Azithromycin - instructions for use, dose, side effects, contraindications

Composition:One capsule contains: active substance: azithromycin dihydrate (in terms of azithromycin) - 250 mg,
auxiliary substances: sodium lauryl sulfate (sodium dodecyl sulfate), magnesium stearate, pregelatinized starch, polyvinylpyrrolidone and low molecular weight medical 12600 ± 2700 (povidone), hard gelatin capsules No. 0 (titanium dioxide, gelatin, methyl hydroxybenzoate, propylhydroxy benzoate, acetic acid).

Description:

Hard gelatin capsules № 0 of white color. The contents of the capsules are granules containing granules and white or almost white powder.

Pharmacotherapeutic group:Antibiotic - azalide

ATX: & nbsp

J.01.F.A.10 Azithromycin

Pharmacodynamics:

Antibacterial broad spectrum agent, azalide, a derivative of macrolides, acts bacteriostatically. Communicating with 50S subunit of ribosomes, inhibits peptidtranslokazu at the stage of translation, inhibits protein synthesis, inhibits the growth and reproduction of bacteria at high concentrations has a bactericidal effect. Effects on extracorporeal and intracellular pathogens. It is active against gram-positive microorganisms: Streptococcus spp. (groups C, F and G, except those resistant to erythromycin), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Staphylococcus epidermidis, Staphylococcus aureus; 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; and Chlamydia trachomatis, Chlamidia pneumoniae, Mycoplasma pneumoniae, Mycobaccterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi. Inactive against Gram-positive bacteria, resistant to erythromycin.

Pharmacokinetics:

Absorption is high, acid-fast, lipophilic. Bioavailability after a single dose of 0.5 g - 37% (the effect of "first passage" through the liver), the maximum concentration in the blood serum (Cmah) after oral intake of 0.5 g - 0.4 mg / l, the time to reach Cmah - 2.5 - 2.9 hours; in tissues and cells, the concentration is 10-50 times higher than in plasma, the volume of distribution -31.1 l / kg. Easily passes the histohematological barriers. It penetrates well into the respiratory tract, urino-genital organs and tissues, into the prostate gland, into the skin and soft tissues; accumulates in a medium with low pH, in lysosomes (which is especially important for the eradication of intracellular pathogens). It is also transported by phagocytes, polymorphonuclear leukocytes and macrophages. Penetrates through cell membranes. The concentration of azithromycin in the foci of infection is significantly higher (by 24-34%) than in healthy tissues and correlates with the severity of the inflammatory edema. It is stored in bactericidal concentrations for 5-7 days after the last dose. The connection with plasma proteins is 7-50% (inversely proportional to the concentration in the blood). In the liver demethylated, the metabolites formed are not active. Plasma clearance is high (630 ml / min). Elimination from serum takes place in two stages: the half-life between 8 and 24 hours after admission is 14-20 hours, the half-life in the interval from 24 to 72 hours is 41 hours. 50% is excreted with bile in unchanged form, 6% by kidneys. Eating significantly changes the pharmacokinetics: Cmah decreases by 52% and the area under the curve "concentration / time" (AUC) by 43%. In elderly men (65-85 years) the parameters of pharmacokinetics do not change, in women - Cmax (by 30-50%).

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation: upper respiratory tract infections and ENT organs: pharyngitis, tonsillitis, laryngitis, sinusitis, otitis media; scarlet fever; infections of the lower respiratory tract: pneumonia (including caused by atypical pathogens, chronic exacerbation), bronchitis; infections of the skin and soft tissues: erysipelas, impetigo, secondarily infected dermatoses; urinary tract infection: gonorrheal and non-renonary urethritis, cervicitis; Lyme disease (initial stage - erythema migrans), peptic ulcer of the stomach and duodenum, associated with Helicobacter pylori (as part of combination therapy).

Contraindications:

Hypersensitivity (including to other macrolides), hepatic and / or renal failure, lactation period, children under 12 years and / or with a body weight of less than 45 kg (for this dosage form).

Carefully:

Pregnancy, arrhythmia (possible ventricular arrhythmias and lengthening of the interval QT), children (12-18 years) with impaired liver or kidney function.

Pregnancy and lactation:

It can be used in cases when the benefit from its use significantly exceeds the risk that exists always when using any drug during pregnancy. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Inside, 1 hour before or 2 hours after meals 1 time per day.

Adults at infections of the top and bottom departments of respiratory ways - 0.5 g / day for 1 reception for 3 days (course dose -1.5 g).

With infections of the skin and soft tissues - 1 g / day on the first day for 1 reception, then 0.5 g / day daily from the 2nd to the 5th day (the course dose is 3 g).

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

With Lyme disease (borreliosis) for the treatment of stage I (erythema migrans) - 1 g on the first day and 0.5 g daily from the 2nd to the 5th day (the course dose is 3 g).

With peptic ulcer of the stomach and duodenum, associated with Helicobacter pylori - 1 g / day for 3 days as a combination of anti-Helicobacter therapy.

Children older than 12 years and / or with a body weight of more than 45 kg at infections of the top and bottom departments of respiratory ways, at infections of a skin and soft tissues 0.5 g once a day for 3 days.

In the treatment erythema migrans in children dose - 1g on the first day and 0.5 g from 2 to 5 days.

Side effects:

From the digestive system: ingestion - diarrhea (5%), nausea (3%), abdominal pain (3%); 1% or less - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of "liver" transaminases; Candidiasis of the oral mucosa; in children: constipation, anorexia, gastritis, taste change.

From the cardiovascular system: palpitation, chest pain (1% or less).

From the nervous system: dizziness, headache, drowsiness; children - headache (with medication otitis media), hyperkinesia, anxiety, neurosis, sleep disorders (1% or less).

From the genitourinary system: vaginal candidiasis, nephritis (1% or less).

Allergic reactions: rash, angioedema, in children: conjunctivitis, itching, urticaria.

Other: increased fatigue; photosensitization

Overdose:

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

Treatment: symptomatic therapy, gastric lavage.

Interaction:

Antacids (aluminum and magnesium-containing), ethanol and food slows down and reduces absorption.

With the co-administration of warfarin and azithromycin (in usual doses), no changes in prothrombin time have been detected, however, given the interaction of macrolides and warfarin, an anticoagulant effect may be enhanced, patients need careful monitoring of prothrombin time. Increases the concentration of digoxin. Ergotamine and dihydroergotamine: increased toxic effect (vasospasm, dysesthesia). Triazolam: reduced clearance and increased pharmacological action of triazolam. Slows down the excretion and increases the plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, and also the drug undergoing microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine phenytoin, oral hypoglycemic agents, theophylline and others xanthine derivatives) - due to the inhibition of microsomal oxidation in hepatocytes with azithromycin. Lincosamines weaken the effectiveness, tetracycline and chloramphenicol - strengthen.

Special instructions:

In case of missed dose, the missed dose should be taken as soon as possible, and the subsequent dose should be taken at intervals of 24 hours.

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

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

Form release / dosage:Capsules 250 mg.

Packaging:

For 6, 10 capsules in a contour mesh package. 1 or 2 contour packs with instructions for use in a pack of cardboard.

Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.

Shelf life:

2 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004914/08

Date of registration:25.06.2008

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp15.08.2015

Illustrated instructions

Instructions

Azithromycin (Azithromycin)