AZOMIN [Azithromycin] 500 mg Film-coated tablets
AZOMIN
instructions for medical use of the medicinal product
Tradename
Azomin, Azomin
International non-proprietary name
Azithromycin, Azithromycin
Compound
Each film-coated tablet contains:
Azithromycin (as dihydrate) 500 mg
Excipients: dibasic calcium phosphate dihydrate, corn starch. talc, croscarmellose sodium, magnesium stearate, hypromellose, titanium dioxide.
Each 5 ml suspension (after dilution) contains:
Azithromycin (as dihydrate) 200 mg
Excipients: sucrose, tribasic sodium phosphate, hydroxypropyl methylcellulose, xanthan gum, cherry flavor (powder), banana flavor (powder).
The solvent is purified water.
Dosage form
Tablets.
Powder for suspension.
Pharmacotherapeutic group
Antimicrobial agents for systemic use. Macrolides.
Pharmacological properties
Pharmacodynamics
Azomin is a macrolide antibiotic of the azalide group. The mechanism of the antibacterial action of azithromycin is due to its ability to inhibit the synthesis of bacterial proteins by binding to the 50S subunit of the ribosome and inhibiting the stage of peptide translocation. Azithromycin has a wide spectrum of antimicrobial activity against gram-positive, gram-negative, intracellular and other microorganisms: Aerobic gram-positive bacteria: Staphylococcus aureus, Streptococcus pneumonia, Streptococcus pyogenes (group A), Streptococcus viridans Aerobic gram-positive bacteria: Haemophilus influenza, Haemophilus parainfluenzae, Haemophilus ducreyi, Legionella ducreyi pneomophila, Moraxella catarrhalis, Pasteurella multocida, Bordetella pertussis, Bordetella parapertussis, Escherichia coli, Neisseria gonorrhoeae, Helibacter pylori Anaerobic bacteria: Bacteroides fragilis, Clostridium perfringens, Fusobcterium spp., Prevotella spp., Porphyromonas spp., Propionibacter Other microorganisms: Chlamidia trachomatis, Chlamidia pneumonia, Mycoplasma pneumonia, Mycoplsma hominis, Borrelia burgdorferi, Treponema pallidum, Ureaplsma ureolyticum. Azithromycin is not active against Gram-positive bacteria resistant to erythromycin.
Pharmacokinetics
After oral administration, the bioavailability of azithromycin is approximately 37%. Maximum plasma levels are established 2-3 hours after taking the drug (C max after a single dose of 500 mg orally was approximately 0.4 mg / l). The active substance binds extensively to tissues (volume of distribution at steady state is approximately 31 l/kg). Concentrations in target tissues, such as lungs, tonsils and prostate, after a single dose of 500 mg, exceeded the MIC90 value for the most commonly encountered pathogens. Azithromycin accumulates in phagocytes, the release is stimulated by active phagocytosis, which contributes to the accumulation of azithromycin in tissues. The binding of azithromycin to serum protein varies depending on plasma concentration from 50% at 0.05 mg/l to 12% at 0.5 mg/l.
The half-life for azithromycin is in the range of 2 to 4 days. The main route of elimination (about 59%) is unchanged in the bile. The rest is metabolized to 10 inactive metabolites. An average of 6% of the dose taken is excreted in the urine.
Indications for use
Diseases caused by microorganisms sensitive to azithromycin:
- infections of the upper respiratory tract and ENT organs (bacterial pharyngitis / tonsillitis, sinusitis, otitis media) and lower respiratory tract (bronchitis, bacterial and atypical pneumonia);
- infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);
- infections of the urogenital tract (uncomplicated urethritis and / or cervicitis caused by Neisseria gonorrhoeae, Chlamydia trachomatis).
Contraindications
Hypersensitivity to azithromycin, erythromycin, other macrolide and ketolide antibiotics or any of the excipients of the drug. Severe liver dysfunction.
Use during pregnancy or lactation
During pregnancy, the use of the drug is possible when the intended benefit to the mother outweighs the potential risk to the fetus.
Azithromycin passes into breast milk. In this regard, breastfeeding should be interrupted for the period of taking the drug. Feeding can be resumed 2 days after the end of azithromycin.
Interaction with other drugs
Antacids. Do not take antacids and azithromycin at the same time. Azithromycin should be taken at least one hour before or two hours after taking antacids.
Digoxin and colchicine (substrates of P-glycoproteins). When co-administered with azithromycin, the possibility of an increase in blood levels of digoxin and colchicine should be considered.
Zidovudine. Increases the concentration of phosphorylated zidovudine, a clinically active metabolite, in peripheral blood mononuclear cells.
Ergot derivatives. The simultaneous use of azithromycin and ergot derivatives is not recommended.
Atorvastatin. There are reports of the development of rhabdomyolysis in patients treated with azithromycin in conjunction with statins.
Anticoagulants. When prescribing azithromycin, patients receiving oral coumarin anticoagulants should regularly monitor prothrombin time.
Cyclosporine. If it is necessary to simultaneously prescribe azithromycin and cyclosporine, special care should be taken to constantly monitor the concentration of cyclosporine and adjust the dose of the drug accordingly.
other antibiotics.
The possibility of core-resistance to macrolide antibiotics should be considered. The simultaneous use of several drugs belonging to the same drug group is not recommended.
Medicines that can prolong the QT interval.
Azithromycin should not be administered simultaneously with other drugs that can prolong the QT interval.
Special instructions and precautions
Children. Children under 12 years of age are not recommended to take pills. In pediatric practice, a suspension is used.
For antibiotics of the macrolide group, the ability to lengthen the repolarization time and the QT interval is characteristic, which is a risk factor for the development of arrhythmia and torsade de pointes. Patients with impaired water and electrolyte balance, with bradycardia, arrhythmias or severe heart failure are not recommended to prescribe Azomin.
As with other broad-spectrum antibiotics, while taking Azomin, there is a risk of developing superinfection caused by non-susceptible microorganisms (for example, fungal infections or pseudomembranous colitis). It is recommended to monitor the patient's condition regarding possible signs of the development of superinfection.
Penicillin is generally the drug of choice for the treatment of pharyngitis/tonsillitis caused by Streptococcus pyogenes and for the prevention of acute rheumatic fever. Azithromycin is generally effective against streptococcal oropharyngeal infections (although not the drug of choice), but there are no data demonstrating the effectiveness of azithromycin in the prevention of acute rheumatic fever.
Use with caution in patients with severely impaired renal and hepatic function.
Azomin is not indicated for the treatment of infected burn wounds.
Dosage and administration
For oral administration.
Dosing regimen is set individually depending on age, weight
body and the severity of the infection. Since the simultaneous intake of food slows down the absorption of azithromycin, Azomin must be taken 1 hour before a meal or 2 hours after a meal. For children aged one year and older (weighing less than 45 kg), it is recommended to prescribe the drug in the form of a suspension.
Adults. For uncomplicated urethritis and cervicitis caused by Chlamydia trachomatis: 1000 mg once orally. For all other indications, the dose is 500 mg 1 time per day for three consecutive days, or the same total dose (1500 mg) can be divided into five days with 500 mg on the first day and 250 mg of the drug on the second to fifth days. The course dose is 1500 mg.
Children. Assign at the rate of 10 mg / kg of body weight 1 time per day for 3 days or on the first day 10 mg / kg and then 5 mg / kg over the next 4 days. Heading dose 30 mg/kg.
An example of calculating the dose of Azomin suspension in children
Weight, kg | Suspension 200 mg/5 ml | A course of treatment | ||
| 1st option (3 days) | 2nd option |
| |
1st day | 2-5th days | |||
ten | 2.5 ml | 2.5 ml | 1.25 ml | 7.5 ml |
twenty | 5 ml | 5 ml | 2.5 ml | 15 ml |
thirty | 7.5 ml | 7.5 ml | 3.75 ml | 22.5 ml |
Suspension preparation.
Dilute the powder contained in the vial with 12 ml of solvent. close the cap and shake the vial until a suspension is formed. The volume of the resulting suspension is 22.5 ml, which corresponds to the full course dose for a child weighing 30 kg. After dilution, store the suspension for no more than 14 days in the refrigerator. Shake before each use. Immediately after taking the suspension, the child is allowed to drink a few sips of tea or juice in order to rinse and swallow the remaining amount of the suspension in the mouth.
Elderly patients:
Elderly patients are prescribed a standard dose for an adult. Since elderly patients may have risk factors for arrhythmias, special caution is recommended due to the risk of developing cardiac arrhythmias and ventricular tachycardia of the "pirouette" type.
Patients with impaired renal function
With mild or moderate impairment (GFR 10-80 ml / min), dose adjustment is not required.
Patients with impaired liver function
For mild or moderate impairment, dose adjustment is not required.
Side effect
Azomin is well tolerated with a low incidence of side effects.
From the gastrointestinal tract: nausea, diarrhea, abdominal pain / spasms, vomiting, flatulence, dyspepsia, constipation, pseudomembranous colitis, pancreatitis, discoloration of teeth, tongue, anorexia.
From the side of the central and peripheral nervous system: dizziness, convulsions, headache, weakness. drowsiness, impaired sense of smell and / or taste perception.
Since the cardiovascular system: palpitations, arrhythmia (including ventricular tachycardia), there are rare reports of prolongation of the QT interval and the development of torsade de pointes.
From the hepatobiliary system: rarely - a violation of the activity of liver enzymes, hepatitis, cholestatic jaundice, rare cases of hepatonecrosis and liver failure, some of them fatal.
Skin and subcutaneous tissue: rash, itching, angioedema, urticaria, photosensitivity, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the musculoskeletal system: arthralgia.
Infections and invasions: vaginitis, candidiasis.
Adverse reactions that developed when taking doses higher than recommended were similar to those at therapeutic doses. The characteristic symptoms of macrolide overdose are reversible hearing loss, severe nausea, severe vomiting, and diarrhea. In case of overdose, gastric lavage and general supportive measures are recommended.