Rifampicin for what diseases. Rifampicin lyophilized powder for solution for intravenous administration, lyophilized powder for solution for intravenous administration
pharmachologic effect
Rifampiin is a broad-spectrum antibiotic. It is active against Mycobacterium tuberculosis and leprosy, acts on gram-positive (especially staphylococci) and gram-negative (meningococci, gonococci) cocci, less active against gram-negative bacteria.Rifampiin is well absorbed from the gastrointestinal tract. The maximum concentration in the blood is reached after 2-2 "/ 2 hours after ingestion.
With intravenous drip injection the maximum concentration of rifampicin is observed towards the end of the infusion (infusion). At the therapeutic level, the concentration of the drug when taken orally and intravenously is maintained for 8-12 hours, for highly sensitive pathogens - for 24 hours. Rifampicin penetrates well into tissues and body fluids and is found at therapeutic concentrations in pleural exudate (accumulating between the membranes, surrounding the lungs, a protein-rich fluid), sputum, the contents of caverns (cavities in the lungs formed due to tissue necrosis), bone tissue. The highest concentration of the drug is created in the tissues of the liver and kidneys. It is excreted from the body with bile and urine.
Rifampicin resistance develops rapidly. Cross-resistance with other antibiotics is not observed (with the exception of rifamiin).
Indications for use
The main indication for use is tuberculosis of the lungs and other organs.In addition, the drug is used for various forms leprosy and inflammatory diseases lungs and respiratory tract: bronchitis (inflammation of the bronchi), pneumonia (pneumonia), - caused by multiresistant (resistant to most antibiotics) staphylococci; with osteomyelitis (inflammation of the bone marrow and adjacent bone tissue); urinary and biliary tract infections; acute gonorrhea and other diseases caused by pathogens sensitive to rifampicin.
Due to the rapid development of resistance in microorganisms, rifampicin is indicated for non-tuberculous diseases only when other antibiotics are ineffective.
Rifampicin has a virulocidal (accompanied by a complete or partial loss of the biological activity of the virus) effect on the rabies virus, inhibits the development of rabies encephalitis (inflammation of the brain caused by the rabies virus); For this reason, it is used for complex treatment rabies in incubation period(the period between the moment of infection and the appearance of the first signs of the disease).
Mode of application
Rifampiin is taken orally on an empty stomach (1/2-1 hour before meals) or administered intravenously by drip (adults only).To prepare the solution, dilute 0.15 g of rifampicin in 2.5 ml of sterile water for injection, vigorously shake the powder ampoules until completely dissolved, dilute the resulting solution in 125 ml of 5% glucose solution. Enter at a rate of 60-80 drops per minute.
In the treatment of tuberculosis, the average daily dose for adults inside 0.45 g 1 time per day. In patients (especially during an exacerbation) with a body weight above 50 kg, the daily dose may be increased to 0.6 g. The average daily dose for children over 3 years old is 10 mg / kg (but not more than 0.45 g per day) 1 once a day. With poor tolerance to rifampicin, the daily dose can be divided into 2 doses.
Intravenous administration of rifampicin is recommended for acutely progressive and widespread forms of destructive pulmonary tuberculosis (pulmonary tuberculosis that occurs with a violation of the structure lung tissue), severe purulent-septic processes (microbial infection of the blood with subsequent formation of abscesses in the tissues), when it is necessary to quickly create a high concentration of the drug in the blood and if the drug is difficult or poorly tolerated by the patient.
With intravenous administration, the daily dose for adults is 0.45 g, for severe rapidly progressive (developing) forms - 0.6 g and is administered in 1 dose. The drug is administered intravenously for 1 month. and more, followed by the transition to oral administration, depending on the tolerability of the drug. The total duration of the use of rifampicin in tuberculosis is determined by the effectiveness of treatment and can reach 1 year.
In the treatment of tuberculosis with rifampicin (intravenously) in patients with diabetes it is recommended to inject 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 antibiotic resistance of the pathogen, so it should be combined with other anti-tuberculosis drugs (streptomycin, isoniazid, ethambutol, etc., 770, 781), to which the sensitivity of Mycobacterium tuberculosis (pathogens of tuberculosis) is preserved. . For leprosy, rifampicin is used according to the following schemes: a) a daily dose of 0.3-0.45 g is administered in 1 dose: in case of poor tolerance - in 2 doses. The 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 0.45 g is prescribed in 2-3 doses for 2-3 weeks. with an interval of 2-3 months. within 1 year - 2 years or at the same dose 2-3 times in 1 week. within 6 months.
Treatment is carried out in a complex with immunostimulating (increasing the body's defenses) means.
For infections of a non-tuberculous nature, adults take rifampicin orally at 0.45-0.9 g per day, and children at 8-10 mg / kg in 2-3 doses. Intravenously administered to adults in a daily dose of 0.3-0.9 g (2-3 injections). Enter within 7-10 days. As soon as the opportunity arises, they switch to taking the drug inside.
In acute gonorrhea, it is 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; in case of severe injuries (bite in 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 application - 5-7 days. Treatment is carried out simultaneously with active immunization (vaccinations).
Side effects
Treatment with rifampicin should be carried out under close medical supervision. Possible allergic reactions(of varying severity), although they are observed relatively rarely; in addition, dyspeptic symptoms (digestive disorders), dysfunction (impaired function) of the liver and pancreas. With prolonged use of the drug, it is necessary to periodically examine the function of the liver and conduct blood tests (due to the possibility of developing leukopenia / a decrease in the level of leukocytes in the blood /).With rapid intravenous administration, blood pressure may decrease, and with prolonged administration, phlebitis (inflammation of the vein) may develop.
The drug reduces the activity indirect anticoagulants(drugs that inhibit blood clotting), oral hypoglycemic agents (drugs taken by mouth that lower blood sugar levels), digitalis preparations. With the simultaneous administration of anticoagulants and rifampicin, when the latter is canceled, the dose of anticoagulants should be reduced.
The drug has a bright brown-red color. It stains (especially at the beginning of treatment) urine, sputum, lacrimal fluid in an orange-reddish color.
Contraindications
Rifampicin is contraindicated in children infancy, pregnant women, with jaundice, kidney diseases with a decrease excretory function, hepatitis (inflammation of the liver tissue) and hypersensitivity to the drug. Intravenous administration is contraindicated in pulmonary heart failure (insufficient supply of oxygen to body tissues due to heart and lung disease) and phlebitis.Description of the drug Rifampicin"on this page is a simplified and expanded version official instructions by application. Before purchasing or using the drug, you should consult your doctor and read the annotation approved by the manufacturer.
Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide on the appointment of the drug, as well as determine the dose and methods of its use.
Rifampicin (rifampicin)
Composition and form of release of the drug
10 pieces. - cellular contour packings (1) - packs of cardboard.
10 pieces. - cellular contour packings (2) - packs of cardboard.
20 pcs. - jars of dark glass (1) - packs of cardboard.
10 pieces. - blister packs (150) - cardboard boxes.
pharmachologic effect
Semi-synthetic broad-spectrum antibiotic of the rifamycin group. It has a bactericidal effect. Suppresses the synthesis of bacterial RNA by inhibiting the DNA-dependent RNA polymerase of the pathogen.
It is highly active against Mycobacterium tuberculosis, is an anti-tuberculosis drug of the 1st line.
Active against gram-positive bacteria: Staphylococcus spp. (including multi-resistant ones), 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.
Rifampicin resistance develops rapidly. Cross-resistance to other anti-tuberculosis drugs (with the exception of other rifamycins) has not been noted.
Pharmacokinetics
After oral administration, it is well absorbed from the gastrointestinal tract. Distributed in most tissues and body fluids. Penetrates through the placental barrier. Protein binding is high (89%). Metabolized in the liver. T 1/2 is 3-5 hours. It is excreted in bile, feces and urine.
Indications
Tuberculosis (including tuberculosis) as part of combination therapy. MAC infection. Infectious and inflammatory diseases caused by pathogens sensitive to rifampicin (including osteomyelitis, pneumonia, pyelonephritis, leprosy; meningococcal carriage).
Contraindications
Jaundice, recent (less than 1 year) infectious hepatitis, severe renal dysfunction, hypersensitivity to rifampicin or other rifamycins.
Dosage
When administered orally to 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 set individually.
In / in adults - 600 mg 1 time / day or 10 mg / kg 2-3 times a week, children - 10-20 mg / kg 1 time / day or 2-3 times a week.
It is possible to introduce into the pathological focus (by inhalation, intracavitary administration, as well as injection into the focus of the skin lesion) at 125-250 mg.
Maximum doses: when taken orally for adults, the daily dose is 1.2 g, for children 600 mg, with intravenous administration for adults and children - 600 mg.
Side effects
From the side digestive system: nausea, vomiting, diarrhea, loss of appetite; increased levels of hepatic transaminases, bilirubin in blood plasma, pseudomembranous colitis, hepatitis.
Allergic reactions: urticaria, bronchospasm, flu-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: renal tubular necrosis, interstitial nephritis, acute.
From the side endocrine system: violation menstrual cycle.
Others: red-brown staining of urine, feces, saliva, sputum, sweat, tears.
drug interaction
Due to the induction of microsomal liver enzymes (CYP2C9, CYP3A4 isoenzymes), rifampicin accelerates the metabolism of oral anticoagulants, oral hypoglycemic drugs, hormonal contraceptives, digitalis, verapamil, phenytoin, quinidine, GCS, chloramphenicol, antifungal drugs, which leads to a decrease in their plasma concentrations and, accordingly, to reduce their effect.
special instructions
Use with caution in liver diseases, exhaustion. In the treatment of nontuberculous infections, the rapid development of resistance of microorganisms is possible; this process can be prevented if rifampicin is combined with other chemotherapeutic agents. With daily rifampicin, its tolerability is better than with intermittent treatment. If it is necessary to resume treatment with rifampicin after a break, then a dose of 75 mg / day should be started, gradually increasing it by 75 mg / day until the desired dose is reached. In this case, kidney function should be monitored; additional appointment of GCS is possible.
At long-term use rifampicin shows a systematic monitoring of the blood picture and liver function; a test with a load of bromsulfalein should not be used, since rifampicin competitively inhibits its excretion.
Preparations containing bentonite (aluminum hydrosilicate) should be prescribed no earlier than 4 hours after taking rifampicin.
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 recent weeks pregnancy increases the risk of bleeding in newborns and mothers in the postpartum period.
Rifampicin is released from breast milk. If necessary, use during lactation should stop breastfeeding.
Application in childhood
In newborns and premature babies, rifampicin is used only in cases of emergency.
For impaired renal function
Contraindicated in severe renal impairment.
For impaired liver function
Contraindicated in jaundice, recent (less than 1 year) infectious hepatitis.
Rifampicin
International non-proprietary name
Rifampicin
Dosage form
Capsules, 300 mg
Compound
One capsule contains
active substance- rifampicin 300 mg,
Excipients: lactose monohydrate, vaseline oil (liquid paraffin), potato starch, sodium lauryl sulfate, anhydrous colloidal silicon dioxide (aerosil), talc, magnesium stearate.
capsule shell: gelatin, titanium dioxide (E 171), azorubine (E 122).
Description
Hard gelatin capsules with 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 reached 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. The highest concentration of the drug is created in the tissues of the liver and kidneys. It is excreted from the body with bile and urine.
Pharmacodynamics
Rifampicin is a semi-synthetic broad-spectrum antibiotic from the rifamycin group. Inhibits the synthesis of ribonucleic acid (RNA).
It has a bacteriostatic, and in high concentrations - a bactericidal effect. Highly active against M.tuberculosis, is a first-line anti-tuberculosis drug. Active against Escherichia coli, Pseudomonas, Indole-positive and Indole-negative, Proteus, Klebsiella, Staphilococcus aureus, Coagulase-negative staphylococci, Neisseria meningitides, Haemophilus influenzae, Legionella species, M.tuberculosis, M.kansassi, M.scrofulaceum, M .intracellulare and M.avium.
Indications for use
Tuberculosis of the lungs and other organs (all forms) as part of complex therapy.
Dosage and administration
Rifampicin is taken orally on an empty stomach (1/2-1 hour before meals).
In the treatment of tuberculosis in adults: daily therapy (1 time per day) or intermittent therapy (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 decrease in physiological renal function, but due to a compensatory increase in liver excretion, the half-life of the drug is the same as in young patients. However, caution should be exercised when using the drug in such patients, especially if there is evidence of impaired liver function.
The duration of the course is 6-9-12 months or more. The duration of treatment is set individually. With poor tolerance to rifampicin, the daily dose can be divided into 2 doses.
Apply as directed by a doctor.
Side effects
skin flushing, itching, rash, urticaria, exfoliative dermatitis, pemphigoid reactions, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome, vasculitis
loss of appetite, anorexia, erosive gastritis, heartburn, nausea, vomiting, flatulence, epigastric pain, abdominal discomfort, intestinal colic, diarrhea, pseudomembranous colitis, constipation
visual impairment
hepatitis, jaundice
exacerbation of gout (increase in serum uric acid)
fatigue, drowsiness, rare cases of psychosis, depression
thrombocytopenia (with or without purpura) usually occurs with intermittent therapy. Possible fatal cerebral hemorrhage if rifampicin treatment continued after purpura appears
rare cases of intravascular coagulation, eosinophilia, leukopenia, edema, muscle weakness, myopathy, agranulocytosis, adrenal insufficiency in patients with adrenal insufficiency, dysuria
gynecomastia in patients with diabetes mellitus
rarely possible dysmenorrhea, induction of porphyria
extremely rare herpes
With intermittent treatment, development is possible:
"flu-like syndrome": fever, chills, headache, dizziness, bone pain appear most often within 3-6 months of therapy. The frequency of the syndrome varies, but this syndrome occurs in 50% of patients who received the drug once a week at a dose of 25 mg / kg or more
shortness of breath and wheezing
decline blood pressure and shock
anaphylactic shock
acute hemolytic anemia
acute renal failure caused by acute tubular necrosis or acute interstitial nephritis, hematuria
If serious complications occur, such as renal failure, thrombocytopenia and hemolytic anemia, the drug should be discontinued.
With long-term treatment with rifampicin in women, there may be cases of menstrual irregularities.
Rifampicin may cause reddish discoloration of the skin, urine, feces, sweat, sputum, and lacrimal fluid. Soft contact lenses can also be dyed.
Contraindications
hypersensitivity to the components of the drug
visual impairment (diabetic retinopathy, optic nerve)
epilepsy, prone to seizures
history of poliomyelitis
history of infectious hepatitis, jaundice
thrombophlebitis
severe atherosclerosis
liver dysfunction
kidney dysfunction
pregnancy, lactation
childhood up to 18 years old
concomitant use with saquinavir/ritonavir
Drug Interactions
Rifampicin is a strong inducer of cytochrome P-450, which can cause potentially dangerous drug interactions. Simultaneous use of rifampicin with other drugs, which are also metabolized by cytochrome P-450, can accelerate their metabolism and reduce their action. In this case, it may be necessary to adjust the dose of these drugs. Examples of drugs metabolized by cytochrome P-450:
antiarrhythmic drugs (eg, disopyramide, mexiletine, quinidine, propafenone, tocainide)
antiepileptics (eg phenytoin)
hormone antagonist (antiestrogen, eg tamoxifen, toremifene, gestinone)
antipsychotics (eg, haloperidol, aripiprazole)
anticoagulants (eg coumarins)
antifungal drugs(eg, fluconazole, itraconazole, ketoconazole, voriconazole)
antiviral drugs(eg, saquinavir, indinavir, efavirenz, amprenavir, nelfinavir, atazanavir, lopinavir, nevirapine)
barbiturates (phenobarbital)
beta blockers (eg, bisoprolol, propranolol)
anxiolytics and hypnotics (eg, diazepam, benzodiazepines, zolpicolone, zolpidem)
calcium channel blockers (eg, diltiazem, nifedipine, verapamil, nimodipine, isradipine, nicardipine, nisoldipine)
antibacterial drugs (eg chloramphenicol, clarithromycin, dapsone, doxycycline, fluoroquinolones, telithromycin),
corticosteroids
cardiac glycosides (digitoxin, digoxin)
clofibrate
hormonal contraceptives
estrogens
antidiabetic drugs (eg, chlorpropamide, tolbutamide, sulfonylurea, rosiglitazone)
immunosuppressants (eg, cyclosporine, sirolimus, tacrolimus)
irinotecan
hormone thyroid gland(eg, levothyroxine)
losartan
analgesics (eg, methadone, narcotic analgesics)
praziquantel
progestogens
riluzole
5-HT3 receptor antagonists (eg, ondansetron)
theophylline
tricyclic antidepressants (eg, amitriptyline, nortriptyline)
cytotoxic drugs(eg imatinib)
diuretics (eg eplerenone)
Patients taking oral contraceptives should be advised to use alternative, non-hormonal methods of contraception.
When taking rifampicin, it becomes more difficult to control the condition of patients with diabetes mellitus.
If rifampicin is co-administered with saquinavir/ritonavir, the risk of hepatotoxicity is increased. Co-administration of rifampicin with saquinavir/ritonavir is contraindicated.
The simultaneous use of ketoconazole and rifampicin leads to a decrease in the concentrations of both drugs.
The parallel use of rifampicin and enalapril leads to a decrease in the concentration of enalaprilat, the active metabolite of enalapril. It is necessary to adjust the dosage of the drug.
The simultaneous use of antacids may reduce the absorption of rifampicin. Daily doses of rifampicin should be taken at least 1 hour before taking antacids.
If the drug is used simultaneously with halothane or isoniazid, the risk of hepatotoxicity increases. Should be avoided simultaneous reception rifampicin and halothane.
In patients receiving both rifampicin and isoniazid, liver function should be carefully monitored.
Para-aminosalicylic acid interferes with the absorption of rifampicin. Para-aminosalicylic acid preparations containing bentonite (aluminum hydrosilicate) should be prescribed no earlier than 4 hours after taking rifampicin.
Co-administration with HIV protease inhibitors (indinavir, nelfinavir) should be avoided.
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.
special instructions
Long-term rifampicin is better tolerated than intermittent (2-3 times a week).
Monotherapy of tuberculosis with rifampicin is often accompanied by the development of resistance of the pathogen to the antibiotic, so it should be combined with other anti-tuberculosis drugs.
Use with caution in pulmonary heart disease II-III degree, in malnourished patients, in patients who abuse alcohol, with porphyria.
Treatment with rifampicin should be carried out under close medical supervision. With prolonged administration, the development of phlebitis is possible. With the development of thrombocytopenia, purpura, hemolytic anemia, kidney failure and other serious adverse reactions, the administration of rifampicin is discontinued. Precautions should be taken in case of renal insufficiency at doses greater than 600 mg/day.
In patients with tuberculosis, liver function should be checked before starting treatment. Adults: The following should be checked: liver enzymes, bilirubin, creatinine, general analysis blood and platelet count. In patients with impaired liver function, the drug should be taken only if 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 (ACT). 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, after normalization of liver function, rifampicin was again prescribed, it is necessary to monitor liver function daily. In patients with impaired liver function, in elderly patients, debilitated patients, caution should be exercised when used simultaneously with isoniazid (the risk of hepatotoxicity increases).
In some patients, hyperbilirubinemia may occur during the first days of treatment. A moderate increase in bilirubin and/or transaminase levels is not an indication for treatment interruption. It is necessary to monitor liver function in dynamics and clinical condition patient. Rifampicin may interfere with biliary secretion of the contrast agent used to visualize the gallbladder due to competition for bile secretion. Thus, the study must be carried out before the introduction of the drug.
Because of the possibility of an immunological reaction, including anaphylactic shock, occurring in connection with intermittent therapy, patients should be closely monitored and should be informed of the dangers of intermittent treatment.
With prolonged use of the drug, it is necessary to control the blood picture due to the possibility of developing leukopenia.
In the case of prophylactic use in bacilli carriers of meningococcus, strict monitoring of the health of patients is necessary in order to promptly identify the symptoms of the disease in the event of resistance to rifampicin. Do not use during treatment microbiological methods concentration determination folic acid and vitamin B12 in serum. Alternative methods of analysis should be considered. Taking the drug may increase the metabolism of endogenous substrates, including adrenal hormones, thyroid hormones and vitamin D.
The period of pregnancy and lactation
Rifampicin has been shown to be teratogenic in animal studies. The drug crosses the placental barrier, but its effect on the human fetus is not known.
Women of childbearing age need reliable contraception (including non-hormonal) for the duration of treatment.
The use of rifampicin during pregnancy and lactation is contraindicated.
Features of the effect of the drug on the ability to drive vehicle or potentially dangerous machinery.
During the period of treatment, driving and other activities that require a high concentration of attention and speed of psychomotor reactions should be avoided.
Overdose
Symptoms: nausea, vomiting, abdominal pain, itching, headache, increased lethargy, increased activity of liver enzymes and / or bilirubin, brownish-red or orange color of the skin, urine, sweat, saliva, tears, feces (color intensity is proportional to the amount of rifampicin taken) , liver disease may cause loss of consciousness, in pediatric practice, facial or periorbital edema may occur, hypotension, sinus tachycardia, ventricular arrhythmia, seizures, cardiac arrest, and even death may occur.
The minimum acute or toxic dose has not been established. However, non-fatal acute overdose in adults ranges from 9 to 12 g of rifampicin. Fatal acute overdose in adults ranges from 14 to 60 g. Some deaths from rifampicin poisoning have been associated with alcohol consumption.
Treatment - symptomatic (no specific antidote): gastric lavage, inducing vomiting, taking activated carbon, with nausea and vomiting - antiemetics, hemodialysis, forced diuresis.
Release form and packaging
10 capsules in a blister pack made of PVC film and printed lacquered aluminum foil.
2 blister packs along with instructions for medical use in the state and Russian languages are placed in cardboard packaging for consumer packaging.
Primary or secondary packages, together with the appropriate number of instructions for medical use in the state and Russian languages, are placed in a corrugated cardboard box.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 °C.
Keep out of the reach of children!
Shelf life
Do not use after the expiration date.
Terms of dispensing from pharmacies
On prescription
Manufacturer
LLP "Pavlodar Pharmaceutical Plant".
Kazakhstan, Pavlodar, 140011, st. Kamzina, 33.
Registration certificate holder
Pavlodar Pharmaceutical Plant LLP, Kazakhstan
The address of the organization that accepts claims from consumers on the quality of products (goods) on the territory of the Republic of Kazakhstan)
Tradename
Rifampicin
International non-proprietary name
Rifampicin
Dosage form
Capsules, 300 mg
Compound
One capsule contains
active substance- rifampicin 300 mg,
Excipients: lactose monohydrate, vaseline oil (liquid paraffin), potato starch, sodium lauryl sulfate, anhydrous colloidal silicon dioxide (aerosil), talc, magnesium stearate.
capsule shell: gelatin, titanium dioxide (E 171), azorubine (E 122).
Description
Hard gelatin capsules with 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 reached 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. The highest concentration of the drug is created in the tissues of the liver and kidneys. It is excreted from the body with bile and urine.
Pharmacodynamics
Rifampicin is a semi-synthetic broad-spectrum antibiotic from the rifamycin group. Inhibits the synthesis of ribonucleic acid (RNA).
It has a bacteriostatic, and in high concentrations - a bactericidal effect. Highly active against M.tuberculosis, is a first-line anti-tuberculosis drug. Active against Escherichia coli, Pseudomonas, Indole-positive and Indole-negative, Proteus, Klebsiella, Staphilococcus aureus, Coagulase-negative staphylococci, Neisseria meningitides, Haemophilus influenzae, Legionella species, M.tuberculosis, M.kansassi, M.scrofulaceum, M .intracellulare and M.avium.
Indications for use
Tuberculosis of the lungs and other organs (all forms) as part of complex therapy.
Dosage and administration
Rifampicin is taken orally on an empty stomach (1/2-1 hour before meals).
In the treatment of tuberculosis in adults: daily therapy (1 time per day) or intermittent therapy (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 decrease in physiological renal function, but due to a compensatory increase in liver excretion, the half-life of the drug is the same as in young patients. However, caution should be exercised when using the drug in such patients, especially if there is evidence of impaired liver function.
The duration of the course is 6-9-12 months or more. The duration of treatment is set individually. With poor tolerance to rifampicin, the daily dose can be divided into 2 doses.
Apply as directed by a doctor.
Side effects
- skin flushing, itching, rash, urticaria, exfoliative dermatitis, pemphigoid reactions, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome, vasculitis
- loss of appetite, anorexia, erosive gastritis, heartburn, nausea, vomiting, flatulence, epigastric pain, abdominal discomfort, intestinal colic, diarrhea, pseudomembranous colitis, constipation
- visual impairment
- hepatitis, jaundice
- exacerbation of gout (increase in serum uric acid)
- fatigue, drowsiness, rare cases of psychosis, depression
- thrombocytopenia (with or without purpura) usually occurs with intermittent therapy. Possible fatal cerebral hemorrhage if rifampicin treatment continued after purpura appears
- rare cases of intravascular coagulation, eosinophilia, leukopenia, edema, muscle weakness, myopathy, agranulocytosis, adrenal insufficiency in patients with adrenal insufficiency, dysuria
- gynecomastia in patients with diabetes mellitus
- rarely possible dysmenorrhea, induction of porphyria
- extremely rare herpes
With intermittent treatment, development is possible:
- "flu-like syndrome": fever, chills, headache, dizziness, bone pain appear most often within 3-6 months of therapy. The frequency of the syndrome varies, but this syndrome occurs in 50% of patients who received the drug once a week at a dose of 25 mg / kg or more
- shortness of breath and wheezing
- hypotension and shock
- anaphylactic shock
- acute hemolytic anemia
- acute renal failure caused by acute tubular necrosis or acute interstitial nephritis, hematuria
If serious complications occur, such as renal failure, thrombocytopenia and hemolytic anemia, the drug should be discontinued.
With long-term treatment with rifampicin in women, there may be cases of menstrual irregularities.
Rifampicin may cause reddish discoloration of the skin, urine, feces, sweat, sputum, and lacrimal fluid. Soft contact lenses can also stain.
Contraindications
- hypersensitivity to the components of the drug
- visual impairment (diabetic retinopathy, optic nerve damage)
- epilepsy, prone to seizures
- history of poliomyelitis
- history of infectious hepatitis, jaundice
- thrombophlebitis
- severe atherosclerosis
- liver dysfunction
- kidney dysfunction
- pregnancy, lactation
- children's age up to 18 years
- concomitant use with saquinavir/ritonavir
Drug Interactions
Rifampicin is a strong inducer of cytochrome P-450 and can cause potentially dangerous drug interactions. Simultaneous use of rifampicin with other drugs, which are also metabolized by cytochrome P-450, can accelerate their metabolism and reduce their action. In this case, it may be necessary to adjust the dose of these drugs. Examples of drugs metabolized by cytochrome P-450:
- antiarrhythmic drugs (eg, disopyramide, mexiletine, quinidine, propafenone, tocainide)
- antiepileptics (eg phenytoin)
- hormone antagonist (antiestrogen, eg tamoxifen, toremifene, gestinone)
- antipsychotics (eg, haloperidol, aripiprazole)
- anticoagulants (eg coumarins)
- antifungals (eg, fluconazole, itraconazole, ketoconazole, voriconazole)
- antivirals (eg, saquinavir, indinavir, efavirenz, amprenavir, nelfinavir, atazanavir, lopinavir, nevirapine)
- barbiturates (phenobarbital)
- beta blockers (eg, bisoprolol, propranolol)
- anxiolytics and hypnotics (eg, diazepam, benzodiazepines, zolpicolone, zolpidem)
- calcium channel blockers (eg, diltiazem, nifedipine, verapamil, nimodipine, isradipine, nicardipine, nisoldipine)
- antibacterial drugs (eg chloramphenicol, clarithromycin, dapsone, doxycycline, fluoroquinolones, telithromycin),
- corticosteroids
- cardiac glycosides (digitoxin, digoxin)
- clofibrate
- hormonal contraceptives
- estrogens
- antidiabetic drugs (eg, chlorpropamide, tolbutamide, sulfonylurea, rosiglitazone)
- immunosuppressants (eg, cyclosporine, sirolimus, tacrolimus)
- irinotecan
- thyroid hormone (eg, levothyroxine)
- losartan
- analgesics (eg, methadone, narcotic analgesics)
- praziquantel
- progestogens
- quinine
- riluzole
- 5-HT3 receptor antagonists (eg, ondansetron)
- statins metabolized by CYP3A4 (eg, simvastatin)
- theophylline
- tricyclic antidepressants (eg, amitriptyline, nortriptyline)
- cytotoxic drugs (eg, imatinib)
- diuretics (eg eplerenone)
Patients taking oral contraceptives should be advised to use alternative, non-hormonal methods of contraception.
When taking rifampicin, it becomes more difficult to control the condition of patients with diabetes mellitus.
If rifampicin is co-administered with saquinavir/ritonavir, the risk of hepatotoxicity is increased. Co-administration of rifampicin with saquinavir/ritonavir is contraindicated.
The simultaneous use of ketoconazole and rifampicin leads to a decrease in the concentrations of both drugs.
The parallel use of rifampicin and enalapril leads to a decrease in the concentration of enalaprilat, the active metabolite of enalapril. It is necessary to adjust the dosage of the drug.
The simultaneous use of antacids may reduce the absorption of rifampicin. Daily doses of rifampicin should be taken at least 1 hour before taking antacids.
If the drug is used simultaneously with halothane or isoniazid, the risk of hepatotoxicity increases. Concomitant use of rifampicin and halothane should be avoided.
In patients receiving both rifampicin and isoniazid, liver function should be carefully monitored.
Para-aminosalicylic acid interferes with the absorption of rifampicin. Para-aminosalicylic acid preparations containing bentonite (aluminum hydrosilicate) should be prescribed no earlier than 4 hours after taking rifampicin.
Co-administration with HIV protease inhibitors (indinavir, nelfinavir) should be avoided.
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.
special instructions
Long-term rifampicin is better tolerated than intermittent (2-3 times a week).
Monotherapy of tuberculosis with rifampicin is often accompanied by the development of resistance of the pathogen to the antibiotic, so it should be combined with other anti-tuberculosis drugs.
Use with caution in pulmonary heart disease II-III degree, in malnourished patients, in patients who abuse alcohol, with porphyria.
Treatment with rifampicin should be carried out under close medical supervision. With prolonged administration, the development of phlebitis is possible. With the development of thrombocytopenia, purpura, hemolytic anemia, renal failure and other serious adverse reactions, the administration of rifampicin is stopped. Precautions should be taken in case of renal insufficiency at doses greater than 600 mg/day.
In patients with tuberculosis, liver function should be checked before starting treatment. Adults: The following should be checked: liver enzymes, bilirubin, creatinine, complete blood count, and platelet count. In patients with impaired liver function, the drug should be taken only if 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 (ACT). 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, after normalization of liver function, rifampicin was again prescribed, it is necessary to monitor liver function daily. In patients with impaired liver function, in elderly patients, debilitated patients, caution should be exercised when used simultaneously with isoniazid (the risk of hepatotoxicity increases).
In some patients, hyperbilirubinemia may occur during the first days of treatment. A moderate increase in bilirubin and/or transaminase levels is not an indication for treatment interruption. It is necessary to monitor the function of the liver and the clinical condition of the patient in dynamics. Rifampicin may interfere with biliary secretion of the contrast agent used to visualize the gallbladder due to competition for bile secretion. Thus, the study must be carried out before the introduction of the drug.
Because of the possibility of an immunological reaction, including anaphylactic shock, occurring in connection with intermittent therapy, patients should be closely monitored and should be informed of the dangers of intermittent treatment.
With prolonged use of the drug, it is necessary to control the blood picture due to the possibility of developing leukopenia.
In the case of prophylactic use in bacilli carriers of meningococcus, strict monitoring of the health of patients is necessary in order to promptly identify the symptoms of the disease in the event of resistance to rifampicin. During the period of treatment, microbiological methods for determining the concentration of folic acid and vitamin B 12 in the blood serum cannot be used. Alternative methods of analysis should be considered. Taking the drug may increase the metabolism of endogenous substrates, including adrenal hormones, thyroid hormones and vitamin D.
The period of pregnancy and lactation
Rifampicin has been shown to be teratogenic in animal studies. The drug crosses the placental barrier, but its effect on the human fetus is not known.
Women of childbearing age need reliable contraception (including non-hormonal) for the duration of treatment.
The use of rifampicin during pregnancy and lactation is contraindicated.
Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms.
During the period of treatment, driving and other activities that require a high concentration of attention and speed of psychomotor reactions should be avoided.
Overdose
Symptoms: nausea, vomiting, abdominal pain, itching, headache, increased lethargy, increased activity of liver enzymes and / or bilirubin, brownish-red or orange color of the skin, urine, sweat, saliva, tears, feces (color intensity is proportional to the amount of rifampicin taken) , liver disease may cause loss of consciousness, in pediatric practice, facial or periorbital edema may occur, hypotension, sinus tachycardia, ventricular arrhythmia, seizures, cardiac arrest, and even death may occur.
The minimum acute or toxic dose has not been established. However, non-fatal acute overdose in adults ranges from 9 to 12 g of rifampicin. Fatal acute overdose in adults ranges from 14 to 60 g. Some deaths from rifampicin poisoning have been associated with alcohol consumption.
Treatment - symptomatic (no specific antidote): gastric lavage, inducing vomiting, taking activated charcoal, with nausea and vomiting - antiemetics, hemodialysis, forced diuresis.
Release form and packaging
10 capsules in a blister pack made of PVC film and printed lacquered aluminum foil.
2 blister packs, together with instructions for medical use in the state and Russian languages, are placed in cardboard packaging for consumer packaging.
Primary or secondary packages, together with the appropriate number of instructions for medical use in the state and Russian languages, are placed in a corrugated cardboard box.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 °C.
Keep out of the reach of children!
Shelf life
Do not use after the expiration date.
Terms of dispensing from pharmacies
On prescription
Manufacturer
LLP "Pavlodar Pharmaceutical Plant".
Registration certificate holder
Pavlodar Pharmaceutical Plant LLP, Kazakhstan
The address of the organization that accepts claims from consumers on the quality of products (goods) on the territory of the Republic of Kazakhstan )
LLP "Pavlodar Pharmaceutical Plant"
Kazakhstan, Pavlodar, 140011, st. Kamzina, 33.
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The site provides reference information for informational purposes only. Diagnosis and treatment of diseases should be carried out under the supervision of a specialist. All drugs have contraindications. Expert advice is required!
Antibiotic Rifampicin
Rifampicin – antibiotic(semi-synthetic), derived from Rifamycin. The spectrum of its action is very wide: the drug is active in low concentrations against pathogens of tuberculosis, leprosy, brucellosis, against Staphylococcus aureus, chlamydia, legionella, pathogen typhus and streptococci. In high doses, Rifampicin acts on meningococci and gonococci, Klebsiella and Escherichia coli, Proteus, whooping cough, anthrax and tularemia. It acts on these pathogens even when they are resistant to other drugs (for example, tuberculosis bacillus resistant to Streptomycin, Isoniazid and PAS, or para-aminobenzoic acid).
V cerebrospinal fluid Rifampicin crosses the blood-brain barrier only in meningitis.
In the kidneys and liver, the highest concentration of the drug is noted.
Excreted from the body with urine and feces. In a small amount, it is excreted with tears, sputum, sweat, breast milk, while staining them in a reddish-orange color.
The antibiotic has the appearance of a crystalline powder of red-brick color. It is practically insoluble in water, poorly soluble in alcohol. Sensitive to light, oxygen and moisture.
Release form
- Tablets of 150, 300, 450, 600 mg, 30-100 pcs. packaged;
- Capsules 150, 300, 450, 600 mg 20, 30, 100 pcs. packaged;
- Capsules for children 50 mg - 30 pcs. packaged;
- Powder for the preparation of a solution for intravenous administration in ampoules of 150 mg - 10 ampoules per pack;
- Ear drops with Rifampicin Otofa (in 1 ml - 26 mg of Rifampicin) - in 10 ml bottles.
Instructions for use Rifampicin
Indications for use
- Tuberculosis of any localization and form (in combination with other anti-tuberculosis drugs);
- various forms of leprosy (leprosy);
- respiratory infections (pneumonia, bronchitis);
- meningococcal infection (treatment of meningococcal meningitis, meningococcal bacterial carriage and prevention for contacts);
- gonorrhea;
- infections biliary tract(cholecystitis);
- kidney infections and urinary tract(pyelonephritis);
- inflammation of the ears (otitis media);
- brucellosis;
- in order to prevent tuberculosis in HIV-infected patients with a decrease in immunogram parameters;
- rabies prevention (in the latent period, after an animal bite).
Contraindications
- Individual intolerance (including other derivatives of Rifamycin);
- jaundice (infectious hepatitis and obstructive jaundice);
- pregnancy;
- children's infancy.
- phlebitis (inflammation of the veins);
- pulmonary heart failure II-III stage;
- childhood.
Side effects
- From the digestive organs: loss of appetite, abdominal pain, vomiting, nausea, diarrhea; erosive gastritis; pseudomembranous colitis; thrush oral cavity; hepatitis with increased activity of liver enzymes and bilirubin levels; inflammation of the pancreas (pancreatitis).
- From the side nervous system: headaches, visual impairment, ataxia (gait disturbance), and spatial disorientation.
- From the side of cardio-vascular system: decrease in blood pressure (when the rate of administration of the drug into the vein is exceeded), phlebitis (inflammation of the veins) with a long course of intravenous infusion of the drug.
- From the blood and hematopoietic organs: decrease in the number of platelets; a decrease in the number of white blood cells in the blood (leukopenia); hemolytic anemia (anemia due to the destruction of red blood cells); bleeding; thrombocytopenic purpura (bleeding on the skin due to a decrease in the number of platelets).
- From the side genitourinary system: inflammation of the kidneys, menstrual irregularities, acute renal failure.
- Allergic reactions: rashes like urticaria, skin itching, bronchospasm, lacrimation; increase in the number of eosinophils in the blood; temperature increase; swelling of the subcutaneous tissue and skin.
- Other effects: joint pain, muscle weakness, flu-like syndrome, herpetic eruptions. Rifampicin can stain body secretions (urine, saliva, tears, sputum, nasal mucus) and soft contact lenses red-orange.
Treatment with Rifampicin
How to use Rifampicin?Rifampicin can be taken by mouth and given intravenously. Inside take tablets or capsules for 30-60 minutes. before meals.
For intravenous administration, a solution is prepared: water for injection (2.5 ml) is injected into the powder ampoule; the ampoule is shaken until the powder is completely dissolved; the resulting solution from the ampoule is injected into 125 ml of 5% glucose solution. The rate of administration of the drug into a vein is 60-80 drops per 1 minute.
Candles ( rectal suppositories) with Rifampicin is administered at night in the rectum.
Otofa ear drops are instilled into the ear (in the patient's sitting position), slightly pulling back for this auricle up and back. The bottle with drops should be warmed in the hand before instillation.
Rifampicin can be administered by inhalation and into the cavity (into the cavity or into the pleural cavity).
Often, Rifampicin is used in the form of compresses or ointments mixed with Dimexide (see point 6).
The method of administration of the drug is determined by the doctor. Daily administration of the drug is tolerated by patients more easily than intermittent administration (2-3 days per week). With the development side effect in the form of a flu-like syndrome, they switch to a daily intake (the dose increases gradually). Intravenous administration should be replaced with internal administration as soon as possible (because of the risk of developing phlebitis).
During treatment with Rifampicin, alcohol should be avoided. If it is necessary to use antacids (drugs that reduce the acidity of the contents of the stomach), as well as PAS, these drugs should be taken after Rifampicin after 4 or more hours.
With prolonged use of Rifampicin, laboratory monitoring of liver and kidney function should be carried out (2 times in the first month, then 1 p. per month).
Women of childbearing age receiving Rifampicin should use reliable non-hormonal contraception for the entire period of treatment.
Compresses from Rifampicin with Dimexide
Many patients ask how to make a compress from Rifampicin with Dimexide; Therefore, we consider this issue in detail. Dimexide is a drug for external use that has anti-inflammatory, antiseptic and analgesic effects. It is able to dissolve and inject deeply into tissues many medicines(Rifampicin included). Dimexide, in addition, increases the sensitivity of pathogens to antibacterial drugs(including Rifampicin).
The drug is produced in the form of a concentrate for the preparation of a solution. Usually Dimexide is used in the form of a 20-25-30% solution (that is, diluted with water in ratios of 1:3 - 1:4 - 1:5).
For a compress, a solution of Rifampicin prepared from an ampoule is added to a dilute solution of Dimexide (the dose is prescribed by a doctor), a gauze napkin is moistened, slightly squeezed out and applied to the area indicated by the doctor. From above, the napkin is covered with plastic wrap and the compress is fixed with a bandage. The compress is applied for 20-30 minutes. 1 time per day.
Before using such compresses, sensitivity to Dimexide should be checked. To do this, moisten a cotton swab in the drug solution and apply it to the skin. The appearance of redness and severe itching of the skin indicate hypersensitivity to the drug and, therefore, the imposition of a compress should be canceled.
Since both Rifampicin and Dimexide have their own contraindications, treatment with compresses should only be carried out as prescribed by a doctor. With caution, it is necessary to apply compresses with Dimexide to children and the elderly, as well as to sharply weakened patients.
, beta-blockers, leukopenia.
Rifampicin analogs
Rifampicin synonyms (contain the same active ingredient):- Benemycin;
- Ripampin;
- Rifadin;
- Rimactan;
- Rifamor;
- Tubocin;
- Rifaldazine;
- Riforal;
- Tibinil;
- Rilamizin;
- Riphodex;
- Tibicin;
- Rifogal;
- Rifaren;
- rimpin;
- Eremfat-600;
- Rifampicin-Ferein;
- Rifaldin;
- Rifampin;
- Rimpatsin;
- Rishima;
- Rifampicin-M.J.