Azithromycin-Alium capsules 250mg, 6pcs

Composition

Composition per capsule:

Active ingredient:

azithromycin dihydrate – in terms of azithromycin) – 250 mg

. excipients:

microcrystalline cellulose,

povidone (low molecular weight medical polyvinylpyrrolidone),

crospovidone, calcium stearate, sodium lauryl sulfate.

Solid gelatin capsules No. 1:

titanium dioxide,

blue patent dye (patent blue V),

diamond black,

crimson dye [Ponceau 4R],

azorubin,

gelatin.

Pharmacological action

Pharmacotherapeutic group:

antibiotic-azalide

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 50S subunit of the ribosome, 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

1. Gram-positive aerobes

Staphylococcus Aureus Methicillin-sensitive;

Streptococcus pneumoniae Penicillin-sensitive;

Streptococcus pyogenes.

2. Gram-negative aerobes

Haemophilus influenzae;

Haemophilus parainfluenzae;

Legionella pneumophila;

Moraxella catarrhalis;

Pasteurella multocida;

Neisseria gonorrhoeae.

3. Anaerobes

Clostridium perfringens;

Fusobacterium spp. ;

Prevotella spp. ;

Porphyriomonas spp.

4. Other microorganisms

are Chlamydia trachomatis;

Chlamydia pneumoniae;

Chlamydia psittaci;

Mycoplasma pneumoniae;

Mycoplasma hominis;

Borrelia burgdorferi.

Microorganisms capable of developing resistance to azithromycin

Gram-positive aerobes

Streptococcuspneumoniae Penicillin is sensitive.

Initially resistant microorganisms

Gram-positive aerobes

Enterococcus Faecalis;

Staphylococci (methicillin-resistant staphylococci exhibit a very high degree of macrolide resistance);

gram-positive bacteria resistant to erythromycin.

Anaerobes

Bacteroidesfragilis.

Pharmacokinetics:

Azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity. It is rapidly distributed throughout the body, while high concentrations of the antibiotic are achieved in the tissues. After oral use of 500 mg, the maximum concentration of azithromycin in blood plasma is reached in 2.5-2.9 hours and is 0.4 mg/l. Bioavailability is 37.5%.

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 blood 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 a 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 mainly in lysosomes is especially important for the elimination of intracellular pathogens.

Phagocytes have been shown to deliver azithromycin to the sites of infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the degree of inflammatory edema.

Azithromycin remains in bactericidal concentrations for 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) treatment courses.

It is demethylated in the liver, and the resulting metabolites are not active.

The elimination of azithromycin from blood plasma takes place 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 1 time / day.

The drug is excreted mainly with bile in unchanged form, a small part is excreted by the kidneys.

Indications

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

· Infections of the upper respiratory tract and ENT organs (pharyngitis/tonsillitis, sinusitis, otitis media);

· infections of the lower respiratory tract: acute bronchitis, exacerbation of chronic bronchitis, including caused by atypical pathogens;

· infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);

· the Initial stage of Lyme disease (borreliosis) is a migratory erythema (Erythemamigrans);

· urinary tract Infection, caused by Chlamydiatrachomatis (urethritis, cervicitis).

Use during pregnancy and lactation

The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, stop breastfeeding (it is excreted in breast milk).

Contraindications

* Hypersensitivity to macrolide antibiotics;

· Severe liver and kidney function disorders

· * Children under 12 years of age with a body weight of less than 45 kg (for this dosage form);

· Breastfeeding;

· 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

Allergic reactions: pruritus, skin rashes, angioedema, urticaria, anaphylactic reaction, including edema (rarely fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrosis.

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: rarely-palpitations, arrhythmia, ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia.

From the digestive system: nausea, vomiting, diarrhea, abdominal pain/cramps, loose stools, flatulence, indigestion, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory parameters of liver function, liver dysfunction, liver necrosis (possibly fatal).

Musculoskeletal system disorders: arthralgia.

From the genitourinary system: nephritis, acute renal failure.

Other: vaginitis, candidiasis, photosensitization.

Interaction

Antacids do not affect the bioavailability of azithromycin, but reduce the maximum concentration in the blood 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.

Careful monitoring of prothrombin time is recommended when warfarin and azithromycin are co-administered.

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 enzyme 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 peripheral vascular mononuclear cells. The clinical significance of this fact is not clear.

Concomitant use of macrolides with ergotamine and dihydroergotamine may cause their toxic effects.

How to take, course of use and dosage

Inside, once a day, at least 1 hour before or 2 hours after a meal.

Adults (including the elderly) and children over 12 years of age with a body weight over 45 kg.

For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues

500 mg (2 capsules) 1 time a day 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 reception, then 0.5 g / day daily from day 2 to 5 (the course dose is 3 g).

With migrating erythema

1 time a day for 5 days: Day 1 – 1.0 g (4 capsules), then from day 2 to day 5-500 mg (2 capsules) (a course dose of 3.0 g).

For urogenital tract infections caused by chlamydiatrachomatis (urethritis, cervicitis)

Uncomplicated urethritis / cervicitis – 1 g (4 capsules) once.

use to patients with impaired renal function

No dose adjustment is necessary for patients with moderate renal impairment (creatinine clearance > 40 ml / min).

Overdose

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

Treatment: gastric lavage, symptomatic therapy.

Special instructions

Do not take with food.

If a missed dose is missed, the missed dose should be taken as early as possible, and subsequent doses should be taken at 24 – hour intervals.

It is necessary to observe a break of 2 hours with simultaneous use of antacids.

After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under the supervision of a doctor.

Influence on the ability to drive vehicles and mechanisms

Azithromycin does not affect the ability to drive vehicles and mechanisms.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Active ingredient

Azithromycin

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

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

Indications

Pneumonia, Otitis Media, Bronchitis, Sore Throat, Skin Infections, Infectious Diseases, Urethritis