Erythromycin 250 mg 20 tablets, enteric-coated

Indications

Bacterial infections caused by erythromycin-sensitive pathogens:
• infections of the ENT organs (laryngitis, pharyngitis, tonsillitis, external and middle ear infections, sinusitis).
• infections of the lower respiratory tract (tracheitis, bronchitis, pneumonia);
• infections of the skin and soft tissues (purulent skin diseases, including acne vulgaris, infected wounds, pressure sores, burns of II-III degree, trophic ulcers);
• infections of the biliary tract (cholecystitis);
• urogenital infections in pregnant women caused by Chlamydia trachomatis;
• uncomplicated chlamydia in adults (localized in the lower urinary tract and rectum) in cases of intolerance or ineffectiveness of tetracyclines;
• primary syphilis (in patients allergic to penicillins);
• gonorrhea;
• scarlet fever, legionellosis (Legionnaires' disease), listeriosis, trachoma;
• diphtheria carrier state, whooping cough, erythrasma, amoebic dysentery.
Prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with rheumatism.
Prevention of infectious endocarditis during dental procedures and surgeries on ENT organs in patients with risk factors (heart defects, prosthetic valves, etc.).
Erythromycin is a reserve antibiotic for patients allergic to penicillin and other penicillin group antibiotics, as well as to other beta-lactams.

Method of administration and doses

Orally. Tablets should be taken 1-2 hours before meals or 2-3 hours after meals. Tablets should not be divided or chewed.
For most infections, the single dose for adults and adolescents over 14 years is 250-500 mg, and the daily dose is 1000-2000 mg. In severe infections, the daily dose may be increased to 4000 mg.
Erythromycin is taken 4 times a day, with an interval of 6 hours between doses. If the daily dose of erythromycin does not exceed 1000 mg/day, the medication can be taken 2 times a day (500 mg every 12 hours).
For children aged 3 to 14 years, depending on age, body weight, and severity of the infection, the dose is 30-50 mg/kg/day in 2-4 doses. In severe infections, the dose may be doubled.
The course of treatment is 5-14 days; after the symptoms disappear, treatment should continue for another 2 days.
Treatment of streptococcal infections of various localizations (including tonsillopharyngitis) should last at least 10 days.
For adolescent acne, 250 mg 2 times a day in conjunction with local therapy; then, after 1 month from the start of treatment, depending on the condition, the dose may be reduced to 250 mg once a day.
For urogenital chlamydial infections during pregnancy, 500 mg 4 times a day for at least 7 days or (if this dose is poorly tolerated) 500 mg 2 times a day every 12 hours for at least 14 days.
For uncomplicated chlamydia (urethral, endocervical, or rectal) in adults with intolerance to tetracycline antibiotics, 500 mg 4 times a day for at least 7 days.
Treatment of primary syphilis – the total course dose is 30-40 g, treatment duration is 10-15 days, frequency of administration is 4 times a day. It is preferable to start treatment with intravenous administration, followed by a transition to oral forms.
For gonorrhea, 500 mg every 6 hours for 3 days, then 500 mg every 12 hours for 7 days.
Treatment of diphtheria carrier state – 250 mg 2 times a day for at least 7 days.
For whooping cough: adults and adolescents over 14 years – 100-250 mg 4 times a day; children aged 3 to 14 years – 40-50 mg/kg/day. Treatment course 5-14 days.
For scarlet fever – in usual doses, treatment course – at least 10 days.
For legionellosis (Legionnaires' disease) – 500-1000 mg 4 times a day until clinical symptoms of the disease disappear (but not less than 14 days).
For listeriosis – 250-500 mg 2-4 times a day for at least 7 days, etiotropic therapy is conducted until the 6th-7th day of normal temperature, and in severe forms – until the 14th-21st day.
For erythrasma – 250 mg 4 times a day for 5-7 days in conjunction with topical agents.
For amoebic dysentery in adults and adolescents over 14 years – 250 mg 4 times a day, for children aged 3 to 14 years – 30-50 mg/kg/day; treatment course – 10-14 days.
Prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with rheumatism for adults – 250-500 mg 2-4 times a day, for children – 20-30 mg/kg/day, treatment duration - at least 10 days.
Prevention of infectious endocarditis in patients with heart defects during dental procedures and ENT surgeries: for adults – 1000 mg, for children – 20 mg/kg 1-2 hours before the therapeutic or diagnostic procedure, then for adults – 500 mg and for children – 10 mg/kg every 6 hours, a total of 8 doses.
For pneumonia in children – 50 mg/kg/day in 4 doses, for at least 3 weeks.

Section: Composition

Active ingredient: erythromycin calculated as 100% substance - 100 mg/250 mg.
Excipients of the core: gelatin - 3.1 mg/7.0 mg, calcium stearate - 1.95 mg/4.40 mg, polysorbate 80 (tween 80) - 0.40 mg/1.05 mg, lactose monohydrate (milk sugar) - 20.28 mg/45.76 mg, sodium carboxymethyl starch (primogel) type A - 7.8 mg/17.6 mg, potato starch - 61.47 mg/114.19 mg; excipients of the coating: methacrylic acid and ethyl acrylate copolymer (1:1) (collicut MAE 100R) - 8.50 mg/18.41 mg, talc - 2.70 mg/5.84 mg, povidone K-30 - 1.62 mg/3.52 mg, titanium dioxide - 0.48 mg/1.05 mg, polysorbate 80 (tween 80) - 1.70 mg/3.68 mg.

tablets, coated with a film, round in shape with biconvex surfaces of white or white with a grayish tint color.

Contraindications

Increased sensitivity to erythromycin, other components of the drug, and other macrolides; significant hearing loss; simultaneous use of terfenadine, ergotamine, dihydroergotamine, astemizole, cisapride, pimozide; age under 3 years; breastfeeding period; lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
With caution

Arrhythmias (in history), prolonged QT interval, jaundice (including in history), liver and/or kidney failure, myasthenia gravis, simultaneous use of hepatotoxic drugs.
If you have any of the listed conditions, be sure to consult your doctor before taking the medication.

Special Instructions

During prolonged therapy, it is necessary to monitor laboratory indicators of liver function. Symptoms of cholestatic jaundice may develop a few days after the start of therapy; however, the risk of development increases after 7-14 days of continuous therapy. The likelihood of developing ototoxic effects is higher in patients with renal and/or hepatic insufficiency, as well as in elderly patients. Some resistant strains of Haemophilus influenzae are sensitive to the simultaneous administration of erythromycin and sulfonamides. It may interfere with the determination of catecholamines in urine and the activity of "liver" transaminases in the blood (colorimetric determination using diphenylhydrazine). It should not be taken with milk or dairy products. Numerous clinical studies have demonstrated the astral and duodenal prokinetic effect of erythromycin. When used in combination with statins, the development of rhabdomyolysis and pseudomembranous colitis is possible.

Section: Side Effects

From the immune system: urticaria, other forms of skin rash (erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome), angioedema, eosinophilia, anaphylactic shock.
From the digestive system: anorexia, nausea, vomiting, abdominal pain, tenesmus, diarrhea, dysbiosis, candidiasis of the oral mucosa, pseudomembranous colitis, liver dysfunction, hepatocellular hepatitis, hepatomegaly, cholestatic jaundice, increased activity of "liver" transaminases, pancreatitis.
From the auditory system: ototoxicity – hearing loss and/or tinnitus (when used in high doses – more than 4 g/day, usually reversible).
From the cardiovascular system: decreased blood pressure, tachycardia, prolonged QT interval on the electrocardiogram, atrial fibrillation and/or flutter (in patients with prolonged QT interval).
From the nervous system: seizures, hallucinations, vertigo, confusion, development of myasthenic syndrome or exacerbation of myasthenia.
From the urinary system: interstitial nephritis.
General disorders and disturbances at the injection site: chest pain, fever, malaise.
If any of the side effects listed in the instructions worsen or you notice any other side effects not listed in the instructions, inform your doctor.

Section: Overdose

Symptoms: liver function impairment, up to acute liver failure, rarely – hearing impairment.
Treatment: activated charcoal, careful monitoring of respiratory system status (if necessary – artificial ventilation of the lungs), acid-base balance and electrolyte exchange, electrocardiogram.
Gastric lavage is effective when a dose is five times higher than the average therapeutic dose.
Hemodialysis, peritoneal dialysis, and forced diuresis are ineffective.

Interaction

Reduces the bactericidal action (antagonism) of beta-lactam antibiotics (penicillins, cephalosporins, carbapenems), lincomycin, clindamycin, chloramphenicol, streptomycin, tetracyclines, colistin.
Increases the concentration of theophylline in the blood: a reduction in the dose of theophylline may be required. At the same time, the concentration of erythromycin may decrease, which can lead to subtherapeutic concentrations of erythromycin and a reduction in its effect.
Enhances the nephrotoxicity of cyclosporine (especially in patients with concomitant renal insufficiency).
Reduces the clearance of triazolam and midazolam, which may enhance the pharmacological effects of benzodiazepines.
Slows the elimination (enhances the effect) of methylprednisolone, felodipine, and anticoagulants of the coumarin group.
When used concurrently with lovastatin and other HMG-CoA reductase inhibitors, the risk of developing rhabdomyolysis increases.
Increases the bioavailability of digoxin.
Reduces the effectiveness of hormonal contraception.
Drugs that block tubular secretion prolong the half-life of erythromycin.
When taken simultaneously with drugs whose metabolism occurs in the liver (acenocoumarol, astemizole, cilostazol, cyclosporine, dihydroergotamine, ergotamine, omeprazole, quinidine, rifabutin, tacrolimus, terfenadine, vinblastine, carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, disopyramide, lovastatin, bromocriptine, antifungal drugs such as fluconazole, ketoconazole, and itraconazole), the concentration of these drugs in plasma may increase.
Drugs that are inducers of CYP3A4 isoenzymes (such as rifampicin, phenytoin, carbamazepine, phenobarbital, St. John's wort) may induce the metabolism of erythromycin, which can lead to subtherapeutic concentrations of erythromycin and a reduction in its effect. The interaction persists for 2 weeks after discontinuation of treatment with CYP3A4 inducers.
Erythromycin alters the metabolism of mizolastine.
When taken together with pimozide, the development of arrhythmia (ventricular flutter and fibrillation), "tornado" ventricular tachycardia, cardiac arrest, up to fatal outcomes is possible.
Protease inhibitors inhibit the metabolism of erythromycin, and monitoring of erythromycin concentration in plasma is necessary.
When used simultaneously with terfenadine or astemizole, the development of arrhythmia (ventricular flutter and fibrillation, ventricular tachycardia, up to fatal outcomes) is possible; with dihydroergotamine or dihydrogenated ergot alkaloids – vasoconstriction up to complete spasm, dysesthesia.
Simultaneous intake of erythromycin with sildenafil may lead to a moderate increase in the maximum concentration of sildenafil in the blood.
An increase in the level of cisapride may lead to a prolongation of the QTc interval, with a possible development of arrhythmia (ventricular flutter and fibrillation), "tornado" ventricular tachycardia.
When taken together with verapamil and other slow calcium channel blockers, hypotension, bradyarrhythmia, and lactic acidosis are observed.
Cimetidine inhibits the metabolism of erythromycin, which may lead to increased plasma concentrations of erythromycin.
Erythromycin reduces the clearance of zopiclone and, thus, may increase the pharmacodynamic effects of this drug.
When used concomitantly with erythromycin, the toxicity of colchicine increases.
If you are taking other medications, it is necessary to consult a doctor.

Pharmacodynamics

Bacteriostatic antibiotic from the macrolide group. It reversibly binds to the 50S ribosomal subunit, disrupting the formation of peptide bonds between amino acid molecules and blocking protein synthesis in microorganisms (does not affect nucleic acid synthesis). When used in high doses, it may exhibit bactericidal action.
Microorganisms sensitive to it are those whose growth is inhibited at antibiotic concentrations of less than 0.5 mg/L, moderately sensitive ones at 1-6 mg/L, and resistant ones at more than 6 mg/L.
The broad spectrum of antimicrobial action of erythromycin includes: gram-positive microorganisms: Staphylococcus spp., both penicillinase-producing and non-producing, including Staphylococcus aureus (except for methicillin-resistant strains MRSA), Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. of the viridans group), Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium minutissimum, Listeria monocytogenes;
gram-negative microorganisms: Bordetella pertussis, Campylobacter jejuni, Legionella spp. (including Legionella pneumophila), Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae; and other microorganisms: Mycoplasma spp. (including Mycoplasma pneumoniae), Neisseria gonorrhoeae, Haemophilus influenzae (some strains may be resistant to erythromycin but sensitive to other macrolide antibiotics);
other microorganisms: Chlamydia spp. (including Chlamydia trachomatis), Mycoplasma spp. (including Mycoplasma pneumoniae), Ureaplasma urealyticum, Treponema spp., Propionibacterium acnes, Entamoeba histolytica.
Erythromycin is resistant to gram-negative rods: Escherichia coli and other members of the Enterobacteriaceae family (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 fragilis), methicillin-resistant strains of Staphylococcus aureus (MRSA), and enterococci Enterococcus spp., mycobacteria.
It is an agonist of motilin receptors. It accelerates gastric emptying by increasing the amplitude of pyloric contractions and improving antral-duodenal coordination, possessing prokinetic properties.

Section: Pharmacokinetics

Absorption - high. Food intake does not affect the absorption of erythromycin in enteric-coated tablets. The time to reach maximum concentration in plasma after oral administration is 2-4 hours. Binding to plasma proteins - 70-90%. Bioavailability - 30-65%. It is distributed unevenly in the body. It accumulates in large amounts in the liver, spleen, and kidneys. In bile and urine, the concentration is ten times higher than in plasma. It penetrates well into the tissues of the lungs, lymph nodes, middle ear, prostatic secretions, sperm, pleural cavity, ascitic, and synovial fluids. In the milk of nursing women, the concentration of erythromycin is 50% of that in serum. It poorly penetrates the blood-brain barrier and into cerebrospinal fluid (its concentration is 10% of the drug content in plasma). In inflammatory processes in the membranes of the brain, their permeability to erythromycin slightly increases. It crosses the placental barrier and enters the fetal blood, where its content reaches 5-20% of that in maternal plasma. It is metabolized in the liver (over 90%), partially forming inactive metabolites. The metabolism of erythromycin involves the isoenzymes CYP3A4, CYP3A5, and CYP3A7, of which it is an inhibitor. The half-life is 1.4-2 hours, and in anuria - 4-6 hours. Excretion with bile is 20-30% in unchanged form, and through the kidneys (in unchanged form) - 2-5%.