Properties
What is it?
TOPT Azithromycin 500 mg film-coated tablets. Active ingredient: Azithromycin. Pharmaceutical form: White, oblong, biconvex, film-coated tablets with a score on one side. Composition: 1 film-coated tablet contains: Azithromycin dihydrate, equivalent to 500 mg Azithromycin. See also: Azibiot - Azibiot 500 mg. 3 tablets. Excipients: Pregelatinized starch, copovidone, hypromellose acetate succinate, anhydrous calcium hydrogen phosphate, crospovidone, anhydrous colloidal silicon dioxide, talc, magnesium stearate, sodium lauryl sulfate; Coating agents (hypromellose, macrogol 6000, talc, titanium dioxide (E 171), dimethicone). Dosage form: 500 mg film-coated tablets. Pharmacological group: Macrolides. Pharmacological properties: TOPT is a broad-spectrum antibacterial agent of the macrolide group. It binds to the 50S ribosomal subunit, inhibits protein synthesis, and hinders bacterial growth and reproduction. At high concentrations, it exhibits bactericidal activity. Active against Gram-positive microorganisms: Streptococcus spp. (group C, F, G), S. pneumoniae, S. pyogenes, S. agalactiae, S. viridans, Staphylococcus epidermidis, Staphylococcus aureus; Gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campilobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; intracellular and other microorganisms: Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacteria avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrella burgdorferi, and also active against Helicobacter pylori. Pharmacokinetics: The drug is rapidly absorbed from the gastrointestinal tract. Food intake reduces azithromycin absorption. Cmax in plasma is reached after 2-3 hours. After a single dose of 500 mg, bioavailability is 37%, t1/2 - 68 hours, volume of distribution (Vd) - 31.1 L/kg. Steady-state plasma concentration is reached after 5-7 days. It easily crosses the histohematic barrier and enters tissues. It is transported by phagocytes, polymorphonuclear leukocytes, and macrophages to the site of inflammation, where it is released in the presence of bacteria. Concentrations in tissues and cells are 10-50 times higher than in plasma, and at the site of infection - 24-34% higher than in healthy tissues. High antibacterial levels in tissues are observed for 5-7 days after the last dose. Plasma clearance - 630 ml/min. It undergoes demethylation in the liver and loses activity. 50% is excreted unchanged in bile, and 6% - with urine. In elderly men (65-85 years), pharmacokinetic parameters do not change; in women - Cmax increases (by 30-50%); in children aged 1 to 5 years - Cmax, T1/2, AUC decrease. Indications: Infectious-inflammatory diseases caused by microorganisms sensitive to the drug: - Infections of the ear, nose, and throat (acute pharyngitis, acute tonsillitis, acute sinusitis, acute otitis media); - Respiratory tract infections (acute bronchitis, chronic bronchitis in the exacerbation phase, interstitial and alveolar pneumonia); - Skin and soft tissue infections (chronic migratory erythema - early stage of Lyme disease, erysipelas, impetigo, secondarily infected dermatoses, uncomplicated forms of Acne vulgaris); - Genitourinary tract infections (urethritis and/or cervicitis); - Gastric and duodenal diseases associated with Helicobacter pylori. Dosage and administration: TOPT is taken orally 1 hour before meals or 2 hours after meals. For adults, it is prescribed 500 mg once daily for three days, or it can be prescribed for 5 days: 500 mg once daily on the first day, then 250 mg once daily on days 2-5 (total dose 1500 mg). For skin and soft tissue infections, upper and lower respiratory tract infections, 0.5 g is prescribed daily for three days (total dose 1.5 g). For acute inflammation of the genitourinary organs (uncomplicated urethritis and/or cervicitis), 1 g is prescribed once. For the treatment of the first stage of Lyme disease (Erythema migrans) - 1 g on the first day, then 0.5 g daily on days 2-5 (total dose - 3 g). For gastric and duodenal diseases associated with Helicobacter pylori - 1 g daily for 3 days in combination with anti-Helicobacter therapy. For the treatment of Acne vulgaris: total dose - 6 g. Recommended treatment regimen: 500 mg once daily for the first 3 days of treatment, then 500 mg once weekly for 9 weeks. In case of a missed dose, the drug should be taken as soon as possible, and subsequent doses should be taken at 24-hour intervals. In children over 12 years of age with a body weight exceeding 45 kg, the drug is prescribed at the same dose as for adults. In children under 12 years of age with a body weight not exceeding 45 kg, other (pediatric) forms of azithromycin are used, and the dosage is determined by the child's age and body weight. 10 mg/kg is prescribed once daily for 3 days (total dose - 30 mg/kg). Side effects: Central nervous system: headache, dizziness; rarely - drowsiness, weakness, excitability, paresthesia; Digestive system: nausea, vomiting, loss of appetite, flatulence, diarrhea, constipation, abdominal pain; very rarely - pseudomembranous colitis; Hepatobiliary system: rarely - cholestatic jaundice; very rarely - hepatitis; Allergic reactions: rarely - rash, angioneurotic edema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis; very rarely - anaphylactic reaction; Cardiovascular system: rarely - chest pain, tachycardia, arrhythmia; Genitourinary system: vaginitis, rarely - candidiasis; very rarely - interstitial nephritis; Laboratory parameters: reversible increase in the activity of liver transaminases, bilirubin, eosinophils. Altered parameters return to normal within 2-3 weeks after discontinuation of treatment; Hematopoietic system: leukopenia, neutropenia, thrombocytopenia, hemolytic anemia; Other: rarely - hyperglycemia, myasthenia, arthralgia; very rarely - transient hearing impairment, photosensitization. If any side effect not listed in the instructions for use occurs, the patient should consult their doctor. Contraindications: Hypersensitivity to macrolides and/or any component of the drug, severe liver and kidney dysfunction. Interactions with other drugs and other types of interactions: Concomitant administration with antacids reduces the maximum plasma concentration of TOPT by 30%. The drug should be taken 1 hour before or 2 hours after taking the antacid. Concomitant use with ergot alkaloids may lead to the development of ergotism. Concomitant use with warfarin may enhance the effect of the latter. Concomitant use of TOPT with digoxin or digitoxin may lead to an increase in the concentration of cardiac glycosides in blood plasma and the development of glycoside intoxication. Cases of ventricular arrhythmia have been described with concomitant use of disopyramide. Cases of rhabdomyolysis have been described with concomitant use of lovastatin. Concomitant administration with rifabutin increases the risk of developing neutropenia and leukopenia. Concomitant administration with cyclosporine disrupts the metabolism of the latter, increasing the risk of side and toxic reactions caused by cyclosporine. Overdose: Overdose may cause the following symptoms: nausea, vomiting, diarrhea, allergic reactions, temporary hearing loss. In such cases, the drug intake should be discontinued and a doctor should be consulted immediately. Treatment: symptomatic. Pregnancy and lactation: During pregnancy, TOPT is prescribed only when the expected benefit to the mother outweighs the expected risk to the fetus. TOPT is excreted in breast milk, so breastfeeding should be discontinued during and for 2 days after completion of the drug. Special instructions: Use with caution in liver and kidney dysfunction, cardiac arrhythmias (possible increase in Q-T interval and development of ventricular arrhythmias). After discontinuation of treatment, some patients may retain hypersensitivity reactions, which require specific therapy under medical supervision. Effect of the drug on the ability to drive vehicles and operate machinery: The drug may cause dizziness, drowsiness, so during treatment, it is necessary to avoid activities that require increased attention and rapid psychomotor reactions. Packaging: 3 film-coated tablets in a blister, 2 blisters in a cardboard box. Storage conditions: Store at a temperature not exceeding 25°C, in a dry, protected from light, and inaccessible place for children. The drug is not allowed to be taken if any defect is found during visual inspection. Shelf life: 3 years. The drug is not allowed to be used after the expiry date indicated on the packaging. Dispensing rule: Pharmaceutical product group - II, dispensed by prescription form №3.
