Artesunate

Generic Details

Generic Name

Artesunate

Other Names

  • Artesunic acid

Drug Class

  • Antimalarial

Chemical Formula

C19H28O8

Molecular Weight

384.42 g/mol

Mechanism of Action

  • Artesunate is a prodrug that is converted to dihydroartemisinin, the active metabolite. It acts by producing free radicals that damage the cell membranes of the Plasmodium parasites.

Indications

  • Treatment of malaria caused by Plasmodium falciparum
  • Severe malaria cases

Common Dosage Forms

  • Tablet
  • Injection

Typical Dosage

  • Adults: 100-200 mg once daily for 3-7 days
  • Children: Dosage varies based on weight and severity of infection

Pediatric Dosage

  • The dosage is weight-based, and it is crucial to follow the prescribed regimen by a healthcare provider.

Geriatric Dosage

  • Dosage adjustments may be needed based on individual health conditions and renal function.

Side Effects

  • Nausea
  • Vomiting
  • Dizziness
  • Headache
  • Rash
  • Neutropenia

Contraindications

  • Hypersensitivity to artesunate or artemisinin derivatives

Pregnancy Category

  • C - Risk cannot be ruled out

Lactation Safety

  • Limited data available; caution advised

Drug Interactions

  • Strong CYP2A6 or CYP2C9 inducers/inhibitors may alter artesunate metabolism

Overdose Symptoms

  • Dizziness
  • Confusion
  • Seizures
  • Cardiac arrhythmias

Antidote for Overdose

  • There is no specific antidote; management is supportive and symptomatic.

Storage Conditions

  • Store at room temperature away from moisture and heat.

Pharmacokinetics

  • Absorption: Rapidly and well absorbed after oral or parenteral administration
  • Distribution: Extensively distributed in the body, including the liver and kidneys
  • Metabolism: Undergoes hepatic metabolism to active dihydroartemisinin
  • Excretion: Primarily excreted in the bile

Precautions

  • Caution in patients with G6PD deficiency due to risk of hemolysis
  • Monitor liver function tests during treatment

Warnings

  • Not to be used as monotherapy due to risk of resistance development

Others

  • Artesunate is a vital component of artemisinin-based combination therapies (ACTs) recommended by the World Health Organization for the treatment of malaria.