Artesunate

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Artesunate
Systematic (IUPAC) name
?
Identifiers
CAS number	83507-69-1 80155-81-3 (sodium salt)
ATC code	P01BE03
PubChem	5464098
Chemical data
Formula	C₁₉H₂₈O₈
Mol. mass	384.421 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status	Not licensed in UK or US
Routes	oral, IV, IM

Artesunate (INN) is part of the artemisinin group of drugs that treat malaria. It is a semi-synthetic derivative of artemisinin that is water-soluble and may therefore be given by injection. It is sometimes abbreviated AS.

[edit] Uses

Artesunate is used primarily as treatment for malaria; but it has also been shown to be >90% efficacious at reducing egg production in Schistosoma haematobium infection.^[1]

[edit] Dosing

There are no licensed forms of artesunate available in the U.S. or UK. In the UK, artesunate is available on a named patient basis only.

Intravenous dose of IV artesunate:

2.4 mg/kg loading dose over 5 minutes
1.2 mg/kg dose 12 hours later
1.2 mg/kg once daily after that

Artesunate must always be given with another antimalarial such as mefloquine^[2]^[3] or amodiaquine^[4] so as to avoid the development of resistance. The combination of artesunate/amodiaquine has been found to be of equivalent to co-artemether.^[5]

[edit] Footnotes

^ Boulangier D, Dieng Y, Cisse B, et al. (2007). "Antischistosomal efficacy of artesunate combination therapies administered as curative treatments for malaria attacks.". Trans R Soc Trop Med Hyg 101 (2): 113–16. DOI:10.1016/j.trstmh.2006.03.003.
^ Looareesuwan S, Viravan C, Vanijanonta S, et al. (1992). "Randomised trial of artesunate and mefloquine alone and in sequence for acute uncomplicated falciparum malaria". Lancet 339 (8797): 821–4. PMID 1347854.
^ Nosten F, van Vugt M, Price R, et al. (2000). "Effects of artesunate-mefloquine combination on incidence of Plasmodium falciparum malaria and mefloquine resistance in western Thailand: a prospective study". Lancet 356 (9226): 297–302. PMID 11071185.
^ Adjuik M, Agnamey P, Babiker A, et al. (2002). "Amodiaquine-artesunate versus amodiaquine for uncomplicated Plasmodium falciparum malaria in African children: a randomised, multicentre trial". Lancet 359 (9315): 1365–72. PMID 11978332.
^ Meremikwu M, Alaribe A, Ejemot R, et al. (2006). "Artemether-lumefantrine versus artesunate plus amodiaquine for treating uncomplicated childhood malaria in Nigeria: randomized controlled trial". Malar J 5: 43. PMID 16704735.

v • d • e Antimalarial drugs (P01B)
Aminoquinolines	Amodiaquine, Chloroquine, Hydroxychloroquine, Pamaquine, Primaquine
Biguanides	Proguanil, Cycloguanil embolate
Methanolquinolines	Mefloquine, Quinine
Diaminopyridines	Pyrimethamine
Artemisinin derivatives	Artemisinin, Artemether, Artesunate, Artemotil, Artenimol
Others	Halofantrine, Lumefantrine