Sodium p-aminosalicylate for injection
Function and Efficacy
[Pharmacology and Toxicology] It has an antibacterial effect only on Mycobacterium tuberculosis. This product is a congener of para-aminobenzoic acid (PABA), which inhibits the growth and reproduction of Mycobacterium tuberculosis by competitive inhibition of folic acid synthesis. [Pharmacokinetics] It is well absorbed from the gastrointestinal tract. It is absorbed more rapidly than other salicylates. After absorption, it is quickly distributed to various body fluids, reaching a very high concentration in pleural effusion, but the concentration in cerebrospinal fluid is very low. This product quickly diffuses to kidney, lung and liver tissues, and can reach a higher concentration in caseous tissue. The protein binding rate is low (15%). The blood drug concentration reaches a peak 1 to 2 hours after oral administration, lasts for about 4 hours, and the half-life (T1/2) is 45 to 60 minutes, which can reach 23 hours in patients with renal impairment. This product is metabolized in the liver, and more than 50% is acetylated to become inactive metabolites. After administration, 85% is rapidly excreted through glomerular filtration and tubular secretion within 7 to 10 hours; 14% to 33% is excreted in its original form through the kidneys, and 50% is metabolites. This product can also be excreted through breast milk. It is unknown whether hemodialysis can remove this product.
Ingredients
The main ingredient of this product is sodium p-aminosalicylate.
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Sodium 4-aminosalicylateIngredients |
It has an antibacterial effect only on Mycobacterium tuberculosis. It inhibits the growth and reproduction of Mycobacterium tuberculosis by competitively inhibiting the synthesis of folic acid. More |
133-10-8 | 8 |
Appearance
This product is white or off-white crystal or crystalline powder.
Indication
It is suitable for pulmonary and extrapulmonary tuberculosis caused by Mycobacterium tuberculosis. Intravenous infusion can be used to treat tuberculous meningitis and acute disseminated tuberculosis. This product is only effective against mycobacteria. When used alone, Mycobacterium tuberculosis can quickly develop drug resistance, so this product must be used in combination with other anti-tuberculosis drugs. When streptomycin and isoniazid are used in combination with this product, it can delay the development of drug resistance of Mycobacterium tuberculosis to the former two. This product is ineffective against atypical mycobacteria. It is mainly used as a second-line anti-tuberculosis drug.
Usage and Dosage
Intravenous drip: 4-12g per day. Add appropriate amount of sterile injection water to dissolve before use, then dilute with 500ml of 5% glucose injection solution, and drip in 2-3 hours. Children: 0.2-0.3g/kg per day.
Adverse Reactions
1. Common symptoms: itchy rash, joint pain and fever, extreme fatigue or weakness, eosinophilia (most commonly caused by allergies). 2. Common symptoms: lower back pain, painful or burning urination (crystallary urine), hematuria; menstrual disorders, chills, decreased male libido, dry skin, swelling in the front of the neck, weight gain (goiter, myxedema); yellowing of the eyes or skin (jaundice, hepatitis); abdominal pain, back pain, pallor (hemolytic anemia, due to G6PD deficiency); fever, headache, rash, sore throat, fatigue (infectious mononucleosis syndrome).
Precautions
Not yet clear.
Special Population Medication
Precautions for children: Use strictly according to the dosage for children. Precautions for pregnancy and lactation: No problems have been confirmed for pregnant women, and the effect of combined therapy on the fetus is currently unclear, but it must be selected after weighing the pros and cons. Aminosalicylic acid can be excreted in breast milk, so breastfeeding women must weigh the pros and cons before using it. Precautions for the elderly: Not yet clear.
Drug Interactions
1. Para-aminobenzoic acid and this product have antagonistic effects, and the two should not be used together; 2. This product can enhance the effect of anticoagulants (coumarin or indandione derivatives), so the dose of oral anticoagulants should be appropriately adjusted when using para-aminosalicylic acid or after using it. 3. When used in combination with ethionamide, adverse reactions may increase. 4. The combination of probenecid or sulfinpyrazone with aminosalicylic acid can reduce the latter's secretion from the renal tubules, leading to increased blood drug concentrations, prolonged duration, and toxic reactions. Therefore, when aminosalicylic acid is used in combination with probenecid or sulfinpyrazone or after the combination, the dose of the former should be appropriately adjusted, and the patient should be closely followed up. However, most people do not use probenecid as an adjuvant drug for aminosalicylic acid treatment. 5. Aminosalicylic acid may affect the absorption of rifampicin, resulting in a decrease in rifampicin blood concentrations.
Storage
Keep away from light and store in a sealed container.
Packaging Specification
2.0g
Validity Period
18 months
Manufacturer
Liaoning PHARMA-UNION Pharmaceutical Co., Ltd.
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Founded in:
2008-05-12 -
Address:
122A Xianghuai Road, Benxi Economic Development Zone -
Tax NO.:
91210500673786474R -
Registered Funds:
110 million yuan -
Email: