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

Description:The capsular biconvex tablets covered with a film membrane from light pink to dark pink color. On the cross section, the core of the tablet is white or almost white in color.

Pharmacotherapeutic group:Anti-tuberculosis drug

ATX: & nbsp

J.04.A.A.01 Aminosalicylic acid

Pharmacodynamics:

Has a bacteriostatic effect. The basis tuberculostatic action is competition with para-aminobenzoic acid (ration) of the active site digidropteroatsintetazy - converting enzyme ration in dihydrofolic acid, and inhibits the synthesis of folic acid in the microbial cell and / or the synthesis of cell wall components of mycobacteria, reducing iron grip 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 in combination with other anti-tuberculosis drugs, which slows the development of resistance to them.

Pharmacokinetics:

Absorption from the gastrointestinal tract - fast and high; has an irritating effect on the mucosa of the gastrointestinal tract. Easily penetrates through the histogematic barriers and is distributed in tissues. Achieves high concentrations in caseous masses. Moderately penetrates into the cerebrospinal fluid (only with inflammation of the meninges). The maximum concentration (C_mOh) after taking in a dose of 4 g averages 20 μg / ml (9 to 35 μg / ml). Connection with plasma proteins - 50-60%. The main pathway of metabolism is acetylation.

Metabolised in the liver (more than 50% acetylated to inactive metabolites) and partially in the stomach.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. Half-life (T_1/2) with normal kidney function - 30-60 minutes, with chronic renal failure - up to 23 hours. Penetrates into breast milk.

Indications:

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

Contraindications:

Hypersensitivity to aminosalicylic acid (including other salicylates), other components of the drug; severe kidney and liver diseases (renal failure and / or liver failure, nephritis of nontuberculous etiology, hepatitis, cirrhosis); amyloidosis of internal organs; peptic ulcer of the stomach and duodenum; inflammatory bowel disease in the acute stage; decompensated hypothyroidism; decompensated chronic heart failure (incl.against the background of heart disease); arterial hypertension; edema caused by hypernatremia; thrombophlebitis, hypocoagulation, epilepsy, children under 3 years old.

Carefully:

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

Pregnancy and lactation:

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

During lactation, the issue of stopping breastfeeding during the treatment with the drug should be resolved.

Dosing and Administration:

Inside, 0.5-1 hour after eating, washing with water.

Adults - 9-12 g / day in 3-4 sessions; a malnourished adult patient (with a body weight of less than 50 kg) - 6 g / day in 3-4 doses.

Children older than 3 years - at a rate of 0.2 g / kg / day in 3-4 doses (daily dose of not more than 10 g).

In conditions of outpatient treatment, the entire daily dose can be administered in one session, 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 / 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, heartburn, vomiting, flatulence, abdominal pain, diarrhea, or constipation; increased activity of "hepatic" transaminases, hyperbilirubinemia, jaundice, hepatomegaly; drug hepatitis (including fatal), partially expressed malabsorption syndrome.

From the hematopoiesis: 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, erythema, a syndrome resembling infectious mononucleosis or lymphoma), fever, bronchospasm, arthralgia, eosinophilia; anaphylactic shock, malignant exudative erythema (Stevens-Johnson syndrome), angioedema, toxic epidermal necrolysis (Lyell's syndrome).

Other: antithyroid effect, goitre, zobogenic effect, drug hypothyroidism,myxedema; pericarditis; hypoglycemia; glucosuria; hypokalemia; optic neuritis; encephalopathy; to raisewurea concentration in the blood plasma; Leffler's syndrome (eosinophilic pneumonia, migratory pulmonary infiltrate); vasculitis; decreased prothrombin content; psychosis, convulsions, symptoms of paralysis.

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.

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.

Disrupts the assimilation of cyanocobalamin (possible development of B12-deficiency anemia). Reduces the concentration of digoxin in the blood by 40 %.

Antacids do not interfere with drug absorption.

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

When using iodine-containing hormones of the thyroid gland, their analogs and antagonists (including antithyroid agents), one should take into account that against the background of para- aminobenzoic acid (PABA) the concentration of thyroxine (T4) and thyrotropic hormone (TSH) in the blood changes.

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.

Special instructions:

Used in combination with more active antituberculous drugs.

During the treatment it is recommended to systematically examine urine and blood, monitor the 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 an examination 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 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:

In connection with the possibility of the appearance of psychosis, seizures and other side effects associated with taking the drug, it is recommended to refrain from driving, other mechanisms and perform work that requires increased concentration.

Form release / dosage:

Tablets, coated with enteric coating, 1 g.

Packaging:

In the production of the drug at the enterprise, SP. Incomed Pvt. Ltd., India

For 10 tablets in an aluminum / PVC blister.

For 1, 3, 5 or 10 blisters together with instructions for medical use in a pack of cardboard.

Packing for hospitals

For 100, 500 or 1000 tablets per package of polyethylene. A label is attached to the package.

The package together with instructions for medical use in a plastic container with a screw cap and first opening control; a label is attached to the container.

When the drug is packaged in the company OOO PharmConcept, Russia

For 1, 3, 5 or 10 blisters together with instructions for medical use in a pack of cardboard.

Packing for hospitals

At 1.5, 10, 20, 30 or 40 containers together with the corresponding number of instructions for medical use in a pack of cardboard.

In the production of the drug at the enterprise OOO PharmConcept, Russia

For 10 tablets in a blister of PVC film and a combined material based on aluminum foil and a film of polyethylene, polypropylene, polyethylene terephthalate.

For 1, 3, 5 or 10 blisters together with instructions for medical use in a pack of cardboard.

Packing for hospitals

For 100, 500 or 1000 tablets in a polymer jar complete with a lid (with the control of the first opening). On the bank stick a label of paper label or writing, or a self-adhesive label.

For 48 cans of 100 tablets, 12 cans of 500 tablets or 6 cans of 1000 tablets together with an equal number of instructions for medical use are placed in a box of cardboardcorrugated. On the box, stick a label of paper label or writing, or a self-adhesive label.

On 1 bank together with the instruction on medical application place in a pack a cardboard.

Storage conditions:

Store in a 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 the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002829

Date of registration:20.01.2015 / 01.11.2017

Expiration Date:20.01.2020

The owner of the registration certificate:S.P.Inkomed Pvt.LtdS.P.Inkomed Pvt.Ltd India

Manufacturer: & nbsp

S.P.INCOMED, Pvt.Ltd. India

FarmKoncept, OOO Russia

Information update date: & nbsp25.05.2018

Illustrated instructions

Instructions

Sodium para-aminosalicylate (Sodium para-aminosalicylate)