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

Antibacterial agent of a wide spectrum of action, azalide, acts bacteriostatically. Communicating with 50S subunit of ribosomes, inhibits peptidranslokase at the stage of translation, suppresses protein synthesis, slows the growth and multiplication of bacteria, has a bactericidal effect at high concentrations. 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, Helicobacter pylori, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; as well as intracellular pathogens: Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium 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 plasma after oral intake of 0.5 g - 0.4 mg / l, the period of reaching the maximum concentration in blood plasma - 2,5-2,9 h; in tissues and cells the concentration is 10-50 times higher than in serum, the volume of distribution is 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. It penetrates the membranes of cells and creates high concentrations in them. The concentration 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 remains in effective 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. In the metabolism of the drug, isozymes participate CYP3A4, CYP3A5, CYP3A7, of which it is an inhibitor. Plasma clearance - 630 ml / min.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 kidney. Eating significantly changes the pharmacokinetics (depending on the dosage form): capsules - the maximum concentration in the blood plasma is reduced (by 52%). In elderly men (65-85 years) pharmacokinetic parameters do not change, in women the maximum concentration in blood plasma increases (by 30-50%), in children aged 1-5 years the maximum content in blood plasma, half-life decreases.

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; infection of the lower respiratory tract (pneumonia (including caused by atypical pathogens), bronchitis); infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses); urinary tract infection (gonorrheal and non-renal 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 other macrolides), severe hepatic / renal failure, lactation period, children under 12 years of age (with a body weight of less than 45 kg).

Carefully:

Arhythm (possible ventricular arrhythmias and lengthening of the interval Q-T), children with impaired liver or kidney function, pregnancy.

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 necessary, the appointment of the drug during lactation should stop 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 1 g. 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 - 3 g). With gastric ulcer and 12 duodenal ulcer associated with Helicobacter pylori, - 1 g / day for 3 days as a combination of anti-Helicobacter therapy.

Children over 12 years of age (with a body weight of more than 45 kg) with infections of the upper and lower respiratory tract, skin and soft tissues appoint 500 mg once a day for 3 days.

In the treatment erythema migrans in children (over 12 years), the drug is prescribed once a day at a dose of 1000 mg on the first day and 500 mg on days 2 to 5.

Side effects:

From the gastrointestinal tract: diarrhea (5%), nausea (3%), abdominal pain (3%); 1% or less - meteorism, vomiting, melena, cholestatic jaundice, increased activity of "liver" transaminases; in children - constipation, decreased appetite, gastritis; candidiasis of the oral mucosa, a change in taste (1% or less).

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 disorders (1% or less).

From the genitourinary system: vaginal candidiasis, nephritis (1% or less).Allergic reactions: rash, hives, itching of the skin, angioedema, in children - conjunctivitis.

Other: asthenia, photosensitivity.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy.

Interaction:

Antacids (aluminum and magnesium-containing), ethanol and food slow down and reduce the absorption of azithromycin.

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.

Increases the concentration of digoxin due to the weakening of its inactivation by intestinal flora.

Ergotamine and dihydroergotamine: increased toxic effect (vasospasm, dysesthesia). Triazolam: reduced clearance and increased pharmacological action of triazolam. Slows the elimination and increases the concentration in the plasma and the toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs undergoing microsomal oxidation (carbamazepine, terfenadine, ciclosporin, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic drugs, theophylline and others xanthine derivatives), due to the inhibition of microsomal oxidation in hepatocytes with azithromycin.

Lincosamides weaken, and tetracycline and chloramphenicol increase the effectiveness of azithromycin.

Special instructions:

Do not take with food.

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 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 for 250 mg.

Packaging:

By 3, 6 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 3, 6, 12, 18, 24, 30, 36, 42, 48, 54 or 60 capsules in cans of polyethylene terephthalate or cans of polymeric for medicinal purposes means.

One jar or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 contour mesh packages together with the instruction for use are placed incardboard packaging (bundle).

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003652/07

Date of registration:07.11.2007 / 01.06.2016

Expiration Date:Unlimited

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp22.06.2017

Illustrated instructions

Instructions

Azithromycin (Azithromycin)