Pharmaceutical Chloroquine Diphosphate Powder Intermediate Chloroquine Diphosphate Powder Chloroquine Diphosphate

Chloroquine phosphate, also known as n ', n' - diethyl-n4 - (7-chloro-4-quinolinyl) - 1,4-pentanediamine diphosphate, is used in the treatment of chloroquine sensitive falciparum malaria, vivax malaria and other malaria. It can also be used in the treatment of extraintestinal amoebiasis and anti rheumatism.

(1) Pharmacodynamics: chloroquine can make Plasmodium nuclear fragmentation, vacuoles appear between cells, Plasmodium pigment agglomerate. It is known that chloroquine can not kill Plasmodium directly, but can interfere with its reproduction. Its mechanism of action is that chloroquine has a strong binding force with nucleoprotein and can be inserted between the two strands of DNA double helix to form a complex with DNA, thus preventing DNA replication and RNA transcription. Chloroquine can also inhibit the incorporation of phosphate into DNA and RNA of Plasmodium and interfere with the reproduction of Plasmodium. Chloroquine accumulates in the infected red blood cells, and the food vesicles and lysosomes of protozoa are the concentrated sites. Because of the loss of hemoglobinase which digests hemoglobin, Plasmodium can not digest the ingested hemoglobin, resulting in the lack of amino acids necessary for the growth and development of Plasmodium and the disintegration of ribonucleic acid. In addition, chloroquine can interfere with fatty acids entering phospholipids, control glutamate dehydrogenase and hexokinase. Chloroquine mainly acted on schizonts in erythrocytic phase. After 48-72 hours, schizonts in blood were killed. This product has no effect on the infrared phase of vivax malaria, so it can not cure vivax malaria. Falciparum malaria can be cured. Chloroquine also has no direct effect on gametophytes, so it can not be used for etiological prevention and interruption of transmission.

The experiment of labeling chloroquine with tritium showed that the release rate of chloroquine from chloroquine resistant Plasmodium falciparum was 40-50 times faster than that from chloroquine sensitive Plasmodium falciparum. This change was caused by the mutation of Plasmodium falciparum gene. After years of research, we have found the gene of chloroquine resistance in Plasmodium. This gene is located in the 36KB DNA fragment of chromosome 7, which is called CG2 gene. It has complex polymorphism. CG2 gene contains 12 significant mutation sites and 3 polymorphic repeats, of which 4-8 have slight variation, which is enough to make Plasmodium resistant to chloroquine.
 

1. When this product is used in the treatment of malaria, there are few adverse reactions. Generally, the possible reactions of oral administration include dizziness, headache, dizziness, loss of appetite, nausea, vomiting, abdominal pain, diarrhea, pruritus, rash, tinnitus, irritability, etc.Most of the reactions are mild and disappear spontaneously after drug withdrawal.2. A considerable part of this product can be accumulated in the tissue, long service can cause mild retinal edema and pigment aggregation, appear dark spots, affect vision, often irreversible.
3. Chloroquine can also damage hearing, pregnant women take a large number of children can cause congenital deafness, mental retardation.
4. Chloroquinol can cause sinus node inhibition, resulting in arrhythmia, shock, and in severe cases, A-S syndrome, which leads to death.
5. This product can also cause drug psychosis, leucopenia, purpura, rash, dermatitis, photosensitive dermatitis and even exfoliative dermatitis, psoriasis, hair whitening, hair depilation, neuromuscular pain, mild transient headache, etc.
6. Hemolysis, aplastic anemia, reversible granulocytosis and thrombocytopenia are rare .