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

Pharmacodynamics:Semisynthetic broad-spectrum antibiotic, first-line anti-tuberculosis drug. At low concentrations, it has a bactericidal effect on Mycobacterium tuberculosis, Brucella spp., Chlamydia trachomatis, Legionella pneumophila, Rickettsia typhi, Mycobacterium leprae; in high concentrations - on some gram-negative microorganisms. Characterized by high activity against Staphylococcus spp. (including penicillinase-forming and many strains of methicillin-resistant), Streptococcus spp., Clostridium spp., Bacillus anthracis; Gram-negative coca: Neisseria meningitidis, Neisseria gonorrhoeae. Ha gram-positive bacteria acts in high concentrations. It is active with respect to intracellular and extracellularly located microorganisms. Suppresses the DNA-dependent RNA polymerase of microorganisms. With rifampicin monotherapy, the selection of rifampicin-resistant bacteria is relatively rapid. Cross-resistance with other antibiotics (with the exception of the other rifamycins) does not develop.

Pharmacokinetics:

With intravenous administration, the therapeutic concentration of rifampicin is maintained for 8-12 hours. The connection with plasma proteins is 84-91%. Quickly distributed to organs and tissues (the highest concentrations are created in the liver and kidneys), penetrates into the bone tissue, the concentration in the saliva is 20% of that in 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. It penetrates through the placenta (the concentration in the plasma of the fetus is 33% of that in the mother's plasma) and is excreted in breast milk, with the child receiving less than 1% of the mother's dose.

Metabolized in the liver with the formation of pharmacologically active metabolite-25-O-deacetyltrifampicin.

It is excreted from the body mainly with bile (in the form of metabolites). Less than 30% of the dose is excreted in the urine in the form of metabolites or unchanged. As the dose increases, the proportion of renal excretion increases. A small amount of rifampicin is excreted with tears, then, with saliva, sputum and other fluids, staining them in an orange-red color.

In patients with impaired renal excretory function, the half-life period (T1 / 2) is prolonged only if the dose exceeds 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 of all forms and localizations in combination therapy.

Leprosy - in combination with dapsone and clofazimine (in combination with dapsone - only in patients older than 18 years).

Infectious diseases caused by microorganisms sensitive to rifampicin. In connection with the rapid development of resistance of microorganisms rifampicin prescribe only with resistance to other antibacterial drugs, as part of combined antimicrobial therapy. Brucellosis - as part of a combination therapy with doxycycline.

Contraindications:Hypersensitivity to rifampicin (and also to other rifamycins) and other components of the drug, jaundice, recently transferred (less than 1 year) infectious hepatitis, the period of breastfeeding, chronic renal failure, severe pulmonary heart failure, children under 2 months.

Carefully:Children age from 2 months to 1 year, pregnancy.In patients who abuse alcohol, with a history of liver disease, in depleted patients.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the potential benefit to the mother exceeds the potential risk to the fetus. With the appointment in the last weeks of pregnancy, there may be bleeding in the mother in the postpartum period and bleeding in the newborn. In this case, prescribe vitamin K.

During the period of breastfeeding the drug is contraindicated.

Dosing and Administration:

Rifampicin is administered parenterally - intravenously drip. To prepare a solution for intravenous administration, every 150 mg of the drug is dissolved in 2.5 ml of water for injection, vigorously shaken until completely dissolved; the resulting solution is mixed with 125 ml of a 5% dextrose solution. The rate of administration is 60-80 drops per minute.

Intravenous administration of the drug is recommended for 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 when taking the drug inside is difficult or badly tolerated by patients.

For the treatment of tuberculosis rifampicin prescribe in combination with other anti-tuberculosis drugs (ethambutol, pyrazinamide, isoniazid, streptomycin). Adults with a body weight of less than 50 kg are prescribed in a dose of 450 mg / day; with a body weight of 50 kg and more - 600 mg / day. Children are prescribed at the rate of 10-20 mg / kg / day. The maximum daily dose should not exceed 600 mg.

The duration of intravenous administration depends on the tolerability of the drug and is 1 month or more (with the subsequent transition to oral administration). The total duration of use for tuberculosis is determined by the effectiveness of treatment and can reach 12 months.

For treatment of lepromatous, borderline-lepromatous and borderline types of leprosy, adults are prescribed 600 mg once a month in combination with dapsone and clofazimine.

The minimum duration of treatment is 2 years. For the treatment of tuberculoid and borderline tuberculoid types of leprosy rifampicin It is prescribed for 600 mg once a month in combination with dapsone. The course of treatment is 6 months. To treat infectious diseases caused by microorganisms that are sensitive to rifampicin, they are prescribed in combination with other antimicrobial agents.Adults appoint 0.6-1.2 grams per day, children - at a rate of 10-20 mg / kg per day. The daily dose is divided into 2-3 injections. The duration of therapy is set individually, depends on the effectiveness of treatment and is 7-14 days.

For the treatment of brucellosis, adults are prescribed 900 mg / day in combination with doxycycline. The duration of treatment is 45 days.

Patients with impaired renal excretory function and preserved liver function need to adjust the dose only when it exceeds 600 mg / day.

Side effects:

From the digestive system: nausea, vomiting, diarrhea, decreased appetite, erosive gastritis, pseudomembranous colitis; increased activity of "hepatic" transaminases in the blood serum, hyperbilirubinemia, hepatitis.

Allergic reactions: urticaria, eosinophilia, angioedema, bronchospasm, arthralgia, fever.

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

From the side of the urinary system: nephronecrosis, interstitial nephritis.

Other: leukopenia, dysmenorrhea, induction of porphyria, myasthenia gravis, hyperuricemia, exacerbation of gout, with prolonged use, development of phlebitis is possible.With occasional use or with the resumption of treatment after an interruption, flu-like syndrome (fever, chills, headache, dizziness, myalgia), skin reactions, hemolytic anemia, thrombocytopenic purpura, acute renal failure are possible.

Overdose:Symptoms: pulmonary edema, lethargy, confusion, convulsions. Treatment: symptomatic; forced diuresis.

Interaction:Reduces the activity of indirect anticoagulants, oral hypoglycemic drugs, hormonal contraceptives, cardiac glycosides, antiarrhythmics (disopyramide, pirmenol, quinidine, mexiletine, tokainid), glucocorticosteroids, dapsone, phenytoin, hexobarbital, nortriptyline, benzodiazepines, sex hormones, theophylline, chloramphenicol, ketoconazole, itraconazole, cyclosporine, azathioprine, beta adrenoblockers, slow calcium channel blockers, enalapril, cimetidine, (rifampicin causes induction of cytochrome P450 isoenzymes, accelerating their metabolism). Isoniazid and / or pyrazinamide increase the frequency and severity of liver function disorders in a greater degree,than the appointment of a single rifampicin in patients with a previous liver disease. Rifampicin reduces the concentration of HIV-protease inhibitors in the blood. Joint use of rifampicin and statins leads to a decrease in the concentration of statins in the blood, and thereby reducing their hypocholesterolemic effects.

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, the development of phlebitis is possible.

To prevent the development of resistance of microorganisms, it is necessary to use the drug 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 prescription of glucocorticosteroids is possible. Women of reproductive age during treatment should use reliable methods of contraception (oral hormonal contraceptives and additional non-hormonal methods of contraception).

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 folic acid and vitamin B 1 2 in the blood serum.

Form release / dosage:

Lyophilizate for the preparation of a solution for infusions, 150 mg, 300 mg, 600 mg

Packaging:

Primary packaging of medicinal product

For 150 mg, 300 mg, 600 mg of rifampicin in a glass bottle of analytical grade III, sealed with a gray butyl plug and a combination aluminum cap (type Flip off).

A label is attached to the vial from a label or writing paper or from polymer materials, self-adhesive.

Secondary packaging of medicinal product

1 bottle with instructions for use in a cardboard box.

At packing at the enterprise of Open Company "FarmKoncept" (Russia):

Secondary packaging of medicinal product

1 bottle with instructions for use in a cardboard box. For 5 or 10 bottles together with an equal number of instructions for use in a cardboard box (for medical and preventive facilities).

At packing at the enterprise Open Society "Farmasintez" (Russia):

Secondary packaging of medicinal product

One bottle together with instructions for use in a pack of cardboard for consumer packaging subgroups chrome or chrome-ersatz or other similar quality. For 5 or 10 bottles together with an equal number of instructions for use in a cardboard box (for medical and preventive facilities).

When the preparation is packaged with a solvent at the OJSC "Pharmasintez" (Russia):

Primary solvent packaging 5 or 10 ml of solvent in a polyethylene cartridge. The ampoule is labeled with a printer.

Secondary packaging of medicinal product

1 bottle with preparation and 1 ampoule with solvent Water for injection, solvent for preparation medicinal forms for injections 5 ml (for dosages of 150 mg and 300 mg) or 10 ml (for a dosage of 600 mg) in contour cell packaging from film polyvinylchloride and aluminum foil printed lacquered.

1 contour pack together with instructions for use in a pack of cardboard for consumer tare subgroups chrome or chrome-ersatz or other of similar quality.

The packets are placed in a group package.

Storage conditions:Store in a 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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002197

Date of registration:22.08.2013/12.02.2016

Date of cancellation:2018-08-22

The owner of the registration certificate:Virend International, Inc.Virend International, Inc. Russia

Manufacturer: & nbsp

SANJIVANI PARANTERAL, Limited India

Information update date: & nbsp13.05.2016

Illustrated instructions

Instructions

Rifampicin (Rifampicin)