Erythromycin-LekT - instructions for use, dose, side effects, contraindications

Tablets are round, biconvex, covered with enteric film membrane, white or grayish-white, on the cross-section the nucleus is white or white with a yellowish hue.

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, 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 depending on the type of pathogen can exhibit bactericidal action.

To sensitive are microorganisms, whose growth is delayed at an antibiotic concentration of less than 0.5 mg / l, to moderately sensitive - 1-6 mg / l, to stable - more than 6 mg / l.

A wide spectrum of antimicrobial action of erythromycin includes:

Gram-positive microorganisms: Staphylococcus spp., producing and non-producing penicillinase, incl. Staphylococcus aureus (except strains resistant to methicillin MRSA); Streptococcus spp. (in t.h. Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. groups viridans): Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium minutissimum, Listeria monocytogenes;

gram-negative microorganisms: Bordetella pertussis, Campylobacter jejuni, Legionella spp (including Legionella pneumophila), Moraxella (Branhamella) catarrhalis; and other microorganisms: Mycoplasma spp. (including Neisseria gonorrhoeae, Haemophilus influenzae (some strains may be resistant to erythromycin, but sensitive to other macrolide antibiotics);

other microorganisms: Chlamydia spp. (incl. Chlamydia trachomatis), Mycoplasma spp. (in t.h. Mycoplasma pneumoniae), Ureaplasma urealyticum, Treponema spp., Propionibacterium acnes, Entamoeba histolytica.

To erythromycin resistant gram-negative rods: Escherichia coli and other members of the family Enterobacteriaceae (Klebsiella spp., Proteus spp., Shigella spp., Salmonella spp. and others); Pseudomonas aeruginosa; Acinetobacter spp. And other non-fermenting bacteria, as well as anaerobic bacteria (Bacteroides spp., including Bacteroides Iragilis), methicillin-resistant strains Staphylococcus aureus (MRSA) and enterococci Enterococcus spp., microbacteria.

Is a receptor agonist motilin. Accelerates the evacuation of gastric contents by increasing the amplitude of contraction of the pylorus and improving the antral-duodenal coordination, possesses prokinetic properties.

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 time to reach the maximum concentration in the blood plasma after ingestion is 2-4 hours, the connection with 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. In the metabolism of erythromycin, isozymes participate CYP3A4, CYP3A5 and CYP3A7, the inhibitor of which it is.

The half-life (T_1/2) - 1,4-2 hours, with anuria 4-6 hours. Excretion with bile - 20-30% unchanged, kidneys (unchanged) after oral administration - 2-5%.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to erythromycin: diphtheria (including bacteriocarrier), trachoma, brucellosis, Legionella pneumophila (Legionnaires' disease), erythrasma, listeriosis, scarlet fever, amoebic dysentery, gonorrhea; infection of the ENT organs (tonsillitis, otitis media, sinusitis); bile duct infection (cholecystitis); whooping cough (including prevention); infections of the upper and lower respiratory tract (tracheitis, bronchitis, pneumonia); Skin and soft tissue infections (pustular skin diseases, including acne vulgaris, infected wounds, pressure ulcers, burns II-III degree, trophic ulcers), infections of the eye mucosa.

Prevention of infectious complications in medical and diagnostic procedures (including preoperative intestinal preparation, dental interventions, endoscopy, in patients with heart defects).

Prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with rheumatism.

Genitourinary infections in pregnant women caused by Chlamydia trachomatis; uncomplicated chlamydia in adults (with localization in the lower sections of the urogenital tract and rectum) with intolerance or inefficiency of tetracyclines, etc.

Contraindications:

Hypersensitivity to erythromycin and other macrolides; significant hearing loss; simultaneous reception of terfenadine, astemizole, pimozide, cisapride, lactation period, children under 14 years (for this dosage form).

Carefully:

Arrhythmias (in the anamnesis), an increase in the duration of the ventricular complex on the electrocardiogram (lengthening of the interval QT), jaundice (history), hepatic and / or renal failure, use during pregnancy.

Pregnancy and lactation:

The use of Erythromycin in pregnancy is possible only if the expected benefit to the mother exceeds the potential risk to the fetus.

During lactation due to the possibility of penetration into breast milk, one should refrain from breast-feeding while using Erythromycin.

Dosing and Administration:

Inside (the mode of taking the drug and eating is determined by the dosage form and its resistance to the effects of gastric juice). The tablet should be taken 1-2 hours before meals or 2-3 hours after meals. The tablet can not be divided and chewed. A single dose for adults is 250-500 mg. The average daily intake for adults is 1-2 g in 2-4 doses, the maximum daily dose is 4 g.

Children from 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 g 4 times a day, the duration of the course - 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.

When gastroparesis - inside (for the treatment of gastroparesis, erythromycin for intravenous administration) for 0.15-0.25 g for 30 minutes before meals 3 times a day.

With scarlet fever - in usual doses, the course of treatment - at least 10 days.

When listeriosis - 250-500 mg 4 times a day for at least 7 days, etiotropic therapy is performed until the 6-7th day of normal temperature, and in severe forms - until 14-21 day.

When erythrasis - 250 mg 4 times a day for 5-7 days at the same time with external means.

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 operation (only 3 g).

For the prevention of streptococcal infection (with tonsillitis, pharyngitis), adults - 20-50 mg / kg / day, children from 14 years - 20-30 mg / kg / day, the course duration - not less than 10 days.

For the prevention of septic endocarditis in patients with heart defects - 1 g for adults and 20 mg / kg for children over 14 years, 1 hour before the treatment 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.

With urogenital infections during pregnancy - 0.5 g 4 times a day for at least 7 days or (with poor tolerance of this dose) to 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:

Allergic reactions: urticaria, other forms of skin rash, eosinophilia, anaphylactic shock.

From the digestive system: nausea, vomiting, gastralgia, abdominal pain, tenesmus, diarrhea, dysbacteriosis, oral cavity candidiasis, pseudomembranous colitis (both during and after treatment), liver dysfunction, cholestatic jaundice, increased activity of "liver" transaminases, pancreatitis .

From the side of the hearing organ: hearing loss and / or tinnitus (when used in high doses - more than 4 g / day, usually reversible).

From the side of the cardiovascular system: tachycardia, prolongation of the Q-T interval on an electrocardiogram, flicker and / or atrial flutter (in patients with an extended Q-T interval on an electrocardiogram).

Overdose:

Symptoms: impaired liver function, up to acute liver failure, hearing loss.

Treatment: Activated carbon, careful monitoring of the state of the respiratory system (if necessary - carrying out artificial ventilation of the lungs), acid-base state and electrolyte exchange, electrocardiogram.

Gastric lavage is effective when taking a dose five times higher than the average therapeutic dose.

Hemodialysis, peritoneal dialysis, forced diuresis are ineffective.

Interaction:

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

Incompatible with lincomycin, clindamycin and chloramphenicol (antagonism).

Increases the concentration of theophylline.

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.

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

When combined with lovastatin, simvastatin and other statins, the risk of rhabdomyolysis increases.

Increases the bioavailability of digoxin.

Reduces the effectiveness of hormonal contraception.

Drugs that block tubular secretion, lengthen T_1/2Erythromycin.

When combined with drugs that are metabolized in the liver by the cytochrome P450 system (carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, disopyramide, lovastatin, bromocriptine), the concentration of these drugs in plasma may increase (since erythromycin is an inhibitor of microsomal liver enzymes).

When combined with terfenadine or astemizole may develop arrhythmias (ventricular flicker and flutter, ventricular tachycardia, or death) with dihydroergotamine or unhydrogenated ergot alkaloids - vasoconstriction before full contraction, dysesthesia.

If you are taking other medications, you should consult your doctor.

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 likelihood of developing an ototoxic effect is higher in patients with renal and / or 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 the urine and the activity of "hepatic" transaminases in the blood (colorimetric determination with the help of de-nylhydrazine).

Do not drink milk or dairy products.

In numerous clinical trials, the antrum and duodenal prokinetic effect of erythromycin was demonstrated.

Effect on the ability to drive transp. cf. and fur:

Data on the adverse effects on the ability to drive vehicles and mechanisms are not identified, but it is recommended that patients administering vehicles use the drug with extreme caution.

Form release / dosage:

Tablets coated with enteric film coating, 250 mg.

Packaging:

For 20 tablets in cans of orange glass.

10 tablets per contour cell pack.

One jar or 1-2 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

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:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001192

Date of registration:11.11.2011

The owner of the registration certificate:Tyumen Chemical - Pharmaceutical Plant, OJSC Tyumen Chemical - Pharmaceutical Plant, OJSC Russia

Manufacturer: & nbsp

Tyumen Chemical - Pharmaceutical Plant, OJSC Russia

Information update date: & nbsp29.09.2015

Illustrated instructions

Instructions

Erythromycin-LekT (Erythromycin-LekT)