Artesunate
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Artesunate
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| Systematic (IUPAC) name | |
| ? | |
| Identifiers | |
| CAS number | 80155-81-3 (sodium salt) |
| ATC code | P01 |
| PubChem | |
| 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.
| 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 |
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