Artesunate

What is Artesunate

Artesunate is a parenteral artemisinin derivative indicated for the treatment of severe malaria caused by P. falciparum.

Artesunate is a hemisuccinate derivative of dihydroartemisinin, which is itself formed from the reduction of artemisinin.

Artemisinin is a sesquiterpene lactone endoperoxide extracted from qinghao, sweet wormwood (Artemisia annua), a plant which has been used for centuries in traditional Chinese medicine.

Artemisinins differ from other antimalarials in that they have the ability to kill all erythrocytic stages of the malaria parasite.

They are also the most rapid-acting of the antimalarials. Rarely, delayed post-artemisinin hemolytic anemia or post-artesunate delayed hemolysis (PADH) has been noted in published case reports.

Artesunate is not FDA-approved; however, it is the only intravenous therapy available for severe cases of malaria. Artesunate is considered an orphan drug for the treatment of malaria.

The drug is available from the CDC under an investigational new drug (IND) protocol. 

Indications

• malaria
• Plasmodium falciparum

Side Effects

1. Dysgeusia or bitter or metallic taste (1% to 10%)
2. Nausea (1% to 10%)
3. vomiting (1% to 10%)
4. anorexia
5. diarrhea (1% to 10%)
6. abdominal pain or cramps (1% to 10%)
7. increase serum amylase (0.01% to 0.1%)
8. pancreatitis (0.01% to 0.1%)
9. Dizziness (1% to 10%)
10. lightheadedness (1% to 10%)
11. headache (1% to 10%)
12. insomnia (1% to 10%)
13. tinnitus with or without a decrease in auditory function (1% to 10%)
14. peripheral neuropathy (less than 0.01%)
15. paresthesias (less than 0.01%)
16. Hypersensitivity to artesunate is uncommon (0.1% to 1%)
17. cough (1% to 10%) 
18. nasal symptoms (1% to 10%)
19. arthralgia (1% to 10%)
20. muscle disorders (1% to 10%)
21. fatigue (1% to 10%)
22. malaise (1% to 10%)
23. fever (1% to 10%)
24. An injection site reaction, including pain at the injection site (1% to 10%)

Monitoring Parameters

• hemoglobin/hematocrit
• LDH

Contraindications

• breast-feeding
• pregnancy

Interactions

No information is available regarding drug interactions associated with Artesunate