Erythromycin tablets 250 mg

Package Insert for Erythromycin tablets 250 mg

Brand Name: Erythromycin

International Nonproprietary Name: Erythromycin

Dosage Form: Enteric-coated film-coated tablets

Composition

Each tablet contains the active substance:
Erythromycin (calculated as the active substance) 250 mg
Polysorbate 80 (Tween-80)	5.8 mg
Calcium stearate	4.8 mg
Povidone (polyvinylpyrrolidone)	29.6 mg
Croscarmellose sodium	9.0 mg
Potato starch	To obtain a core tablet weighing 450.0 mg
Coating ingredients:
Titanium dioxide	0.5 mg
Propylene glycol	2.3 mg
Kollicoat MAE 100P	15.1 mg
Talc	4.1 mg

Description:

Round, biconvex, film-coated tablets, white or white with a greyish tint; the core is white or almost white in cross-section.

Pharmacotherapeutic group:  Antibiotic - macrolide.

ATC Code: J01FA01

Pharmacological properties:

Pharmacodynamics

Bacteriostatic antibiotic from the macrolide group, reversibly binds to the 50S subunit of bacterial ribosomes, blocks protein synthesis, inhibiting bacterial growth and reproduction (does not affect nucleic acid synthesis). May exhibit bactericidal action at high doses. Spectrum of activity includes Gram-positive bacteria (Staphylococcus spp., including Staphylococcus aureus; Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes), alpha-hemolytic streptococcus (Viridans group), Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium minutissimum) and Gram-negative microorganisms (Neisseria gonorrhoeae, Haemophilus influenzae, Bordetella pertussis, Brucella spp., Legionella spp., including Legionella pneumophila) and other microorganisms: Mycoplasma spp. (including Mycoplasma pneumoniae), Chlamydia spp. (including Chlamydia trachomatis), Treponema spp., Rickettsia spp., protozoa: Entamoeba histolytica, Listeria monocytogenes.

Gram-negative bacteria such as Escherichia coli, Pseudomonas aeruginosa, as well as Shigella spp., Salmonella spp. and others are resistant to erythromycin. Microorganisms whose growth is inhibited at an antibiotic concentration of less than 0.5 mg/L are considered sensitive, moderately sensitive at 1-6 mg/L, and moderately resistant and resistant at 6-8 mg/L.

Pharmacokinetics

Absorption is high. Food intake does not affect the absorption of enteric-coated erythromycin tablets. Maximum concentration (Cmax) is reached in 2-4 hours. Plasma protein binding is 70-90%.

Bioavailability is 30-65 %. Distributed unevenly in the body. Accumulates in high concentrations in the liver, spleen, and kidneys. Concentrations in bile and urine are tens of times higher than in plasma. Penetrates well into lung tissue, lymph nodes, middle ear, prostatic secretion, semen, pleural cavity, ascitic and synovial fluids. Concentration in breast milk is 50% of the serum concentration. Penetrates poorly through the blood-brain barrier. With inflammatory processes in the meninges, their permeability to erythromycin increases somewhat. Crosses the placental barrier.

Metabolized in the liver (more than 90 %), partially forming inactive metabolites. Elimination half-life (T1/2) is 1.4-2 hours, in anuria - 4-6 hours. Excretion in bile is 20-30 % unchanged, by kidneys (unchanged) is 2-5 %.

Indications for use

Infectious and inflammatory diseases caused by susceptible microflora: diphtheria (including carrier state), whooping cough (including prophylaxis), trachoma, brucellosis, Legionnaires' disease, erythrasma, listeriosis, scarlet fever, amoebic dysentery, gonorrhea; urogenital infections in pregnant women caused by Chlamydia trachomatis; uncomplicated chlamydia in adults (with localization in the lower urogenital tract and rectum), in case of intolerance or ineffectiveness of tetracyclines, etc.; ENT infections (tonsillitis, otitis media, sinusitis); biliary tract infections (cholecystitis); upper and lower respiratory tract infections (tracheitis, bronchitis, pneumonia); skin and soft tissue infections (acne vulgaris, infected wounds, bedsores, 2nd-3rd degree burns, trophic ulcers), conjunctival infections.

Infections caused by streptococci (tonsillitis, pharyngitis).

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

Treatment of infectious and inflammatory diseases caused by pathogens (particularly Staphylococcus spp.) resistant to penicillin, tetracycline, chloramphenicol, streptomycin.

Contraindications

Hypersensitivity, significant hearing loss, concurrent use of terfenadine or astemizole, lactation period, children under 14 years of age (for this dosage form). 

Precautions

Arrhythmias (in history), prolonged Q-T interval, renal insufficiency, pregnancy, lactation period.

Dosage and administration:

Orally.

A single dose for adults and adolescents over 14 years of age is 250-500 mg, the daily dose is 1-2 g. The interval between doses is 6 hours. For severe infections, the daily dose may be increased to 4 g.

For the treatment of diphtheria carrier state - 250 mg twice a day.

For amoebic dysentery in adults - 250 mg four times a day, course duration - 10-14 days.

For Legionnaires' disease - 500-1000 mg four times a day for 14 days.

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

For tonsillitis, pharyngitis in adults - 20-50 mg/kg/day, in children - 20-30 mg/kg/day, course duration - at least 10 days.

For the prevention of septic endocarditis in patients with heart defects - 1 g for adults 1 hour before a therapeutic or diagnostic procedure, then 0.5 g for adults repeated after 6 hours.

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

For urogenital infections during pregnancy - 500 mg four times a day for 7 days or (if tolerated) - 250 mg four times a day for 14 days.

In adults, for uncomplicated chlamydia and intolerance to tetracyclines - 500 mg four times a day for at least 7 days. 

Adverse reactions

Digestive system: nausea, vomiting, epigastric pain, abdominal pain, tenesmus, diarrhea, dysbacteriosis, rarely - oral candidiasis, pseudomembranous enterocolitis, impaired liver function, cholestatic jaundice, increased activity of "hepatic" transaminases, pancreatitis.

Hearing organs: ototoxicity - hearing loss and/or tinnitus (when used in high doses - more than 4 g/day, usually reversible).

Cardiovascular system: prolongation of the Q-T interval on ECG, atrial fibrillation and/or flutter (in patients with a prolonged Q-T interval on ECG).

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

Overdose

Symptoms: impaired liver function, up to acute liver failure, rarely - hearing impairment.

Treatment: activated charcoal, careful monitoring of respiratory status (mechanical ventilation if necessary), acid-base balance and electrolytes, ECG. Gastric lavage is effective if performed after ingestion of a dose five times the average therapeutic dose. Hemodialysis, peritoneal dialysis and forced diuresis are ineffective.

Interaction with other medicinal products

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

Increases the nephrotoxicity of cyclosporine (especially in patients with concomitant renal insufficiency).

Reduces the clearance of triazolam and midazolam, thereby potentially enhancing the pharmacological effects of benzodiazepines.

Slows the elimination (enhances the effect) of methylprednisolone, felodipine and coumarin anticoagulants.

Increases the bioavailability of digoxin.

Reduces the effectiveness of hormonal contraceptives.

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

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

Concurrent use with terfenadine or astemizole - possibility of arrhythmia development; with dihydroergotamine or non-hydrogenated ergot alkaloids - vasoconstriction to spasm, dysesthesia.

Incompatible with chloramphenicol (antagonism).

Concurrent use with lovastatin increases the risk of rhabdomyolysis. 

Special instructions

Due to the possibility of penetration into breast milk, breastfeeding should be discontinued while taking erythromycin.

With long-term therapy, laboratory monitoring of liver function should be performed.

Symptoms of cholestatic jaundice may develop several days after the start of therapy, but the risk increases after 7-14 days of continuous therapy.

The likelihood of ototoxic effects is higher in patients with renal and hepatic insufficiency, as well as in elderly patients.

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

May interfere with the determination of urinary catecholamines and the activity of "hepatic" transaminases in the blood (colorimetric determination using dinitrophenylhydrazine). 

Pharmaceutical form

Enteric-coated film-coated tablets 250 mg.

10 tablets in a blister pack made of polyvinyl chloride film and printed lacquered aluminum foil. 10 or 20 tablets in polymer jars with screw-on lids or plastic containers for medicines.

Each jar or container, or 1, 2 blister packs are placed in a cardboard carton together with the package insert.

Storage conditions:

Store in a dry place, protected from light, at a temperature not exceeding 25⁰C. Keep out of reach of children.

Shelf life:

2 years. Do not use after the expiration date. 

Regulatory status:

Prescription only.

Name and address of the marketing authorization holder / organization for claims:

JSC "AVVA RUS", Russia, 121614,

Moscow, Krylatskie Kholmy st., 30, building 9.

Tel/Fax: +7 (495) 956-75-54.

avva.com.ru

Manufacturing address:

JSC "AVVA RUS",  Russia, 610044, Kirov region, Kirov, Luganskaya st., 53a.

Tel.: +7 (8332) 25-12-29; +7 (495) 956-75-54.