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

active substance: sodium aminosalicylate dihydrate - 1 g; Excipients: microcrystalline cellulose-0.0533 g, povidone (polyvinylpyrrolidone medium molecular weight) 0.0275 g, silicon dioxide colloid (aerosil) 0.0090 g, citric acid monohydrate 0.0003 g, stearic acid 0.0099 g.

shell: ACRYL-I pink (lacquer aluminum based on dye azorubin [E 122], aluminum lacquer based on the dye indigo carmine [E132], methacrylic acid and ethyl acrylate copolymer [1: 1], lacquer aluminum based on the dye crimson [Ponso 4R] [E 124 ], lacquer aluminum based on dye quinoline yellow [E 104], silicon dioxide colloid, sodium bicarbonate, sodium lauryl sulfate, talc, titanium dioxide, triethyl citrate) -0.1100 g.

Description:The oval tablets are covered with a pink film cover. On the fracture are visible two layers, the core of white or white with a creamy hue of color.

Pharmacotherapeutic group:Anti-tuberculosis drug

ATX: & nbsp

J.04.A.A.01 Aminosalicylic acid

Pharmacodynamics:

Has bacteriostatic action against Mycobacterium tuberculosis. The mechanism of action is associated with inhibition of the synthesis of folic acid and suppression of the formation of mycobacterium (a component of the mycobacterial wall), which leads to a decrease in the capture of iron M. tuberculosis.

Aminosalicylic acid is active against M. tuberculosis, which are in a state of active reproduction, and practically does not affect the mycobacteria at rest and are located intracellularly. Does not affect other mycobacteria. Aminosalicylic acid reduces the likelihood of bacterial resistance to streptomycin and isoniazid.

Pharmacokinetics:

Well absorbed when taken internally. After ingestion in a dose of 4 g, the maximum concentration in the blood serum is achieved after 1.5-2 hours and is 75 μg / ml. (Binding to plasma proteins is low (15%) .It easily passes through histohematic barriers and is distributed in tissues.In the cerebrospinal fluid it penetrates only with inflammation of the meninges.

Metabolised in the liver (more than 50% acetylated to inactive metabolites) and partially in the stomach. Half-life (T_1/2) with normal kidney function is 30-60 minutes, with disturbed - up to 23 hours Excreted by glomerular filtration and tubular secretion, reaching very high concentrations in the urine. 85% of the dose is excreted within 7-10 hours, 14-33% in unchanged form, 50% in the form of metabolites.

Indications:

Tuberculosis of various forms and localizations (in combination with other anti-TB drugs) With multiple drug resistance to other anti-tuberculosis drugs.

Contraindications:

- Hypersensitivity to any component of the drug;

- Severe diseases of the kidneys and liver;

- Chronic heart failure in the stage of decompensation;

- Peptic ulcer of the stomach and duodenum;

- Amyloidosis;

- Enterocolitis in the phase of exacerbation;

- Myxedema in the phase of decompensation;

- Epilepsy;

- Children up to 3 years.

Pregnancy and lactation:It is possible to use the drug during pregnancy, if the expected benefit for the mother exceeds the potential risk to the fetus. For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Inside, 0.5-1 hour after eating. Adults 9-12 grams per day (3-4 g 3 times a day), children - 0.2 g / kg per day in 3-4 doses (daily dose of not more than 10 g). Exhausted adult patients (with a body weight of less than 50 kg), as well as with poor tolerance, the drug is prescribed in a dose of 6 g per day.

In conditions of outpatient treatment, the entire daily dose can be administered in a single dose, but with a bad tolerance, the daily dose is divided into 2-3 doses.

Side effects:

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): impaired synthesis of prothrombin, hemolytic anemia (with deficiency of glucose-6-phosphate dehydrogenase); rarely - thrombocytopenia, leukopenia (up to agranulocytosis), B₁₂-deficient megaloblastic anemia.

On the part of the organs of the gastrointestinal tract: nausea, vomiting, worsening or loss of appetite, flatulence, diarrhea or constipation, abdominal pain, increased activity of "liver" transaminases, hyperbilirubinemia, hepatomegaly, rarely - drug-induced hepatitis.

From the genitourinary system: crystalluria, proteinuria, hematuria.

Allergic reactions: urticaria, purpura, enanthema, drug fever, bronchospasm, arthralgia, eosinophilia.

Other: hypothyroidism, goiter, myxedema (with prolonged use in high doses).

Overdose:

In case of an overdose, urgent gastric lavage and symptomatic therapy are indicated.

Interaction:

Aminosalicylic acid increases the concentration of isoniazid in the blood.

Violates the absorption of rifampicin, erythromycin and lincomycin.

When combined with capreomycin, it is possible to increase electrolyte disturbances, decrease the potassium concentration and pH.

Disrupts the assimilation of cyanocobalamin (vitamin B₁₂), resulting in the development of anemia.

Aminosalicylic acid can enhance the effect of anticoagulants (coumarin derivatives or indanedione).

Antacids do not interfere with drug absorption.

Insulin increases the tuberculostatic effect of aminosalicylic acid, and estrogens, barbiturates and sulfonamides that reduce blood glucose, it weakens.

Special instructions:At the first signs indicating an allergic reaction, the drug should be stopped immediately and desensitizing therapy should be given. During the treatment, it is necessary to systematically examine urine and blood and check the functional state of the liver. When treatment is recommended to monitor the activity of "liver" transaminases. Decreased kidney function against tuberculous intoxication or a specific lesion is not a contraindication to the appointment of aminosalicylic acid. The development of proteinuria and hematuria requires a temporary discontinuation of the drug.

Effect on the ability to drive transp. cf. and fur:

There is still evidence that aminosalicylic acid has any adverse effect on a patient's ability to engage in potentially hazardous activities requiring increased attention and speed of mental and motor reactions, was not.

Form release / dosage:

Tablets, coated with enteric coating, 1 g.

Packaging:

For 10 tablets in a planar cell package.

For 50, 100 or 500 tablets in a polymer can.

2, 5 or 10 contour mesh packages or each bank along with instructions for use in a pack of cardboard.

Packing for hospitals:

50 or 100 contour packs, or 5, 10, 20, 50 cans of 50 or 100 tablets or 1, 4, 6, 10 cans of 500 tablets together with instructions for use in a cardboard box.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 of the year. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003659 / 01

Date of registration:04.05.2010 / 12.12.2012

Expiration Date:Unlimited

The owner of the registration certificate:NIZHFARM, JSC NIZHFARM, JSC Russia

Manufacturer: & nbsp

MAKIZ-PHARMA, LLC Russia

SKOPINSKY FARM ZAVOD, LLC Russia

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp09.08.2017

Illustrated instructions

Instructions

Aminosalicylic acid (Aminosalicylic asid)