Active substanceRifampicinRifampicin
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  • Dosage form: & nbsplyophilizate for solution for infusion
    Composition:
    1 bottle with G26.4 mg of the drug contains:

    Active substance: rifampicin sodium 616.4 mg (corresponding to 600 mg rifampicin)

    Excipients: sodium ascorbate 10.0 mg.
    Description:red crystalline powder.
    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 antracis; Gram-negative cocci: Neisseria meningitidis, Neisseria gonorrhoeae. Ha gram-positive bacteria act 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 otherantibiotics (with the exception of the other rifamycins) does not develop.
    Pharmacokinetics:
    At intravenous drip introduction the maximum concentration of rifampicin is observed by the end of infusion (infusion). At the therapeutic level, the concentration of the drug with intravenous administration is maintained for 8-12 hours, for highly sensitive pathogens - within 24 hours. Rifampicin penetrates well into tissues and body fluids and is found in therapeutic concentrations in pleural exudate (accumulating between the membranes surrounding the lungs, a protein-rich fluid), sputum, cavern contents (cavities in the lungs resulting from necrosis of tissue), bone tissue. The greatest concentration of the drug is created in the tissues of the liver and kidneys.

    Through the blood-brain barrier penetrates only in the 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 the drug). Metabolised in the liver with the formation of pharmacologically active metabolite - 25-O-deacetyltrifampicin. It is excreted mainly with bile, 80% - in the form of a metabolite; kidneys - 20%.

    In patients with impaired renal excretory function, T1 / 2 is prolonged only when its dose exceeds 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.

    Resistance to rifampicin develops rapidly. Cross-resistance with other antibiotics is not observed (with the exception of rifamycin).
    Indications:Tuberculosis of all forms and localizations in combination therapy.

    Leprosy (in combination with dapsone and clofazimine multibacillary types of the disease).

    Infectious diseases caused by rifampicin-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:
    - increased sensitivity to rifampicin and other rifamycins or to any of the components of the drug;

    - jaundice, recently transferred (less than a year) infectious hepatitis;

    - pregnancy (only for life indications);

    - the period of breastfeeding;

    - chronic renal failure;

    - pulmonary heart failure of II - III degree;

    - thoracic age up to 2 months.
    Carefully:
    They are used with caution in patients who abuse alcohol, with evidence of liver disease in history, in newborns, premature infants (due to the age immaturity of liver enzyme systems) and in depleted patients, with the resumption of rifampicin after a break.
    Pregnancy and lactation:
    It is not recommended to prescribe the drug to pregnant women, except when the doctor, evaluating the ratio of benefit and risk to the pregnant and fetus, decides that the use of the drug is necessary.

    During the treatment, the drug should stop breastfeeding.
    Dosing and Administration:

    Parenterally, intravenously (IV), drip. In / in - with acute and progressive forms of destructive pulmonary tuberculosis,severe purulent-septic processes, when it is necessary to quickly create high concentrations of the drug in the blood and in the focus of the infection, in cases when taking the drug inside is difficult or badly tolerated by patients.

    Preparation of solution for IV infusion: dilute lyophilizate, adding 10 ml of water for injection into the vial with the drug. Shake the vial to ensure complete dissolution of the contents of the vial. Then mix the resulting solution with 500 ml of 5% dextrose solution, 5% fructose solution or 0.9% sodium chloride solution. If a smaller dose of rifampicin is needed, the required amount of ml from the vial with the dissolved drug (10 ml = 600 mg of rifampicin, 5 ml, = 300 mg of rifampicin, etc.) is taken and mixed with a 5% solution of dextrose, 5% solution of fructose or 0.9% solution of sodium chloride. The rate of administration is 60 - 80 cap / min. Dosage regimen is set by the doctor individually depending on the severity of the disease and the patient's response to treatment.

    If the doctor is not assigned otherwise, the following dosing regimens are recommended:

    Adults: 10 mg / kg body weight, the maximum daily dose - 600 mg.

    Children under 6 years and infants older than 2 months: 15 mg / kg of body weight per day.

    Children from 6 to 12 years: 10-20 mg / kg per day, with long-term therapy should exceed 450 mg daily.

    Children over 12 years of age: in the same doses as for adults.

    For the treatment of tuberculosis

    With IV administration, the daily dose for adults is 0.45 g, in severe fast-progressing forms - 0.6 g, is given in 1 dose. The duration of IV administration depends on the tolerability and is 1 month or more (with the subsequent transition to oral administration). The total duration of use for tuberculosis is determined by the effectiveness of treatment and can be achieved 1d.

    For the treatment of tuberculosis, at least one antituberculous agent is combined (isoniazid, pyrazinamide, ethambutol, streptomycin). Adults with a body weight of less than 50 kg - 450 mg / day; 50 kg and more - 600 mg / day. Children and newborns - 10 -20 mg / kg per day; the maximum daily dose is 600 mg.

    In case of tuberculous meningitis, disseminated tuberculosis, spinal cord injury with neurological manifestations, when tuberculosis is combined with HIV 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), 7 months - in combination with isoniazid.

    In the case of pulmonary tuberculosis and detection of mycobacteria in sputum, the following 3 regimens are used (all with a duration of 6 months):

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

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

    3 Throughout the course - the reception in combination with isoniazid, pyrazinamide and ethambutol (or streptomycin) 3 times during each week. In cases where antituberculous drugs are used 2-3 times "per week (as well as in case of exacerbations of the disease or inefficiency of therapy), their reception should be carried out under the supervision of medical personnel.

    With infections of non-tuberculous etiology

    The daily dose for adults is 0,3 - 0,9 g (maximum - 1,2 g), for children over 2 months - 10-20 mg / kg. The daily dose is divided into 2 - 3 injections. Duration of treatment

    is set individually, depending on the effectiveness and can be 7 -

    10 days. I / O administration should be discontinued as soon as possible for admission

    inside.

    For the treatment of leprosy:

    For the treatment of multibacillary types of leprosy (lepromatous, borderline,lepromatous and borderline) adults - 600 mg once a month in combination with dapsone (100 mg once a day) and clofazimine (50 mg once a day + 300 mg once a month); Children 10 mg / kg once a month in combination with dapsone (1-2 mg / kg / day) and clofazimine (50 mg every other day + 200 mg once a month). The minimum duration of treatment is 2 years.

    For treatment of multibacillary types of leprosy (tuberculoid and border tuberculoid) adults - 600 mg once a month, in combination with dapsone - 100 mg (1-2 mg / kg) once a day; Children - 10 mg / kg once a month. Duration of treatment - 6 months.

    For treatment of brucellosis - 900 mg / day once in combination with doxycycline; the average duration of treatment is 45 days.

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

    5 mg / kg.

    Patients with impaired hepatic and / or renal function:

    Patients with impaired renal excretory function and preserved liver function dose adjustment is required only when it exceeds 600 mg / day. Features of application after interruption of therapy

    After interruption of therapy rifampicin is prescribed with a gradual increase in the dose.It is necessary to monitor the function of the kidneys, if necessary, the appointment of glucocorticosteroids is recommended.

    Side effects:

    Side effects are listed below in descending order of frequency: often (1-10% of patients), infrequently (0.1-1% of patients), rarely (0.01 - 0.1% of patients), very rarely (less than 0, 01% of patients), including individual reports.

    Allergic reactions: urticaria, eosinophilia, Quincke's edema, bronchospasm, arthralgia, fever.

    From the gastrointestinal tract: often: nausea, vomiting, diarrhea, anorexia, rarely: erosive gastritis, pseudomembranous colitis, increased activity of "liver" transaminases and alkaline phosphatase in the blood serum, hyperbilirubinemia, hepatitis, acute pancreatitis.

    From the side of the eyes: rarely: visual acuity reduction

    From the nervous system: rarely: dizziness, headache, ataxia,

    disorientation, muscle weakness.

    From the hematopoiesis: rarely: leukopenia.

    From the urinary system: interstitial nephritis, nephronecrosis. Other: induction of porphyria, violation of the menstrual cycle, myasthenia gravis, hyperuricemia, exacerbation of gout.

    Local reactions: phlebitis at the site of administration.

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

    If any of the side effects listed in the instruction are aggravated, andwhether You noticed any other side effects not listed in the instructions tell your doctor.

    Overdose:Symptoms: pulmonary edema, confusion, convulsions. Treatment: symptomatic therapy, forced diuresis.
    Interaction:
    Rifampicin induces the induction of the enzyme system of the liver of the cytochrome P-450 system, accelerating the metabolism of drugs. Rifampicin accelerates the metabolism, (the concentration in the blood plasma decreases and, accordingly, the effect decreases) of antiarrhythmics (disopyramide, pyrmenol, quinidine, mexiletine, tokainid), theophylline, some tricyclic antidepressants, oral hypoglycemic drugs, indirect anticoagulants, azathioprine, barbiturates, (phenobarbital, hexobarbital, etc.), buspirone, blockers of "slow" calcium channels (diltiazem, nifedipine, verapamil), antifungal drugs (itraconazole , etc.), cimetidine, thyroxine, glucocorticosteroids, carbamazepine, hydantoins (phenytoin), zidovudine, dapsone, chloramphenicol, terbinafine, neuroleptics (haloperidol and others), tranquilizers (diazepam and others), beta-blockers (propranolol and others), cardiac glycosides (digoxin , etc.), propafenone, cyclosporine, sex hormones, enalapril, inhibitors of cyclooxygenase 2 (celecoxib , etc.), hypolipidemic drugs (simvastatin and others), losartan, antimalarial drugs (mefloquine and others), cytostatics (tamoxifen and etc.). Joint use should be avoided with HIV protease inhibitors (indinavir, nelfinavir). Rifampicin accelerates the metabolism of estrogens and gestagens (the contraceptive effect of oral contraceptives decreases).
    Isoniazid and / or pyrizinamide increases the frequency and severity of liver function disorders more than with the administration of a single rifampicin in patients with a previous liver disease.Co-trimaxosol (sulfamethoxazole / trimethoprim) increases the concentration of rifampicin in the blood.
    Special instructions:Treatment with rifampicin should be done under close medical supervision. Intravenous infusion is carried out under the control of arterial pressure, with prolonged administration, the development of phlebitis is possible. With prolonged use, a systematic control of the pattern of peripheral blood and liver functions is shown.
    Drug treatment should be started after a study of liver function (determination of bilirubin concentration and aminotransferase activity in the blood, timol assay), and in the process of treatment it should be carried out monthly. With increasing phenomena of liver function disorder, the use of the drug should be discontinued. With prolonged use, a systematic control of the peripheral blood picture and liver function is shown.

    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.

    In the case of a flu-like syndrome, not complicated by thrombocytopenia, hemolytic anemia, bronchospasm, dyspnea, shock, and renal failure in patients receiving medication for intermittent scheme, you should consider switching to a daily intake. In these cases, the dose is increased slowly: on the first day, 75-150 mg is prescribed, and the required therapeutic dose is achieved in 3 to 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 I trimester) is possible only for health reasons. In the appointment of the last weeks of pregnancy may experience post-partum haemorrhage in the mother and the newborn bleeding. 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 preventive use, meningococcal bacilli carriers require strict monitoring of patients for.In order to timely identify the symptoms of the disease in the event of resistance to rifampicin. 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. A false-positive result is possible in the immunological determination of opiates in urine. It should be borne in mind that rifampicin interacts with contrast preparations used in cholecystography. Under its influence, the result of X-ray diffraction can be distorted.
    Effect on the ability to drive transp. cf. and fur:During the period of treatment, one should refrain from engaging in potentially dangerous activities requiring increased attention and rapid psychomotor reactions.
    Form release / dosage:
    Liofilizate for the preparation of a solution for infusions 600 mg.

    Packaging:626.4 mg of lyophilizate into bottles of transparent glass type I, sealed with a cork of gray bromobutyl rubber and a "flip-off" cap (an aluminum cap with a plastic cover of red color). 10 vials with instructions for use are placed 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:
    2 years

    The drug should not be used after the expiry date indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N009790
    Date of registration:29.12.2011
    The owner of the registration certificate:Fatol Artsynmittel GmbHFatol Artsynmittel GmbH Germany
    Manufacturer: & nbsp
    Information update date: & nbsp14.05.2016
    Illustrated instructions
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