Verbutin - instructions for use, doses, side effects, contraindications

Excipients: magnesium stearate 1 mg, talc 20 mg, microcrystalline cellulose 80 mg, empty gelatin capsule, size "0": water, gelatin, iron dye red oxide, iron oxide black oxide, titanium dioxide, povidone, methyl parahydroxybenzoate, propyl parahydroxybenzoate.

Description:

Capsules, size "O" with a red-brown body and a red-brown lid.

The contents of the capsules are a reddish-violet powder with white impregnations.

Pharmacotherapeutic group:Antibiotic, Ansamycin

ATX: & nbsp

J.04.A.B Antibiotics

J.04.A.B.04 Rifabutin

Pharmacodynamics:

Semisynthetic broad-spectrum antibiotic. The mechanism of action is a selective inhibitor of DNA-dependent RNA polymerase; bactericidin.It is active against extracellular and intracellular microorganisms. Highly active against Mycobacterium spp. (M.tuberculosis, M.avium intracellular complex and other atypical mycobacteria); many gram-positive and gram-negative bacteria. Rifabutin is active against 25-40% of M. tuberculosis, atypical mycobacteria resistant to rifampicin and other antibacterial drugs, indicating an incomplete cross-resistance between these drugs. The rate of development of resistance to rifabutin is lower than to rifampicin.

It is also active against many conditionally pathogenic microorganisms: Staphylococcus aureus is coagulase-negative, including methicillin-resistant; most types of streptococci (Streptococcus pneumoniae, including penicillin-resistant, S.viridans, S.pyogenes, moderately active against Enterococcus spp.). Gram-positive anaerobes are also sensitive to rifabutin: Bacillus anthracis, Clostridium spp., Including C. difficile; some pathogens of dangerous infectious diseases: Francisella tularensis, Brucella spp.

It is used in combination with other antibacterial drugs in monotherapy - resistance develops rapidly. The activity of rifabutin in vivo in experimental tuberculosis is 10 times higher than that of rifampicin, which corresponds to the data in vitro.

Pharmacokinetics:Ingestion rifabutin quickly absorbed, the maximum concentration in the blood (Cmax) is reached after 2-4 hours, and the concentration in the blood serum, depending on the dose taken (300 mg and 900 mg) is 0.4 and 0.9 mg / l, respectively. After taking a single dose, the bioavailability was 20%. The area under the rifabutin concentration curve depends on the intake and is significantly higher on the 1st day of treatment than on the 28th day, due to the activation of the metabolism. Taking the drug simultaneously with food reduces the rate of absorption, but its degree remains unchanged. The apparent volume of distribution is about 8-9 l / kg, the connection with blood proteins ranges from 70 to 94%. The concentration of rifabutin in the tissues (after 5-12 hours after administration in a dose of 150-300 mg) is 8.5 times higher than in serum. It is well distributed in organs and tissues, penetrates into cells. The ratio of the intracellular concentration of the antibiotic to the extracellular for polynuclears is 9, for monocytes it is 15. The half-life of rifabutin (T1 / 2), depending on the characteristics of the patient's organism and the method of conducting the study, ranges from 32 to 67 hours. After a single intake of rifabutin, the total amount of the withdrawn drug (rifabutin + inactive metabolites) in urine is 44% at 72 hours and 53% at 96 hours, in faeces at the same time intervals of 24 and 49%.

Indications:As part of combination therapy with other antibacterial drugs. Tuberculosis of the lung is chronic multidrug-resistant, caused by rifamycin-resistant strains of M.tuberculosis, mycobacteriosis (localized and disseminated forms) caused by M.avium intracellular complex (MAC) and other atypical bacteria. Rifabutin It is also recommended for the treatment of MAS infections in patients with immunodepression with a CD-4-lymphocyte count of 200 μl or less.

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 moment of receiving negative seeding.

With newly diagnosed pulmonary tuberculosis - 5 mg / kg body weight (no more than 2 capsules per 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:

Nausea, vomiting, change in taste (dysgeusia), diarrhea, abdominal pain, increased activity of "liver" enzymes, 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:

It induces cytochrome P450, accelerates the metabolism of drugs metabolized by this system (an increase in dosage is required). It is unlikely the development of clinically significant interactions with ethambutol, theophylline, sulfonamides, 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). Rifabutin reduces the concentration of zidovudine in plasma.

The combined use of rifabutin with pyrazinamide, protionamide and isoniazid is indicated due to pronounced synergism at the microbiological level. It is not recommended simultaneous administration of fluoroquinolones.

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. As the prevention of anemia, folic acid is effective.

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.

To prevent the development of anemia, it is advisable to take folic acid. 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 can be ineffective, you should use other contraceptives.

Form release / dosage:Capsules of 150 mg.

Packaging:For 10 capsules in a blister of Al / Pv., 3 blisters are placed in a cardboard box with instructions for use.

Storage conditions:In a dry, the dark place at a temperature of no higher than 25 C. Keep out of reach of children.

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-005931/08

Date of registration:28.07.2008 / 12.01.2016

Expiration Date:Unlimited

The owner of the registration certificate:Vertex ExportsVertex Exports India

Manufacturer: & nbsp

SWISS PHARMA, PVT. Ltd. India

Representation: & nbspVirend International, Inc.Virend International, Inc.Russia

Information update date: & nbsp29.01.2017

Illustrated instructions

Instructions

Verbutin (Verbutin)