Rifampicin (frozen-dried powder for injections 0,15 г)
Rifampicinum 0,15 pro injectionibus
International non-patented name
Antibiotic from ansamicines group. Antituberculous agent.
1 ampoule contain 150mg of rifampicin (powder for injection).
Rifampicin Ч semisynthetic antibiotic with wide range of antimicrobic action from the group of rifampicines (ansamicines). Has bactericidal effect. Affect to RNA synthesis in bacterial cell, by inhibit of DNA-dependent RNA- polymerase. Highly active in respect of Mycobacterium tuberculosis, act as antituberculous agent of I series.
Active to gram-positive bacteria (Staphylococcus spp, including polyresistant cultures), Streptococcus spp., Bacillus anthracis, Clostridium spp.) and some gram-negative bacteria (Neisseria meningitidis, N.gonorrhoeae, Haemophilus influenzae, Brucella spp., Legionella pneumophila). Active to Chlamydia trachomatis, Rickettsia prowazekii,† Mycobacterium leprae. Do not have affect to fungi. Rifampicin has viricidal action to hydrophobia virus, suppress the development of encephalitis.
Resistance to rifampicin is rapidly progress. Crossed resistance with other antibacterial preparations (with the exception for others rifampicines) was not discover.
During intravenous steam injection rifampicin peak concentration observed by the end of infusion (10 mcg/ml after 600g of rifampicin injection). Rifampicin has well penetration in tissues and fluids of the body, detected in therapeutic concentration in pleural exudation, phlegm, honeycombs secretion, bone tissue; the largest concentration created in liver and kidneys. Bonding with plasma proteins constitutes 80Ч90%. Rifampicin penetrates through blood-cerebrospinal fluid, through placenta, detected in human milk. Drug biotransformation carried out in liver. Half-period is 2-5 hours. Drug concentration on therapeutic level maintained during 8-12 hours, in relation to highly sensitive causative agents Ч during 24 hours. Removed from the body with bile, faeces and urine.
Rifampicin used for treatment of tuberculosis (including tuberculous meningitis), in combination therapy; in case of infectious-inflammatory sicknesses caused by causative agents sensitive to preparation (including osteomyelitis, pneumonia, pyelonephritis, lepra, gonorrhoea, otitis, cholecystitis etc.), as well as Neisseria meningococci in carriers. Preparation is recommended to use in case of acute progressive and extensive forms of destructive pulmonary tuberculosis, severe purulent septic processes if high concentrations of preparation with blood is needed rapidly, as well as in cases when preparation intake is difficult or badly carried by patients.
In connection with fast development of stability to the antibiotic during treatment, application of rifampicin at diseases not tubercular etiology is limited to the cases when other antibiotics not giving in to therapy.
Method of usage and dosage regimen
For preparation of a solution 0,15 г rifampicin dissolved in 2,5 ml of sterile water for injections, vigorously stir up an ampoule with a powder before the full dissolution, the received solution is dissolved in 125 ml of a solution of glucose of 5 %. Enter intravenously with speed of 60-80 drops into a minute.
At treatment of a tuberculosis the daily doze for adults is 0,45 g, at severe rapidly progressive forms - 0,6 g. The preparation is entered 1 time per day within 1 month and more with the subsequent purpose of a preparation inside.
At infections of not tubercular nature intravenously injected daily doze for the adult is 0,3-0,9 g (2 3 introductions). Duration of treatment is defined individually depending on efficiency and tolerance of a preparation and could be 7-10 days. In case of opportunity switch to reception of a preparation inside.
Treatment by rifampicin should be carried out under careful medical supervision.
Preparation reception could be accompanied with colored of urine, feces, saliva, sweat, tears and contact lenses in red.
During preparation usage are possible: nausea, vomiting, diarrhea, downturn of appetite, increase of a hepatic transaminases level, bilirubin in blood plasma, pseudomembranous colitis, cholestatic jaundice, a hepatites, a headache, arthralgia, ataxy, canalicular necrosis, interstitial nephritis, acute liver insufficiency, infringements of sight, leukopenia, it is rare - a thrombocytopenia, thrombocytopenic purpura, eosinophilia, hemolytic anemia, menstrual cycle abnormality, urticaria, angioneurotic edema, bronchismus, influenza syndrome.
During fast intravenous injection arterial pressure can decrease, and during continuous introduction the phlebitis can be developed.
The risk of undesirable reactions increases in case of long treatment by a preparation, and also at a combination of rifampicin with isoniazid.
Heightened sensibility to rifampicin or another rifampicines, a jaundice (including mechanical), recently transmitted (less than 1 year) an infectious hepatites, diseases of a liver and kidneys, pregnancy and a lactation (refusal of chest feeding is obligatory), children's age, heart-lung insufficiency, phlebitises.
With care applied with emaciated patients, at the patients abusing alcohol, in case of porphyria.
In case of development of a thrombocytopenia, purples, hemolytic anemia, anaphylactic shock, renal insufficiency and other serious undesirable reactions rifampicin treatment should be stoped.
Treatment by a preparation should be start after research of function of a liver (definition of bilirubin and aminotransferasas level in blood, thymol test), and during treatment to spend it monthly. At the accrueing phenomena of infringement of function of a liver application of a preparation should be stopped. At long application of a preparation it is necessary to supervise a picture of blood in connection with possibility of leukopenia development.
Monotherapy of a tuberculosis by rifampicin is often accompanied by development of stability of the activator to an antibiotic, therefore it should be combined with other antitubercular means. At treatment of not tubercular infections probably fast development of resistency of microorganisms; this process can be warned if to combine rifampicin with other chemotherapeutic means.
The preparation is not shown for faltering therapy.
Interaction with other drugs
Rifampicin - strong P-450cytochrome inductor, can cause potentially dangerous medicinal interactions. Rifampicin accelerates a metabolism (concentration in plasma of blood decreases and accordingly action decreases) of theophyllin, thyroxin, corticosteroides, carbamazepine, fenitoin, peroral anticoagulants, пероральных hypoglycemic preparations, dapsone, the some tricyclic energizers, chloramphenicol, fluknazol, ketoconazole, terbinafil, haloperidol, diazepam, bisoprolol, propandolol, diltiazem, nifedipine, verapamil, heart glycoside, quinidin, disopyramide, propafenone, cyclosporine.
It is necessary to avoid combined application with HIV-proteases inhibitors. Rifampicin accelerates a metabolism of estrogen and gestagenes (the contraceptive effect peroral contraceptives decreases). Ketoconazole can reduce concentration of rifampicin in plasma of blood.
Symptoms: nausea, vomiting, drowsiness, liver enlargement, jaundice, bilirubin and hepatic transaminase level in blood plasma increase; mahogany of orange skin, urine, saliva, sweat, tears and feces in proportion to preparation dosage accepted.
Treatment: preparation intake should be stopped. Symptomatic therapy (specific antidote is not existed). Vital functions maintenance.
Medicinal form and package
Frozen-dried powder for injection solution preparation in ampoules for 150 mg. Package of 10 ampoulas.