Aminosalicylic acid - instructions for use, dose, side effects, contraindications

Active substance: sodium 4-aminosalicylate dihydrate in terms of anhydrous substance 13.49 g (equivalent to 11.72 g of free acid 4-aminosalicylic and 1.77 g of sodium ions).

Description:Powder from white to light gray.

Pharmacotherapeutic group:Anti-tuberculosis drug

ATX: & nbsp

J.04.A.A.01 Aminosalicylic acid

Pharmacodynamics:

Anti-tuberculosis drug. Has a bacteriostatic effect. The tuberculostatic action is based on competition with para-aminobenzoic acid (PABA) for the active center of dihydropteroate synthetase, the enzyme that converts PABA to dihydrofolic acid, and inhibits the synthesis of folic acid in the microbial cell and / or the synthesis of the components of the cell wall of the microbacteria, reducing the last iron capture. On tuberculostatic activity inferior to isoniazid and streptomycin. Is active only in relation to Mycobacterium tuberculosis (minimal inhibitory concentration in vitro 1-5 μg / ml). It acts on mycobacteria, which are in a state of active reproduction and practically does not affect the mycobacteria at rest. Slightly affects the pathogen, located intracellularly. Does not affect other mycobacteria. Primary resistance is rare, secondary develops slowly. It is used only in combination with other anti-tuberculosis drugs, which slows the development of resistance to them.Irritant effect on the mucosa of the gastrointestinal tract.

Pharmacokinetics:

Easily penetrates through the histogematic barriers and is distributed in tissues. Achieves high concentrations in caseous masses. Moderately penetrates into the cerebrospinal fluid (only with inflammation of the meninges). Relationship with plasma proteins 50-60%. The main pathway of metabolism is acetylation. Metabolised in the liver (more than 50% acetylated to inactive metabolites) and partially in the stomach. 80% is excreted by the kidneys by glomerular filtration (50% in the form of an acetylated derivative). The total clearance depends on both the metabolic rate and the excretion of the kidneys. Half-life with normal kidney function is 30-60 minutes, with chronic renal failure - up to 23 hours. It penetrates into breast milk.

Indications:

Different forms and localization of tuberculosis in combination with other anti-TB drugs. Most often aminosalicylic acid is prescribed. patients with multiple drug resistance to other anti-TB drugs.

Contraindications:

Hypersensitivity to the components of the drug and to other salicylates; heavykidney and liver diseases (renal and / or liver failure, non-tuberculous etiology nephritis, hepatitis, liver cirrhosis); Decompensated heart failure; peptic ulcer of the stomach and duodenum; inflammatory bowel disease in the acute stage; Myxedema in the stage of decompensation; epilepsy; lactation period.

Carefully:Hepatic insufficiency of medium degree, deficiency of glucose-6-phosphate dehydrogenase, compensated hypothyroidism, pregnancy.

Dosing and Administration:

Intravenously infuzionalno.

Adults and children over 14 years of age - 10-15 g / day; children under 14 years of age - 200-300 mg / kg / day;

The number of courses and the total duration of treatment are determined individually.

Side effects:

From the digestive system: decreased or loss of appetite, increased salivation, nausea, vomiting, flatulence, abdominal pain, diarrhea, or constipation; increased activity of "liver" transaminases, hyperbilirubinemia, jaundice; drug hepatitis (including fatal).

From the hematopoiesis: thrombocytopenia, leukopenia (up to agranulocytosis), B12-deficiency anemia,Hemolytic anemia with a positive breakdown of Coombs.

From the genitourinary system: proteinuria, hematuria, crystalluria.

Allergic reactions: Rash (hives, purpura, exfoliative dermatitis, a syndrome resembling infectious mononucleosis or lymphoma), fever, bronchospasm, arthralgia, eosinophilia.

Other: antithyroid action; zobogenic effect, drug hypothyroidism, myxedema; pericarditis, hypoglycemia, optic neuritis, encephalopathy, Leffler's syndrome (eosinophilic pneumonia, migratory pulmonary infiltrate), vasculitis, decreased prothrombin.

Overdose:

Symptoms: may increase dose-related side effects. Treatment: withdrawal of the drug, symptomatic therapy.

Interaction:

Compatible with other antituberculous drugs.

Slows the emergence of resistance to isoniazid and streptomycin. When combined with isoniazid increases its concentration in the blood due to competition for common metabolic pathways.

It interferes with absorption and reduces the effectiveness of rifampicin, erythromycin and lincomycin.

Disrupts the assimilation of cyanocobalamin (possibly the development of B12-deficiency anemia).

Reduces the concentration of digoxin in the blood by 40%.

Strengthens the effect of indirect anticoagulants - derivatives of coumarin and indanedione (correction of the dose of anticoagulants is required).

When using iodine-containing hormones of the thyroid gland, their analogs and antagonists (including antithyroid agents), it should be taken into account that the concentration of thyroxine and thyroid-stimulating hormone in the blood changes in the background of PABA.

Ammonium chloride increases the risk of developing crystalluria.

Simultaneous administration with ethionamide increases the risk of hepatotoxicity.

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

Special instructions:

Used in combination with more active antituberculous drugs.

During the treatment it is recommended to systematically examine urine and blood, monitor the activity of "liver" transaminases.

Reduction of kidney function against tuberculous intoxication or specific tuberculosis lesions are not contraindication to the use. The development of proteinuria and hematuria requires a temporary discontinuation of the drug. At the first signs, indicating an allergic reaction, the drug should be stopped and desensitizing therapy should be given.

Form release / dosage:

Liofilizate for the preparation of solution for infusions 13.49 g.

Packaging:

Primary packaging of medicinal product.

For 13.49 g of the preparation in a glass vial (glass of analytical class III), with a capacity of 500 ml, with a plug of bromobutyl rubber covered with an aluminum cap. The label is labeled with label paper or writing paper or from polymer materials, self-adhesive.

Secondary packaging of medicinal product.

One bottle together with transflo and instructions for use are placed in a pack of cardboard.

When the product is packaged at the enterprise OAO "Pharmasintez" (Russia):

Secondary packaging of medicinal product.

One bottle together with transflo and instructions for use are placed in a pack of cardboard for consumer containers.

For 5 or 10 vials, together with an equal amount of transflo and instructions for use in a cardboard box (for hospitals). On the box, paste a label from paper label or writing or from polymer materials, self-adhesive.

When packaging the kit (Aminosalicylic acid with solvent Water for injection) at the OJSC Pharmasynthez (Russia):

Secondary packaging of medicinal product

One bottle with the drug (13.49 g of active substance) together with transflo complete with 1 bottle of 500 ml water-injection solvent, together with the instructions for use, is placed in a pack of cardboard for consumer containers. The packets are placed in a group package.

Storage conditions:

In case of preparation without solvent:

In the dark place at a temperature of no higher than 25 ° C.

In case of preparation with solvent:

In a dry, dark place at a temperature of 2 to 25 ° C

Shelf life:

4 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006691/10

Date of registration:15.07.2010 / 19.12.2014

Expiration Date:Unlimited

The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia

Manufacturer: & nbsp

SANJIVANI PARANTERAL, Limited India

Information update date: & nbsp09.08.2017

Illustrated instructions

Instructions

Aminosalicylic acid (Aminosalicylic asid)