PAS Sodium - instructions for use, dose, side effects, contraindications

Aminosalicylic acid has a bacteriostatic effect against Mycobacterium tuberculosis, reduces the likelihood of bacterial resistance to streptomycin and isoniazid. 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 iron M. tuberculosis. Aminosalicylic acid acts against actively multiplying Mycobacterium tuberculosis (MIC of 1-5 μg / ml). Virtually does not work on Mycobacterium tuberculosis in the stage of rest and located intracellularly. Does not affect other mycobacteria. It is used only in combination with other anti-tuberculosis drugs.

Under the influence of gastric juice aminosalicylic acid quickly turns into an inactive metabolite. Acid-resistant shell protects the granules from the destructive effects of gastric juice.In a neutral environment, for example, in the small intestine, the granule membrane dissolves and the drug releases.

Pharmacokinetics:

Quickly and well absorbed from the gastrointestinal tract. The mean time to reach the maximum concentration (C_m_Oh) after taking a dose of 4 g is 6 hours (varies from 1.5 to 24 hours). FROM_m_Ohon average, 20 μg / ml (9 to 35 μg / ml). The concentration of aminosalicylic acid in the plasma is 2 μg / ml maintained for 7.9 hours (variability from 5 to 9 hours), and 1 μg / ml - an average of 8.8 hours (6 to 11.5 hours). Binding to plasma proteins - 50-60%. 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 moderately (only with inflammation of the meninges). Penetrates into breast milk. Metabolised in the liver (more than 50% acetylated to inactive metabolites) and partially in the stomach. The half-life (T1 / 2) with normal kidney function is 30-60 minutes, with disturbed - up to 23 hours. 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.

Indications:

Tuberculosis of various forms and localizations (in combination with other anti-TB drugs), including multidrug-resistant tuberculosis to other anti-tuberculosis drugs.

Contraindications:

- Hypersensitivity to aminosalicylic acid and other components of the drug, other salicylates;

- Kidney and liver diseases (severe renal / hepatic insufficiency, nephritis of nontuberculous etiology, hepatitis, cirrhosis of the liver);

- Amyloidosis of internal organs;

- Stomach ulcer and duodenal ulcer, inflammatory bowel disease in the acute stage;

- Decompensated hypothyroidism;

- Epilepsy;

- Decompensated chronic heart failure;

- Individual intolerance to the drug;

- Hypocoagulation;

- Thrombophlebitis;

- Children under 3 years;

- Lactation period.

Carefully:

Moderate hepatic insufficiency, deficiency of glucose-6-phosphate dehydrogenase, compensated hypothyroidism, chronic heart failure, gastrointestinal tract diseases (in the anamnesis).

Pregnancy and lactation:

In pregnancy, the drug is used only if the expected benefit to the mother exceeds the potential risk to the fetus. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Inside. Adults 9-12 grams per day (measured with a dosage spoon (3 g of aminosalicylic acid in 1 serving spoon)), dividing into 2-3 doses, or as prescribed by the doctor (day and night). The drug should be taken after meals, washed down with water.

Children over 3 years are prescribed 0.2 g / kg body weight per day in 3-4 doses (daily dose 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.

You can appoint the entire daily dose in one dose, but with poor tolerability, the daily dose is divided into 2-3 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: loss / loss of appetite, nausea, vomiting, flatulence,increased salivation, abdominal pain, diarrhea or constipation, hepatomegaly, increased activity of "hepatic" transaminases, hyperbilirubinemia, drug-induced hepatitis, jaundice, and partially expressed malabsorption syndrome.

From the urinary system: proteinuria, hematuria, crystalluria.

From the hematopoietic system: thrombocytopenia, leukopenia (up to agranulocytosis), B 12-deficient megaloblastic anemia, hemolytic anemia with a positive breakdown of Coombs.

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

Other: hypothyroidism, goitre, myxedema, decreased prothrombin content, pericarditis, hypoglycemia, hypokalemia, decreased prothrombin content, optic neuritis, encephalopathy, Leffler's syndrome (eosinophilic pneumonia, migratory pulmonary infiltrate), vasculitis.

Overdose:

Symptoms: dizziness, vomiting, diarrhea, psychosis.

Treatment: symptomatic therapy.

Interaction:

Increases the concentration of isoniazid in the blood due to competition for common metabolic pathways.Simultaneous use with isoniazid increases the risk of hemolytic anemia.

It interferes with absorption and reduces the effectiveness of rifampicin, erythromycin and lincomycin. If it is necessary to use together with rifampicin, you should divide the time of taking the drugs.

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

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

Antacid preparations do not interfere with drug absorption.

When using thyroid hormones, their analogs, antagonists (including antithyroid drugs), it should be borne in mind that aminosalicylic acid is used to change the concentration of thyroxine and thyroid-stimulating hormone.

Simultaneous use with ethionamide increases the risk of hepatotoxicity. Diphenhydramine reduces the effectiveness of aminosalicylic acid.

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

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

the drug should be immediately discontinued and desensibilization therapy should be performed. During the treatment, it is necessary to systematically examine urine and blood and check the functional state of the liver (activity of "liver" transaminases). Decreased kidney function against tuberculous intoxication or specific damage is not a contraindication to the appointment. The development of proteinuria and hematuria require a temporary discontinuation of the drug.

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

Not installed.

Form release / dosage:

Granules coated with enteric coating, 600 mg / 1 g.

Packaging:4 g, 5 g, 5.34 g, 5.52 g, 6 g, 6.67 g, 6.7 g, 8.34 g, 9.2 g of the preparation in an aluminum foil bag, together with silica gel and instructions, 10, 20, 50 and 100 pieces in a cardboard box; for 100 g of the drug in a foil bag made of aluminum, together with a measuring spoon and a bag of silica gel and instructions enclosed in a plastic container.

Storage conditions:

In a dry, 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 time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002302

Date of registration:08.11.2013

The owner of the registration certificate:Rowecq LimitedRowecq Limited United Kingdom

Manufacturer: & nbsp

VIVIMED LABS, Ltd. India

Information update date: & nbsp13.03.2015

Illustrated instructions

Instructions

PAS Sodium (PAS Sodium)