Halofantrinum
Halofantrinum Uses, Dosage, Side Effects, Food Interaction and all others data.
Halofantrinum 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. Halofantrinum has been shown to preferentially block open and inactivated HERG channels leading to some degree of cardiotoxicity.
Halofantrinum is a synthetic antimalarial which acts as a blood schizonticide. It is effective against multi drug resistant (including mefloquine resistant) P. falciparum malaria.
| Trade Name | Halofantrinum |
| Availability | Discontinued |
| Generic | Halofantrine |
| Halofantrine Other Names | Halofantrina, Halofantrine, Halofantrinum |
| Related Drugs | doxycycline, clindamycin, hydroxychloroquine, Plaquenil, Cleocin |
| Type | |
| Formula | C26H30Cl2F3NO |
| Weight | Average: 500.424 Monoisotopic: 499.165654616 |
| Protein binding | 60-70%; |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Halofantrinum is an antimalarial used for the treatment of severe malaria.
For treatment of Severe malaria
How Halofantrinum works
The mechanism of action of Halofantrinum may be similar to that of chloroquine, quinine, and mefloquine; by forming toxic complexes with ferritoporphyrin IX that damage the membrane of the parasite.
Toxicity
Side effects incldue coughing noisy, rattling, troubled breathing, loss of appetite, aches and pain in joints, indigestion,and skin itching or rash.
Food Interaction
- Take on an empty stomach. Food increases the bioavailability 6-fold, which may increase the risk of cardiotoxicity.
[Major] GENERALLY AVOID: Grapefruit juice may increase the plasma concentration of halofantrine.
The mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits.
After administration of 500 mg with 250 mL regular-strength grapefruit juice daily for 3 days, average halofantrine AUC increased 2.8-fold and peak plasma concentrations increased 3.2-fold, compared to water, in healthy subjects (n=12).
QT interval prolongation increased from an average of 17 ms with water to 31 ms with grapefruit juice.
Halofantrinum, even at recommended doses, can cause dose-related prolongation of the QT interval, resulting in an elevated risk of potentially fatal ventricular arrhythmias including ventricular tachycardia and torsade de pointes.
ADJUST DOSING INTERVAL: The presence of food may increase the absorption and toxicity of halofantrine.
Peak plasma concentrations increased seven-fold and AUC increased three-fold in healthy subjects when halofantrine was administered with high-fat food.
MANAGEMENT: The authors of the study recommend that grapefruit juice be avoided during halofantrine therapy.
The manufacturer recommends performing an ECG before initiating halofantrine therapy and cardiac monitoring during and for 8 to 12 hours after completion of therapy.
Halofantrinum should be taken on an empty stomach at least 1 hour before or 2 hours after food.
Halofantrinum Drug Interaction
Unknown: amoxicillin / clavulanate, amoxicillin / clavulanate, glucose, glucose, acetaminophen, acetaminophen, tiotropium, tiotropium
Half Life
6-10 days
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