Halofantrine
You don't need to be Editor-In-Chief to add or edit content to WikiDoc. You can begin to add to or edit text on this WikiDoc page by clicking on the edit button at the top of this page. Next enter or edit the information that you would like to appear here. Once you are done editing, scroll down and click the Save page button at the bottom of the page.
| Image:Halofantrine.svg | |
| Halofantrine
| |
| Systematic (IUPAC) name | |
| 3-dibutylamino-1-[1,3-dichloro-6-(trifluoromethyl) phenanthren-9-yl]-propan-1-ol | |
| 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. |
? |
| Legal status | |
| Routes | Oral |
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, New York: Lange Medical Books, 874–5. ISBN 0-07-141092-9.
Antiprotozoals: Antimalarial drugs (P01B) | |
|---|---|
| Aminoquinolines | 4-Aminoquinoline (Amodiaquine, Chloroquine, Hydroxychloroquine) • 8-Aminoquinoline (Pamaquine, Primaquine) |
| Methanolquinolines | Mefloquine • Quinine |
| Biguanides | Proguanil • Cycloguanil embolate |
| Diaminopyridines | Pyrimethamine |
| Artemisinin derivatives | Artemisinin • Artemether • Artesunate • Artenimol • Arteether/Artemotil |
| Others | Halofantrine • Lumefantrine |
 | This antimicrobial-related article is a stub. You can help Wikipedia by expanding it. |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
