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Dihydroartemisinin is a derivative of artemisinin, which has a powerful and rapid killing effect on the intra-erythrocytic stage of Plasmodium falciparum, and can rapidly control clinical attacks and symptoms. Dihydroartemisinin is a derivative of artemisinin, which has a powerful and rapid killing effect on the intra-erythrocytic stage of Plasmodium falciparum, and can rapidly control clinical attacks and symptoms.
Dihydroartemisinin Powder has the same efficacy as anti-chloroquine and anti-piperaquine falciparum malaria. White needle crystal, odorless, bitter taste. White needle crystal, odorless, bitter taste. Soluble in trichloromethane, soluble in acetone. Slightly soluble in methanol or ethanol, Dihydroartemisinin is almost insoluble in water. Melting point 145~150℃.
Dihydroartemisinin tablets are an ideal oral therapeutic agent, Dihydroartemisinin Manufacturer Henrikang Supply this product.
Uses and functions of Dihydroartemisinin Powder.
Dihydroartemisinin is a derivative of artemisinin, which has a powerful and rapid killing effect on the intra-erythrocytic stage of Plasmodium falciparum, and can rapidly control clinical episodes and symptoms.
It has the same efficacy as anti-chloroquine and anti-piperaquine falciparum malaria. The toxicity of this product is low, in terms of reproductive toxicity, animal experiments found that the administration of the drug in the induction period of pregnancy in mice can increase the incidence of absorption of the fetus, but there is no teratogenic effect. Oral absorption is good, oral administration of the product 2mg/kg, tmax is 1.33h, Cmax is 0.71μg/ml.
It is clinically used for all types of malaria, especially for the rescue of cerebral and aggressive falciparum malaria which is resistant to chloroquine and piperaquine.
Dihydroartemisinin is the first artemisinin derivative created by Tu Youyou in 1973 to identify the carbonyl group in the chemical structure of artemisinin, and subsequently developed artemether, artesunate and other important artemisinin derivatives, which is not only important because of the carbonyl group has been proved to exist;
The significance lies not only in the confirmation of the existence of the carbonyl group, but also in the introduction of the hydroxyl group in the structure of artemisinin through the successful creation of dihydroartemisinin.
It took nearly seven years to develop dihydroartemisinin and its tablets into two new-generation Class I new drugs with independent property rights, whose efficacy is 10 times higher than that of artemisinin, and which have the advantages of "high efficiency, quick-acting, safety, small dosage, easy development and especially low toxicity", and have become the most important new drug of the current generation of artemisinins.
Its efficacy is 10 times higher than that of artemisinin, and it has more prominent advantages such as "high efficiency, quick effect, safety, small dose, easy development, especially low toxicity".
Pharmacological Effects of Dihydroartemisinin Powder.
Dihydroartemisinin tablets is an ideal oral therapeutic drugs, efficacy is not only better than artemisinin, through the comparison of the clinical killing rate, but also shows that the dihydroartemisinin tablets, although oral route of administration, but has caught up with the injection of artesunate, and better than intramuscular injections of artemether, and in terms of toxicity, rekindling rate and the cost of development is lower than the two drugs.
Dihydroartemisinin's pharmacological effect is similar to artemisinin, artemisinin's effect on the ultrastructure of Plasmodium berghei's red inner stage is mainly to make its membrane system structure change.
The drug first acts on the food vesicle membrane, surface membrane, mitochondria, followed by the nuclear membrane and endoplasmic reticulum. In addition, there is some effect on chromatin in the nucleus.
It may act on the food vesicle membrane, blocking the earliest stage of nutritional uptake by Plasmodium, causing Plasmodium to experience amino acid starvation faster, rapidly form autophagic vesicles and continuously expel them from the body, losing a large amount of cytoplasmic and nutrient substances without replenishing them, and thus dying quickly.
Its mode of action is mainly to interfere with the surface membrane-mitochondrial function of Plasmodium.
Through its internal peroxide (hydrogen peroxide) bridge, mediated by free iron produced by hemoglobin decomposition, unstable organic radicals and/or other electrophilic intermediates are generated, which then form covalent adducts with Plasmodium proteins and cause death of Plasmodium.
The uptake of tritium-labeled isoleucine by Plasmodium falciparum cultured in vitro also suggests that the mode of initiation of action may be inhibition of protozoan protein synthesis.
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