Lumefantrine
Mechanism :
The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. However, available data suggest that lumefantrine inhibits the formation of ß-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.
Indication :
- Malaria (used in combination with artemisinin derivatives as ACT)
Contraindications :
Hypersensitivity to drug/class/component.
Caution if severe renal or severe hepatic impairment, QT prolongation or QT prolongation family history, severe cardiac disease, arrhythmias, bradycardia or electrolyte abnormalities.
Dosing :
Artemether + Lumefantrin (Available as 20 mg of
artemether + 120 mg lumefantrine FDC or 40 mg of
artemether + 240 mg lumefantrine):
Oral therapy for 3 days
5-14 kg: 20 mg of
artemether + 120 mg of lumefantrine BID
15-24 kg: 40 mg of
artemether + 240 mg of lumefantrine BID
25-34 kg: 60 mg of
artemether + 360 mg of lumefantrine BID
>35 kg: 80 mg of
artemether + 480 mg of lumefantrine BID
Adverse Effect :
Serious Reactions: Hypersensitivity reaction, QT prolongation, bullous dermatitis.
Common Reactions: Headache, myalgia, anorexia, dizziness, asthenia, arthralgia/myalgia,
nausea, fever, chills, rigors, sleep disorders, palpitations, vomiting, abdominal pain, fatigue, hepatomegaly, splenomegaly, diarrhea, cough, insomnia, anemia, malaise, pruritus, rash, vertigo. Elevated AST.
Interaction :
Contraindicated:
Cisapride, Dronedarone, Mifepristone, Pimozide, Ranolazine, Thioridazine, Toremifene.
Avoid/Use Alternative:
Alfuzosin, Amiodarone, Apomorphine, Arsenic Trioxide, Asenapine, Azithromycin, Bedaquiline, Boceprevir, Chloroquine, Chlorpromazine, Ciprofloxacin, Citalopram, Clarithromycin, Clozapine, Cobicistat, Conivaptan, Crizotinib, Dabrafenib, Dasatinib, Degarelix, Disopyramide, Dofetilide, Dolasetron, Dolutegravir, Droperidol, Ephedra, Ephedrine, Eribulin, Erythromycin, Escitalopram, Flecainide, Fluconazole, Fluphenazine, Fluvoxamine, Gemifloxacin, Goserelin, Granisetron, Haloperidol, Histrelin, Ibutilide, Iloperidone, Ixabepilone, Lapatinib, Leuprolide, Levofloxacin, Lopinavir/Ritonavir, Mefloquine, Methadone, Moxifloxacin, Nilotinib, Norfloxacin, Ofloxacin, Ondansetron, Paliperidone, Pasireotide, Pazopanib, Pentamidine, Perphenazine, Posaconazole, Procainamide, Prochlorperazine, Promethazine, Propafenone, Quetiapine, Quinidine (Antiarrhythmic), Quinidine (CYP2D6 Booster), Quinine, Rilpivirine, Romidepsin, Saquinavir, Simeprevir, Solifenacin, Sorafenib, Sotalol, Sunitinib, Tacrolimus, Telaprevir, Telavancin, Telithromycin, Temsirolimus, Tetrabenazine, Tolvaptan, Trazodone, Trifluoperazine, Triptorelin, Vandetanib, Vardenafil, Vemurafenib, Venlafaxine, Voriconazole, Ziprasidone.
Hepatic Dose :
Dosage adjustments are not recommended in mild or moderate impairment. Use caution in severe impairment.