Aminosalicylic acid (Tablets, Solution, Lyophilisate) Instructions for Use

Instructions
Dosage forms

ATC Code

J04AA01 (Aminosalicylic acid)

Active Substance

Aminosalicylate sodium (USP Pharmacopoeia)

Clinical-Pharmacological Group

Antituberculosis drug

Pharmacotherapeutic Group

Agents active against mycobacteria; antituberculosis agents; aminosalicylic acid and its derivatives

Pharmacological Action

Antituberculosis agent, which is the sodium salt of aminosalicylic acid. Aminosalicylate sodium (para-aminosalicylate sodium) has a bacteriostatic effect.

It is active only against Mycobacterium tuberculosis. Compared to other antituberculosis drugs, it has a weaker effect. When used as monotherapy, resistance to aminosalicylic acid develops rapidly.

Pharmacokinetics

Absorption is high. In case of meningeal inflammation, it penetrates into the cerebrospinal fluid to a moderate extent.

It easily penetrates histohematic barriers and is distributed in tissues. It undergoes metabolism. 50% of the dose is determined in the urine as an acetylated derivative. T_1/2 is 30 min. The total clearance depends on both the rate of metabolism and renal excretion.

Indications

Treatment of tuberculosis when it is not possible to use other, more potent agents.

ICD codes

Open the list of 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.

Administer all formulations orally with food or immediately after meals to minimize gastrointestinal irritation.

For adult patients, the total daily dose is 10-12 grams. Divide this daily dose into 2-3 equally spaced administrations.

For pediatric patients, calculate the total daily dose as 150-300 mg per kilogram of body weight. Do not exceed the maximum adult daily dose. Divide the calculated daily dose into 3-4 equally spaced administrations.

Always use aminosalicylic acid as part of a combination therapy regimen with other antituberculosis drugs to prevent the rapid development of resistance.

Adjust the dosage interval or total daily dose with particular caution in patients with any degree of renal or hepatic impairment, even if not severe enough to be a formal contraindication.

Regularly monitor renal function, hepatic function, and serum potassium levels during treatment due to risks of nephrotoxicity, hepatotoxicity, and hypokalemia.

Instruct patients to swallow tablets whole and not to crush or chew them. For the solution or reconstituted lyophilisate, advise patients to mix the dose in a acidic fruit juice or carbonated beverage immediately before ingestion to mask the unpleasant taste and improve stability.

Adverse Reactions

Possible nausea, vomiting, diarrhea, hypokalemia.

Rarely skin reactions, fever, arthralgia, lymphadenopathy, hepatosplenomegaly, a syndrome similar to infectious mononucleosis, jaundice, encephalitis, renal failure, hemolytic anemia in patients with glucose-6-phosphate dehydrogenase deficiency, agranulocytosis, eosinophilia, leukopenia, thrombocytopenia.

In isolated cases psychoses.

With long-term use in high doses hypothyroidism, goiter.

Contraindications

Renal and/or hepatic failure, hepatitis, liver cirrhosis, amyloidosis of internal organs, gastric and duodenal ulcer, myxedema, epilepsy, pregnancy, hypersensitivity to aminosalicylic acid and its salts.

Use in Pregnancy and Lactation

Use is contraindicated during pregnancy.

Aminosalicylic acid is excreted in small amounts in breast milk.

Use in Hepatic Impairment

Contraindicated in hepatic failure, hepatitis, liver cirrhosis. Use with particular caution in patients with impaired liver function.

Use in Renal Impairment

Contraindicated in renal failure. Use with particular caution in patients with impaired renal function.

Pediatric Use

Used according to indications in children.

Geriatric Use

Use with caution, taking into account the state of renal function.

Special Precautions

Aminosalicylic acid and its salts should be used in combination with other antituberculosis drugs.

Use with particular caution in patients with impaired renal and liver function.

In the presence of aminosalicylates, tests for glycosuria that use copper-containing reagents are disrupted.

Drug Interactions

Aminosalicylic acid increases the T_1/2 of isoniazid.

The side effects of aminosalicylates and salicylates are additive.

Probenecid may increase the toxicity of aminosalicylate by impairing its renal excretion and increasing plasma concentration.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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

Aminosalicylic acid [Avexima JSC (Russia)]
Enteric-coated film-coated tablets, 500 mg: 5, 10, 20, 30, 50, 100, 375, or 500 pcs.
Enteric-coated film-coated tablets, 1000 mg: 5, 10, 20, 30, 50, 100, 375, or 500 pcs.

Marketing Authorization Holder

Avexima JSC (Russia)

Manufactured By

Irbit Chemical Pharmaceutical Plant, JSC (Russia)

Avexima Siberia LLC (Russia)

Dosage Forms

	Aminosalicylic acid	Enteric-coated film-coated tablets, 500 mg: 5, 10, 20, 30, 50, 100, 375, or 500 pcs.
		Enteric-coated film-coated tablets, 1000 mg: 5, 10, 20, 30, 50, 100, 375, or 500 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated film-coated tablets white or almost white, round, biconvex in shape; on the cross-section, the tablet core is white or white with a grayish tint.

	1 tab.
Sodium aminosalicylate dihydrate	500 mg

Excipients: hypromellose E5 – 5 mg, povidone K-30 – 26 mg, macrogol 6000 – 3 mg, colloidal silicon dioxide – 3 mg, sodium stearyl fumarate – 3 mg.

Film coating composition ready-made enteric coating (Aquarius Control ENA MAY318017 white) – 60 mg, with composition: methacrylic acid and ethyl acrylate copolymer (1:1) – 32.52 mg, macrogol 6000 (polyethylene glycol 6000) – 1.5 mg, talc – 15 mg, triethyl citrate – 7.02 mg, titanium dioxide – 3.96 mg.

10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (10) – cardboard packs.
5 pcs. – polyethylene jars (1) – cardboard packs.
10 pcs. – polyethylene jars (1) – cardboard packs.
20 pcs. – polyethylene jars (1) – cardboard packs.
50 pcs. – polyethylene jars (1) – cardboard packs.
100 pcs. – polyethylene jars (1) – cardboard packs.
375 pcs. – polyethylene jars (1) – cardboard packs.
500 pcs. – polyethylene jars (1) – cardboard packs.

Enteric-coated film-coated tablets white or almost white, oblong, biconvex in shape; on the cross-section, the tablet core is white or white with a grayish tint.

	1 tab.
Sodium aminosalicylate dihydrate	1000 mg

Excipients: hypromellose E5 – 10 mg, povidone K-30 – 52 mg, macrogol 6000 – 6 mg, colloidal silicon dioxide – 6 mg, sodium stearyl fumarate – 6 mg.

Film coating composition ready-made enteric coating (Aquarius Control ENA MAY318017 white) – 120 mg, with composition: methacrylic acid and ethyl acrylate copolymer (1:1) – 65.04 mg, macrogol 6000 (polyethylene glycol 6000) – 3 mg, talc – 30 mg, triethyl citrate – 14.04 mg, titanium dioxide – 7.92 mg.

Aminosalicylic acid [Vertex, JSC (Russia)]
Enteric-coated film-coated tablets, 500 mg: 100 or 500 pcs.

Marketing Authorization Holder

Vertex, JSC (Russia)

Dosage Form

Aminosalicylic acid

Enteric-coated film-coated tablets, 500 mg: 100 or 500 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated film-coated tablets pink, oblong, biconvex; on the cross-section, the core is white or almost white.

	1 tab.
Sodium aminosalicylate dihydrate	500 mg

Excipients: sorbitol, povidone K-30, citric acid monohydrate, crospovidone, talc, colloidal silicon dioxide, calcium stearate.

Film coating composition No. 1 (hypromellose, talc, titanium dioxide, macrogol 4000 (polyethylene glycol 4000)) or (dry mixture for film coating, containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)).
Film coating composition No. 2 dry mixture containing methacrylic acid and ethyl acrylate copolymer (1:1) (55%), talc (19.8%), titanium dioxide (12.72%), poloxamer 407 (6.6%), calcium silicate (4%), sodium bicarbonate (1.1%), iron oxide yellow dye (0.07%), iron oxide red dye (0.21%), sodium lauryl sulfate (0.5%).

100 pcs. – jars (1) – cardboard packs.
500 pcs. – jars (1) – cardboard packs.

Aminosalicylic acid [Vertex, JSC (Russia)]
Enteric-coated film-coated tablets, 1000 mg: 100 or 500 pcs.

Marketing Authorization Holder

Vertex, JSC (Russia)

Dosage Form

Aminosalicylic acid

Enteric-coated film-coated tablets, 1000 mg: 100 or 500 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated film-coated tablets pink, oblong, biconvex; on the cross-section, the core is white or almost white.

	1 tab.
Sodium aminosalicylate dihydrate	1000 mg

Excipients: sorbitol, povidone K-30, citric acid monohydrate, crospovidone, talc, colloidal silicon dioxide, calcium stearate.

100 pcs. – jars (1) – cardboard packs.
500 pcs. – jars (1) – cardboard packs.

Aminosalicylic acid [Kraspharma, PJSC (Russia)]
Solution for infusion 30 mg/ml: 200 ml vial 1 or 24 pcs., 200 ml vial 1 or 12 pcs.

Marketing Authorization Holder

Kraspharma, PJSC (Russia)

Dosage Form

Aminosalicylic acid

Solution for infusion 30 mg/ml: 200 ml vial 1 or 24 pcs., 200 ml vial 1 or 12 pcs.

Dosage Form, Packaging, and Composition

Solution for infusion	1 ml
Sodium para-aminosalicylate	30 mg

200 ml – bottles.
200 ml – bottles (1) – cardboard packs.
200 ml – bottles (24) – cardboard boxes.
400 ml – bottles.
400 ml – bottles (1) – cardboard packs.
400 ml – bottles (12) – cardboard boxes.
400 ml – bottles (24) – cardboard boxes.

Aminosalicylic acid [Pharmasintez, JSC (Russia)]
Lyophilisate for preparation of solution for infusion 13.49 g: vial 1, 5 or 10 pcs.