Arteether is a semi-synthetic derivative of artemisinin, a potent antimalarial agent isolated from the plant Artemisia annua. It is a fast-acting blood schizontocide specifically indicated for the treatment of severe and complicated Plasmodium falciparum malaria, including cerebral malaria. In the Indian context, it is a critical component of the national malaria control program's arsenal against drug-resistant malaria, particularly in regions with high P. falciparum burden. It is administered via intramuscular injection, ensuring reliable delivery in critically ill patients who cannot take oral medication.
Adult: 3.2 mg/kg body weight intramuscularly on Day 1, followed by 1.6 mg/kg body weight intramuscularly on Days 2 and 3. Total course: 3 days. Maximum single dose should not exceed 150mg (one vial).
Note: For DEEP INTRAMUSCULAR INJECTION only. Do not administer intravenously or subcutaneously. Use a 2 ml vial. The oil-based formulation requires aspiration before injection to avoid intravascular administration. Administer in the upper outer quadrant of the gluteal region or the anterolateral thigh. Rotate injection sites. The solution is viscous; use a sufficiently wide-bore needle (e.g., 21-23G).
Arteether's antimalarial activity is mediated by its endoperoxide bridge. Inside the infected erythrocyte, the iron-rich environment (heme from hemoglobin digestion) catalyzes the cleavage of this bridge, generating reactive oxygen species (ROS) and carbon-centered free radicals. These highly reactive intermediates alkylate and damage specific parasite proteins (including PfATP6, a SERCA-type calcium ATPase), inhibit nucleic acid and protein synthesis, and cause oxidative stress, leading to rapid parasite death.
Pregnancy: CONTRANDICATED in the first trimester due to evidence of embryolethality in animal studies. In second and third trimesters, use only for life-threatening severe malaria if no safer alternative exists (WHO category: Not recommended in first trimester; use with caution in later trimesters). The benefit of treating severe malaria outweighs potential risk.
Driving: Dizziness may occur; patients should be cautioned against driving or operating machinery until they know how the drug affects them, especially during the acute treatment phase.
| Other QT-prolonging drugs (e.g., Antiarrhythmics, Macrolides, Fluoroquinolones) | Additive risk of cardiac arrhythmias, including Torsades de Pointes. | Major |
| Enzyme Inducers (e.g., Rifampicin, Phenytoin, Carbamazepine, St. John's Wort) | May increase metabolism of Arteether, reducing its plasma concentration and efficacy. | Moderate |
| Enzyme Inhibitors (e.g., Ketoconazole, Itraconazole, Ritonavir) | May decrease metabolism of Arteether, potentially increasing plasma levels and risk of toxicity. | Moderate |
| Mefloquine | Concomitant use may increase risk of neurotoxicity (based on animal data). Administer sequentially; WHO recommends Arteether first. | Moderate |