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Halofantrine

 
Drug Info: Halofantrine

Brand names: Halfan®

Chemical formula:



Halofantrine tablets

What are halofantrine tablets?

HALOFANTRINE (Halfan®) is an antimalarial agent. Halofantrine treats malarial infection, which is transmitted by the bite of a mosquito. Because halofantrine may cause serious side effects, it is only used to treat malarial infections in areas where it is known that other medicines may not work. Halofantrine should not be prescribed for the self-treatment of malaria. Generic halofantrine tablets are not available.

NOTE: This drug is discontinued in the United States.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• chronic diarrhea
• dehydrated
• loss of appetite, poor eating habits, or an eating disorder like anorexia or bulimia
• heart disease
• heart rhythm problems
• history of low levels of calcium, potassium, or magnesium
• kidney disease
• liver disease
• other chronic illness
• vomiting
• an unusual or allergic reaction to halofantrine, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take halofantrine tablets by mouth. Follow the directions on the prescription label. Halofantrine should only be taken on an empty stomach with a full glass (8 ounces or 240 ml) of water. Do not take halofantrine with grapefruit juice. Take you doses at regular intervals and on the same day of the week. Do not take your medicine more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What drug(s) may interact with halofantrine?

• antacids
• arsenic trioxide
astemizole
bepridil
cimetidine
cisapride
diltiazem
• diuretics (water pills)
dolasetron
droperidol
• food
halothane
imatinib, STI-571
levomethadyl
• local anesthetics
• medicines for treating heart-rhythm problems (examples: amiodarone, disopyramide, dofetilide, procainamide, quinidine, sotalol)
mefloquine
nicardipine
pentamidine
probucol
quinine
• some antibiotics (examples: clarithromycin, erythromycin, gatifloxacin, grepafloxacin, levofloxacin, moxifloxacin, sparfloxacin, troleandomycin)
• some medicines for treating fungal or yeast infections (fluconazole, itraconazole, ketoconazole, voriconazole)
• some medicines for treating HIV or AIDS infection
• some medicines for treating depression or mental illness
• some medicines for treating cancer (daunorubicin, doxorubicin)
terfenadine
verapamil
zafirlukast
zileuton

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking halofantrine?

If you are taking mefloquine or have taken mefloquine in the past 3 weeks, you should not take halofantrine. Dangerous heart side effects may occur. Talk to your health care provider.

If you get a fever during or after you start taking halofantrine, do not treat yourself. Contact your healthcare provider immediately.

Tell your prescriber or health care professional if your symptoms do not improve in a few days.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that requires mental alertness until you know how halofantrine affects you. To reduce the risk of dizzy or fainting spells, do not sit or stand up quickly.

While in areas where malaria is common, certain steps can be taken to prevent being bit by mosquitoes. They include:
1) Stay in air-conditioned or well-screened rooms to reduce mosquito contact.
2) Sleep under mosquito netting (preferably has a pyrethrum insecticide).
3) Wear long-sleeved shirts and long trousers to protect arms and legs.
4) Apply mosquito repellents containing DEET to uncovered areas of skin.
5) Use a pyrethrum-containing flying insect spray to kill mosquitoes.

What side effects may I notice from taking halofantrine?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• fainting spells
• fever or chills
• chest pain
• palpitations
• severe diarrhea
• severe vomiting
• shortness of breath
• slow, fast or irregular heartbeat

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• fatigue
• headache
• nausea
• stomach pain

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open. It is important to keep halofantrine out of reach of children; overdose is very dangerous.

Store at controlled room temperature between 20 and 25 degrees C (68 and 77 degrees F) and protect from light. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Wikipedia: Halofantrine
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Halofantrine
Systematic (IUPAC) name
3-dibutylamino-1-[1,3-dichloro-6-(trifluoromethyl)
phenanthren-9-yl]-propan-1-ol
Identifiers
CAS number 69756-53-2
ATC code P01BX01
PubChem 37393
DrugBank APRD00419
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. Halofantrine's structure contains a substituted phenanthrene, and is related to the antimalarial drugs quinine and lumefantrine. Marketed as Halfan, halofantrine is never used to prevent malaria and its mode of action is unknown.

Contents

Adverse reactions

Halofantrine can cause abdominal pain, diarrhoea, vomiting, rash, headache, itching and elevated liver enzymes.

It can be associated with cardiotoxicity.[1] The most dangerous side effect is cardiac arrhythmias: halofantrine causes significant QT prolongation,[2] 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

  1. ^ Wesche DL, Schuster BG, Wang WX, Woosley RL (May 2000). "Mechanism of cardiotoxicity of halofantrine". Clin. Pharmacol. Ther. 67 (5): 521–9. doi:10.1067/mcp.2000.106127. PMID 10824631. 
  2. ^ 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:10.1007/s00210-004-0995-5. PMID 15558243. 

 
 
Learn More
Halofantrine tablets
Malaria: Treatment
Mefloquine Hydrochloride Oral tablet

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