Generic Name: artesunate

Drug Class: Antimalarials; Antimalarials, Artemisinin Derivative

What is artesunate, and what is it used for?

Artesunate is a medication administered intravenously to treat serious malaria, a disease with high fevers, shaking chills, and flu-like illness, in adults and children.

Malaria is caused by microscopic unicellular parasites belonging to the Plasmodium species, and the disease caused by Plasmodium falciparum is the type most likely to result in severe infections that can even lead to death, if not promptly treated.

Malaria is transmitted by the bite of infective female Anopheles mosquitos. Malarial parasites grow and multiply in the human liver first and then get into red blood cells and multiply further. The parasites grow digesting the hemoglobin inside red blood cells, eventually rupturing them and releasing daughter parasites that invade other blood cells. The blood stage parasites cause malarial symptoms in humans.

Artesunate is a semisynthetic drug derived from artemisinin, a compound obtained from the plant sweet wormwood, Artemisia annua. Artesunate is active against the blood-stage asexual adult parasites and germ cells (gametocytes) of Plasmodium species, including chloroquine resistant strains, but not against hypnozoites, the liver stage forms of P. vivax and P. ovale, which can remain dormant and invade the blood after months or even years.

Artesunate is rapidly metabolized in the blood into its active metabolite dihydroartemisinin (DHA). Artesunate, like other artemisinins, contains an endoperoxide bridge, a structural feature that is activated by the heme iron in the hemoglobin. This generates free radicals (reactive oxygen species) which cause oxidative stress, make ultrastructural changes and inhibit the synthesis of proteins and DNA in the parasites, preventing their growth and survival.

Warnings

  • Do not use in patients with known serious hypersensitivity (anaphylaxis) to artesunate or any of its components.
  • If the patient develops hypersensitivity symptoms such as generalized rash, urticaria, hypotension or shortness of breath from artesunate injection consider discontinuing the drug and continuing treatment with another antimalarial drug.
  • Artesunate treatment may cause delayed hemolysis. Monitor patients for hemolytic anemia for 4 weeks after artesunate therapy.
  • Administration of IV artesunate in early pregnancy may cause loss of pregnancy and fetal malformations, however, delay in treatment of severe malaria during pregnancy may result in serious morbidity and mortality to the mother and fetus.

What are the side effects of artesunate?

Common side effects of artesunate in patients with severe malaria include:

Less common side effects of artesunate in patients with severe malaria include:

Side effects of artesunate in patients with uncomplicated malaria (unapproved indication) and healthy volunteers include:

Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:

  • Serious heart symptoms include fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness;
  • Severe headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady;
  • Severe nervous system reaction with very stiff muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, and feeling like you might pass out; or
  • Serious eye symptoms include blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

SLIDESHOW

Bacterial Infections 101: Types, Symptoms, and Treatments See Slideshow

What are the dosages of artesunate?

Injection, Lyophilized Powder for Reconstitution

  • 110 mg/vial

Adult and Pediatric:

Severe Malaria

  • Indicated for initial treatment of severe malaria; should always be followed by a complete treatment course of an appropriate oral antimalarial regimen
  • 2.4 mg/kg intravenous (IV) at 0, 12, and 24 hours, THEN once every day until able to tolerate oral antimalarial therapy  
  • Administer with an antimalarial agent that is active against the hypnozoite liver-stage forms of Plasmodium (e.g., 8-aminoquinoline drug) to patients with severe malaria caused by P. vivax or P. ovale

Dosage Modifications

Renal or hepatic impairment

  • No specific dosage adjustments are needed for patients with renal or hepatic impairment
  • No specific pharmacokinetic studies have been carried out in patients with renal or hepatic impairment
  • Most patients with severe malaria present with some degree of related renal or hepatic impairment

Dosing Considerations

Limitations of use

  • Does not treat hypnozoite liver-stage forms of Plasmodium and therefore does not prevent relapses of malaria caused by P. vivax or P. ovale
  • Concomitant therapy with an antimalarial agent (e.g., 8-aminoquinoline drug) is necessary for the treatment of severe malaria caused by P. vivax or P. ovale

Overdose

  • Artesunate injection is administered under clinical settings and experience of overdose is limited.
  • One overdose record of inadvertent rectal administration of artesunate in a 5-year-old child resulted in drop in all count of all types of blood cells (pancytopenia), black tarry stools (melena), seizures, multiorgan failure and death.
  • Artesunate overdose must be managed with symptomatic and supportive treatment.

What drugs interact with artesunate?

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

QUESTION

Bowel regularity means a bowel movement every day. See Answer

Pregnancy and breastfeeding

  • Available information on intravenous (IV) artesunate in pregnant women is insufficient to identify a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Animal reproductive studies show loss of pregnancy and fetal malformations with administration of IV artesunate in early pregnancy.
  • Extensive experience with oral artesunate (not an approved route of administration) and other artemisinin class drugs in pregnant women has not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
  • Delay in treatment of severe malaria during pregnancy may result in serious morbidity and mortality to the mother and fetus. Treatment should not be withheld from pregnant women with severe malaria.
  • Dihydroartemisinin (DHA), the active metabolite of artesunate is present in milk. There is no information on its effects on milk production or the breastfed infant. Decision to nurse during therapy should be based on the mother’s clinical need, benefits of breastfeeding to the infant, and the potential risks to the infant from exposure to the drug and adverse effects from the mother’s underlying condition.
  • There is a pregnancy safety study that monitors pregnancy outcomes in women who are administered artesunate IV during pregnancy. Healthcare providers are encouraged to report artesunate exposure during pregnancy by contacting Amivas LLC at 1-855-526-4827 (1-855-5AMIVAS) or www.amivas.com/our-products.

What else should I know about artesunate?

  • In addition to artesunate injection, it is important to take other oral antimalarial therapy as prescribed to prevent relapse of malaria. Complete the course of medications as prescribed by your physician.
  • Check with your physician for follow-up blood nests for 4 weeks after treatment with artesunate injection.
  • Report to your physician immediately if you develop any hypersensitivity symptoms such as generalized rash, hives, shortness of breath or low blood pressure after receiving artesunate injection.
  • Artesunate injection could be toxic to the embryo/fetus and cause loss of pregnancy or fetal malformations. Inform your physician if you are pregnant or think you may be pregnant. Serious malaria must be treated promptly, delay can lead to serious disease and death.

Subscribe to MedicineNet's General Health Newsletter

By clicking Submit, I agree to the MedicineNet's Terms & Conditions & Privacy Policy and understand that I may opt out of MedicineNet's subscriptions at any time.

Summary

Artesunate is a medication administered intravenously to treat serious malaria, a disease with high fevers, shaking chills, and flu-like illness, in adults and children. Common side effects of artesunate in patients with severe malaria include low red blood cell count (anemia), low platelet count (thrombocytopenia), high count of leukocyte immune cells (leukocytosis), low count of neutrophil immune cells (neutropenia), low count of lymphocyte immune cells (lymphopenia), elevation of liver enzymes (transaminases), high bilirubin levels in blood (hyperbilirubinemia), jaundice, acute renal failure requiring dialysis, and others. Consult your doctor if pregnant or breastfeeding.

Treatment & Diagnosis

Medications & Supplements

Prevention & Wellness

Health Solutions From Our Sponsors

FDA Logo

Report Problems to the Food and Drug Administration

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.

Medically Reviewed on 8/9/2022
References
REFERENCES:

https://www.rxlist.com/consumer_artesunate/drugs-condition.htm

https://reference.medscape.com/drug/artesunate-342684#0

https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213036s000lbl.pdf

https://www.uptodate.com/contents/artesunate-drug-information

https://pubmed.ncbi.nlm.nih.gov/25348537/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2758403/

https://www.cdc.gov/malaria/about/