Drug Instructions

Alias: dipyrone, NOVALGIN; Noramidopyrine, Metamizole sodium,metamizole Property: This product is white or yellow-white crystal or crystalline powder, odorless, slightly bitter taste, soluble in water. Action: Dipyrone is the derivative of aminopyrine, its has a significant effect of antipyretic analgesia. The antipyretic effect of it is three times as aminopyrine, the analgesic effect is similar to that of aminopyrine. Process vivo: Easily absorbed orally, mainly metabolized by the liver and excreted of renal Indications: It is mainly used for cooling, acute arthritis, headache, rheumatic neuralgia, toothache and muscle pain etc. Dosage Oral or intranasal administration. For oral, the adult should take 0.5g of the medicine and three times a day, the amount of the child is 8-10mg/ kg, the number of the times is according to the necessary. For intranasal, the child under 5 years old can take 1-2drops for each nostril, can take the medicine another time if necessary,for the patient above 5 years old increase the dosage appropriately. Note 1, The dosage should be controled strictly to prevent collapse. 2, The intramuscular injection can cause atrophy and erosion to the local muscle, it is abandoned now. 3, The patient who has a allergy to the praziquantel can not use the dipyrone 4, It not suitable for a long-term application, Please pay attention to the granulocytes. Specification Tablets:each table is weight for 0.25g or 0.5g; Injection: each ingection has the specification of 0.25g/1ml or 0.5g/2ml; Drops: solution with the concentration of 10%~20%

Side effects of dipyrone

1, The side effects contain the allergies, exhaustion, leukopenia, thrombocytopenia even the severe aplastic anemia. 2, Some people may also suffering the nephrotoxicity and gastrointestinal bleeding after they take the dipyrone.The most serious side effect is lethal agranulocytosis.

Hazards & Safety Information

Category Toxic Chemicals Acute toxicity For oral – the lethal dose for rat LD50: 3000 mg/kg; For oral – the lethal dose for mouse LD50: 2891 mg/kg Toxicity grading Moderately toxic Flammability hazard characteristic It is combustible and can produce the toxic fumes contained nitrogen oxides, sulfur oxides and sodium oxide during the combustion Storage Characteristic The storeroom should be airy, low-temperature and dried. Extinguishing agent Dry powder, foam, sand, carbon dioxide, water mist

World Health Organization (WHO)

Metamizole sodium, a pyrazolone derivative with analgesic, antipyretic and antinflammatory activity, was introduced in 1921 and has since been widely available in over-the-counter products. By the early 1970s its use had been associated, as with some other pyrazolones, with serious and sometimes fatal adverse reactions, notably cases of blood dyscrasias including agranulocytosis, which led to its withdrawal by some regulatory authorities. Although preparations of metamirole sodium are prohibited in certain countries, they remain widely available in others and, in some cases, in over-the-counter products.

Safety Profile

Poison by subcutaneous route. Moderately toxic by several other routes. An experimental teratogen. Other experimental reproductive effects. Human mutation data reported. Questionable carcinogen with experimental neoplastigenic data. See also SULFONATES. When heated to decomposition it emits very toxic fumes of NOx,, Na2O, and SOx,.

Synthesis

Methamizole sodium, 1-phenyl-2,3-dimethyl-4-methylaminopyrazolone-5-N-sodium methansulfonate (3.2.16), is synthesized in a multi-stage synthesis from acetoacetic ester and phenylhydrazine. Their reaction leads to the formation of 1-phenyl- 3-methylpyrazolone-5 (3.2.9). Methylation of this product with methyl iodide gives 1-phenyl- 2,3-dimethylpyrazolone-5 (3.2.10). This compound is used independently in medicine as a fever-reducing and anti-inflammatory analgesic under the name antipyrin. It undergoes nitrozation by sodium nitrite in an acidic medium, forming 1-phenyl-2,3-dimethyl-4- nitrozopyrazolone-5 (3.2.11). Reduction of the nitrous derivative (3.2.11) by different reducing agents leads to the formation of 1-phenyl-2,3-dimethyl-4-aminopyrazolone-5 (3.2.12). This product is reacted with benzaldehyde, forming an easily separable crystalline 1-phenyl- 2,3-dimethyl-4-benzylidenaminopyrazolone-5 (3.2.13), which is methylated at the imine atom of nitrogen by dimethylsulfate, giving a quaternary salt (3.2.14). Hydrolysis of the resulting salt gives 1-phenyl-2,3-dimethyl-4-methylaminopyrazolone-5 (3.2.15). Treating the product with a water solution of a mixture of sodium bisulfite and formaldehyde leads to the formation of 1-phenyl-2,3-dimethyl-4-methylaminopyrazolone-5-N-sodium methanesulfonate (3.2.16), the desired sodium methamizole [72–75].

Definition

ChEBI: An organic sodium salt of antipyrine substituted at C-4 by a methyl(sulfonatomethyl)amino group, commonly used as a powerful analgesic and antipyretic.

Brand name

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