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 gWbShanghai Natural Bio-engineering Co., Ltd

Product name Artesunate 99%
Botanical Name Artemisinin from Artemisia annua L
CAS number 88495-63-0
Synonyms AS, ARINET, ARTESUNET, ARTEX-50, MALINATE, Arsumax (TN), Artesunate (USAN), Artesunic acid, BB_NC-1045, SM 804, STK801911, AKOS004119951, Succinyl dihydroartemisinin, D02482, 88495-63-0
Appearance White Crystaline powder, odorless
Taste Bitter in taste
Molecular Formula C19H2808
Molecular Weight Specification
Loss on drying ≤0.5% (0.31%)
Dosage 2.4 mg of artesunate / kg body weight
Main benefits Malaria treatment, Parasite treatment, Cancer treatment
Application Pharmaceuticals, drugs, medicines
solubility water soluble 

What is artesunate?

Artesunate (AS), according to Wikipedia, is a semi-synthetic derivative of artemisinin from Artemisia annua extract, a natural product produced by the sweet wormwood plant. This compound is used to treat severe cases of malaria in areas where there is resistance to other anti-malarial drugs. Widely used in Africa and Asia, the drug has recently received approval to be used in the United States to treat severely ill patients who meet certain criteria. Like other drugs to treat malaria, artesunate should always be used in combination with other classes of anti-malarial drugs to prevent the development of resistance by the parasites.gWbShanghai Natural Bio-engineering Co., Ltd

Artesunate is derived synthetically from dihydroartemisinin and is soluble in water. The drug can be given orally, rectally, or injected into muscles or veins. It has an active peroxide bond, which reacts with the malaria-infected red blood cells and produces reactive oxygen species that poison the organisms inside the cell.gWbShanghai Natural Bio-engineering Co., Ltd

General information from WHO

Artesunate is a water-soluble hemisuccinate derivative of artemisinin. It is unstable in neutral solution and the injectable formulation must be prepared immediately before use in 5% (w/v) sodium bicarbonate solution to produce the salt sodium artesunate. After parenteral administration, it is rapidly hydrolysed to the active metabolite dihydroartemisinin. The oral formulation is probably hydrolysed completely before entering the systemic circulation.gWbShanghai Natural Bio-engineering Co., Ltd

Artesunate has been reported to clear fever in patients with severe falciparum malaria 16-25 hours after parenteral administration.gWbShanghai Natural Bio-engineering Co., Ltd

Mechanism of action of artesunate

How Artesunate works? Artesunate is closed related with artemisinin. So to large extent, the mechanism of action of artesunate is the mechanism of action of artemisinin. Artesunate is a hemisuccinate derivative of dihydroartemisinin, which is itself formed by the reduction of artemisinin. Artemisinin is a sesquiterpene lactone endoperoxide extracted fromqinghao (sweet wormwood, Artemisia annua L.), a plant which has been used for centuries in traditional Chinese medicine. The mechanism of action of the artemisinins likely involves cleavage of the internal endoperoxide bridge through reaction with haeme within the infected erythrocyte, thereby generating free radicals which alkylate vital parasite proteins. However, artemisinins have also been reported to inhibit an essential parasite calcium adenosine triphosphatase.gWbShanghai Natural Bio-engineering Co., Ltd

The artemisinins are distinguished from other antimalarials by their ability to kill all erythrocytic stages of the malaria parasite, including the relatively inactive ring stage and late schizonts, as well as the gametocytes responsible for malaria transmission. Artesunate and the artemisinins are the most rapid acting of the antimalarials, and they have also been shown to enhance splenic clearance of infected erythrocytes by reducing cytoadherence. In vitro, dihydroartemisinin (DHA), the active metabolite of artesunate, exhibits similar potency against chloroquine-resistant and chloroquine-sensitive clones of P. falciparum. Artesunate and the other artemisinins are essentially inactive against extra-erythrocytic forms, sporozoites, liver schizontes or merozoites. gWbShanghai Natural Bio-engineering Co., Ltd

Pharmacokinetic Properties of Artesunate and Dihydroartemisinin

Artesunate is the only artemisinin derivative available in oral, rectal and intravenous formulations for use in human. Pharmacokinetics of AS and its active metabolite DHA has been studied quite extensively in different populations. However, Artesunate data were very limited in these studies due to the fact that AS is rapidly converted to DHA and that the assays used were not sensitive enough to detect AS in the samples collected. Consequently, many pharmacokinetic studies of AS either report only the pharmacokinetic parameters for DHA without the parameters related to AS, or report the combined anti-malarial activities of AS and DHA.gWbShanghai Natural Bio-engineering Co., Ltd

Advanced Effect of Artesunate Compared to Artemether and Quinine

Artesunate is a semisynthetic derivative of artemisinin whose water solubility facilitates absorption and provides an advantage over artemisinin because it can be formulated as oral, rectal, intramuscular, and intravenous preparations. Artesunate is rapidly hydrolyzed to dihydroartemisinin, which is the most active schizonticidal metabolite. Injectable administration of artesunate results in a more rapid systemic availability of AS compared with intramuscular AM. This pharmacokinetic advantage may provide a clinical advantage in the treatment of severe malaria. Rectal AS has been shown to be absorbed rapidly, with a considerable inter-individual variability. Artesunate is highly effective against multidrug-resistant falciparum malaria and severe malaria in Vietnam, Thailand, China, and Myanmar; however, only limited studies have been carried out in Africa.gWbShanghai Natural Bio-engineering Co., Ltd

Clinical trials show that artesunate produces fewer life-threatening side-effects than quinine, with fewer recorded incidences of low blood sugar (hypoglycaemia), and anaemia. Furthemore, quinine can induce potentially serious hyperinsulinaemic hypoglycaemia, especially during pregnancy and cardiotoxicity. Quinine IM is also painful and locally toxic.gWbShanghai Natural Bio-engineering Co., Ltd

Artesunate in Treatments of Severe Malaria 

Artesunate is a more attractive formulation than artemether for pharmacokinetic reasons, as it can be administered either intravenously or intramuscularly, and it achieves therapeutic plasma concentrations rapidly when administered by either route. Theoretically, therefore, Artesunate may be more effective than AM, because artemether is as effective as quinine. Initial trial results in adults were encouraging, with some evidence of survival benefits compared with quinine, albeit with small numbers. gWbShanghai Natural Bio-engineering Co., Ltd

Benefits of taking artesunate medicines

Artesunate is used for the treatment of uncomplicated cases of malaria. Artesunate indicated only for attacks due to Plasmodium falciparum (a particular type of malaria parasite), against which the medicine is active. It reduces the number of malaria parasites in your body. Your doctor has found that you have malaria and so has prescribed the tablets to treat your malaria infection. For complete cure it is important that you complete the prescribed dose as advised by your doctor, health care worker or pharmacist.gWbShanghai Natural Bio-engineering Co., Ltd

Side Effects of Artesunate

Like all medicines, artesunate can cause side effects, although not everybody gets them. The following side effects are uncommon (between 1 in 1,000 and 1 in 100 patients treated): Slow heart rate, mild gastrointestinal disturbances, abnormal liver function tests (high liver enzyme levels in blood), low counts of pre-stages of red blood cells (reticulocytopenia), and low white blood cell counts.gWbShanghai Natural Bio-engineering Co., Ltd

If any of the side effects becomes serious, or if you notice any side effects not listed in this leaflet, gWbShanghai Natural Bio-engineering Co., Ltd

please tell your doctor, health care worker or pharmacist.gWbShanghai Natural Bio-engineering Co., Ltd

Cardiotoxicity has been observed following administration of high doses.gWbShanghai Natural Bio-engineering Co., Ltd

Storage of artesunate

Tablets and powder for injection should be stored in tightly closed containers, protected from light.gWbShanghai Natural Bio-engineering Co., Ltd

Dosage and administration of artesunate

Adults and children over 6 months: 5 mg/kg orally on the first day followed by 2.5 mg/kg on the second and third days in combination with mefloquine (15 mg/kg) in a single dose on the second day. In a few areas, a higher dose (25 mg/kg) of mefloquine may be required for a cure to be obtained.gWbShanghai Natural Bio-engineering Co., Ltd

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