Description

Simple

A medication used to treat severe malaria.

Clinical

An antimalarial used for the treatment of severe malaria.

Overview

Halofantrine is an antimalarial. It belongs to the phenanthrene class of compounds that includes quinine and lumefantrine. It appears to inhibit polymerisation of heme molecules (by the parasite enzyme "heme polymerase"), resulting in the parasite being poisoned by its own waste. Halofantrine has been shown to preferentially block open and inactivated HERG channels leading to some degree of cardiotoxicity.

Pharmacology

Indication

For treatment of Severe malaria

Pharmacodynamic

Halofantrine is a synthetic antimalarial which acts as a blood schizonticide. It is effective against multi drug resistant (including mefloquine resistant) P. falciparum malaria.

Mechanism of action

The mechanism of action of Halofantrine may be similar to that of chloroquine, quinine, and mefloquine; by forming toxic complexes with ferritoporphyrin IX that damage the membrane of the parasite.

Absorption

Information currently not available.

Protein binding

60-70%;

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

6-10 days

Route of elimination

Information currently not available.

Toxicity

Side effects incldue coughing noisy, rattling, troubled breathing, loss of appetite, aches and pain in joints, indigestion,and skin itching or rash.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

  • Take on an empty stomach. Food increases the bioavailability 6-fold, which may increase the risk of cardiotoxicity.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Halofantrine.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Halofantrine.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Halofantrine.
5-methoxy-N,N-dimethyltryptamine
The metabolism of 5-methoxy-N,N-dimethyltryptamine can be decreased when combined with Halofantrine.
7-Nitroindazole
The therapeutic efficacy of 7-Nitroindazole can be decreased when used in combination with Halofantrine.
Abatacept
The metabolism of Halofantrine can be increased when combined with Abatacept.
Abexinostat
The risk or severity of QTc prolongation can be increased when Abexinostat is combined with Halofantrine.
Abiraterone
The metabolism of Halofantrine can be decreased when combined with Abiraterone.
Acalabrutinib
The metabolism of Halofantrine can be decreased when combined with Acalabrutinib.
Acebutolol
The metabolism of Acebutolol can be decreased when combined with Halofantrine.
Acepromazine
The risk or severity of QTc prolongation can be increased when Halofantrine is combined with Acepromazine.
Aceprometazine
The risk or severity of QTc prolongation can be increased when Halofantrine is combined with Aceprometazine.
Acetaminophen
The metabolism of Acetaminophen can be decreased when combined with Halofantrine.
Acetazolamide
The therapeutic efficacy of Acetazolamide can be decreased when used in combination with Halofantrine.
Acetophenazine
The risk or severity of QTc prolongation can be increased when Halofantrine is combined with Acetophenazine.
Acetylcysteine zinc
Acetylcysteine zinc can cause a decrease in the absorption of Halofantrine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetyldigoxin
The risk or severity of QTc prolongation can be increased when Acetyldigoxin is combined with Halofantrine.
Acrivastine
The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Halofantrine.
Adalimumab
The metabolism of Halofantrine can be increased when combined with Adalimumab.
Adenosine
The risk or severity of QTc prolongation can be increased when Adenosine is combined with Halofantrine.