AzitRus Forte
AzitRus Forte: 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. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: AzitRuse Forte
ATX code: J01FA10
Active ingredient: azithromycin (Azithromycin)
Manufacturer: JSC Sintez (Russia)
Description and photo update: 2019-10-07
Prices in pharmacies: from 102 rubles.
Buy
AzitRus Forte is a broad-spectrum antibiotic.
Release form and composition
The drug is produced in the form of film-coated tablets: oval, white or white-yellowish (3 or 6 pcs. In blister strip packs or polymer cans, in a cardboard box 1 pack of 6 tablets, or 1-2 packs of 3 tablets, or 1 can and instructions for the use of AzitRus Forte).
Composition of 1 tablet:
- active substance: azithromycin (in the form of a dihydrate) - 500 mg;
- auxiliary components (core): lactose monohydrate (milk sugar), povidone (low molecular weight medical polyvinylpyrrolidone 12 600 ± 2700, plasdon K-17), potato starch, calcium stearate, crospovidone (collidon CL-M) (type B), microcrystalline cellulose talc, starch;
- film shell: macrogol 4000 (polyethylene glycol 4000, polyethylene oxide 4000), titanium dioxide (titanium dioxide), hypromellose (hydroxypropyl methylcellulose).
Pharmacological properties
Pharmacodynamics
AzitRus Forte is a bacteriostatic antibacterial agent of a broad spectrum of action, a representative of the group of macrolides-azalides. The mechanism of its action is due to the ability to suppress protein synthesis of the microbial cell. By binding to the 50S subunit of the ribosome, the drug inhibits peptide translocase at the translation stage, and also suppresses and inhibits protein synthesis, as a result of which the reproduction and growth of bacteria is slowed down. In high concentrations, it exhibits bactericidal properties.
Active against the following microorganisms:
- aerobic gram-negative bacteria: Haemophilus parainfluenzae, Haemophilus influenzae, Neisseria gonorrhoeae, Moraxella catarrhalis, Legionella pneumophila, Pasteurella multocida;
- aerobic gram-positive bacteria: Streptococcus pyogenes, penicillin-sensitive strains of Streptococcus pneumoniae, methicillin-sensitive strains of Staphylococcus aureus;
- anaerobic bacteria: Fusobacterium spp., Porphyromonas spp., Prevotella spp., Clostridium perfringens;
- others: Borrelia burgdorferi, Chlamydia psittaci, Chlamydia pneumoniae, Chlamydia trachomatis, Mycoplasma hominis, Mycoplasma pneumoniae.
The following aerobic gram-positive microorganisms are able to develop resistance to the action of azithromycin: Streptococcus pneumoniae (strains with medium sensitivity to penicillin and penicillin-resistant strains).
Initial drug resistance is possessed by:
- anaerobic gram-positive microorganisms: Bacteroides fragilis;
- aerobic gram-positive microorganisms: Enterococcus faecalis, methicillin-resistant Staphylococcus strains.
The scale of the sensitivity of microorganisms to azithromycin:
- Staphylococcus: MIC (minimum inhibitory concentration) - no more than 1 mg / l;
- Streptococcus A, B, C, G: MIC - no more than 0.25 mg / l;
- Streptococcus pneumoniae: MIC - no more than 0.25 mg / l;
- Haemophilus influenzae: MIC - no more than 0.12 mg / l;
- Moraxella catarrhalis: MIC - no more than 0.5 mg / l;
- Neisseria gonorrhoeae: MIC - no more than 0.25 mg / l.
The scale of microorganism resistance to azithromycin:
- Staphylococcus: MIC - more than 2 mg / l;
- Streptococcus A, B, C, G: MIC - more than 0.5 mg / l;
- Streptococcus pneumoniae: MIC - more than 0.5 mg / l;
- Haemophilus influenzae: MIC - more than 4 mg / l;
- Moraxella catarrhalis: MIC - more than 0.5 mg / l;
- Neisseria gonorrhoeae: MIC - more than 0.5 mg / l.
Pharmacokinetics
After oral administration from the gastrointestinal tract, azithromycin is rapidly absorbed, since it is lipophilic and stable in an acidic environment. It is intensively distributed throughout the body, reaching the highest concentrations in tissues.
After application of AzitRus Forte at a dose of 500 mg C max (maximum plasma concentration) of azithromycin is 0.4 mg / l and is noted after 2.5-2.9 hours. Bioavailability - 37.5%. The drug penetrates well into soft tissues and skin, respiratory tract, tissues and organs of the urogenital tract (including the prostate gland).
Low binding to plasma proteins, as well as the ability of azithromycin to penetrate eukaryotic cells and concentrate in an environment with a low pH of the surrounding lysosome, determine the long half-life (T ½) of the drug and its higher concentrations in tissues (10–50 times higher than in blood plasma). This, in turn, explains the high plasma clearance and the large apparent volume of distribution (31.1 l / kg). Azithromycin is able to accumulate directly in lysosomes, which plays a key role in the elimination of intracellular pathogens. It is reliably known that phagocytes deliver the drug to the sites of infection, where it is released by phagocytosis. The concentration of azithromycin is on average 24–34% higher in the foci of infection than in healthy tissues, and correlates with the severity of inflammatory edema. Bactericidal concentrations of the drug persist for 5-7 days after the last dose of AzitRus Forte, so treatment can be carried out in short courses (3 and 5 days).
Azithromycin undergoes demethylation in the liver, resulting in the formation of pharmacologically inactive metabolites.
The drug is excreted from the body in two stages: the half-life (T ½) in the range from 8 to 24 hours after taking azithromycin is 14-20 hours, in the range from 24 to 72 hours - 41 hours. This allows you to take AzitRus Forte 1 time per day …
About 50% of the dose is excreted unchanged through the intestines, about 6% is excreted by the kidneys.
Indications for use
AzitRus Forte is prescribed for the treatment of infectious and inflammatory diseases caused by sensitive microorganisms:
- infections of the skin and soft tissues, including impetigo, erysipelas, secondarily infected dermatoses, moderate acne vulgaris;
- infections of ENT organs and upper respiratory tract, including otitis media, tonsillitis, sinusitis, pharyngitis;
- lower respiratory tract infections, including exacerbation of chronic bronchitis, acute bronchitis, pneumonia, including caused by atypical pathogens;
- urinary tract infections, including cervicitis and urethritis, caused by Chlamydia trachomatis.
AzitRus Forte is also used in the treatment of erythema migrans (erythema migrans) - the initial stage of Lyme disease (borreliosis).
Contraindications
Absolute:
- lactose intolerance, lactase or isomaltase deficiency, glucose-galactose malabsorption;
- severe renal / liver dysfunction;
- children under 12 years of age and / or body weight less than 45 kg;
- lactation period;
- the simultaneous use of ergotamine / dihydroergotamine;
- hypersensitivity to any component of the drug, erythromycin, other ketolides or macrolides.
Relative (AzitRus Forte tablets should be used with caution):
- diabetes;
- myasthenia gravis;
- mild to moderate renal dysfunction (CC> 40 ml / min);
- mild to moderate liver dysfunction (Child-Pugh grades A and B);
- the presence of proarrhythmogenic factors (especially in elderly patients), such as arrhythmia, clinically significant bradycardia, congenital or acquired prolongation of the QT interval, severe heart failure, imbalance in water and electrolyte balance (especially hypokalemia / hypomagnesemia);
- the combined use of class IA antiarrhythmic drugs (procainamide, quinidine), class III (amiodarone, dofetilide, sotalol), terfenadine, cisapride, fluoroquinolones (levofloxacin, moxifloxacin), antidepressants (citalopram), antipsychotics (pimozide);
- simultaneous administration of digoxin, warfarin, cyclosporin;
- pregnancy.
AzitRus Forte, instructions for use: method and dosage
AzitRus Forte tablets should be taken orally, between meals - 1 hour before or 2 hours after meals.
Recommended dosage regimens for adults and adolescents over 12 years of age (weighing over 45 kg):
- infections of ENT organs, respiratory tract, soft tissues and skin: 500 mg 1 time per day for 3 days;
- infections of the genitourinary system caused by Chlamydia trachomatis: 1000 mg once;
- erythema migrans: on the first day - 1000 mg once a day, during the next 4 days - 500 mg once a day.
If a dose is missed, AzitRus Forte should be taken as soon as possible, and the next and subsequent doses should be taken at intervals of 24 hours.
Side effects
The adverse reactions described below AzitRus Forte are classified as follows: very often - ≥ 10%, often - from ≥ 1% to <10%, infrequently - from ≥ 0.1% to <1%, rarely - from ≥ 0.01% to <0.1%, very rarely - <0.01%, unspecified frequency - available data do not allow to accurately determine the incidence of adverse effects:
- allergic reactions: infrequently - angioedema, hypersensitivity reactions; unknown frequency - anaphylactic reaction;
- infectious diseases: infrequently - candidiasis (including the mucous membrane of the oral cavity and genitals), rhinitis, pharyngitis, gastroenteritis, respiratory diseases, pneumonia; unknown frequency - pseudomembranous colitis;
- liver, biliary tract: infrequently - hepatitis; rarely - cholestatic jaundice, liver dysfunction; unspecified frequency - liver necrosis, liver failure (in rare cases with fatal outcome, mainly due to severe liver dysfunction), fulminant hepatitis;
- blood, lymphatic system: infrequently - eosinophilia, neutropenia, leukopenia; very rarely - hemolytic anemia, thrombocytopenia;
- organs of sight and hearing: infrequently - visual impairment, hearing impairment, vertigo; unspecified frequency - tinnitus, hearing impairment, deafness;
- respiratory system: infrequently - shortness of breath, nosebleeds;
- cardiovascular system: infrequently - flushing of the face, palpitations; unspecified frequency - an increase in the QT interval on the electrocardiogram, ventricular tachycardia, pirouette-type arrhythmias, a decrease in blood pressure;
- musculoskeletal system: infrequently - neck / back pain, myalgia, osteoarthritis; unspecified frequency - arthralgia;
- gastrointestinal tract: very often - diarrhea; often - abdominal pain, nausea, vomiting; infrequently - increased secretion of salivary glands, dryness of the oral mucosa, ulcers of the oral mucosa, belching, flatulence, bloating, constipation, dyspepsia, dysphagia, gastritis; very rarely - discoloration of the tongue, pancreatitis;
- metabolism: infrequently - anorexia;
- kidneys and urinary tract: infrequently - pain in the kidney area, urinary disorders; unspecified frequency - interstitial nephritis, acute renal failure;
- genitals, mammary gland: infrequently - dysfunction of the testicles in men, metrorrhagia in women;
- nervous system: often - headache; infrequently - a violation of taste, paresthesia, dizziness, nervousness, drowsiness, insomnia; rarely - agitation; unspecified frequency - perversion / loss of smell, loss of taste, fainting, convulsions, hallucinations, delirium, aggression, anxiety, myasthenia gravis, hypesthesia, psychomotor hyperactivity;
- skin, subcutaneous tissue: infrequently - dry skin, itching, excessive sweating, urticaria, skin rash, dermatitis; rarely - photosensitivity; unspecified frequency - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis;
- laboratory data: often - an increase or decrease in the concentration of bicarbonates in the blood plasma, a decrease in the number of lymphocytes, an increase in the number of basophils, eosinophils, monocytes and / or neutrophils; infrequently - a change in the content of potassium / sodium in the blood plasma, an increase in hematocrit, an increase in the number of platelets, an increase in the activity of alanine aminotransferase, aspartate aminotransferase and / or alkaline phosphatase in the blood plasma, an increase in the content of chlorine and concentration of glucose in the blood, an increase in the concentration of creatinine, urea and / or bilirubin in blood plasma;
- others: infrequently - facial edema, peripheral edema, fever, fatigue, malaise, asthenia, chest pain.
Overdose
In case of an overdose, diarrhea, nausea, vomiting, and temporary hearing loss may occur.
Gastric lavage is recommended as a first aid measure. Treatment of the developed disorders is symptomatic.
special instructions
Do not take AzitRus Forte tablets with food. The recommended duration of therapy must not be exceeded.
If signs of impaired hepatic function appear, AzitRus Forte should be canceled immediately and appropriate studies should be carried out. Alarming symptoms are: darkening of urine, a tendency to bleeding, jaundice, rapidly increasing asthenia, hepatic encephalopathy.
Against the background of any antibiotic therapy, the growth of refractory microorganisms and the development of superinfection (including fungal) are possible. In this regard, it is necessary to regularly examine patients.
AzitRus Forte with long-term use can cause pseudomembranous colitis associated with the bacterium Clostridium difficile, which can manifest itself as mild diarrhea and severe colitis. Taking medications that inhibit intestinal motility are contraindicated. In the case of the development of antibiotic-associated diarrhea, as well as 2 months after the end of therapy, it is necessary to conduct an examination to exclude clostridial pseudomembranous colitis.
In some patients, hypersensitivity reactions may persist even after discontinuation of treatment. They need medical supervision and specific therapy.
AzitRus Forte can cause the development of myasthenic syndrome or exacerbation of myasthenia gravis.
Macrolides, including azithromycin, are able to prolong cardiac repolarization and the QT interval. These conditions increase the risk of cardiac arrhythmias, including pirouette-type arrhythmias, which can cause cardiac arrest. In this regard, AzitRus Forte should be used with caution in the treatment of patients with existing proarrhythmogenic factors, especially in the elderly.
Influence on the ability to drive vehicles and complex mechanisms
Patients who experience adverse reactions from the organ of vision and / or the central nervous system should take precautions when performing activities that require quick reactions and visual acuity, including driving a car.
Application during pregnancy and lactation
In pregnant women, AzitRus Forte can only be used in cases where the benefits of the forthcoming therapy definitely outweigh the potential risks.
Azithromycin is excreted in breast milk, therefore it is contraindicated in nursing mothers. If antibiotic therapy is required, breastfeeding should be discontinued.
Pediatric use
AzitRus Forte is contraindicated for the treatment of children under 12 years of age and / or weighing less than 45 kg.
With impaired renal function
Prescribing AzitRus Forte is strictly contraindicated in severe renal impairment [creatinine clearance (CC) <40 ml / min].
Mild to moderate renal impairment (CC> 40 ml / min) are a relative contraindication to the appointment of AzitRus Forte, i.e., treatment should be carried out with extreme caution, under close monitoring of the functional state of the kidneys.
For violations of liver function
Appointment of AzitRus Forte is strictly contraindicated in severe liver dysfunction (class C according to Child-Pugh classification).
Mild and moderate liver dysfunctions (classes A and B according to the Child-Pugh classification) are a relative contraindication to the appointment of AzitRus Forte, that is, treatment should be carried out with extreme caution due to the risk of severe liver failure and fulminant hepatitis.
Use in the elderly
With extreme caution, AzitRus Forte should be used in elderly patients due to the possible presence of proarrhythmogenic conditions in patients of this category.
Drug interactions
There are no data on the possible interaction of azithromycin with ergotamine and dihydroergotamine derivatives (including ergot alkaloids). However, there are cases of development of ergotism with their simultaneous use, therefore, the appointment of this combination is not recommended.
Antacids do not affect the bioavailability of azithromycin, however, reduce its maximum concentration by 30%. If necessary, the joint use of AzitRus Forte preparations should be taken at least 1 hour before or 2 hours after antacids.
The combined use of azithromycin (once in a dose of 1000 mg and repeatedly in 600 or 1200 mg) with zidovudine has a slight effect on the pharmacokinetics of the latter, including the excretion of zidovudine and its glucuronide metabolite by the kidneys, but increases the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral mononuclear cells blood. The clinical significance of this phenomenon has not been established.
Macrolide antibiotics increase the plasma concentration of the P-glycoprotein substrate when used simultaneously with drugs that are P-glycoprotein substrates, including digoxin. For this reason, in patients receiving such a combination, this indicator should be monitored.
The simultaneous use of azithromycin (500 mg daily) and atorvastatin (10 mg daily) does not cause changes in plasma concentrations of drugs. However, rare cases of rhabdomyolysis have been reported in patients who received azithromycin in combination with statins.
Azithromycin weakly interacts with isoenzymes of the cytochrome P 450 system. It is neither an inducer nor an inhibitor of cytochrome P 450 isoenzymes. Similar to erythromycin and other macrolides, the participation of azithromycin in pharmacokinetic interactions was not revealed. The studies were carried out with the simultaneous use with azithromycin of drugs metabolized with the participation of isoenzymes of the cytochrome P 450 system.
With the combined use of cyclosporine (once at a dose of 10 mg / kg per day) and azithromycin (once at a dose of 500 mg), an increase in its C max and AUC (area under the concentration-time curve) was revealed. In this regard, you should be careful and control the concentration of the drug in the blood, if necessary, adjust the dose.
In pharmacokinetic studies, azithromycin had no effect on the anticoagulant effect of warfarin in a single dose of 15 mg. It has been reported that after the use of azithromycin, the effect of indirect anticoagulants (coumarin derivatives) has been reported. And although a reliable link with the antibiotic has not been established, it is recommended to monitor the prothrombin time more closely.
With the simultaneous use of azithromycin (at a dose of 1200 mg) and nelfinavir (750 mg 3 times a day), an increase in equilibrium plasma concentrations of azithromycin was noted. There were no clinically significant side effects, so no dose adjustment was necessary.
Taking a single dose of cimetidine does not affect the pharmacokinetics of azithromycin, provided that the first dose is taken 2 hours earlier.
With the simultaneous use of azithromycin (in a single dose of 1200 mg) and fluconazole (in a single dose of 800 mg), no changes in the pharmacokinetics of fluconazole, the total exposure and the half-life of azithromycin were revealed. A decrease of 18% C max of azithromycin was noted, but this phenomenon has no clinical significance.
When taking azithromycin and rifabutin together, there are no changes in plasma concentrations of both drugs. However, the development of neutropenia has been reported. This disorder has been associated with the use of rifabutin; the role of azithromycin in the onset of this condition has not been established.
In the course of pharmacokinetic studies, there was no evidence of a negative interaction of azithromycin with terfenadine. There are isolated cases when the likelihood of such an interaction could not be ruled out, but there was not a single reliable confirmation. It has been established that the combination of terfenadine and macrolides can contribute to the prolongation of the QT interval and the development of arrhythmias.
There was no interaction with the simultaneous use of azithromycin and methylprednisolone, sildenafil, theophylline, triazolam or midazolam (in therapeutic doses), trimethoprim / sulfamethoxazole, cetirizine (20 mg), didanosine (400 mg per day), carbamazepine, efavirenza (400 mg per day) within 7 days), indinavir (800 mg 3 times a day for 5 days).
Analogs
Analogs of AzitRus Forte are: Ziromin, AzitRus, Zitrocin, Sumaclid, Sumamed, Azitrox, Tremak-Sanovel, Azivok, Hemomycin, etc.
Terms and conditions of storage
Keep out of the reach of children, protected from light, at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about AzitRus Forte
According to reviews, AzitRus Forte is a cheap, but no less effective antibiotic than its expensive counterparts containing the same active ingredient. However, many patients note that it is worse tolerated. Adverse reactions include nausea, diarrhea, abdominal pain, vomiting, and difficulty breathing. Some users, due to their development, were unable to complete the course of treatment.
Price for AzitRus Forte in pharmacies
The approximate price for AzitRus Forte is 105–129 rubles. per pack of 3 film-coated tablets of 500 mg.
AzitRus Forte: prices in online pharmacies
|
Drug name Price Pharmacy |
|
AzitRus forte 500 mg film-coated tablets 3 pcs. 102 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
