Thursday, February 15, 2018

Halofantrine - antimalarial drug and its therapeutic uses


DESCRIPTION:
Halofantrine is a drug used to treat malaria. It belongs to the phenthene class of compounds that include given and lumefantrine. Marketed as Halofan.
Halofantrine was developed at SRI  International for the Walter Reed Army Institute of Research from 1965 to1975 by a team led by medicinal chemist  “William Colwell”.

MECHANISM  OF ACTION :
Halofantrine is a synthetic antimalarial which acts as a blood schizonticide, and by the forming toxic complexes with  ferritporphyrin IX that  damage the membrane of the parasite.

PHARAMACOLOGY :
 Absorption :  Halafantarine  is erratic but is increased when taken with fatty food b because of fears of toxicity due to increased halofantrine blood levels, and it should be taken on an empty stomach.
Metabolism :  Hepatic
Half Life : 6-10 days
Protein binding : 60 -70%

 THERAPEUTIC USES:
Halofantrine is only used to treat malaria.

ADVERSE EFFECT:
Cardiotoxicity (due to damaging of heart  muscle , in which heart may not able to to pump blood through the body)

Cardiac arrthythmias  (due to abnormal automaticity or impaired conduction or both , or by altering electrophysiological properties of cardiac fibres , i.e ; any change or damaging in cardiac rhythm)
QT prolongation  ( it occurs due to premature action potentials during the late phases of         depolarization)
Diarrhoea (due to increase in peristalsis movement)
Abdominal pain
Rash ,headache, itching, and  vomiting

DRUG-DRUG  INTERACTION :
Ketoconzole + Halofantrine = It may decrease the effectiveness of halofantrine.
Cisapride, Clarithromycin, Droperidol + Halofantrine = Risk of side effect such as QT prolongation may be  increase.

REFERENCE
Tripathi KD, Essential of Medical Pharmacology ,7th edition, Page No. 831

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