Halofantrine

Source: Wikipedia, the free encyclopedia.
Not to be confused with the Halfan culture.
Halofantrine
Clinical data
Trade namesHalfan
AHFS/Drugs.comConsumer Drug Information
MedlinePlusa603030
Routes of
administration		Oral
ATC code
Pharmacokinetic data
Protein binding60–70%
MetabolismHepatic (CYP3A4-mediated)
Elimination half-life6–10 days
Identifiers
  • 3-(Dibutylamino)-1-[1,3-dichloro-6-(trifluoromethyl)-9-phenanthryl]-1-propanol
JSmol)
  • FC(F)(F)c3ccc2c(cc1c(Cl)cc(Cl)cc1c2c3)C(O)CCN(CCCC)CCCC
  • InChI=1S/C26H30Cl2F3NO/c1-3-5-10-32(11-6-4-2)12-9-25(33)23-16-22-21(14-18(27)15-24(22)28)20-13-17(26(29,30)31)7-8-19(20)23/h7-8,13-16,25,33H,3-6,9-12H2,1-2H3 checkY
  • Key:FOHHNHSLJDZUGQ-UHFFFAOYSA-N checkY
  (verify)

Halofantrine is a drug used to treat

haemoglobin degrading enzyme unique to the malarial parasites.[2]

Halofantrine was developed at SRI International for the Walter Reed Army Institute of Research from 1965 to 1975 by a team led by medicinal chemist William Colwell.[3]

Adverse reactions

Halofantrine can cause abdominal pain,

diarrhoea
, vomiting, rash, headache, itching and elevated liver enzymes.

It can be associated with

QT prolongation,[5] 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. A survey from 2009 suggests that the drug is safe when correctly administered.[6]

Other adverse reactions

Consumption of grapefruit combined with certain medications can cause serious side effects, even death. Halofantrine combined with this fruit or grapefruit juice is dangerous. The mechanism of action is inhibition of CYP3A4, which is necessary to metabolize the drug and eliminate it from the body. Without CYP3A4, levels of the drug will become toxic in the body.

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 course of treatment (6 tablets) costs US$
1.40 in the developing world. Halofantrine is not available in the UK or U.S.

References

  1. PMID 18508124
    .
  2. S2CID 14642593. Archived from the original
    (PDF) on 2020-08-07. Retrieved 2019-04-08.
  3. ISBN 978-0974520810
    .
  4. S2CID 23780132
    .
  5. S2CID 1948028
    .
  6. PMID 20003315
    .
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