Artesunate
Artesunate is an antimalarial agent. It is a water-soluble hemisuccinate derivative of dihydroartemisinin. Artesunate and its active metabolite dihydroartemisinin are potent blood schizonticides, active against the ring stage of the parasite. Artesunate is ideal for the treatment of severe malaria, including cerebral malaria. It is also active against chloroquine and mefloquine resistant strains of P. falciparum. It is unstable in neutral solution and is therefore only available for injections as artesunic acid. The injectable formulation must be prepared immediately before use in 5% (w/v) sodium bicarbonate solution to produce the salt sodium artesunate.
Primary Characteristics
It is of Semi Synthetic origin.
Molecular Weight: 384.42 · Non-proprietary name: Artesunate.
Pharmacokinetics
Elimination: plasma half-life is 45 min.
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Indications
Artesunate is primarily indicated in conditions like Cerebral malaria, Chloroquine resistant malaria.
Contraindications
Artesunate is contraindicated in conditions like Hypersensitivity, Pregnancy.
Dosage
Artesunate's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 2.4 mg/kg | 2.4 mg/kg | — | IM | Severe malaria: This dose is followed by 1.2mg/Kg at 12 and 24 hours then 1.2mg/Kg daily for 6 days. If the patient can swallow, the daily dose can be given orally. |
| 2.4 mg/kg | 2.4 mg/kg | — | IV | Severe malaria: This dose is followed by 1.2mg/Kg daily until the patient can take orally artesunate or another effective antimalarial drug. |
| 4 mg/kg | 4 mg/kg | — | PO | Monotherapy: 4mg/Kg loading dose on the first day followed by 2mg/Kg once a day for 6 days. |
| 4 mg/kg | 4 mg/kg | — | PO | Combination therapy: 4mg/Kg once a day for 3 days plus mefloqine (15mg or 25mg of base per Kg) as a single dose or split dose on the second and/or third day. |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
The signs and symptoms that are produced after acute overdosage of Artesunate are Cardiotoxicity .
Artesunate is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Convulsions , Diarrhea, Dizziness, Fever, Flatulence, Hair loss, Headache, Itching, Rashes , Vomiting .
Warnings / Precautions
Available Brands
Drug Classification
- 1.6.4.3 — Antimalarials