Rifampicin
Rifampicin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Rifampicin
ATX code: J04AB02
Active ingredient: rifampicin (rifampicin)
Manufacturer: Virend International, LLC (Russia), Belmedpreparaty, RUP (Republic of Belarus), Pharmasintez, JSC (Russia), Valenta Pharm, PJSC (Russia), Severnaya Zvezda, JSC (Russia), Krasfarma, JSC (Russia), Sandzhivani Paranteral Limited (India)
Description and photo update: 03.10.2019
Prices in pharmacies: from 399 rubles.
Buy
Rifampicin is a semi-synthetic antibiotic with anti-tuberculosis and a broad spectrum of antibacterial action.
Release form and composition
Dosage forms of Rifampicin:
- lyophilisate for the preparation of a solution for infusion: a powdery hygroscopic mass of brown-red color (in ampoules: 150 ml, in a cardboard box 5 or 10 pcs. complete with an ampoule knife; 5 pcs. in contoured plastic trays, in a cardboard box 1 or 2 pallets or in a cardboard box 20, 25, 50, 100, 200 pallets; 5 pcs. In a blister strip, in a cardboard bundle 1 or 2 packages or in a cardboard box 20, 25, 50, 100, 200 packages; in vials: 150, 300 or 600 mg, in a cardboard box 1, 5 or 10 pcs.; 450 mg each, in a cardboard box 1, 10, 50 or 100 pcs.; 150 or 300 mg each, in a cardboard box 1 bottle included with solvent (5 ml each in ampoules); 600 mg each, in a cardboard box 1 bottle complete with solvent (5 or 10 ml each in ampoules); 150, 300, 450 or 600 mg each: 5 pcs. in a contour plastic pallet,in a cardboard box 1 or 2, in a box - 10, 20 pallets; 5 pcs. in a contour acheikova packing, in a cardboard box 1 or 2, in a box - 10 or 20 packages; 600 mg, in a cardboard box of 50, 100 or 500 vials);
- capsules: hard gelatinous orange-red (No. 1) or red (No. 0), inside the capsules are red-brown or red powder with white splashes (150 mg each: 20 or 30 pcs. in dark glass jars, polymer jars or vials, in a cardboard box 1 jar, can or bottle; 150 or 300 mg each: in a plastic bag 500, 1000, 2000 or 5000 pcs., in a polyethylene can 1 package; 10 pcs. in a blister strip, in a cardboard box 2, 3, 5, 10 packs or in a cardboard box 150 packs with 150 mg capsules; 100 or 1000 pcs per pack).
Each pack also contains instructions for the use of Rifampicin.
The lyophilisate contains:
- active ingredient: rifampicin, in 1 vial - 150 mg, 300 mg, 450 mg or 600 mg, in 1 ampoule - 150 mg;
- auxiliary components: sodium sulfite, ascorbic acid, sodium hydroxide.
The capsule contains:
- active substance: rifampicin, in 1 capsule - 150 mg or 300 mg;
- auxiliary components: primogel (sodium carboxymethyl starch), microcrystalline cellulose, corn starch, colloidal silicon dioxide (aerosil grade A-300), basic magnesium carbonate, magnesium stearate;
- body and cap of capsules: gelatin, sodium lauryl sulfate, Ponso 4R E 124 dye, titanium dioxide, purified water;
- additionally as part of the shell: No. 1 - sunset yellow dye (E 110); No. 0 - dye azorubin (E 122).
Pharmacological properties
Pharmacodynamics
Rifampicin is a semi-synthetic antibiotic with a broad spectrum of action; it belongs to the number of first-line anti-tuberculosis drugs.
When used in low concentrations, it has a bactericidal effect on Legionella pneumophila, Mycobacterium tuberculosis, Mycobacterium leprae, Chlamydia trachomatis, Brucella spp., Rickettsia typhi, in high concentrations - on some gram-negative microorganisms.
The substance is characterized by high activity against Staphylococcus spp. (including penicillinase-forming and many methicillin-resistant strains), Clostridium spp., Streptococcus spp., Bacillus anthracis, as well as gram-negative coca (Neisseria gonorrhoeae, Neisseria meningitidis).
In high concentrations, Rifampicin has an effect on gram-positive bacteria. Shows activity against intracellular / extracellular microorganisms. Selectively inhibits DNA-dependent (deoxyribonucleic acid) RNA polymerase (ribonucleic acids) of sensitive microorganisms.
In the case of monotherapy, the selection of Rifampicin-resistant bacteria is noted relatively quickly. Cross-resistance with other antibacterial drugs (except for other rifamycins) does not develop.
Pharmacokinetics
The absorption of rifampicin when taken orally is fast; when used simultaneously with food, the absorption of the drug is reduced. When 600 mg is taken on an empty stomach, C max (maximum concentration of the substance) in the blood is 10 μg / ml, the time to reach it is from 2 to 3 hours. Binds to plasma proteins in the range from 84 to 91%. The substance is quickly distributed to tissues and organs (the highest concentration is observed in the kidneys and liver), penetrates into the bone tissue, the concentration in saliva is 20% of the plasma concentration. The apparent V d (volume of distribution) in adults and children is 1.6 and 1.1 l / kg, respectively.
With max with intravenous drip, it is observed towards the end of the infusion. Concentration at the therapeutic level is maintained for 8-12 hours, in relation to highly sensitive pathogens - within 24 hours. The connection with blood plasma proteins is from 80 to 90%. Rifampicin penetrates well into body fluids and tissues and is found in therapeutic concentrations in pleural exudate (accumulates between the membranes surrounding the lungs, in a protein-rich fluid), sputum, bone tissue, the contents of cavities (cavities in the lungs that are formed due to tissue death). The highest concentrations of rifampicin are found in kidney and liver tissues.
The substance penetrates through the blood-brain barrier only in the presence of inflammation of the meninges. Penetration of rifampicin through the placenta is noted (the plasma concentration in the fetus is 33% of that of the mother) and excretion in breast milk (children fed with breast milk receive up to 1% of the therapeutic dose of the drug).
Metabolism occurs in the liver with the formation of the metabolite 25-O-deacetylrifampicin, which exhibits pharmacological activity. It is an autoinducer (it helps to accelerate its metabolism in the liver), as a result of this, the systemic clearance after repeated administration increases from 6 l / h (after the first application) to 9 l / h. 80% of the dose is excreted in the bile as a metabolite, 20% - by the kidneys.
In case of impaired renal excretory function, the value of T 1/2 (half-life) increases only in cases where doses above 600 mg are used. It is excreted during hemodialysis and peritoneal dialysis.
With violations of hepatic function, an increase in the plasma concentration of the substance and an increase in T 1/2 are observed. Rifampicin resistance develops rapidly. Cross-resistance with other antibiotics is not observed (except for rifamycin).
Indications for use
The use of Rifampicin is indicated as part of antimicrobial combination therapy:
- tuberculosis - all forms and localizations;
- treatment of infectious diseases caused by microorganisms sensitive to the drug, but resistant to other antibiotics (after excluding the diagnosis of leprosy and tuberculosis);
- brucellosis, in combination with doxycycline (an antibiotic of the tetracyclines group);
- multibacillary types of leprosy (with the simultaneous use of dapsone and clofazimine).
In addition, Rifampicin capsules are prescribed to carriers of Neisseria meningitidis and, after close contact with patients with meningococcal meningitis, to prevent the disease.
Contraindications
Absolute for both dosage forms of the drug:
- pulmonary heart failure II – III degree;
- chronic renal failure;
- recent infectious hepatitis (less than 1 year), jaundice;
- the period of pregnancy (except when therapy is necessary for health reasons);
- period of breastfeeding;
- children's age up to 12 months;
- hypersensitivity to rifampicin, other rifamycins or one of the components of the drug.
Rifampicin in the form of a lyophilisate for the preparation of infusions is used with caution in malnourished patients when rifampicin therapy is resumed after a break, in patients prone to alcohol abuse, and if there is a history of liver disease.
Rifampicin, instructions for use: method and dosage
Lyophilisate for preparation of solution for infusion
The ready-made lyophilisate solution is intended for intravenous drip administration at a rate of 60–80 drops per minute.
A solution for intravenous administration is prepared by dissolving the lyophilisate in water for injection in the proportion: for 150 mg of the drug - 2.5 ml of water for injection. After complete dissolution of the lyophilisate, the solution is mixed with 125 ml of 5% dextrose solution.
Intravenous administration of Rifampicin is prescribed for the rapid creation of high concentrations in the focus of infection and in the blood in patients with rapidly progressive and widespread forms of destructive pulmonary tuberculosis, severe purulent-septic processes, for which oral administration of the drug is difficult or poorly tolerated.
Recommended dosage:
- tuberculosis, in combination with isoniazid, ethambutol, pyrazinamide, streptomycin (anti-tuberculosis drugs): adults - 450 mg per day with a body weight of up to 50 kg, 600 mg per day with a weight of 50 kg and above; children - the dose is determined at the rate of 10–20 mg per 1 kg of the child's weight per day. The duration of treatment depends on individual tolerance and can be 1 month or more. After stabilization of the patient's condition, the patient is transferred to receive Rifampicin inside, which can last up to 12 months. The maximum daily dose is 600 mg;
- lepromatous, borderline lepromatous or borderline type of leprosy: adults - 600 mg once a month in combination with clofazimine and dapsone, the minimum course of therapy is 24 months;
- tuberculoid or borderline tuberculoid type of leprosy: 600 mg once a month in combination with dapsone, duration of treatment - 6 months;
- infectious pathologies caused by microorganisms sensitive to rifampicin (with the simultaneous use of other antimicrobial agents): adults - 600–1200 mg per day, children - at the rate of 10–20 mg per 1 kg of body weight per day, the prescribed dose is divided by 2–3 introduction. The course of treatment is 7-14 days, it is set individually depending on the clinical effect;
- brucellosis: adults - 900 mg per day in combination with doxycycline, duration of treatment - 1.5 months.
With intact liver function and impaired renal excretory function, dose adjustment is required for conditions requiring more than 600 mg per day.
Capsules
Rifampicin capsules are taken orally 0.5 hours before meals.
Recommended dosage:
- tuberculosis (in combination with at least one of the anti-tuberculosis drugs - streptomycin, isoniazid, ethambutol, pyrazinamide): adult patients with a body weight of up to 50 kg - 450 mg each, with a body weight of 50 kg and more - 600 mg per day; children - at the rate of 10–20 mg per 1 kg of child's weight per day. Treatment is carried out for the first two months in combination with isoniazid, streptomycin or pyrazinamide and ethambutol, then 7 months in combination with isoniazid. The total duration of therapy for tuberculous meningitis, disseminated tuberculosis, spinal lesions with neurological manifestations, tuberculosis in combination with HIV infection with daily drug intake is 9 months. The daily dose is no more than 600 mg;
- pulmonary tuberculosis with mycobacteria in sputum: adults with a body weight of less than 50 kg - 450 mg, 50 kg and above - 600 mg per day; children - 10–20 mg per 1 kg of body weight per day. Treatment is prescribed according to one of the schemes with a duration of 6 months. During the first two months in combination with isoniazid, streptomycin or pyrazinamide and ethambutol, then 4 months in combination with isoniazid, taking it daily or (according to another scheme) 2-3 times a week. When choosing the next treatment regimen, the patient takes isoniazid, pyrazinamide and ethambutol or streptomycin 3 times a week for 6 months of using Rifampicin;
- multibacillary types of leprosy (lepromatous, borderline, borderline lepromatous): adults - 600 mg once a month in combination with a daily intake of 100 mg of dapsone and 50 mg of clofazimine, in addition to 300 mg of clofazimine once a month; children - 10 mg per 1 kg once a month in combination with taking dapsone at a dose of 1-2 mg per 1 kg per day (daily), 50 mg of clofazimine (every other day) and an additional 200 mg of clofazimine once a month. Duration of treatment is 24 months or more;
- Tuberculoid and borderline-tuberculoid type of leprosy: Rifampicin is taken once a month. Adults - 600 mg each (with 100 mg of dapsone daily); children - 10 mg per 1 kg of body weight (dapsone - 1-2 mg per 1 kg per day). The course of treatment is 6 months;
- infectious diseases: adults - 600-1200 mg, children - 10-20 mg per 1 kg per day, the dose is divided into 2 doses;
- brucellosis: 900 mg 1 time per day (in the morning before meals), in combination with doxycycline. The duration of treatment is 1.5 months;
- prevention of meningococcal meningitis: adults - 600 mg, children - 10 mg per 1 kg, newborns - 5 mg per 1 kg for two days every 12 hours.
Dose adjustment for patients with impaired renal excretory function and intact liver function is required only for pathologies with a dose of therapy above 600 mg per day.
It is recommended to take anti-tuberculosis drugs under the supervision of medical personnel.
Side effects
- nervous system: headache, disorientation, ataxia, decreased visual acuity;
- digestive system: nausea, vomiting, decreased appetite or anorexia, diarrhea, pseudomembranous colitis, hepatitis, erosive gastritis, hyperbilirubinemia, increased activity of liver enzymes in the blood serum;
- urinary system: interstitial nephritis;
- allergic reactions: urticaria, fever, angioedema (Quincke's edema), bronchospasm, eosinophilia, arthralgia;
- others: myasthenia gravis (muscle weakness), dysmenorrhea, leukopenia, induction of porphyria; possibly (against the background of irregular intake of Rifampicin or resumption of therapy after a break) - skin reactions, thrombocytopenic purpura, acute renal failure, hemolytic anemia, flu-like syndrome, which may be accompanied by headache, fever, chills, dizziness, myalgia.
In addition, the use of lyophilisate can cause nephronecrosis, exacerbation of gout, hyperuricemia, with prolonged intravenous administration - the development of phlebitis.
Overdose
The main symptoms: confusion, pulmonary edema, convulsions.
Therapy: symptomatic, forced diuresis is indicated.
special instructions
In order to prevent the development of microorganism resistance to rifampicin, the drug should be prescribed as part of combination therapy with other agents with antimicrobial action.
The patient should be warned about the effect of the drug, which affects the discoloration of the skin, sweat, sputum, urine, lacrimal fluid, soft contact lenses, feces - they acquire an orange-red tint.
The intravenous administration of the drug solution should be carried out under the control of blood pressure.
When symptoms of flu-like syndrome appear with an intermittent treatment regimen, the patient should be transferred to a daily intake of the drug. The transition begins with the appointment of 75-150 mg of rifampicin per day and within 3-4 days is brought to a therapeutic dose.
If the flu-like syndrome is complicated by shortness of breath, hemolytic anemia, thrombocytopenia, bronchospasm, renal failure, shock Rifampicin is canceled.
Treatment should be accompanied by monitoring of renal function, if necessary, additional use of glucocorticosteroids is indicated.
During the period of Rifampicin therapy, patients of childbearing age should use reliable methods of contraception (oral hormonal drugs for oral administration with the additional use of barrier contraceptives).
Rifampicin should be prescribed during pregnancy (especially in the first trimester) only in special cases when the expected benefit from therapy for the mother outweighs the potential threat to the fetus. Taking the drug in the last weeks of gestation can cause bleeding after childbirth in the mother and newborn, vitamin K is prescribed for treatment.
Due to the risk of resistance to rifampicin, prophylactic intake of capsules with bacilli carriers of meningococcus must be accompanied by regular monitoring of the patient's condition for timely detection of symptoms of the disease.
With long-term treatment, the patient should systematically monitor liver function and peripheral blood parameters. Against the background of rifampicin, microbiological methods for the determination of vitamin B12 and folic acid in serum cannot be used.
The use of dapsone in combination therapy is indicated only for patients over 18 years of age.
Influence on the ability to drive vehicles and complex mechanisms
During the period of therapy, patients are advised to refrain from driving vehicles, complex mechanisms and engaging in potentially hazardous activities that require speed of psychomotor reactions and high concentration of attention.
Application during pregnancy and lactation
- pregnancy: Rifampicin can be used exclusively for health reasons;
- lactation period: therapy is contraindicated.
Pediatric use
Rifampicin is not recommended for patients under 12 months of age. For newborns and premature babies, the drug can be prescribed by a doctor only if absolutely necessary.
With impaired renal function
In chronic renal failure, Rifampicin is contraindicated.
For violations of liver function
In patients with jaundice, as well as in patients who have recently undergone infectious hepatitis (less than a year), Rifampicin is contraindicated.
The drug in the form of a lyophilisate with a burdened history of liver disease should be used with caution.
Drug interactions
With simultaneous use with Rifampicin, oral hypoglycemic agents, indirect anticoagulants, hormonal contraceptives, antiarrhythmic drugs (pyrmenol, quinidine, disopyramide, tocainid, mexiletine), cardiac glycosides, glucocorticosteroids, phenytodiex, dapsalinone, are reduced. theophylline, cyclosporine, ketoconazole, chloramphenicol, itraconazole, cimetidine, beta-blockers, azathioprine, slow calcium channel blockers, enalapril.
Combination therapy with isoniazid and / or pyrazinamide contributes to a more frequent development of severe liver dysfunction than rifampicin monotherapy in patients with a history of liver disease.
With concomitant therapy, statins decrease their concentration in the blood, causing a decrease in the cholesterol-lowering effect.
The bioavailability of rifampicin decreases when capsules are combined with antacids, opiates, anticholinergics, and ketoconazole.
Para-aminosalicylic acid medicines containing bentonite can interfere with the absorption of the drug, so they should be taken only 4 hours after taking the capsules.
Analogs
Analogues of Rifampicin are: Rifampicin-Ferein, Rifampin, Makox, R-Tsin, Rifacin, Rimpin, Rifampicin-Binergia, Eremfat.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 25 ° C.
Protect the lyophilisate from light.
Shelf life: lyophilisate - 2 years, capsules - 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Rifampicin
Reviews of Rifampicin are predominantly positive. The advantages are considered to be a wide range of applications and an affordable cost. There are reports of the development of adverse reactions.
Price for Rifampicin in pharmacies
The approximate price for Rifampicin is: lyophilisate (10 bottles) - 445 rubles, capsules (20 pcs.) - 45 rubles.
Rifampicin: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Rifampicin 150 mg lyophilisate for preparation of solution for infusion 10 pcs. 399 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
