Amiktobin (Tablets) Instructions for Use

Marketing Authorization Holder

Pharmasintez-Tyumen, LLC (Russia)

ATC Code

J04AA02 (Aminosalicylate sodium)

Active Substance

Aminosalicylate sodium (USP)

Dosage Forms

	Amiktobin	Enteric-coated film-coated tablets, 500 mg: 50, 100, 372 or 500 pcs.
		Enteric-coated film-coated tablets, 1000 mg: 50, 100, 372 or 500 pcs.
		Enteric-coated film-coated tablets, 1500 mg: 50, 100, 372 or 500 pcs.
		Enteric-coated film-coated tablets, 2000 mg: 50, 100, 372 or 500 pcs.

Dosage Form, Packaging, and Composition

Enteric-coated film-coated tablets are white, biconvex, capsule-shaped; on the cross-section, the tablet core is white or white with a grayish tint.

Excipients: hypromellose E5 – 5 mg, povidone K30 – 26 mg, macrogol 6000 – 3 mg, colloidal silicon dioxide – 3 mg, sodium stearyl fumarate – 3 mg.

Coating ready-made enteric coating – 60 mg (coating 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).

50 pcs. – jars (1-250) – group packaging (for hospitals).
100 pcs. – jars (1-250) – group packaging (for hospitals).
372 pcs. – jars (1-250) – group packaging (for hospitals).
500 pcs. – jars (1-250) – group packaging (for hospitals).

Enteric-coated film-coated tablets are white, biconvex, capsule-shaped, with a score on one side; on the cross-section, the tablet core is white or white with a grayish tint.

Excipients: hypromellose E5 – 10 mg, povidone K30 – 52 mg, macrogol 6000 – 6 mg, colloidal silicon dioxide – 6 mg, sodium stearyl fumarate – 6 mg.

Coating ready-made enteric coating – 120 mg (coating 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).

50 pcs. – jars (1-250) – group packaging (for hospitals).
100 pcs. – jars (1-250) – group packaging (for hospitals).
372 pcs. – jars (1-250) – group packaging (for hospitals).
500 pcs. – jars (1-250) – group packaging (for hospitals).

Enteric-coated film-coated tablets are white, biconvex, capsule-shaped; on the cross-section, the tablet core is white or white with a grayish tint.

Excipients: hypromellose E5 – 15 mg, povidone K30 – 78 mg, macrogol 6000 – 9 mg, colloidal silicon dioxide – 9 mg, sodium stearyl fumarate – 9 mg.

Coating ready-made enteric coating – 180 mg (coating composition: methacrylic acid and ethyl acrylate copolymer (1:1) – 97.56 mg, macrogol 6000 (polyethylene glycol 6000) – 4.5 mg, talc – 45 mg, triethyl citrate – 21.06 mg, titanium dioxide – 11.88 mg).

50 pcs. – jars (1-250) – group packaging (for hospitals).
100 pcs. – jars (1-250) – group packaging (for hospitals).
372 pcs. – jars (1-250) – group packaging (for hospitals).
500 pcs. – jars (1-250) – group packaging (for hospitals).

Enteric-coated film-coated tablets are white, biconvex, oval-shaped; on the cross-section, the tablet core is white or white with a grayish tint.

Excipients: hypromellose E5 – 20 mg, povidone K30 – 104 mg, macrogol 6000 – 12 mg, colloidal silicon dioxide – 12 mg, sodium stearyl fumarate – 12 mg.

Coating ready-made enteric coating – 240 mg (coating composition: methacrylic acid and ethyl acrylate copolymer (1:1) – 130.08 mg, macrogol 6000 (polyethylene glycol 6000) – 6 mg, talc – 60 mg, triethyl citrate – 28.08 mg, titanium dioxide – 15.84 mg).

50 pcs. – jars (1-250) – group packaging (for hospitals).
100 pcs. – jars (1-250) – group packaging (for hospitals).
372 pcs. – jars (1-250) – group packaging (for hospitals).
500 pcs. – jars (1-250) – group packaging (for hospitals).

Clinical-Pharmacological Group

Antituberculosis drug

Pharmacotherapeutic Group

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

Pharmacological Action

Amiktobin is an antituberculosis agent, representing the sodium salt of aminosalicylic acid.

Aminosalicylate sodium (para-aminosalicylate sodium) exerts 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 passes through histohematic barriers and is distributed in tissues.

It undergoes metabolism.

50% of the dose is determined in the urine as an acetylated derivative.

The elimination half-life (T_1/2) is 30 minutes.

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

Dosage Regimen

Take orally. Swallow tablets whole. Do not crush or chew.

For adults, the total daily dosage is 10-12 grams. Divide the total daily dose into 2-3 administrations.

For pediatric patients, the total daily dosage is 150-300 mg per kg of body weight. Divide the total daily dose into 3-4 administrations.

Always administer Amiktobin in combination with other antituberculosis drugs to prevent the rapid development of resistance.

Take doses at regular intervals to maintain stable plasma concentrations.

Adjust the dosage carefully based on the available tablet strengths (500 mg, 1000 mg, 1500 mg, 2000 mg) to achieve the prescribed total daily dose.

Use with particular caution and potential dosage adjustment in patients with impaired renal or hepatic function.

Monitor renal and hepatic function, as well as serum potassium levels, during therapy.

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

Contraindicated for use 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 kidney 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 kidney and liver function.

In the presence of aminosalicylates, the conduction of tests for glucosuria using reagents containing copper is impaired.

Drug Interactions

Aminosalicylic acid increases the elimination half-life (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.