Description
Release form
Lyophilisate for the preparation of an infusion solution in the form of a powder or a mass of white or almost white solidified in a tablet.
Packaging
500 mg – glass vials (1) – packs of cardboard.
Pharmacological action of
Azithromycin is a macrolide antibiotic of the azalide group. By reversibly binding to the 50S subunit of the bacterial cell ribosome, it disrupts the translocation of the growing polypeptide chain from the aminoacyl to the peptide region, which
inhibits protein synthesis in bacterial cells.
Sensitive: aerobic gram-positive microorganisms – Staphylococcus aureus (methicillin-sensitive), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes aerobic gram-negative microorganisms – Haemophilus influenzae, Haemophilus parainfionenila pneuminfenenila Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae anaerobic microorganisms – Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp. others – Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.
Moderately sensitive: Streptococcus pneumoniae (moderately sensitive or resistant to penicillin).
Resistant: aerobic gram-positive microorganisms – Enterococcus faecalis, beta-hemolytic Streptococcus spp. Groups A, Staphylococcus spp. (methicillin-resistant), including Staphylococcus aureus, resistant to erythromycin and other macrolides, anaerobic lincosamides: Bacteroides fragilis.
Indications
Community-acquired severe pneumonia caused by Chlamydia pneumoniae, Haemophilus influenzae, Legionella pneumophila, Moraxella catarrhalis, Mycoplasma pneumoniae, Staphylococcus aureus or Streptococcus pneumoniae
Infectious and inflammatory diseases of the pelvic organs of the heavy course (endometritis and salpingitis) caused by Chlamydiaisschaeromis goromatis or Nechromis geromomis geromaomatis
Contraindications
Hypersensitivity to azithromycin or other components of the
preparation hypersensitivity to erythromycin, other macrolides,
ketolides severe liver dysfunction
severe renal impairment (clearance of creatinine s min less than 40 ml less than 40 ml Concomitant use with ergotamine and dihydroergotamine.
Precautions
Myasthenia gravis, impaired liver function of mild to moderate severity, impaired renal function of mild to moderate severity (creatinine clearance greater than 40 ml / min), in patients with proarrhythmogenic factors (especially in elderly patients): with congenital or acquired prolongation of the QT interval, in patients receiving therapy with antiarrhythmic drugs of classes IA (quinidine, procainamide) and III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with impaired water-electrolyte balance, especially in case of hypokalemia or hypomagnesemia, with a clinically significant bradycard diya, cardiac arrhythmias or severe heart failure, simultaneous use of digoxin, warfarin, cyclosporine.
Use during pregnancy and lactation
Use of the drug during pregnancy is possible only in cases where the benefits of its use for the mother outweigh the possible risk to the fetus. During lactation, breastfeeding is suspended.
Composition of
1 bottle contains the active substance – azithromycin (in the form of azithromycin dihydrate 524.00 mg) 500 mg excipients: citric acid monohydrate – 110 mg 146 mg, sodium hydroxide – up to pH 6.0 – 7.0.
Dosage and administration
The drug should be used only in inpatient medical facilities!
Recommended doses for intravenous administration of azithromycin in the treatment of adults and patients over 18 years of age with the following diseases:
Community-acquired pneumonia (CAP)
500 mg once daily intravenously (iv) for at least 2 days (if necessary, by the decision of the attending physician, the iv course can be extended, but should not be more than 5 days). Intravenous administration should be followed by subsequent oral administration of azithromycin in the form of a single daily dose of 500 mg until the completion of the 7-10 day general course of treatment.
Infectious and inflammatory diseases of the pelvic organs
500 mg once a day intravenously for at least 2 days (iv treatment is no more than 5 days). Intravenous administration should be followed by subsequent oral administration of azithromycin in the form of a single daily dose of 250 mg until the completion of the 7-day general course of treatment.
The timing of the transition to oral treatment is determined in accordance with the data of the clinical examination.
Patients with impaired renal function
When used in patients with impaired renal function of mild to moderate severity (creatinine clearance> 40 ml / min) dose adjustment not required.
Patients with impaired liver function
Dose adjustment is not required in patients with impaired liver function of mild to moderate severity.
Elderly patients
In elderly patients, dose adjustment is not required.
The solution for infusion is prepared in 2 stages:
stage 1 – preparation of the reconstituted solution:
, add 4.8 ml of sterile water for injection into a 500 mg vial and shake thoroughly until the powder is completely dissolved.
1 ml of the resulting solution contains 100 mg of azithromycin.
The prepared solution remains stable for 24 hours at room temperature.
stage 2 – dilution of the reconstituted solution (100 mg / ml) is carried out immediately before administration in accordance with the table below.
Concentration of azithromycin in
infusion solution Amount of solvent
1.0 mg / ml
500 ml
2.0 mg / ml
250 ml
The reconstituted solution is added to the solvent vial (0.9% sodium chloride solution, 5% dextrose, Ringer’s solution) obtaining a final concentration of azithromycin of 1.0-2.0 mg / ml in the infusion solution.
Chemomycin solution should not be administered intravenously by stream or intramuscularly!
It is recommended to administer the prepared solution intravenously dropwise for 3 hours – a solution for infusion at a concentration of 1 mg / ml, for 1 hour – at a concentration of 2 mg / ml.
Before administration, the solution is subjected to visual inspection. If the finished solution contains particles of the substance, then it should not be used.
The prepared solution is stable at room temperature for 24 hours.
Side effects
From the side of the central nervous system: dizziness / vertigo, headache, drowsiness, convulsions paresthesia, asthenia, insomnia, irritability, fainting, aggressiveness, anxiety, nervousness.
On the part of the sensory organs: tinnitus, reversible hearing loss up to deafness (when taking high doses for a long time), impaired vision, impaired perception of taste and smell.
From the cardiovascular system: palpitations, arrhythmia, including ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia, decreased blood pressure.
From the digestive system: nausea, vomiting, diarrhea, abdominal pain and lubrication, loose stools, flatulence, indigestion, cholestatic jaundice, hepatitis, gastritis, changes in laboratory parameters of liver function, constipation, discoloration of the tongue, pseudomembranous colitis, pancreatitis, necrosis liver liver failure (possibly fatal).
From the circulatory and lymphatic systems: thrombocytopenia, neutropenia, leukopenia, neutrophilia.
Allergic reactions: itching, skin rashes, angioedema, urticaria, photosensitivity, anaphylactic reaction, including edema (in rare cases, fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the musculoskeletal system: arthralgia.
From the genitourinary system: nephritis, acute renal failure.
Local reactions: pain and inflammation at the injection site.
Other: candidiasis, incl. oral cavity and genitals, fatigue, malaise, anorexia, vaginitis.
Drug Interaction
Azithromycin does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim / sulfamethoxazole, rifabutin and methylprednisolone in the blood when used together.
When co-administered with cyclosporine, it is recommended that blood cyclosporine be monitored.
When digoxin and azithromycin are used together, it is necessary to control the concentration of digoxin in the blood, because many macrolides increase the absorption of digoxin in the intestine, thereby increasing its concentration in blood plasma.
When combined with indirect anticoagulants (warfarin, other coumarin series anticoagulants), patients should be monitored closely for prothrombin time.
Concomitant administration of terfenadine and macrolide-class antibiotics causes arrhythmia and QT prolongation. These data should be considered when combined with terfenadine and azithromycin.
When combined with nelfinavir, an increase in the incidence of azithromycin side effects may occur.
Consideration should be given to inhibiting the CYP3A4 isoenzyme by azithromycin when co-administered with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole, and other enzymatic metabolites.
When combined with azithromycin and zidovudine, azithromycin does not affect the pharmacokinetic parameters of zidovudine in blood plasma or the renal excretion of its and its glucuronide metabolite. However, the concentration of active metabolite – phosphorylated zidovudine in mononuclear cells of peripheral vessels increases. The clinical significance of this fact has not yet been determined.
When combined with azithromycin with ergotamine and dihydroergotamine, their toxic effects (vasospasm, dysesthesia) can be manifested.
Pharmaceutically incompatible with heparin.
Overdose
Symptoms: severe nausea, temporary hearing loss, vomiting, diarrhea, abdominal pain, impaired liver function.
Treatment: symptomatic.
Storage conditions
Store at a temperature of 10 ° to 25 ° C. Keep out of the reach of children.
Shelf suitability
3 Year
Deystvuyuschee substances
Azithromycin
Dosage form
dosage form
infusion solution
