Azitral, 500 mg capsules 3 pcs

Pharmacological action Pharmacological action – broad spectrum antibacterial.

Pharmacodynamics

A broad spectrum antibiotic. It is a representative of the subgroup of macrolide antibiotics – azalides. It has a broad spectrum of antimicrobial action. Binding to 50S-subunit of ribosome, it inhibits protein biosynthesis of the microorganism. At high concentrations in the center of inflammation it produces bactericidal action.

Active against Gram-positive aerobic microorganisms: Streptococcus spp. (groups A, B, C, G), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes, Staphylococcus aureus (methicillin-sensitive); Gram-negative aerobic microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Legionella pneumophila, Neisseria gonorrhoeae, Pasteurella multocida; some anaerobic microorganisms: Prevotella spp., Clostridium perfringens, Fusobacterium spp., Porphyriomonas spp.; and Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

Microorganisms capable of developing resistance to azithromycin: Gram-positive aerobes (Streptococcus pneumoniae (penicillin-resistant).

Initially resistant microorganisms: Gram-positive aerobes (Enterococcus faecalis, Staphylococcus spp. (methicillin-resistant staphylococci show very high resistance to macrolides), erythromycin-resistant gram-positive bacteria); anaerobes (Bacteroides fragilis).

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, Cmax of azithromycin in plasma is reached after 2.5-2.96 hours and is 0.4 mg/l. Bioavailability is 37%.

Asithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular the prostate gland), skin and soft tissues. High tissue concentrations (10-50 times higher than in blood plasma) and long T1/2 are due to low binding of azithromycin to blood plasma proteins and to its ability to penetrate into eukaryotic cells and to concentrate in low pH environment surrounding lysosomes. This, in turn, determines the large apparent Vd (31.1 L/kg) and high plasma clearance. The ability of azithromycin to accumulate predominantly in lysosomes is particularly important for the elimination of intracellular pathogens. It is proved that phagocytes deliver azithromycin to the sites of infection localization, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in the healthy tissues (on the average by 24-34%), and correlates with the degree of inflammatory edema. Despite its high concentration in phagocytes, azithromycin has no significant effect on their function. Azithromycin persists in bactericidal concentrations for 5-7 days after the last dose, which allowed to develop short (3- and 5-day) courses of treatment.

50% is excreted unchanged in the bile, 6% – by the kidneys, in the liver it is demethylated, the resulting metabolites are inactive.

Eating significantly changes pharmacokinetics (depending on the dosage form): Capsules – Cmax in plasma is decreased (by 52%) and AUC by 43%.

In elderly men (65-85 years old) pharmacokinetic parameters do not change, in women Cmax increases by 30-50%.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin:

Infections of the upper respiratory tract and ENT (sore throat, sinusitis, tonsillitis, pharyngitis, otitis media);

Lower respiratory tract infections (bacterial pneumonia, including.

infections of the lower respiratory tract (bacterial pneumonia, including those caused by atypical pathogens, bronchitis);

dermal and soft tissue infections (rye, impetigo, secondary infectious dermatoses);

infections of the urogenital tract (uncomplicated urethritis and/or cervicitis) caused by Chlamydia trachomatis;

Lyme disease (borreliosis), to treat the initial stage (erythema migrans).

Active ingredient

Composition

1 capsule contains:

The active ingredient: azithromycin dihydrate – 525.0 mg, in terms of azithromycin – 500.0 mg;

Excipients: sodium lauryl sulfate – 3.0 mg, magnesium stearate – 2.0 mg.

The capsule shell (cap and casing): titanium dioxide (E171) – 1.1999%; water – 14.5 ± 1.5%; sodium lauryl sulfate – 0.08%; methyl parahydroxybenzoate – 0.64 to 0.8%; propyl parahydroxybenzoate – 0.16 to 0.2%; gelatin – up to 100%

How to take, the dosage

Ingestion, 1 hour before or 2 hours after meals once a day.

Infections of the upper and lower respiratory tract, ENT, skin and soft tissue in adults (including elderly people) and children over 12 years of age with body weight over 45 kg – 500 mg/d by 1 course for 3 days (course dose – 1.5 g).

In acute infections of the urogenital tract (uncomplicated urethritis or cervicitis) 1 g once.

In Lyme disease (borreliosis) to treat stage I (erythema migrans) – 1 g on day 1 and 500 mg daily from day 2 to day 5 (course dose – 3 g).

For patients with moderate renal dysfunction (Cl creatinine >40 ml/min) no dose adjustment is required.

Interaction

Antacids (aluminum- and magnesium-containing), ethanol and food reduce absorption of azithromycin, so the interval between their intake should be 1 h before or 2 h after meals and these drugs.

If co-administration with warfarin is necessary, close monitoring of PV is recommended. When concomitant use with cyclosporine, blood concentrations should be monitored and the dose of the latter should be adjusted.

Asithromycin increases zidovudine triphosphate (active metabolite of zidovudine) in mononuclear cells; the clinical significance of this phenomenon is unknown.

Digoxin: Increased concentration of digoxin.

Ergotamine and dihydroergotamine: increased toxic effects (vasospasm, dysesthesia).

Triazolam: decreased clearance and increased pharmacological action of triazolam.

Delays excretion and increases plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, and drugs that undergo 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.

Caution should be exercised when co-administering terfenadine and azithromycin, because concomitant administration of terfenadine and various types of antibiotics has been found to cause arrhythmias and prolongation of the QT interval. Therefore, these complications cannot be excluded when terfenadine and azithromycin are taken together.

The lincosamines impair efficacy; tetracycline and chloramphenicol increase efficacy.

Special Instructions

If a dose is missed, the missed dose should be taken as soon as possible, and the next dose should be taken 24 hours apart.

A 2-hour break should be observed with concomitant use of antacids.

As with any antibiotic therapy, treatment with azithromycin may lead to superinfection (including fungal infection). In pharyngitis and tonsillitis caused by Streptococcus pyogenes, penicillins are the antibiotics of choice. The effectiveness of azithromycin for prevention of rheumatic fever is unknown.

After treatment withdrawal, hypersensitivity reactions may persist in some patients, requiring specific therapy under medical supervision.

The effect on the ability to drive vehicles, machinery. Azithromycin in doses greater than recommended may affect the ability to operate a vehicle or equipment.

Contraindications

Hypersensitivity to azithromycin, other components of the drug and other macrolides;

Severe hepatic and/or renal impairment;

Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

concomitant use with ergotamine and dihydroergotamine;

Period of lactation (suspend the treatment);

children under 12 years of age (body weight less than 45 kg).

With caution: hepatic and/or renal insufficiency; simultaneous use with terfenadine, warfarin, digoxin; arrhythmias or predisposition to arrhythmias and QT interval prolongation.

Side effects

Digestive system disorders: diarrhea, nausea, abdominal pain; dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased liver transaminase activity; in children – constipation, anorexia, gastritis, indigestion, discolored tongue, pseudomembranous colitis, hepatitis, liver dysfunction, liver necrosis (possibly with fatal outcome).

Cardiovascular disorders: palpitations, chest pain, arrhythmia, ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia.

Nervous system disorders: dizziness, headache, somnolence, vertigo, seizures, paresthesia, asthenia, hyperactivity, aggressiveness, restlessness, nervousness; in children – headache (in otitis media therapy), hyperkinesia, anxiety, neurosis, sleep disorders.

Sensory organs: tinnitus, reversible hearing impairment up to deafness (when taking high doses for a long time), disorders of perception of taste and smell.

Allergic reactions: rash, photosensitization, Quincke’s edema, skin itching, anaphylactic reaction, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Urogenital system disorders: acute renal failure, vaginal candidiasis, nephritis.

Other: thrombocytopenia, neutropenia, vaginitis, arthralgia, increased fatigue, oral candidomycosis; in children – conjunctivitis, urticaria.

Overdose

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

Treatment: symptomatic. There is no specific antidote.

Pregnancy use

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