Primaquine, mainly used to eradicate vivax malaria and control malaria transmission, is often used in combination with chloroquine or pyrimethamine.It has weak effect on the erythrocytic phase, but has no effect on the erythrocytic phase of falciparum malaria, and cannot be used as a drug to control symptoms.It also has an impact on the pre erythrocytic stage of some malaria parasites, but because the required dosage is large, it is close to the maximum and is not safe enough, so it cannot be used as a preventive medicine for the cause of disease.
Chinese alias: N - (6-methoxyquinoline-8-yl) pentane-1,4-diamine;Primaquine;Primaquine phosphate;Primaquinine;Pimaquinoline phosphate;Primaquinine phosphate;Primaquine phosphate
English name: primaquine
English alias: N4 - (6-methody-8-quinolinyl) 1,4-pentanediamine;Primaquinum; N'-(6-methoxy-8-quinolinyl)-1,4-pentanediamine; Primachin; 8-(4-Amino-1-methylbutylamino)-6-methoxyquinoline;
CAS No.: 90-34-6
Molecular formula: CfifteenHtwenty-oneNthreeO
Structural type:
Molecular weight: 259.34700
Precision quality: 259.16800
PSA：60.17000
LogP：3.55600
Physicochemical properties
Boiling point: 175-179 º C
Melting point: 200 ～ 205 ℃ (decomposition)
Its phosphate is commonly used.Orange red crystal powder, bitter in taste.This product is dissolved in water and insoluble in chloroform or ether.
security information
Customs code: 2933499090[1]
purpose
It has a strong insecticidal effect on the infrared phase of Plasmodium vivax and the gametophytes of various types of malaria parasites, and is an effective drug to eradicate Plasmodium vivax and block the transmission of various types of malaria.Primaquine has weak effect on erythrocytic schizoites, but has no effect on erythrocytic schizoites of Plasmodium falciparum. Therefore, it cannot be used to control symptoms.It is used to control the recurrence and transmission of vivax and three-day malaria and prevent the transmission of falciparum malaria[1]。
Pharmacopoeia standard
Announce
edit
[Identification] (1) Take about 10mg of this product, add 5ml of water to dissolve it, add 1ml of 5% ammonium cerium sulfate dilute nitric acid solution, and it will appear dark purple.(2) Take this product, add 0.01mol/L hydrochloric acid solution to make a solution containing about 15 µ g per lml, and determine it by ultraviolet visible spectrophotometry (Appendix IVA). The maximum absorption is at 265nm and 282nm, and the absorbance is 0.50-0.52 and 0.49-0.51 respectively.(3) The infrared absorption spectrum of this product should be consistent with the control spectrum (spectrum set 578 figure).(4) Take about 50mg of this product, add 5ml of water to dissolve it, add 2ml of sodium hydroxide test solution, shake up, filter, neutralize the filtrate with dilute nitric acid, and then identify the phosphate reaction (Appendix III).
[Inspection] Acidity: Take 0.50g of this product, add 50ml of water to dissolve it, and then measure it according to the law (Appendix VI H). The pH value should be 2.5~3.5.Related substances Take this product and prepare a solution containing 10mg per 1ml with water methanol (1:1) as the test solution;Precisely test appropriate amount, dilute with the same solvent to a solution containing 0.2mg, 0.1mg and 0.02mg per 1ml as the reference solution (1), (2) and (3).Carry out the thin layer chromatography (Appendix V B) test. Take 10 µ l of each of the four solutions and dab them on the same silica gel GF254 thin layer plate respectively. With ethyl acetate isopropanol concentrated ammonia solution (43:35:5) as the developing agent, develop them, dry them in the air, and inspect them under the ultraviolet light (254mn).The control solution (3) should show an obvious spot;If there are no more than 2 impurity spots below the main spot of the test solution, it should not be deeper than the main spot of the reference solution (2). If there is more than one spot, it should not be deeper than the main spot of the reference solution (1).Residual solvents: methanol, ethanol and toluene Take about 0.2g of this product, weigh it accurately, place it in a top empty bottle, add 5ml of water precisely, seal it, shake it to dissolve it, and use it as the test solution.Take another methanol, ethanol and toluene, weigh them precisely, add water to dissolve them and dilute them to prepare a mixed solution containing 0.12mg, 0.2mg and 35.6 µ g per 1ml, respectively. Weigh 5ml precisely and place them in an empty top bottle, seal them, and use them as the reference solution.Test according to the residual solvent determination method (Appendix Ⅷ P Method 2), and use 6% cyanopropylphenyl-94% dimethyl polysiloxane (or similar polarity) as the capillary column of the fixed liquid;The initial temperature is 40 ℃, and the temperature is maintained for 10 minutes. The temperature is raised to 200 ℃ at the rate of 10 ℃ per minute, and the temperature is maintained for 4 minutes;The sample inlet temperature is 250 ℃, and the detector temperature is 300 ℃;The balance temperature of the headspace bottle is 85 ℃, the balance time is 45 minutes, the temperature of the injection probe is 100 ℃, and the temperature of the transmission line is 110 ℃.Take the headspace sample of the reference solution, and the resolution between the components should meet the requirements.Then take the test solution and the reference solution into the headspace respectively, record the chromatogram, and calculate the peak area according to the external standard method, which should meet the requirements.Loss on drying Take the product, dry it at 105 ℃ to constant weight, and the weight loss shall not exceed 0.5% (Appendix VIII L).
[Content determination] Take about 0.15g of this product, weigh it accurately, add 40ml of glacial acetic acid to dissolve it, titrate it with perchloric acid titrant (0.1mol/L) according to the potentiometric titration method (Appendix VII A), and correct the titration result with blank test.Each lml of quotient chlorate titrant (0. lmol/L) is equivalent to 22.77mg of C15H21N30 · 2H3P04.
[Category] Anti disease drugs.
[Storage] Protect from light and seal.
Drug description
Announce
edit
pharmacology
This product and pamaquine belong to 8-aminoquinoline derivatives, and its antimalarial effect may be related to interfering with the DNA synthesis of plasmodium.Primaquine can inhibit the oxidation of mitochondria and reduce the oxygen uptake of malaria parasites.Quinoline quinone derivatives, the metabolites of this product in vivo, are highly oxidizing, which can transform reduced glutathione in red blood cells into oxidized glutathione, interfere with the reduction process of pyridine triphosphate nucleotides in the infrared phase of the malaria parasite, affect the energy metabolism and respiration of the malaria parasite and cause death.It has strong killing effect on infrared phase and gametophyte, and is an effective drug to prevent recurrence and interrupt transmission.After oral administration, the absorption is rapid and complete, reaching the peak blood concentration in 1-3 hours;It disappeared quickly, and there was little residual in the blood after 8 hours.T1/2 is about 5.8 hours.Vd is 205L.The total amount of urinary excretion is only about 1% of the oral dose, and the rest is its metabolites.Because the effective concentration in blood is not maintained for a long time, it must be used continuously every day.
indication
It is mainly used to eradicate vivax malaria and control malaria transmission. It is often used in combination with chloroquine or pyrimethamine.It has weak effect on the erythrocytic phase, but has no effect on the erythrocytic phase of falciparum malaria, and cannot be used as a drug to control symptoms.It also has an impact on the pre erythrocytic stage of some malaria parasites, but because the required dosage is large, it is close to the maximum and is not safe enough, so it cannot be used as a preventive medicine for the cause of disease.
Usage and dosage
Due to different dosage forms and specifications, please read the drug manual carefully or follow the doctor's advice.
Adverse reactions
(1) It is more toxic than other antimalarial drugs.When the daily dose exceeds 52.8 mg, fatigue, dizziness, nausea, vomiting, abdominal pain, cyanosis, drug fever and other symptoms are likely to occur, and they can recover automatically after stopping the drug.(2) A few idiosyncratic patients may have acute hemolytic anemia (because their red blood cells lack glucose 6-phosphate dehydrogenase), so they should stop taking the medicine immediately, and give dexamethasone or prednisone to alleviate it, and intravenous drip 5% glucose and sodium chloride injection, and blood transfusion in severe cases.In case of methemoglobinemia, methylene blue l~2mg/kg can be injected intravenously.
contraindication
It is forbidden for pregnant women.
matters needing attention
Patients with liver, kidney and blood system diseases and diabetes should use it with caution.
preparation
Tablets: each tablet contains 13.2mg of primaquine phosphate (equivalent to 7.5mg of primaquine base).
