Artesunate (AS) is a medication used to treat malaria. The intravenous form is preferred to quinine for severe malaria. Often it is used as part of combination therapy, such as artesunate plus mefloquine. It is not used for the prevention of malaria. Artesunate can be given by injection into a vein, injection into a muscle, by mouth, and by rectum.The most common side effects include kidney failure requiring dialysis, hemoglobinuria (the presence of hemoglobin in urine) and jaundice.Artesunate is generally well tolerated. Side effects may include a slow heartbeat, allergic reaction, dizziness, and low white blood cell levels. During pregnancy it appears to be a safer option, even though animal studies have found harm to the baby. Use is likely fine during breastfeeding. It is in the artemisinin class of medication.Artesunate was developed by Liu Xu in 1977. It is on the World Health Organizations List of Essential Medicines. It was approved for medical use in the United States in May 2020. It is in the class of medications known as artemisinins, which are derivatives from "qinghao," or sweet wormwood plant (Artemisia annua). Medical uses
Artesunate is the first-line treatment for children or adults with severe malaria, usually in combination with another antimalarial drug. There is moderate-quality evidence that treatment with artesunate plus mefloquine is superior to treatment with artesunate plus amodiaquine or artesunate plus sulfadoxine-pyrimethamine. Artemisinin-based combination therapy may be used by mouth in persons that can tolerate it after 24 hours by injection.Artesunate is preferred over parenteral quinine for severe malaria treatment.
In absence of other viable treatment options, artesunate may be used. Children
Artesunate is safe for use in children. Artesunate + sulfadoxine/pyrimethamine should be avoided in the newborns due to sulfadoxine/pyrmethamine effects on bilirubin. Parenteral artesunate dosing for treatment of severe malaria in children less than 20 kg should be higher than that of adults in order to increase exposure. When artesunate cannot be given orally or intramuscularly due to an individuals weakness or inability to swallow, rectal administration may be given as pre-referral treatment as long as parenteral administration is initiated after transfer to a more advanced facility. Adverse effects
Artesunate may cause serious side effects including hemolytic anemia (a condition in which red blood cells are destroyed), and severe allergic reactions.Artesunate is generally safe and well tolerated. Artesunate-based regimens are less likely to cause vomiting and tinnitus than quinine plus anti-malarial antibiotic therapy. The best recognised adverse effect of the artemisinins is that they lower reticulocyte counts. This is not usually of clinical relevance.With increased use of I.V. artesunate, there have been reports of post-artesunate delayed haemolysis (PADH). Delayed haemolysis (occurring around two weeks after treatment) has been observed in people treated with artesunate for severe malaria. Contraindications
Artesunate is typically a well tolerated medicine. Known contraindications include a previous severe allergic reaction to artesunate.Drugs that should be avoided while on artesunate are the drugs that inhibit the liver enzyme CYP2A6. These drugs include amiodarone, desipramine, isoniazid, ketoconazole, letrozole, methoxsalen and tranylcypromine. Mechanisms of action
The mechanisms of action of artesunate remains unclear and debatable.