Molecular Formula | C7H6NNaO3 |
Molar Mass | 175.12 |
Melting Point | 265-270 °C |
Appearance | crystalline |
Color | white |
Storage Condition | Sealed in dry,Room Temperature |
Physical and Chemical Properties | White or pale white crystals or crystalline powders. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
RTECS | VO1700000 |
EPA chemical substance information | information provided by: ofmpeb.epa.gov (external link) |
Overview | sodium p-aminosalicylate is a white or almost white crystalline powder, soluble in water, slightly soluble in ethanol, insoluble in acetone. It can be used as an anti-tuberculosis drug, mainly for the comprehensive treatment of tuberculosis infection. |
anti-tuberculosis drugs | sodium para-aminosalicylate is a commonly used anti-tuberculosis drug, 4-amino-2-hydroxybenzoic acid sodium dihydrate, PAS-Na, white or almost white crystalline powder, odorless, sweet and salty, soluble in water, slightly soluble in ethanol, insoluble in acetone, almost insoluble in ether, chloroform, benzene. 2% aqueous solution pH6.5 ~ 8. Aqueous solution is easy to remove carbon dioxide into M-aminophenol, so it should be freshly prepared. This product is similar to P-aminobenzoic acid (PABA) in structure, and is the same kind of p-aminobenzoic acid (PABA). It inhibits the growth and reproduction of Mycobacterium tuberculosis by competitive inhibition of folic acid synthesis. This product is only effective against mycobacteria, and is not effective against atypical mycobacteria. When used alone, Mycobacterium tuberculosis can quickly produce drug resistance, this product must be combined with other anti-tuberculosis drugs, such as streptomycin and isoniazid combined with Mycobacterium tuberculosis can delay the emergence of drug resistance to the latter two. Clinically, it is mainly used for pulmonary and extrapulmonary tuberculosis caused by Mycobacterium tuberculosis. Also for hyperthyroidism and has a strong hypolipidemic effect. |
pharmacokinetics | good absorption from gastrointestinal tract. More rapidly absorbed than other salicylic acids. After absorption, it is rapidly distributed into various body fluids, reaching a very high concentration in pleural effusion, but the concentration in cerebrospinal fluid is very low. This product quickly diffused to the kidney, lung and liver tissue, in the caseous tissue up to a higher concentration. Low protein binding rate (15%). After oral administration of 1~2 hours of blood drug concentration peak, the duration of about 4 hours, T1/2 45~60 minutes, renal damage up to 23 hours. This product in the liver metabolism, more than 50% by acetylation into inactive metabolites. After administration, 85% was rapidly excreted by glomerular filtration and tubular secretion within 7-10 hours; 14%-33% was excreted by the kidney as the original form, and 50% was the metabolite. This product can also be excreted by the milk. Hemodialysis can clear this product is unknown. |
indication | is applicable to pulmonary and extrapulmonary tuberculosis caused by Mycobacterium tuberculosis. Sodium p-aminosalicylate is effective only against mycobacteria and not against non-tuberculous mycobacteria. When used alone, it can quickly develop drug resistance, so it must be combined with other anti tuberculosis drugs. The combination of streptomycin and isoniazid can delay the emergence of drug resistance of Mycobacterium tuberculosis to the former two. Mainly used as second-line anti-tuberculosis drugs. It can also be used for hyperthyroidism, which is more suitable for patients with hyperthyroidism complicated with tuberculosis. When the iodine agent is ineffective and affects the operation, it can be used for a short time to create conditions for the operation. Intravenous injection is generally used in severe cases such as tuberculous meningitis. |
medication instructions | (1) When intravenous drip, dissolve in isotonic sodium chloride injection or 5% glucose solution. (2) gastric irritation can be reduced after meals or with antacids. If there is stomach discomfort, the symptoms can be relieved by temporary reduction or temporary withdrawal for 2 weeks, then start with a small dose and gradually increase to a sufficient amount. (3) patients with restricted sodium intake may switch to calcium p-aminosalicylate. (4) patients with renal impairment must be reduced or discontinued. (5) the combination with P-aminobenzoic acid produces antagonism, and the two drugs are not suitable for combination. (6) when combined with ethylisocyanamide, it can increase the side effects. (7) sodium p-aminosalicylate can affect the absorption of rifampicin, resulting in the decrease of the blood concentration of the latter. If the two drugs need to be applied, the interval should be more than 6 hours. (8) with vitamin B12 when taken, can affect the absorption of the latter, should increase the dose of vitamin B12 dig. (9) the intravenous drip solution should be freshly prepared, and the drip should be protected from light. The drip should be finished within 5 hours, and the solution should not be used if it changes color. |
adverse reactions | gastrointestinal symptoms loss of appetite, Nausea, Vomit, stomach burning sensation, pain in the epigastric region, abdominal distension, Diarrhea, it can even cause ulcers and bleeding, and the drug can reduce the reaction after a meal. Liver damage, symptoms of hepatomegaly and tenderness, dark urine (jaundice), elevated GPT, bile stasis, etc., should be immediately discontinued. Allergic reactions such as skin itching, skin rashes, exfoliative dermatitis, drug fever and eosinophilia should be stopped immediately. Long-term use of drugs can cause loss of libido, hypothyroidism, and inhibition of thrombin production. Intravenous drip administration can cause venous sclerosis, phlebitis, or chills, high fever and other reactions. Rare adverse reactions: (1) Long-term medication, occasionally can cause goiter or myxedema, (2) large dose can inhibit the generation of coagulation factor II, so that the time is prolonged. |
precautions | it should be used with caution in patients with hypothyroidism, liver function damage, renal insufficiency, pregnant women and nursing mothers. Ulcer disease, bleeding tendency of patients should not be used. This product is incompatible with anticoagulant drugs, Aminobenzoic acid drugs, probenecid, rifampicin and its semi-synthetic drugs. But with streptomycin, isoniazid and other drugs, synergistic effect. (1) Cross-allergy: to other salicylic acids including methyl salicylate (wintergreen oil) or other amino-containing benzene groups (such as certain sulfa drugs or dyes) allergic patients can also be allergic to this product. (2) congestive heart failure, gastric ulcer, glucose -6-phosphate dehydrogenase deficiency, severe liver function damage, severe renal damage with caution. (3) the solution of intravenous drip should be newly prepared, and the solution should be protected from light, and the solution should not be used if it changes color. Intravenous drip used for a long time is easy to cause phlebitis. (4) There is no confirmed problem for pregnant women, and the effect of combination therapy on the fetus is not clear, but the pros and cons must be weighed. Amino salicylic acid can be excreted by the milk, lactating women must weigh the pros and cons. (5) interference to the diagnosis: sodium aminosalicylate can make the copper sulfate method for the determination of urine sugar false positive; The determination of urobilinogen in urine was false positive reaction (aminosalicylic acid and Ehrlich reagent reaction, production of orange-red turbidity or yellow, the results of some commercially available test strips made according to the above principles can also be affected); Increase the serum alanine aminotransferase and aspartate aminotransferase measurements. |
Use | anti-tuberculosis drugs, mainly used for the comprehensive treatment of tuberculosis infection anti-tuberculosis drugs, mainly for the comprehensive treatment of various tuberculosis infection |
category | toxic substances |
toxicity grade | low toxicity |
Acute toxicity | oral-rat LD50: 8000 mg/kg; Oral-mouse LD50: 6900 mg/kg |
flammability hazard characteristics | flammable; Toxic sodium oxide and nitrogen oxide gases generated during combustion |
storage and transportation characteristics | The warehouse is ventilated and dried at low temperature; Stored separately from alkali |
fire extinguishing agent | water, foam, dry sand, carbon dioxide |