HOME > Artesunate
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|Appearance||white crystalline powder, odorless, bitter taste.|
|Properties||Soluble in chloroform, dissolved in acetone, slightly soluble in methanol or ethanol, almost insoluble in water.|
|Antiparasitic drug||Artesunate is a kind of commonly used anti-parasitic drug and belongs to reduced artemisinin succinate monoester, and is the derivative of artemisinin containing a sesquiterpene lactone structure, and has a stronger efficacy on treating parasite than artemisinin and is also effective on treating chloroquine resistant strains. It acts on the Plasmodium schizonts on the erythrocytic stage. It takes effect by inhibiting cytochrome oxidase through reduced artemisinin to achievement of the inhibition on the function of cytochrome oxidase of malaria parasite surface membrane-food vacuole membrane, mitochondrial membrane, and thus blocking the supplying of nutrition from the host cell cytoplasm. It has a strong killing effect on the asexual form of plasmodium with a rapid efficacy enabling the rapid control of the onset of malaria. It has good efficacy on treating cerebral malaria, falciparum malaria and vivax malaria with similar efficacy in treating chloroquine-resistant strain of the falciparum malaria, especially with more significant effect on treating cerebral malaria. It can quickly control the emergence of malaria but has no effect on falciparum malaria gametophyte. It has a shorter T1/2 than artemether with blood concentration rapid decreasing after intravenous injection. Its T1/2 is about 30 min. It is widely distributed in the body with the content in intestine, liver, kidney being relative high. Urine and fecal excretion account for only a small fraction. It mainly undergoes metabolic conversion. It is clinically suitable for rescue of critically ill patients with acute malaria and can be used as the first-choice drug for the treatment of patients with cerebral malaria and a variety of dangerous malaria. But its shortcoming is the recrudescence rate. No adverse reactions have been observed at the recommended therapeutic dose; the application of large doses may cause a transient reduction of the outer peripheral reticulocyte which will return to normal level after stopping drug. Women within 2 months of pregnancy should be disabled. Whether it will cause teratogenicity demands further study.|
|Dosage and administration||Powder: 60mg; each artesunate is also attached with one 5% sodium bicarbonate injection. Upon application, first dissolve the drug in sodium bicarbonate injection, and then diluted to 10 ml with glucose injection after intravenous infusion at a rate of 3 ~ 4ml/min. For the treatment of patients of chloroquine-resistant falciparum malaria: 60 mg per time with the first dose being doubled; intravenously inject 1 times per day with 4 days as a course of treatment. The total dose is 300mg. When the symptom gets controlled, you can change with other anti-malarial drugs to reduce the recrudescence rate. The exact dosage and tablets should be according to the exact condition.|
The clinical application of artesunate has been as long as ten years. It is made through using the artemisia annua grass which is unique in China as raw material for extracting the active ingredient artemisinin and further going through chemical synthesis. Its major role is in treating plasmodia asexual form. It is also currently the only artemisinin derivatives which can be made into water-soluble formulation. It can be used to kill the parasite in inner phase of red blood cells to achieve the anti-malarial effect, and therefore being used in patients with various types of malaria, especially for treating and saving the patients with anti-chloroquine and anti-piperaquine falciparum malaria and severe-type cerebral malaria. It is characterized by high anti-malarial activity, high rate of fever abatement, short parasite clearance time and low drug toxic and side effects. It is the first-choice of drugs for the treatment of severe malaria.
For the application of artesunate tablets, using a total amount of 0.28 g in 3d course of treatment and a total amount of 0.44 g in 5d course of treatment, wherein applying the total amount 0.44 g (equivalent to 8.8 mg / kg) in 5d course for treatment of falciparum malaria can lead to the protozoa recrudescence rate being as low as 4.4% after clinical curing of the patients with no significant toxicity and side effect and no decline in reticulocytes, clarifying that the patients have good tolerance on this dose. Oral administration has low toxicity and rapid efficacy and is more convenient and simple for applying.
Applying 0.24 g/kg of artesunate for treatment of 72 cases of chloroquine-resistant falciparum malaria results in both the cooling time and asexual parasite clearance time being within 36 h and severely sicken patients being clinically cured. This clarifies that artesunate injection has many advantages including rapid insecticidal effect, short-term efficacy, safety, etc., it is suitable for the treatment and saving of patients with severe chloroquine-resistant falciparum malaria.
1. It has a relative strong killing effect on the asexual body of plasmodium falciparum and can result in rapid control of malaria episodes.
2. It is a kind of anti-malarial drug.
|Usage||Derivative of Artemisinin. Antimalarial|
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