Drug information of Halofantrine

Mechanism of effect

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. It appears to inhibit polymerisation of heme molecules (by the parasite enzyme "heme polymerase"), resulting in the parasite being poisoned by its own waste.

Pharmacodynamic

Halofantrine has been shown to preferentially block open and inactivated HERG channels leading to some degree of cardiotoxicity.

Pharmacokinetics

Protein binding: 60-70%;

Metabolism: Hepatic

Metabolite: N-debutylhalofantrine

Half life: 6-10 days

Dosage

Usual Adult Dose for Malaria

Mild to moderate Plasmodium falciparum and Plasmodium vivax malaria:
Nonimmune patients: 500 mg orally every 6 hours for 3 doses; repeat course in 7 days.

Semi-immune patients: 500 mg orally every 6 hours for 3 doses.

Usual Pediatric Dose for Malaria

Mild to moderate Plasmodium falciparum and Plasmodium vivax malaria:

<18 years, <40 kg: 8 mg/kg orally every 6 hours for 3 doses. Repeat course in 7 days if patient is nonimmune.

<18 years, >=40 kg:
Nonimmune patients: 500 mg orally every 6 hours for 3 doses; repeat course in 7 days.

Semi-immune patients: 500 mg orally every 6 hours for 3 doses

Side effects

Diarrhea , Headache , nausea , abdominal pain , vomiting , vertigo , myalgia , itching

Interactions

Promazine , Abiraterone , Vasopressin , Atomoxetine , Amitriptyline , Amiodarone , Aprepitant , Epirubicin , Adenosine , vemurafenib , Typhoid vaccine (live), oral , lofexidine , conivaptan , bosutinib , Bepridil , Pasireotide , bedaquiline , levomethadyl acetate , glasdegib , Ceritinib , Nilutamide , Methenamine , norfloxacin , Romidepsin , Deutetrabenazine , Cabozantinib , Rucaparib , Troleandomycin , Lomefloxacin , gilteritinib , Foscarnet , encorafenib , midostaurin , Triclabendazole , ivosidenib , Telavancin , ezogabine , Isavuconazonium , Iloperidone , Perflutren , Pimavanserin , Degarelix , Triflupromazine , Terfenadine , Asenapine , Alfuzosin , Paliperidone , Pazopanib , Dolutegravir , Gatifloxacin , Grepafloxacin , Mibefradil , cobicistat , Delavirdine , Lumefantrine / artemether , Arsenic trioxide , Efavirenz , EMTRICITABINE , Telaprevir , lumacaftor and Ivacaftor , Goserelin , Anagrelide , Idelalisib , Ivacaftor , probucol , Trandolapril , Ribociclib , Dofetilide , Ibutilide , Eribulin , Inotuzumab‎ , Idarubicin , Indinavir , Mesoridazine , Procainamide , Polyethylene glycol , Mefloquine , Panobinostat , Droperidol , Halothane , Osimertinib , Quinine , Chloroquine , sparfloxacin , Palonosetron , dasabuvir , vandetanib , Lopinavir , Telithromycin , boceprevir , valbenazine , Amprenavir , Fosamprenavir , Ivabradine , Mifepristone , Dolasetron , ritonavir , saquinavir , nelfinavir , Mirtazapine , paritaprevir , primaquine , propoxyphene , protriptyline , meperidine , Nefazodone , ISOPROTERENOL , dronedarone , Metaproterenol , Prochlorperazine , Quinidine , Amoxapine , Ziprasidone , Histrelin , Pentamidine , Quetiapine , lithium , Buprenorphine , Toremifene , Tamoxifen , Leuprolide acetate , escitalopram , Clofazimine , Ranolazine , Darunavir , astemizole , Clomipramine , Solifenacin , Enzalutamide , Flecainide , Bicalutamide , ritodrine , Voriconazole , Ketoconazole , Clarithromycin , Chlorpromazine , Clotrimazole , Clozapine , Nilotinib , Haloperidol , Hydroxychloroquine , Vardenafil , Verapamil , Venlafaxine , Granisetron , Lapatinib , Letrozole , Methadone , Moxifloxacin , Nortriptyline , Flutamide , Fluphenazine , Fluvoxamine , Fluoxetine , Fluconazole , Fingolimod , Sotalol , Sorafenib , Sevoflurane , Ciprofloxacin , Cisapride , Cyclosporine , Diltiazem , Risperidone , Zafirlukast , Sunitinib , Cimetidine , Sertraline , Daunorubicin , Danazol , Desipramine , Doxepin , Doxorubicin , Disopyramide , Terbutaline , Triptorelin , Trimipramine , Tenofovir , Thioridazine , Gemifloxacin , Posaconazole , Pimozide , Tacrolimus , Tetrabenazine , Trazodone , Tramadol , Imatinib , Imipramine , Papaverine , perphenazine , Propafenone , Promethazine , Erythromycin , Ofloxacin , Oxaliplatin , Ondansetron , Itraconazole , Isoniazid , Amisulpride , lenvatinib , oleandomycin , Dasatinib , voxelotor , tucatinib

Alerts

Heart problems, especially abnormal heartbeat or

Thiamine deficiency or

Unexplained sudden fainting—These conditions increase the chance of side effects affecting the heart, including fast irregular heartbeat

Points of recommendation

Halofantrine is best taken on an empty stomach to decrease the chance of side effects.

To help clear up your infection completely, take halofantrine exactly as directed by your doctor for the full time of treatment. Your symptoms may come back if you stop your treatment too early.

It is important that your doctor check your progress after treatment. This is to make sure that the infection is cleared up completely, and to allow your doctor to check for any unwanted effects.

If your symptoms do not improve after you have taken halofantrine for the full course of treatment, or if they become worse, check with your doctor.

Pregnancy level

Group c - Not adequate studies in pregnant women

Related drugs

Hydroxychloroquine , primaquine , Quinine , Chloroquine , Mefloquine