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

Active substance: rifabutin (in terms of 100% substance) - 150 mg; Auxiliary substances: sodium lauryl sulfate (dodecyl sulfate), povidone (low molecular weight polyvinylpyrrolidone (12600 ± 2700), silicon dioxide colloid (aerosil), magnesium stearate, talc, pregelatinized starch, titanium dioxide, azorubin (acidic red 2 C), quinoline yellow, diamond black, patented blue, ponso 4 R, gelatin.

Description:Capsules number 0 in red. The contents of the capsules are a non-uniform powder in the dispersion, from the dark purple to the violet-brown color with light inclusions.

Pharmacotherapeutic group:Anti-TB drug (antibiotic-ansamycin)

ATX: & nbsp

J.04.A.B Antibiotics

J.04.A.B.04 Rifabutin

Pharmacodynamics:Semisynthetic broad-spectrum antibiotic. Effective against intracellular and extracellularly distributed microorganisms. Selectively inhibits the DNA-dependent RNA polymerase of sensitive bacteria. Has a bactericidal effect. Highly active against Mycobacterium spp. (M.tuberculosis, M.avium intracellulare complex and other atypical mycobacteria). From 1/3 to 1/2 strains of M. tuberculosis resistant to rifampicin, are sensitive to rifabutin, indicating an incomplete cross-resistance between these antibiotics. It is also active against many Gram-positive microorganisms. With monotherapy, resistance develops rapidly.

Pharmacokinetics:Absorption from the gastrointestinal tract (GIT) - fast (fatty food reduces the speed, but not the degree of absorption). Bioavailability - 20%. The time to reach the maximum concentration is 2-4 hours. The connection with plasma proteins is 85%. The plasma content is maintained above the minimum inhibitory concentration for M. tuberculosis up to 30 hours after administration. With a single admission of 300, 450 and 600 mg, the pharmacokinetics is linear, with the maximum concentration being determined in the range of 0.4-0.7 μg / ml.Well penetrates into the cells of various organs and tissues. The ratio of intracellular to extracellular concentration is 9 for neutrophils and 15 for monocytes. It penetrates the blood-brain barrier (the concentration in the cerebrospinal fluid is about 50% of the concentration in the plasma). The highest concentration was in the lungs (24 hours after ingestion it was 5-10 times higher than the plasma one). The volume of distribution is 9 l / kg. Metabolized in the liver with the formation of inactive metabolites. It is excreted by the kidneys in the form of metabolites (53%) and with bile (30%). The half-life is 35-40 hours.

Indications:Tuberculosis of the lung is chronic multidrug-resistant, caused by rifampicin-resistant strains of M. tuberculosis (as part of combination therapy). Infections (both localized and disseminated forms) caused by M. tuberculosis, M. avium intracellulare complex, M.xenopi, etc. by atypical bacteria (including in patients with immunodeficiency with a number of SB4-lymphocytes 200 / μl and below ) - treatment (as part of complex therapy) and prevention (monotherapy).

Contraindications:Hypersensitivity (including rifampicin), pregnancy, lactation.

Carefully:Severe renal / hepatic insufficiency.

Dosing and Administration:Inside, 1 time per day, regardless of food intake. Prevention of infection in patients with immunosuppression - 300 mg / day. In combination with other drugs: with non-tuberculous mycobacterial infection -450-600 mg / day, up to 6 months from the time of receiving negative seeding. In chronic multidrug-resistant pulmonary tuberculosis - 300-450 mg / day, up to 6 months from the time of receiving negative seeding. With newly diagnosed pulmonary tuberculosis -150-300 mg / day, for 6 months. When the creatinine clearance is below 30 ml / min, the dose is reduced by 50%. With moderate violations of the liver and / or kidneys do not require dose adjustment.

Side effects:

On the part of the digestive system: nausea, vomiting, taste change (dysgeusia), diarrhea, abdominal pain, increased activity of "liver" transaminases, jaundice.

From the musculoskeletal system: arthralgia, myalgia. Laboratory indicators: leukopenia, thrombocytopenia, anemia.

Allergic reactions: fever, rash, rarely - eosinophilia, bronchospasm, anaphylactic shock, uveitis.

Interaction:It induces cytochrome CYP3A, accelerates the metabolism of drugs metabolized by this system (dosage increase is required).It is unlikely to develop clinically significant interactions with ethambutol, theophylline, sulfonamides, pyrazinamide, fluconazole, zalcitabine. Fluconazole and clarithromycin increase the concentration of the drug in plasma (with a simultaneous reception with clarithromycin, the daily dose is reduced to 300 mg). Reduces the concentration of zidovudine in plasma.

Special instructions:During the treatment period, it is necessary to periodically monitor the number of leukocytes, platelets in the peripheral blood, the activity of "liver" enzymes. The risk of uveitis increases with combination with clarithromycin or in high doses. With the development of uveitis, consultation of an ophthalmologist, temporary withdrawal of the drug is indicated. May impart a reddish-orange color to urine, skin and secreted fluids. Patients taking the drug should not wear contact lenses because of the possibility of their coloring in orange. The use of rifabutin as monotherapy for the prevention of M.avium disease in patients with tuberculosis can lead to the development of cross-resistance to rifabutin and rifampicin. It is advisable to combine with anti-tuberculosis drugs that do not belong to the rifamycin group.Oral contraceptives may be ineffective, other contraceptive methods should be used.

Form release / dosage:Capsules containing 150 mg of rifabutin.

Packaging:10 capsules per contour cell package. 1, 2, 3 contour packs with instructions for use in a pack of cardboard.

Storage conditions:List B. In a dry, the dark place at a temperature of not more than + 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005200/08

Date of registration:03.07.2008

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp03.05.2016

Illustrated instructions

Instructions

Rifabutin (Rifabutin)