Rifamycin (Rifamycinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Ansamycins

Included in the formulation
  • Otofa
    drops tion. 
    Bouchard-Recordati Laboratories     France
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    S.01.A.A   Antibiotics

    S.02.A.A.12   Rifamycin

    Pharmacodynamics:

    Antibiotic of the rifamycin group, obtained from the radial fungus Streptomyces mediterranei. Has a bactericidal effect. The mechanism of action is associated with the suppression of RNA synthesis by forming a complex with DNA-dependent RNA polymerase.

    At low concentrations, it is active against Mycobacterium tuberculosis, Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae), Neisseria gonorrhoeae, Neisseria meningitidis; in higher concentrations is active against Escherichia coli, Proteus spp.

    It is active against strains of microorganisms resistant to semisynthetic penicillins and cephalosporins. Do not cross-react with other antibiotics (except rifampicin).

    Pharmacokinetics:Quickly absorbed when administered intramuscularly, with topical application in the form of ear drops and from the digestive tract - a low degree of absorption in the systemic circulation. TCmax 30 min, the therapeutic concentration is maintained for 6-8 hours. Half-life period is 2 hours. With an increase in the dose 4 times, Cmax increases by 1.5-3 times and with iv injection is higher than with v / m, but decreases more rapidly. Do not cumulate. Relationship with plasma proteins 60-70%. Distribution: Cmax is defined in the liver, less in the kidneys, lungs, ascites and pleural fluids. Long stay in the foci of inflammation. Does not penetrate the BBB.Penetrates through the placental barrier. Metabolized with the formation of an active metabolite. Two hours after intravenous administration of 250 and 500 mg, the concentration in the blood plasma was 2 and 11 μg / ml, respectively. It is excreted with feces (60-90% within 8-24 hours), in an insignificant quantity by kidneys. In the intestine there is a partial reverse absorption, which causes a prolonged circulation in the body. With cholestasis, the concentration in the plasma increases.
    Indications:

    Infectious-inflammatory diseases caused by microorganisms sensitive to rifamycin, including gonorrhea, tuberculosis.

    ICD-10

    I.A15-A19.A15   Tuberculosis of respiratory organs, confirmed bacteriologically and histologically

    I.A15-A19.A17   Tuberculosis of the nervous system

    I.A15-A19.A18.8   Tuberculosis of other specified organs

    I.A50-A64.A54   Gonococcal infection

    Contraindications:Hypersensitivity (including for topical application).
    Jaundice, infectious hepatitis (including recently transferred - less than 1 year).
    Chronic renal failure, cardiopulmonary insufficiency of II-III degree.
    Breast age, pregnancy, breast-feeding.
    Acute and chronic otitis media (including with isolated purulent lesions of the tympanic membrane and its perforation), states after operations on the middle ear.
    Carefully:

    Violation of the function of the liver.

    Pregnancy and lactation:

    Systemic use is contraindicated. Penetrates into breast milk. Safety of topical application is not defined.

    Category of recommendations FDA is not defined.

    Dosing and Administration:Intramuscularly adults and children over 6 years old with a body weight of more than 25 kg - 500-750 mg every 8 and 12 hours respectively; children under 6 years - 125 mg every 12 hours.

    Intravenously adults and children with a body weight of more than 25 kg - 500 mg per day; for children weighing less than 25 kg - the daily dose is 10-30 mg / kg, the frequency of administration is 2-4 times / day.

    For topical use in the treatment of tuberculosis lesions, a single dose of 125 mg.

    Ear drops 5 drops (children - 3 drops) 3 times a day or twice a day poured into the external auditory meatus for several minutes. Course - 1-3 days (no more).

    Side effects:

    From the digestive system: nausea, vomiting, diarrhea, anorexia, erosive gastritis, pseudomembranous enterocolitis, increased activity of hepatic transaminases, hyperbilirubinemia, hepatitis.

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

    On the part of the hematopoiesis system: leukopenia.

    On the part of the reproductive system: dysmenorrhea.

    From the side of the central nervous system and the peripheral nervous system: headache, visual impairment, ataxia, disorientation, muscle weakness.

    From the urinary system: nephronecrosis, interstitial nephritis.

    Other: herpes, phlebitis (with iv introduction), induction of porphyria.

    When topical application in the form of ear drops: allergic reactions, staining of the tympanic membrane in pink (visible with otoscopy).

    Overdose:Due to the low degree of absorption in the systemic blood flow, an overdose is unlikely.
    Interaction:Antacids, opioids, anticholinergics and ketoconazole reduce (in the case of simultaneous ingestion) bioavailability of rifamycin.

    With simultaneous application isoniazid and / or pyrazinamide increase the frequency and severity of liver function disorders to a greater extent (in patients with a previous liver disease).

    With simultaneous application rifamycin reduces the activity of oral anticoagulants, oral hypoglycemic drugs, hormonal contraceptives, digitalis preparations, antiarrhythmics (disopyramide, quinidine, mexiletine, tokainid), glucocorticosteroids, dapsone, hydantoins (phenytoin), hexobarbital, nortriptyline, benzodiazepines, sex hormones, theophylline, chloramphenicol, ketoconazole, itraconazole, cyclosporin A, azathioprine, beta adrenoblockers, slow calcium channel blockers, enalapril, cimetidine (rifamycin causes the induction of certain enzyme systems of the liver, accelerates metabolism).

    Special instructions:

    On the background of treatment in patients, skin, sputum, sweat, feces, tear fluid, urine acquire an orange-red color. Can persistently stain soft contact lenses.

    Avoid contact with the solution on clothing (leaves stains).

    Contains sulphites, which must be taken into account when appointing patients with hypersensitivity to sulfur.

    Before using ear drops, it is recommended to warm the bottle holding it in your hand, in order to avoid the unpleasant sensations associated with the ingress of cold liquid into the external auditory canal.

    It is not represented in the United States Pharmacopeia.

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