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

Excipients: sorbitol 7 mg / 17.5 mg, povidone K-30 6.6 mg / 16.5 mg, silicon dioxide colloid (aerosil 300) 2.2 mg / 5.5 mg, calcium stearate 2.2 mg / 5.5 mg, citric acid monohydrate 2 mg / 5 mg.

Sheath: film coating (methacrylic acid and ethyl acrylate copolymer [1: 1] (40.0%), talc (37.25%), titanium dioxide (15.0%), triethyl citrate (4.8%), silicon dioxide colloid (1 , 25%), sodium hydrogen carbonate (1.2%), sodium lauryl sulfate (0.5%)) 22 mg / 55 mg.

Description:

Round, biconvex tablets covered with a coat, white or almost white with a creamy shade of color. On the cross-section the nucleus is from white to yellowish color.

Pharmacotherapeutic group:Anti-tuberculosis drug

ATX: & nbsp

J.04.A.A.01 Aminosalicylic acid

Pharmacodynamics:

Aminosalicylic acid has a bacteriostatic effect against Mycobacterium tuberculosis (minimal inhibitory concentration in vitro 1-5 μg / ml).

Mechanism of action: aminosalicylic acid competes with paraaminobenzoic acid (PABA) and suppresses the synthesis of folic acid in mycobacteria tuberculosis, inhibits the formation of mycobacterium, a component of the mycobacterial wall, which leads to a decrease in the capture of iron Mycobacterium tuberculosis.

Aminosalicylic acid 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, is active only in relation to Mycobacterium tuberculosis, does not affect other non-tuberculosis mycobacteria.

Reduces the likelihood of bacterial resistance to streptomycin and isoniazid.

It is used only in combination with other anti-tuberculosis drugs, which slows the development of resistance to them.

Pharmacokinetics:

Well absorbed when taken orally. Easily passes through the histohematological barriers and is distributed along the tissues. High concentrations of the drug are found in the lungs, kidneys and liver. In the cerebrospinal fluid the drug penetrates only with inflammation of the meninges. Binding to blood proteins - 50-60%. The maximum concentration in the blood serum after oral administration of a dose of 4 g is 20 μg / ml (it can vary from 9 to 35 μg / ml). The average time to reach the maximum plasma concentration is 6 hours (varies from 1.5 to 24 hours). The concentration of aminosalicylic acid in plasma 2 mg / ml is maintained for 7.9 hours (varies from 5 to 9 hours), and 1 mg / ml on average for 8.8 hours (variability from 6 to 11.5 hours). Metabolised in the liver. Aminosalicylic acid is excreted by glomerular filtration: 80% is excreted by the kidneys, more than 50% is excreted in the acetylated form. The half-life is 0.5-1 hour. In renal failure and in elderly people, renal elimination of the drug is slowed down.

Indications:

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

Contraindications:

Hypersensitivity to aminosalicylic acid (including other salicylates) and other components of the drug, individual intolerance to salicylates (in anamnesis); severe renal and / or hepatic insufficiency; heart failure in the stage of decompensation; peptic ulcer of the stomach and duodenum; inflammatory bowel disease in the acute stage; uncompensated hypothyroidism; epilepsy; thrombophlebitis; hypocoagulation; the period of breastfeeding; deficiency of glucose-6-phosphate dehydrogenase; arterial hypertension; edema caused by hypernatremia; amyloidosis of internal organs; intolerance to fructose; children's age up to 3 years.

Carefully:

Renal and / or hepatic insufficiency of moderate and mild severity, compensated hypothyroidism, chronic heart failure, gastrointestinal diseases in history, diabetes mellitus, acute hepatitis.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the intended benefit from therapy for the mother exceeds the potential risk to the fetus.

If necessary, use during lactation should stop breastfeeding.

Dosing and Administration:

Inside, 0.5-1 hour after a meal, washed down with acidic liquids (juices: orange, tomato, apple). Do not chew! With increased acidity of gastric juice, the drug should be washed down with water.

Adults on 9-12 g / day in 3-4 reception. Exhausted adult patients (with a body weight of less than 50 kg), as well as with poor tolerability - in a dose of 6 g per day.

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

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

The number of courses and the total duration of treatment are determined individually.

In conditions of outpatient treatment, the entire daily dose can be used for one dose (in case of good tolerability).

Side effects:

From the gastrointestinal tract: decrease and loss of appetite; increased salivation; nausea; heartburn; vomiting; flatulence; abdominal pain; diarrhea or constipation; hepatomegaly; increased activity of "liver" transaminases; jaundice; drug hepatitis, including fatalities; partially expressed malabsorption syndrome; bleeding from peptic ulcer.

On the part of the organs of hematopoiesis: thrombocytopenia; leukopenia (up to agranulocytosis); neutropenia; lymphocytosis; eosinophilia; a decrease in prothrombin, an increase in prothrombin time, accompanied by bleeding and hemorrhagic purpura; hyperbilirubinemia; AT₁₂-deficient megaloblastic anemia; Hemolytic anemia with a positive breakdown of Coombs.

Allergic reactions: itching, rash (urticaria, purpura, enantema, exfoliative dermatitis, erythema, a syndrome resembling infectious mononucleosis or lymphoma), bronchospasm, Leffler's syndrome (eosinophilic pneumonia, migratory pulmonary infiltrate), vasculitis, anaphylactic shock, malignant exudative erythema (Stevens-Johnson syndrome ), angioedema, Lyell's syndrome.

From the genitourinary system: proteinuria, hematuria, crystalluria, glucosuria.

Other: arthralgia; fever; a sore throat; unusual bleeding and bruising; hypoglycemia; increased urea concentration in blood plasma; psychosis; convulsions; symptoms of paralysis; with prolonged use in high doses - hypothyroidism, goitre (with or without myxedema); pericarditis; swelling of the joints; lupus-like syndrome accompanied by lesions of the spleen, liver, kidneys, digestive tract, bone marrow and nervous system (eg, radicular pain, meningism); encephalopathy; optic neuritis; superinfection.

Overdose:

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

Treatment: withdrawal of the drug, symptomatic therapy.

Interaction:

Compatible with other antituberculous drugs.

Slows the emergence of resistance to isoniazid and streptomycin.

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

Violates the absorption of rifampicin, erythromycin and lincomycin. If you need co-therapy with rifampicin, taking medications should be divided in time.

Disrupts the assimilation of cyanocobalamin (possible development of B₁₂-deficit anemia).

Antacids do not interfere with drug absorption.

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

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.

Ammonium chloride increases the risk of developing crystalluria.

Simultaneous administration 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 plasma.

With simultaneous application with phenytoin, the concentration in the blood plasma of phenytoin increases.

Simultaneous use with salicylates, phenylbutazone or other anti-inflammatory drugs,possessing an increased ability to bind to blood 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.

The drug can reduce the absorption of digoxin and its concentration in the blood plasma. Digoxin dose adjustment may be required.

Special instructions:

Used in combination with other antituberculous drugs.

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 (control the activity of "liver" transaminases).

It is necessary to maintain the pH of the urine neutral or alkaline to prevent crystalluria.

Decreased kidney function against tuberculous intoxication or a specific lesion is not a contraindication to the prescription of the drug. The development of proteinuria and hematuria requires a temporary discontinuation of the drug.

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

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.

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:

Intestinal-coated tablets, 200 mg and 500 mg.

Packaging:

For hospital: 100, 372 or 500 tablets per package of polyethylene film made of high-density polyethylene. The plastic bag together with the instruction for use is packed in a polymer jar with a screw cap made of polypropylene.

8 cans are placed in a group package.

Storage conditions:

In the 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 expiry date.

Terms of leave from pharmacies:For hospitals

Registration number:LP-004004

Date of registration:07.12.2016

Expiration Date:07.12.2021

The owner of the registration certificate:EDVANSD TRADING, LLCEDVANSD TRADING, LLC Russia

Manufacturer: & nbsp

RAFARMA, JSC Russia

Representation: & nbspAdvansd Trading, OOOAdvansd Trading, OOO

Information update date: & nbsp25.05.2018

Illustrated instructions

Instructions

Sodium para-aminosalicylate (Sodium para-aminosalicylate)