Chloroquine Phosphate

For the treatment of chloroquine-sensitive falciparum malaria, plasmodium vivax malaria and other malaria. Can also be used to treat the treatment of intestinal amoeba disease, as well as the effect of anti-rheumatism.

Chloroquine can cause plasmodium nuclear fragmentation, vacuoles between cells, malaria pigment clumps. It is known that chloroquine cannot kill plasmodium directly, but can interfere with its reproduction. Its mechanism of action is that the product has a strong binding force with nuclear protein, which is inserted between the two strands of DNA double helix and can form a complex with DNA, thus preventing DNA replication and RNA transcription. Chloroquine also interferes with the reproduction of plasmodium by inhibiting the incorporation of phosphoric acid into ITS DNA and RNA. Chloroquine accumulates in large quantities in infected erythrocytes, and is concentrated in the food vesicles and lysosomes of protozoa. The loss of haemoglobin, which digests hemoglobin, makes the plasmodium unable to digest the hemoglobin it ingests, leading to the deficiency of amino acids necessary for the growth and development of the plasmodium, and the disintegration of RNA.

Function

Plasmodium falciparum, plasmodium vivax and other malaria sensitive to chloroquine phosphate (resistant to this drug strain widely appeared at home and abroad), also used for the treatment of extra-intestinal amoebiasis, as well as anti-rheumatism

Chloroquine phosphate can also interfere with fatty acids into phospholipids and control glutamate dehydrogenase and hexokinase. Chloroquine mainly acts on the schizozoites in the inner red stage, and the schizozoites are killed in the blood after 48~72 hours. This product has no effect on the infrared phase of p. vivax, so it cannot cure p. vivax. Falciparum malaria can be cured radically.

After oral administration, the intestinal absorption of chloroquine is fast and full, and the blood concentration is the highest 1~2 hours after taking the drug. About 55% of drugs combine with plasma components in blood. The blood concentration of chloroquine was maintained for a long time, with a half-life of 2.5-10 days (T1/2). The concentration of chloroquine in erythrocytes was 10-20 times that in plasma, and the concentration of chloroquine in erythrocytes invaded by plasmodium was about 25 times higher than that in normal subjects. Chloroquine binds more to histone, and the concentration in liver, spleen, kidney, and lung is 200 times higher than that in plasma. The concentration in brain tissue and spinal cord tissue is 10~30 times of plasma concentration. The metabolic transformation of chloroquine in vivo is carried out in liver, and its main metabolite is deethyl chloroquine, which still has antimalarial effect.