 10 days |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | Oral |
Halofantrine is a drug used to treat malaria. Halofantrine's structure contains a substituted phenanthrene, and is related to the antimalarial drugs quinine and lumefantrine. Halofantrine is never used to prevent malaria and its mode of action is unknown.
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[edit] 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,[1] 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.
[edit] 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.
[edit] 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.
[edit] Dosing
- Adult dose: Three doses of 500 mg six hours apart.
Halofantrine should be taken on an empty stomach.
[edit] 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.
[edit] References
- ^ Sánchez-Chapula JA, Navarro-Polanco RA, Sanguinetti MC (2004). "Block of wild-type and inactivation-deficient human ether-a-go-go-related gene K+ channels by halofantrine". Naunyn Schmiedebergs Arch. Pharmacol. 370 (6): 484–91. doi:. PMID 15558243.
- Rosenthal, Philip J. (2004). "Antiprotozoal drugs", in Katzung BG.: Basic & Clinical Pharmacology, 9, New York: Lange Medical Books, 874–5. ISBN 0-07-141092-9.
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