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

Kernel composition: active substance: erythromycin (in terms of the active substance) - 100 mg, 250 mg; Excipients: povidone-12.6 thousand (polyvinylpyrrolidone low molecular weight medical 12600 ± 2700) - 3.4 mg / 9.45 mg, crospovidone (kollidone TSL, kollidone CL-M) - 6.0 mg / 13.5 mg, calcium stearate - 1.85 mg / 4.14 mg, talc - 4.64 mg / 10.35 mg, potato starch - up to the core weight of 200 mg / 450 mg.

Shell composition: cellulose (acetylphthalic cellulose) - 8.1 mg / 16.2 mg, titanium dioxide (titanium dioxide - 0.4 mg / 0.8 mg), castor oil 1.5 mg / 3.0 mg.

Description:

Tablets are white or almost white, round, biconvex, covered with a film intestine-soluble coat, one layer of white is visible on the transverse section.

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 macro-lidov.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. (at 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. (in t.h. Legionella pneumophila), Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae; Haemophilus influenzae (some strains may beto erythromycin, but sensitive to other macrolide antibiotics);

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

Gram-negative rods are resistant to erythromycin: Escherichia coli and otherfamily members Enterobacteriaceae (Klebsiella spp., Proteus spp., Salmonella spp., Shigella spp. and others); Pseudomonas aeruginosa; Acinetobacter spp. and other non-fermenting bacteria, as well as anaerobic bacteria (Bacteroides spp., including Bacteroides fragilis), methicillin-resistant strains Staphylococcus aureus (MRSA) and enterococci Enterococcus spp., mycobacteria.

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 a film intestine-soluble membrane.

Time to reach the maximum concentration in the blood plasma after taking the tablets inside - 2-4 h, the connection with proteins - 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 ten times higher than that in 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 (BBB), into the cerebrospinal fluid (CSF) (the 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 increases somewhat. 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% in unmodified form, kidneys (unchanged) after oral administration - 2-5%.

Indications:

Bacterial infections caused by susceptible pathogens:

- infection of ENT organs (laryngitis, pharyngitis, tonsillitis, sinusitis, external and middle otitis media);

- infections of the lower respiratory tract (tracheitis, bronchitis, pneumonia);

- infections of the skin and soft tissues (pustular skin diseases, including youthful acne, infected wounds, pressure sores, burns II-III article, trophic ulcers);

- bile duct infection (cholecystitis);

- genitourinary infections in pregnant women caused by Chlamydia trachomatis;

- uncomplicated chlamydia in adults (with localization in the lower parts of the urogenital tract and rectum) with intolerance or inefficiency of tetracyclines;

- primary syphilis (in patients with an allergy to penicillins);

- gonorrhea;

- diphtheria (including bacteriocarriers), whooping cough (including prophylaxis), scarlet fever, trachoma, legionellosis (legionnaires' disease), erythrasma, listeriosis, amoebic dysentery;

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

Prevention of infectious endocarditis in dental procedures and operations on ENT organs in patients with risk factors (heart defects, prosthetic valves, etc.).

Erythromycin is a reserve antibiotic for allergy to penicillin and other antibiotics of the penicillin group, as well as to other beta-lactams.

Contraindications:

Hypersensitivity to erythromycin and other macrolides; significant hearing loss; simultaneous reception of terfenadine, astemizole, pimozide, ergotamine, dihydroergotamine, children under 14 years of age, the period of breastfeeding.

Carefully:

Arrhythmias (in the anamnesis), lengthening of the interval Q-T, jaundice (including history), hepatic and / or renal insufficiency.

If you have any of the listed diseases before taking the drug, be sure to consult a doctor.

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 tablet should be taken 1-2 hours before meals or 2-3 hours after meals.

The tablet can not be divided and chewed.

Adults and adolescents over 14 years of age: usual doses for most infections: single dose 250-500 mg, daily dose 1000-2000 mg (1-2 g). Erythromycin take 4 times a day, the interval between doses is 6 hours. With a daily dose of Erythromycin no more than 1 g / day - it is possible to take the drug 2 times a day (500 mg every 12 hours).

In severe infections, the daily dose of Erythromycin can be increased to 4 g (4000 mg). The maximum daily dose of Erythromycin for an adult is 4 g (4000 mg).

The course of treatment is 5-14 days, after the disappearance of symptoms the treatment is continued for another 2 days.

Treatment of streptococcal infections of various localizations (incl.tonsillo-pharyngitis) should last no less than 10 days.

For adolescents - 250 mg twice a day simultaneously with local therapy, then 1 month after the start of treatment, depending on the condition of the dose can be reduced to 250 mg once a day.

With urogenital chlamydial infections during pregnancy - 500 mg 4 times a day for at least 7 days or (with poor tolerance of this dose) - 250 mg 4 times a day (or 500 mg 2 times a day after 12 hours) for at least 14 days.

In uncomplicated chlamydia (urethral, endocervical or rectal) with intolerance tetracycline antibiotics - adults 500 mg 4 times a day for at least 7 days.

Treatment of primary syphilis - the course dose is 30-40 g duration of treatment - 10-15 days, the frequency of reception - 4 times a day. Treatment is preferable to begin with intravenous administration, with the subsequent transition to oral forms.

With gonorrhea - 500 mg g every 6 hours for 3 days, then 250 mg every 6 hours for 7 days.

Treatment of diphtheria bacteriocarrier - 250 mg twice a day for at least 7 days.

In whooping cough - 100-250 mg 4 times a day, the course of treatment 5-14 days.

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

In legionellosis (Legionnaires' disease) - in a daily dose of 2-4 g / day, divided into 4 doses (500-1000 mg 4 times a day) until the clinical symptoms of the disease disappear (but not less than 14 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.

With amoebic dysentery: adults and adolescents over 14 years - 250 mg 4 times a day. Duration of treatment is 10-14 days.

Prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with adult rheumatism - 250-500 mg 4 times a day, duration of the course - not less than 10 days.

Prophylaxis of infectious endocarditis in patients with heart defects in dental procedures and operations on ENT organs - adults 1 g (1000 mg) 1-2 hours before the treatment or diagnostic procedure, then 500 mg every 6 hours, 8 in total.

Side effects:

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

From the digestive system: nausea, vomiting, gastralgia, abdominal pain, tenesmus, diarrhea, dysbiosis, candidiasis of the oral cavity,pseudomembranous colitis, impaired liver function, cholestatic jaundice, increased activity of "liver" transaminases, pancreatitis.

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

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

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: impaired liver function, until acute liver failure, rarely hearing impairment.

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 and forced diuresis are ineffective.

Interaction:

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

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 methylprednisolone, 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 (LS), blocking tubular secretion, extend 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 the plasma may increase (because 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 until complete spasm, dysesthesia.

If you are taking other drugs, 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 ototoxic effect was higher in patients with renal and / or hepatic insufficiency, as well as in elderly patients.

May interfere with the determination of catecholamines in the urine and the activity of "liver" enzymes in the blood (colorimetric determination using definil- hydrazine).

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:

The use of the drug does not affect the management of vehicles and the maintenance of machines and mechanisms that require concentration of attention.

Form release / dosage:

Tablets, film-coated enteric-coated, 100 mg and 250 mg.

Packaging:

10 tablets in contoured cell packs.

1, 2 contour cells with instructions for use are placed in packs of cardboard.

Storage conditions:

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 expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N002882 / 01

Date of registration:14.07.2009

The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp29.09.2015

Illustrated instructions

Instructions

Erythromycin (Erythromycin)