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Artemether + Lumefantrine

Antimalarial combination (artemisinin derivative + arylaminoalcohol) · Antimalarial

Also known as Coartem, Lumerax, Artenam, Artemether-lumefantrine, Riamet

START
Confirm malaria diagnosis (RDT or microscopy); start weight-based dosing immediately; give with fatty food or milk
TYPICAL MAX
4 tablets per dose for >/=50 kg adults; complete all 6 doses over 3 days
STOP IF
Complete full 6-dose course; do not stop early even if feeling better
WATCH
Hemoglobin at days 7, 14, 21, 28 (delayed hemolysis), ECG if cardiac risk, parasite clearance at day 3, ensure fatty food with each dose
CDSCO approvedSchedule HATC P01BF01
Dose laddermg/d
1start2titrate3titrate4ceiling
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo renal adjustment needed090

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
2hONSET2hPEAK4d3wDURATION
ONSET
2h · Rapid fever and parasite clearance
PEAK
2h · Artemether peak
4d · Lumefantrine half-life (3-6 days)
DURATION
3w · Lumefantrine post-treatment prophylaxis (2-3 weeks)
EXCRETION
Fecal (both components)
route + CYP
INTERACTIONS
2 major
incl. contraindicated
PREGNANCY
First trimester: avoid unless no alternative; Second/third trimester: recommended for malaria treatment
FDA category + note
Top interactionssee all 5
  • Qt Prolonging DrugsContraindicatedDatabaseKimi deep-research + Cla
  • RifampicinContraindicatedDatabaseKimi deep-research + Cla
Available in India

0 branded formulations and 347 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Mechanism

Artemether: Endoperoxide bridge cleaved by heme iron generates free radicals that alkylate parasite proteins and inhibit PfATP6. Lumefantrine: Accumulates in parasite food vacuole, inhibiting hematin polymerization. Combined for rapid parasite clearance and prevention of recrudescence.

Indications

Uncomplicated Plasmodium falciparum malaria (first-line ACT per WHO)Mixed malaria infections

Dosing

Adult
Weight-based: 20-24 kg: 1 tab; 25-34 kg: 2 tabs; 35-49 kg: 3 tabs; >/=50 kg: 4 tabs. Dose at 0, 8, 24, 36, 48, 60 hours (6 doses over 3 days). Take with fatty food/milk.
Pediatric
Same weight-based dosing; tablets can be crushed for children unable to swallow
Renal adjustment
No adjustment needed
Hepatic adjustment
No adjustment in mild-moderate; avoid in severe hepatic impairment
Geriatric
Standard weight-based dosing
Max dose
4 tablets per dose (>/=50 kg adult)

Pharmacokinetics

Onset
Rapid (fever clearance within 24-48 hours)
Peak effect
Artemether: 2 hours; Lumefantrine: 6-8 hours
Duration
Lumefantrine provides post-treatment prophylaxis for ~2-3 weeks
Half-life
Artemether: 1-2 hours; Lumefantrine: 3-6 days
Bioavailability
Artemether: variable; enhanced by food. Lumefantrine: highly lipophilic, absorption increased 2-4x with fatty meal
Protein binding
Artemether: ~95%; Lumefantrine: >99%
Metabolism
Artemether: Hepatic CYP3A4/5 to active metabolite DHA. Lumefantrine: Hepatic CYP3A4 to desbutyl-lumefantrine (active)
Excretion
Artemether: Biliary/fecal. Lumefantrine: Fecal (major)

Contraindications

  • First trimester pregnancy (relative)
  • Previous hypersensitivity to artemether, lumefantrine, or structurally related compounds
  • Family history of congenital QT prolongation or sudden death
  • Ventricular arrhythmias
  • Severe hepatic impairment
  • Concurrent use with CYP3A4 inducers (strong) or QT-prolonging drugs

Side effects

Common
HeadacheDizzinessAnorexiaNauseaVomitingAbdominal painArthralgiaMyalgiaSleep disorders
Serious
  • QT interval prolongation
  • Hepatotoxicity
  • Severe skin reactions
  • Delayed hemolytic anemia (1-4 weeks post-treatment)
  • Prolonged QT leading to torsades de pointes (rare)

Pregnancy & lactation

Pregnancy

First trimester: avoid unless no alternative; Second/third trimester: recommended for malaria treatment

Lactation

Both components excreted in breast milk; infant should receive own antimalarial treatment if indicated; compatible per WHO

Drug interactions

Qt Prolonging Drugs
Contraindicated
Database

Additive QT prolongation; risk of torsades de pointes

Avoid concurrent use

Source: Kimi deep-research + Cla

Rifampicin
Contraindicated
Database

Significantly reduces artemether and lumefantrine exposure, risking treatment failure

Avoid concurrent use; choose alternative antimalarial

Source: Kimi deep-research + Cla

Antiretrovirals
Moderate
Database

CYP induction may reduce ACT efficacy; protease inhibitors may increase levels

Monitor parasite clearance; consider dose adjustment if available

Source: Kimi deep-research + Cla

Ketoconazole
Moderate
Database

Increases lumefantrine levels and QT prolongation risk

Use with caution; monitor ECG

Source: Kimi deep-research + Cla

Grapefruit Juice
Mild
Database

CYP3A4 inhibition increases lumefantrine absorption

Avoid grapefruit juice during treatment

Source: Kimi deep-research + Cla

Related guidelines

Ask House about Artemether + Lumefantrine

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