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

auxiliary substances: ethylcellulose, polyvinylpyrrolidone medium molecular weight (povidone), microcrystalline cellulose, milk sugar (lactose), shellac, oidragit, tropeolin 0 - up to 4 g.

5 g in the package active substance: sodium para-aminosalicylate - 4.0 g;

auxiliary substances: ethylcellulose, polyvinylpyrrolidone medium molecular weight (povidone), microcrystalline cellulose, milk sugar (lactose), shellac, oidragit, tropeolin 0 - up to 5 g.

100 g in the pot active substance: sodium para-aminosalicylate - 80.0 g; auxiliary substances: ethyl cellulose, polyvinylpyrrolidone, medium molecular weight (povidone), microcrystalline cellulose, milk sugar (lactose), shellac, oidragit, tropeolin 0 - up to 100 g.

Description:

Description: granules coated with enteric coating, from yellow-orange to dark-orange color, round in shape.

Pharmacotherapeutic group:anti-tuberculosis drug

ATX: & nbsp

J.04.A.A.01 Aminosalicylic acid

Pharmacodynamics:

Sodium para-aminosalicylate has a bacteriostatic action in relation to Mycobacterium tuberculosis. The mechanism of action is associated with the inhibition of the synthesis of folic acid and with the suppression of the formation of mycobacterium, a component of the mycobacterial wall, which leads to a decrease in the capture of iron M. tuberculosis.

Sodium para-aminosalicylate 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.

Sodium para-aminosalicylate is active only in relation to M. tuberculosis. Does not affect other non-tuberculosis mycobacteria.

Sodium para-aminosalicylate reduces the likelihood of bacterial resistance to streptomycin and isoniazid.

Pharmacokinetics:

Features of clinical pharmacology aminosalicylic acid - is the rapid formation in the acidic environment of a toxic inactive metabolite and a short half-life in the serum, which for an unbound drug is one hour. Since the pellets are protected by an enteric coating, their absorption does not begin until they reach the small intestine. Well absorbed when taken orally. The maximum concentration in the blood serum after oral administration of a dose of 4 g is 75 μg / ml. Metabolised in the liver. Sodium para-aminosalicylate is excreted by glomerular filtration. 80% of the drug is excreted in the urine, with more than 50% excreted in the acetylated form. In the cerebrospinal fluid the drug penetrates only with inflammation of the meninges. About 50-60% of aminosalicylic acid binds to proteins.

Indications:

Treatment of various forms and localizations of tuberculosis in combination with other anti-TB drugs. (More often sodium para-aminosalicylate is prescribed for patients with multiple drug resistance to other anti-tuberculosis drugs).

Contraindications:

-Individual intolerance of the drug;

-Heavy kidney and liver diseases;

- Cardiac insufficiency in the stage of decompensation;

- Stomach ulcer and duodenal ulcer;

-Hypothyroidism, myxedema

-Trombophlebitis

-Corruption of blood clotting

- Enterocolitis in the phase of exacerbation;

-Epilepsy;

Pregnancy and lactation:

It is possible to use sodium para-aminosalicylate in pregnancy, when the expected benefit for the mother exceeds the potential risk to the fetus.

If it is necessary to use sodium para-aminosalicylate during lactation, breastfeeding should be stopped.

Dosing and Administration:

Assign sodium para-aminosalicylate to 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). Take 0.5-1 hour after eating.

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:

The most common side effects from the gastrointestinal tract are nausea, vomiting, worsening or loss of appetite, abdominal pain, diarrhea, or constipation.

Also noted are fever, urticaria and other allergic diseases, dermatitis, purpura, enantema, bronchospasm, joint pain, eosinophilia, rarely agranulocytosis, leukopenia, thrombocytopenia, drug hepatitis, proteinuria and hematuria.

With prolonged use in higher doses - hypothyroidism, goiter.

Interaction:

Sodium para-aminosalicylate increases the concentration of isoniazid in the blood, disrupts the absorption of rifampicin, erythromycin and lincomycin, disrupts the absorption of the vitamin B12, resulting in the possible development of anemia, may enhance the effect of anticoagulants (coumarin derivatives or indanedione).

Antacids do not interfere with the absorption of sodium para-aminosalicylate.

Special instructions:

At the first sign indicating an allergic reaction, the drug should be immediately discontinued and desensitizing therapy should be performed.

During the treatment, it is necessary to systematically examine urine and blood and check the functional state of the liver.

In the treatment it is recommended to monitor the activity of "liver" enzymes. Decreased kidney function against tuberculous intoxication or a specific lesion is not a contraindication to the administration of sodium para-aminosalicylate. The development of proteinuria and hematuria require a temporary discontinuation of the drug.

Form release / dosage:

Granules coated with enteric coating, 800 mg / g.

Packaging:4 grams, 5 grams in heat-sealed bags.

For 1, 10, 25, 50, 100 packages of 4 grams together with instructions for use in a pack of cardboard.

For 1, 10, 20, 50, 100 packages of 5 grams together with instructions for use in a pack of cardboard.

For 1000 packages of 4 grams or 1000 packages of 5 grams, along with instructions for use in a box of corrugated cardboard (for inpatient).

To 100 grams in a plastic jar with a measuring spoon and instructions for use in a pack of cardboard.

Storage conditions:Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000230

Date of registration:10.06.2010

The owner of the registration certificate:ZIO-HEALTH, JSC ZIO-HEALTH, JSC Russia

Manufacturer: & nbsp

ZIO-HEALTH, JSC Russia

Information update date: & nbsp26.06.2014

Illustrated instructions

Instructions

Aminosalicylic acid (Aminosalicylic asid)