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

Pharmacodynamics:Rifabutin is a semisynthetic antibiotic from the group of rifamycins. The mechanism of action is associated with inhibition of amino acid synthesis by inhibiting DNA-dependent RNA polymerase. Rifabutin is active against Mycobacterium tuberculosis (both sensitive and resistant to rifampicin strains). Besides, rifabutin is active against non-tuberculosis (atypical) mycobacteria, including Mycobacterium avium intracellular complex (MAC).

Pharmacokinetics:Rifabutin quickly absorbed and the maximum concentration of the drug in the blood plasma (Cmax) is reached about 2-4 hours after ingestion. The plasma level of the drug is maintained above the minimum inhibitory concentration (MIC) for M. tuberculosis up to 30 hours after administration. The pharmacokinetics of rifabutin is linear, with Cmax being determined in the range 0.4-0.7 μg / ml. Rifabutin is distributed in various organs, with the exception of the brain and spinal cord. In particular, the concentration of rifabutin in human lung tissue 24 hours after intake was 5-10 times higher than the concentration of the drug in the blood plasma. High intracellular concentration provides high efficiency of rifabutin against intracellularly positioned mycobacteria. Rifabutin and its metabolites are excreted in the urine. The half-life of rifabutin is approximately 35 to 40 hours.

Indications:

Rifabutin is indicated for the treatment of infections caused by M. tuberculosis, M.avium intracellulare complex (MAC), M.xenopi (including patients with immunodeficiency).

Rifabutin is recommended to be prescribed for the prevention of MAC infections in patients with immunodepression with a 200-μL or less C04-lymphocyte count. Rifabutin are used to treat both localized and disseminated infection caused by M. avium in patients with AIDS.

Rifabutin is shown both in cases of newly diagnosed pulmonary tuberculosis and in cases of multidrug-resistant chronic pulmonary tuberculosis caused by rifampicin-resistant strains of M. tuberculosis.

In accordance with the generally accepted principles of treatment of mycobacterial infections Rifabutin should always be given in combination with other anti-tuberculosis drugs that do not belong to the rifamycin family.

Contraindications:

Rifabutin is contraindicated in patients with hypersensitivity to rifabutin or other rifamycins (for example, rifampicin) in history, with liver failure, with severe renal failure.

Due to the lack of clinical experience in pregnant women, nursing mothers and children, Rifabutin should not be used in these groups of patients.

Dosing and Administration:

Rifabutin is prescribed to adults once a day, regardless of food intake. Rifabutin prescribe in combination with other drugs. With non-tuberculous mycobacterial infection: 450 to 600 mg (3 to 4 capsules) for up to 6 months

In chronic multidrug-resistant pulmonary tuberculosis: 300 - 450 mg (2 - 3 capsules) for up to 9 months.

With newly diagnosed pulmonary tuberculosis: 150 mg (1 capsule) for 6 months.

Prevention of MAC infection in patients with immunosuppression: 300 mg (2 capsules). In severe violations of kidney function (when creatinine clearance is less than 30 ml / min.), A dose reduction of 50% is required.

Side effects:

The most common side effects, located in frequency in descending order, are associated with:

- gastrointestinal system, such as nausea, vomiting, increased levels of hepatic enzymes, jaundice;

- blood and lymphatic system, such as leukopenia, thrombocytopenia and anemia;

- musculoskeletal system: arthralgia and myalgia.

There may also be fever, rashes and, rarely, other reactions of increased individual sensitivity, such as eosinophilia, bronchospasm, shock, reversible uveitis (whose severity can range from mild to severe).

Overdose:In case of overdosage, gastric lavage is used, symptomatic therapy is used and diuretics are prescribed.

Interaction:It was shown that Rifabutin induces enzymes of the cytochrome P450 OA family and thus can influence the pharmacokinetics of drugs metabolized by these enzymes. With simultaneous administration with Rifabutin, an increase in the dose of such drugs may be necessary. For the same reason, oral contraceptives may be ineffective in the treatment of Rifabutin, and the patient should use other contraceptive methods. Rifabutin does not affect the pharmacokinetics of didanosine, isoniazid and ethambutol. It is unlikely that drug interactions with theophylline, sulfonamides, pyrazinamide, fluconazole and zalcitabine, however fluconazole can increase the level of rifabutin in plasma. When rifabutin is administered with clarithromycin, rifabutin levels in the plasma may increase.

When rifabutin is combined with isoniazid, pyrazinamide and especially with protionamide, their antimicrobial activity is significantly increased.

Special instructions:

Rifabutin can give a reddish-orange color of urine, skin and secreted fluids.

Patients receiving Rifabutin, do not wear contact lenses. In cases of minor violations of the liver and kidneys, the dose can not be changed. During treatment it is recommended to periodically monitor the number of leukocytes, platelets and liver enzymes.

There are no reports on the impact on the ability to drive and use technical equipment.

When Rifabutin is administered in combination with clarithromycin, the daily dose of Rifabutin should be reduced to 300 mg. Because of the potential for uveitis, patients should be monitored when Rifabutin is administered in combination with clarithromycin (or other macrolides) and / or fluconazole (and similar compounds). With the development of uveitis, the patient should be consulted by an ophthalmologist, and if necessary, Rifabutin therapy should be temporarily discontinued.

Form release / dosage:Capsules of 150 mg.

Packaging:For 10 capsules in aluminum / PVC blister, for 13 or 10 blisters together with instructions for use in a cardboard box.

Storage conditions:In a dry, dark place at a temperature of no higher than 15 - 25 0 C. Keep out of reach of children.

Shelf life:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002486

Date of registration:10.02.2012/12.04.2016

The owner of the registration certificate:Lock-Beta Pharmaceuticals (I) Pvt.LtdLock-Beta Pharmaceuticals (I) Pvt.Ltd India

Manufacturer: & nbsp

LOK-BETA PHARMACEUTICALS (I), Pvt. Ltd. India

Representation: & nbspLock-Beta Pharmaceuticals (I) Pvt.LtdLock-Beta Pharmaceuticals (I) Pvt.Ltd

Information update date: & nbsp03.05.2016

Illustrated instructions

Instructions

Rifabutin (Rifabutin)