| Customization: | Available |
|---|---|
| CAS No.: | 130-95-0 |
| Formula: | C20h24n2o2 |
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| Product name | Quinine |
| Cas number | 130-95-0 |
| Appearance | White Powder |
| MF | C20H24N2O2 |
| MW | 324.417 |
Pharmacological action
The drug is a derivative of quinoline, and has a strong killing effect on the intracellular schizozoites of various plasmodium parasites. This drug can bind to the DNA of Plasmodium parasite to form a complex, inhibit DNA replication and RNA transcription, and thus inhibit protozoan protein synthesis, but the effect is weaker than chloroquine. The drug can also reduce the oxygen consumption of Plasmodium, inhibit the phosphorylase in plasmodium and interfere with its glucose metabolism. The drug also causes malarial pigment agglutination, but it develops slowly and rarely forms large clumps. In the blood, a certain concentration of this drug can cause the premature rupture of the parasitic red blood cells, thereby preventing the maturation of the schizozoite. This drug is ineffective in infrared stage and can not cure benign malaria. A long course of treatment can cure falciparum malaria, but it has no direct effect on the gametophyte of falciparum malaria, so transmission cannot be interrupted. In addition, this drug has an inhibitory effect on myocardium, can prolong the refractory period, slow down conduction, and weaken its contractility. It has a weak excitatory effect on the pregnant uterus.
pharmacokinetics
The oral absorption was rapid and complete, and the blood concentration reached the peak in 1 ~ 3h. After absorption, the drug was distributed in the whole body, with the highest concentration in liver, followed by lung, kidney and spleen, and the least in skeletal muscle and nerve tissue, with a protein binding rate of about 70%. This drug is decomposed by oxidation in the liver, and its metabolites and a small amount of the protodrug (about 10%) are excreted through the kidney, which appear in the urine 15 minutes after taking the drug, and almost all are excreted after 24 hours, so this drug has no accumulation. The half-life is 8.5h.
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