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

Excipients: milk sugar (lactose), cellulose microcrystalline, polyvinylpyrrolidone low molecular weight medical (povidone), magnesium stearate, silicon dioxide colloid (aerosil).

Capsule composition: gelatin, water, titanium dioxide.

Description:

Hard gelatin capsules of white color number 0. Contents of capsules - white or white powder with a yellowish tinge.

Pharmacotherapeutic group:Antibiotic-azalide

ATX: & nbsp

J.01.F.A.10 Azithromycin

Pharmacodynamics:

Antibiotic of a wide spectrum of action. Is a representative of a subgroup of macrolide antibiotics - azalides.When creating a high inflammation in the focus of inflammation has a bactericidal effect.

Gram-positive cocci is sensitive to azithromycin: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococcus groups C, F and G, Staphylococcus aureus, Staphylococcus viridans; Gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, B. parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; and Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi. Azithromycin is inactive against gram-positive bacteria resistant to erythromycin.

Pharmacokinetics:

Azithromycin is rapidly absorbed from the digestive tract, which is due to its resistance to acidic environment and lipophilicity. After oral administration of 500 mg, the maximum concentration of azithromycin in the blood plasma is achieved after 2.5 - 2.96 hours and is 0.4 mg / l. Bioavailability is 37%.

Azithromycin well penetrates the respiratory tract, organs and tissues of the urogenital tract (particularly the prostate gland), the skin and soft tissues. High concentrations in tissues (10-50 times higher than in plasma) and a long half-life are due to low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a medium with a low pH surrounding the lysosome.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. It is proved that phagocytes deliver azithromycin in places of infection localization, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (an average of 24-34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin does not have a significant effect on their function. Azithromycin remains in bactericidal concentrations in the inflammatory focus within 5-7 days after the last dose, which allowed to develop short (3-day and 5-day) treatment courses.

In the liver demethylated, the metabolites formed are not active.

Excretion of azithromycin from the blood plasma takes place in 2 stages: the half-life period is 14-20 hours in the interval from 8 to 24 hours after the drug administration and 41 hours in the interval from 24 to 72 hours, which allows using the drug once a day.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

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

Scarlet fever;

Infections of the lower respiratory tract (including those caused by atypical pathogens);

Infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);

Infections of the urogenital tract (uncomplicated urethritis and / or cervicitis);

Lyme disease (borreliosis), for treatment of the initial stage (erythema migrans);

Disease of the stomach and duodenum associated with Helicobacter Pylori (as part of combination therapy).

Contraindications:

Hypersensitivity (including to other macrolides); hepatic and / or renal insufficiency; lactation period;

Children under 12 years (weighing less than 45 kg).

Carefully:Arrhythmia.

Pregnancy and lactation:

Can be used during pregnancy, when the benefit of using it significantly exceeds the risk that exists always when using any drug during pregnancy.

If it is necessary to appoint during the lactation period, it is necessary to resolve the issue of stopping breastfeeding.

Dosing and Administration:

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

Adults with infections of the upper and lower respiratory tract - 500 mg / day for 1 reception for 3 days (course dose - 1500 mg).

For infections of the skin and soft tissues - 1000 mg / day on the first day for 1 reception, then 500 mg / day daily from 2 to 5 days (course dose - 3000 mg).

In acute infections of the urogenital organs (uncomplicated urethritis or cervicitis) - once 1000 mg.

With Lyme disease (borreliosis) for treatment of stage I (erythema migrans) - 1000 mg on the first day and 500 mg daily from 2 to 5 days (course dose - 3000 mg).

With peptic ulcer of the stomach and duodenum, associated with Helicobacter pylori - 1000 mg / day for 3 days as a combination of anti-Helicobacter therapy.

Children older than 12 years (weighing more than 45 kg) with infections of the lower and upper respiratory tract, skin and soft tissues - 500 mg / day for 1 reception for 3 days.

In the treatment erythema migrans - 1st day of 1000 mg, from 2nd to 5th 500 mg once a day.

Side effects:

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

From the side of 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 disturbance (1% or less).

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

Allergic reactions: rash, angioedema, itching, hives. Children - conjunctivitis, itching, hives.

Other: increased fatigue.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy.

Interaction:

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

When co-administration of warfarin and azithromycin (in normal doses) changes in prothrombin time were found, however, given that the interaction of macrolides and warfarin may be increased anticoagulant effect, patients requires careful monitoring of the prothrombin time.

Digoxin: increased digoxin concentration.

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

Triazolam: reduced clearance and increased pharmacological action of triazolam.

Slows down the excretion and increases plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs exposed to microsomal oxidation (carbamazepine, terfenadine, ciclosporin, 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 of 250 mg.

Packaging:

6 or 10 capsules per contour cell package; for 6 or 10 capsules in a can of light-protective glass or in a can of polymer or a polymer bottle.

Each jar or vial or one contour mesh package together with the instruction for use is placed in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006658/08

Date of registration:15.08.2008 / 14.05.2010

Expiration Date:Unlimited

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp22.06.2017

Illustrated instructions

Instructions

Azithromycin (Azithromycin)