Para-aminosalicylate sodium - instructions for use, dose, side effects, contraindications

Anti-tuberculosis drug. Has a bacteriostatic effect on the mycobacterium tuberculosis (Mycobacterium tuberculosis), being in a state of active reproduction, and practically does not affect the mycobacteria at rest. The mechanism of action is associated with the inhibition of the synthesis of folic acid in a microbial cell and with the suppression of the formation of mycobactin, a component of the bacterial wall, which leads to a decrease in the capture of iron by mycobacteria. Slightly affects the pathogen, located intracellularly. Does not affect other non-tuberculous mycobacteria. It is used in combination with other anti-tuberculosis drugs, slowing the development of resistance to them.

Pharmacokinetics:Metabolised in the liver. 80% of aminosalicylic acid is excreted by the kidneys through glomerular filtration (more than 50% - in the form of acetylated derivative). Easily penetrates through the histogematic barriers and is distributed in tissues. Achieves high concentrations in caseous masses. In the cerebrospinal fluid the drug penetrates only with inflammation of the meninges. The connection with plasma proteins is 50-60%.The total clearance depends on both the metabolic rate and the excretion of the kidneys. Half-life with normal kidney function is 30-60 minutes, with chronic renal failure - up to 23 hours. Penetrates into breast milk.

Indications:Drug-resistant tuberculosis of various forms and localizations in combination with other reserve antituberculous agents.

Contraindications:

hypersensitivity to the drug, incl. to other salicylates;

severe kidney and liver diseases (renal and / or hepatic insufficiency, nephritis of non-tuberculous etiology, hepatitis, cirrhosis);

Decompensated chronic heart failure (including against the background of malformation heart);

amyloidosis;

peptic ulcer of stomach and duodenum;

inflammatory bowel disease in the acute stage;

decompensated hypothyroidism;

epilepsy;

lactation period.

thrombophlebitis, blood clotting disorder;

severe atherosclerosis.

Carefully:Moderate hepatic insufficiency, deficiency of glucose-6-phosphate dehydrogenase, compensated hypothyroidism.

Dosing and Administration:

Intravenously (drip).

As a solvent, 500 ml of water for injection should be used.

The daily dose for adults and children over 14 years is 10-15 g.

For children under 14 years old the daily dose is 200-300 mg / kg body weight.

The infusion process by intravenous administration should take 2-4 hours at a rate of 30 drops per minute, and after 15 minutes in the absence of local and general reactions - 40-60 drops per minute. At the first infusion - no more than 250 ml of solution, in the absence of side effects - 500 ml-5-6 times a week or every other day, alternating with admission inside.

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

Precautions for use

Ready to use the solution immediately after its preparation.

A solution that has lost transparency or has changed its coloring is unsuitable for use.

If it is necessary to use the preparation for a long period of time, it is recommended to maintain the electrolyte balance of potassium salts by oral administration or addition of a certain amount of appropriate potassium preparations for infusions, based on the preliminary assessment of the potassium content in the plasmablood. It is recommended to regularly monitor activity "hepatic" enzymes, urine and blood tests. With the development of hematuria and proteinuria, a temporary withdrawal of the drug is required.

Side effects:

From the digestive system: decreased or loss of appetite, increased salivation, nausea, vomiting, flatulence, abdominal pain, diarrhea, or constipation; increased activity of "hepatic" transaminases, hyperbilirubinemia, jaundice, drug hepatitis (including fatal). .

From the side hemopoiesis: thrombocytopenia, leukopenia (up to agranulocytosis), B 12-deficiency anemia, hemolytic anemia with a positive Coombs breakdown.

From the genitourinary system: proteinuria, hematuria, crystalluria.

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

Other: at the maximum dose (500 ml 5-6 times a week) - antithyroid effect; with prolonged use - zobogenous effect, drug hypothyrosis, myxedema; pericarditis, hypoglycaemia, optic neuritis, encephalopathy, syndrome Leffler (eosinophilicpneumonia, migratory pulmonary infiltrate), vasculitis, decline prothrombin content.

Overdose:

In case of anaphylactic shock, the drug should be stopped immediately and appropriate measures taken: administration of histamine receptor blockers, glucocorticosteroids, sympathomimetics, artificial respiration.

When overdosing, the drug should be discontinued, if necessary - hemodialysis.

Interaction:

Compatible with other anti-TB drugs.

Slows the emergence of resistance to isoniazid and streptomycin.

When combined with isoniazid or phenytoin increases their concentration in the blood plasma due to competition for common metabolic pathways. It interferes with absorption and reduces the effectiveness of rifampicin, erythromycin and lincomycin. Do not simultaneously inject with solutions of rifampicin and protionamide in the total mixture.

Application of the drug together from salicylates, phenylbutazone or other anti-inflammatory drugs with 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.

Diphenhydramine reduces the effectiveness aminosalicylic acid.

Inhibits the absorption of folate and can enhance the toxicity of folate antagonists, for example, methotrexate.

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).

When applying 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 blood changes against aminosalicylic acid.

Ammonium chloride increases the risk of developing crystalluria.

Simultaneous use with ethionamide increases the risk of hepatotoxicity. Probenecid reduces the excretion of aminosalicylic acid, increasing its concentration in the plasma.

Special instructions:

Used in combination with more active antituberculous drugs.

During the treatment it is recommended to regularly monitor the activity of "liver" - transaminases.

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

At the first signs, indicating an allergic reaction, the drug should be stopped and desensitizing therapy should be given.

Effect on the ability to drive transp. cf. and fur:Evidence that the drug may hinder the performance of work requiring concentration of attention and speed of psychomotor reactions (driving vehicles, control mechanisms, instruments, etc.) was not revealed.

Form release / dosage:

Lyophilizate for solution for infusion, 13.49 g.

Packaging:To 14.14 g. Of the drug in a glass bottle of neutral glass (type I) (500 ml capacity, sealed with a rubber stopper under an aluminum runner unclosed plastic cover), wrapped in a black plastic bag. 1 bottle together with transflo (a device for dissolving lyophilizate in a vial through a stopper), plastic spiral for hanging the bottle and instructions for use in a pack of cardboard.

Storage conditions:Store in a dark place at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:3 years.
Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000742

Date of registration:29.09.2011

The owner of the registration certificate:Roushan Pharma Co., Ltd.Roushan Pharma Co., Ltd. India

Manufacturer: & nbsp

RUSAN PHARMA, Ltd. India

Information update date: & nbsp29.09.2011

Illustrated instructions

Instructions

Para-aminosalicylate sodium (Sodium para-aminosalicylate)