- Brand Name: Malartin, Artesor
International non-proprietary name: Artesunate
Chemical Name: Dihydroartemisinine-10-a-hemisuccinate
Molecular Formula: C19H28O8 = 383.43
Artesunate is a white crystalline powder odorless and almost tasteless.
- Pharmacologic Effects
Artesunate has an excellent anti-malarial activity on the asexual forms of malaria parasites with high, quick efficiency to bring about rapid control of an acute attack. It has advantages of no cross resistance to Chloroquine.
- Absorption, Distribution and Excretion The concentration in plasma decreases rapidly after administered intravenously. The plasma half- life time is about 30 minutes. It distributes widely throughout the body and with high concentration in intestines, liver and kidneys. Only a small quantity excretes in urine and stools. It is mainly eliminated by metabolic bio-transformation.
Artesunate is developed for killing the erythrocytic stage of plasmodium asexual form. It is effective to malaria caused by chloroquine resistant stain of plasmodium falciparum. It can quickly and reliably control the acute attack of malaria. It is suitable to salvage the patients with pernicious malaria and treat P. falciparum malaria and P. vivax malaria. Artesunate Injection is indicated for the treatment of serious malaria infections and the patients with cerebral malaria.
- Administration and Dosage
- Artesunate for Injection (60 mg/vial)
- It should be administered in a dose of 60 mg via intra-muscular or intravenous infusion, once daily for 5-7 days for a course. Double the first dose! Total doses are 360-480 mg for adults.
- The vial of Artesunate powder should be mixed with 1 ml of 5% sodium biocarbonate solution (provided) and shaken 2-3 minutes for better dissolution.
- Add 5 ml of 5% glucose or normal saline to make the concentration of Artesunate in 10 mg/ml for slow intravenous infusion!
Doses for Children: 1.2mg/kg for children.
- Adverse Reactions:
No adverse reactions were observed with recommended dose up to now. Transient eticulocytopenia may occur when overdose of Artesunate Injection (more than 3.75 mg/kg) is given.
- The solution should be used immediately after the powder is dissolved. It should not be used for intravenous infusion if the solution appears cloudy or sediment occurs.
- The speed for intravenous infusion is 3-4 ml per minute.
- A dose of 60 mg Artesunate Injection should be given 4-6 hour following the first dose of 120 mg in the patients infected with high parasitemia (Over 10% of RBC infection rate).
- The recrudescence rate is less than 10% of cases with Chloroquine resistance if the patient is treated using Artesunate Injection for 5 days. A 7-day treatment is recommended for patients with serious infection and non-immune. It will be helpful taking Artesunate Tablets for another 7 days after malaria symptoms are controlled by the injection.
- Embryo-toxic effects were observed in some animal studies. Use Artesunate carefully in pregnant women during the first three months!
- Store Injectable Artesunate at room temperature, 15-30°C (59-86°F)! Keep out of light!
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