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

Excipients: calcium stearate - 0,9 mg, magnesium hydroxycarbonate hydrate - 15 mg, sodium carboxymethyl starch - 15 mg, lactose monohydrate - up to the mass of the contents of the capsule 300 mg.

The composition of the capsule.

Housing: titanium dioxide - 2%, azorubin - 0.0328%, sunset yellow - 0.2190%, gelatin up to 100%.

Cap: titanium dioxide - 2%, azorubin - 0.0328%, solar sunset yellow - 0.2190%, gelatin up to 100%.

Description:Hard gelatin capsules № 1. Body and capsule capsules are orange. The contents of capsules are a powder of red-brown color, white inclusions are possible.

Pharmacotherapeutic group:Antibiotic-rifamycin.

ATX: & nbsp

J.04.A.B Antibiotics

J.04.A.B.02 Rifampicin

Pharmacodynamics:Semisynthetic broad-spectrum antibiotic, antituberculous drug of the 1st series. 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 cocci: 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:

Absorption - fast, eating reduces the absorption of the drug. When administered on an empty stomach 600 mg the maximum concentration is 10 μg / ml. Time to reach the maximum concentration - 2-3 hours. Communication with plasma proteins - 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 L l / kg in children. Through the blood-brain barrier penetrates only in case of inflammation of the meninges. Penetrates through the placenta (concentration in the plasma of the fetus - 33% of the concentration in the mother's plasma) and excreted in breast milk (breastfed babies receive no more than 1% of the therapeuticdose 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, resulting in a systemic clearance of 6 l / h after the first dose, increases to 9 l / h after repeated administration. When ingestion is also possible, induction and enzymes of the intestinal wall.

Half-life after ingestion 300 mg - 2,5 h, 600 mg - 3-4 h, 900 mg - 5 h. After several days of repeated intake, bioavailability decreases and the half-life after repeated intake of 600 mg is shortened to 1-2 hours. 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 from 4 to 20%. In patients with impaired renal excretory function, the half-life period 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 the half-life period are 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).

Brucellosis - as part of combination therapy with the antibiotic group of tetracyclines (doxycycline).

Meningococcal meningitis (prophylaxis in persons who were in close contact with meningococcal meningitis who fell ill, in Neisseria meningitidis bacilli carriers).

Contraindications:

Hypersensitivity to rifampicin and / or other components of the drug, jaundice, recently transferred (less than 1 year) infectious hepatitis, chronic renal failure, pulmonary heart disease of II-III degree, lactose intolerance, lactase insufficiency, glucose-galactose malabsorption, 3 years, lactation. Contraindicated simultaneous reception with ritonavir, saquinavir, atazanavir, darunavir, fosamprenavir, tipranovir.

Carefully:porphyria.

Pregnancy and lactation:

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).

Dosing and Administration:

Is taken orally, on an empty stomach (0.5-1 hour before meals).

In the treatment of tuberculosis, the average daily intake for adults is 450 mg once a day. In patients (especially during an exacerbation) with a body weight of more than 50 kg, the daily dose can be increased to 600 mg. The average daily dose for children over 3 years is 10 mg / kg (but not more than 450 mg per day) once a day. With poor rifampicin tolerance, the daily dose can be divided into 2 doses.

The monotherapy of tuberculosis with rifampicin is often accompanied by the development of the resistance of the pathogen to the antibiotic, so it should be administered in combination with other anti-tuberculosis drugs (streptomycin, isoniazid, ethambutol, etc.), to which the sensitivity of mycobacteria of tuberculosis is maintained. With leprosy apply rifampicin according to the following schemes:

a) a daily dose of 300-450 mg is administered in a single dose; with poor tolerance - in 2 divided doses. Duration of treatment is 3-6 months. The courses are repeated at intervals of 1 month;

b) on the background of combined therapy, a daily dose of 450 mg is administered 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 times per 1 week for 6 months.

Treatment is carried out in complex with immunostimulating agents. To treat multibacillary types of leprosy (lepromatous and borderline) adults - 600 mg once a month in combination with dapsone (100 mg once a day). The minimum duration of treatment is 2 years.

To treat pausibacillary types of leprosy (tuberculoid and border tuberculoid) adults - 600 mg once a month, in combination with dapsone - 100 mg (1-2 mg / kg) once a day. Duration of treatment - 6 months.

For the treatment of 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), it is prescribed in combination with other antimicrobial agents.The daily dose of 600-1200 mg, for children older than 3 years 10-20 mg / kg. Multiplicity of reception 2 times a day. For treatment of brucellosis - 900 mg / day once, 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 dose for adults 600 mg, for children over 3 years of age 10 mg / kg.

Side effects:

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

From the cardiovascular system: thrombocytopenic purpura, thrombopenia and leukopenia, bleeding, acute hemolytic anemia.

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

From the urinary system: nephronecrosis, interstitial nephritis. Allergic reactions: urticaria, eosinophilia, angioedema, bronchospasm, arthralgia, fever.

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

With an irregular reception or with the resumption of treatment after the break, an influenza-like syndrome (fever, chills, headache, dizziness, myalgia), skin reactions, hemolytic anemia, thrombocytopenic purpura, acute renal failure are possible.

If any of the side effects indicated in the manual are aggravated, or any other side effects not indicated in the instructions are noted, you should inform the doctor immediately.

Overdose:

Symptoms: nausea, vomiting, abdominal pain, enlarged liver, jaundice, periorbital edema or swelling of the face, "red man syndrome" (red-orange coloration of the skin, mucous membranes and sclera), pulmonary edema, lethargy, confusion, convulsions.

Treatment: symptomatic; gastric lavage, reception of activated charcoal; forced diuresis.

Interaction:

Reduces the activity of indirect anticoagulants, oral hypoglycemic drugs, hormonal contraceptives, cardiac glycosides, antiarrhythmic drugs (disopyramide, pirmenol, quinidine, mexiletine, tokainid), glucocorticosteroids, dapsone, phenytoin, hexobarbital, nortriptyline, benzodiazepines, theophylline, chloramphenicol, ketoconazole, itraconazole, cyclosporine, azathioprine, beta adrenoblockers, slow calcium channel blockers, enalapril, cimetidinerifampicin causes induction of cytochrome P450 isoenzymes, accelerating their metabolism).

Co-trimoxazole (sulfamethoxazole + trimethoprim) increases the concentration of rifampicin in the blood. With the simultaneous use of rifampicin (600 mg / day), ritonavir (100 mg twice daily) and saquinavir (1000 mg), it is possible to develop severe hepatotoxicity. When combined rifampicin significantly reduces plasma concentrations of atazanavir, darunavir, fosamprenavir, saquinavir and tipranavir, which may lead to a decrease in antiviral activity.

Rifampicin accelerates the metabolism of certain tricyclic antidepressants, hypolipidemic drugs (simvastatin and others), antimalarial drugs (mefloquine and others), cytostatics (tamoxifen and etc.).

Antacids, narcotic analgesics, anticholinergic drugs and ketoconazole reduce (in the case of simultaneous ingestion) bioavailability of rifampicin.

Isoniazid and / or pyrazinamide Increase the frequency and severity of liver function disorders more than with the administration of a single rifampicin in patients with a previous liver disease.

Preparations of sodium para-aminosalicylate should be prescribed no earlier than 4 hours after taking the drug, tk. absorption impairment is possible.

Special instructions:

At pregnancy a preparation appoint or nominate only on "vital" indications. Women of childbearing age during treatment should use reliable methods of contraception (oral hormonal contraceptives and additional non-hormonal methods of contraception). A false-positive result is possible in the immunological determination of opiates in urine. It should be borne in mind that rifampicin interacts with contrast preparations used in cholecystography. Under its influence, the results of X-ray studies may be distorted. During treatment the skin, mucus, sweat, feces, lacrimal fluid, urine becomes orange-red color. Can persistently stain soft contact lenses.

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 prescription of glucocorticosteroids is possible.

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. When there are signs of toxic hepatitis the drug is canceled.

Effect on the ability to drive transp. cf. and fur:The drug can cause headaches and reduced visual acuity, caution is required when managing transport, when working with mechanisms.

Form release / dosage:

10 capsules are placed in a contour mesh package made of a polyvinylchloride film and a flexible package based on aluminum foil for medicinal preparations.

For 10, 20, 30, 50, 100 capsules are placed in cans of polymeric with screw caps.

The bank or 1, 2, 3, 5, 10 contour cell packs together with the instruction for use are placed in a pack of cardboard. Packing for hospitals.

50, 100, 150, 200, 300, 500 contour mesh packages together with an equal number of instructions for use are placed in a box of corrugated cardboard.

For 100, 500, 1000 capsules are placed in cans of polymeric with screw caps. For 4, 6, 10, 12 cans, together with an equal number of instructions for use, are placed in a box of corrugated cardboard.

Packaging:Capsules 150 mg.

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

Shelf life:

4 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-002348

Date of registration:15.01.2014

Date of cancellation:2019-01-15

The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia

Manufacturer: & nbsp

BRYNTSALOV-A, CJSC Russia

Information update date: & nbsp13.05.2016

Illustrated instructions

Instructions

Rifampicin-Ferein® (Rifampicin-Ferein®)