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

active substance: rifampicin (in terms of 100% substance) - 150 mg; Excipients: magnesium hydroxycarbonate - 15 mg, calcium stearate - 3 mg, lactose monohydrate - up to the mass of the contents of the capsule 300 mg.

Composition of hard gelatin capsule: gelatin - 61.359, glycerol (glycerol) 0.095 mg, methylparahydroxybenzoate 0.268 mg, propyl parahydroxybenzoate 0.067 mg, purified water 10.585 mg, titanium dioxide 0.429 mg, sodium lauryl sulfate 0.044 mg, brilliant blue E-133 0.001 mg quinoline yellow E-104 - 0.071 mg, red charming E-129-0.081 mg.

Description:

Capsules from orange-red to dark red No. 1. Contents of capsules - powder from light red to brownish-red with white impregnations.

Pharmacotherapeutic group:Antibiotic-rifamycin.

ATX: & nbsp

J.04.A.B Antibiotics

J.04.A.B.02 Rifampicin

Pharmacodynamics:

Semisynthetic broad-spectrum antibiotic, first-line anti-tuberculosis drug. At low concentrations, it has a bactericidal effect on Mycobacterium tuberculosis, Brucella spp., Chlamydia trachomatis, Legionella pneumophila, Rickettsia typhi, Mycobacterium leprae; in high concentrations - on some gram-negative microorganisms.

Characterized by high activity against Staphylococcus spp. (including penicillinase-forming and many staffs of methicillin-resistant), Streptococcus spp., Clostridium spp., Bacillus anthracis; Gram-negative cocci: Neisseria meningitidis, Neisseria gonorrhoeae.Gram-positive bacteria acts in high concentrations. It is active with respect to intracellular and extracellularly located microorganisms. Selectively inhibits the DNA-dependent RNA polymerase of sensitive microorganisms. When the drug is monotherapy, the selection of rifampicin-resistant bacteria is observed relatively quickly. Cross-resistance with other antibiotics (with the exception of the other rifamycins) does not develop.

Pharmacokinetics:

Absorption - fast, eating reduces the absorption of the drug. When administered on an empty stomach 600 mg, the maximum concentration in the blood-10 μg / ml, the time to reach the maximum concentration in the blood - 2-3 hours. Communication with plasma proteins - 84-91%.

Quickly distributed to organs and tissues (the highest concentration in the liver and kidneys), penetrates into the bone tissue, the concentration in the saliva - 20% of the plasma. The apparent volume of distribution is 1.6 l / kg in adults and 1.1 l / kg in children. Through the blood-brain barrier penetrates only in case of inflammation of the meninges. Penetrates through the placenta (concentration in the plasma of the fetus - 33% of the concentration in the mother's plasma) and excreted in breast milk (breastfed babies receive no more than 1% of the therapeutic dose of rifampicin).

Metabolised in the liver with the formation of pharmacologically active metabolite - 25-O-deacetyltrifampicin. It is an autoinducer - it accelerates its metabolism in the liver, as a result of which the creatinine clearance is 6 l / h after the first dose, increases to 9 l / h after repeated administration. When ingestion is also possible, induction and enzymes of the intestinal wall. The half-life of the drug (T1 / 2) after ingestion is 300 mg - 2.5 hours, 600 mg -3-4 hours, 900 mg - 5 hours. After several days of repeated administration, the bioavailability decreases, and T1 / 2 after repeated administration of 600 mg is shortened to 1-2 hours. It is excreted mainly with bile, 80% - in the form of a metabolite; kidneys - 20%.

After taking 150-900 mg of the drug, the amount of rifampicin excreted by the kidneys in unchanged form depends on the value of the dose taken and is 4-20%.

In patients with impaired renal excretory function, T1 / 2 is prolonged only when its doses exceed 600 mg. It is excreted in peritoneal dialysis and hemodialysis. In patients with impaired hepatic function, an increase in rifampicin plasma concentration and an elongation of T1 / 2 were noted.

Indications:

Tuberculosis of all forms and localizations in combination therapy.

Leprosy (in combination with dapsone) - multibacterial types of the disease.

Infectious diseases caused by sensitive microorganisms (in cases of resistance to other antibiotics and in combination antimicrobial therapy, after excluding the diagnosis of tuberculosis and leprosy).

Brucellosis - as part of combination therapy with the antibiotic group of tetracyclines (doxycycline).

Meningococcal meningitis (prophylaxis in persons who were in close contact with meningococcal meningitis who fell ill, in Neisseria meningitidis bacilli carriers).

Contraindications:Hypersensitivity, jaundice, recently transferred (less than 1 year) infectious hepatitis, lactation period, chronic renal failure, pulmonary heart failure II-III st, children under the age of 3 years.

Carefully:Pregnancy (only for life indications).

Dosing and Administration:

Inside, on an empty stomach, 30 minutes before meals.

For the treatment of tuberculosis combined with at least one antituberculous agent (isoniazid, pyrazinamide, ethambutol, streptomycin). Adults with a body weight of less than 50 kg - 450 mg / day; 50 kg and more - 600 mg / day.

The average daily dose of rifampicin for children older than 3 years is 10 mg / kg

body weight (but not more than 450 mg per day), take an antibiotic once a day. With poor rifampicin tolerance, the daily dose can be divided into 2 doses.

With tuberculous meningitis, disseminated tuberculosis, tuberculosis of the spine with neurological manifestations, when tuberculosis is combined with HIV infection the total duration of treatment is 9 months, the drug is used daily, the first 2 months in combination with isoniazid, pyrazinamide and ethambutol (or streptomycin), the next 7 months - in conjunction with isoniazid. In the case of pulmonary tuberculosis and the detection of mycobacteria in sputum, the following 3 regimens are used (all with a duration of 6 months):

- The first 2 months are as above; 4 months - daily, in combination with isoniazid.

- The first 2 months are as above; 4 months - in combination with isoniazid, 2-3 times during each week.

- Throughout the course - the reception in combination with isoniazid, pyrazinamide and ethambutol (or streptomycin) 3 times during each week. In cases where anti-TB drugs are used 2-3 times a week (as well as in case of exacerbation of the disease or inefficiency of therapy), they should be taken under the supervision of medical personnel.

For the treatment of multibacterial leprosy types (lepromatous, borderline, lepromatous and borderline) adults - 600 mg once a month in combination with dapsone (100 mg once a day); children older than 3 years - 10 mg / kg once a month in combination with dapsone (1-2 mg / kg / day). The minimum duration of treatment is 2 years.

For the treatment of multibacterial leprosy types (tuberculoid and border tuberculoid) adults - 600 mg once a month, in combination with dapsone - 100 mg (1-2 mg / kg) once a day; children older than 3 years - 10 mg / kg once a month, in combination with dapsone - 1-2 mg / kg / day. Duration of treatment - 6 months.

For the treatment of infectious diseases, caused by sensitive microorganisms, is prescribed in combination with other antimicrobial agents. The daily intake for adults is 0.6-1.2 g; for children older than 3 years - 10-20 mg / kg (not more than 450 mg / day). Multiplicity of admission - 2 times a day.

For the treatment of brucellosis - 900 mg / day once, in the morning on an empty stomach, in combination with doxycycline; the average duration of treatment is 45 days.

For the prevention of meningococcal meningitis - 2 times a day every 12 hours for 2 days. Single doses for adults - 600 mg; for children older than 3 years - 10 mg / kg.

Patients with impaired renal excretory function and preserved liver function need to adjust the dose only when it exceeds 600 mg / day.

Side effects:

On the part of the digestive system: nausea, vomiting, diarrhea, decreased appetite, erosive gastritis, pseudomembranous colitis; increased activity of "hepatic" transaminases in the blood serum, hyperbilirubinemia, hepatitis. Allergic reactions: urticaria, eosinophilia, angioedema, bronchospasm, arthralgia, fever.

From the nervous system: headache, reduced visual acuity, ataxia, disorientation.

From the urinary system: nephronecrosis, interstitial nephritis. Other: leukopenia, dysmenorrhea, induction of porphyria, myasthenia gravis, hyperuricemia, exacerbation of gout.

With an irregular reception or with the resumption of treatment after the break, an influenza-like syndrome (fever, chills, headache, dizziness, myalgia), skin reactions, hemolytic anemia, thrombocytopenic purpura, acute renal failure are possible.

Overdose:

Symptoms: pulmonary edema, confusion, convulsions.

Treatment: gastric lavage, the use of activated charcoal; symptomatic therapy, forced diuresis.

Interaction:Antacids, opiates, cholinesterase inhibitors and ketoconazole reduce (in the case of simultaneous ingestion) bioavailability of rifampicin. Isoniazid and / or pyrazinamide increase the frequency and severity of liver function disorders to a greater extent than with the appointment of a single rifampicin, in patients with a previous liver disease. Preparations PASK and antacids, should be prescribed no earlier than 4 hours after taking the drug, since it is possible to violate the absorption. Reduces the activity of oral anticoagulants, oral hypoglycemic drugs, hormonal contraceptives, cardiac glycosides, antiarrhythmics (disopyramide, pirmenol, quinidine, mexiletine, tokainid), glucocorticosteroids, dapsone, hydantoins (phenytoin), hexobarbital, nortriptyline, benzodiazepines, sex hormones, theophylline, chloramphenicol, ketoconazole, itraconazole, cyclosporine, azathioprine, beta-adrenoblockers, "slow" calcium channel blockers, enalapril, cimetidine (rifampicin causes the induction of the enzyme system of the liver of the cytochrome P-450 system, accelerating the metabolism of drugs).

Special instructions:During treatment the skin, mucus, sweat, feces, lacrimal fluid, urine becomes orange-red color.Can persistently stain soft contact lenses. To prevent the development of resistance of microorganisms, it is necessary to use in combination with other antimicrobial agents. Щ In case of development of the flu-like syndrome, uncomplicated thrombocytopenia, hemolytic anemia, bronchospasm, dyspnea, shock and renal insufficiency, patients receiving the medication according to the intermittent scheme should consider the possibility of switching to a daily reception. In these cases, the dose is increased slowly on the first day prescribe 75-150 mg, and the desired therapeutic dose is achieved in 3-4 days. In the event that the above serious complications are noted, rifampicin cancel. It is necessary to monitor kidney function; an additional prescription of glucocorticosteroids is possible. Therapy during pregnancy (especially in the first trimester) is possible only for life indications. At appointment in the last weeks of pregnancy, postpartum bleeding in the mother and bleeding in

newborn. In this case, prescribe vitamin K.

Women of childbearing age during treatment should use reliable methods of contraception (oral hormonal contraceptives and additional non-hormonal methods of contraception).

In the case of prophylactic use, meningococcal bacilli carriers require strict monitoring of patients in order to timely identify the symptoms of the disease in the event of rifampicin resistance. With prolonged use, a systematic control of the peripheral blood picture and liver function is shown.

During the treatment period, it is impossible to apply microbiological methods for determining the concentration of folic acid and vitamin B12 in the blood serum.

Form release / dosage:

Capsules 150 mg.

Packaging:

10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil. For 1, 2 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Packaging for hospitals: 150 contour packs with the appropriate number of instructions for use are placed in a cardboard box.

Storage conditions: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:

2 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N016246 / 01

Date of registration:25.02.2010/04.03.2015

The owner of the registration certificate:BELMEDPREPARATY, RUP BELMEDPREPARATY, RUP Republic of Belarus

Manufacturer: & nbsp

BELMEDPREPARATY, RUP Republic of Belarus

Information update date: & nbsp15.05.2016

Illustrated instructions

Instructions

Rifampicin (Rifampicin)