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ARTESUNATE

IUPAC Name: 4-oxo-4-[[(1R,4S,5R,8S,9R,10S,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.04,13.08,13]hexadecan-10-yl]oxy]butanoic acid

Symbol: AR

Molecular Formula: C19H28O8

Molecular weight: 384.4 g/mol

CAS No: 88495-63-0

Drug Class: Antimalarials; Antimalarials, Artemisinin Derivative

General Properties:

Artesunate is an artemisinin derivative that is the hemisuccinate ester of the lactol resulting from the reduction of the lactone carbonyl group of artemisinin. It is used, generally as the sodium salt, for the treatment of malaria. It has a role as an antimalarial, a ferroptosis inducer and an antineoplastic agent. It is an artemisinin derivative, a sesquiterpenoid, a dicarboxylic acid monoester, a cyclic acetal, a semisynthetic derivative and a hemisuccinate.

Artesunate is indicated for the initial treatment of severe malaria.

Artesunic acid is a natural product found in Artemisia carvifolia, Artemisia apiacea, and Acronychia pubescens with data available.

Indication:

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’s efficacy is comparable to that of artemether, another artemisinin derivative, in treating adults for severe malaria caused by Plasmodium falciparum, though artesunate clears more parasites initially. Artesunate combination drugs have a number of advantages over artemether-based drugs in terms of its uptake and administration routes and may be more effective in treatment of severe and complicated malaria in children.

Artesunate is also used to treat less severe forms of malaria when it can be given orally. It has activity against P. ovale, P. malariae, and severe P. knowlesi.

Artesunate + sulfadoxine/pyrimethamine for treatment of P. vivax is not recommended due to high rates of resistance.[citation needed]

While artesunate is used primarily as treatment for malaria, there is some evidence that it may also have some beneficial effects in Schistosoma haematobium infection, but has not been evaluated in large randomized trials.

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