Drug reference

Artemisinin

Antimalarial

Also known as Qinghaosu, Artemisinin anhydrous

AntimalarialATC P01BE01

CDSCO approvedATC P01BE01

EXCRETION

—

not curated

INTERACTIONS

—

none in our sources

PREGNANCY

Category C (based on older FDA system). While animal studies show adverse effects, there are no adequate human studies for artemisinin itself. WHO recommends ACTs in 2nd/3rd trimester for uncomplicated malaria, and in 1st trimester only when benefits outweigh risks for severe malaria. Caution is advised for artemisinin use in the first trimester.

FDA category + note

Mechanism

Artemisinin produces free radicals within the malaria parasite's food vacuole upon activation by intraparasitic heme iron. These highly reactive species alkylate and damage key parasite macromolecules including proteins and lipids, leading to rapid parasite clearance. It targets multiple stages of the parasite's lifecycle, particularly the asexual blood stages, inhibiting parasite growth and reproduction.

Indications

Treatment of uncomplicated Plasmodium falciparum malaria (primarily as part of Artemisinin-based Combination Therapies - ACTs)Treatment of multidrug-resistant Plasmodium falciparum malaria (always as part of ACTs)(Off-label) Potential adjunctive therapy in certain cancers (experimental)(Off-label) Other parasitic infections like schistosomiasistreatment of severe p. falciparum malariafirst-line treatment of uncomplicated malaria (as ACT)significant reduction of parasite burden

Dosing

Adult: Artemisinin monotherapy is not recommended for uncomplicated malaria due to rapid resistance development and high recrudescence rates; current guidelines advise its use only in Artemisinin-based Combination Therapies (ACTs). Historically, oral doses for uncomplicated P. falciparum malaria, when used, ranged from 200 mg once daily for 5-7 days.
Pediatric: Similar to adults, artemisinin monotherapy is not recommended. Pediatric dosing for ACTs is weight-based and follows specific guidelines for combination products.
Renal adjustment: No specific dose adjustment for artemisinin is generally required in renal impairment, as it is primarily metabolized by the liver.
Hepatic adjustment: Use with caution in severe hepatic impairment due to extensive hepatic metabolism. No specific dose reduction guidelines exist; monitor for increased side effects.
Geriatric: No specific dose adjustment is typically required. Use with caution considering potential comorbidities and polypharmacy, which may affect drug metabolism or increase susceptibility to side effects.
Max dose: Not applicable for monotherapy as it is not recommended for routine clinical use. Maximum doses for artemisinin derivatives in ACTs are formulation-specific.

Pharmacokinetics

Onset

Rapid (within hours)

Peak effect

Approximately 1-2 hours (Tmax)

Duration

Short, typically due to rapid metabolism and short half-life

Half-life

Approximately 1.5-3 hours

Bioavailability

Variable, approximately 30-50% orally

Protein binding

Approximately 40-60%

Metabolism

Extensive hepatic metabolism, primarily via CYP2B6, CYP2C19, and CYP3A4 to dihydroartemisinin (DHA), which is also active

Excretion

Primarily through feces (bile) as metabolites, with some renal excretion

Contraindications

Known hypersensitivity to artemisinin or its derivatives
First trimester of pregnancy (relative contraindication; use only if benefits outweigh risks, particularly for severe malaria, and as part of an ACT)
Use as monotherapy for uncomplicated malaria is contraindicated due to rapid development of resistance and high recrudescence rates
not recommended during the first trimester of pregnancy
not recommended for the treatment of children weighing 5 kg or less

Side effects

Common

NauseaVomitingAbdominal painDiarrheaDizzinessHeadacheTinnitusDecreased appetiteTransient neutropeniadose-related and reversible decreases in reticulocyte and neutrophil countsincreases in transaminase levels

Serious

Neurotoxicity (rare, especially with high doses or prolonged use, manifesting as ataxia, dizziness, hearing loss, convulsions)
Hematologic effects (agranulocytosis, severe neutropenia, hemolytic anemia - rare but reported)
Hypersensitivity reactions
Cardiac abnormalities (e.g., QT prolongation with some derivatives, less directly with artemisinin itself)
allergic reaction (1 in 3000 patients)

Pregnancy & lactation

Pregnancy

Lactation

Limited data are available. Artemisinin and its active metabolite dihydroartemisinin are excreted in breast milk in small amounts. WHO generally considers artemisinin-based therapies compatible with breastfeeding when clinically indicated, but caution is advised, and monitoring the infant for side effects is prudent.