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

Sheath (hard gelatin capsule, size "0"): iron oxide dye red 1,2799 mg, ferric oxide black oxide 0.1279 mg, titanium dioxide 0.2079 mg. Gelatine 79.4271 mg, water purified 13.9200 mg, sodium lauryl sulfate 0.0768 mg, propyl parahydroxybenzoate 0.1920 mg, methyl parahydroxybenzoate 0.7680 mg.

Description:Hard gelatin capsules, size "0", with a red-brown body and a red-brown lid. The contents of the capsules are a reddish-violet powder, or a powder pressed into a column ("slug") that decomposes on pressing, or a powder containing parts of a column that has not decayed.

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

ATX: & nbsp

J.04.A.B Antibiotics

J.04.A.B.04 Rifabutin

Pharmacodynamics:Rifabutin is a semisynthetic antibiotic from the group of rifamycins. The mechanism of action is associated with inhibition of the synthesis of amino acids by inhibiting the 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 intracellulare complex (MAC).

Pharmacokinetics:

Rifabutin is quickly absorbed and the maximum concentration of the drug in the blood plasma (Cmax) is reached approximately 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 35-40 hours.

Indications:

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

Rifabutin is recommended to be prescribed for the prevention of MAC infections in patients with immunosuppression with a number of SB4-lymphocytes 200 / μl and lower. 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 hepatic insufficiency.

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

Carefully:Rifabutin should be used with caution in cases of severe renal failure.

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: 450-600 mg / day (3-4 capsules) for up to 6 months.

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

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

Prevention of MAC infection in patients with immunosuppression: 300 mg / day (2 capsules).

Patients with severe renal impairment, with creatinine clearance below 30 ml / min, showed a 50% reduction in Rifabutin dose. Minor and moderate renal dysfunction does not require dose adjustment.

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, when treating rifabutin, oral contraceptives may be ineffective, and the patient should use other contraceptive methods. Rifabutin does not affect the pharmacokinetics of didanosine (DDI), isoniazid and ethambutol. It is unlikely that drug interactions will occur with theophylline, sulfonamides, pyrazinamide, fluconazole, and zalcitabine (DDC), 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.

Effect on the ability to drive transp. cf. and fur:

The drug does not affect driving and other potentially hazardous activities requiring increased concentration and speed

psychomotor reactions.

Form release / dosage:

Capsules 150 mg.

Packaging:

For 10 capsules in a blister of PVC / aluminum foil. For 3 blisters with instructions for use in a cardboard box.

For 30, 100 or 500 capsules in a package of low-density polyethylene. One package, together with instructions for use in a container of high-density polyethylene (with the control of the first opening).

Packing for hospitals. 500 capsules per package of low density polyethylene, followed by a high density polyethylene container, together with instructions for use (with the control of the first autopsy).

When packaging and packaging at the enterprise OAO PHARMASINTEZ (Russia) packs 30 capsules per package of low-density polyethylene. One package, together with instructions for use in a container of high-density polyethylene (with the control of the first opening).

At packing at the enterprise OAO "FARMASINTEZ" (Russia) packs 3 blisters with instructions for use in a cardboard box.

At packing at the enterprise CJSC "MAKIZ-PHARMA" (Russia) packs 3 blisters with instructions for use in a cardboard box.

At packing at the enterprise JSC "SKOPINSKIY PHARMACEUTICAL FACTORY" (Russia) packs 3 blisters with instructions for use in a cardboard box.

Storage conditions:Store in a dry, dark 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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014112 / 01

Date of registration:03.04.2008

The owner of the registration certificate:Lupine Co., Ltd.Lupine Co., Ltd. India

Manufacturer: & nbsp

LUPIN, Ltd. India

Representation: & nbspLUPIN LIMITEDLUPIN LIMITED

Information update date: & nbsp04.05.2016

Illustrated instructions

Instructions

Rifabutin (Rifabutin)