Product information:
| Product name |
Primaquine Phosphate Tablets |
| Specifications |
15mg; 7.5mg |
| Package |
10*10/Box |
| Storage |
Cool & Dry Place |
| Shelf Life |
2 Years |
| Usage |
Antimalarial |
Indication:
It is mainly used to cure vivax malaria and control malaria transmission.
Adverse reactions:
1. The adverse reaction of this product is higher than that of other antimalarial drugs. When the daily dosage is more than 30mg (matrix), it is prone to fatigue, dizziness, nausea, vomiting, abdominal pain and other adverse reactions; a few people may have drug fever, agranulocytosis and so on, which can be recovered after withdrawal.
2. Patients with glucose-6-phosphate dehydrogenase deficiency may develop acute hemolytic anemia. This hemolytic reaction is limited to aging red blood cells, and can stop the development by itself, which is generally not serious. Once it happens, the drug should be stopped and appropriate symptomatic treatment should be given. When glucose-6-phosphate dehydrogenase is deficient, it will cause methemoglobinemia, cyanosis, chest tightness and other symptoms. Intravenous injection of methylene blue 1-2mg / kg can quickly improve the symptoms.
Taboo:
Glucose-6-phosphate dehydrogenase deficiency, systemic lupus erythematosus and rheumatoid arthritis are forbidden.
Matters needing attention:
1. Ask carefully whether you have a history of faba bean disease and other hemolytic anemia, and whether you have a history of glucose-6-phosphate dehydrogenase deficiency and nicotinamide adenine dinucleotide reductase (NADH) deficiency.
2. Patients with liver, kidney, blood system diseases, acute bacterial and viral infection and diabetes should be cautious.
3. Red blood cell count and hemoglobin should be checked regularly.
4. Lactating women should be cautious.
Medicine interactions:
1. This product acts on the infrared phase of Plasmodium vivax and can cure Plasmodium vivax when combined with chloroquine.
2. The metabolism of primaquine can be inhibited by the two drugs. Therefore, when primaquine is used together with the two drugs, the plasma concentration of primaquine is greatly increased, the maintenance time is prolonged, and the toxicity is increased, but the curative effect is not increased.
3. It is not suitable to use with other drugs with hemolysis and inhibition of bone marrow hematopoiesis.
Pharmacology and Toxicology:
This product can kill Plasmodium vivax, Plasmodium vivax, Plasmodium falciparum and Plasmodium ovale in tissue phase, especially Plasmodium vivax. It can also kill gametophytes of various Plasmodium. It has a strong effect on Plasmodium falciparum, so that it can not develop in mosquitoes, so as to block transmission. The effect of this product is very weak on erythrocytic stage. The antimalarial mechanism of primaquine is not completely clear, which may be related to the interference of DNA synthesis. The infrared phase of Plasmodium and tissue cells were cultured together in primaquine solution for 8 hours. Electron microscope observation showed that primaquine could change the morphology of Plasmodium mitochondria, showing swelling of mitochondria and cytoplasmic vacuoles. The drug can inhibit the oxidation of mitochondria and significantly reduce the oxygen uptake of Plasmodium. Primaquine is metabolized in vivo to quinoline quinone derivatives, which can convert reduced glutathione (GSH) into oxidized glutathione (gssh) in red blood cells. When the latter is reduced, NADPH is consumed. Because of the depletion of NADP during the development of Plasmodium in the liver parenchymal cells in the infrared phase, primaquine interferes with the reduction process of NADP, resulting in the decrease of NADP, which seriously destroys the sugar metabolism and oxidation process of Plasmodium.
Pharmacokinetics:
The bioavailability (f) was about 96%. After oral administration of 45 mg (matrix), the plasma concentration reached the peak (Cmax) within 1 hour, about 250 mg / L. It was mainly distributed in liver tissue, followed by lung, brain and heart. T1 / 2 is 5.8 hours (3.7-7.4 hours). Most of them are metabolized in the body. Only 1% of them are excreted in the urine, which is usually completed within 24 hours. Because the blood concentration maintained for a short time, it requires repeated medication to be effective.
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