Rifampicin spectrum of action. Medicinal reference book geotar

Rifampicin (Rifadin, Benemycin, Rimpacin) is a bactericidal antibiotic drug. It is one of four drugs used in the standard treatment of tuberculosis.

Introduced oral by or by intravenous injections.

Indications for use

Rifampicin is one of the strongest And effective drugs against tuberculosis, is indicated in the treatment of all its forms and at any stage. With repeated treatment of tuberculosis, intravenous administration of Rifadin is prescribed. If necessary, it can be administered to children from birth (including preterm), but it is recommended to start giving the drug when the child reaches at least one year old.

Important! Microorganisms quickly develop resistance to Rifampicin, so regular antibiotic susceptibility testing is required during treatment.

Rifampicin tablets: instructions for use

At the initial stage of therapy, it is recommended to take Rifampicin in combination with Isoniazid And Pyrazinamide. Often added as a fourth remedy Streptomycin or Ethambutol. The need for a fourth drug depends on the results of susceptibility testing. With a low level of resistance of microorganisms to antibiotics, it is possible to use fewer medicines. The course of treatment continues within two months.

Photo 1. Packing of Rifamycin, 20 capsules of 150 mg each, manufactured by JSC Pharmasyntez.

After passing the initial phase, treatment is continued using two drugs: Rifadina And Isoniazid. The course lasts at least four months. If necessary, as well as for HIV-infected people, the course is extended for a longer period.

In the treatment of latent tuberculosis, the drug is taken for four months without Isoniazid. For children and HIV-infected people, the course can be extended up to six months.

Important! To achieve the result, you need to pass full course treatment, the duration of which is determined by the doctor. If the course is interrupted prematurely, the bacteria will not be completely killed, which will lead to a decrease in the effectiveness of the treatment. In addition, bacteria will become resistant to Rifampicin. This will require the use stronger medicines.

Rifampicin tablets are taken once a day or two(usually in the morning or evening) three or five times a week. Either you need to take an antibiotic in one hour before meals, or two hours after drinking big amount water. The drug should not be taken with milk.

For solution for infusion 600 mg powder diluted 10 ml sterile water. The mixture is well shaken so that the antibiotic is completely dissolved. The solution contains 60 mg rifampicin per milliliter and can be stored at room temperature for 24 hours.

Before administration, add to the required amount of the drug 100 ml infusion solution, mix well and inject intravenously for 30 minutes. When used as an infusion fluid 5% glucose solution, the drug can be stored at room temperature for 4 hours; when using saline, the drug is stable at room temperature for 24 hours.

Dosage

Oral and intravenous doses for Rifampicin are equivalent.

Maximum dose medication for treatment active form tuberculosis should be:

• for adults(including seniors and adolescents) 10 mg/kg/day (max. 600 mg/day);
• for children(including newborns) - 20 mg / kg / day (max. 600 mg / day).

The maximum dose of the drug in the treatment of latent tuberculosis should be 10 mg / kg / day (max. 600 mg / day) for both adults and children.

Reference. If the patient is unable to take the capsule, its contents are mixed with applesauce or gelatin.

Minimum dose, leading to death or acute poisoning of the body, has not been established. There have been cases of acute overdose of Rifampicin in adults with doses of 9 to 12 grams, as well as cases of acute overdose of adults with a fatal outcome with doses of 14 to 60 grams. In children from 1 to 4 years of age, an overdose may begin at 100 mg / kg.

Attention! Rifadin should be taken at the same time, if you miss the time of taking the medicine, you need to take the dose as soon as possible. If less than 12 hours are left before the next dose, skip the dose and return to the usual schedule. Skipping a medication can cause side effects.

Contraindications and precautions

Rifampicin is not recommended in cases where infection has not been established bacterial infection, as well as in preventive purposes. This antibiotic can harm the body, and taking it increases the risk of developing drug-resistant bacteria.

Due to the fact that taking Rifampicin can provoke an exacerbation of a number of diseases, with some diagnoses it should be taken with great care.

For liver disease, tests to check liver function are done twice a month. Hepatic side effects include cases of hepatitis and acute hepatotoxicity. In patients with liver dysfunction, as well as in patients with normal liver function taking other hepatotoxic drugs, complications were observed leading to death.

Adrenal dysfunction may develop adrenal insufficiency.

When taking Rifadin, it is possible exacerbation of porphyria.

People with diabetes should use Rifampicin with caution as this antibiotic will make it difficult to control the disease.

Intravenous administration of the drug is undesirable when cardio-pulmonary insufficiency And phlebitis.

Pregnant women should only use Rifampicin if the potential benefit justifies the potential risk to the baby.

With the introduction of the drug in the last trimester of pregnancy, hemorrhages both mother and baby. Women taking rifampicin should give up breastfeeding baby.

Rifadin is contraindicated in people with hypersensitivity to rifamycins. Due to high hepatocellular toxicity, Rifampicin should not be given to people taking Saquinavir in combination with Ritonavir.

Attention! Rifampicin is better tolerated by the body when permanent reception, intermittent therapy often causes side effects and is considered undesirable.

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Rifampicin and alcohol, their compatibility

Drinking alcohol while taking Rifampicin (or drinking too much alcohol before starting the drug) can cause severe liver damage and lead to lethal outcome. In addition, Rifampicin may be accompanied by drowsiness or dizziness. These symptoms may be aggravated by alcohol.

Side effects and overdose

Side effects may occur when taking Rifampicin. The greatest likelihood of their occurrence is associated with lengthy or intermittent course of treatment.

Side effects requiring immediate medical attention:

• pallor of the skin;
• painful urination;
• chest pain;
• pain in the abdomen or stomach;
• pain in the bones or joints;
• backache;
• inflammation of the joints;
• headache;
• dizziness;
• depression;
• diarrhea;
• diplopia;
• thirst;
• difficulty in swallowing;
• difficult or slow speech;
• significant weight gain or loss;
• skin itching, rash, or redness;
• cough or hoarseness;
• hives;
• bleeding gums;

Photo 2. Bleeding gums, one of the possible side effects from taking Rifampicin.

• blood in urine or stool;
• fever;
• lack of coordination;
• persistent bleeding at puncture sites, mouth, or nose;
• bad smell from mouth;
• fainting;
• chills;
• swelling of the face, ankles, fingers, hands, or feet;
• swelling of the eyelids, the area around the eyes, face, lips, tongue;
• feeling of weakness;
• paralysis;
• high blood pressure;
• redness, eye irritation;
• darkening of the skin;
• loss of appetite;
• sweating;
• psychomotor agitation;
• irritability;
• erratic breathing;

Photo 3. Yellowing of the whites of the eyes in a man.

• light feces;
• tightness in the chest;
• bruises;
• decreased frequency of urination or amount of urine;
• dark urine;
• nausea or vomiting;
• enlarged lymph nodes;
• enlargement of the tonsils;
• cardiopalmus;
• fast or weak pulse;
• cold, clammy skin;
• peeling of the skin;
• sores, pus, or white spots on the lips or in the mouth.

Some of the side effects that occur when taking Rifampicin are do not require immediate recourse medical care . As the body begins to get used to the antibiotic, they may pass. If any of the symptoms persist for a long time or cause concern, a specialist should be consulted.

Side effects, not requiring immediate medical attention:

• a sore throat;
• bloating;
• visual or auditory hallucinations;
• change in the menstrual cycle in women;
• muscle pain;
• slight weight loss;
• belching;
• the feeling that others hear your thoughts;
• Bad mood;
• increased gas formation;
• distraction of attention;
• drowsiness;
• the feeling that you are being watched or controlled in your behavior.

Important! Rifampicin can cause discoloration of urine, tears, feces, saliva, sputum, and sweat. brownish red or orange. This is due to the excretion of the drug from the body and is not a side effect that requires a visit to a doctor.

The reaction of organs and systems of the body to the drug

From the gastrointestinal tract

At 2% of people nausea and dyspepsia are observed. Heartburn, erosive gastritis, anorexia, vomiting, flatulence, convulsions, diarrhea, candidiasis, colitis, pancreatic dysfunction, decreased or loss of appetite are also possible.

From the side of the liver

Photo 4. A man on the left with a normal skin color, on the right - with a symptom of jaundice.

At 3% of patients hyperbilirubinemia and hepatitis were detected. In half of the cases, hepatotoxicity was observed during the first month of therapy. Possible development of jaundice, increased levels of serum bilirubin, alkaline phosphatase and serum transaminases.

From the side of the immune system

When Rifampicin is taken intermittently, it is possible to develop flu-like syndrome, which is a complex of symptoms: malaise, fever, chills, vomiting, nausea.

From the side of the kidneys

Renal side effects include increased urea levels and uric acid in blood. There have been cases of hemoglobinuria, interstitial nephritis, hematuria, acute tubular necrosis, renal failure.

From the hematopoietic system

At 1% hosts Rifampicin observed petechiae associated with thrombocytopenia. It is also possible to decrease hemoglobin, a short-term decrease in the number of leukocytes, hemolytic anemia.

From the side of the skin

Skin reactions usually flow gently and are not associated with hypersensitivity to Rifampicin. Manifested in the form of itching and redness of the skin.

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From the side of the nervous system

Side effects include headache, paresthesia And weakness. Drowsiness, fatigue, dizziness, disorientation, decreased concentration, mental disorders, ataxia, behavioral changes, fever, muscle weakness, pain and numbness. In rare cases, psychosis and myopathy may occur.

From the side of metabolism

Long-term medication ( more than 3 months) it is possible to accelerate the hepatic metabolism of thyroxine and triiodothyronine.

In some cases, it is necessary to increase the dosage of Rifampicin to keep it within the therapeutic range.

From the side of the cardiovascular system

Side effects rare. Possible reduction blood pressure if doses of the drug are administered intermittently.

From the endocrine system

Perhaps the development of adrenal insufficiency in violation of the functions of the adrenal glands and menstrual disorders in women.

From the side of the musculoskeletal system

Side effects include myopathy and myasthenia gravis.

From the side of view

Visual impairment, diplopia, conjunctivitis, blurred vision.

From the respiratory system

There may be shortness of breath, wheezing or wheezing, shortness of breath.

If symptoms of an overdose occur while taking Rifampicin, stop taking the drug And seek medical attention.

Overdose symptoms:

• pain in the upper part of the stomach or abdomen;
• dizziness or weakness with a sharp change in body position;
• low blood pressure;
• swelling of the face or area around the eyes;
• yellowing of the whites of the eyes or skin;
• clouding in the eyes;
• memory loss;
• loss of consciousness;
• severe weakness or fatigue;
• convulsions;
• nausea or vomiting;
• heaviness in the stomach or abdomen;
• fast, irregular, or weak heartbeat.

What is important to remember when treating with Rifampicin?

Rifampicin is the mainstay of anti-tuberculosis therapy, but at the same time it can cause significant harm to the body. At liver diseases Rifampicin is taken only in case of emergency And under constant medical supervision.

The severity of liver damage during treatment with Rifampicin ranges from asymptomatic elevation of serum aminotransferase levels and jaundice without overt liver damage to acute liver failure and death. For this reason, during the course of treatment, you should completely give up alcohol and closely monitor the occurrence possible side effects.

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**** *PHARMASINTEZ AO* IPCA Laboratories AKRIKHIN / BIOPHARM M.J. Akrikhin KhPK AO BELMEDPREPRATY, RUE Biochemist, OAO BRYNTSALOV BRYNTSALOV-A, ZAO Ipka Laboratories Limited/Akrikhin OAO Moskhimfarmpreparaty FSUE im. Semashko Sintez ACO OJSC Pharmasintez JSC Pharmsintez, PJSC FEREIN SCHELKOVSKY VITAMIN PLANT

Country of origin

India Republic of Belarus Russia

Product group

Antibacterial drugs

Semi-synthetic broad-spectrum antibiotic of the rifamycin group

Release form

• 10 - cellular contour packs (1) - packs of cardboard. 10 - cellular contour packs (2) - packs of cardboard. 20 - dark glass jars (1) - cardboard packs. 10 - blister packs contour 150 mg - ampoules (10) - packs of cardboard. Capsules 150mg in blisters No. 10x10

Description of the dosage form

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

pharmachologic effect

Rifampicin is a semi-synthetic broad-spectrum antibiotic from the group of rifamycins (ansamycins). Acts bactericidal. Violates RNA synthesis in a bacterial cell by inhibiting DNA-dependent RNA polymerase. It is highly active against Mycobacterium tuberculosis, is an anti-tuberculosis agent of the first line. Active against gram-positive bacteria (Staphylococcus spp, including multi-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 work on mushrooms. Rifampicin has a virucidal effect on the rabies virus, inhibits the development of rabies encephalitis. Rifampicin resistance develops rapidly. Cross stability with others antibacterial drugs(with the exception of other rifamycins) not detected

Pharmacokinetics

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

Special conditions

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. 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. The drug is not indicated for intermittent therapy. The introduction of the drug may be accompanied by staining of urine, feces, saliva, sweat, lacrimal fluid, contact lenses in red. Treatment with rifampicin should be carried out under close medical supervision. Treatment with the drug should be started after a study of liver function (determination of the level of bilirubin and aminotransferases in the blood, thymol test), and during the treatment it should be carried out monthly. With increasing symptoms of liver dysfunction, the use of the drug should be discontinued. At long-term use the drug, it is necessary to control the blood picture in connection with the possibility of developing leukopenia. Overdose Symptoms: nausea, vomiting, diarrhea, drowsiness, liver enlargement, jaundice, increased levels of bilirubin, hepatic transaminases in blood plasma; brown-red or orange coloration of the skin, urine, saliva, sweat, tears and feces in proportion to the dose of the drug. Treatment: discontinuation of the drug. Gastric lavage. Symptomatic therapy (there is no specific antidote). Maintenance of 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; in infectious and inflammatory diseases caused by pathogens sensitive to the drug (including osteomyelitis, pneumonia, pyelonephritis, leprosy, gonorrhea, otitis media, cholecystitis, etc.), as well as in meningococcal carriage. Due to the rapid development of antibiotic resistance during treatment, the use of rifampicin in diseases of non-tuberculous etiology is limited to cases that are not amenable to treatment with other antibiotics.

Rifampicin contraindications

• Jaundice, recent (less than 1 year) infectious hepatitis, pronounced violations kidney function, hypersensitivity to rifampicin or other rifamycins

Rifampicin dosage

• 0.15 g 150 mg

Rifampicin side effects

• Functional disorders may occur during treatment with rifampicin. gastrointestinal tract(loss of appetite, nausea, vomiting, diarrhea). These phenomena usually disappear on their own after 2-3 days without discontinuation of the drug. Rifampicin can have a hepatotoxic effect (increased levels of transaminases and bilirubin in the blood serum, jaundice). For the timely detection and prevention of hepatotoxic effects, treatment with rifampicin should be started after a study of liver function (determination of the level of bilirubin and aminotransferases in the blood, thymol test), and during the treatment it should be carried out monthly. In patients with a history of hepatitis or liver cirrhosis, these studies should be performed every 2 weeks. Moderate liver dysfunction is usually transient and may disappear without discontinuation of the drug with the appointment of allochol, methionine, pyridoxine, vitamin B, etc. With increasing symptoms of liver dysfunction, the use of rifampicin should be discontinued. Leukopenia and thrombocytopenia may develop during treatment with rifampicin. allergic reactions. The latter are manifested in the form of skin rashes, eosinophilia, rarely - bronchospasm and Quincke's edema. With intermittent treatment, irregular use of the drug, or when rifampicin treatment is resumed after a break, severe allergic reactions in the form of hypnoid fever, acute renal liver failure or thrombopenic purpura may be observed. These complications are sometimes preceded by signs of drug sensitization (fever after taking the drug, increasing eosinophilia, bronchospasm, and positive tests Shelley, Waigner, 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). With good tolerance, the dose of the antibiotic can be increased to the usual therapeutic dose. If allergic reactions occur, rifampicin is canceled and desensitizing therapy is carried out (antihistamines, calcium preparations, 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, lacrimal fluid, 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 intravenous infusion of the drug should be carried out under the control of blood pressure during the administration of the drug. With prolonged intravenous administration, the development of phlebitis is possible.

drug interaction

Rifampicin is a strong inducer of cytochrome P-450, which can cause potentially dangerous drug interactions. Rifampicin accelerates the metabolism (the concentration in the blood plasma decreases and the action decreases accordingly) of theophylline, thyroxine, corticosteroids, carbamazepine, phenytoin, oral anticoagulants, oral hypoglycemic drugs, dapsone, some tricyclic antidepressants, chloramphenicol, fluconazole, ketoconazole, terbinafine, haloperidol, diazepam, bisoprolol , propranolol, diltiazem, nifedipine, verapamil, cardiac glycosides, quinidine, disopyramide, propafenone, cyclosporine. Co-administration with HIV protease inhibitors (indinavir, nelfinavir) should be avoided. Rifampicin accelerates the metabolism of estrogens and progestogens (the contraceptive effect of oral contraceptives decreases). 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

Gross formula

C 43 H 58 N 4 O 12

Pharmacological group of the substance Rifampicin

Nosological classification (ICD-10)

CAS code

13292-46-1

Characteristics of the substance Rifampicin

Semi-synthetic derivative of natural rifamycin. Crystalline powder of brick or brick-red color, odourless. Practically insoluble in water, sparingly soluble in formamide, slightly soluble in ethyl alcohol, soluble in ethyl acetate and methyl alcohol, freely soluble in chloroform. Sensitive to the action of oxygen, light and air moisture.

Pharmacology

pharmachologic effect- bactericidal, anti-tuberculosis, broad-spectrum antibacterial, anti-leprosy.

Violates RNA synthesis in a bacterial cell: binds to the beta subunit of DNA-dependent RNA polymerase, preventing its attachment to DNA, and inhibits RNA transcription. Does not affect human RNA polymerase. Effective against extra- and intracellular microorganisms, especially rapidly multiplying extracellular pathogens. There is evidence of blocking the last stage of the formation of poxviruses, possibly due to a violation of the formation of the outer shell. At low concentrations, it acts on Mycobacterium tuberculosis, Brucella spp., Chlamidia trachomatis, Legionella pneumophila, Rickettsia typhi, Mycobacterium leprae, Staphylococcus aureus, including methicillin resistant strains Staphylococcus epidermidis, streptococci; in high concentrations - on some gram-negative microorganisms (Escherichia coli, Klebsiella, Proteus, Neisseria meningitidis, Neisseria gonorrhoeae, including beta-lactamase-forming). Active towards haemophilus influenzae(including resistant to ampicillin and chloramphenicol), Haemophilus ducreyi, Bordetella pertussis, Bacillus anthracis, Listeria monocytogenes, Francisella tularensis, Clostridia difficile and other Gram-positive anaerobes. Not valid on Mycobacterium fortuitum, representatives of the family enterobacteraceae, non-fermenting Gram-negative bacteria (Pseudomonas spp., Acinetobacter spp., Stenothrophomonas spp.). In the lesions creates concentrations almost 100 times higher than the MIC for Mycobacterium tuberculosis(0.125-0.25 µg/ml). With monotherapy, resistance of the pathogen develops relatively quickly due to a decrease in the penetration of rifampicin into the cell or a mutation in the DNA-dependent RNA polymerase. Cross-resistance with other antibiotics (with the exception of the rifamycin group) is not observed.

Rapidly and completely absorbed from the gastrointestinal tract; food intake, especially rich in fats, reduces absorption (by 30%). After absorption, it is rapidly excreted in the bile, undergoes enterohepatic recirculation. Bioavailability decreases with long-term treatment. Plasma protein binding - 84-91%. Cmax in the blood after ingestion of 600 mg of rifampicin is achieved after 2-2.5 hours and is 7-9 mcg / ml in adults, and 11 mcg / ml in children after taking a dose of 10 mg / kg. With the on / in the introduction of C max is achieved by the end of the infusion and is 9-17.5 μg / ml; therapeutic concentration is maintained for 8-12 hours. The apparent volume of distribution in adults is 1.6 l / kg, in children - 1.2 l / kg. Most of the fraction unbound to plasma proteins in a non-ionized form penetrates well into tissues (including bone) and body fluids. It is found in therapeutic concentrations in pleural and peritoneal exudate, cavern contents, sputum, saliva, nasal secretions; the highest concentration is created in the liver and kidneys. It penetrates well into the cells. Passes through the BBB only in case of inflammation meninges, with tuberculous meningitis is found in the cerebrospinal fluid at concentrations of 10-40% of that in plasma. Metabolized in the liver to pharmacologically active 25-O-deacetylrifampicin and inactive metabolites (rifampinquinone, deacetylrifampinquinone and 3-formylrifampin). A strong inducer of microsomal enzymes of the cytochrome P450 system and intestinal wall enzymes. It has the properties of self-induction, accelerates its biotransformation, as a result of which the systemic clearance, after taking the first dose, equal to 6 l / h, increases to 9 l / h after repeated administration. T 1/2 after ingestion of 300 mg is 2.5 hours; 600 mg - 3-4 hours, 900 mg - 5 hours; shortened with prolonged use (600 mg - 1-2 hours). In patients with impaired renal excretory function, T 1/2 is prolonged if the dose exceeds 600 mg; in violation of liver function, there is an increase in plasma concentration and lengthening of T 1/2. It is excreted from the body with bile in the form of metabolites (60-65%) and in the urine, unchanged (6-15%), in the form of 25-O-deacetylrifampicin (15%) and in the form of 3-formylrifampin (7%). With increasing dose, the proportion of renal excretion increases. A small amount of rifampicin is excreted in tears, sweat, saliva, sputum and other liquids, turning them orange-red.

The effectiveness of rifampicin in the treatment of atypical mycobacteriosis, incl. in HIV-infected people and to prevent infection caused by haemophilus influenzae type b (Hib). There is evidence of a virucidal effect on the rabies virus and the suppression of the development of rabies encephalitis.

The use of the substance Rifampicin

Tuberculosis (all forms) - as part of combination therapy. Leprosy (in combination with dapsone - multibacillary types of the disease). Infectious diseases caused by susceptible microorganisms (in case of resistance to other antibiotics and as part of combination antimicrobial therapy). Brucellosis - as part of combination therapy with an antibiotic of the tetracycline group (doxycycline). Meningococcal meningitis (prophylaxis in people who have been in close contact with cases of meningococcal meningitis; in bacillus carriers Neisseria meningitidis).

Contraindications

Hypersensitivity, incl. to other drugs of the rifamycin group, impaired liver and kidney function, infectious hepatitis transferred less than 1 year ago, jaundice, incl. mechanical.

In / in the introduction: cardiopulmonary insufficiency II-III degree, phlebitis, children's age.

Application restrictions

Age up to 1 year, alcoholism (risk of hepatotoxicity).

Use during pregnancy and lactation

Contraindicated in the first trimester of pregnancy. In the II and III trimesters, it is possible only under strict indications, after comparing the expected benefits for the mother and the potential risk to the fetus.

Rifampicin crosses the hematoplacental barrier (fetal serum concentration at birth is 33% of maternal serum concentration). Teratogenicity has been established in animal studies. In rabbits treated with doses up to 20 times the usual daily dose for humans, osteogenesis disorders and toxic effects on the embryo were noted. In experiments on rodents, it was shown that rifampicin at doses of 150-250 mg/kg/day caused birth defects development, mainly a crevice upper lip and palate, spina bifida. When used in the last weeks of pregnancy, it can cause postpartum haemorrhage in the mother and haemorrhage in the newborn.

Stands out from breast milk, while the child receives less than 1% of the dose taken by the mother. Although no adverse reactions have been reported in humans, breastfeeding should be discontinued during treatment.

Women of childbearing age need reliable contraception (including non-hormonal) for the duration of treatment.

Side effects of Rifampicin

From the side nervous system and sense organs: headache, blurred vision, ataxia, disorientation.

From the side of cardio-vascular system and blood (hematopoiesis, hemostasis): lowering blood pressure (with rapid intravenous administration), phlebitis (with prolonged intravenous administration), thrombocytopenic purpura, thrombocytopenia and leukopenia, bleeding, acute hemolytic anemia.

From the digestive tract: candidiasis oral cavity, loss of appetite, nausea, vomiting, erosive gastritis, indigestion, abdominal pain, diarrhea, pseudomembranous colitis, increased levels of hepatic transaminases and bilirubin in the blood, jaundice (1-3%), hepatitis, pancreatic damage.

From the side genitourinary system: tubular necrosis, interstitial nephritis, acute renal failure, menstrual disorders.

Allergic reactions: skin rash, itching, urticaria, fever, angioedema, bronchospasm, lacrimation, eosinophilia.

Others: arthralgia, muscle weakness, herpes, induction of porphyria, flu-like syndrome (with intermittent or irregular therapy).

Interaction

Being a strong inducer of cytochrome P450, it can cause potentially dangerous interactions.

Reduces the activity of indirect anticoagulants, corticosteroids, oral hypoglycemic agents, digitalis preparations, antiarrhythmic agents (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, BCC, fluvastatin, enalapril, cimetidine (due to induction of microsomal liver enzymes and acceleration of the metabolism of these drugs). It should not be taken simultaneously with indinavir sulfate and nelfinavir, because. their plasma concentrations are significantly reduced due to the acceleration of metabolism. PAS preparations containing bentonite (aluminum hydrosilicate) and antacids, when taken simultaneously, disrupt 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. Simultaneous use with isoniazid or pyrazinamide increases the incidence and severity of liver dysfunction (against the background of liver disease) and the likelihood of developing neutropenia.

Overdose

Symptoms: nausea, vomiting, abdominal pain, liver enlargement, jaundice, periorbital or facial edema, pulmonary edema, clouding of consciousness, convulsions, mental disorders, lethargy, "red man syndrome" (red-orange staining of the skin, mucous membranes and sclera).

Treatment: gastric lavage, activated charcoal, forced diuresis, symptomatic therapy.

Routes of administration

Inside, in / in the drip.

Rifampicin Substance Precautions

In non-tuberculous diseases, it is prescribed only if other antibiotics are ineffective (rapid development of resistance). Patients with impaired renal function require dose adjustment if it exceeds 600 mg / day. Use with caution in newborns, premature babies (due to age-related immaturity of liver enzyme systems) and in malnourished patients. Newborns should be administered simultaneously with vitamin K (prevention of bleeding). Use with caution in HIV-infected patients receiving HIV protease inhibitors. With intravenous administration of rifampicin to patients diabetes it is recommended to inject 2 units of insulin for every 4-5 g of glucose (solvent). If a flu-like syndrome occurs with an intermittent regimen, if possible, switch to a daily intake; while increasing the dose gradually. When possible, you should switch from intravenous administration to oral administration (risk of phlebitis). During treatment should be monitored general analysis blood, kidney and liver function - first 1 time in 2 weeks, then monthly; an additional appointment or increase in the dose of glucocorticoids is possible. In the case of prophylactic use in bacilli carriers Neisseria meningitidis strict medical supervision of the patient is necessary for the timely detection of symptoms of the disease (with the development of resistance of the pathogen). PASK preparations containing bentonite (aluminum hydrosilicate) should be taken no earlier than 4 hours after taking rifampicin. Alcohol should be avoided during treatment (risk of hepatotoxicity increases).

Reviews of site visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of the antibiotic Rifampicin in their practice are presented. We kindly ask you to actively add your reviews about the drug: the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not declared by the manufacturer in the annotation. Rifampicin analogues in the presence of existing structural analogues. Use for the treatment of tuberculosis in adults, children, as well as during pregnancy and lactation.

Rifampicin is a 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 (mycobacterium tuberculosis), is an anti-tuberculosis drug of the 1st line.

Active against gram-positive bacteria: Staphylococcus spp. (including multidrug resistant) (staphylococcus aureus), Streptococcus spp. (streptococcus), Bacillus anthracis, Clostridium spp., as well as against some gram-negative bacteria: Neisseria meningitidis, Haemophilus influenzae, Brucella spp., Legionella pneumophila (legionella).

Active against Rickettsia prowazekii, Mycobacterium leprae, Chlamydia trachomatis (chlamydia).

Rifampicin resistance develops rapidly. Cross-resistance to other anti-tuberculosis drugs (with the exception of other rifamycins) has not been noted.

Rifampicin + excipients.

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. Excreted in bile, feces and urine.

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

Capsules 150 mg and 300 mg (sometimes erroneously called tablets).

Lyophilisate for solution for injection (injections in ampoules for injection).

There are no other dosage forms, whether it be candles or drops.

Instructions for use and dosage

Inside, on an empty stomach, minutes before meals.

Tuberculosis mg per day (taking into account body weight), the average daily dose for children over 3 years old is 10 mg / kg (but not more than 450 mg per day) 1 time per day 30 minutes before meals.

Carriage of meningococcal per day for 2-4 days, children - 20 mg / kg 2 times a day for 2-4 days.

Gonorrhea on the 1st day mg per day, on the 2nd and 3rd days mg per day.

For other infections in the acute period, 0 mg per day in 2 doses, after the disappearance of symptoms, treatment is continued for another 2-3 days; children under 7 years mg / kg per day, newborns mg / kg per day in 2 divided doses.

Perhaps the introduction into the pathological focus (by inhalation, intracavitary administration, as well as the introduction into the focus of skin lesions) pomg.

• nausea, vomiting;
• diarrhea;
• loss of appetite;
• pseudomembranous colitis;
• hepatitis;
• hives;
• angioedema;
• bronchospasm;
• flu-like syndrome;
• thrombocytopenia, thrombocytopenic purpura, eosinophilia, leukopenia, hemolytic anemia;
• headache;
• ataxia;
• visual impairment;
• interstitial nephritis;
• acute renal failure;
• violation of the menstrual cycle;
• red-brown staining of urine, feces, saliva, sputum, sweat, tears.

• 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 evaluated.

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 postpartum period.

Rifampicin is excreted in breast milk. If necessary, use during lactation should stop breastfeeding.

In newborns and premature babies, rifampicin is used only in cases of emergency.

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 it is necessary to start with a dose of 75 mg per day, gradually increasing it by 75 mg per day until the desired dose is reached. In this case, kidney function should be monitored; additional administration of glucocorticosteroids (GCS) is possible.

With prolonged use of rifampicin, systematic monitoring of the blood picture and liver function is shown; a test with a load of bromsulfalein should not be used, since rifampicin competitively inhibits its excretion.

PAS preparations containing bentonite (aluminum hydrosilicate) should be prescribed no earlier than 4 hours after taking rifampicin.

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 preparations, verapamil, phenytoin, quinidine, GCS, chloramphenicol, antifungal drugs, which leads to a decrease in their concentration in blood plasma and, accordingly, to a decrease in their action.

Analogues medicinal product Rifampicin

Structural analogues for the active substance:

Analogues for the therapeutic effect (drugs for the treatment of tuberculosis):

RIFAPEX

Tablets, coated film sheath red-brown, round, with a separating notch on one side and smooth on the other.

Excipients: microcrystalline cellulose (RANQ PH102), sodium carboxymethyl starch, pregelatinized starch, sodium ascorbate, sodium lauryl sulfate, disodium edetate, hyprolose (Klucel EXF), colloidal silicon dioxide (Aerosil 200), calcium stearate.

The composition of the film shell: hypromellose (Methocel E5 LPV), hypromellose (Methocel E15 LPV), macrogol 4000, titanium dioxide, talc, iron dye red oxide (Sicopharm Red 30), simethicone emulsion 30%.

8 pcs. - strips (8) - packs of cardboard.

Rifapentia is a derivative of rifamycin and has approximately the same microbiological activity profile as rifampicia, inhibits DNA-dependent RNA polymerase in susceptible strains of Mycobacterium tuberculosis, but not in mammalian cells. Within therapeutic concentrations, rifapentine exhibits a bactericidal effect against both extracellular and intracellular bacteria M. tuberculosis.

In the treatment of TB, resistant bacteria present in small numbers among a large population of susceptible organisms can rapidly multiply and become dominant. The sensitivity of M. tuberculosis isolates to isoniazid, rifampicin, pyrazinamide, ztambutol, rifapentine, and other anti-tuberculosis drugs should be determined. If test results show resistance to any of these drugs and the patient is not responding to treatment, then the therapy regimen should be changed. There is a high level of M. tuberculosis cross-resistance between rifapentine and other rifamycins, whereas M. tuberculosis bacteria resistant to rifampicin and rifapentine are not cross-resistant to other non-rifamycin anti-TB drugs such as isoniazid and streptomycin.

Bioavailability after taking a single dose of 600 mg is 70%. After taking 600 mg, the maximum plasma concentration of rifapentine is reached after 5-6 hours. The degree of binding to plasma proteins of rifapentine and its active metabolite 25-deacetylrifapentine is 97.7 and 93.2%, respectively. 17% of rifapentine and related compounds are excreted in the urine. The half-life of rifapentine is approximately hours.

It is prescribed in complex therapy, in combination with other anti-tuberculosis drugs that do not belong to the rifamycin group.

Hypersensitivity to rifamycins;

Diseases of the liver and gastrointestinal tract in the acute phase;

In patients with severe atherosclerosis;

Inside, 1 time per day, regardless of the meal. The daily dose of rifapentine is 10 mg/kg body weight per week.

Simultaneously with rifapentine in the acute phase of treatment, first-line anti-TB drugs are prescribed: isoniazid, ethambutol, pyrazinamide in doses corresponding to the instructions for the use of these drugs.

If necessary, streptomycin is administered intramuscularly, or if it is resistant, kanamycin.

Allergic reactions: fever, dermatitis, eosinophilia, anaphylactic shock.

From the gastrointestinal tract: nausea, vomiting, diarrhea. Increased activity of "liver" transaminases, drug-induced hepatitis, jaundice.

From the blood system: thrombocytopenia, leukopenia, anemia.

Symptoms: nausea, vomiting, diarrhea, increased activity of "liver" transaminases, hepatitis, jaundice, thrombocytopenia, leukopenia, anemia.

Treatment: gastric lavage, symptomatic therapy, the appointment of choleretic drugs, diuretics.

Rifapentine induces enzymes of the cytochrome P450 system; accelerates drug metabolism.

Pyrazinamide slows down the excretion of rifapentine.

Rifapentine can impart a reddish-orange color to urine, skin, and secreted fluids.

Patients taking rifapentine should not wear contact lenses. During treatment with rifapentine, it is necessary: ​​monthly blood and urine tests; determination of the activity of "liver" transaminases; bilirubin direct and indirect.

Rifapentine should not be combined with drugs belonging to the rifamycin group. Oral contraceptives in combination with rifapentine are ineffective. Other means of contraception should be used.

What is "Ref"?

The most popular drugs used in the treatment of tuberculosis are Rifampicin, Pyrazinamide, Ethambutol. This group is used together with Isoniazid. As a rule, such a treatment regimen is prescribed for those who fell ill for the first time and the body has not developed resistance to this medicine. For some people, it is enough to drink these pills for four months, and they forget about tuberculosis forever. But the whole next year they restore hearing, vision, treat the liver and stomach.

"Rifampicin", for example, is also very toxic, it strongly irritates the mucous membrane, so it should be washed down with as much water as possible. If, God forbid, this capsule gets stuck in the esophagus and sticks to its wall, then in ten minutes you will feel as if you ate burning coals from a barbecue grill for breakfast. But this antibiotic kills a huge number of a wide variety of bacteria.

Well, when you need a new watch, go to www.watcheshop.ru. There you will find not only cheap and simple watches, but also many branded and prestigious watches for every taste.

Please check with your doctor before following any advice.

Rifampicin

Description current as of 06/06/2015

• Latin name: Rifampicin
• ATX Code: J04AB02
• Active ingredient: Rifampicin
• Manufacturer: North Star (Russia), Kraspharma (Russia), Pharmsintez (Russia), Omela (Russia)

Compound

One ampoule contains 150, 300, 450 or 600 mg of the active ingredient rifampicin. Additional elements are: ascorbic acid, sodium sulfite

One capsule contains 150 or 300 mg of the active ingredient.

Release form

Capsules and lyophilisate for solution for infusion.

pharmachologic effect

Semi-synthetic antibiotic. It has anti-tuberculosis and antibacterial action.

Pharmacodynamics and pharmacokinetics

Low concentrations of the drug have a bactericidal effect on chlamydia, mycobacterium tuberculosis, rickettsia, legionella, mycobacterium leprosy. High concentrations of the drug are active against gram-negative flora.

Rifampicin is a first-line anti-tuberculosis drug. High activity is observed when exposed to staphylococci, clostridia, gonococci, meningococci. The drug acts on extracellular, as well as intracellularly located bacteria.

The mechanism of action is based on the suppression of the RNA polymerase of microorganisms. Cross-resistance with other antibacterial agents is not recorded. With monotherapy with a drug, a rapid development of the selection of microorganisms for an antibiotic is observed.

Indications for the use of Rifampicin

The drug is used as part of combination therapy for all forms of tuberculosis, for leprosy. With multibacillary leprosy, the antibiotic is prescribed together with dapsone.

What other indications are there for use? The drug is prescribed for brucellosis, infectious diseases, meningococcal meningitis.

Contraindications

The medicine is not used for breastfeeding, jaundice, intolerance to the main substance, infants, with severe forms of cardiopulmonary insufficiency, with kidney pathology, infectious hepatitis. During pregnancy, Rifampicin is used for "vital" indications.

Side effects of Rifampicin

Digestive tract: pseudomembranous enterocolitis, vomiting, anorexia, nausea, elevated liver enzymes, hepatitis, hyperbilirubinemia, diarrhea, erosive gastritis.

Nervous system: disorientation, decreased visual acuity, headache, ataxia.

Genitourinary system: interstitial nephritis, nephronecrosis.

Perhaps the development of hyperuricemia, myasthenia gravis, leukopenia, allergies, exacerbation of gout, dysmenorrhea, porphyria infusion.

With irregular use of the drug, a flu-like condition and such side effects may develop: myalgia, chills, fever, dizziness, headaches.

Instructions for use Rifampicin (Method and dosage)

The drug is taken orally, injected intravenously.

Rifampicin tablets, instructions for use

Take half an hour before meals, on an empty stomach.

In the treatment of tuberculosis, this drug must be combined with other anti-tuberculosis drugs (ethambutol, pyrazinamide, isoniazid). Adults are prescribed 10 mg / kg every 24 hours. Not more than 1200 mg per day, children - not more than 600 mg.

The combination of tuberculosis with HIV, lesions of the tuberculous process of the spinal column with neurological symptoms, disseminated tuberculosis, tuberculous meningitis: 2 months Rifampicin is used with pyrazinamide, isoniazid, ethambutol, streptomycin, for the next 7 months the antibiotic is combined with isoniazid.

If mycobacteria is found in sputum, pulmonary tuberculosis, the patient is prescribed one of three antimicrobial therapy regimens used in combination with other drugs.

Multibacillary leprosy (borderline, lepromatous, mixed): 600 mg once a month with dapsone 100 mg once a day and clofazimine (300 mg once a month, 50 mg daily).

Pausibacillary types of leprosy (borderline tuberculoid, simple tuberculoid): once a month 600 mg together with dapsone 100 mg daily, the course of therapy is designed for half a year.

Brucellosis therapy: once 900 mg on an empty stomach in morning time together with doxycycline, the course is designed for 45 days.

Prevention of meningococcal meningitis: every 12 hours 600 mg, course for 2 days.

Solution use

In / in adults appoint 600 mg per day, children 10 mg per kg once a day. The maximum dose for intravenous administration is 600 mg.

Overdose

Manifested by confusion, convulsive syndrome, pulmonary edema.

Gastric lavage, forced diuresis, intake of enterosorbents are necessary.

Interaction

Rifampicin reduces the activity of digitalis preparations, oral hypoglycemic drugs, anticoagulants, contraceptives, antiarrhythmic drugs (tocainide, pyrmenol, disopyramide, mexiletine, quinidine), phenytoin, dapsone, glucocorticosteroids, ketoconazole, dloramphenicol, sex hormones, benzodiazepines, nortriptyline, cyclohexobarine , epalapril, BMKK, beta-blockers, azathioprine (rifampicin is able to accelerate metabolism due to the induced induction of certain enzymes of the hepatic system).

Ketoconazole, anticholinergics, opiates, antacids reduce the bioavailability of the antibiotic.

With the simultaneous administration of pyrazinamide or isoniazid, the hepatotoxic effect is enhanced.

PAS preparations can be administered after 4 hours after the use of rifampicin to prevent absorption.

Terms of sale

Storage conditions

In a dark, dry place inaccessible to children at a temperature not exceeding 25 degrees Celsius.

Best before date

No more than two years.

special instructions

Antibacterial therapy can cause urine, tears, feces, sweat, skin, and sputum to become reddish. Permanent staining of contact lenses is possible.

Intravenous infusions of rifampicin are administered under supervision blood pressure. Long-term therapy leads to the formation of phlebitis. For the prevention of resistance, the drug is used in combination with other antibiotics, antimicrobial agents.

When registering a flu-like syndrome (without bronchospasm, hemolytic anemia, shortness of breath, renal failure, shock, thrombocytopenia) in patients who take medication according to an intermittent regimen, the attending physician should consider switching to a daily antibiotic. In this case, the dose increase is slow, titration takes 3-4 days. Regular monitoring of the state of the renal system is required, the use of glucocorticosteroids is possible.

Rifampicin during pregnancy is used exclusively for health reasons. The appointment of an antibiotic in the last days of pregnancy can cause bleeding in the newborn, as well as postpartum hemorrhage in the mother. In such cases, the appointment of vitamin K is recommended. Women during the period of antibiotic therapy should be reliably protected from pregnancy.

When carrying out the prevention of bacillus carriers of meningococcus, strict control over the group is required for the timely detection of symptoms in the development of resistance to an antibacterial drug.

Long-term therapy requires regular monitoring of the state of the hepatic system, peripheral blood.

The drug affects the levels of vitamin B12 and folic acid in blood serum.

Rifampicin - instructions for use, analogues, reviews, price

Antibiotic Rifampicin

Release form

• Tablets of 150, 300, 450, 600 mg pcs. packaged;
• Capsules 150, 300, 450, 600 mg 20, 30, 100 pcs. packaged;
• Capsules for children 50 mg - 30 pcs. packaged;
• Powder for solution for intravenous administration in 150 mg ampoules - 10 ampoules per pack;
• Ear drops with Rifampicin Otofa (in 1 ml - 26 mg of Rifampicin) - in 10 ml bottles.

Candles with Rifampicin can be prepared at the pharmacy by prescription; suppositories are not produced in a factory way.

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);
• osteomyelitis;
• 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);
• kidney failure;
• liver failure;
• pregnancy;
• children's infancy.

For intravenous administration of Rifampicin, contraindications are:

• 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; oral thrush; hepatitis with increased activity of liver enzymes and bilirubin levels; inflammation of the pancreas (pancreatitis).
• From the nervous system: headaches, blurred vision, ataxia (gait disturbance) and disorientation in space.
• From the side of the cardiovascular 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 genitourinary system: inflammation of the kidneys, menstrual irregularities, acute renal failure.
• Allergic reactions: rashes like urticaria, pruritus, bronchospasm, lacrimation; increase in the number of eosinophils in the blood; temperature increase; edema 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.

The risk of adverse reactions increases with the simultaneous use of Rifampicin with Isoniazid and other drugs with toxic effect on the liver; in the presence of alcoholism in a patient; with prolonged use.

Treatment with Rifampicin

Rifampicin can be taken by mouth and given intravenously. Inside take tablets or capsules Zamin. before meals.

For tuberculosis, the average daily dose is 450 mg for adults (orally and intravenously in 1 dose). The dose may be increased to 600 mg. The highest daily dose for adult patients is 1.2 g (1200 mg). The doctor determines the duration of the treatment course depending on the form of tuberculosis, the severity of the course and dynamic changes in the course of treatment. The duration of application sometimes reaches 1 year. During the course of treatment, the sensitivity of the pathogen to Rifampicin should be checked.

a) a daily dose of 450 mg, divided into 2-3 doses, is prescribed for 2-3 weeks; courses of treatment with interruptions for 2-3 months are carried out for 1-2 years;

b) the same dose 3 days a week for 6 months.

Rifampicin overdose

To provide assistance, gastric lavage, heavy drinking and forced diuresis are used, Activated carbon inside.

Rifampicin for children

Use during pregnancy and lactation

Compresses from Rifampicin with Dimexide

drug interaction

• Rifampicin reduces the effectiveness of tableted indirect anticoagulants (drugs that reduce blood clotting), tableted antihyperglycemic drugs, Theophylline, digitalis preparations, Disopyramide, Verapamil, Enalapril, Quinidine, Chloramphenicol, Mexiletine, Dapsone, glucocorticosteroids, Cimetidine, antifungals, hormonal contraceptives, beta - adrenoblockers, Cyclosporine, benzodiazepines, Hexobarbital, Nortriptyline, Diazepam, sex hormones, Bisoprolol, Nifedipine, cardiac glycosides, Haloperidol, Diltiazem, Azathioprine, Thyroxine, Fluvastatin. With this in mind, it is necessary to adjust the dosages of these drugs while taking Rifampicin and after its withdrawal.
• Antacids, Ketoconazole, PAS, opiates reduce the absorption and activity of Rifampicin.
• It is undesirable to prescribe Rifampicin to HIV-infected patients together with Indinavir, Nelfinavir, as their blood concentrations decrease.
• The concentration of Rifampicin in the blood is increased by Biseptol and Probenecid when they are administered together.
• The combined use of Rifampicin with Pyrazinamide or Isoniazid increases the risk of developing toxic effects on the liver, the occurrence of leukopenia.

Rifampicin analogs

Drugs similar in action (analogues): Cycloserine, Tricox, Capreomycin, Florimycin sulfate.

Reviews about the drug

The price of the drug in Russia and Ukraine

• Capsules of 150 mg - from 13 to 63 rubles. (depending on the manufacturer, the number of capsules and the city).
• Ampoules with powder for injections of 150 mg - from 595 to 801 rubles. (depending on the manufacturer, the number of capsules and the city).
• Otofa ear drops 10 ml - from 200 rubles.

Rifapex

Producer: JSC "Chemical-Pharmaceutical Plant "AKRIKHIN" Russia

ATC code: J04AB05

Release form: Solid dosage forms. Pills.

Indications for use: Tuberculosis.

General characteristics. Compound:

Active substance: 150 mg rifapentine.

Auxiliary substances: microcrystalline cellulose (RANQ PH 102), sodium carboxymethyl starch, pregelatinized starch, sodium ascorbate, sodium lauryl sulfate, disodium edetate, hyprolose (Klucel EXF), colloidal silicon dioxide (Aerosil 200), calcium stearate. Shell: hypromellose (Methocel E5 LVP ), hypromellose (Methocel E15 LVP), macrogol 4000, titanium dioxide, talc, iron dye red oxide (Sicopharm Red 30), simethicone emulsion (30%).

Pharmacological properties:

Pharmacodynamics. Rifapentine is a derivative of rifamycin and has approximately the same microbiological activity profile as rifampicin, inhibiting DNA-dependent RNA polymerase in susceptible strains of Mycobacterium tuberculosis, but not in mammalian cells. Within therapeutic concentrations, rifapentine exhibits a bactericidal effect against both extracellular and intracellular bacteria M. tuberculosis.

In the treatment of TB, resistant bacteria present in small numbers among a large population of susceptible organisms can rapidly multiply and become dominant. The sensitivity of M. tuberculosis isolates to isoniazid, rifampicin, pyrazinamide, ethambutol, rifapentine, and other anti-tuberculosis drugs should be determined. If test results show resistance to any of these drugs and the patient is not responding to treatment, then the therapy regimen should be changed. There is a high level of M. tuberculosis cross-resistance between rifapentine and other rifamycins, whereas M. tuberculosis bacteria resistant to rifampicin and rifapentine are not cross-resistant to other non-rifamycin anti-TB drugs such as isoniazid and streptomycin.

Pharmacokinetics. Bioavailability after taking a single dose of 600 mg is 70%. After taking 600 mg, the maximum plasma concentration of rifapentine is reached after 5-6 hours. The degree of binding to plasma proteins of rifapentine and its active metabolite 25-deacetylrifapentine is 97.7 and 93.2%, respectively. 17% of rifapentine and related compounds are excreted in the urine. The half-life of rifapentine is approximately hours.

Indications for use:

Newly diagnosed drug-susceptible tuberculosis (all forms); V acute stage tuberculosis and in the aftercare stage. Rifapentine is prescribed in complex therapy, in combination with other anti-TB drugs that do not belong to the rifamycin group.

Dosage and administration:

Inside, 1 time per day, regardless of the meal. The daily dose of rifapentine is 10 mg/kg body weight per week. Simultaneously with rifapentine in the acute phase of treatment, first-line anti-TB drugs are prescribed: isoniazid, ethambutol, pyrazinamide in doses corresponding to the instructions for the use of these drugs.

If necessary, streptomycin is administered intramuscularly, or if it is resistant, kanamycin.

If one of the drugs prescribed with rifapentine is intolerant, it can be replaced with prothionamide, cycloserine, or levofloxacin.

Application Features:

Rifapentine can impart a reddish-orange color to urine, skin, and secreted fluids. Patients taking rifapentine should not wear contact lenses.

During treatment with rifapentine, it is necessary: ​​monthly blood and urine tests; determination of the activity of "liver" transaminases; bilirubin direct and indirect.

Clinical material for the cultivation of mycobacteria and the determination of their sensitivity should be taken before the start of treatment, as well as during treatment after a two-three-day break in treatment and in order to monitor the therapeutic response.

Rifapentine should not be combined with drugs belonging to the rifamycin group.

Oral contraceptives in combination with rifapentine are ineffective. Other means of contraception should be used.

When prescribing prednisolone, cardiac glycosides (digitalis derivatives), phenazepam together with rifapentine, a decrease in the concentration of these drugs should be taken into account.

Side effects:

Allergic reactions: fever, dermatitis, eosinophilia, anaphylactic shock. From the gastrointestinal tract: nausea, vomiting, diarrhea. Increased activity of "liver" transaminases, drug-induced hepatitis, jaundice.

Interaction with other drugs:

Rifapentin induces enzymes of the cytochrome P 450 system; accelerates drug metabolism. Pyrazinamide slows down the excretion of rifapentine.

Isoniazid with rifapentine, protionamide with rifapentine - synergists; their combination increases antimicrobial activity.

Concomitant alcohol intake may increase the risk of liver damage.

Contraindications:

• Hypersensitivity to rifamycins.
• Diseases of the liver and gastrointestinal tract in the acute phase.
• Pregnancy, lactation.
• Thrombophlebitis.
• Children under 12 years old.

In patients with severe atherosclerosis,

With hepatitis B and C.

Overdose:

Treatment: gastric lavage, symptomatic therapy, the appointment of choleretic drugs, diuretics.

Storage conditions:

In a dry place, at a temperature not exceeding 25 ° C. Keep out of the reach of children. Do not use after the expiry date stated on the packaging. With rock shelf life - 2 years.

Leave conditions:

Package:

Film-coated tablets, 150 mg. 8 tablets in an aluminum/aluminum strip laminated with polyethylene. 1 or 8 strips are placed in a cardboard box along with instructions for use.

100 tablets in a plastic bag, followed by an investment in a high-density polyethylene container along with instructions for use.

Packaging for hospitals. 100 or 500 tablets in a plastic bag, followed by an investment in a high-density polyethylene container, along with instructions for use.

Rifampicin is a semi-synthetic broad-spectrum antibiotic with bactericidal properties; first-line anti-tuberculosis drug.

Release form and composition

Dosage forms of Rifampicin:

• Capsules: #1, orange-red to dark red; the contents of the capsules are a powder from light red to brown-red with white patches (10 pcs. in a blister pack of aluminum foil and polyvinyl chloride film, in a carton pack of 1, 2 or 10 packs; for hospitals - in a carton box of 150 packs );
• Lyophilisate for solution for infusion: red to brick-red powder (150, 300 and 600 mg each in an analytical class III glass vial sealed with a butyl gray stopper and a combined aluminum cap (Flip off type); in a carton box 1 bottle; in a carton box 5 or 10 vials; 1 vial with the preparation complete with 1 solvent ampoule: 10 ml each for a dose of 600 mg, 5 ml each for a dose of 150 and 300 mg; in a blister pack made of aluminum printed varnished foil and film polyvinyl chloride, 1 set; in a cardboard pack 1 pack, packs are placed in a group package).

1 capsule contains:

• Active substance: rifampicin (in terms of 100% substance) - 150 mg;
• Additional components: calcium stearate, magnesium hydroxycarbonate, lactose monohydrate;
• Hard gelatin shell: propyl parahydroxybenzoate, gelatin, methyl parahydroxybenzoate, glycerol (glycerin), brilliant blue E-133, sodium lauryl sulfate, titanium dioxide, charming red E-129, purified water, quinoline yellow E-104.

1 bottle with lyophilisate contains:

• Active substance: rifampicin - 150, 300 and 600 mg;
• Additional components: sodium hydroxide, sodium formaldehyde sulfoxylate dihydrate.

Solvent: water for injection, solvent for the preparation of dosage forms for injection.

Indications for use

• Tuberculosis, all forms different localization(as part of combination therapy);
• Leprosy in combination with dapsone and in addition to the solution - with clofazimine (solution in combination with dapsone - only for patients over 18 years of age);
• Infectious diseases caused by microorganisms sensitive to rifampicin (in case of resistance to other antibacterial agents, as well as in combination antimicrobial therapy, after excluding the diagnosis of leprosy and tuberculosis);
• Brucellosis - as part of complex treatment with an antibiotic of the tetracycline group (doxycycline).

Capsules are additionally used for prophylaxis in persons who have been in close contact with patients with meningococcal meningitis, as well as in Neisseria meningitidis bacillus carriers.

Contraindications

• Chronic renal failure;
• Infectious hepatitis (including the period for 1 year after recovery);
• Jaundice;
• Pulmonary heart failure II-III degree;
• Age up to 2 months - for solution, up to 3 years - for capsules;
• The period of breastfeeding;
• Hypersensitivity to the components of the drug.

With caution, the drug should be used in children from 2 to 12 months (for solution), persons who abuse alcohol, malnourished patients, as well as in liver diseases (including history data).

During pregnancy, Rifampicin is prescribed only for health reasons. When using the solution in the last weeks of pregnancy, bleeding may develop in the newborn and in the mother in the postpartum period. In this case, vitamin K is recommended.

Method of application and dosage

Lyophilisate for solution for infusion
The drug is used intravenously.

To prepare an infusion solution, 150 mg of lyophilisate is diluted with 2.5 ml of water for injection, vigorously shaken until completely dissolved, and 125 ml of isotonic (5%) dextrose solution is added to the resulting solution. Infusion is carried out at a rate of 60-80 drops per minute.

Intravenous drip administration of Rifampicin is recommended for severe purulent-septic processes, common and acutely progressive forms. destructive tuberculosis lungs, in cases where it is necessary to quickly achieve high concentrations of the agent in the focus of infection and in the blood, as well as in case of poor tolerance or the impossibility of oral administration.

For the treatment of tuberculosis, the drug is used in combination with isoniazid, pyrazinamide, ethambutol or streptomycin. Adults with a body weight of less than 50 kg are administered 450 mg of the drug per day, with a weight of more than 50 kg - 600 mg. For children, rifampicin is prescribed per day at the rate of 10-20 mg/kg of body weight. The maximum allowable daily dose should not exceed 600 mg. The duration of the course of intravenous infusions is set taking into account the tolerability of the drug and can be 30 days or more (with a further transition to taking capsules). The total duration of treatment for tuberculosis with a drug depends on its therapeutic effect and can be up to 1 year old.

In the treatment of borderline, borderline-lepromatous and lepromatous types of leprosy, the solution is administered to adults once a month, 600 mg in combination with clofazimine and dapsone. The duration of treatment is at least 2 years. In the treatment of tuberculoid and borderline tuberculoid types of leprosy, the drug is prescribed once a month in the same dose, only in combination with dapsone. Course - 6 months.

In infectious diseases caused by microorganisms sensitive to rifampicin, the solution is used in combination with other antimicrobial agents. Adults are prescribed a dose of 600-1200 mg per day, children - at the rate of 10-20 mg / kg, divided into 2-3 injections. The course of treatment is determined individually and can vary from 7 to 14 days.

For the treatment of brucellosis, adults are prescribed 900 mg of rifampicin per day in combination with doxycycline, the course is 45 days.

Capsules
Rifampicin capsules are taken orally, on an empty stomach, 30 minutes before meals.

In the treatment of tuberculosis, the drug is combined with anti-tuberculosis drugs (streptomycin, ethambutol, pyrazinamide, isoniazid) in daily dose depending on the age and weight of the patient:

• Adults, with body weight<50 кг – 450 мг;
• Adults weighing ≥50 kg - 600 mg;
• Children over 3 years old - 10 mg / kg body weight, but not more than 450 mg.

It is allowed to divide the daily dose into 2 doses (in case of poor tolerance).

For the treatment of tuberculous meningitis, disseminated tuberculosis, tuberculous lesions of the spine with neurological manifestations, when HIV infection is combined with tuberculosis, the drug is used daily for 9 months: during the first 2 months, combined with ethambutol, pyrazinamide, isoniazid (or streptomycin), the next 7 months with isoniazid.

With pulmonary tuberculosis and the detection of mycobacteria in sputum, the following 3 treatment regimens are used (the course of each is 6 months):

• First 2 months - as recommended above; the next 4 months - daily, combining with isoniazid;
• First 2 months - as recommended above; the next 4 months - every week 2-3 times, in combination with isoniazid;
• All six months - 3 times each week, combined with ethambutol, pyrazinamide, isoniazid (or streptomycin).

When using Rifampicin 2-3 times a week, as well as in case of treatment failure or the development of exacerbations of the lesion, it is required to take it under medical supervision.

For the treatment of multibacillary types of leprosy, the drug is prescribed for adults 1 time per month, 600 mg per day in combination with dapsone (100 mg 1 time per day), for children - 10 mg / kg in combination with dapsone at a dose of 1-2 mg / kg / day. day The course of therapy for borderline, lepromatous and borderline-lepromatous types of leprosy is at least 2 years, tuberculoid and borderline-tuberculoid - 6 months.

In the treatment of infectious diseases caused by susceptible microorganisms, as part of combination therapy, adults take the drug at 600-1200 mg per day, children - 10-20 mg / kg / day. (not exceeding 450 mg per day), divided into two times.

With brucellosis, 900 mg of rifampicin is taken once a day in combination with doxycycline, the course is 45 days.

In order to prevent meningococcal meningitis, adults are prescribed 600 mg, children - 10 mg / kg, every 12 hours for 2 days.

When prescribing doses exceeding 600 mg per day, patients with impaired renal excretory function require dose adjustment.

Side effects

• Digestive system: erosive gastritis, loss of appetite, nausea, diarrhea, vomiting, pseudomembranous colitis, hyperbilirubinemia, increased activity of "liver" transaminases in the blood serum, hepatitis, hyperbilirubinemia;
• Nervous system: disorientation, ataxia, decreased visual acuity, headache;
• Allergic reactions: fever, arthralgia, bronchospasm, angioedema, eosinophilia, urticaria;
• Urinary system: interstitial nephritis, nephronecrosis;
• Others: exacerbation of gout, hyperuricemia, myasthenia gravis, induction of porphyria, dysmenorrhea, leukopenia.

In case of irregular use or when the course is resumed after a break, skin reactions, flu-like syndrome (myalgia, dizziness, headache, chills, fever), thrombocytopenic purpura, hemolytic anemia, acute renal failure may occur.

Overdose symptoms: convulsions, confusion, lethargy, pulmonary edema. In this condition, symptomatic therapy is prescribed, forced diuresis.

special instructions

During drug therapy, staining of the skin, lacrimal fluid, sweat, sputum, urine, feces in orange-red color is observed. Permanent staining of soft contact lenses is also possible.

When conducting intravenous infusion, it is necessary to control blood pressure; in the case of prolonged administration, phlebitis may develop.

Rifampicin must be used in combination with other antimicrobial agents to prevent the emergence of microbial resistance.

If bronchospasm, hemolytic anemia, uncomplicated thrombocytopenia, shortness of breath, flu-like syndrome, renal failure, shock occur against the background of an intermittent regimen, it is recommended to consider the possibility of daily administration of the drug. In such cases, the dose should be slowly increased, starting with 75-150 mg on the first day, and gradually increasing over 3-4 days to the required therapeutic. If the above complications persist after adjusting the dose, drug therapy is canceled.

During the period of treatment, it is necessary to monitor the activity of the kidneys, additional use of glucocorticosteroids may be required.

Women of reproductive age using the drug should use reliable methods of contraception.

When taking Rifampicin for prophylactic purposes in bacilli-carriers of meningococcus, it is necessary to strictly monitor the patient's condition for the timely detection of signs of the disease in case of development of resistance to the agent.

During therapy, microbiological methods for determining the level of vitamin B 12 and folic acid in the blood serum cannot be used.

drug interaction

Possible interaction reactions when combining rifampicin with other drugs:

• Ketoconazole, cholinesterase inhibitors, opiates, antacids (when taken orally) - the bioavailability of rifampicin in the form of capsules decreases;
• Statins - the level of their content in the blood decreases, which helps to reduce their hypocholesterolemic effects;
• Pyrazinamide and / or isoniazid - the risk of an increase in the frequency and severity of manifestations of functional liver disorders in patients with its previous lesion is aggravated;
• HIV protease inhibitors - their concentration in the blood decreases;
• Azathioprine, cyclosporine, itraconazole, ketoconazole, chloramphenicol, theophylline, sex hormones, benzodiazepine, nortriptyline, hexobarbital, phenytoin, dapsone, glucocorticosteroids, antiarrhythmic drugs (tocainide, mexiletine, quinidine, pyrmenol, disopyramide), cardiac glycosides, hormonal contraceptives, indirect coagulants, blockers of "slow" calcium channels, beta-blockers, cimetidine, enalapril, oral hypoglycemic agents - the activity of these drugs decreases.

Terms and conditions of storage

Store in a place protected from moisture and light, out of the reach of children, at a temperature not exceeding 25 °C.

Shelf life - 2 years.