Rifampicin - instructions for use, dose, side effects, contraindications

Composition:each ampoule contains: active substance: rifampicin (in terms of 100% substance) - 150 mg; auxiliary substances: ascorbic acid - 15 mg, sodium sulfite - 3 mg.

Description:

lyophilized powder or porous mass of a reddish-brown or brownish-red color, odorless. Sensitive to light, moisture and air.

Pharmacotherapeutic group:Antibiotic-rifamycin.

ATX: & nbsp

J.04.A.B Antibiotics

J.04.A.B.02 Rifampicin

Pharmacodynamics:

Rifampicin is a semisynthetic antibiotic of a broad spectrum of antimicrobial activity from the group of rifamycins (ansamycins). It is bactericidal. It disrupts the synthesis of RNA in a bacterial cell by inhibiting DNA-dependent RNA polymerase. Highly active against Mycobacterium tuberculosis, is a first-line anti-tuberculosis drug.

It is active against Gram-positive bacteria (Staphylococcus spp, including polyresistant strains, Streptococcus spp., Bacillus anthracis, Clostridium spp.) And some gram-negative bacteria (Neisseria meningitidis, N. gonorrhoeae, Haemophilus influenzae, Brucella spp., Legionella pneumophila). It is active against Chlamydia trachomatis, Rickettsia prowazekii, Mycobacterium leprae. It does not affect fungi. Rifampicin Suppress the development of rabies encephalitis.

Resistance to rifampicin develops rapidly. Cross-resistance with other antibacterial drugs (with the exception of the other rifamycins) has not been identified.

Pharmacokinetics:

At intravenous drip introduction the maximum concentration of rifampicin is observed by the end of infusion. At the therapeutic level, the concentration of the drug for ingestion and intravenous administration is maintained for 8 to 12 hours, for highly sensitive pathogens - within 24 hours. The connection with plasma proteins is 84-91%.

Quickly distributed to organs and tissues (the highest concentration in the liver and kidneys), penetrates into the bone tissue, the concentration in the saliva - 20% of the plasma. The apparent volume of distribution is 1.6 l / kg - in adults and 1.1 l / kg - in children. Through the blood-brain barrier penetrates only in case of inflammation of the meninges. Penetrates through the placenta (concentration in fetal plasma - 33% of the concentration in the mother's plasma) and excreted in breast milk (breastfed babies receive no more than 1% of the therapeutic dose of the drug). Metabolized in the liver with the formation of pharmacologically active metabolite-25-O-deacetyltrifampicin. It is an autoinducer - it accelerates its metabolism in the liver, as a result of which the creatinine clearance is 6 l / h after the first dose, increases to 9 l / h after repeated administration.

It is excreted mainly with bile - 80% in the form of a metabolite; kidneys - 20%. After taking 150-900 mg of the drug, the amount of rifampicin excreted by the kidneys in unchanged form depends on the value of the dose taken and is 4-20%. In patients with impaired renal excretory function, the half-life period (T1 / 2) is prolonged only when its doses exceed 600 mg. It is excreted in peritoneal dialysis and hemodialysis. In patients with impaired hepatic function, an increase in rifampicin plasma concentration and an elongation of T1 / 2 were noted.

Indications:

Tuberculosis (all forms) - as part of combination therapy.

Leprosy (in combination with dapsone - multibacillary types of the disease).

Infectious diseases caused by sensitive microorganisms (in cases of resistance to other antibiotics and in combination antimicrobial therapy, after excluding the diagnosis of tuberculosis and leprosy).

Meningococcal meningitis (prophylaxis in individuals who were in close contact with diseased meningococcal meningitis; y bacilli carrier neisseria meningitidis) Due to the rapid development of resistance to an antibiotic in the treatment process,The use of rifampicin in diseases of non-tuberculous etiology is limited to cases that can not be treated with other antibiotics.

Contraindications:

Hypersensitivity to rifampicin and other components of the drug, jaundice, recently transferred (less than 1 year) infectious hepatitis, lactation period, chronic renal failure, severe pulmonary heart failure, children's age.

With the development of thrombocytopenia, purpura, hemolytic anemia, anaphylactic shock and other serious unwanted adverse reactions, treatment with rifampicin is discontinued.

Carefully:at pregnancy (only on "vital" indications), at the depleted patients, at the patients abusing alcohol, at porphyria.

Pregnancy and lactation:

The use of the drug is contraindicated during lactation.

During pregnancy, use the drug with extreme caution and only in those cases where the intended use for the mother exceeds the possible risk to the fetus.

Dosing and Administration:

Intravenously drip.

Intravenous - with acute and progressive forms of destructive pulmonary tuberculosis,severe purulent-septic processes, when it is necessary to quickly create high concentrations of the drug in the blood and in the focus of infection, in cases where the intake of the drug inside is difficult or poorly tolerated by patients. With intravenous administration, the daily dose for adults is 450 mg, in severe, rapidly progressive forms - 600 mg, is administered in a single dose. The duration of intravenous administration depends on the tolerability and is 1 month or more (with subsequent transition to oral administration).

With the preventive purpose and for the eradication of meningococcal carriage in children younger than 1 month. a dose of 5 mg / kg / day is administered, divided into 2 doses every 12 hours, for 2 days.

In children older than 1 month. and in adults, a dose of 10 mg / kg (but not more than 600 mg / day) every 12 hours for 2 days is applied. The use of oral dosage forms is preferred. The drug is taken on an empty stomach (1 hour before or 2 hours after eating), with a full glass of water. Patients who can not take the drug inside, it is administered intravenously in the same dose. The drug is not administered subcutaneously and intramuscularly.

Total duration of application in tuberculosis is determined by the effectiveness of treatment and can reach 1 year.

With infections of non-tuberculous etiology daily dose of 300-900 mg (maximum - 1200 mg). The daily dose is divided into 2-3 injections. The duration of treatment is set individually, depends on the effectiveness and can be 7-10 days. Intravenous administration should be discontinued as soon as possible for oral administration.

To prepare a solution for intravenous administration, 600 mg of rifampicin is dissolved in 10 ml of water for injection; the resulting solution is mixed with 500 ml of a 5% dextrose solution. The rate of administration is 60-80 cap / min.

Side effects:

From the nervous system: headache, decreased visual acuity, ataxia, disorientation.

From the digestive system: erosive gastritis, pseudomembranous colitis, decreased appetite, nausea, vomiting, diarrhea (usually temporary).

Liver: increased activity of transaminases and bilirubin concentration in the blood; drug hepatitis. Risk factors: alcoholism, liver disease, combination with other hepatotoxic drugs.

Allergic reactions: rash, urticaria, arthralgia, fever, bronchospasm,severe allergic reactions, eosinophilia, Quincke's edema; skin syndrome (at the beginning of treatment), manifested by reddening, itchy skin of the face and head, lacrimation.

Grippopodobny syndrome: headache, fever; pain in the bones (usually develops with irregular intake of the drug).

Hematologic reactions: thrombocytopenic purpura (sometimes with bleeding during intermittent therapy); neutropenia (more often in patients receiving rifampicin in combination with pyrazinamide and isoniazid),

From the urinary system: reversible renal failure, nephronecrosis, interstitial nephritis.

Other: leukopenia, dysmenorrhea, induction of porphyria, myasthenia gravis, hyperuricemia, exacerbation of gout.

Local reactions: phlebitis at the site of administration.

With irregular admission or with the resumption of treatment after a break, skin reactions, hemolytic anemia, are possible.

The risk of unwanted reactions increases with prolonged treatment with the drug, as well as with combination of rifampicin with isoniazid.

Overdose:

Symptoms: nausea, vomiting, drowsiness, enlarged liver, jaundice, increased bilirubin concentration in the blood,hepatic transaminases in blood plasma; brownish-red or orange coloration of the skin, urine, saliva, sweat, tears and feces in proportion to the dose taken.

Treatment: discontinuation of the drug. Symptomatic therapy (there is no specific antidote). Maintaining vital functions.

Interaction:Reduces the activity of oral anticoagulants, oral hypoglycemic drugs, hormonal contraceptives, cardiac glycosides, antiarrhythmic drugs (disopyramide, pirmenol, quinidine, mexiletine, tokainid), glucocorticosteroids, dapsone, phenytoin, hexobarbital, nortriptyline, benzodiazepines, sex hormones, theophylline, chloramphenicol, ketoconazole, itraconazole, cyclosporine A, azathioprine, beta adrenoblockers, slow calcium channel blockers, enalapril, cimetidinerifampicin causes the induction of certain enzyme systems of the liver, accelerates metabolism). Isoniazid and / or pyrazinamide increase the frequency and severity of liver function disorders to a greater extent than with the appointment of a single rifampicin, in patients with a previous liver disease.

Special instructions:

During treatment the skin, mucus, sweat, feces, lacrimal fluid, urine becomes orange-red color. Can persistently stain soft contact lenses.

Intravenous infusion is carried out under the control of arterial pressure; with prolonged administration, it is possible to develop phlebitis. With rapid intravenous administration, blood pressure may decrease.

To prevent the development of resistance, microorganisms must be used in combination with other antimicrobial drugs. In the case of a flu-like syndrome, not complicated by thrombocytopenia, hemolytic anemia, bronchospasm, dyspnea, shock, and renal failure in patients receiving medication for intermittent scheme, you should consider switching to a daily intake. In these cases, the dose is increased slowly on the first day prescribe 75-150 mg, and the desired therapeutic dose is achieved in 3-4 days. In the event that the above serious complications are noted, rifampicin cancel. It is necessary to monitor kidney function; an additional appointment of glucocorticosteroids (GCS).Therapy during pregnancy (especially in the first trimester) is possible only by "vital" indications. In the appointment of the last weeks of pregnancy may experience post-partum haemorrhage in the mother and the newborn bleeding. In this case, prescribe vitamin K.

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

In the case of prophylactic use, meningococcal bacilli carriers require strict monitoring of patients in order to timely identify the symptoms of the disease in the event of rifampicin resistance. With prolonged use, a systematic control of the peripheral blood picture and liver function is shown. During the treatment period, it is impossible to apply microbiological methods for determining the concentration of folic acid and vitamin B12 in the blood serum.

Effect on the ability to drive transp. cf. and fur:in connection with the possible development of adverse reactions from the nervous system, it is not recommended to operate vehicles and other dangerous mechanisms.

Form release / dosage:

Lyophilizate for the preparation of a solution for infusions of 150 mg.

Packaging:

For 150 mg of active substance in ampoules of neutral glass. For 10 ampoules, together with the instructions for use and the ampoule scarifier, are placed in a pack of cardboard. When using ampoules with a break ring, it is allowed to pack ampoules without an ampoule scarifier.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-000741

Date of registration:29.09.2011/04.03.2015

Date of cancellation:2016-09-29

The owner of the registration certificate:BELMEDPREPARATY, RUP BELMEDPREPARATY, RUP Republic of Belarus

Manufacturer: & nbsp

BELMEDPREPARATY, RUP Republic of Belarus

Information update date: & nbsp15.05.2016

Illustrated instructions

Instructions

Rifampicin (Rifampicin)