Active substanceErythromycinErythromycin
Dosage form: & nbspenteric coated tablets
Composition:

1 tablet contains:

active substance: erythromycin (in terms of the active substance) 100 mg or 250 mg;

Excipients: potato starch, calcium stearate, povidone (low molecular weight polyvinylpyrrolidone 12600 ± 2700), polysorbate 80 (tween 80);

composition of the shell: cellulose acetate (acetylphthalyl cellulose), castor oil, titanium dioxide.

Description:

The tablets covered with a cover, the round form with biconcave surfaces of white or white with a grayish shade of color.

Pharmacotherapeutic group:antibiotic-macrolide
ATX: & nbsp

S.01.A.A.17   Erythromycin

J.01.F.A.01   Erythromycin

Pharmacodynamics:

Bacteriostatic antibiotic from the group of macrolides, reversibly binds to 50S subunit of ribosomes in its donor part, which disrupts the formation of peptide bonds between amino acid molecules and blocks the synthesis of proteins of microorganisms (does not affect the synthesis of nucleic acids).When used in high doses, it may exhibit bactericidal action. The spectrum of action includes gram positive (Staphylococcus spp., producing and not producing penicillinase, incl. Staphylococcus aureus; Streptococcus spp. (incl. Streptococcus pneumoniae, Streptococcus pyogenes), alpha-hemolytic streptococcus (groups Viridans), Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium minutissimum) and gram-negative microorganisms (Neisseria gonorrhoeae, Haemophilus influenzae, Bordetella pertussis, Brucella spp., Legionella spp., incl. Legionella pneumophila) and other microorganisms: Mycoplasma spp. (in t.h. Mycoplasma pneumoniae), Chlamydia spp. (in t.h. Chlamydia trachomatis), Treponema spp., Rickettsia spp., Entamoeba histolytica, Listeria monocytogenes.

Gram-negative rods are stable: Escherichia coli, Pseudomonas aeruginosa, and Shigella spp., Salmonella spp. and etc. Sensitive groups include microorganisms, whose growth is delayed at an antibiotic concentration of less than 0.5 mg / l, medium sensitivity - 1-6 mg / l, moderately resistant and stable - 6-8 mg / l.

Pharmacokinetics:

Absorption is high. The ingestion of food does not affect the oral forms of erythromycin in the form of a base, covered with an enteric membrane. The maximum concentration (CmOh) is achieved after oral administration in 2-4 hours. Communication with plasma proteins is 70-90%.

Bioavailability is 30-65%. In the body it is distributed unevenly. In large quantities, it accumulates in the liver, spleen, kidneys. In bile and urine, the concentration is tens of times higher than the concentration in the plasma.It penetrates well into the tissues of the lungs, lymph nodes, exudate of the middle ear, secretion of the prostate gland, sperm, pleural cavity, ascitic and synovial fluid. The milk of lactating women contains 50% of the concentration in the plasma. Poorly penetrates the blood-brain barrier, into the cerebrospinal fluid (its concentration is 10% of the content of the drug in the plasma). In inflammatory processes in the membranes of the brain, their permeability for erythromycin slightly increases. It penetrates the placental barrier and enters the blood of the fetus, where its content reaches 5-20% of the content in the mother's plasma.

Metabolised in the liver (more than 90%), partially with the formation of inactive metabolites. The half-life (T1/2) - 1.4-2 h, with anuria - 4-6 hours Excretion with bile - 20-30% in unmodified form, kidneys (unchanged) after oral administration - 2-5%.

Indications:

- Bacterial infections caused by sensitive microflora: diphtheria (including bacteriocarrier), whooping cough (including prophylaxis), trachoma, brucellosis, legionnaires, erythrasma, listeriosis, scarlet fever, amoebic dysentery, gonorrhea; conjunctivitis of newborns, pneumonia in children, urogenital infections in pregnant women, caused by Chlamydia trachomatis.

- Primary syphilis (in patients with penicillin allergy), uncomplicated chlamydia in adults (with localization in the lower sections of the urogenital tract and rectum) with intolerance or inefficiency of tetracyclines, etc.

- Infections of the ENT organs (tonsillitis, otitis, sinusitis).

- Infections of the biliary tract (cholecystitis);

- Infections of the upper and lower respiratory tract (tracheitis, bronchitis, pneumonia);

- Infections of the skin and soft tissues (pustular skin diseases, including youth acne, infected wounds, pressure sores, burns II-III st, trophic ulcers).

- Infections of the mucous membrane of the eyes.

- Prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with rheumatism. Prevention of infectious complications in medical and diagnostic procedures (including preoperative intestinal preparation, dental interventions, endoscopy, in patients with heart defects).

Contraindications:

Hypersensitivity, hearing loss, simultaneous reception of terfenadine or astemizole, children's age to 3 years, lactation.

Carefully:

Arrhythmias (in the anamnesis), lengthening of the interval QT, jaundice (history), hepatic and / or renal insufficiency.

Pregnancy and lactation:

In connection with the possibility of penetration into breast milk, it is necessary to refrain from breast-feeding while prescribing erythromycin.

Dosing and Administration:

Inside.

A single dose for adults and adolescents over the age of 14 is 0.25-0.5 g, daily - 1-2 g. The interval between administration is 6 hours. In severe infections, the daily dose can be increased to 4 g.

Children from 3 to 14 years, depending on the age, body weight and severity of infection - 30-50 mg / kg / day in 2-4 admission. In case of severe infections, the dose can be doubled.

For the treatment of diphtheria carriage - 0.25 g 2 times a day. The course dose for the treatment of primary syphilis is 30-40 g, the duration of treatment is 10-15 days.

With amoebic dysentery adults - 0.25 grams 4 times a day, children - 30-50 mg / kg / day; the duration of the course is 10-14 days.

In legionellosis, 0.5-1 g four times a day for 14 days.

With gonorrhea - 0.5 g every 6 hours for 3 days, then 0.25 g every 6 hours for 7 days.

For preoperative preparation of the intestine in order to prevent infectious complications - inside, 1 g for 19 hours, 18 hours and 9 hours before the start of surgery (only 3 g).

To prevent streptococcal infection (with tonsillitis, pharyngitis), adults - 20-50 mg / kg / day, children - 20-30 mg / kg / day, the course duration - at least 10 days.

For the prevention of septic endocarditis in patients with heart defects, 1 g for adults and 20 mg / kg for children, 1 hour before the therapeutic or diagnostic procedure, then 0.5 g for adults and 10 mg / kg for children , again after 6 hours.

In whooping cough - 40-50 mg / kg / day for 5-14 days.

When pneumonia in children, 50 mg / kg / day in 4 divided doses, for at least 3 weeks.

For urogenital infections during pregnancy - 0.5 g 4 times a day for at least 7 days or (if the tolerance is poor) - 0.25 g 4 times a day for at least 14 days.

In adults, with uncomplicated clamidiosis and intolerance to tetracyclines - 0.5 g 4 times a day for at least 7 days.

Side effects:

Hypersensitivity reactions: skin allergic reactions (hives, other forms of rash), eosinophilia, rarely anaphylactic shock.

Nausea, vomiting, gastralgia, tenesmus, abdominal pain, diarrhea, dysbacteriosis, rarely oral candidiasis, pseudomembranous enterocolitis (both during and after treatment), liver dysfunction, cholestatic jaundice, increased activity of "liver" transaminases, pancreatitis , hearing loss and / or tinnitus (when using high doses - more than 4 g / day, hearing loss after withdrawal of the drug is usually reversible).

Rarely - tachycardia, lengthening of the interval QT on ECG, ventricular arrhythmias, including ventricular tachycardia (of the "pirouette" type), in patients with an elongated interval QT.

Overdose:Symptoms: a violation of the liver, up to acute liver failure, hearing loss.
Treatment: activated charcoal, careful monitoring of the state of the respiratory system. Gastric lavage is effective when taking a dose five times higher than the average therapeutic dose. Hemodialysis, peritoneal dialysis, forced diuresis are ineffective.
Interaction:

Drugs that block tubular secretion, prolong the half-life of erythromycin.

Incompatible with lincomycin, clindamycin and chloramphenicol (antagonism).

Reduces the bactericidal action of beta-lactam antibiotics (penicillins, cephalosporins, carbopenems).

With simultaneous administration with drugs metabolized in the liver (theophylline, carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, disopyramide, lovastatin, bromocriptine), the concentration of these drugs in the plasma may increase (it is an inhibitor of microsomal liver enzymes).

Increases the nephrotoxicity of cyclosporine (especially in patients with concomitant renal failure). Reduces the clearance of triazolam and midazolam, and therefore can enhance the pharmacological effects of benzodiazepines.

With simultaneous reception with terfenadine or astemizole - the possibility of arrhythmia development, with dihydroergotamine or unhydrogenated ergot alkaloids - vasoconstriction before spasm, dysesthesia.

Slows down the elimination (increases the effect) of methylprednisolone, felodipine and anticoagulants of the coumarin series.

With a joint appointment with lovastatinum, rhabdomyolysis is increased. Increases the bioavailability of digoxin.

Reduces the effectiveness of hormonal contraception.

Special instructions:

With prolonged therapy, it is necessary to monitor the laboratory parameters of liver function.

Symptoms of cholestatic jaundice can develop a few days after the start of therapy, but the risk of developing increases after 7-14 days of continuous therapy. The probability of development of ototoxic effect is higher in patients with renal and hepatic insufficiency, as well as in elderly patients.

Some resistant strains Haemophilus influenzae are sensitive to the simultaneous administration of erythromycin and sulfonamides.

May interfere with the determination of catecholamines in urine and the activity of "liver" transaminases in the blood (colorimetric determination with the help of de-nylhydrazine).
Form release / dosage:

Tablets, covered with enteric coating, 100 mg and 250 mg.

Packaging:

For 10 or 20 tablets in cans of orange glass or in polymer cans. For 10 tablets in a contoured cell packaging made of polyvinylchloride film and aluminum foil printed lacquered or paper with polyethylene coating.

Each bank, 1 or 2 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry 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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription
Registration number:LSR-009305/08
Date of registration:24.11.2008
The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia
Manufacturer: & nbsp
Representation: & nbspBIOSINTEZ JSC BIOSINTEZ JSC Russia
Information update date: & nbsp30.09.2015
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