Chemomycin 500 mg (tablets)
Antacids
Antacids do not affect the bioavailability of azithromycin, but reduce the maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and eating.
Cetirizine
Concomitant use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not lead to pharmacokinetic interaction or a significant change in the QT interval.
Didanosine (dideoxyinosine)
The simultaneous use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients did not reveal changes in the pharmacokinetic parameters of didanosine compared to the placebo group.
Digoxin (P-glycoprotein substrates)
Concomitant use of macrolide antibiotics, including azithromycin, with P-glycoprotein substrates, such as digoxin, leads to increased concentrations of P-glycoprotein substrate in the blood serum. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum.
Zidovudine
Concomitant use of azithromycin (single dose of 1000 mg and multiple doses of 1200 mg or 600 mg) has little effect on the pharmacokinetics, including renal excretion, of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear.
Azithromycin interacts weakly with isoenzymes of the cytochrome P450 system. Azithromycin has not been shown to participate in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes.
Ergot alkaloids
Given the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended. Pharmacokinetic studies were conducted on the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of isoenzymes of the cytochrome P450 system.
Atorvastatin
Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on an HMC-CoA reductase inhibition assay). However, in the post-marketing period, isolated case reports of rhabdomyolysis have been received in patients receiving concomitant azithromycin and statins.
Carbamazepine
Pharmacokinetic studies involving healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin.
Cimetidine
In pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin, no changes in the pharmacokinetics of azithromycin were detected when cimetidine was used 2 hours before azithromycin.
Indirect anticoagulants (coumarin derivatives)
In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single 15 mg dose of warfarin administered to healthy volunteers. Potentiation of the anticoagulant effect has been reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, the need for frequent monitoring of prothrombin time should be considered when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives).
Cyclosporine
In a pharmacokinetic study involving healthy volunteers who took azithromycin (500 mg/day once) orally for 3 days, followed by cyclosporine (10 mg/kg/day once), a significant increase in maximum plasma concentration (Cmax) and area under the concentration-time curve (AUC0-5) of cyclosporine. Caution is advised when using these drugs together. If simultaneous use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.
Efavirenz
Concomitant use of azithromycin (600 mg/day once) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.
Fluconazole
Concomitant use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and half-life of azithromycin did not change with simultaneous use of fluconazole, however, a decrease in Cmax of azithromycin was observed (by 18%), which had no clinical significance.
Indinavir
Concomitant use of azithromycin (1200 mg once) did not cause a statistically significant effect on the pharmacokinetics of indinavir (800 mg three times a day for 5 days).
Methylprednisolone
Azithromycin does not have a significant effect on the pharmacokinetics of methylprednisolone.
Nelfinavir
The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the equilibrium concentrations of azithromycin in the blood serum. No clinically significant side effects were observed and no dose adjustment of azithromycin was required when used concomitantly with nelfinavir.
Rifabutin
The simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood serum. Neutropenia has sometimes been observed with simultaneous use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.
Sildenafil
When used in healthy volunteers, there was no evidence of the effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite.
Terfenadine
In pharmacokinetic studies, there was no evidence of interaction between azithromycin and terfenadine. There have been isolated cases reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction occurred.
It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval.
Theophylline
No interaction has been detected between azithromycin and theophylline.
Triazolam/midazolam
No significant changes in pharmacokinetic parameters were detected with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses.
Trimethoprim/sulfamethoxazole
Concomitant use of trimethoprim/sulfamethoxazole with azithromycin did not show a significant effect on Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Azithromycin serum concentrations were consistent with those found in other studies.
Chemomycin 500 mg 3 pcs. film-coated tablets
pharmachologic effect
Broad-spectrum antibiotic.
It is a representative of a subgroup of macrolide antibiotics – azalides. In high concentrations it has a bactericidal effect. Gram-positive cocci are sensitive to azithromycin: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci of groups C, F and G, Staphylococcus aureus, Streptococcus viridans; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. Azithromycin is inactive against gram-positive bacteria resistant to erythromycin.
Composition and release form Hemomycin 500 mg 3 pcs. film-coated tablets
1 film-coated tablet contains the active substance azithromycin 500 mg (in the form of azithromycin dihydrate); excipients - microcrystalline cellulose silicate - 69.00 mg, microcrystalline cellulose - 57.00 mg, sodium carboxymethyl starch (type A) - 46.00 mg, povidone - 24.00 mg, magnesium stearate - 10.00 mg, talc - 10.00 mg, colloidal silicon dioxide – 1.00 mg; shell: titanium dioxide – 10.58 mg, talc – 9.57 mg, copovidone – 4.95 mg, ethylcellulose – 4.95 mg, macrogol 6000 – 1.32 mg, indigo carmine (indigotine) E 132 – 1.22 mg , dye varnish green 8% (indigo carmine (indigotine) E 132, quinoline yellow E 104) – 0.41 mg Film-coated tablets 500 mg.
3 tablets per AL/PVC blister. 1 blister with instructions for use in a cardboard box.
Description of the dosage form
Film-coated tablets
Characteristic
Round, biconvex tablets, film-coated, grayish-blue in color.
Directions for use and doses
Orally, 1 hour before or 2 hours after meals, 1 time per day. For adults and children over 12 years of age with infections of the upper and lower respiratory tract - 0.5 g / day per 1 dose for 3 days (course dose - 1.5 g).
For infections of the skin and soft tissues - 1 g / day on the first day for 1 dose, then 0.5 g / day daily from days 2 to 5 (course dose - 3 g).
For acute infections of the genitourinary organs (uncomplicated urethritis or cervicitis) - 1 g once.
For Lyme disease (borreliosis) for the treatment of stage I (erythema migrans) - 1 g on the first day and 0.5 g daily from days 2 to 5 (course dose - 3 g).
For gastric and duodenal ulcers associated with Helicobacter pylori - 1 g/day for 3 days as part of combination anti-Helicobacter pylori therapy.
Pharmacokinetics
Azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic environment and lipophilicity. After oral administration of 500 mg, the maximum concentration of azithromycin in the blood plasma is reached after 2.5 - 2.96 hours and is 0.4 mg/l. Bioavailability is 37%.
Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular the prostate gland), skin and soft tissues. The high concentration in tissues (10-50 times higher than in plasma) and the long half-life are due to the low binding of azithromycin to plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in the low pH environment surrounding lysosomes. This, in turn, determines the large apparent volume of distribution (31.1 l/kg) and high plasma clearance. The ability of azithromycin to accumulate predominantly in lysosomes is especially important for the elimination of intracellular pathogens. It has been proven that phagocytes deliver azithromycin to sites of infection, where it is released during the process of phagocytosis. The concentration of azithromycin in foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the degree of inflammatory edema. Despite its high concentration in phagocytes, azithromycin does not have a significant effect on their function. Azithromycin remains in bactericidal concentrations for 5-7 days after the last dose, which has made it possible to develop short (3-day and 5-day) courses of treatment.
It is demethylated in the liver, the resulting metabolites are not active.
The elimination of azithromycin from blood plasma occurs in 2 stages: the half-life is 14-20 hours in the range from 8 to 24 hours after taking the drug and 41 hours in the range from 24 to 72 hours, which allows the drug to be used once a day. Food intake significantly changes pharmacokinetics (depending on the dosage form): tablets - the maximum concentration (Cmax) increases (by 31%), the area under the curve (AUC) does not change.
Indications for use Chemomycin 500 mg 3 pcs. film-coated tablets
Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:
Infections of the upper respiratory tract and ENT organs (sore throat, sinusitis,
tonsillitis, pharyngitis, otitis media);
Scarlet fever;
Infections of the lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
Infections of the skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses);
Infections of the urogenital tract (uncomplicated urethritis and/or cervicitis);
Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans);
Diseases of the stomach and duodenum associated with Helicobacter Pylori (as part of combination therapy).
Contraindications
Hypersensitivity (including to other macrolides); liver and/or kidney failure; children under 12 years of age (for this dosage form), lactation period.
With caution - pregnancy, arrhythmia (possible ventricular arrhythmias and prolongation of the QT interval), children with severe impairment of liver or kidney function.
Application Hemomycin 500 mg 3 pcs. film-coated tablets during pregnancy and breastfeeding
Use during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.
If it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.
special instructions
The drug should not be taken during meals.
It is recommended to maintain an interval of at least 2 hours between taking Hemomycin and antacid medications.
After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy and medical monitoring.
Overdose
Symptoms: severe nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: symptomatic; gastric lavage.
Side effects Hemomycin 500 mg 3 pcs. film-coated tablets
From the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%); 1% or less - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of “liver” transaminases; in children - constipation, anorexia, gastritis.
From the cardiovascular system: palpitations, chest pain (1% or less).
From the nervous system: dizziness, headache, vertigo, drowsiness; in children - headache (during treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disturbance (1% or less).
From the genitourinary system: vaginal candidiasis, nephritis (1% or less).
Allergic reactions: rash, photosensitivity, Quincke's edema.
Other: increased fatigue; in children - conjunctivitis, itching, urticaria.
Drug interactions
Antacids (aluminum and magnesium), ethanol and food slow down and reduce absorption.
When warfarin and azithromycin were co-administered (in usual doses), no changes in prothrombin time were detected, however, given that the interaction of macrolides and warfarin may enhance the anticoagulation effect, patients need careful monitoring of prothrombin time.
Digoxin: increased digoxin concentrations.
Ergotamine and dihydroergotamine: increased toxic effects (vasospasm, dysesthesia).
Triazolam: decreased clearance and increased pharmacological action of triazolam. Slows down the elimination and increases the plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs subject to microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, theophylline and other xanthine derivatives) - due to inhibition of microsomal oxidation in hepatocytes by azithromycin.
Lincosamines weaken the effectiveness, tetracycline and chloramphenicol enhance it.
Pharmaceutically incompatible with heparin.
