Absorption – fast, eating reduces the absorption of the drug. When administered on an empty stomach 600 mg maximum concentration – 10 mg / ml. Time to andriol testosterone maximum concentration – 2-3 hours Connection with the plasma protein..
Rapidly distributed in organs and tissues (the highest concentration in the liver and kidney), penetrates into the bone tissue, the concentration in saliva – 20% from plasma. The apparent volume of distribution – 1.6 l / kg for adults.
It penetrates the blood-brain barrier only in case of inflammation of the meninges. Penetrates through the placenta (fetal plasma concentration – 33% of maternal plasma concentrations) and is excreted in breast milk (children breastfed receive no more than 1% of the therapeutic dose).
It is metabolized in the liver with the formation of the pharmacologically active metabolite -25-O-deatsetilrifampitsina. Autoinducer is – accelerates its metabolism in the liver, resulting in systemic clearance – 6 l / h after the first dose, increased to 9 l / h after the second administration. If ingestion is likely also the induction of enzymes and the intestinal wall.
The half-life after oral administration of 300 mg – 2.5 hours, 600 mg – 04.03 h, 900 mg – 5 hours, a few days repeated administration decreases the bioavailability and half-life after multiple-dose 600 mg shortened to 1-2 hours. The.
Write mainly in the bile, 80% – in andriol testosterone the form of metabolites; kidney – 20%. After receiving the amount of 150-900 mg of rifampicin, are excreted renally in unchanged form, it depends on the size of the dose and ranges from 4 to 20%.
Patients with impaired renal excretion half-life is extended only in those cases where it exceeds 600 mg dose. Displayed in peritoneal dialysis and hemodialysis. In patients with impaired hepatic function there is an increase in the plasma concentration of rifampicin and extending the half-life.
Indications for use:
Tuberculosis (all forms) – in a combination therapy.
Leprosy (in combination with dapsone – Multibacillary types of diseases).
Infectious diseases caused by susceptible microorganisms (in the case of resistance to other antibiotics, and as part of combination antimicrobial therapy after exclusion of diagnosis of tuberculosis and leprosy).
Brucellosis – in a combination therapy with the antibiotic tetracycline (doxycycline).
Meningococcal meningitis (prophylaxis in individuals who were in close contact with sick meningococcal meningitis; bacilli carrier from Neisseria meningitidis).
Increased sensitivity to rifampicin andriol testosterone other components of the drug, jaundice, recently transferred (less than 1 year), infectious hepatitis, chronic renal failure, pulmonary heart disease II-III degree, lactose intolerance lack lactase, glucose-galactose malabsorption, children under 3 years, the period of lactation. Contraindicated with concomitant use of ritonavir, saquinavir, atazanavir, darunavir, fosamprenavir, tipranovirom.
Application of pregnancy and during breastfeeding
Treatment during pregnancy (especially in I trimester) is possible only in “real life” testimony. In the appointment of the last weeks of pregnancy may experience post-partum haemorrhage in the mother and the newborn bleeding. In this case, the prescribed vitamin K.
Women of reproductive age during treatment should use reliable methods of contraception (oral hormonal contraceptives and additional non-hormonal methods of contraception).
Dosing and Administration
Inside, on an empty stomach (at 0.5-1 hour before meals).
When treating tuberculosis average daily adult dose of 450 mg 1 time per day. Patients (particularly during exacerbations) weighing more than 50 kg the daily dose may be increased to 600 mg. The average daily intake for children older than 3 years, 10 mg / kg (but not more than 450 mg per day) 1 times a day. When poor tolerability rifampin daily dose can be divided into 2 doses.
Monotherapy TB rifampicin often accompanied by the development of resistance of the pathogen to the antibiotic, so it should be used in combination with other anti-TB drugs (streptomycin, isoniazid, ethambutol, and others.), Which retained the sensitivity of Mycobacteria tuberculosis.
When rifampicin leprosy andriol testosterone used for the following schemes:
a) a daily dose of 300-450 mg is administered in 1 reception; bad Portability – in 2 divided doses. Duration of treatment 3-6 months. Courses are repeated at intervals of 1 month,
b) combination therapy administered daily dose of 450 mg in 2-3 doses for 2-3 weeks at intervals of 2-3 months for 1 year – 2 years, or at the same dose 2-3 1 times a week for 6 months.
Treatment is carried out comprehensively with immunostimulatory agents.
For the treatment of multibacillary types of leprosy (lepromatous and border) for adults – 600 mg 1 time per month in combination with dapsone (100 mg 1 time per day). The minimum duration of treatment – 2 years.
For the treatment of pausibatsillyarnyh types of leprosy (tuberculoid tuberculoid and border) for adults – 600 mg 1 time per month, in combination with dapsone – 100 mg (1-2 mg / kg) 1 time per day. Duration of treatment – 6 months.
For the treatment of infectious diseases caused by susceptible microorganisms (in the case of resistance to other antibiotics, and in a combination antimicrobial therapy after diagnosis of exclusion and leprosy tuberculosis), administered in combination with other antimicrobial agents. The daily dose of 600-1200 mg for children older than 3 years, 10-20 mg / kg. Multiplicity reception 2 times a day.
For the treatment of brucellosis – 900 mg / once a day, in the morning on an empty stomach, in combination with doxycycline for 45 days.
For the prevention of meningococcal meningitis – 2 times a day every 12 hours for 2 days. Single doses of 600 mg for adults. for children over 3 years old to 10 mg / kg.