Artesunate for Injection
1. Brand Name: MalartinŽ, ArtesorŽ
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.
3. 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.
4. 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.
6. 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!
Add 2 ml of 5% glucose or normal saline to make the concentration of Artesunate in 20 mg/ml
for intra-muscular injection!
Doses for Children: 1.2mg/kg for children.
7. Adverse Reactions:
No adverse reactions were observed with recommended dose up to now. Transient
reticulocytopenia may occur when overdose of Artesunate Injection (more than 3.75 mg/kg) is
(a) 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.
(b) The speed for intravenous infusion is 3-4 ml per minute.
(c) 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).
(d) 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.
(e) 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!
Artesunate Injection: 60 mg/vial with one ampule (1 ml) of 5% sodium bicarbonate solution.
Guilin Pharmaceutical Co. Ltd, Guilin, Guangxi, China
Tri-Health Co. Ltd., Hong Kong