Sodium para-aminosalicylate - instructions for use, dosage, adverse effects, contraindications

Excipients (core): cellulose microcrystalline - 55.0 mg, silicon dioxide colloid - 5.0 mg, povidone-K25 - 34.40 mg, calcium stearate - 10.0 mg, polysorbate-80 - 5.60 mg, citric acid monohydrate - 10, 0 mg.

Auxiliary substances (shell): a mixture of "Acryl-EZE WHITE

93 A) (methacrylic acid and ethyl acrylate copolymer [1: 1], talc, titanium dioxide, silicon dioxide colloid, sodium hydrogen carbonate, sodium lauryl sulfate) - 72.0 mg, triethyl citrate - 8.0 mg.

Description:

Oval-shaped tablets with a risk on one side, coated with a coat of white or almost white.

On the cross-section: the core is white or white with a yellowish or beige shade of color, the shell is white or almost white.

Pharmacotherapeutic group:Anti-tuberculosis drug

ATX: & nbsp

J.04.A.A.01 Aminosalicylic acid

Pharmacodynamics:

Aminosalicylic acid has a bacteriostatic effect against Mycobacterium tuberculosis. The mechanism of action is associated with 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 M. tuberculosis.

Aminosalicylic acid acts on M. tuberculosis, which are in a state of active reproduction, and practically does not act on M.tuberculosis at rest. Slightly affects the pathogen, located intracellularly.

Aminosalicylic acid is active only against M. tuberculosis. Does not affect other non-tuberculosis mycobacteria.

It is used only in combination with other antituberculosis drugs, which reduces the likelihood of bacterial resistance to them.

Pharmacokinetics:

Suction.

Well absorbed from the gastrointestinal tract. After ingestion in a dose of 4 g, the maximum concentration in the serum is reached after 1.5-2 hours and is 20 μg / ml.

Distribution.

Binding to plasma proteins is 50-60%. Easily passes the histohematological barriers, penetrates into breast milk. It is well distributed in tissues and body fluids, kidneys, lungs, liver. Achieves high concentrations in pleural efflorescence and caseous tissue. 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.

The 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 liver function.

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

Children and teenagers.

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

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

Contraindications:

Hypersensitivity to aminosalicylic acid (including other salicylates), other components of the drug;
Individual intolerance to salicylates (in history);
Deficiency of glucose-6-phosphate dehydrogenase;
Epilepsy;
Severe renal and / or hepatic insufficiency;
Stomach ulcer and duodenal ulcer, inflammatory bowel disease in the acute stage;
Decompensated hypothyroidism;
Chronic heart failure in the stage of decompensation;
Arterial hypertension;
Thrombophlebitis;
Hypocoagulation;
Edema caused by hypernatremia;
Amyloidosis of internal organs;
Children under 3 years old (for this dosage form);
Breastfeeding period.

Carefully:Renal / hepatic insufficiency of moderate and mild severity. Compensated hypothyroidism.Chronic heart failure. Diseases of the gastrointestinal tract in the anamnesis. Diabetes. Acute hepatitis. Pregnancy.

Pregnancy and lactation:Possible use of aminosalicylic acid during pregnancy in the case when the expected benefit for the mother exceeds the potential risk to the fetus. If you need to use aminosalicylic acid during lactation, breastfeeding should be stopped.

Dosing and Administration:

Assign inside, 0.5-1 hour after meals, washed down with acidic liquids (juices: orange, tomato, apple).

With increased acidity of gastric juice wash down with water.

Adults - 9-12 grams per day (3-4 grams 3 times a day); for malnourished patients with a body weight of less than 50 kg, and also with poor tolerance, the drug is used in a dose of 6 g / day, the daily dose is divided into 2-3 doses.

Children from 3 to 18 years - the drug is prescribed at the rate of 0.15-0.2 g / kg body weight per day in 3-4 doses (daily dose of not more than 10 g).

In conditions of outpatient treatment, the entire daily dose can be used in one dose, with poor tolerability in 2 divided doses.

With concomitant diseases of the gastrointestinal tract and the initial forms of amyloidosis, the maximum daily dose is 4-6 g.

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; increased activity of "hepatic" transaminases, hyperbilirubinemia, jaundice; drug-induced hepatitis (including fatal), hepatomegaly, partially pronounced malabsorption syndrome, bleeding peptic ulcers.

On the part of the organs of hematopoiesisThrombocytopenia, neutropenia, an elongation of prothrombin time, accompanied by bleeding and hemorrhagic lymphocytosis purpura, leukopenia (up to agranulocytosis), B-12 deficiency megaloblastic anemia, hemolytic anemia, Coombs positive sample.

From the genitourinary system: proteinuria, hematuria, crystalluria, glucosuria, increased urea concentration in blood plasma.

Allergic reactionsItching, erythema, rash (urticaria, purpura, enanthema, exfoliative dermatitis syndrome resembling infectious mononucleosis or lymphoma), angioneurotic edema, fever, bronchospasm, arthralgia, eosinophilia, Stevens-Johnson syndrome, Lyell syndrome, anaphylactic shock.

Other: antithyroid action; zobogenny effect, drug hypothyroidism, myxedema (with long-term use in high doses); pericarditis, hypoglycemia, hyperglycemia, hypokalemia, optic neuritis, encephalopathy, psychosis, seizures, paralysis symptoms, Leffler's syndrome (eosinophilic pneumonia, migratory pulmonary infiltrate), vasculitis, decreased prothrombin, superinfection, joint edema, lupus-like syndrome accompanied by spleen, liver damage , kidneys, digestive tract, bone marrow and nervous system (for example, pain of radicular nature, meningism).

Overdose:

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

Treatment: withdrawal of the drug, symptomatic therapy.

Interaction:

Aminosalicylic acid disrupts the absorption of rifampicin, erythromycin and lincomycin. If it is necessary to use together with rifampicin, you should divide the time of taking the drugs.

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

Simultaneous use with phenytoin may lead to an increase in the concentration of phenytoin in the blood plasma and the appearance of its toxicity.

It interferes with the assimilation of cyanocobalamin (vitamin B12), which can lead to the development of 12-deficiency anemia.

Antacids do not interfere with drug absorption.

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

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

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.

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 with increased ability to bind to plasma proteins, leads to an increase in the concentration and increase in the duration of aminosalicylic acid in the blood plasma.

Special instructions:

Used in combination with other anti-tuberculosis drugs.

At the first signs indicating an allergic reaction, the drug should be stopped immediately and symptomatic 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 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.

In the presence of symptoms of impaired liver function, such as increased activity of "liver" transaminases, jaundice, fever,The drug should be discontinued and an examination of the functional state of the liver should be carried out.

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

There is no data on the study of the effect of aminosalicylic acid on the ability to drive vehicles and perform other actions that require concentration of attention and speed of psychomotor reactions. Patients should be warned about the possibility of developing paralysis, seizures, optic neuritis, and when these undesirable phenomena appear, one should refrain from performing these activities.

Form release / dosage:

Tablets coated with enteric coating 1000 mg.

Packaging:

100, 200, 300, 400, 500, 1000 tablets (for hospitals) in cans of polyethylene terephthalate for medicines or polypropylene for drugs sealed with high-pressure polyethylene caps with a control of the first opening or with polypropylene caps with a "click-turn" system ", or low-density polyethylene caps with a first opening control.

3, 4, 5, 6, 7, 8, 9, 10, 12, 15 cans, together with an equal number of instructions for use, are placed in a group package (shipping container).

Storage conditions:

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

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:For hospitals

Registration number:LP-000118

Date of registration:28.12.2010 / 17.10.2017

Expiration Date:Unlimited

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp25.05.2018

Illustrated instructions

Instructions

Sodium para-aminosalicylate (Sodium para-aminosalicylate)