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

1 tablet contains active substance sodium aminosalicylate dihydrate - 500 mg; Excipients: cellulose microcrystalline - 13.75 mg,povidone (polyvinylpyrrolidone medium molecular weight) - 26.65 mg, silicon dioxide colloid (aerosil) - 4.5 mg, citric acid monohydrate - 0.15 mg, stearic acid - 4.95 mg; sheath 55.0 mg; lacquer aluminum based on the dye azorubin [E 122] - 0.96%, aluminum lacquer based on the dye indigo carmine [E 132] - 0.06%, methacrylic acid and ethyl acrylate copolymer [1: 1] - 40.0%, aluminum lacquer on the basis of the dye crimson [Ponso 4R] [Е 124] - 0,705%, lacquer aluminum based on dye quinoline yellow [E 104] - 0,14%, silicon dioxide colloid - 1,25%, sodium bicarbonate - 1,2%, sodium lauryl sulfate - 0,5%, talc - 37.25%, titanium dioxide - 13.135%, triethyl citrate - 4.8%.

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:

Anti-tuberculosis agent. Has a bacteriostatic effect. The basis of tuberculostatic action is competition with para-aminobenzoic acid for the active center of dihydropteroate synthetase, an enzyme that converts para-aminobenzoic acid to dihydrofolic acid, and inhibits the synthesis of folic acid

acid in the microbial cell and / or synthesis of the components of the cell wall of the microbacteria, reducing the capture of iron by the latter. 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 development is slow. It is used only in combination with other antituberculosis drugs, which slows the development of resistance to them.

Pharmacokinetics:

Suction. Well absorbed from the gastrointestinal tract. 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.

Distribution. Binding to blood plasma proteins is 50-70%. Easily passes the histohematological barriers and is distributed in tissues, penetrates into breast milk. In the cerebrospinal fluid penetrates only with inflammation of the meninges.

Metabolism. Metabolised in the liver (more than 50% acetylated to inactive metabolites) and partially in the stomach.

Excretion. Half-life (T_1/2) with normal kidney function is 30-60 minutes, with chronic renal failure - up to 23 hours. Excreted by glomerular filtration and tubular secretion, reaching very high concentrations in the urine. 80% of aminosalicylic acid is excreted by the kidneys, while 50% - in the form of an acetylated derivative. The total clearance depends on both the metabolic rate and the excretion of the kidneys.

Patients with impaired renal function

In patients with severe renal failure, cumulation of aminosalicylic acid and its acetyl metabolite is noted, but the formation of an inactive acetylated derivative continues. The half-life of free aminosalicylic acid in patients with kidney disease is approximately the same as in healthy volunteers, however T_1/2 inactive acetylated derivative in patients with uremia increased by 6 times. Although aminosalicylic acid is derived from dialysis, the frequency of chronic hemodialysis sessions is usually not enough to compensate for the lowered excretion due to renal failure.

Patients with impaired hepatic function

In patients with impaired liver function, the metabolism of aminosalicylic acid is comparable to that in healthy volunteers.

Children and teens

Data on the pharmacokinetics of aminosalicylic acid in children and adolescents are absent.

Indications:

Tuberculosis of various forms and localizations (in conjunction with other anti-tuberculosis drugs), including with multiple drug resistance to other anti-tuberculosis drugs.

Contraindications:

Hypersensitivity to aminosalicylic acid (including other salicylates), other components of the drug; severe kidney and liver diseases (severe renal and / or hepatic insufficiency, nephritis of tuberculosis etiology, hepatitis, cirrhosis of the liver); decompensated chronic heart failure; arterial hypertension; edema due to hypernatremia; peptic ulcer of the stomach and duodenum; inflammatory bowel disease in the acute stage; amyloidosis of internal organs; uncompensated hypothyroidism; thrombophlebitis, blood clotting disorder; epilepsy; children's age up to 3 years (for this dosage form).

Carefully:Liver failure of moderate severity, deficiency of glucose-6-phosphate dehydrogenase, compensated hypothyroidism, chronic heart failure, history of gastrointestinal disease, diabetes mellitus.

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, washed down with water.

Adults 9-12 grams per day (3-4 grams 3 times a day), children over 3 years - 0.2 g / kg per day in 3-4 times (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. When concomitant diseases of the gastrointestinal tract, the maximum daily dose - 4-6 g / 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, heartburn, peptic ulcer bleeding; increased activity of "hepatic" transaminases, hyperbilirubinemia, jaundice, hepatomegaly; drug hepatitis (including fatal).

From the hematopoiesis: Thrombocytopenia, leukopenia (up to agranulocytosis), B 12-deficiency anemia, hemolytic anemia with a positive Coombs breakdown, eosinophilia, neutropenia, lymphocytosis.

From the genitourinary system: proteinuria, hematuria, crystalluria.

Allergic reactions: rash (hives, purpura, enanthema, exfoliative dermatitis, erythema, a syndrome that resembles infectious mononucleosis or lymphoma), fever, bronchospasm, arthralgia; anaphylactic shock, malignant exudative erythema (Stevens-Johnson syndrome), angioedema, toxic epidermal necrolysis (Lyell's syndrome).

Other: antithyroid action; zobogenny effect, drug hypothyroidism, myxedema (with long-term use in high doses); pericarditis, hypoglycemia, glucosuria, optic neuritis, encephalopathy,Leffler's syndrome (eosinophilic pneumonia, migratory pulmonary infiltrate), vasculitis, a decrease in prothrombin content, an increase in prothrombin time, an increase in urea concentration in the blood plasma; psychosis, convulsions, symptoms of paralysis.

Overdose:

Symptoms: it is possible to increase dose-dependent side effects.

Treatment: withdrawal of the drug, symptomatic therapy.

Interaction:

Aminosalicylic acid disrupts the absorption of rifampicin, erythromycin and lincomycin.

When combined with isoniazid or phenytoin increases their concentration in the blood plasma due to competition for common metabolic pathways.

Disrupts the assimilation of cyanocobalamin (vitamin B₁₂), as a result of which development of B12-deficiency anemia is possible.

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).

Inhibits the absorption of folic acid and can enhance the toxicity of folic acid antagonists, such as, for example, methotrexate.

The use of the drug together with salicylates, phenylbutazone or other anti-inflammatory drugs,possessing an increased ability to bind to plasma proteins, leads to an increase in the concentration and an increase in the duration of the presence of aminosalicylic acid in the blood plasma.

Antacids do not interfere with drug absorption.

When using iodine-containing thyroid hormones, 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 with aminosalicylic acid.

The use of the drug together with diphenhydramine leads to a decrease in the concentration of aminosalicylic acid in the blood plasma.

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

Simultaneous use with ethionamide increases the risk of hepatotoxicity.

Ammonium chloride increases the risk of developing crystalluria.

Special instructions:

Used in combination with other antituberculous drugs.

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 monitor liver function (activity of "liver" transaminases).

In the presence of symptoms of liver dysfunction, such as increased activity of "liver" transaminases, jaundice, fever, therapy with the drug should be discontinued and a study of the functional state of the liver.

In patients with diabetes it is necessary to monitor the concentration of glucose in the blood plasma.

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, 500 mg.

Packaging:

Packing for hospitals

500 tablets in a polymer can with a polymer lid.

1, 4, 6, 10 cans along 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 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002571

Date of registration:07.08.2014

Expiration Date:07.08.2019

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

Manufacturer: & nbsp

MAKIZ-PHARMA, LLC Russia

Information update date: & nbsp09.08.2017

Illustrated instructions

Instructions

Aminosalicylic acid (Aminosalicylic asid)