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Sodium para-aminosalicylate (Tablets, Granules, Solution, Lyophilisate) Instructions for Use

ATC Code

J04AA01 (Aminosalicylic acid)

Active Substance

Aminosalicylate sodium (USP United States Pharmacopeia)

Clinical-Pharmacological Group

Antituberculosis drug

Pharmacotherapeutic Group

Antitubercular agent

Pharmacological Action

Antituberculosis agent, it is the sodium salt of aminosalicylic acid. Para-aminosalicylic acid and its sodium salt possess bacteriostatic activity against Mycobacterium tuberculosis and belong to the main antituberculosis drugs.

Pharmacokinetics

When taken orally, sodium para-aminosalicylate is well absorbed and penetrates into the blood serum and tissues of internal organs. Absorption is high; it moderately penetrates into the cerebrospinal fluid (only with meningeal inflammation).

It easily passes through histohematic barriers and is distributed in tissues. Protein binding is 50-60%. It is metabolized in the liver and partially in the stomach. T1/2 is 0.5-1 hour. 80% is excreted by the kidneys via glomerular filtration (50% as an acetylated derivative). The total clearance depends on both the rate of metabolism and renal excretion.

Indications

  • Tuberculosis (various forms and localizations) in combination with other antituberculosis drugs.

ICD codes

ICD-10 code Indication
A15 Respiratory tuberculosis, bacteriologically and histologically confirmed
A17 Tuberculosis of nervous system
A18 Tuberculosis of other organs
ICD-11 code Indication
1B10.0 Respiratory tuberculosis, bacteriologically or histologically confirmed
1B11.Z Tuberculosis of nervous system, unspecified
1B12 Tuberculosis of other systems and organs

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Granules, Solution, Lyophilisate

It is taken orally. For adults, the daily dose is 10-12 g, frequency of administration is 2-3 times/day. For children – 150-300 mg/kg/day, frequency of administration is 3-4 times/day.

Tablets

The drug is taken orally 1/2-1 hour after meals, washed down with milk, alkaline mineral water, or a 0.5-2% sodium bicarbonate solution.

For adults – 9-12 g/day in 3-4 doses; for debilitated adult patients (with body weight less than 50 kg) – 6 g/day in 3-4 doses.

For children — 0.2 g/kg/day in 3-4 doses, maximum dose 10 g/day.

Adverse Reactions

From the digestive system decreased or loss of appetite, increased salivation, nausea, vomiting, flatulence, abdominal pain, diarrhea or constipation; increased activity of hepatic transaminases, hyperbilirubinemia, jaundice; rarely – drug-induced hepatitis (including fatal cases).

From the hematopoietic system rarely – thrombocytopenia, leukopenia (up to agranulocytosis), B12-deficiency anemia, hemolytic anemia with a positive Coombs test.

From the urinary system proteinuria, hematuria, crystalluria.

Allergic reactions rash (urticaria, purpura, enanthema, exfoliative dermatitis, syndrome resembling infectious mononucleosis or lymphoma), fever, bronchospasm, arthralgia, eosinophilia.

Other in large doses – antithyroid action; with prolonged use – goitrogenic effect, drug-induced hypothyroidism, myxedema; pericarditis, hypoglycemia, optic neuritis, encephalopathy, Loeffler’s syndrome (eosinophilic pneumonia, migrating pulmonary infiltrate), vasculitis, decreased prothrombin.

Contraindications

  • Renal/hepatic failure;
  • Decompensated chronic heart failure;
  • Gastric and duodenal ulcer;
  • Epilepsy;
  • Enterocolitis (exacerbation);
  • Myxedema (exacerbation);
  • Lactation period;
  • Children under 12 years;
  • Hypersensitivity to aminosalicylic acid and its salts and to the excipients of the drug.

With caution: pregnancy, moderately severe hepatic failure, glucose-6-phosphate dehydrogenase deficiency, compensated hypothyroidism.

Use in Pregnancy and Lactation

The drug should be used with caution during pregnancy.

Contraindicated during lactation.

Use in Hepatic Impairment

Contraindicated in hepatic failure.

With caution: moderately severe hepatic failure. During treatment, it is recommended to monitor the activity of hepatic transaminases.

Use in Renal Impairment

Decreased renal function against the background of tuberculous intoxication or specific lesions is not a contraindication for prescription.

Contraindicated in renal failure.

Pediatric Use

Contraindicated in children under 12 years.

For children — 0.2 g/kg/day in 3-4 doses, maximum dose 10 g/day.

Special Precautions

It is used in combination with more active antituberculosis drugs.

During treatment, it is recommended to monitor the activity of hepatic transaminases.

Decreased renal function against the background of tuberculous intoxication or specific lesions is not a contraindication for prescription.

The development of proteinuria and hematuria requires temporary withdrawal of the drug.

Overdose

Symptoms possible intensification of dose-dependent adverse effects.

Treatment drug withdrawal, symptomatic therapy.

Drug Interactions

It is compatible with other antituberculosis drugs.

It delays the emergence of resistance to isoniazid and streptomycin. When used concomitantly with isoniazid, it increases its blood concentration due to competition for common metabolic pathways.

It impairs the absorption of rifampicin, erythromycin, and lincomycin.

It impairs the absorption of cyanocobalamin (possible development of B12-deficiency anemia).

Antacids do not impair the absorption of the drug.

It enhances the effect of indirect anticoagulants – coumarin and indandione derivatives (dose adjustment of anticoagulants is required).

When using iodine-containing thyroid hormones, their analogues and antagonists (including antithyroid agents), it should be taken into account that against the background of PAS, the concentration of T4 and TSH in the blood changes.

Ammonium chloride increases the risk of crystalluria.

Concomitant use with ethionamide increases the risk of hepatotoxicity.

Diphenhydramine reduces the effectiveness of aminosalicylic acid.

Probenecid reduces the excretion of aminosalicylic acid, increasing its plasma concentration.

Storage Conditions

The drug should be stored in a dry, light-protected place, at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life – 2 years. Do not use after the expiration date

Dispensing Status

For hospitals.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Marketing Authorization Holder

Rusan Pharma, Ltd. (India)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Lyophilisate for preparation of solution for infusion 13.49 g: vial 1 pc.

Dosage Form, Packaging, and Composition

Lyophilisate for preparation of solution for infusion 1 vial
Sodium para-aminosalicylate 13.49 g

13.49 g – vials (1) – cardboard packs.

Marketing Authorization Holder

ZiO-Health CJSC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Enteric-coated tablets 1 g: 50, 100, 500 or 1000 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated tablets 1 tab.
Sodium para-aminosalicylate 1 g

50 pcs. – polymer jars (1) – cardboard packs.
100 pcs. – polymer jars (1) – cardboard packs.
500 pcs. – polyethylene bags (1) – polymer containers.
1000 pcs. – polyethylene bags (1) – polymer containers.

Marketing Authorization Holder

ZiO-Health CJSC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Coated granules for oral use 80 g/100 g: 4 g sachet 1 or 1000 pcs., 100 g sachet or jar

Dosage Form, Packaging, and Composition

Coated granules for oral use 100 g of granules
Sodium para-aminosalicylate 80 g

4 g – Sachets made of combined material (1) – cardboard packs.
4 g – Sachets made of combined material (1000) – cardboard boxes.
100 g – polymer jars (1) with a measuring spoon – cardboard packs.
100 g – bags (1) with a measuring spoon – cardboard packs.

Marketing Authorization Holder

Interpharma, LLC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Enteric-coated film-coated tablets, 1000 mg: 10, 30, 50, or 100 pcs.

Dosage Form, Packaging, and Composition

Enteric-soluble, film-coated tablets from light pink to dark pink, capsule-shaped, biconvex; on the cross-section, the tablet core is white or almost white.

1 tab.
Sodium para-aminosalicylate dihydrate 1000 mg

Excipients : microcrystalline cellulose (type 101) – 60 mg, povidone K30 – 10 mg, colloidal silicon dioxide – 14 mg, talc – 8 mg, magnesium stearate – 8 mg.

Shell composition cellacefate – 70 mg, dibutyl phthalate – 20 mg, titanium dioxide – 9.5 mg, dye ponceau 4R – 0.5 mg.

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (5) – cardboard packs.
10 pcs. – contour cell packs (10) – cardboard packs.

Marketing Authorization Holder

Ozon, LLC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Enteric-soluble, film-coated tablets 1000 mg: 100, 200, 300, 400, 500 or 1000 pcs.

Dosage Form, Packaging, and Composition

Enteric-soluble, film-coated tablets white or almost white, oval, with a score; on the cross-section, two layers are visible: a core of white or white with a yellowish or brownish tint and a coating – white or almost white.

1 tab.
Sodium para-aminosalicylate 1000 mg

Excipients : microcrystalline cellulose (MCC-101) – 55 mg, povidone K25 – 34.4 mg, citric acid monohydrate – 10 mg, calcium stearate – 10 mg, polysorbate 80 – 5.6 mg, colloidal silicon dioxide – 5 mg.

Shell composition : mixture “Acryl-EZE WHITE 93A” – 72 mg, incl. methacrylic acid and ethyl acrylate copolymer [1:1] – 47.52 mg, talc – 11.88 mg, titanium dioxide – 10.8 mg, colloidal silicon dioxide – 0.72 mg, sodium bicarbonate – 0.72 mg, sodium lauryl sulfate – 0.36 mg, triethyl citrate – 8 mg.

100 pcs. – jars (1) – cardboard packs (for hospitals).
200 pcs. – jars (1) – cardboard packs (for hospitals).
300 pcs. – jars (1) – cardboard packs (for hospitals).
400 pcs. – jars (1) – cardboard packs (for hospitals).
500 pcs. – jars (1) – cardboard packs (for hospitals).
1000 pcs. – jars (1) – cardboard packs (for hospitals).

Marketing Authorization Holder

Ozon, LLC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Enteric-coated film-coated tablets, 500 mg: 10, 50, 100, 250, 372, or 500 pcs.

Dosage Form, Packaging, and Composition

Enteric-soluble, film-coated tablets white or almost white, round, biconvex; on the cross-section, two layers are visible: a core of white or almost white with a yellowish or brownish tint and a coating of white or almost white.

1 tab.
Sodium aminosalicylate dihydrate 500 mg

Excipients : microcrystalline cellulose – 27.5 mg, povidone K25 – 17.2 mg, citric acid monohydrate – 5 mg, calcium stearate – 5 mg, polysorbate 80 – 2.8 mg, colloidal silicon dioxide – 2.5 mg.

Coating Acryl-EZE WHITE 93A – 36 mg, incl. methacrylic acid and ethyl acrylate copolymer [1:1] – 66%, talc – 16.5%, titanium dioxide – 15%, colloidal silicon dioxide – 1%, sodium bicarbonate – 1%, sodium lauryl sulfate – 0.5%, triethyl citrate – 4 mg.

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (5) – cardboard packs.
10 pcs. – contour cell packs (10) – cardboard packs.
50 pcs. – contour cell packs (1) – cardboard packs.
50 pcs. – contour cell packs (5) – cardboard packs.
50 pcs. – contour cell packs (10) – cardboard packs.
50 pcs. – jars (1) – cardboard packs.
100 pcs. – jars (1) – cardboard packs.
372 pcs. – jars (1) – cardboard packs.
500 pcs. – jars (1) – cardboard packs.

Marketing Authorization Holder

Rapharma, JSC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Enteric-coated tablets 1 g: 500 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated tablets 1 tab.
Sodium para-aminosalicylate 1 g

500 pcs. – polyethylene bags (1) – polyethylene jars.
500 pcs. – polyethylene bags (1) – polypropylene jars.

Marketing Authorization Holder

S.P. Incomed, LLC (Russia)

Manufactured By

Pharmconcept, LLC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Enteric-coated tablets 1 g: 10, 30, 50 or 100 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated tablets from light pink to dark pink, capsule-shaped, biconvex; on the cross-section, the tablet core is white or almost white.

1 tab.
Sodium para-aminosalicylate 1 g

Excipients : microcrystalline cellulose – 30 mg, povidone K30 – 10 mg, colloidal silicon dioxide – 8 mg, talc – 7 mg, magnesium stearate – 5 mg.

Shell composition cellacephate – 64 mg, dibutyl phthalate – 18 mg, titanium dioxide – 7.5 mg, purple dye (Ponceau 4R) – 0.5 mg.

10 pcs. – blisters (1) – cardboard packs.
10 pcs. – blisters (3) – cardboard packs.
10 pcs. – blisters (5) – cardboard packs.
10 pcs. – blisters (10) – cardboard packs.

Marketing Authorization Holder

Pharmasintez, JSC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Coated granules for oral use 80 g/100 g: 4 g sachets 1 or 10 pcs., 5 g sachets 10 or 100 pcs., 100 g sachets

Dosage Form, Packaging, and Composition

Enteric-coated granules for oral use 100 g of granules
Sodium para-aminosalicylate 80 g

4 g – sachets (1) – cardboard packs.
4 g – sachets (10) – cardboard packs.
5 g – sachets (10) – cardboard packs.
5 g – sachets (100) – cardboard boxes.
100 g – sachets (1) with a measuring spoon – cardboard packs.

Marketing Authorization Holder

Pharmconcept, LLC (Russia)

Manufactured By

Pharmconcept, LLC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Enteric-coated film-coated tablets, 500 mg: 50 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated film-coated tablets white, oval, biconvex; on the cross-section, the core is white or almost white with a slightly creamy-yellowish or pinkish tint.

1 tab.
Sodium para-aminosalicylate dihydrate 500 mg

Excipients: microcrystalline cellulose type 101 – 15 mg, povidone K30 – 5 mg, colloidal silicon dioxide – 4 mg, talc – 3.5 mg, magnesium stearate – 2.5 mg.

Ready enteric coating “VIVACOAT®” (53 mg): methacrylic acid and ethyl acrylate copolymer type B – 67.5%, talc – 21.25%, triethyl citrate – 6.75%, titanium dioxide – 4.5%.

10 pcs. – contour cell packs (5) – cardboard packs.
50 pcs. – jars – cardboard packs.
50 pcs. – jars – cardboard packs (for hospitals).
100 pcs. – jars – cardboard packs (for hospitals).
500 pcs. – jars – cardboard packs (for hospitals).

Marketing Authorization Holder

Pharmconcept, LLC (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate Enteric-coated film-coated tablets 1000 mg: 50 or 100 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated film-coated tablets from light pink to dark pink, oval, biconvex; on the cross-section, the tablet core is white or almost white with a slightly yellowish or pinkish tint.

1 tab.
Sodium para-aminosalicylate dihydrate 1000 mg

Excipients: microcrystalline cellulose type 102 – 30 mg, povidone K30 – 10 mg, colloidal silicon dioxide – 8 mg, talc – 7 mg, magnesium stearate – 5 mg.

Composition of the coating Vinkoat WT-NAQ-01319 red: methacrylic acid and ethyl acrylate copolymer – 67.5%, triethyl citrate – 0.6%, silicon dioxide – 6.25%, titanium dioxide – 4.5%, talc – 19.9%, crimson dye [Ponceau 4R] aluminum lake – 1.2%, indigo carmine aluminum lake – 0.05%.

10 pcs. – contour cell packs (5) – cardboard packs.
50 pcs. – jars – cardboard packs.
100 pcs. – jars – cardboard packs (for hospitals).
500 pcs. – jars – cardboard packs (for hospitals).

Marketing Authorization Holder

Advanced Trading, LLC (Russia)

Manufactured By

Advanced Pharma, LLC (Russia)

Dosage Forms

Bottle Rx Icon Sodium para-aminosalicylate Enteric-coated tablets 200 mg: 100, 372 or 500 pcs.
Enteric-coated tablets 500 mg: 100, 372 or 500 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated tablets white or almost white with a creamy tint, round, biconvex; on the cross-section, the core is from white to yellowish.

1 tab.
Sodium para-aminosalicylate dihydrate 200 mg

Excipients: sorbitol – 7 mg, povidone (K-30) – 6.6 mg, colloidal silicon dioxide (aerosil 300) – 2.2 mg, calcium stearate – 2.2 mg, citric acid monohydrate – 2 mg.

Shell composition: film coating – 22 mg:(methacrylic acid and ethyl acrylate copolymer [1:1] – 40%, talc – 37.25%, titanium dioxide – 15%, triethyl citrate – 4.8%, colloidal silicon dioxide – 1.25%, sodium bicarbonate – 1.2%, sodium lauryl sulfate – 0.5%)

100 pcs. – polyethylene bags (1) – polymer jars (8) – group packaging (for hospitals).
372 pcs. – polyethylene bags (1) – polymer jars (8) – group packaging (for hospitals).
500 pcs. – polyethylene bags (1) – polymer jars (8) – group packaging (for hospitals).

Enteric-coated tablets white or almost white with a creamy tint, round, biconvex; on the cross-section, the core is from white to yellowish.

1 tab.
Sodium para-aminosalicylate dihydrate 500 mg

Excipients: sorbitol – 17.5 mg, povidone (K-30) – 16.5 mg, colloidal silicon dioxide (aerosil 300) – 5.5 mg, calcium stearate – 5.5 mg, citric acid monohydrate – 5 mg.

Shell composition: film coating – 22 mg:(methacrylic acid and ethyl acrylate copolymer [1:1] – 40%, talc – 37.25%, titanium dioxide – 15%, triethyl citrate – 4.8%, colloidal silicon dioxide – 1.25%, sodium bicarbonate – 1.2%, sodium lauryl sulfate – 0.5%)

100 pcs. – polyethylene bags (1) – polymer jars (8) – group packaging (for hospitals).
372 pcs. – polyethylene bags (1) – polymer jars (8) – group packaging (for hospitals).
500 pcs. – polyethylene bags (1) – polymer jars (8) – group packaging (for hospitals).

Marketing Authorization Holder

Binergia JSC (Russia)

Manufactured By

Armavir Biopharmaceutical Plant, FSE (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate-Binergia Lyophilisate for preparation of solution for infusion 13.49 g: vial 1, 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Lyophilisate for preparation of solution for infusion as a white or almost white powder.

1 vial
Sodium para-aminosalicylate (calculated as 100% anhydrous substance) 13.49 g
   (equivalent to 11.72 g of free aminosalicylic acid and 1.77 g of sodium ions)

13.49 g – colorless glass vials with a capacity of 500 ml (1) with trans-flo – cardboard packs.
13.49 g – colorless glass vials (5) with trans-flo – cardboard boxes (for hospitals).
13.49 g – colorless glass vials (10) with trans-flo – cardboard boxes (for hospitals).

Marketing Authorization Holder

Binergia JSC (Russia)

Manufactured By

Kursk Biopharmaceutical Plant – Firm “Biok”, FKP (Russia)

Dosage Form

Bottle Rx Icon Sodium para-aminosalicylate-Binergia Infusion solution 30 mg/1 mL: 200 mL or 400 mL bottle

Dosage Form, Packaging, and Composition

Infusion solution clear, colorless or with a yellowish tint.

1 ml
Sodium aminosalicylate dihydrate (calculated as 100% anhydrous substance) 30 mg

Excipients: disodium edetate – 0.5 mg, sodium sulfite (calculated as 100% anhydrous substance) – 5 mg, water for injections – up to 1 ml.

200 ml – bottles (1) – cardboard packs.
400 ml – bottles (1) – cardboard packs.
200 ml – bottles (20) – cardboard boxes (for hospitals).
200 ml – bottles (24) – cardboard boxes (for hospitals).
200 ml – bottles (28) – cardboard boxes (for hospitals).
400 ml – bottles (12) – cardboard boxes (for hospitals).
400 ml – bottles (15) – cardboard boxes (for hospitals).

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