Rifabutin

When ATH:
J04AB04

Characteristic.

TB drugs II series. Semisynthetic antibiotic from the group ansamycins. Spiropiperidilnoe derivative of rifamycin S, vysokolipofilnoe Connect. The red-purple powder. Soluble in methanol and chloroform, slightly soluble in ethyl alcohol, practically insoluble in water. Molecular weight 847,02.

Pharmacological action.
Broad-spectrum antibacterial, bactericide, TB.

Application.

Tuberculosis is a chronic pulmonary MDR, caused by rifampicin-resistant strains Mycobacterium tuberculosis (in a combination therapy). Infection (as localized, and disseminated forms), caused Mycobacterium tuberculosis, Mycobacterium avium (incl. located intracellularly), Mycobacterium xenopy and other atypical bacteria (incl. in immunocompromised patients with CD4 lymphocytes 200/µL and below) — treatment (in the complex therapy) and prevention.

Contraindications.

Hypersensitivity, incl. other ansamicinam (for example, rifampicin).

Restrictions apply.

Severe violations of the liver and/or kidney disease, Age to 14 years.

Pregnancy and breast-feeding.

When pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies in humans have not held).

Studies in rats and rabbits, receiving rifabutin in doses up to 200 mg / kg / day (in 40 times the recommended daily dose for a person) teratogenic properties of rifabutin is not revealed. Rats, dosed 40 mg / kg / day, There had been an increase in the incidence of skeletal malformations in fetuses, at a dose 200 mg/kg/day is to reduce their viability. In rabbits at a dose of 80 mg/kg/day was observed toxic effects on the body of a female and an increase in the frequency of malformations of fetuses skeleton.

Category actions result in FDA - B. (The study of reproduction in animals revealed no risk of adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not done.)

At the time of treatment should abandon breastfeeding (unknown, whether the rifabutin in breast milk).

Side effects.

From the nervous system and sensory organs: insomnia, headache, asthenia, uveitis, aglia (Propafenone).

Cardio-vascular system and blood (hematopoiesis, hemostasis): anemia, leukopenia, thrombocytopenia, eozinofilija, inhibition of hematopoiesis, gemoliz (rarely).

From the digestive tract: dyspepsia, change in taste (disgevziya), nausea, vomiting, diarrhea, gepatotoksichnostь (raising transaminaz liver, jaundice), hepatitis, abdominal pain.

Allergic reactions: skin rashes, itch, hives, dermatitis, bronchospasm, anaphylactic shock, drug fever.

Other: myalgia, arthralgia, chest pain, flu-like symptoms.

Cooperation.

Do effects of TB. Reduces the effect of oral contraceptives, Zidovudine, cyclosporine, oral protivodiabeticakih funds, antykoahulyantov, corticosteroids, cardiac glycosides, ʙarʙituratov, beta-blockers, chloramphenicol, diazepama, dapsone, dizopiramida, ketoconazole, phenytoin, mexiletine, aminofillina, teofillina, verapamil, hinidina and other medicines, metaboliziruthan with the participation of zitohroma P450 (a dose adjustment of these HP). Fluconazole, itraconazole, clarithromycin and rifabutin metabolism inhibit macrolides, increasing its concentration in the blood (together with klaritromitinom rifabutin dose reduced to 300 mg / day). Antiviral agents also increase its plasma concentration: If you are applying and rifabutin dose should be reduced to increase the dose of indinavir sulfate, When taking nelfinavir rifabutin dose reduced by half. You should avoid combination with ritonavir (risk of uveitis).

Overdose.

Symptoms: increased side effects.

Treatment: gastric lavage, Diuretic, simptomaticheskaya therapy.

Dosing and Administration.

Inside, regardless of the meal, 1 once a day, daily or every other day. Tuberculosis is grown on 150-300 mg/day (no more 600 mg / day) during 6 months from the date of receipt of the negative seeding. Prevention of MAC infections is 300 mg / day. Netuberkuleznaja mikobacterialnaya infection is on 450-600 mg/day until 6 months from the date of receipt of the negative seeding (in combination with other drugs). When creatinine clearance below 30 mL/min dose reduced by 50%.

Precautions.

During treatment should carefully monitor liver function and picture peripheral blood. To apply caution in elderly patients, given the possible age-related changes in liver function and related risk cumulation and hepatotoxicity. Risk of Uveitis is enhanced using high doses together with the admission or clarithromycin. When an Uveitis should temporarily stop receiving rifabutin and consult ophthalmologist.

Cautions.

During treatment the staining in a reddish-orange color of urine, Kala, skin, tear and sweat liquid, Saliva, Sputum. Can stain contact lenses. Patients, Unable to swallow the capsule whole, the contents can be mixed with applesauce.