Paskonat

General characteristics. Structure:

Active ingredient: 3,0 g of sodium of para-aminosalicylate on 100 ml of solution.

Excipients: disodium salt of ethylene diamine tetraacetic acid, sodium pyrosulphite technical, water for injections.

Antituberculous remedy, active only against Mycobacterium tuberculosis.

Pharmacological properties:

Pharmacodynamics. Antituberculous remedy. Reveals bacteriostatic activity to tuberculosis mycobacteria, in combination with other antitubercular drugs slows down development of medicinal resistance and strengthens effect of the corresponding drugs. The tuberculostatic effect of a paskonat is caused by its competitive relationship with paraaminobenzoic acid and biotin which is growth factors of mycobacteria.

Pharmacokinetics. At in introduction almost instantly gets into bodies and fabrics, creating in them high concentration. Drug is metabolized preferential in a liver in 30–60 min. after introduction where there is its acetylation and connection with glycine. Per day with urine 90–100% of the entered dose are removed.

Indications to use:

Active, progressing, preferential fibrous and cavernous, a pulmonary tuberculosis, extra pulmonary tuberculosis of various localization which was earlier inefficiently treated by combinations of various antitubercular drugs. For strengthening of medical effect at polychemotherapy tuberculosis.

Route of administration and doses:

Solution of sodium of para-aminosalicylate is entered intravenously kapelno, since 15 drops a minute. In the absence of local and general reactions rate of administering is increased till 40-60 by drops in a minute. At the first injection by the adult enter 200 ml of 3% of solution. In the absence of side reactions the dose is increased to 400 ml and enter it 5-6 weekly or every other day serially with oral administration of PASK. The course of treatment makes 1-2 months, rarely it is more. To children appoint drug from calculation 0,2gkg body weights, (6,5 ml of 3% of solution for 1 kg of body weight of the child). A daily dose - 200-300 ml.

Features of use:

Apply thin needles and serial introduction to different veins to prevention of emergence of hematomas and phlebitis. In order to avoid depressed cases solution should be entered slowly. During treatment it is necessary to carry out laboratory control of urine and a functional condition of a liver. At prolonged use reveals anti-thyroid action therefore carefully appoint the patient with hypofunction of a thyroid gland.

Side effects:

Most often there are gastrointestinal frustration, deterioration or loss of appetite, nausea, vomiting, abdominal pains, a diarrhea or a lock. Allergic reactions in the form of a small tortoiseshell, purple, enantema, fever, joint pains, the asthmatic phenomena, an eosinophilia can be observed. Increase in the size and liver pain. The specified phenomena, as a rule, disappear at reduction of a dose or short-term cancellation of administration of drug, they are less expressed at the healthy thrice regular nutrition. At allergic manifestations appoint antihistamines, Calcii chloridum, ascorbic acid, at long allergic reactions - corticosteroids. It is necessary to consider a possibility of emergence of hematomas and phlebitis.

Interaction with other medicines:

PASK slows down development of resistance to an isoniazid, slows down acetylation, competes with an isoniazid for the liver N-acetyltransferase metabolizing these drugs that leads to increase in concentration of GINK in blood. Breaks absorption of rifampicin, erythromycin, lincomycin. Breaks digestion of B12 vitamin owing to what perhaps development of anemia. Let's combine with other antitubercular drugs.

Contraindications:

Intravenous administration is contraindicated at hepatitises, nephrosonephrites, a myxedema, cardiovascular insufficiency ІІ-ІІІ to a stage, heavy atherosclerosis, thrombophlebitises, blood coagulation disturbance. Due to the lack of adequate data on safety should not appoint pregnant women and women in the period of a lactation.

Overdose:

The dispepsichesky phenomena, feverish, depressed cases are possible. At the specified manifestations administration of drug should be stopped immediately. Appoint antihistamines, an artificial diuresis, at depressed cases morphine and heart drugs.

Storage conditions:

In dry, protected from light, the place, unavailable to children, at a temperature from +4 to +15 ºС.

Issue conditions:

According to the recipe

Packaging:

Solution for infusions of 3% in glass bottles on 100, 200, 400 ml.