Simpas - instructions for use, doses, side effects, contraindications

Excipients (core): pregelatinized starch 80.0 mg; sorbitol - 15.0 mg; copovidone - 10.0 mg; magnesium stearate - 9.0 mg; talc - 6.0 mg; croscarmellose sodium - 30.0 mg;

Auxiliary substances (shell): Acrylic-From Pink - 220.0 mg: (methacrylic acid and ethyl acrylate copolymer [1: 1] - 40.00%, titanium dioxide 14.83%, talc 36.98%, triethyl citrate 4.80%, silicon colloidal dioxide 1.25%, sodium hydrogen carbonate - 1,20%, iron dye red oxide - 0,30%, sodium lauryl sulfate - 0.50%, iron dye oxide yellow - 0.14%.

Description:

Capsule pills covered with a pink coating.

On the fracture, the core of the tablet is white or almost white

Pharmacotherapeutic group:anti-tuberculosis drug

ATX: & nbsp

J.04.A.A.01 Aminosalicylic acid

Pharmacodynamics:

Anti-tuberculosis drug. Has a bacteriostatic effect. The tuberculostatic action of the drug is based on competition with para-aminobenzoic acid (PABA) for the active center of the enzyme that converts PABA to dihydrofolic acid and inhibits the synthesis of folic acid in a microbial cell. On tuberculostatic activity inferior to isoniazid and streptomycin. Is active only in relation to Mycobacterium tuberculosis (minimum suppressive concentration (MIC) 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 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 acetylsalicylic 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 h.

With renal insufficiency and elderly people renal elimination of the drug is slowed down.

Indications:

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

Contraindications:

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

- individual intolerance to salicylates (in history);

- severe renal and / or liver failure;

- chronic heart failure in the stage of decompensation;

- arterial hypertension;

- thrombophlebitis;

- hypocoagulation;

- deficiency of glucose-6-phosphate dehydrogenase;

edema due to hypernatremia;

- amyloidosis of internal organs;

- intolerance to fructose;

- Stomach ulcer and duodenal ulcer;

- inflammatory bowel disease in the acute stage;

- Decompensated hypothyroidism;

- epilepsy,

- the period of breastfeeding;

- Children up to 3 years (for this dosage form).

Carefully:

- Renal and / or liver failure of moderate or mild severity (it is recommended to monitor hepatic enzymes during treatment);

- Chronic heart failure;

- Diseases of the gastrointestinal tract in the anamnesis;

- diabetes;

acute hepatitis;

compensated hypothyroidism.

Pregnancy and lactation:

Possible use in pregnancy, if the expected effect of therapy for the mother exceeds the potential risk to the fetus.

Penetrates into breast milk, if necessary, use the drug at the time of treatment should stop breastfeeding.

Dosing and Administration:

Inside, 0.5-1 hour after meals, washed down with acidic liquids (juices: orange, apple, tomato). With increased acidity of gastric juice wash down with water.

Adults appoint 9-12 g / day 3 times a day; a malnourished adult patient (with a body weight of less than 50 kg) - 6 g / day;

Children over 3 years old appoint at the 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 gastrointestinal tract: heartburn, decrease or loss of appetite, increased salivation, nausea, vomiting, flatulence, abdominal pain, diarrhea or constipation; partially pronounced malabsorption syndrome, bleeding from peptic ulcers, increased activity "liver" enzymes, hyperbilirubinemia, jaundice, hepatosplenomegaly; drug hepatitis (including fatal).

From the side of blood and blood-forming organs: thrombocytopenia, leukopenia (up to agranulocytosis), neutropenia, lymphocytosis, eosinophilia, decreased prothrombin, prothrombin time increase, accompanied by bleeding and hemorrhagic purpura, B₁₂-deficit anemia, hemolytic anemia with a positive breakdown of Coombs.

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

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

Other: arthralgia, fever, sore throat, unusual bleeding and bruising, hypoglycemia, increased urea concentration in blood plasma, psychosis, seizures, symptoms of paralysis, with prolonged use in high doses - hypothyroidism, goitre (with or without myxedema), pericarditis, swelling 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 the dose-dependent side effects of the drug.

Treatment: withdrawal of the drug, symptomatic therapy.

Interaction:

Compatible with other antituberculous drugs.

Slows the emergence of resistance to isoniazid and streptomycin.

Simultaneous use with isonazide increases the risk of hemolytic anemia.

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

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-deficit anemia).

Antacids do not interfere with drug absorption.

Enhances the effect of derivatives of coumarin and indandione (requires correction of the dose of indirect anticoagulants).

The use of the drug together with phenytoin leads to an increase in the duration of the presence of phenytoin in the blood plasma.

The use of drugs along with salicylates, phenylbutazone or other non-steroidal anti-inflammatory drugs with increased ability to bind proteins, leads to an increase in the concentration and increase in the duration of the presence of aminosalicylic acid in the blood plasma.

When using thyroid hormones, their analogs and antagonists (including antithyroid means) it should be taken into account that the concentration of thyroxine (T4) and thyroid-stimulating hormone (TSH) in the blood changes with aminosalicylic acid.

Simultaneous use with ethionamide increases the risk of hepatotoxicity.

The use of the drug together with diphenhydramine leads to a decrease in the concentration of aminosalicylicacid in the blood plasma.

Probenecid reduces the excretion of aminosalicylic acid, increasing its concentration in the 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 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 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:

The drug does not affect the performance of potentially hazardous activities requiring special attention and quick reactions (driving and other vehicles, working with moving mechanisms, dispatcher and operator work, etc.)

Form release / dosage:Tablets, coated with enteric coating, 2 g.

Packaging:

For 50, 100 tablets in a sealed, transparent plastic bag; the package is placed in a bottle of high density polyethylene, sealed with aluminum foil with the manufacturer's logo in English, the bottle is closed with a plastic lid. Each bottle is placed in a cardboard box with instructions for use.

For 165, 200, 300, 500, 600, 1000 tablets in a sealed, transparent plastic bag; the package is placed in a bottle of high-density polyethylene, together with an instruction for use, sealed with aluminum foil with the manufacturer's logo in English, the bottle is closed with a plastic lid (for hospitals).

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:On prescription

Registration number:LP-003546

Date of registration:01.04.2016

Date of cancellation:2021-04-01

The owner of the registration certificate: Simpex Pharma Pvt Ltd. Simpex Pharma Pvt Ltd. India

Manufacturer: & nbsp

SIMPEX PHARMA, Pvt. Ltd. India

Representation: & nbspKORAL-MED, CJSCKORAL-MED, CJSC

Information update date: & nbsp13.06.2016

Illustrated instructions

Instructions

Simpas (Simpas)