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

Excipients: calcium hydrophosphate dihydrate, microcrystalline cellulose, giprolase (hydroxypropylcellulose), calcium stearate, croscarmellose sodium (impellosis);

shell: Opadrai II (series 85): polyvinyl alcohol partially hydrolyzed, macrogol 3350, talc, titanium dioxide E 171, iron dye oxide yellow E 172, aluminum lacquer based on the dye yellow quinoline E 104.

Description:

The tablets covered with a film cover of yellow color, round,

biconvex. At the break of yellow color.

Pharmacotherapeutic group:anti-tuberculosis drug

ATX: & nbsp

J.04.A.D.01 Prothionamide

Pharmacodynamics:

Second-line anti-tuberculosis drug. It blocks the synthesis of mycolic acids, which are the most important structural component of the mycobacterium tuberculosis cell wall. Has the properties of a nicotinic acid antagonist. In high concentrations, it breaks the synthesis of the protein of the microbial cell.

Has a bacteriostatic effect. Active, especially in an acidic environment, with respect to fast and slow breeding Mycobacterium tuberculosis, located outside and intracellularly. In high concentrations, it acts on Mycobacterium leprae and some atypical mycobacteria. Effective against mycobacteria tuberculosis, resistant to drugs of the I series. Strengthens phagocytosis in the focus of specific inflammation.

In the process of treatment, the resistance of microorganisms rapidly develops, complete cross-resistance to ethionamide is noted. It inhibits the development of resistance to other anti-tuberculosis drugs. Transported better than ethionamide.

Pharmacokinetics:

Prothionamide is rapidly absorbed in the gastrointestinal tract, creating a maximum concentration of the drug in the blood plasma 2-3 hours after ingestion.Penetrates into healthy and pathologically altered tissues (tubercular foci and caverns in the lungs, serous and purulent pleural effusion, cerebrospinal fluid with meningitis), metabolized in the liver, one of the metabolites - sulfoxide - has tuberculosis about static activity. It is excreted by the kidneys and with bile (15-20% unchanged).

Indications:

Combined therapy of tuberculosis (pulmonary and extrapulmonary forms, with poor tolerance or resistance to treatment with anti-tuberculosis drugs of the first series): infiltrative, ulcerative and exudative processes.

Contraindications:

Prothionamide can not be used for individual hypersensitivity to the components of the drug, acute gastritis, peptic ulcer and duodenal ulcer, erosive ulcerative colitis, acute hepatitis, liver cirrhosis, chronic alcoholism, during pregnancy and lactation, in childhood (not recommended appoint children under 14 years old).

Carefully:

Diabetes mellitus, severe hepatic insufficiency.

Pregnancy and lactation:

When pregnancy is contraindicated - protionamide passes through the placenta.

For the duration of treatment, breastfeeding should be discontinued.

Dosing and Administration:

Take the drug inside after eating.

Adults appoint 250 mg 3 times a day; with good tolerability - 500 mg 2 times a day. The daily dose for adults is 500-1000 mg.

In patients older than 60 years and with a body weight of less than 50 kg, the daily dose should not exceed 750 mg (more often prescribed 250 mg twice a day).

Duration of the course is 8-9 months.

Children over 14 years of age are prescribed at the rate of 10-20 mg / kg of body weight per day.

Side effects:

From the digestive system: loss of appetite, nausea, vomiting, dryness or hypersalivation, metallic taste in the mouth. After the withdrawal of the drug, these phenomena tend to quickly pass.

Often during treatment there is an increase in the activity of transaminases. Rare violations of liver function with signs of hepatitis and jaundice are rare. Hepatotoxicity of the drug depends on the existing violations of the liver, such as liver damage as a result of alcoholism. These side effects are noted especially in combination therapy with isoniazid, rifampicin and pyrazinamide.

From the central nervous system: insomnia, agitation, depression, anxiety, rarely - dizziness, drowsiness, headache, asthenia, in single cases - paresthesia, peripheral neuropathy, optic neuritis. Simultaneous reception of other antituberculous drugs acting on the central nervous system, such as isoniazid or cycloserine, can lead to an increase in side effects from the central nervous system. The same effect can have a simultaneous reception of alcohol.

From the side of the cardiovascular system: tachycardia, orthostatic hypotension.

From the endocrine system: Sometimes there are violations of the endocrine system: hypoglycemia in patients with diabetes mellitus, the development of gynecomastia (an increase in mammary glands in men). Rarely there is a violation of the menstrual cycle and a decrease in potency, as well as hypothyroidism (a decrease in thyroid function).

Allergic reactions: skin rash. Skin reactions are rare, in some cases described pellagro-like reactions, respectively, with a combination of skin manifestations and disorders from the central nervous system.

Interaction:

Compatible with isoniazid, pyrazinamide, cycloserine and other antituberculous drugs.

Isoniazid increases the concentration of protionamide in plasma.

With combined therapy of tuberculosis, the additive hepatotoxic effect of individual drugs should be taken into account. This is especially true for the combination of a protionamide with isoniazid, rifampicin and pyrazinamide. Additive effect on the central nervous system is noted with the combined use of isoniazid and cycloserine.

Simultaneous reception of alcohol leads to depression of the central nervous system.

In certain cases, when taking protionamide, it is necessary to reduce the dose of insulin or hypoglycemic drugs used inside.

Special instructions:

The course of treatment is recommended to start after determining the sensitivity of bacteria and determine the dose based on individual sensitivity and tolerability.

Joint use of protionamide and alcohol should be avoided because of the danger of the emergence of conditions of central nervous system depression (associated with increased toxic effect of alcohol).

With the combined use of a protionamide with isoniazid and cycloserine, special attention should be paid to the possibility of mental disorders.

Because the drug is constantly used in combination with other anti-TB drugs, regular monitoring of serum transaminases, gamma-glutamintransferase and alkaline phosphatase is necessary.

Patients with diabetes need to monitor blood glucose at least once a month, and also adjust the dose of insulin or oral hypoglycemic agents.

Skin reactions may be the first signs of pellagruide-like side effects. This should be regarded as the reason for the necessary withdrawal of the drug.

To reduce the risk of side effects are combined with taking pyridoxine (vitamin B₆) in a dose of 150-300 mg / day.

Form release / dosage:Tablets, film-coated, 250 mg.

Packaging:

For 10 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil printed lacquered.

5 or 10 contour mesh packages with instructions for use in a pack of cardboard.

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:P N003856 / 01

Date of registration:18.11.2009

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

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Representation: & nbspVALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Information update date: & nbsp09.09.2015

Illustrated instructions

Instructions

Prothionamide (Protionamide )