Chloroquine Phosphate Tablets

Chloroquine mainly acts on erythrozoites, and after 48 to 72 hours, schizonts in the blood are killed. This product is ineffective against the infrared stage of Plasmodium vivax malaria, so it cannot cure Plasmodium vivax malaria. It can cure falciparum malaria. Chloroquine is ineffective against the infrared stage and has no direct effect on gametocytes, so it cannot be used for etiology prevention and interruption of transmission. After the action of chloroquine, the nucleus of the malarial parasite is fragmented, vacuoles appear in the cytoplasm, and the hemochromatin aggregates into clumps. It is known that chloroquine cannot directly kill malarial parasites, but it can interfere with its reproduction. This product has a strong binding force with nucleoprotein, and the negatively charged 7-chloro group on its quinoline ring is close to the 2-amino group on the guanine of DNA, so that chloroquine is inserted between the two strands of the double helix of DNA. It forms a complex with DNA, thereby preventing DNA replication and RNA transcription. Chloroquine can also inhibit the incorporation of phosphate into the DNA and RNA of malarial parasites, and interfere with the reproduction of malarial parasites due to the reduction of nucleic acid synthesis. Experiments using isotope-labeled chloroquine have shown that infected red blood cells can cause a large amount of chloroquine to accumulate inside them, and the food vacuole and lysosome of the protozoa are the sites of its concentration. The amount of chloroquine concentrated is related to the pH in the food vacuole. The pH in the food vacuole is acidic (the optimal pH for decomposing hemoglobin is 4), which can lead to the concentration of the alkaline drug chloroquine. The concentration of this drug consumes the hydrogen ions in the food vacuole, thereby further increasing the pH value in the food vacuole, causing the loss of hemoglobin digesting hemoglobin. The malarial parasite cannot digest the ingested hemoglobin, resulting in a lack of amino acids necessary for the growth and development of the malarial parasite, and causing the disintegration of ribonucleic acid. In addition, chloroquine can interfere with the entry of fatty acids into phospholipids, control glutamate dehydrogenase and hexokinase, etc. In recent years, some people believe that the early effect of chloroquine on malarial parasites is to cause the aggregation of hemochromatin. Ferroporphyrin IX (FP), the main component of hemochromatin, can damage red blood cells and form a complex with chloroquine to mediate the chemotherapy effect of chloroquine. It is speculated that the protozoa have one or more receptors, namely "FP binders", which may be an albumin that can bind to FP to form a non-toxic complex, protecting the protozoan biofilm from FP damage. The mechanism of action of chloroquine may be to separate the "FP binder" from FP and form a toxic chloroquine-FP complex, thereby exerting its antimalarial effect. Due to the change in receptors, chloroquine loses its due effect, which may be one of the reasons why malarial parasites develop resistance to chloroquine.

The main ingredient is chloroquine phosphate, chemical name: Nˊ,Nˊ-diethyl-N4-(7-chloro-4-quinolyl)-1,4-pentanediamine diphosphate Molecular formula: C18H26ClN3·2H3PO4 Molecular weight: 515.87

This product is white tablets or white sugar-coated tablets.

It is used to treat chloroquine-sensitive malignant malaria, vivax malaria and malaria malaria. It can also be used to suppress the symptoms of malaria. It can also be used to treat extraintestinal amebiasis, connective tissue diseases, photosensitivity diseases (such as sunburn erythema), etc.

1 Common dosage for adults ① For vivax malaria, take 1g orally for the first dose, and 0.75g on the second and third days. ② For suppressive prevention of malaria, take 0.5g orally once a week. ③ For extraintestinal amebiasis, take 1g orally daily, and change to 0.5g daily after taking it for 2 consecutive days. The total course of treatment is 3 weeks. ④ For rheumatoid arthritis, take 0.25~0.5g daily, and change to 0.125g 2~3 times a day after the symptoms are controlled. It takes 6 weeks to 6 months to achieve the maximum therapeutic effect. It can be used as an auxiliary drug for salicylic acid preparations and decreasing adrenal cortex hormones. 2 Common dosage for children ① For vivax malaria, take the first oral dose of 10mg/kg body weight (calculated as chloroquine, the same below), the maximum amount does not exceed 600mg, take another dose of 5mg/kg body weight after 6 hours, and take 5mg/kg body weight daily on the second and third days. ② For extraintestinal amebiasis, take 10 mg/kg (maximum dose not exceeding 600 mg) orally daily according to body weight, divided into 2 to 3 doses, for 2 weeks. After 1 week of rest, the course of treatment can be repeated.

(1) When this product is used to treat malaria, adverse reactions are rare. Oral reactions that may occur include: dizziness, headache, blurred vision, loss of appetite, nausea, vomiting, abdominal pain, diarrhea, skin itching, rash, and even exfoliative dermatitis, tinnitus, irritability, etc. Most reactions are mild and disappear on their own after stopping the drug. (2) When treating paragonimiasis, clonorchiasis, and connective tissue diseases, large dosages and long courses of treatment may cause more severe reactions. The most common one is eye toxicity, because chloroquine can be secreted by the lacrimal glands and absorbed by the cornea, and diffuse white particles appear on the cornea, which disappear after stopping the drug. (3) A considerable part of this product accumulates in the tissues. Long-term use can cause mild retinal edema and pigment aggregation, dark spots, and affect vision, which is often irreversible. (4) Chloroquine can also damage hearing. If pregnant women take large amounts, it can cause congenital deafness, mental retardation, hydrocephalus, limb defects, etc. in children. (5) Chloroquine may occasionally cause inhibition of the sinoatrial node, leading to arrhythmia and shock. In severe cases, it may cause Adams-Stokes syndrome, leading to death. (6) This product may also cause drug-induced psychosis, leukopenia, purpura, rash, dermatitis, photosensitive dermatitis and even exfoliative dermatitis, psoriasis, hair whitening, hair loss, neuromuscular pain, mild transient headache, etc. (7) Hemolysis, aplastic anemia, reversible granulocytosis, thrombocytopenia, etc. are relatively rare.

It is forbidden for pregnant women to use.

Precautions for children: Not yet clear. Precautions for pregnancy and lactation: Not for use by pregnant women. Precautions for the elderly: Not yet clear.

① This product can easily cause allergic dermatitis when used together with phenylbutazone; ② It can easily increase the burden on the liver when used together with chlorpromazine; ③ This product has a direct inhibitory effect on neuromuscular junctions, and streptomycin can aggravate this adverse reaction; ④ The use of this product after digitalization can easily cause heart block; ⑤ This product can increase the chance of bleeding when used together with heparin or penicillamine; ⑥ This product can cure vivax malaria when used together with primaquine; ⑦ It can accelerate excretion and reduce blood concentration when used together with ammonium chloride; ⑧ It can increase toxicity when used together with monoamine oxidase inhibitors; ⑨ It can easily cause exfoliative erythroderma when used together with flurandrenolide; ⑩ When used together with chloroquine analogs (aminoquine, hydroxychloroquine, etc.), the blood concentration of chloroquine can be increased.

Keep away from light and store in sealed container.

0.25g

24 months