Rifampicin

General characteristics. Structure:

Active ingredient: 100 mg or 300 mg of rifampicin.

Rifampicin is a semi-synthetic antibiotic of a broad spectrum of activity. It is active concerning mycobacteria of tuberculosis and leprosy, works on gram-positive (especially staphylococcus) and gram-negative (meningokokk, gonokokk) cocci, is less active concerning gram-negative bacteria.

Pharmacological properties:

Pharmacodynamics. Antituberculous remedy. Semi-synthetic antibiotic of a broad spectrum of activity. In low concentration has bactericidal effect on Mycobacterium tuberculosis, Brucella spp., Chlamydia trachomatis, Legionella pneumophila, Rickettsia typhi, Mycobacterium leprae; in high concentration – on some gram-negative microorganisms. It is effective in the relation intracellularly and vnekletochno the located microorganisms. Suppresses a DNA-dependent RNA polymerase of microorganisms. At monotherapy drug rather quickly notes selection of bacteria, resistant to rifampicin. Cross resistance with other antibiotics (except for other Rifamycinums) does not develop.

Pharmacokinetics. It is soaked up in digestive tract quickly. Meal reduces drug absorption. Cmax in 2-2.5 hours. It is quickly distributed on bodies and fabrics (the greatest concentration in a liver and kidneys), gets into a bone tissue. Through GEB gets only in case of an inflammation of a meninx. Gets through a placenta (concentration in fruit plasma – 33% of concentration in mother's plasma) and it is allocated with breast milk (the children raised by breast milk receive no more than 1% of a therapeutic dose of drug). Has properties of a self-induction, accelerates the biotransformation. It is metabolized in a liver with formation pharmacological of an active metabolite. 80% - in the form of a metabolite are removed preferential with bile; kidneys - 20%. After reception of 150-900 mg of drug the amount of the rifampicin which is removed kidneys in not changed look depends on the size of the accepted dose and makes 4-20%. At patients with disturbances of secretory function of kidneys the elimination half-life is extended only when its doses exceed 600 mg. At patients with abnormal liver functions increase in concentration of rifampicin in plasma and lengthening of an elimination half-life is noted that can demand correction of doses of drug.

Indications to use:

Tuberculosis (all forms) - as a part of a combination therapy. The infectious diseases caused by sensitive microorganisms (in resistance cases to other antibiotics and as a part of the combined antimicrobic therapy; after an exception of the diagnosis of tuberculosis and a leprosy).

Route of administration and doses:

Inside, on an empty stomach, in 30 min. prior to food. The adult with body weight less than 50 kg - 450 mg/days; 50 kg and more - 600 mg/days. The maximum daily dose - 600 mg. To children and newborns - 10-мг/кг/сут. The general duration of use of rifampicin at tuberculosis is defined by efficiency of treatment. At tubercular meningitis, the disseminated tuberculosis, damage of a backbone with neurologic manifestations, at a tuberculosis combination to HIV infection the general duration of treatment - 9 months. For treatment of the infectious diseases caused by microorganisms, sensitive to drug, appoint in a combination with other antimicrobic means. A daily dose for the adult – 600-1200 mg, for children and newborns – 10-20 mg/kg of body weight. Frequency rate of reception 2 times a day.

Features of use:

Against the background of treatment skin, a phlegm, sweat, kcal, the lacrimal liquid, urine gain orange-red color.

Can paint soft contact lenses with firmness. In case of transition to daily reception of the patients receiving drug according to the intermittent scheme increase a dose slowly: in the first day appoint 75-150 mg, and reach the necessary therapeutic dose in 3-4 days.

Therapy during pregnancy (especially in the I trimester) is possible only according to vital indications.

At purpose in recent weeks of pregnancy puerperal bleeding at mother and bleeding at the newborn can be observed. In this case appoint vitamin K.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, loss of appetite, erosive gastritis, pseudomembranous coloenteritis; increase in activity of "hepatic" transaminases in blood serum, a hyperbilirubinemia, hepatitis. From a nervous system: headache, decrease in visual acuity, ataxy, disorientation. From an urinary system: intersticial nephrite, it is extremely rare нефронекроз, Allergic reactions: urticaria, eosinophilia, Quincke's disease, bronchospasm, arthralgia, fever. Other: leukopenia, dysmenorrhea, induction of a porphyria, myasthenia, hyperuricemia, exacerbation of gout.

Interaction with other medicines:

The isoniazid and/or Pyrazinamidum increase the frequency and weight of abnormal liver functions more than at purpose of one rifampicin, at patients with the previous liver disease.

It is necessary to appoint drug PASK not earlier than in 4 h after rifampicin reception since absorption disturbance is possible.

Reduces activity of peroral anticoagulants, peroral hypoglycemic drugs, hormonal contraceptives, drugs of a foxglove, antiarrhytmic drugs (Disopyramidum, quinidine, мексилетин, токаинид), glucocorticosteroids, benzodiazepines, sex hormones, theophylline, a ketokonazol, an itrakonazol, cyclosporine A, Azathioprinum, beta adrenoblockers, blockers of ring channels, enalapril, Cimetidinum (rifampicin causes induction of some fermental systems of a liver, accelerates metabolism).

Antacids, opiates, anticholinergic HP and кетоконазол reduce (in case of a concomitant use inside) bioavailability of rifampicin.

Contraindications:

Hypersensitivity, jaundice, recently postponed (less than 1 year) infectious hepatitis, the period of a lactation, HPN, a pulmonary heart of the II-III St, chest age.

Overdose:

Symptoms: fluid lungs, lethargy, confusion of consciousness, spasm. Treatment: symptomatic; gastric lavage, purpose of absorbent carbon; artificial diuresis.

Storage conditions:

In the place protected from light at the room temperature.

Issue conditions:

According to the recipe

Packaging:

Capsules 150 mg, 2 blisters on 10 capsules in cardboard packaging; capsules 300 mg, 2 blisters on 10 capsules in cardboard packaging.