**** *PHARMASINTEZ JSC* IPCA Laboratories AKRIKHIN / BIOPHARM M.J. Akrikhin KhFK JSC BELMEDPREPARATY, RUE Biokhimik, JSC BRYNTSALOV BRYNTSALOV-A, JSC Ipka Laboratories Limited/Akrikhin JSC Moskhimfarmpreparaty FSUE im. Semashko Sintez AKO JSC Pharmasintez JSC Pharmsintez, PJSC FEREIN SHCHELKOVSKY VITAMIN PLANT

Country of origin

India Republic of Belarus Russia

Product group

Antibacterial drugs

Semi-synthetic broad-spectrum antibiotic of the rifamycin group

Release forms

• 10 - contour cell packaging (1) - cardboard packs. 10 - contour cell packaging (2) - cardboard packs. 20 - dark glass jars (1) - cardboard packs. 10 - contour blister packs 150 mg - ampoules (10) - cardboard packs. Capsules 150 mg in blister pack No. 10x10

Description of the dosage form

• Capsules Lyophilisate for the preparation of solution for injections Lyophilisate for the preparation of solution for injections of brick or red-brown color.

pharmachologic effect

Rifampicin is a semisynthetic antibiotic with a broad spectrum of antimicrobial action from the group of rifamycins (ansamycins). Acts bactericidal. It disrupts RNA synthesis in bacterial cells by inhibiting DNA-dependent RNA polymerase. Highly active against Mycobacterium tuberculosis, it is a first-line anti-tuberculosis agent. Active against gram-positive bacteria (Staphylococcus spp, including multidrug-resistant strains), Streptococcus spp., Bacillus anthracis, Clostridium spp.) and some gram-negative bacteria (Neisseria meningitidis, N.gonorrhoeae, Haemophilus influenzae, Brucella spp., Legionella pneumophila). Active against Chlamydia trachomatis, Rickettsia prowazekii, Mycobacterium leprae. Does not affect mushrooms. Rifampicin has a virucidal effect on the rabies virus and suppresses the development of rabies encephalitis. Resistance to rifampicin develops rapidly. No cross-resistance with other antibacterial drugs (except for other rifamycins) has been identified.

Pharmacokinetics

Rifampin is quickly and completely absorbed from the gastrointestinal tract. Bioavailability reaches 90-95%. The maximum concentration of rifampicin in blood plasma is achieved 2-2.5 hours after oral administration. Rifampicin is found in therapeutic concentrations in pleural exudate, sputum, cavity contents, and bone tissue; the highest concentration is created in the liver and kidneys. Plasma protein binding is 80-90%. Rifampin penetrates the blood-brain barrier, the placenta, and is found in breast milk. Biotransformed in the liver. The half-life is 2-5 hours. At a therapeutic level, the concentration of the drug is maintained for 8-12 hours after administration, for highly sensitive pathogens - within 24 hours. It is excreted from the body with bile, feces and urine.

Special conditions

Monotherapy for tuberculosis with rifampicin is often accompanied by the development of pathogen resistance to the antibiotic, so it should be combined with other antituberculosis drugs. When treating non-tuberculosis infections, rapid development of microbial resistance is possible; this process can be prevented by combining rifampicin with other chemotherapeutic agents. The drug is not indicated for intermittent therapy. The administration of the drug may be accompanied by staining of urine, feces, saliva, sweat, tear fluid, and contact lenses red. Treatment with rifampicin should be carried out under close medical supervision. Treatment with the drug should begin after testing liver function (determining the level of bilirubin and aminotransferases in the blood, thymol test), and during treatment it should be carried out monthly. In case of increasing signs of liver dysfunction, the use of the drug should be discontinued. With long-term use of the drug, it is necessary to monitor the blood count due to the possibility of developing leukopenia. Overdose Symptoms: nausea, vomiting, diarrhea, drowsiness, liver enlargement, jaundice, increased levels of bilirubin, hepatic transaminases in the blood plasma; brownish-red or orange coloration of the skin, urine, saliva, sweat, tears and feces in proportion to the dose of the drug taken. Treatment: stop taking the drug. Gastric lavage. Symptomatic therapy (there is no specific antidote). Maintaining vital functions.

Compound

• 1 amp. rifampicin 150 mg 1 amp. rifampicin 150 mg, excipients: ascorbic acid, sodium sulfite, sodium hydroxide. 1 capsule contains 150 mg of rifampicin.

Rifampicin indications for use

• Rifampicin is used for tuberculosis (including tuberculous meningitis), as part of combination therapy; for infectious and inflammatory diseases caused by pathogens sensitive to the drug (including osteomyelitis, pneumonia, pyelonephritis, leprosy, gonorrhea, otitis, cholecystitis, etc.), as well as for meningococcal carriage. Due to the rapid development of antibiotic resistance during treatment, the use of rifampicin for diseases of non-tuberculosis etiology is limited to cases that are not amenable to treatment with other antibiotics.

Rifampicin contraindications

• Jaundice, recent (less than 1 year) infectious hepatitis, severe renal impairment, hypersensitivity to rifampicin or other rifamycins

Rifampicin dosage

• 0.15 g 150 mg

Rifampicin side effects

• When treated with rifampicin, disorders of the gastrointestinal tract function (decreased appetite, nausea, vomiting, diarrhea) are possible. These phenomena usually go away on their own after 2-3 days without stopping the drug. Rifampicin may have a hepatotoxic effect (increased levels of transaminases and bilirubin in the blood serum, jaundice). For timely detection and prevention of hepatotoxicity, treatment with rifampicin should begin after testing liver function (determining the level of bilirubin and aminotransferases in the blood, thymol test), and during treatment it should be carried out monthly. In patients who have had hepatitis in the past or suffer from liver cirrhosis, these studies should be performed every 2 weeks. Moderate liver dysfunction is usually transient and can disappear without discontinuation of the drug when prescribing allochol, methionine, pyridoxine, vitamin B, etc. If signs of liver dysfunction worsen, the use of rifampicin should be discontinued. When treated with rifampicin, the development of leukopenia and thrombocytopenia and allergic reactions is possible. The latter manifest themselves in the form of skin rashes, eosinophilia, and rarely - bronchospasm and Quincke's edema. With intermittent treatment, irregular use of the drug, or when resuming treatment with rifampicin after a break, severe allergic reactions in the form of hipposis-like fever, acute renal failure or thrombopenic purpura may occur. These complications are sometimes preceded by signs of drug sensitization (a rise in temperature after taking the drug, increasing eosinophilia, bronchospasm, as well as positive Shelley, Wannier tests, etc.). To prevent these phenomena, the drug should be prescribed in small doses (0.15 g per day). In cases where at the previous stage of treatment there were signs of sensitization to rifampicin, it is used under the control of temperature measurement after taking the drug (within 3 hours in the first 2-3 days). If well tolerated, the dose of the antibiotic can be increased to the usual therapeutic dose. If allergic reactions occur, rifampin is discontinued and desensitizing therapy is carried out (antihistamines, calcium supplements, corticosteroid hormones, etc.). In cases of severe allergic reactions, large doses of corticosteroid hormones, antihistamines, intravenous hemodez, isotonic sodium chloride solution, diuretics, etc. should be administered parenterally. In patients taking the drug, urine, tear fluid, and sputum acquire an orange-red color. With rapid intravenous administration of rifampicin in patients, a decrease in blood pressure is possible, as a result of which the intravenous infusion of the drug should be carried out under the control of blood pressure during drug administration. With prolonged intravenous administration, phlebitis may develop.

Drug interactions

Rifampicin is a strong cytochrome P-450 inducer and may cause potentially dangerous drug interactions. Rifampicin accelerates the metabolism (the concentration in the blood plasma decreases and the effect decreases accordingly) of theophylline, thyroxine, corticosteroids, carbamazepine, phenytoin, oral anticoagulants, oral hypoglycemic drugs, dapsone, some tricyclic antidepressants, chloramphenicol, fluconazole, ketoconazole, terbinafine, haloperidol, diazepam, bisoprolo la , propranolol, diltiazem, nifedipine, verapamil, cardiac glycosides, quinidine, disopyramide, propafenone, cyclosporine. Avoid combined use with HIV protease inhibitors (indinavir, nelfinavir). Rifampicin accelerates the metabolism of estrogens and gestagens (the contraceptive effect of oral contraceptives is reduced). Ketoconazole may reduce plasma concentrations of rifampicin.

Storage conditions

• store in a dry place
• keep away from children
• store in a place protected from light

Information provided

Catad_pgroup Antimicrobial (different groups)

Rifampicin-Ferein - instructions for use

Registration number:

LP-002348

Tradename:

Rifampicin-Ferein ®

International nonproprietary name:

rifampicin

Dosage form:

capsules

Compound:

1 capsule contains:
Active substance: rifampicin (calculated as 100% substance) - 150 mg.
Excipients: calcium stearate - 0.9 mg, magnesium hydroxycarbonate hydrate - 15 mg, sodium carboxymethyl starch - 15 mg, lactose monohydrate - up to the weight of the capsule contents 300 mg.

Composition of the capsule.
Frame: titanium dioxide - 2%, azorubine - 0.0328%. sunset yellow - 0.2190%. gelatin up to 100%.
Cap: titanium dioxide - 2%, azorubine - 0.0328%. sunset yellow - 0.2190%, gelatin up to 100%.

Description

Hard gelatin capsules No. 1. The body and cap of the capsules are orange. The contents of the capsules are red-brown powder, possibly containing white inclusions.

Pharmacotherapeutic group:

antibiotic-rifamycin.

ATX code:

J04AB02

Pharmacological properties

Pharmacodynamics

Semi-synthetic antibiotic with a wide spectrum of action, first-line anti-tuberculosis drug. In low concentrations, it has a bactericidal effect on Mycobacterium tuberculosis, Brucella spp., Chlamydia trachomatis, Legionella pneumophila, Rickettsia typhi, Mycobacterium leprae; in high concentrations - against some gram-negative microorganisms. Characterized by high activity against Staphylococcus spp. (including penicillinase-forming and many methicillin-resistant strains), Streptococcus spp., Clostridium spp., Bacillus anthracis; gram-negative cocci: Neisseria meningitidis, Neisseria gonorrhoeae. Ha gram-positive bacteria acts in high concentrations. Active against intracellular and extracellular microorganisms. Suppresses DNA-dependent RNA polymerase of microorganisms. With rifampicin monotherapy, selection of rifampicin-resistant bacteria is observed relatively quickly. Cross-resistance with other antibiotics (with the exception of other rifamycins) does not develop.

Pharmacokinetics
Absorption is rapid; food intake reduces absorption of the drug. When taken orally on an empty stomach, 600 mg maximum concentration is 10 mcg/ml. The time to reach maximum concentration is 2-3 hours. Communication with plasma proteins is 84-91%.

It is quickly distributed throughout organs and tissues (the highest concentration in the liver and kidneys), penetrates bone tissue, the concentration in saliva is 20% of the plasma concentration. The apparent volume of distribution is 1.6 l/kg in adults and 1.1 l/kg in children.

It penetrates the blood-brain barrier only in case of inflammation of the meninges. Penetrates through the placenta (concentration in fetal plasma is 33% of the concentration in maternal plasma) and is excreted in breast milk (breastfed children receive no more than 1% of the therapeutic dose of the drug).

Metabolized in the liver to form the pharmacologically active metabolite -25-O-deacetylrifampicin. It is an autoinducer - it accelerates its metabolism in the liver, resulting in systemic clearance of 6 l/h after taking the first dose, increasing to 9 l/h after repeated dosing. When taken orally, induction of intestinal wall enzymes is also likely.

The half-life after oral administration of 300 mg is 2.5 hours, 600 mg is 3-4 hours, 900 mg is 5 hours. After a few days of repeated administration, bioavailability decreases and the half-life after repeated administration of 600 mg is shortened to 1-2 hours.

Excreted mainly in bile, 80% - in the form of a metabolite; kidneys - 20%. After taking 150-900 mg of the drug, the amount of rifampicin excreted unchanged by the kidneys depends on the dose taken and ranges from 4 to 20%.

In patients with impaired renal excretory function, the half-life is prolonged only when doses exceed 600 mg. It is excreted during peritoneal dialysis and hemodialysis. In patients with impaired liver function, an increase in plasma concentrations of rifampicin and a prolongation of the half-life are observed.

Indications for use:

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 as part of combination antimicrobial therapy; after excluding the diagnosis of tuberculosis and leprosy).

Brucellosis - as part of combination therapy with a tetracycline antibiotic (doxycycline).

Meningococcal meningitis (prevention for persons who have been in close contact with patients with meningococcal meningitis; for carriers of Neisseria meningitidis bacilli).

Contraindications:

Hypersensitivity to rifampicin and/or other components of the drug, jaundice, recent (less than 1 year) infectious hepatitis, chronic renal failure, pulmonary heart failure of II-III degree, lactose intolerance, lactase deficiency, Glucose-galactose malabsorption, children under 3 years old, lactation period. Concomitant use with ritonavir, saquinavir, atazanavir, darunavir, fosamprenavir, tipranovir is contraindicated.

Carefully: porphyria.

Use during pregnancy and breastfeeding

Therapy during pregnancy (especially in the first trimester) is possible only for “vital” indications. When prescribed in the last weeks of pregnancy, postpartum bleeding in the mother and bleeding in the newborn may occur. In this case, vitamin K is prescribed.

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

Directions for use and doses

Take orally on an empty stomach (0.5-1 hour before meals).

When treating tuberculosis, the average daily dose 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 of age is 10 mg/kg (but not more than 450 mg per day) 1 time per day. If rifampicin is poorly tolerated, the daily dose can be divided into 2 doses.

Monotherapy for tuberculosis with rifampicin is often accompanied by the development of pathogen resistance to the antibiotic, so it should be prescribed in combination with other antituberculosis drugs (streptomycin, isoniazid, ethambutol, etc.), to which the sensitivity of Mycobacterium tuberculosis is preserved.

For leprosy, rifampicin is used according to the following regimens:

a) a daily dose of 300-450 mg is administered in 1 dose; in case of poor tolerance - in 2 doses. Duration of treatment is 3-6 months. The courses are repeated with an interval of 1 month;
b) against the background of combination therapy, a daily dose of 450 mg is prescribed in 2-3 doses over 2-3 weeks with an interval 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 combination with immunostimulating agents.

For the treatment of multibacillary types of leprosy (lepromatous and borderline) for adults - 600 mg once a month in combination with dapsone (100 mg once a day). The minimum duration of treatment is 2 years.

For the treatment of pausibacillary types of leprosy (tuberculoid and borderline tuberculoid) for 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 as part of combination antimicrobial therapy; after excluding the diagnosis of tuberculosis and leprosy), it is prescribed in combination with other antimicrobial agents. Daily dose 600-1200 mg, for children over 3 years old 10-20 mg/kg. The frequency of administration is 2 times a day.

For the 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 doses for adults 600 mg. for children over 3 years old 10 mg/kg.

Side effect

From the digestive system: nausea, vomiting, diarrhea, loss of appetite, erosive gastritis, pseudomembranous colitis; increased activity of “liver” 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: nephronecosis, interstitial nephritis.

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

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

If taken irregularly or when treatment is resumed after a break, flu-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 instructions worsen, or any other side effects not listed in the instructions are noted, you should immediately inform your doctor.

Overdose

Symptoms: nausea, vomiting, abdominal pain, liver enlargement, jaundice, periorbital edema or swelling of the linden, “red man syndrome” (red-orange coloring of the skin, mucous membranes and sclera), pulmonary edema, lethargy, confusion, convulsions.

Treatment: symptomatic; gastric lavage, taking activated carbon; forced diuresis.

Interaction with other drugs

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

Co-trimoxazole (sulfamethoxazole + trimethoprim) increases the concentration of rifampicin in the blood. With simultaneous use of rifampcin (600 mg/day), ritonavir (100 mg 2 times a day) and saquinavir (1000 mg), severe hepatotoxicity may develop. When used together, 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 some tricyclic antidepressants, lipid-lowering drugs (simvastatin, etc.), antimalarial drugs (mefloquine, etc.), cytostatics (tamoxifen, etc.).

Antacids, narcotic analgesics, anticholinergic drugs and ketoconazole reduce (if taken orally) the bioavailability of rifampicin.

Isoniazid and/or pyrazinamide increase the incidence and severity of liver dysfunction to a greater extent than rifampicin alone in patients with pre-existing liver disease.

Sodium para-aminosalicylate preparations should be prescribed no earlier than 4 hours after taking the drug, because Possible malabsorption

special instructions

During pregnancy, the drug is prescribed only for “vital” indications.

Women of childbearing age should use reliable methods of contraception (oral hormonal contraceptives and additional non-hormonal methods of contraception) during treatment. A false-positive result is possible with the immunological determination of opiates in urine. It should be taken into account that rifampicin interacts with contrast agents used in cholecystography. Under its influence, the results of X-ray studies may be distorted.

During treatment, the skin, sputum, sweat, feces, tear fluid, and urine become orange-red in color. Can permanently stain soft contact lenses.

To prevent the development of resistance of microorganisms, it must be used in combination with other antimicrobial drugs.

In the event of the development of influenza-like syndrome, uncomplicated by thrombocytopenia, hemolytic anemia, bronchospasm, shortness of breath, shock and renal failure, in patients receiving the drug on an intermittent regimen, the possibility of switching to daily dosing should be considered. In these cases, the dose is increased slowly: 75-150 mg is prescribed on the first day, and the desired therapeutic dose is reached in 3-4 days. If the above serious complications are noted, rifampicin is discontinued. Renal function must be monitored; additional administration of glucocorticosteroids is possible.

In the case of prophylactic use in meningococcal bacilli carriers, strict monitoring of patients is necessary in order to promptly identify symptoms of the disease in the event of resistance to rifamnicin.

With long-term use, systematic monitoring of peripheral blood patterns and liver function is indicated. During the treatment period, microbiological methods for determining the concentration of folic acid and vitamin B12 in blood serum should not be used. If signs of toxic hepatitis appear, the drug is discontinued.

Information about the possible effect of a medicinal product for medical use on the ability to drive vehicles and machinery
The drug may cause headaches and decreased visual acuity; caution is required when driving or operating machinery.

Release form:

Capsules 150 mg.
10 capsules are placed in a blister pack made of polyvinyl chloride film and flexible packaging based on aluminum foil for medicines.

10, 20, 30, 50, 100 capsules are placed in polymer jars with screw caps.

A jar or 1, 2, 3, 5, 10 blister packs along with instructions for use are placed in a cardboard pack.

Packaging for hospitals.
50, 100, 150, 200, 300, 500 blister packs along with an equal number of instructions for use are placed in a corrugated cardboard box,

100, 500, 1000 capsules are placed in polymer jars with screw caps.

4, 6, 10, 12 cans, along with an equal number of instructions for use, are placed in a corrugated cardboard box.

Best before date

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

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C.
Keep out of the reach of children.

Conditions for dispensing from pharmacies:

By doctor's prescription.

Name, address of the manufacturer of the medicinal product and address of the place of production of the medicinal product

JSC "Bryntsalov-A"
Legal address: Russia. 117105. Moscow, st. Nagatinskaya, 1
Production address: Russia, 142530, Moscow region, Elektrogorsk. Mechnikova proezd, 1

Semi-synthetic broad-spectrum antibiotic of the rifamycin group.
Active substance of the drug: RIFAMPICIN / RIFAMPICIN

Pharmacological action Rifampicin / rifampicin

Semi-synthetic broad-spectrum antibiotic of the rifamycin group. Has a bactericidal effect. Suppresses bacterial RNA synthesis by inhibiting the DNA-dependent RNA polymerase of the pathogen.
Highly active against Mycobacterium tuberculosis, it is a first-line anti-tuberculosis drug.
Active against gram-positive bacteria: Staphylococcus spp. (including multidrug-resistant), Streptococcus spp., Bacillus anthracis, Clostridium spp., as well as against some gram-negative bacteria: Neisseria meningitidis, Haemophilus influenzae, Brucella spp., Legionella pneumophila.
Active against Rickettsia prowazekii, Mycobacterium leprae, Chlamydia trachomatis.
Resistance to rifampicin develops rapidly. Cross-resistance to other anti-tuberculosis drugs (with the exception of other rifamycins) was not observed.

Pharmacokinetics of the drug.

After oral administration, it is well absorbed from the gastrointestinal tract. Distributed in most tissues and body fluids. Penetrates through the placental barrier. Plasma protein binding is high (89%). Metabolized in the liver. T1/2 is 3-5 hours. It is excreted in bile, feces and urine.

Indications for use:

Tuberculosis (including tuberculous meningitis) as part of combination therapy. MAS infection. Infectious and inflammatory diseases caused by pathogens sensitive to rifampicin (including osteomyelitis, pneumonia, pyelonephritis, leprosy; meningococcal carriage).

Dosage and method of administration of the drug.

When taken orally for adults and children - 10 mg/kg 1 time/day or 15 mg/kg 2-3 times a week. Take on an empty stomach, the duration of treatment is determined individually.
IV for adults - 600 mg 1 time/day or 10 mg/kg 2-3 times a week, for children - 10-20 mg/kg 1 time/day or 2-3 times a week.
It is possible to administer 125-250 mg to the pathological focus (by inhalation, intracavitary administration, as well as injection into the focus of the skin lesion).
Maximum doses: when taken orally for adults, the daily dose is 1.2 g, for children 600 mg, when administered intravenously for adults and children - 600 mg.

Side effects of Rifampicin / rifampicin:

From the digestive system: nausea, vomiting, diarrhea, loss of appetite; increased levels of liver transaminases, bilirubin in the blood plasma, pseudomembranous colitis, hepatitis.
Allergic reactions: urticaria, eosinophilia, Quincke's edema, bronchospasm, influenza-like syndrome.
From the hematopoietic system: rarely - thrombocytopenia, thrombocytopenic purpura, eosinophilia, leukopenia, hemolytic anemia.
From the central nervous system: headache, ataxia, blurred vision.
From the urinary system: necrosis of the kidney tubules, interstitial nephritis, acute renal failure.
From the endocrine system: menstrual irregularities.
Other: red-brown coloring of urine, feces, saliva, sputum, sweat, tears.

Contraindications to the drug:

Jaundice, recent (less than 1 year) infectious hepatitis, severe renal dysfunction, hypersensitivity to rifampicin or other rifamycins.

Use during pregnancy and lactation.

If it is necessary to use rifampicin during pregnancy, the expected benefit of therapy for the mother and the potential risk to the fetus should be assessed.
It should be borne in mind that the use of rifampicin in the last weeks of pregnancy increases the risk of bleeding in newborns and mothers in the postpartum period.
Rifampin is excreted in breast milk. If necessary, use during lactation should stop breastfeeding.

Special instructions for use of Rifampicin / rifampicin.

Use with caution for liver diseases and exhaustion. When treating non-tuberculosis infections, rapid development of microbial resistance is possible; this process can be prevented by combining rifampicin with other chemotherapeutic agents. Rifampicin is better tolerated when taken daily than when taken intermittently. If it is necessary to resume treatment with rifampicin after a break, then you should start with a dose of 75 mg/day, gradually increasing it by 75 mg/day until the desired dose is reached. In this case, renal function should be monitored; additional administration of GCS is possible.
With long-term use of rifampicin, systematic monitoring of blood counts and liver function is indicated; You cannot use a test with a load of bromsulfalein, since rifampicin competitively inhibits its excretion.
PAS preparations containing bentonite (hydrosilicate of aluminum) should be prescribed no earlier than 4 hours after taking rifampicin.
In newborns and premature infants, rifampicin is used only when absolutely necessary.

Interaction of Rifampicin / rifampicin with other drugs.

Due to the induction of microsomal liver enzymes (CYP2C9, CYP3A4 isoenzymes), rifampicin accelerates the metabolism of theophylline, oral anticoagulants, oral hypoglycemic drugs, hormonal contraceptives, digitalis drugs, verapamil, phenytoin, quinidine, corticosteroids, chloramphenicol, antifungal drugs, which leads to a decrease in their plasma concentrations blood and, accordingly, to a decrease in their effect.

Rifampicin

International nonproprietary name

Rifampicin

Dosage form

Capsules, 150 mg

Compound

One capsule contains

active substance- rifampicin 150 mg,

Excipients: lactose monohydrate, petroleum jelly (liquid paraffin), potato starch, sodium lauryl sulfate, anhydrous colloidal silicon dioxide (Aerosil), talc, magnesium stearate,

capsule shell composition: gelatin, titanium dioxide (E 171), acid red 2C (E 122).

Description

Hard gelatin capsules with a red body and cap.

The contents of the capsules are red-brown or brick-red powder or granules.

Pharmacotherapeutic group

Anti-tuberculosis drugs. Antibacterial drugs. Rifampicin.

ATX code J04AB02

Pharmacological properties

Pharmacokinetics

Rifampicin is well absorbed from the gastrointestinal tract. When taken, the maximum concentration of the drug in plasma is achieved after 2-4 hours and remains at a detectable level for up to 8 hours. However, in the blood and tissues, effective concentrations can persist for 12-24 hours. Plasma protein binding is 80-90%. The half-life is 2-5 hours. Rifampicin is metabolized in the liver. Rifampicin penetrates well into tissues and body fluids and is found in therapeutic concentrations in pleural exudate, sputum, cavity contents, and bone tissue. Passes through the blood-brain barrier (BBB) ​​only in the case of inflammation of the brain fluid in concentrations of 10-40% of those in the blood plasma. Metabolized in the liver to the pharmacologically active 25-O-diacetylrifampicin and inactive metabolites (rifampinquinone, diacetylrifampinquinone and 3-formylrifampin). The highest concentration of the drug is created in the tissues of the liver and kidneys. With increasing dose, the proportion of renal excretion increases. Small amounts of rifampicin are excreted in tears, sweat, saliva, sputum, and other fluids, turning them orange-red. It is excreted from the body with bile and urine.

Pharmacodynamics

Rifampicin is a semisynthetic broad-spectrum antibiotic from the rifampicin group. It disrupts RNA synthesis in a bacterial cell: it binds to the beta subunit of DNA-dependent RNA polymerase, preventing it from joining DNA, and inhibits RNA transcription. Has no effect on human RNA polymerase. Effective against extra- and intracellular pathogens.

It has a bacteriostatic and, in high concentrations, a bactericidal effect. Highly active against M. tuberculosis, it is a first-line anti-tuberculosis drug. Active against Escherichia coli, Pseudomonas, indole-positive and indole-negative Proteus, Klebsiella, Staphylococcus aureus, Coagulase-negative staphylococci, Neisseria meningitides, Haemophilus influenzae, Legionella species, M.tuberculosis, M.kansasii, M.scrofulaceum, M. intracellulare and M. avium.

Indications for use

Tuberculosis of the lungs and other organs (all forms) as part of complex therapy.

Directions for use and doses

Rifampin is taken orally on an empty stomach (1/2-1 hour before meals).

When treating tuberculosis, adults weighing less than 50 kg - 0.45 g, 50 kg and more - 0.60 g 1 time per day every day or 3 times a week.

The maximum daily dose should not exceed 750 mg.

With insufficient liver function the daily dose should not exceed 8 mg/kg.

Use in elderly patients: In elderly patients, renal excretion of rifampicin decreases in proportion to the decline in physiological renal function, but due to a compensatory increase in liver excretion, the half-life of the drug is the same as in younger patients. However, caution should be exercised when using the drug in such patients, especially if there is evidence of liver dysfunction.

The duration of the course is 6-9-12 months or more. The duration of treatment is determined individually. If rifampicin is poorly tolerated, the daily dose can be divided into 2 doses.

Side effects

loss of appetite, heartburn, nausea, flatulence, epigastric pain, constipation

headache, dizziness, fatigue, drowsiness

visual impairment

increased levels of liver transaminases and bilirubin in the blood

pain in the limbs, fever, chills, flushing, itching, rash

vomiting, erosive gastritis, intestinal colic, diarrhea

ataxia, disorientation, psychosis, depression, muscle weakness, myopathy

oral candidiasis, hepatitis, jaundice, pancreatic lesions, pseudomembranous colitis

exacerbation of gout, increase in serum uric acid,

dysuria, hematuria, renal dysfunction, interstitial nephritis, acute renal failure, renal tubular necrosis

hemolytic anemia, leukopenia, agranulocytosis, eosinophilia

menstrual irregularities

urticaria, Quincke's edema, bronchospasm, anaphylactic shock, exfoliative dermatitis, pemphigoid reactions, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome, vasculitis

influenza-like syndrome (with intermittent or irregular therapy), shortness of breath, wheezing, decreased blood pressure

Thrombocytopenia (with or without purpura) usually occurs with intermittent therapy. Possible fatal cerebral hemorrhage if treatment with rifampicin is continued after the onset of purpura

cases of intravascular coagulation

Very rarely:

If serious complications occur, such as renal failure, thrombocytopenia, hemolytic anemia and other serious adverse reactions, the drug should be discontinued.

Contraindications

hypersensitivity to the components of the drug

visual impairment (diabetic retinopathy, optic nerve damage)

epilepsy, tendency to seizures

history of poliomyelitis

history of infectious hepatitis, jaundice

thrombophlebitis

severe atherosclerosis

liver dysfunction

renal dysfunction

pregnancy, lactation period

children and teenagers up to 18 years of age

simultaneous use with saquinavir/ritonavir drugs

Drug interactions

Rifampin, being a strong inducer of cytochrome P-450, can cause potentially dangerous drug interactions.

Reduces the activity of indirect anticoagulants, corticosteroids, oral hypoglycemic agents, digitalis drugs, antiarrhythmic drugs (including disopyramide, quinidine, mexiletine), antiepileptic drugs, dapsone, methadone, hydantoins (phenytoin), hexobarbital, nortriptyline, haloperidol, benzodiazepines, drugs sex hormones, incl. oral contraceptives, thyroxine, theophylline, chloramphenicol, doxycycline, ketoconazole, itraconazole, terbinafine, cyclosporine A, azathioprine, beta-blockers, CCBs, fluvastatin, enalapril, cimetidine (due to the induction of microsomal liver enzymes and acceleration of the metabolism of these drugs). Should not be taken simultaneously with indinavir sulfate and nelfinavir, because their plasma concentrations are significantly reduced due to accelerated metabolism. Antacids, when taken simultaneously, interfere with the absorption of rifampicin. When taken simultaneously with opiates, anticholinergics and ketoconazole, the bioavailability of rifampicin decreases; probenecid and co-trimoxazole increase its concentration in the blood. Concomitant use with isoniazid or pyrazinamide increases the incidence and severity of liver dysfunction (due to liver disease) and the likelihood of developing neutropenia.

Para-aminosalicylic acid preparations containing bentonite (hydrosilicate of aluminum) should be prescribed no earlier than 4 hours after taking rifampicin. Rifampicin helps reduce the activity of antidiabetic drugs. Rifampin alters the elimination parameters of bromsulfalein. It should also be taken into account that rifampicin interacts with contrast agents used in cholecystography. Under its influence, the results of radiographic studies may be distorted.

During treatment you should not use:

Test with a load of bromsulfalein, since rifampicin competitively disrupts its excretion;

Microbiological methods for determining the concentration of folic acid and vitamin B 12 in blood serum;

Immunological methods, KIMS method when conducting screening tests for opiates.

Taking the drug can enhance the metabolism of endogenous substrates, including adrenal hormones, thyroid hormones and vitamin D.

When drinking alcohol during treatment and when used in patients with a history of alcoholism, the risk of hepatotoxicity increases.

special instructions

Treatment with rifampicin should be carried out under close medical supervision.

Monotherapy for tuberculosis with rifampicin is often accompanied by the development of pathogen resistance to the antibiotic, so it should be combined with other antituberculosis drugs.

Continuous administration of rifampicin is better tolerated than intermittent administration (2-3 times a week). With the development of thrombocytopenia, purpura, hemolytic anemia, renal failure and other serious adverse reactions, the administration of rifampicin is stopped. Liver function should be checked before starting treatment. In adults: The following parameters should be checked: liver enzymes, bilirubin, creatinine, complete blood count and platelet count. During long-term treatment, systematic monitoring of liver function is necessary (at least once a month). In patients with impaired liver function, the drug should be taken only when necessary and under close medical supervision. In such individuals, it is necessary to adjust the dose of the drug and monitor liver function, especially alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Studies should be carried out before starting therapy, weekly for 2 weeks, then every 2 weeks for the next 6 weeks. If signs of liver dysfunction appear, the drug should be discontinued. Other anti-tuberculosis drugs should be considered after consulting a specialist. If rifampicin is reintroduced after normalization of liver function, liver function should be monitored daily. In patients with impaired liver function, in elderly patients, in debilitated patients, caution should be exercised when used simultaneously with isoniazid (the risk of hepatotoxicity increases).

In some patients, hyperbilirubinemia may occur in the first days of treatment. A moderate increase in bilirubin and/or transaminase levels is not an indication for interruption of treatment. It is necessary to dynamically monitor liver function and the clinical condition of the patient.

Because of the possibility of an immunological reaction, including anaphylactic shock, occurring in connection with intermittent therapy, patients should be closely monitored and advised of the dangers of intermittent treatment.

The drug is prescribed with extreme caution to elderly and debilitated patients. During long-term treatment, systematic monitoring of liver function (at least once a month), peripheral blood pictures, and observation by an ophthalmologist are indicated. Alternative methods of analysis need to be considered. Rifampicin stains the skin, sputum, sweat, feces, tears, urine, and soft contact lenses orange-red.

The drug "Rifampicin", capsules, 150 mg, contains lactose. Patients with rare hereditary diseases such as galactose intolerance, Lapp lactose deficiency or glucose-galactose malabsorption should not use this drug.

Pregnancy and lactation period

Women of childbearing age need reliable contraception (including non-hormonal) during treatment.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms.

During the treatment period, you should avoid driving vehicles and other activities that require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: nausea, vomiting, abdominal pain, liver enlargement, jaundice, increased levels of bilirubin and liver transaminases in the blood plasma, pulmonary edema, blurred consciousness, convulsions, mental disorders, lethargy, arterial hypotension, sinus tachycardia, ventricular arrhythmia, “red man syndrome” (red-orange coloration of the skin, mucous membranes and sclera).

Treatment: drug withdrawal, gastric lavage and administration of activated charcoal, symptomatic therapy, in severe cases - forced diuresis, hemodialysis. There is no specific antidote.

Release form and packaging

10 capsules are placed in a blister pack made of polyvinyl chloride film or similar imported film and printed varnished aluminum foil or similar imported one.

Primary packaging, together with the appropriate number of instructions for medical use in the state and Russian languages, is placed in a box made of corrugated cardboard.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C.

Keep out of the reach of children!

Shelf life

Do not use after expiration date.

Conditions for dispensing from pharmacies

On prescription

Manufacturer

Packer

Pavlodar Pharmaceutical Plant LLP.

Kazakhstan, Pavlodar, 140011, st. Kamzina, 33.

Registration Certificate Holder

Pavlodar Pharmaceutical Plant LLP, Kazakhstan

Address of the organization that accepts claims from consumers regarding the quality of products (goods) on the territory of the Republic of Kazakhstan)

Name:

Rifampicin

Pharmacological
action:

Rifampiin is broad spectrum antibiotic.
It is active against mycobacteria tuberculosis and leprosy, acts on gram-positive (especially staphylococci) and gram-negative (meningococci, gonococci) cocci, and is less active against gram-negative bacteria.
Rifampin is well absorbed from the gastrointestinal tract.
The maximum concentration in the blood is reached 2-2"/2 hours after oral administration.
With intravenous drip administration maximum concentration of rifampicin observed towards the end of the infusion.
At the therapeutic level, the concentration of the drug when administered orally and intravenously is maintained for 8-12 hours, for highly sensitive pathogens - for 24 hours. Rifampicin penetrates well into the tissues and fluids of the body and is found in therapeutic concentrations in pleural exudate (accumulating between the membranes, protein-rich fluid surrounding the lungs), sputum, the contents of caverns (cavities in the lungs formed as a result of tissue necrosis), bone tissue.
The highest concentration of the drug is created in the tissues of the liver and kidneys.
From the body excreted in bile and urine.
Resistance to rifampicin develops rapidly. Cross-resistance with other antibiotics is not observed (with the exception of rifamiin).

Indications for
application:

Tuberculosis of the lungs and other organs;
- for various forms of leprosy and inflammatory diseases of the lungs and respiratory tract: bronchitis (inflammation of the bronchi), pneumonia (pneumonia), - caused by multiresistant (resistant to most antibiotics) staphylococci;
- for osteomyelitis (inflammation of the bone marrow and adjacent bone tissue);
- infections of the urinary and biliary tract;
- acute gonorrhea and other diseases caused by pathogens sensitive to rifampicin;
- for non-tuberculosis diseases only in cases where other antibiotics are ineffective.

Rifampicin has virulocidal (accompanied by complete or partial loss of biological activity of the virus) effect on the rabies virus, suppresses the development of rabies encephalitis (inflammation of the brain caused by the rabies virus); in this regard, it is used for the complex treatment of rabies in the incubation period (the period between the moment of infection and the appearance of the first signs of the disease).

Mode of application:

Rifampiiin taken orally on an empty stomach("/2-1 hour before meals) or administered intravenously (adults only).
To prepare the solution, dilute 0.15 g of rifampicin in 2.5 ml of sterile water for injection, shake the ampoules with powder vigorously until completely dissolved, and dilute the resulting solution in 125 ml of 5% glucose solution.
Inject at a rate of 60-80 drops per minute.
When treating tuberculosis, the average daily dose for adults is 0.45 g orally once a day.
In patients (especially during an exacerbation) with a body weight above 50 kg, the daily dose can be increased to 0.6 g.
The average daily dose for children over 3 years of age is 10 mg/kg (but not more than 0.45 g per day) 1 time per day.
If rifampicin is poorly tolerated, the daily dose can be divided into 2 doses.

Intravenous rifampicin is recommended in acutely progressive and widespread forms of destructive pulmonary tuberculosis (pulmonary tuberculosis occurring with a violation of the structure of the lung tissue), severe purulent-septic processes (microbial infection of the blood with subsequent formation of ulcers in the tissues), when it is necessary to quickly create a high concentration of the drug in the blood and if taking the drug inside is difficult or poorly tolerated by the patient.
When administered intravenously, the daily dose for adults is 0.45 g, for severe rapidly progressing (developing) forms - 0.6 g and is administered in 1 dose.
The drug is administered intravenously for 1 month. or more, followed by a transition to oral administration, depending on the tolerability of the drug.
The total duration of use of rifampicin for tuberculosis is determined by the effectiveness of treatment and can reach 1 year.

When treating tuberculosis with rifampicin (intravenously) in patients with diabetes mellitus It is recommended to administer 2 units of insulin for every 4-5 g of glucose (solvent).
Monotherapy (treatment with one drug) of tuberculosis with rifampicin is often accompanied by the development of pathogen resistance to the antibiotic, so it should be combined with other antituberculosis drugs (streptomycin, isoniazid, ethambutol, etc., 770, 781), to which the sensitivity of Mycobacterium tuberculosis (the causative agent of tuberculosis) is preserved.
For leprosy, rifampicin is used according to the following regimens:: a) a daily dose of 0.3-0.45 g is administered in 1 dose: if tolerated poorly - in 2 doses.
Duration of treatment is 3-6 months, courses are repeated at intervals of 1 month; b) against the background of combination therapy, a daily dose of 0.45 g is prescribed 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 every 1 week. within 6 months.
Treatment is carried out in combination with immunostimulating (increasing the body's defenses) agents.

For non-tuberculosis infections adults take rifampicin orally at 0.45-0.9 g per day, and children - 8-10 mg/kg in 2-3 doses.
Administered intravenously to adults in a daily dose of 0.3-0.9 g (2-3 injections).
Administer over 7-10 days.
As soon as the opportunity arises, switch to taking the drug orally.
For acute gonorrhea prescribed orally at a dose of 0.9 g per day once or for 1-2 days.
For the prevention of rabies adults are given orally 0.45-0.6 g per day; for severe injuries (bite to the face, head, hands) - 0.9 g per day; children under 12 years old - 8-10 mg/kg.
The daily dose is divided into 2-3 doses.
Duration of use: 5-7 days.
Treatment is carried out simultaneously with active immunization (vaccinations).

Side effects:

From the digestive system: nausea, vomiting, diarrhea, loss of appetite; increased levels of liver transaminases, bilirubin in the blood plasma, pseudomembranous colitis, hepatitis.
Allergic reactions: urticaria, Quincke's edema, bronchospasm, influenza-like syndrome.
From the hematopoietic system: rarely - thrombocytopenia, thrombocytopenic purpura, eosinophilia, leukopenia, hemolytic anemia.
From the side of the central nervous system: headache, ataxia, blurred vision.
From the urinary system: necrosis of kidney tubules, interstitial nephritis, acute renal failure.
From the endocrine system: menstrual irregularities.
Other: red-brown coloring of urine, feces, saliva, sputum, sweat, tears.

Contraindications:

Infants;
- pregnant women;
- with jaundice;
- kidney diseases with decreased excretory function;
- for hepatitis (inflammation of liver tissue);
- with hypersensitivity to the drug.
Intravenous administration is contraindicated with pulmonary-heart failure (insufficient supply of body tissues with oxygen due to heart and lung disease) and phlebitis.

Carefully used for liver diseases and exhaustion.
When treating non-tuberculosis infections, rapid development of microbial resistance is possible; this process can be prevented by combining rifampicin with other chemotherapeutic agents.
Rifampicin is better tolerated when taken daily than when taken intermittently. If it is necessary to resume treatment with rifampicin after a break, then you should start with a dose of 75 mg/day, gradually increasing it by 75 mg/day until the desired dose is reached.
In this case, renal function should be monitored; additional administration of GCS is possible.
With long-term use of rifampicin systematic monitoring of blood patterns and liver function is indicated; You cannot use a test with a load of bromsulfalein, since rifampicin competitively inhibits its excretion.
PAS preparations containing bentonite (hydrosilicate of aluminum) should be prescribed no earlier than 4 hours after taking rifampicin.
In newborns and premature infants, rifampicin is used only when absolutely necessary.

Interaction
other medicinal
by other means:

Due to the induction of microsomal liver enzymes (CYP2C9, CYP3A4 isoenzymes), rifampicin accelerates the metabolism of theophylline, oral anticoagulants, oral hypoglycemic drugs, hormonal contraceptives, digitalis drugs, verapamil, phenytoin, quinidine, corticosteroids, chloramphenicol, antifungal drugs, which leads to a decrease in their plasma concentrations blood and, accordingly, to a decrease in their effect.

Pregnancy:

If it is necessary to use rifampicin during pregnancy, the expected benefit of therapy for the mother and the potential risk to the fetus should be assessed.
It should be borne in mind that the use of rifampicin in the last weeks of pregnancy increases the risk of bleeding in newborns and mothers in the postpartum period.
Rifampin is excreted in breast milk.
If necessary, use during lactation should stop breastfeeding.

1 ampoule of Rifampicin lyophilisate for solution for infusion (600 mg) contains:
- active ingredient: rifampicin - 600 mg;
- excipients: ascorbic acid 60 mg, sodium sulfite 12 mg, sodium hydroxide to pH 8.0-9.0.

1 capsule Rifampicin (150 mg) contains:
- active ingredient: rifampicin - 150 mg;
- excipients: lactose, potato starch, sodium lauryl sulfate, liquid paraffin, purified talc, colloidal silicon oxide, magnesium stearate.