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

Excipients (core): starch pregelatinized 114.0 mg, sorbitol - 36,0 mg, copovidone 8.0 mg, magnesium stearate 6.0 mg, talc 12.0 mg, croscarmellose sodium 24.0 mg.

Auxiliary substances (shell): Acryl-Iz (methacrylic acid and ethylacrylate copolymer [1: 1] 75.25 mg, titanium dioxide 7.05 mg, talc 6.30 mg, triethyl citrate 7.80 mg, silicon dioxide colloid 1.20 mg, sodium hydrogen carbonate 1.70 mg, iron oxide red 0 , 20 mg, sodium lauryl sulfate 0.50 mg) - 100.0 mg.

Description:

Capsule pills covered with a pink coating.

On the fracture, 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:

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 inhibitory concentration (MIC) in vitro 1-5 μg / ml). Effects on mycobacteria in the 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:

Absorption is high - quickly and well absorbed from the gastrointestinal tract (GIT), has an irritant effect on the mucosa of the gastrointestinal tract. Easily penetrates through histohematetic barriers and distributed in tissues. Achieves high concentrations in caseous masses Moderately penetrates into the cerebrospinal fluid (only with inflammation of the meninges). The maximum concentration (Cmah) after taking a dose of 4 g delivers 75 mcg / ml. The connection with plasma proteins is 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. It is excreted by the kidneys by glomerular filtration (50% in the form of an acetylated derivative). General information The clearance depends on both the metabolic rate and the excretion of the kidneys. The half-life (T1 / 2) with normal kidney function is 30-60 minutes, with broken - up to 23 hours. It penetrates into breast milk.

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:

increased sensitivity to aminosalicylic acid, (including to other salicylates), other components of the drug;

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

decompensated chronic heart failure;

peptic ulcer of the stomach and duodenum;

inflammatory bowel disease in the acute stage;

decompensated hypothyroidism;

epilepsy,

children up to 3 years (for this dosage form).

Carefully:

Moderately expressed hepatic insufficiency (in the treatment it is recommended to carry out control of hepatic enzymes).

Deficiency of glucose-6-phosphate dehydrogenase.

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, during the treatment should stop breastfeeding.

Dosing and Administration:

Inside, 0.5-1 hour after meals, washed down with water, milk, alkaline mineral water, weak (0.5-2%) sodium bicarbonate solution (baking soda).

Adults appoint 9-12 g / day in 3-4 hours; a depleted adult patient (with body weight less than 50 (kg) - 6 g / day in 3-4 doses;

Children over 3 years of age are prescribed at a rate of 0.2 g / kg / day in 3-4 doses (daily dose 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: loss or loss of appetite, increased salivation,nausea, vomiting, flatulence, abdominal pain, diarrhea, or constipation; increased activity of "liverwort" transaminases, hyperbilirubinemia, jaundice; drug hepatitis (including fatal).

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 (Urticaria, purpura, enanthema, exfoliative dermatitis syndrome resembling infectious mononucleosis or lymphoma), fever, bronchospasm, arthralgia, eosinophilia.

Other: antithyroid action; with prolonged use - zobogenous effect, drug hypothyrosis, myxedema; pericarditis, hypoglycemia, optic neuritis, encephalopathy, Leffler's syndrome (eosinophilic pneumonia, migratory pulmonary infiltrate), vasculitis, a decrease in prothrombin content.

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.

It inhibits 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.

It interferes with absorption and reduces the effectiveness of rifampicin, erythromycin and lincomycin.

Disrupts the assimilation of cyanocobalamin (possible development of 12-deficiency 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).

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

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 plasma.

Reduces the concentration of digoxin in the blood by 40%. Ammonium chloride increases the risk

development of crystalluria.

Special instructions:

Used in combination with more active antituberculous drugs means.

When treatment is recommended to monitor the activity of "liver" transaminases. Decreased kidney function against tuberculous intoxication or a specific lesion (nephrotuberculosis) 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:

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 1 g.

Packaging: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 can is placed in a cardboard box with instructions for medical use.

For 165, 200, 300 tablets in a sealed, transparent plastic bag, the package is placed in a bottle of high-density polyethylene, along with a medical instruction, sealed with aluminum foil with the manufacturer's logo in English, the bottle is closed with a plastic lid.

For 500, 600, 1000 tablets in a sealed, transparent plastic bag, the package is placed in a bottle of high-density polyethylene, together with a medical instruction, 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-001367

Date of registration:16.12.2011

The owner of the registration certificate:KORAL-MED, CJSC KORAL-MED, CJSC Russia

Manufacturer: & nbsp

SIMPEX PHARMA, Pvt. Ltd. India

Information update date: & nbsp17.01.2013

Illustrated instructions

Instructions

Simpas (Simpas)