Протионамид-Акри®

General characteristics. Structure:

Active ingredient: 250 mg of Prothionamidum.

Excipients: cellulose microcrystallic, potato starch, povidone, gipromelloz, silicon dioxide colloid, magnesium stearate, sodium carboxymethylstarch, talc, macrogoal, hydroxypropyl cellulose, titanium dioxide, dye yellow-orange (оранж S).

Pharmacological properties:

Pharmacodynamics. Antituberculous remedy of the II row. Works bacteriostatically, blocks synthesis of the mikoliyevy acids which are the most important structural component of a cell wall of mycobacteria of tuberculosis. Has properties of the antagonist of niacin. In high concentration breaks synthesis of protein of a microbic cell and works bakteritsidno. It is effective concerning the mycobacteria of tuberculosis steady against row drugs I.

Use in a combination with other antituberculous remedies reduces probability of emergence of resistance of the causative agent of tuberculosis.

Pharmacokinetics. Prothionamidum is quickly soaked up in zheludochno — an intestinal path, creating the maximum concentration of drug in a blood plasma in 2-4 hours after intake, gets in healthy and patholologically the changed types of fabric (tuberculous focuses and cavities in lungs, a serous and purulent pleural exudate, cerebrospinal fluid at meningitis).

In an organism partially turns into the sulphoxide having tuberculostatic activity. It is partially allocated in not changed look (to 15-20% of the accepted dose) with urine and excrements.

Indications to use:

Prothionamidum is applied to treatment of all forms of tuberculosis, including at resistance of the activator to other antitubercular drugs (the I row) or their intolerance.

Route of administration and doses:

Accept drug inside after food. The adult appoint 0,25 g 3 times a day, at good tolerance — on 0,5 g 2 times a day. At patients 60 years are more senior and at body weight less than 50 kg the daily dose should not exceed 0,75 g (more often appoint 0,25 g 2 times a day).

To children appoint at the rate of 10-20 mg/kg of body weight a day.

Features of use:

It is necessary to avoid combined use of Prothionamidum and alcohol because of danger of emergence of a condition of oppression of TsNS (connected with strengthening of toxic effect of alcohol).

At the combined use of Prothionamidum with an isoniazid and Cycloserinum it is necessary to pay special attention to a possibility of disturbance of mentality.

As drug is constantly used in a combination with other antitubercular medicines, regular control of serumal transaminases, gamma глутаматтрансферазы and an alkaline phosphatase is necessary. At patients with a diabetes mellitus control of level of glucose in blood at least once a month is necessary.

Skin reactions can be the first signs of pellagropodobny side effects. It should be regarded as the reason of necessary drug withdrawal.

Side effects:

From cardiovascular system: tachycardia, weakness, orthostatic hypotension.

From digestive tract: appetite loss, nausea, vomiting, dryness in a mouth or hypersalivation, "metal" smack. After drug withdrawal these phenomena, as a rule, quickly pass.

Often during treatment rise in blood of level of transaminases is noted. The expressed abnormal liver functions with symptoms of hepatitis and jaundice are seldom noted.

Hepatotoxic of drug depends on the available abnormal liver functions, such as injury of a liver as a result of alcoholism or after operative measures. These side effects are noted especially at a combination therapy with an isoniazid, rifampicin and Pyrazinamidum.

Skin reactions are noted seldom, pellagropodobny reactions according to a combination of skin manifestations and disturbances from the central nervous system are in some cases described.

Disturbances from endocrine system are sometimes noted. Along with development of a hypoglycemia (decrease in sugar in blood less than 50 mg/%) at patients with a diabetes mellitus, development of a gynecomastia is described (increase in chest glands at men). Disturbance of a menstrual cycle and impotence, and also a hypothyroidism (depression of function of a thyroid gland) is seldom noted.

Prothionamidum in rare instances causes disturbances peripheral and the central nervous system: sleeplessness, excitement, a depression, uneasiness, it is rare — dizziness, drowsiness.

In a combination with an isoniazid polyneuropathy cases are described. Reception of Prothionamidum can cause dizziness, headaches, weakness, disturbance of concentration of attention, frustration of mentality. Seldom — an optic neuritis, tachycardia. The concomitant use of other antitubercular drugs operating on TsNS, such as an isoniazid and Cycloserinum can lead to strengthening of side effects from the central nervous system. The same effect can accord also a concomitant use of alcohol. Allergic reactions and disturbances from marrow are in some cases described.

Interaction with other medicines:

At a combination therapy of tuberculosis it is necessary to take the additive hepatotoxic effect of separate drugs into account. Especially it belongs to Prothionamidum combination with an isoniazid, rifampicin and Pyrazinamidum. The active effect on the central nervous system is noted at combined use of an isoniazid and Cycloserinum.

The concomitant use of alcohol leads to oppression of TsNS. In certain cases at reception of Prothionamidum it is necessary to lower a dose of insulin or peroral anti-diabetic drugs.

Contraindications:

Prothionamidum cannot be applied at individual hypersensitivity to drug components, during pregnancy and a lactation, acute gastritis, a peptic ulcer of a stomach and a 12-perstny gut, erosive and ulcer colitis, an acute hepatitis, cirrhosis, an alcoholism. Children's age up to 3 years (for this dosage form).

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Not to apply after a period of validity. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 250 mg. On 10 tablets in a blister strip packaging. On 50 or 100 tablets in bank of orange glass or bank from polypropylene (polyethylene). Each can or on 5 or 10 blister strip packagings together with the application instruction is placed in a pack from a cardboard. On 500 or 1000 tablets in a package from a film polyethylene. The plastic bag together with the application instruction is placed in a container from polypropylene (polyethylene) (for a hospital).

From 0,5 to 15 kg of tablets in a package from a film polyethylene. The plastic bag together with the application instruction is placed in a cardboard drum (for a hospital).