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

Excipients: lactose, corn starch, microcrystalline cellulose, hypromellose (Methocel E5 LVP), silicon dioxide colloid, magnesium stearate, sodium starch glycolate;

shell: hypromellose (Methocel E5 LVP), polyethylene glycol 400, talc, titanium dioxide, dye quinoline yellow.

Description:

Tablets, film-coated, yellow, round, biconvex, with oblique margins, smooth on both sides.

Pharmacotherapeutic group:anti-tuberculosis drug

ATX: & nbsp

J.04.A.D.01 Prothionamide

Pharmacodynamics:

Second-line anti-tuberculosis drug. It acts bacteriostatically, 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 and acts bactericidal.

Effective against mycobacteria tuberculosis, resistant to drugs of the I series.

The use in combination with other anti-tuberculosis drugs reduces the likelihood of developing tuberculosis resistance.

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). In the body it is partially converted into sulfoxide, which has tuberculostatic activity. Partially excreted unchanged (up to 15-20% of the dose) with urine and feces.

Indications:

Treatment of all forms of tuberculosis, including with the resistance of the pathogen to other anti-tuberculosis drugs (I series) or their intolerance.

Contraindications:Prothionamide should not be used with individual hypersensitivity to the components of the drug, during pregnancy and lactation, acute gastritis, peptic ulcer and duodenal ulcer, erosive ulcerative colitis, acute hepatitis, cirrhosis, chronic alcoholism.

Carefully:

Diabetes mellitus, severe hepatic insufficiency.

Dosing and Administration:

Take the drug inside after eating.

Adults appoint 0.25 g 3 times a day; with good tolerance - 0.5 g 2 times a day.

In patients older than 60 years and with a body weight of less than 50 kg the daily dose should not exceed 0.75 g (more often prescribed 0.25 g 2 times a day).

Children appoint at the rate of 10-20 mg / kg body weight per day.

Side effects:

From the gastrointestinal tract: loss of appetite, nausea, vomiting, diarrhea, dryness or hypersalivation, a "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 liver function, such as liver damage due to alcoholism or after surgery. These side effects are noted especially in combination therapy with isoniazid, rifampicin and pyrazinamide.

Skin Reactions are rare, in some cases described pellagrope-like reactions, respectively, with a combination of skin manifestations and disorders from the central nervous system: insomnia, agitation, depression, anxiety, rarely - dizziness, drowsiness, headache, asthenia, in single cases - paresthesia, peripheral neuropathy, optic neuritis.

From the cardiovascular system: tachycardia, weakness, orthostatic hypotension.

In some cases, allergic reactions and disorders of the bone marrow.

Sometimes violations are noted from the endocrine system. Along with the development hypoglycemia (a decrease in blood glucose less than 2.75 mmol / l) in patients with diabetes mellitus, described the development of gynecomastia (an increase in mammary glands in men).Rarely there is a violation of the menstrual cycle and impotence, as well as hypothyroidism.

Interaction:

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 a combination with isoniazid cases of polyneuropathy are described. Simultaneous reception of other antituberculosis 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.

In certain cases, when taking protionamide, it is necessary to reduce the dose of insulin or oral antidiabetic drugs.

Special instructions:

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.

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

In patients with diabetes, blood glucose levels need to be monitored at least once a month.

From the side of the skin and especially the mucous membranes, the 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.

Form release / dosage:

The tablets covered with a cover, 250 mg.

Packaging:

50 or 100 tablets are placed in a bag of low density polyethylene. One package, together with the instruction for use, is placed in a jar of high density polyethylene with a lid of the same material, the neck of the jar is sealed with a diaphragm made of aluminum, laminated with polyethylene on the inside, with an inscription "LUPIN". A label is attached to the jar.

Packing for hospitals

For 500 or 1000 tablets are placed in a package of low-density polyethylene.One package together with the instruction for use is placed in a jar of high-density polyethylene with a lid of the same material, the neck of the can is sealed with a membrane of aluminum laminated polyethylene on the inside, with an inscription "LUPIN". A label is attached to the jar.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014936 / 01

Date of registration:07.09.2007

The owner of the registration certificate:Lupine Co., Ltd.Lupine Co., Ltd. India

Manufacturer: & nbsp

LUPIN, Ltd. India

Representation: & nbspLUPIN LIMITEDLUPIN LIMITED

Information update date: & nbsp09.09.2015

Illustrated instructions

Instructions

Prothionamide (Protionamide )