Rifampicin

General characteristics. Structure:

Active ingredient: 150 mg of rifampicin.

Rifampicin — a semi-synthetic antibiotic of a wide range of antimicrobic action from group of Rifamycinums (ansamitsin).

Pharmacological properties:

Pharmacodynamics. Works bakteritsidno. Breaks synthesis of RNA in a bacterial cell, inhibiting a DNA-dependent RNA polymerase. It is highly active concerning Mycobacterium tuberculosis, is an antituberculous remedy of the I row.

Streptococcus spp is active concerning gram-positive bacteria (Staphylococcus spp, including polyresistant strains)., Bacillus anthracis, Clostridium spp.) and some gram-negative bacteria (Neisseria meningitidis, N.gonorrhoeae, Haemophilus influenzae, Brucella spp., Legionella pneumophila). Rickettsia prowazekii, Mycobacterium leprae is active concerning Chlamydia trachomatis. Does not affect mushrooms. Rifampicin has virulotsidny effect on a rhabdovirus, suppresses development of rabichesky encephalitis.

Rifampicin resistance develops quickly. Cross stability with other antibacterial drugs (except for other Rifamycinums) is not revealed.

Pharmacokinetics. Rifampicin is quickly and fully soaked up in digestive tract. Bioavailability reaches 90 — 95%. The maximum concentration of rifampicin in a blood plasma is reached in 2 — 2,5 hours after intake. Rifampicin is found in therapeutic concentration in pleural exudate, a phlegm, contents of cavities, a bone tissue; the greatest concentration is created in a liver and kidneys.

Linkng with proteins of a blood plasma makes 80 — 90%. Rifampicin gets through a blood-brain barrier, a placenta, it is found in breast milk. It Biotransformirutsya in a liver. An elimination half-life — 2 — 5 hours. At the therapeutic level concentration of drug is maintained within 8 — 12 hours after reception, concerning highly sensitive activators — during 24 h. It is brought out of an organism with bile, a stake and urine.

Indications to use:

Rifampicin is applied at tuberculosis (including at tubercular meningitis), as a part of a combination therapy; at the infectious and inflammatory diseases caused by activators, sensitive to drug (including at osteomyelitis, pneumonia, pyelonephritis, a leprosy, gonorrhea, otitis, cholecystitis, etc.), and also at a meningococcal carriage.

Due to the bystry development of antibiotic resistance in the course of treatment, use of rifampicin at diseases of not tubercular etiology is limited to the cases which are not giving in to therapy by other antibiotics.

Route of administration and doses:

Use drug inside on an empty stomach (for 1/2 — 1 hour to food).

At treatment of tuberculosis the average daily dose for adults makes 0,45 g, drug is accepted 1 time a day. At patients (especially in the period of an aggravation) with body weight more than 50 kg the daily dose can be increased to 0,6 g. The average daily dose of rifampicin for children over 3 years makes 10 mg/kg of body weight (but no more than 0,45 g a day), accept an antibiotic of 1 times a day. At bad portability of rifampicin the daily dose can be divided into 2 receptions.

At a leprosy the daily dose of rifampicin (0,3 — 0,45 g) is entered into 1 reception, at bad portability — into 2 receptions. Treatment duration — 3 — 6 months, courses repeat with an interval of 1 month.

Against the background of the combined antileprotic therapy appoint drug in a daily dose of 0,45 g in 2 — 3 receptions within 2 — 3 weeks with an interval of 2 — 3 months during 1 year — 2 years or in the same dose 2 — 3 times in 1 week within 6 months. Treatment is carried out in a complex with immunoexcitants.

At infections of not tubercular nature the adult appoint rifampicin on 0,45 — 0,9 g a day, to children — on 8 — 10 mg/kg of body weight a day. Accept drug in 2 — 3 receptions. Duration of treatment is defined individually depending on efficiency and portability of drug and can make 7 — 10 days.

At acute gonorrhea appoint inside in a dose 0,9 g a day once or within 2 days.

For prevention of rage by the adult appoint inside 0,45 — 0,6 g a day; at heavy damages (a sting in a face, the head, hands) — on 0,9 g a day. To children up to 12 years appoint in a dose 8 — 10 mg/kg of body weight a day. The daily dose is divided into 2 — 3 receptions. Drug use duration — 5 — 7 days. Treatment is carried out along with active immunization.

Features of use:

Monotherapy of tuberculosis rifampicin often is followed by development of resistance of the activator to an antibiotic therefore it should be combined with other antituberculous remedies. At treatment of not tuberculosis infections perhaps bystry development of resistance of microorganisms; this process can be prevented if to combine rifampicin with other chemotherapeutic means.

Drug is not shown for discontinuous therapy.

Administration of drug can be followed by urine coloring, a calla, saliva, sweat, the lacrimal liquid, contact lenses in red color.

Side effects:

At purpose of drug are possible: nausea, vomiting, diarrhea, a loss of appetite, increase in level of hepatic transaminases, bilirubin in a blood plasma, pseudomembranous colitis, cholestatic jaundice, hepatitis, a headache, arthralgias, an ataxy, a canalicular necrosis, intersticial nephrite, an acute renal failure, vision disorders, a leukopenia, it is rare — thrombocytopenia, a Werlhof's disease, an eosinophilia, hemolitic anemia, disturbances of a menstrual cycle, a small tortoiseshell, and a rifampicin combination to an isoniazid.

Interaction with other medicines:

Rifampicin — the strong inductor of R-450 cytochrome, can cause potentially dangerous medicinal interactions.

Rifampicin accelerates metabolism (concentration in a blood plasma decreases and respectively action decreases) theophylline, thyroxine, corticosteroids, carbamazepine, Phenytoinum, peroral anticoagulants, peroral hypoglycemic drugs, dapsone, some tricyclic antidepressants, chloramphenicol, a flukonazol, ketokonazol, terbinafin, haloperidol, diazepam, a bisoprolol, propranolol, diltiazem, nifedipine, verapamil, cardiac glycosides, quinidine, Disopyramidum, propafenon, cyclosporine.

It is necessary to avoid combined use with HIV protease inhibitors (индинавир, нельфинавир).

Rifampicin accelerates metabolism of estrogen and gestagen (the contraceptive effect of oral contraceptives decreases). Ketokonazol can reduce concentration of rifampicin in a blood plasma.

Contraindications:

Hypersensitivity to rifampicin or other rifampicin, jaundice (including mechanical), recently postponed (less than 1 year) infectious hepatitis, diseases of a liver and kidneys, pregnancy and a lactation (the refusal of breastfeeding is obligatory).

At newborn and premature children rifampicin is applied only in urgent cases, with extra care.

With care apply at children, the exhausted patients, at the patients abusing alcohol at a porphyria.

At development of thrombocytopenia, a purpura, hemolitic anemia, an acute anaphylaxis, a renal failure and other serious undesirable reactions treatment by rifampicin is stopped.

Treatment by rifampicin has to be carried out under careful medical observation. Treatment by drug should be begun after the research of function of a liver (determination of level of bilirubin and aminotransferases in blood, a thymol turbidity test), and in the course of treatment to carry out it monthly. At the accruing phenomena of an abnormal liver function use of drug should be stopped. At prolonged use of drug it is necessary to control a blood pattern in connection with a possibility of development of a leukopenia.

Overdose:

Symptoms: nausea, vomiting, diarrhea, drowsiness, increase in a liver, jaundice, increase in level of bilirubin, hepatic transaminases in a blood plasma; brown-red or orange coloring of skin, urine, saliva, sweat, tears and excrements is proportional to the accepted drug dose.

Treatment: termination of administration of drug. Gastric lavage. Symptomatic therapy (there is no specific antidote). Maintenance of the vital functions.

Issue conditions:

According to the recipe

Packaging:

Capsules of 150 mg in a blister strip packaging No. 10х2.