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

Excipients: pregelatinized starch 114.0 mg, sorbitol 36.0 mg, copovidone 8.0 mg, magnesium stearate 6.0 mg, talc 12.0 mg, croscarmello for sodium 24.0 mg;

sheath: triethyl citrate 10.0 mg, ACRYL-Iz 93A240027 90.0 mg: methacrylic acid copolymer 66.00%, talc 16.50%, titanium dioxide E 171 14.66%, silicon dioxide colloid 1.00%, sodium bicarbonate 1 , 00%, sodium lauryl sulfate 0.50%, ferric oxide red oxide E 172 0.23%, lacquer aluminum based on the dye crimson [Ponso 4 R] E 124 0.10%, lacquer aluminum based on indigo carmine E 132 0.01 %.

Description:

Tablets, covered with an enteric-insoluble coat of pink color, capsular. On the fracture 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. At the heart of the tuberculostatic effect of the drug is 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). Operates on mycobacteria,Being 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:

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 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 (Cmah) after taking a dose of 4 g is 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).The total 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 the disturbed - 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:

Hypersensitivity, including other salicylates;

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;

enterocolitis in the acute stage;

Myxedema in the stage of decompensation;

epilepsy,

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

Carefully:

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

Deficiency of glucose-6-phosphate dehydrogenase.

Hypofunction of the thyroid gland.

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

Children 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: deterioration or loss of appetite, increased salivation, nausea, vomiting, flatulence, abdominal pain, diarrhea, or constipation; increased activity of "hepatic" transaminases, hyperbilirubinemia. Rarely - drug-induced hepatitis (including fatal).

Co side of the blood system: rarely - thrombocytopenia, leukopenia (up to agranulocytosis), B 12-deficient megaloblastic anemia.

From the genitourinary system: proteinuria, hematuria, crystalluria.

Allergic reactions: rash (hives, purpura, enanthema), febrile reaction, asthmatic phenomena (bronchospasm), joint pain, eosinophilia.

Other: in large doses has anti-thyroid effect. With prolonged use, there may be a zobogenic effect, drug hypothyroidism, myxedema.

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.

Violates the absorption of vitamin B12 (possibly the development of 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 applied thyroid hormones, their analogs and antagonists (including antithyroid drugs) should be taken into account that aminosalicylic acid background changes and the concentration of thyroid stimulating hormone in blood.

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.

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:

For 300 or 600 tablets in cans of polymer complete with lids.

Banks are placed in a box of cardboard with the application instructions for use.

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:For hospitals

Registration number:LSR-004406/10

Date of registration:18.05.2010 / 03.04.2017

Expiration Date:Unlimited

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Information update date: & nbsp24.06.2017

Illustrated instructions

Instructions

Aquapasc® (Aquapask®)