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

Hard gelatin capsules number 0. The capsule body and capsule are bright red. The contents of the capsules are red-violet powder, with insignificant white impregnations.

It is allowed to compact the contents of the capsule according to the shape of the capsule, disintegrating upon pressing.

Pharmacotherapeutic group: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 bacteria. Has a bactericidal effect. Highly active against Mycobacterium spp. (Mycobacterium tuberculosis, Mycobacterium avium, including those located intracellularly) and other atypical mycobacteria. About 1/3 to 1/2 strains of Risfampycin-resistant Mycobacterium tuberculosis 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 - fast (fatty food reduces the speed, but not the degree of absorption). Bioavailability - 20%. TSam - 2-4 hours. The connection with plasma proteins is 85%. The concentration in the plasma is maintained above the minimum maintenance concentration for Mycobacterium tuberculosis until 30 hours from the time of admission. With a single admission of 300, 450 and 600 mg, the pharmacokinetics is linear in nature, while the C max value is determined in the range 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 hemato-encephalic barrier (the concentration in the cerebrospinal fluid is about 50% of the concentration in the plasma). The highest concentration is in the lungs (24 hours after ingestion it is 5-10 times higher than in the blood plasma). The volume of distribution is 9 l / kg.

Metabolized in the liver with the formation of inactive metabolites. It is the inducer of the isoenzymes CYP3A4, CYP3A5 and CYP3A7 in the liver. It is excreted by the kidneys in the form of metabolites (53%) and with bile (30%). T1 / 2 - 35-40 hours.

Indications:Tuberculosis of the lung is chronic multidrug-resistant, caused by rifampicin-resistant strains of Mycobacterium tuberculosis (as part of combination therapy). Infections (both localized and disseminated forms) caused by Mycobacterium tuberculosis, Mycobacterium avium (including those located intracellularly), Mycobacterium xenopi and other atypical bacteria (including patients with immunodeficiency with the number of C04 lymphocytes 200 / mkl and below) - treatment (as part of complex therapy) and prevention (monotherapy).

Contraindications:Hypersensitivity to rifabutin or other rifamycins in the anamnesis. Due to the lack of clinical experience, they are not prescribed during pregnancy and lactation, and also for children.

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 moment 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 kidney function, no dose adjustment is required.

Side effects:

Nausea, vomiting, taste change (dysgeusia), diarrhea, abdominal pain, increased activity of "liver" transaminases, jaundice. Leukopenia, thrombocytopenia, anemia. Arthralgia, myalgia.

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

Overdose:

Symptoms: increased side effects.

Treatment: gastric lavage, symptomatic therapy, the appointment of diuretics.

Interaction:Accelerates the metabolism of the drug in the liver (requires an increase in dosage).Reduces the concentration of zidovudine in plasma.

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).

Special instructions:

Heart failure must first be compensated. In the treatment it is necessary to monitor the functions of the cardiovascular system, the respiratory system, the content of glucose and electrolytes in the blood, the volume of circulating blood and the amount of excreted urine. In newborns and infants, severe hemodynamic effects were noted. Can prolong the P-Q interval at a plasma concentration above 30 ng / ml. It is not recommended to stop treatment suddenly.

During the treatment period, it is necessary to periodically monitor the number of leukocytes, platelets in 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 Mycobacterium avium disease in tuberculosis patients 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 can be ineffective, you should use other contraceptives.

Form release / dosage:

Capsules of 150 mg.

Packaging:

For 5, 10 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 10, 20, 30, 40, 50, 60 or 100 capsules in a polymer container for medicines. One container or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

For 5, 10 or 20 containers or 20, 40, 60, 80 and 100 contour mesh packages together with the corresponding number of instructions for use are placed in a cardboard box (forhospitals).

Storage conditions:List B. Store in a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003091/08

Date of registration:24.04.2008

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp03.05.2016

Illustrated instructions

Instructions

Rifabutin (Rifabutin)