Artesunate

What is Artesunate?

• Artesunate is an antimalarial indicated for the initial treatment of severe malaria in adult and pediatric patients.

What are the uses of this medicine?

• This medicine is indicated for the initial treatment of severe malaria in adult and pediatric patients.
• Treatment of severe malaria with Artesunate for Injection should always be followed by a complete treatment course of an appropriate oral antimalarial regimen.

How does this medicine work?

• Artesunate is an antimalarial drug.
• A water-soluble, semi-synthetic derivative of the sesquiterpine lactone artemisinin with anti-malarial, anti-shistosomiasis, antiviral, and potential anti-neoplastic activities.
• Upon hydrolysis of artesunate’s active endoperoxide bridge moiety by liberated heme in parasite-infected red blood cells, reactive oxygen species and carbon-centered radicals form, which have been shown to damage and kill parasitic organisms.
• Additionally, in vitro studies demonstrate that this agent induces DNA breakage in a dose-dependent manner.
• Artesunate has also been shown to stimulate cell differentiation, arrest the cell cycle in the G1 and G2/M phases, inhibit cell proliferation, and induce apoptosis through mitochondrial and caspase signaling pathways.
• Artemisinin is isolated form the plant Artemisia annua.

Who Should Not Use this medicine ?

This medicine cannot be used in patients if:

• Serious hypersensitivity to artesunate, such as anaphylaxis.

Limitation of use:

• Artesunate does not treat the hypnozoite liver stage forms of Plasmodium and will therefore not prevent relapses of malaria due to Plasmodium vivax or Plasmodium ovale.
• Concomitant therapy with an antimalarial agent such as an 8-aminoquinoline drug is necessary for the treatment of severe malaria due to P. vivax or P. ovale.

What drug interactions can this medicine cause?

• Avoid co-administration of Artesunate with Ritonavir, Nevirapine or Strong UDP-Glucuronosyltransferase (UGT) Inducers (e.g., rifampin, carbamazepine, phenytoin).
• Avoid co-administration of Artesunate with Strong UGT Inhibitors (e.g., axitinib, vandetanib, imatinib, diclofenac).

Is this medicine FDA approved?

• It was approved for use in the United States in 2020.

How should this medicine be used?

• The recommended dosage of Artesunate for Injection is 2.4 mg/kg administered intravenously at 0 hours, 12 hours, and 24 hours, and thereafter, administered once daily until the patient is able to tolerate oral antimalarial therapy.
• Administer constituted Artesunate for Injection intravenously as a slow bolus over 1 minute to 2 minutes .
• Do NOT administer Artesunate for Injection via continuous intravenous infusion.
• Administer Artesunate for Injection with an antimalarial agent that is active against the hypnozoite liver stage forms of Plasmodium, such as an 8-aminoquinoline drug, to patients with severe malaria due to P. vivax or P. ovale.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form: As Injection: 110 mg of artesunate as a powder in a single-dose vial for constitution with the supplied sterile diluent.

This medicine is available in fallowing brand namesː

• ARTESUNATE

What side effects can this medication cause?

Common possible side effects of this medicine include:

• acute renal failure requiring dialysis
• hemoglobinuria
• jaundice

What special precautions should I follow?

• Cases of post-treatment hemolytic anemia have been reported.
• Monitor patients for 4 weeks after treatment for evidence of hemolytic anemia.
• Serious hypersensitivity reactions including anaphylaxis have been reported with this drug .
• Discontinue if signs of serious hypersensitivity occur.

What to do in case of emergency/overdose?

• The overdose was associated with pancytopenia, melena, seizures, multiorgan failure and death.
• Treatment of overdose should consist of general supportive measures.

Can this medicine be used in pregnancy?

• Based on animal data, may cause fetal harm.
• However, administration of Artesunate for Injection for the treatment of severe malaria may be lifesaving for the pregnant woman and fetus. Treatment should not be delayed due to pregnancy.

Can this medicine be used in children?

• The safety and effectiveness of Artesunate for Injection for the treatment of severe malaria have been established in pediatric patients.

What should I know about storage and disposal of this medication?

• Store vials of Artesunate for Injection and sterile diluent in the carton at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
• Do not freeze.
• Avoid exposure to heat.
• Keep protected from light.
• Do not use beyond the expiration date.

• Dailymed label info on Artesunate
• FDA Artesunate