What Is Aminopyrine?

The chemical name of aminophenazone is 1-phenyl-2,3-dimethyl-4-dimethylaminopyrazolone, a white or almost white crystalline powder; odorless, slightly bitter; Deterioration; aqueous solution shows alkaline reaction. This product is easily soluble in ethanol or chloroform, and soluble in water or ether. The molecular formula is C ₁₃ H ₁₇ N ₃ O, the molecular weight is 231.29400, the density is 1.17 g / cm3, the melting point is 107-109 ° C (lit.), and the boiling point is 319.7ºC at 760 mmHg.

The chemical name of aminophenazone is 1-phenyl-2,3-dimethyl-4-dimethylaminopyrazolone. It is a white or almost white crystalline powder. Deterioration; aqueous solution shows alkaline reaction. This product is easily soluble in ethanol or chloroform, and soluble in water or ether. The molecular formula is C ₁₃ H ₁₇ N ₃ O, the molecular weight is 231.29400, the density is 1.17 g / cm3, the melting point is 107-109 ° C (lit.), and the boiling point is 319.7ºC at 760 mmHg.

Chinese name

Aminopyrine

Foreign name

aminophenazone

CAS number

58-15-1

Molecular formula

C13H17N3O

Aminopyrine compounds

Aminopyrine Basic Information

Chinese name amino

Chinese alias: Fenoprofen calcium salt hydrate; Piramidon; 4-dimethylamino-2,3-dimethoxy-1-phenylpyrazol-5-one; 4-dimethylamino-1 , 5-dimethyl-2-phenyl-3-pyrazolinone; Annalin impurity D;

English name: aminophenazone

English alias: 4- (dimethylamino) -1,5-dimethyl-2-phenylpyrazol-3-one; 4-Dimethylaminoantipyrine; 3H-Pyrazol-3-one, 4- (dimethylamino) -1,2-dihydro-1,5 -dimethyl-2-phenyl-;

CAS number: 58-15-1

Molecular formula: C ₁₃ H ₁₇ N ₃ O

Molecular weight: 231.29400

Structural formula:

Exact mass: 231.13700

PSA: 30.17000

LogP: 1.55040 ^[1]

Aminopyrine physical and chemical properties

Appearance and properties: white crystalline powder

Density: 1.17g / cm3

Melting point: 107-109 ° C (lit.)

Boiling point: 319.7ºC at 760mmHg

Flash point: 125.9ºC

Refractive index: 1.614

Water solubility: 5.55 g / 100 mL

Stability: Stable. Incompatible with strong oxidizing agents, strong acids, strong bases. Light sensitive. Degrades under the action of mild oxidizing agents in the presence of moisture or water.

Storage conditions: Store in a tightly closed container. Store in a cool, dry, well-ventilated area away from incompatible substances. Store protected from light. ^[1]

Aminopyrine Pharmacopoeia Standard

Aminopyrine source

This product is 1-phenyl-2,3-dimethyl-4-dimethylaminopyrazolone [5]. Containing C13H17N3O shall not be less than 99.0%. ^[2]

Aminopyrine traits

This product is a white or almost white crystalline powder; odorless, slightly bitter; it can be altered in the presence of light; the aqueous solution is alkaline. This product is easily soluble in ethanol or chloroform, and soluble in water or ether. Melting point The melting point (page 13 of the Appendix) of this product is 107 to 109 ° C. ^[2]

Aminopyrine identification

Take about 0.6g of this product, add 15ml of water to dissolve, and test according to the following method:

(1) Take 5ml of solution, add 3 drops of dilute hydrochloric acid and 1ml of ferric chloride test solution, it will become violet-colored; add a few drops of dilute sulfuric acid to turn purple.

(2) Take 5ml of the solution, add 5 drops of silver nitrate test solution, it will become violet-colored, and gray-black metallic silver will gradually precipitate.

(3) Take 5ml of solution and add dilute potassium ferricyanide test solution, which is dark blue or precipitation occurs (different from antipyrine). ^[2]

Aminopyrine check

Take 0.5g of this product, add 15ml of water to dissolve it, add 3ml of dilute nitric acid and 1ml of silver nitrate test solution, and shake well; if turbidity occurs, compare with the control solution made of 1ml of standard sodium chloride solution, it must not be more concentrated ( 0.002%). Antipyrine and aminoantipyrine take 0.1g of this product, add 0.1g of vanillin and 7ml of sulfuric acid solution (2 7), heat in a water bath for 5 minutes and shake from time to time. Liquid [take 0.1 g of vanillin, add 7 ml of sulfuric acid solution (2 7), heat in a water bath for 5 minutes and shake constantly].

Take 0.5g of this product for easy carbonization, check according to law, the solution should be almost colorless.

The burning residue shall not exceed 0.1%.

Take 1g of this product, add 4ml of hydrochloric acid solution (1mol / L) and water to dissolve it into 25ml, check according to law, the content of heavy metal must not exceed 15 parts per million. ^[2]

Determination of aminopyrine content

Take about 1g of this product, accurately weigh, add 40ml of water, dissolve it warmly, let it cool, add 0.15ml of methyl orange-methylene blue mixed indicator liquid, and titrate with hydrochloric acid solution (0.5mol / L) until the color of the solution Consistent with the control solution [take 50ml of water, add the above mixed indicator solution 0.15ml and hydrochloric acid solution (0.5mol / L) 0.05ml], subtract 0.05ml from the number of ml of the consumed hydrochloric acid solution (0.5 mol / L) to obtain. Each 1 ml of hydrochloric acid solution (0.5 mol / L) is equivalent to 115.6 mg of C ₁₃ H ₁₇ N ₃ O. ^[2]

Aminopyrine Compound Related Drugs

Aminopyrine drug name:

[Common name] Aminopyrine caffeine tablets

[English name] Aminopyrine and Caffeine Tablets

[Chinese Pinyin] An Ji Bi Lin Ka Fei Yin Pian ^[3]

Aminopyrine ingredients:

This product is a compound tablet. Its main ingredients are: 150mg aminopyrine and 40mg caffeine. ^[3]

Aminopyrine properties:

This product is a white tablet. ^[3]

Aminopyrine indications:

It is used to alleviate symptoms such as fever and headache caused by colds and upper respiratory tract infections. It can also be used for neuralgia, rheumatism and toothache. ^[3]

Aminopyrine usage and dosage:

oral. 1-2 tablets at a time, 3 times a day, or as directed by your doctor. ^[3]

Aminopyrine adverse reactions:

1. Gastrointestinal damage can cause indigestion, mucous membrane erosion, bleeding from gastric and duodenal ulcers.
2. Renal damage is manifested in acute renal insufficiency, interstitial nephritis, renal papillary necrosis, water and sodium retention, and hyperkalemia.
3 Liver damage. Large doses of aminopyrine can cause liver damage and cause jaundice and hepatitis.
4 other. This product can cause headaches, dizziness, tinnitus, optic neuritis and other central nervous system diseases; aminopyrine can cause granulocytopenia. ^[3]

Aminopyrine is contraindicated:

1. Patients with gastrointestinal bleeding are contraindicated.
2. Peptic ulcers are disabled. ^[3]

Aminopyrine precautions:

1. Patients who cannot tolerate non-steroidal anti-inflammatory drugs or use non-steroidal anti-inflammatory drugs in large doses, are elderly, have a history of gastrointestinal bleeding, history of ulcers, or use glucocorticoids and anticoagulants at the same time can cause stomach Intestinal damage should be used with caution.
2. Elderly with heart, liver, kidney and other complications, those who use diuretics, this product is easy to cause kidney damage, should be used with caution.
3 Aminopyrine can cause granulocytopenia, and long-term or large doses of this product should be checked for blood. ^[3]

Medication for pregnant and lactating women:

still uncertain. ^[3]

Aminopyrine for the elderly:

Reduce or use with caution in elderly patients. ^[3]

Aminopyrine drug interactions:

still uncertain. ^[3]

Aminopyrine pharmacology and toxicology:

This product is an antipyretic and analgesic. Aminopyrine is a pyrazolone antipyretic and analgesic anti-inflammatory drug, which can inhibit the synthesis and release of prostaglandin E ₁ in neurons in the anterior hypothalamus, restore body temperature and regulate the normal responsiveness of central sensory neurons and play an antipyretic effect. Aminopyrine can also inhibit the synthesis and release of prostaglandins in inflammatory local tissues, stabilize the lysosomal membrane, affect the phagocytosis of phagocytic cells, and play an anti-inflammatory effect. As a central stimulant, caffeine can excite the cerebral cortex, improve the sensitivity to the outside world, and has the effect of constricting cerebral blood vessels to strengthen aminopyrine to relieve headaches, and has a synergistic antipyretic analgesic effect. ^[3]