Erythromycin enterosoluble filmcoated tablets (Tablets, Lyophilisate) Instructions for Use

ATC Code

J01FA01 (Erythromycin)

Active Substance

Erythromycin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antibiotic of the macrolide group

Pharmacotherapeutic Group

Antibiotic-macrolide

Pharmacological Action

An antibiotic from the macrolide group. It reversibly binds to bacterial ribosomes, thereby suppressing protein synthesis (does not affect nucleic acid synthesis). It has a bacteriostatic effect.

However, in high doses against susceptible microorganisms, it has a bactericidal effect.

Erythromycin is active against gram-positive bacteria Staphylococcus spp. (including strains producing and not producing penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Bacillus anthracis, Corynebacterium diphtheriae; gram-negative bacteria Neisseria gonorrhoeae, Haemophilus influenzae, Bordetella pertussis, Brucella spp., Legionella spp.

Erythromycin is also active against Mycoplasma spp., Chlamydia spp., Treponema spp., Rickettsia spp.

Escherichia coli, Pseudomonas aeruginosa, Shigella spp., Salmonella spp. are resistant to erythromycin.

Microorganisms whose growth is inhibited at an antibiotic concentration of 1 mg/L are considered sensitive, moderately sensitive at 4 mg/L, and moderately resistant and resistant at 6 mg/L.

Pharmacokinetics

Absorption is high when taken orally. C_max in blood plasma is reached 2-4 hours after oral administration. Bioavailability is 30-65%.

Plasma protein binding is 70-90%. It is distributed unevenly in the body. It accumulates in large quantities in the liver, spleen, and kidneys. The concentration in bile and urine is tens of times higher than the concentration in plasma.

It penetrates well into lung tissue, lymph nodes, middle ear exudate, prostate secretion, semen, pleural cavity, ascitic and synovial fluids. Breast milk contains 50% of the plasma concentration. It penetrates poorly through the blood-brain barrier into the cerebrospinal fluid (its concentration is 10% of the erythromycin content in plasma).

In inflammatory processes in the meninges, their permeability to erythromycin increases somewhat. It crosses the placental barrier and enters the fetal blood, where its content reaches 5-20% of the concentration in the maternal plasma.

It is metabolized in the liver (more than 90%), partially with the formation of inactive metabolites. Isoenzymes CYP3A4, CYP3A5, and CYP3A7, of which it is an inhibitor, are involved in the metabolism of erythromycin. T_1/2 is 1.4-2 hours, in anuria – 4-6 hours. Excretion with bile is 20-30% unchanged, by the kidneys (unchanged) after oral administration – 2-5%.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to erythromycin: diphtheria (including diphtheria carriage); whooping cough (including prevention of the disease in persons at risk of infection); trachoma; brucellosis; Legionnaires’ disease; scarlet fever; amoebic dysentery; gonorrhea; pneumonia in children caused by Chlamydia trachomatis; urogenital 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 ineffectiveness of tetracyclines; primary syphilis (in patients allergic to penicillins); ENT infections (tonsillitis, otitis media, 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.

Prevention of infectious complications during therapeutic and diagnostic procedures (including dental interventions, endoscopy) in patients with heart defects.

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

It is a reserve antibiotic for the treatment of bacterial infections caused by strains of gram-positive pathogens (in particular, staphylococci) resistant to penicillin.

ICD codes

Dosage Regimen

Tablets

The dosage regimen is set individually, depending on the indications for use, the severity of the disease, the patient’s age, and the tolerability of therapy.

When taken orally, the dosage regimen and food intake are determined taking into account the dosage form used and its resistance to the effects of gastric juice.

Lyophilisate

Erythromycin phosphate is used only intravenously by slow bolus (over 3-5 minutes) or by drip.

A single dose of the drug for adults is 200 mg, the daily dose is 600 mg. In severe infections, the daily dose can be increased to 1 g.

Children of all age groups are prescribed the drug at a daily dose of 20 mg/kg (in 2-3 doses).

The drug is administered intravenously for 5-6 days (until a therapeutic effect occurs) followed by a switch to oral erythromycin.

With good tolerance and the absence of phlebitis and periphlebitis, the course of treatment can be extended to 2 weeks or more.

Rules for solution preparation

For intravenous bolus administration, the powder is dissolved in water for injection or isotonic sodium chloride solution at the rate of 5 mg of the drug per 1 ml of solvent.

For intravenous drip administration, the powder is dissolved in isotonic sodium chloride solution or 5% glucose solution to a concentration of 1 mg/ml and administered at a rate of 60-80 drops/min.

Adverse Reactions

From the digestive system: impaired liver function, increased activity of hepatic transaminases, nausea, vomiting, tenesmus, diarrhea, abdominal pain, cholestatic jaundice, pseudomembranous enterocolitis (both during treatment and after its completion).

From the organ of hearing: hearing loss and/or tinnitus (ototoxicity is usually reversible after discontinuation).

Allergic reactions: urticaria, skin rash, eosinophilia, anaphylactic shock.

From the cardiovascular system: tachycardia, atrial fibrillation and/or flutter (in patients with a prolonged QT interval on ECG).

Other: dysbacteriosis, oral candidiasis, pseudomembranous colitis (both during treatment and after its completion).

Contraindications

Hypersensitivity to erythromycin and other macrolides; significant hearing loss; simultaneous use of terfenadine, astemizole, pimozide, cisapride; lactation (breastfeeding); children under 3 or under 14 years of age – depending on the dosage form used.

With caution

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

Use in Pregnancy and Lactation

If it is necessary to use during pregnancy, the expected benefit for the mother and the potential risk to the fetus should be assessed.

If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

Use in Hepatic Impairment

Should be used with caution in hepatic insufficiency.

Use in Renal Impairment

Should be used with caution in renal insufficiency.

Pediatric Use

Contraindicated for oral administration in children under 3 years or under 14 years, depending on the dosage form used. Should be used strictly according to indications, in doses and dosage forms appropriate for age.

Geriatric Use

Use with caution in elderly patients to avoid exacerbation of chronic diseases.

Special Precautions

With long-term therapy, liver function parameters should be monitored.

Symptoms of cholestatic jaundice may develop several days after the start of therapy, but the risk of development 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.

Drugs that increase the acidity of gastric juice and acidic drinks inactivate Erythromycin.

The use of erythromycin may interfere with the determination of catecholamines in urine and the activity of hepatic transaminases in blood.

Erythromycin should not be taken with milk or dairy products.

Numerous clinical studies have proven the antral and duodenal prokinetic effect of erythromycin.

Drug Interactions

Erythromycin is incompatible with lincomycin, clindamycin, and chloramphenicol due to antagonism of action.

When used concomitantly with terfenadine or astemizole, the risk of arrhythmia increases.

When used concomitantly with drugs that block tubular secretion, the T_1/2 of erythromycin is prolonged.

When used concomitantly, Erythromycin reduces the bactericidal effect of beta-lactam antibiotics (penicillins, cephalosporins, carbapenems).

When used concomitantly with theophylline, its plasma concentration increases.

When used concomitantly with drugs whose metabolism is carried out in the liver (carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, disopyramide, lovastatin, bromocriptine), the concentration of these drugs in plasma may increase, because Erythromycin is an inhibitor of liver microsomal enzymes.

When used concomitantly, Erythromycin enhances the nephrotoxicity of cyclosporine (especially in patients with concomitant renal failure).

When used concomitantly, Erythromycin reduces the clearance of triazolam and midazolam, which may enhance the pharmacological effects of these benzodiazepines.

When used concomitantly with dihydroergotamine or non-hydrogenated ergot alkaloids, vasoconstriction with the development of spasms and dysesthesia is noted.

When used concomitantly, Erythromycin slows down the excretion and enhances the effects of methylprednisolone, felodipine, and coumarin anticoagulants.

When used concomitantly with lovastatin, the development of rhabdomyolysis is possible.

When used concomitantly, Erythromycin increases the bioavailability of digoxin and reduces the effectiveness of hormonal contraception.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.