Faminoalk - instructions for use, dose, side effects, contraindications

Core: hypromellose E5 - 15.0 mg, povidone K30 - 78.0 mg, macrogol 6000 - 9.0 mg, silicon colloidal dioxide - 9.0 mg, sodium stearyl fumarate - 9.0 mg.

Sheath:

Ready enteric coating - 180.0 mg.

(Composition of the shell: methacrylic acid and ethyl acrylate copolymer (1: 1) - 97.56 mg, macrogol 6000 (polyethylene glycol 6000) 4.5 mg, talc 45 mg, triethyl citrate 21.06 mg, titanium dioxide 11.88 mg).

Description:

The tablets are enteric, coated with a white color, biconvex, capsular shaped, on the transverse section of the tablet the nucleus is white or white with a grayish hue of 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 inhibits 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 M. tuberculosis. Aminosalicylic acid acts on the mycobacteria that are in the active state propagation, and virtually no effect on Mycobacterium in the resting stage. 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 isoniazid and streptomycin.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 gistogematicheskie barriers and is distributed on tissues. High concentrations of the drug are found in the kidneys, lungs, liver. In the cerebrospinal fluid the drug penetrates only with inflammation of the meninges. Binding to blood plasma 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 % of the drug is excreted by the kidneys, more than 50 % is displayed in 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), including with multiple drug resistance to other anti-tuberculosis 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; children under 3 years.

Carefully:

Renal and / or liver failure of moderate or mild severity, compensated hypothyroidism, chronic cardiac insufficiency, diseases of the gastrointestinal tract in the anamnesis, diabetes mellitus, acute hepatitis.

Pregnancy and lactation:

The use of aminosalicylic acid in pregnancy is possible when the expected benefit to the mother exceeds the potential risk to the fetus.

If it is necessary to use aminosalicylic acid during lactation, breastfeeding should be stopped.

Dosing and Administration:

Inside, 0.5-1 hour after meals, washed down with acidic liquids (juices: orange, apple, tomato). Do not chew! With increased acidity of gastric juice wash down with water.

Adults - 9-12 grams per day (3-4 g 3 times a day), for emaciated 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 from 3 to 18 years of age are used at the rate of 0.15-0.2 g / kg body weight per day in 3-4 doses, not more than 10 g per day.

With concomitant diseases of the gastrointestinal tract and the initial forms of amyloidosis, the maximum daily dose is 4-6 g per 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 or loss of appetite, increased salivation, nausea, heartburn, vomiting, flatulence, abdominal pain, diarrhea or constipation; hepatomegaly, increased activity of "liver" enzymes, jaundice, drug-induced hepatitis, including fatalities, in part pronounced malabsorption syndrome, bleeding from peptic ulcer.

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, hyperbilirubinemia, B12-deficient megaloblastic anemia, hemolytic anemia, Coombs positive sample.

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

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

Other: arthralgia; fever, sore throat, unusual bleeding and bruising; hypoglycaemia, increased urea concentration in blood plasma; psychosis, convulsions, symptoms of paralysis; with prolonged use in high doses - hypothyroidism, goitre (with myxedema or without it); 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 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. Aminosalicylic acid disturbs the absorption of rifampicin, erythromycin and lincomycin. If it is necessary to use together with rifampicin, you should divide the time of taking the drugs.

Aminosalicylic acid disrupts the absorption of vitamin B12 by almost 55%, resulting in the development of anemia.

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

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

Antacids do not interfere with drug absorption.

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 using iodine-containing hormones of the thyroid gland, their analogs and antagonists (including antithyroid agents)that against the background of paraminobenzoic acid the concentration of thyroxine and thyroid-stimulating hormones in the blood changes.

Ammonium chloride increases the risk of developing crystalluria.

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

Special instructions:

Used in combination with antituberculous drugs. At the first signs, indicating an allergic reaction, the drug should be stopped and desensitizing therapy should be given.

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 an examination 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. Given the side effects of the drug, you should refrain from performing these activities.

Form release / dosage:

Tablets are enteric, coated with 1500 mg.

Packaging:

For 50, 100, 372 or 500 tablets (for hospitals) in a can of polymer with a cover pulled with the control of the first opening. The space free from tablets is filled with cotton absorbent cotton. On the bank stick a label of paper label or writing, or a self-adhesive label. Banks, together with an equal number of instructions for use, are placed in a group package.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

4 years. Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:For hospitals

Registration number:LP-004464

Date of registration:19.09.2017

Expiration Date:19.09.2022

The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia

Manufacturer: & nbsp

FARMASINTEZ, JSC (Irkutsk) Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Faminoalk (Faminosalk)