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arteether

Sesquiterpine lactone · Antimalarial

Sesquiterpine lactoneAntimalarialATC P01BE05
CDSCO approvedATC P01BE05
EXCRETION
not curated
INTERACTIONS
2 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • RifampicinSevereDatabase
  • RitonavirSevereDatabase

Mechanism

Arteether is an artemisinin derivative. The endoperoxide bridge in its molecule interacts with heme in the parasite, causing ferrous iron-mediated cleavage and release of highly reactive free radical species. These free radicals bind to membrane proteins, cause lipid peroxidation, damage endoplasmic reticulum, and ultimately result in lysis of the parasite. It is a potent and rapid blood schizontocide.

Indications

severe and complicated falciparum malaria (parenteral, used only in India)Complicated malaria (i.m. administration only to adults)Severe and complicated falciparum malaria (i.m., preferred over quinine)

Dosing

Adult
Severe/complicated falciparum (IM): 3.2 mg/kg on day 1, followed by 1.6 mg/kg daily for the next 4 days (switch to 3-day oral ACT when possible).

Pharmacokinetics

Onset
fastest
Peak effect
short
Half-life
23 hours (elimination)

Pregnancy & lactation

Lactation

Safety not yet proven in 1st trimester of pregnancy.

Drug interactions

Rifampicin
Severe
Database

Rifampicin is a potent inducer of CYP3A4, the primary enzyme responsible for arteether metabolism. Co-administration can significantly decrease arteether plasma concentrations, leading to reduced efficacy and potential treatment failure for malaria.

Avoid concomitant use. If rifampicin is essential, consider alternative antimalarial treatments or closely monitor for treatment failure and consider increasing arteether dose if clinically appropriate and safe, though this is not well-studied.

Ritonavir
Severe
Database

Ritonavir is a potent inhibitor of CYP3A4. Co-administration can significantly increase arteether plasma concentrations, potentially leading to increased risk of dose-dependent adverse effects, including cardiotoxicity (QT prolongation) and neurotoxicity.

Avoid concomitant use if possible. If co-administration is unavoidable, consider reducing the arteether dose and closely monitor for adverse effects, including ECG changes and neurological symptoms. Therapeutic drug monitoring for arteether, if available, would be beneficial.

Amiodarone
Moderate
Database

Both arteether and amiodarone can prolong the QT interval. Co-administration increases the risk of additive QT prolongation, potentially leading to serious ventricular arrhythmias like Torsades de Pointes.

Avoid concomitant use if possible. If unavoidable, perform baseline and regular ECG monitoring, monitor electrolytes (potassium, magnesium), and consider alternative antiarrhythmic or antimalarial agents. Use with extreme caution.

Carbamazepine
Moderate
Database

Carbamazepine is a moderate inducer of CYP3A4. Co-administration may reduce arteether plasma concentrations, potentially leading to decreased antimalarial efficacy.

Monitor for signs of treatment failure. Consider alternative antimalarial agents or a different anticonvulsant if possible. If co-administration is necessary, close clinical and parasitological monitoring is recommended.

Clarithromycin
Moderate
Database

Clarithromycin is a moderate inhibitor of CYP3A4. Co-administration may increase arteether plasma concentrations, potentially increasing the risk of adverse effects.

Monitor for increased adverse effects of arteether. Consider reducing the arteether dose if co-administration is necessary. Use with caution.

Haloperidol
Moderate
Database

Both arteether and haloperidol can prolong the QT interval. Co-administration increases the risk of additive QT prolongation, potentially leading to serious ventricular arrhythmias.

Avoid concomitant use if possible. If unavoidable, perform baseline and regular ECG monitoring, monitor electrolytes, and consider alternative antipsychotic or antimalarial agents. Use with caution.

Itraconazole
Moderate
Database

Itraconazole is a potent inhibitor of CYP3A4. Co-administration can increase arteether plasma concentrations, potentially increasing the risk of adverse effects.

Monitor for increased adverse effects of arteether. Consider reducing the arteether dose if co-administration is necessary. Use with caution.

Ketoconazole
Moderate
Database

Ketoconazole is a potent inhibitor of CYP3A4. Co-administration can increase arteether plasma concentrations, potentially increasing the risk of adverse effects.

Monitor for increased adverse effects of arteether. Consider reducing the arteether dose if co-administration is necessary. Use with caution.

Mefloquine
Moderate
Database

Both arteether and mefloquine can cause neurotoxicity (e.g., dizziness, vertigo, seizures) and cardiotoxicity (QT prolongation). Co-administration may increase the incidence and severity of these adverse effects.

While often used sequentially in malaria treatment, concurrent use should be avoided. If sequential use, ensure a washout period if possible, and monitor closely for neurological and cardiac adverse events.

Phenytoin
Moderate
Database

Phenytoin is a moderate inducer of CYP3A4. Co-administration may reduce arteether plasma concentrations, potentially leading to decreased antimalarial efficacy.

Monitor for signs of treatment failure. Consider alternative antimalarial agents or a different anticonvulsant if possible. If co-administration is necessary, close clinical and parasitological monitoring is recommended.

Quinidine
Moderate
Database

Both arteether and quinidine can prolong the QT interval. Co-administration increases the risk of additive QT prolongation, potentially leading to serious ventricular arrhythmias like Torsades de Pointes.

Avoid concomitant use if possible. If unavoidable, perform baseline and regular ECG monitoring, monitor electrolytes (potassium, magnesium), and consider alternative antiarrhythmic or antimalarial agents. Use with extreme caution.

Grapefruit Juice
Mild
Database

Grapefruit juice can inhibit intestinal CYP3A4, potentially leading to a modest increase in arteether bioavailability and plasma concentrations.

Advise patients to avoid consuming grapefruit juice during arteether treatment, especially if they are prone to adverse effects or on higher doses.

Related guidelines

Other Sesquiterpine lactone drugs

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Sources: KD Tripathi 7e·Verified: 2026-05-10 · House clinical team