Rifabutin

General characteristics. Structure:

Active ingredient: 150 mg of a rifabutin.

Semi-synthetic antibiotic of a broad spectrum of activity, active against mycobacteria.

Pharmacological properties:

Pharmacodynamics. Rifabutin - the semi-synthetic antibiotic of a broad spectrum of activity relating to group of ansamitsin. It is effective in the relation intracellularly and vnekletochno the located microorganisms. Selectively suppresses a DNA-dependent RNA polymerase of bacteria. Has bactericidal effect. From 5 to 15% of strains of Mycobacterium tuberculosis, resistant to rifampicin, are sensitive to a rifabutin that indicates incomplete cross resistance between these antibiotics. It is active also concerning not tubercular mycobacteria, including M. of avium complex (MAC) and many gram-positive microorganisms. At monotherapy stability quickly develops.

Pharmacokinetics. Rifabutin is quickly soaked up from digestive tract. Cmax reaches approximately in 2-4 hours after intake. Drug level in plasma is supported above the minimum inhibiting concentration (MIC) for M. by tuberculosis to 30 h from the moment of reception. Rifabutin well gets in cells of various bodies and fabrics, gets through GEB (concentration in SMZh makes about 50% of concentration in plasma). High intracellular concentration plays probably a key role in ensuring high performance of a rifabutin concerning M. of tuberculosis. It is metabolized in a liver with formation of inactive metabolites. It is removed by kidneys in the form of metabolites (53%) and with bile (30%). The elimination half-life makes 35-40 h.

Indications to use:

The pulmonary tuberculosis is the chronic polyresistant, caused rifampicin - resistant strains of Mycobacterium tuberculosis (as a part of a combination therapy). The infections (both localized, and the disseminated forms), the caused Mycobacterium tuberculosis, Mycobacterium avium (including located intracellularly), Mycobacterium xenopi, etc. atypical bacteria (including at patients with an immunodeficiency with quantity of CD4 lymphocytes 200/mkl below) - treatment (as a part of complex therapy) and prevention (monotherapy).

Route of administration and doses:

Inside, 1 time a day, irrespective of meal. At again diagnosed pulmonary tuberculosis - 150-300 mg/days, within 6 months. At a chronic polyresistant pulmonary tuberculosis - 300-450 mg/days, up to 6 months from the moment of receiving negative crops. In a combination with other drugs: at not tuberculosis mikobakterialny tuberculosis infection - 450-600 mg/days, up to 6 months from the moment of receiving negative crops. Prevention of an infection at patients with an immunosuppression - 300 mg/days. At KK lower than 30 ml/min. lower a dose by 50%. At moderate abnormal liver functions and/or kidneys are not required to dose adjustment.

Features of use:

It is necessary to be careful at purpose of a rifabutin to patients with a heavy renal/liver failure. During treatment it is necessary to control periodically number of leukocytes, thrombocytes in peripheral blood, activity of "hepatic" enzymes. Can give reddish-orange color to urine, skin and the cosecreted liquids. The patients accepting drug should not carry contact lenses because of a possibility of their coloring in orange color.

Side effects:

From a GIT, liver: nausea, vomiting, taste change, diarrhea, abdominal pain, increase in activity of "hepatic" transaminases, jaundice.

From system of a hemopoiesis: leukopenia, thrombocytopenia, anemia.

From skeletal and muscular system: arthralgia, mialgiya.

Allergic reactions: fever, rash, it is rare - an eosinophilia, a bronchospasm, an acute anaphylaxis, a uveitis.

Interaction with other medicines:

Accelerates metabolism of HP (induces enzymes of family of P4503A cytochrome and by that can influence pharmacokinetics) in a liver that increase in a dosage of such medicines can demand. Flukonazol and кларитромицин increase concentration of drug in plasma (at a concomitant use with klaritromitsiny the daily dose is reduced to 300 mg).

Contraindications:

Hypersensitivity (including to rifampicin). Due to the insufficient clinical experience of use for pregnant women, nursing mothers and children, рифабутин it should not be applied at these groups of patients.

Overdose:

Symptoms: strengthening of side effects. Treatment: gastric lavage, symptomatic therapy, purpose of diuretics.

Storage conditions:

At the room temperature in the place protected from light.

Issue conditions:

According to the recipe

Packaging:

Capsules of 150 mg, in a polymeric can No. 100.