Azithromycin capsules 250mg, 6pcs

Composition

1 capsule contains: Active ingredient:

azithromycin dihydrate (equivalent to anhydrous azithromycin) – 250 mg

. excipients:

microcrystalline cellulose-40.6 mg,

povidone low molecular weight (polyvinylpyrrolidone low molecular weight) – 1.0 mg,

magnesium stearate-3.7 mg,

sodium lauryl sulfate-0.7 mg,

lactose monohydrate-until the contents of a capsule weighing 370 mg are obtained;

solid gelatin capsules:

titanium dioxide 2%,

gelatin up to 100%.

Pharmacological action

Pharmacodynamics

Azithromycin is a broad-spectrum bacteriostatic antibiotic from the group of macrolides-azalides. It has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of microbial cell protein synthesis. Binding to the 508-subunit of ribosomes, it inhibits peptidtranslase at the translation stage and suppresses protein synthesis, slowing down the growth and reproduction of bacteria. In high concentrations, it has a bactericidal effect.

It has activity against a number of gram-positive, gram-negative, anaerobic, intracellular and other microorganisms. Microorganisms may initially be resistant to the action of an antibiotic or may become resistant to it. In most cases, sensitive microorganisms

Microorganisms capable of developing resistance to azithromycingram-positive aerobesstreptococcus pneumoniae Penicillin-resistant Initially resistant microorganisms Gram-positive aerobesenterococcus faecalis, Staphylococci (Methicillin-resistant staphylococci show a very high degree of resistance to macrolides). Gram-positive bacteria resistant to erythromycin. Anaerobesbacteroides fragilis

Pharmacokinetics

After oral use, azithromycin is well absorbed and quickly distributed in the body. After a single 500 mg dose, the bioavailability is 37% (the “first pass” effect), the maximum concentration (0.4 mg/ml) in the blood is created after 2-3 hours, the apparent volume of distribution is 31.1 l / kg, binding to proteins is inversely proportional to the concentration in the blood and is 7-50%. Penetrates cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes to the site of infection, where it is released in the presence of bacteria. It easily passes through histohematic barriers and enters the tissues. The concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection-24-34% higher than in healthy tissues.

Azithromycin has a very long half-life of 35-50 hours. The tissue half-life is significantly longer. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is mainly excreted unchanged-50% by the intestines,6% by the kidneys. In the liver, it is demethylated, losing its activity.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• infections of the upper respiratory tract and ENT organs (sinusitis, tonsillitis, pharyngitis, otitis media);
• infections of the lower respiratory tract: acute bronchitis, exacerbation of chronic bronchitis, pneumonia, including those caused by atypical pathogens;
• infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses, acne vulgaris moderate severity);
• the initial stage of Lyme disease (borreliosis) is a migratory erythema (erythema migrans);
• urinary tract infection caused by chlamydia trachomatis (urethritis, cervicitis).

Contraindications

• Hypersensitivity to macrolide antibiotics,
• severe hepatic and / or renal failure,
• children under 12 years of age (with a body weight of less than 45 kg),
• breast-feeding,
• concomitant use with ergotamine and dihydroergotamine.

With caution, moderate hepatic and renal dysfunction, with arrhythmias or predisposition to arrhythmias and prolongation of the QT interval, with the combined use of terfenadine, warfarin, digoxin.

Side effects

From the circulatory and lymphatic systems: thrombocytopenia, neutropenia. From the central nervous system: dizziness/vertigo, headache, convulsions, drowsiness, paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness. From the sensory organs: tinnitus, reversible hearing loss up to deafness (when taking high doses for a long time), impaired perception of taste and smell. From the cardiovascular system: palpitations, arrhythmia, ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia. Gastrointestinal disorders: nausea, vomiting, diarrhea, abdominal pain/cramps, flatulence, indigestion, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory liver function, liver failure, liver necrosis (possibly fatal). Allergic reactions: pruritus, skin rashes, angioedema, urticaria, photosensitization, anaphylactic reaction, including edema (rarely fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. Musculoskeletal system disorders: arthralgia. From the genitourinary system: nephritis, acute renal failure. Other: vaginitis, candidiasis.

Interaction

Antacids do not affect the bioavailability of azithromycin, but reduce the maximum concentration of azithromycin in blood plasma by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and eating. Azithromycin does not affect the concentration of carbamazepine, didanosine, rifabutin and methylprednisolone in the blood when used together.

When used parenterally, azithromycin does not affect the concentration of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, trimethoprim/sulfamethoxazole in the blood when used together, but the possibility of such interactions should not be excluded when prescribing azithromycin for oral use. Azithromycin does not affect the pharmacokinetics of theophylline, but when co-administered with other macrolides, the concentration of theophylline in blood plasma may increase.

If combined use with cyclosporine is necessary, it is recommended to monitor the content of cyclosporine in the blood. Despite the fact that there is no data on the effect of azithromycin on changes in the concentration of cyclosporine in the blood, other representatives of the macrolide class are able to change its level in blood plasma. When taking digoxin and azithromycin together, it is necessary to monitor the level of digoxin in the blood, since many macrolides increase the absorption of digoxin in the intestine, thereby increasing its concentration in the blood plasma. If co-use with warfarin is necessary, careful monitoring of prothrombin time is recommended.

Concomitant use of terfenadine and macrolide antibiotics has been found to cause arrhythmia and prolongation of the QT interval. Based on this, the above-mentioned complications cannot be excluded when taking terfenadine and azithromycin together. Since there is a possibility of inhibition of the CYP3A4 isoenzyme by azithromycin in parenteral form when co-administered with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs that are metabolized with the participation of this enzyme, the possibility of such interaction should be considered when prescribing azithromycin for oral use.

When azithromycin and zidovudine are co-administered, azithromycin does not affect the pharmacokinetic parameters of zidovudine in blood plasma or the renal excretion of it and its metabolite glucuronide. However, the concentration of the active metabolite, phosphorylated zidovudine, increases in the multinucleated cells of peripheral vessels. The clinical significance of this fact is not clear. Concomitant use of macrolides with ergotamine and dihydroergotamine may result in toxic effects (vasospasm, dysesthesia).

How to take it, course of use and dosage

Inside,1 hour before or 2 hours after meals 1 time a day. Adults with upper and lower respiratory tract infections – 500 mg / day for 1 dose for 3 days (course dose-1.5 g). For skin and soft tissue infections-1000 mg / day on the first day for 1 dose, then 500 mg / day daily from day 2 to day 5 (course dose – 3 g). In acute infections of the genitourinary organs (uncomplicated urethritis or cervicitis) – a single multiple of 1000 mg. In Lyme disease (borreliosis) for the treatment of stage I (erythema migrans) – 1000 mg on the first day and 500 mg daily from day 2 to 5 (course dose-3 g). In gastric and duodenal ulcers associated with Helicobacter pylori – 1 g / day for 3 days as part of combined anti-helicobacter therapy. Children over 12 years of age (with a body weight of 50 kg or more) with infections of the upper and lower respiratory tract, skin and soft tissues – 500 mg once a day for 3 days.When treating erythema migrans in children, the dose is 1000 mg on the first day and 500 mg daily from day 2 to day 5.

Overdose

Symptoms: nausea, temporary hearing loss, vomiting, diarrhea.

Treatment: taking activated charcoal, gastric lavage, symptomatic therapy.

Special instructions

If one dose of the drug is missed, the missed dose should be taken as early as possible, and the subsequent ones should be taken at intervals of 24 hours.

As with any antibiotic therapy, superinfection (including fungal infection) may occur during treatment with azithromycin. Azithromycin should be taken at least one hour before or two hours after taking antacid medications.

Influence on the ability to drive vehicles and mechanisms. During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Capsules

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Azithromycin

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

Pregnant women as prescribed by a doctor, Children over 12 years of age, Children as prescribed by a doctor, For adults, For adults as prescribed by a doctor, Nursing mothers as prescribed by a doctor

Indications

Gastrointestinal infections caused by Helicobacter Pylori, Pneumonia, Tonsillitis, Urinary Tract Infections, Respiratory Tract Infections, Bronchitis, Laryngitis, Infectious Diseases, Urethritis, Skin Infections, Otitis Media, Sore Throat