Rifampicin, capsules on 0,15 g No. 20

General characteristics. Structure:

Active ingredient: rifampicin; 1 capsule contains rifampicin - 150 mg or 300 mg in

recalculation for 100% dry matter;

excipients: lactoses monohydrate, magnesium carbonate the main, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Rifampicin - a semi-synthetic antibiotic of a broad spectrum of activity, antitubercular medicine I of a row. It is active 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.      Shows the most expressed activity    concerning  mycobacteria  of tuberculosis, atypical mycobacteria of different types (except for M.fortuitum), gram-positive cocci. Affects gram-negative cocci - N.meningitidis  and N.gonorrhoeae (including β-lactamazoforming) - however the last quickly gain drug resistance in the course of treatment. Rifampicin is active concerning H.influenzae (including steady against ampicillin and chloramphenicol), H.ducreyi, B.pertussis, B.anthracis, L.monocytogenes, F.tularensis, легионелл, rickettsiae. Representatives of the Enterobacteriaceae family and nonfermentative gram-negative bacteriums (Pseudomonas spp., Acinetobacter spp.,  Stenothrophomonas spp.  etc.) are insensitive. Rifampicin is active concerning gram-positive anaerobe bacterias (including C.difficile).

Pharmacokinetics. Absorption - bystry, meal reduces drug absorption. At intake on an empty stomach 600 mg of drug the maximum concentration in blood (Cmax) - 10 mkg/ml, time of achievement of the maximum concentration (Tmax) - 2-3 h. Communication with proteins of plasma - 84-91%. It is quickly distributed on bodies and fabrics (the greatest concentration in a liver and kidneys), concentration in saliva - 20% from plasma gets into a bone tissue. The seeming volume of distribution of-1,6 l/kg of body weight at adults and 1,1 l/kg of body weight - at children. Through a blood-brain barrier 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). It is metabolized in a liver with formation pharmacological of an active metabolite - 25-O diatsetilrifampitsin. Is an autoinduktor - accelerates the metabolism in a liver therefore system clearance - 6 l/h after reception of the first dose, increase up to 9 l/h after repeated reception.  At intake also induction and intestines wall enzymes is probable. An elimination half-life (Ti/g) after intake of 300 mg - 2,5 h, 600 mg - Ь h, 900 mg - 5 h. In  several  days  of repeated  reception  bioavailability  decreases,  and  T1/2 after multiple dose of 600 mg is shortened to 1-2 h. 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 of T1/2udlinyaetsya only when its doses exceed 600 mg. It is removed at peritoneal dialysis and at a hemodialysis. At patients with abnormal liver functions increase in concentration of rifampicin in plasma and lengthening of T1/2 is noted.

Pharmaceutical characteristics.

The main physical and chemical svoystva:tverdy gelatin capsules with a lid and the case of orange-red color, No. 1 containing powder of brick or brick-red color with white impregnations.

Indications to use:

Treatment of tuberculosis (to apply only in combination with other antituberculous remedies in connection with bystry development of stability of mycobacteria of tuberculosis). Prevention and treatment of atypical mikobakterioz at HIV-positive patients (in combination with azithromycin, ciprofloxacin). A leprosy (in combination with clofazimine, dapsone, Etioniamidum). The severe forms of a staphylococcal infection caused by MRSA (in combination with fusidic acid, Vancomycinum). Legionellosis (in combination with antibiotics macroleads). Prevention of the infections caused by H.influenzae of type B. Drug is used also as anti-virus means of protective complex rabies treatment in an incubation interval. A brucellosis - as a part of a combination therapy with an antibiotic of group of tetracyclines (doxycycline).

Route of administration and doses:

Rifampicin is appointed inside on an empty stomach (in 0,5-1 hour prior to food).

For treatment of tuberculosis the average daily dose for adults makes 450 mg at a single dose (the daily dose should not exceed 600 mg); At bad portability of drug the daily dose can be divided into 2-3 receptions. Drug is used also more is long (depending on a disease form up to I year). In order to avoid development of stability of mycobacteria drug is appointed, as a rule, in combination with other protivotuberkulezyony drugs I and II of a row in their usual doses.

For treatment of acute infections of not tubercular etiology Rifampicin appoint in a daily dose 900-1200 mg in 2-3 receptions. After disappearance of symptoms of a disease drug continues to be used within 2-3 days.

At acute gonorrhea Rifampicin the adult is appointed once in a daily dose by 900 mg, duration of treatment is established individually depending on a look and disease severity (from 1-2 days to 2 weeks and more).

As anti-virus means for protective rabies treatment Rifampicin is appointed inside the adult in a daily dose of 450-600 mg, at - heavy damages (a sting in a face, the head, hands) it is possible to increase a daily dose to 900 mg. The daily dose is recommended to distribute for 2-3 receptions. Duration of treatment is 5-7 days. Use of Rifampicin has to be carried out against the background of passive active immunization (an antirabic vaccine, antirabic gamma globulin).

For treatment of multibacillar types of a leprosy (lepromatous, boundary, boundary and lepromatous) to adult - 600 mg once a month in a combination with dapsone (100 mg of 1 times a day) and clofazimine (50 mg of 1 times a day + 300 mg once a month). The minimum duration of treatment - 2 years.

For treatment of pausibatsillyarny types of a leprosy (tuberculoid and boundary and tuberculoid) to adult - 600 mg once a month, in a combination with dapsone - 100 mg (1-2 mg/kg of body weight) of 1 times a day. Treatment duration - 6 months.

For treatment of a brucellosis at adults - 900 mg/days once, in the morning on an empty stomach, in a combination with doxycycline. The average duration of treatment - 45 days.

Dose adjustment is required to patients with disturbances of secretory function of kidneys and safe function of a liver only in that case when it exceeds 600 mg/days.

Features of use:

Use during pregnancy or feeding by a breast.

It is contraindicated at pregnancy. At a research has teratogenic effect on experimental animals. Gets through a placenta (to 33% of concentration in mother's plasma) and can be the cause of a hemorrhagic disease of newborn and uterine bleedings in a puerperal period. Gets into breast milk in small amounts (about 1% of concentration in mother's plasma). Apply at nursing mothers carefully, only in the absence of safer alternatives.

Children. For treatment of children up to 12 years use drug in other dosage form.

Despite ample therapeutic opportunities of rifampicin, in each case               the specific   patient should estimate potential advantage of its appointment   and   risk of distribution  of stability  and  loss  of value  of rifampicin    as  the main antituberculous remedy. At people of advanced age it has to be applied with care in connection with possible age changes of function of a liver. With care to apply at instructions on liver diseases in the anamnesis. Rifampicin is contraindicated at heavy abnormal liver functions in connection with increase of risk of a hepatotoxic.

At alcoholism the risk of a hepatotoxic increases.

Against the background of treatment by rifampicin skin, a phlegm, sweat, kcal, the lacrimal liquid, urine get

orange-red color. Can paint soft contact lenses with firmness.

  In case of  development  of the grippopodobny  syndrome    which is not complicated by thrombocytopenia, hemolitic anemia, a bronchospasm, an asthma, shock and a renal failure in the patients   receiving  drug  according to  the intermittent   scheme  it is necessary  to consider the possibility of transition to daily reception. In these cases the dose is increased slowly: in the first day appoint 150 mg, and reach the necessary therapeutic dose in 3-4 days. If the serious complications stated above are noted, cancel rifampicin.

At use of rifampicin it is necessary to control function of kidneys.                  

Women of reproductive age during treatment should apply reliable methods of contraception (oral hormonal contraceptives and additional non-hormonal methods of contraception).

At prolonged use systematic control of a picture of peripheral blood and function of a liver is shown.

Ability to influence the speed of reactions at control of motor transport or other mechanisms. Does not influence the speed of neuromuscular reaction, however, in connection with possible development of decrease in visual acuity and a disorientation, appoint with care to the drivers and persons working with dangerous mechanisms.

Side effects:

  From  a nervous  system:    headache,  decrease    in visual acuity,  ataxy, disorientation. From digestive tract: loss of appetite, nausea, vomiting, diarrhea (as a rule, temporary).

From a liver: increase in activity of transaminases and level of bilirubin in blood; seldom - medicinal hepatitis. Risk factors: alcoholism, liver diseases, combination to others

gepatotoksichny drugs.

Allergic reactions: rash, eosinophilia, Quincke's edema; the skin syndrome (in an initiation of treatment) which is shown reddening, an itch of face skin and head, dacryagogue.

Grippopodobny syndrome: a headache, fever, an ostealgia, a mialgiya (develop at irregular reception more often).

From blood: a Werlhof's disease (sometimes with bleeding at intermittent therapy); a neutropenia (is more often at the patients receiving rifampicin in a combination with Pyrazinamidum and an isoniazid).

From bodies of urination: нефронекроз, intersticial nephrite.

Others: leukopenia, dysmenorrhea, induction of a porphyria, myasthenia, hyperuricemia, exacerbation of gout.

Interaction with other medicines:

резистентное™ microorganisms to rifampicin it is necessary to apply to prevention of development in a combination with other antimicrobic medicines. Rifampicin is the inductor of microsomal  enzymes of system of P450 cytochrome; accelerates metabolism of many medicines.

The concomitant use of rifampicin with indirect anticoagulants in connection with easing of their effect is not recommended.
At the combined use of rifampicin with oral contraceptives reliability of the last decreases. Rifampicin weakens effect of glucocorticoids. Rifampicin lowers concentration in a blood plasma and shortens action of peroral antidiabetic  means,  digitoxin,  quinidine,  cyclosporine,  chloramphenicol, doxycycline, a ketokonazol, itrakonazol, to a lesser extent - a flukonazola.

Pyrazinamidum lowers concentration of rifampicin in a blood plasma as a result of impact on hepatic or renal clearance of the last.

Contraindications:

Hypersensitivity to drug components. Jaundice. Recently postponed (less than 1 year) infectious hepatitis. Chronic renal failure. Heavy pulmonary heart. Rifampicin is not used at treatment of asymptomatic forms of a meningococcal infection and a spotted fever because of a possibility of bystry development of stability of an infestant. Chest age. Pregnancy, lactation period.

Overdose:

Symptoms: nausea, vomiting, abdominal pain, headache, confusion of consciousness, spasm, lethargy, fluid lungs.
Treatment: the specific antidote is absent. A gastric lavage, purpose of absorbent carbon, in hard cases an artificial diuresis. Symptomatic further treatment.

Storage conditions:

Period of validity. 2 years. To store in original packaging, in the place, unavailable to children, at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in blister strip packagings, on two packagings in cardboard boxes. On 1000, 2500 or 3000 capsules in containers plastic.