Erythromycin-Lect tablets 250mg, No. 20

Infectious and inflammatory diseases caused by susceptible to microorganisms:

• 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;

• conjunctivitis of newborns;

• pneumonia in children caused by Chlamydia trachomatis;

• genitourinary infections in pregnant women caused by Chlamydia trachomatis;

• uncomplicated chlamydia in adults (with localization in the lower urogenital tract and rectum) with intolerance or ineffectiveness of tetracyclines;

• primary syphilis (in patients allergic to penicillins);

• ENT infections (tonsillitis, otitis media, sinusitis);

• biliary tract infections (cholecystitis);

• infections of the upper and lower respiratory tract (tracheitis, bronchitis, pneumonia);

• infections of the skin and soft tissues.

• Prevention of infectious complications during medical 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) that are resistant to penicillin.

The dose and treatment regimen are set individually, depending on the patient's age, indications for use, the severity of the disease, and the tolerance of therapy.

Enteric-coated tablets

1 tab. erythromycin

• Hypersensitivity to erythromycin and other macrolides;

• significant hearing loss;

• concomitant use of terfenadine, astemizole, pimozide, cisapride, lactation period;

• for oral administration - children up to 3 or up to 14 years old, depending on the dosage form used;

• With caution, arrhythmias (in history), an increase in the duration of the ventricular complex on the electrocardiogram (prolongation of the OT interval), jaundice (in history), hepatic and / or renal failure, use in pregnancy.

pharmachologic effect

An antibiotic from the macrolide group. Reversibly binds to bacterial ribosomes, thereby inhibiting protein synthesis (does not affect the synthesis of nucleic acids). Has a bacteriostatic effect. However, in high doses, it has a bactericidal effect against sensitive microorganisms.

The drug 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.

The drug is also active against Mycoplasma spp., Chlamydia spp., Treponema spp., Rickettsia spp.

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

The sensitive group includes microorganisms whose growth is delayed at an antibiotic concentration of 1 mg / l, medium-sensitive - 4 mg / l, moderately resistant and resistant - 6 mg / l.

Pharmacokinetics

When taken orally, absorption is high. The time to reach Cmax in blood plasma is achieved within 2-4 hours after oral administration, after intravenous administration - after 20 minutes. Bioavailability is 30-65%.

Plasma protein binding 70-90%. It is distributed unevenly in the body. It accumulates in large quantities in the liver, spleen, and kidneys. In bile and urine, the concentration is tens of times higher than the concentration in plasma. It penetrates well into the tissues of the lungs, lymph nodes, middle ear exudate, prostate secretions, sperm, pleural cavity, ascitic and synovial fluids. Breast milk contains 50% of the plasma concentration. Poorly penetrates the BBB, into the 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 increases slightly. It penetrates the placental barrier and enters the fetal bloodstream, where its content reaches 5-20% of the concentration in the mother's blood plasma.

It is metabolized in the liver (more than 90%), partly with the formation of inactive metabolites. The isoenzymes CYP3A4, CYP3A5 and CYP3A7 are involved in the metabolism of erythromycin, of which it is an inhibitor. T1 / 2 - 1.4-2 hours, with anuria - 4-6 hours. Excretion with bile - 20-30% unchanged, by the kidneys (unchanged) after oral administration - 2-5%, after intravenous administration - 12-15%.

Side effect

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 termination).

On the part of the organ of hearing: hearing loss and / or tinnitus (ototoxicity after withdrawal is usually reversible).

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

From the side of the cardiovascular system: tachycardia, atrial fibrillation and / or atrial flutter (in patients with an extended QT interval on an ECG).

Others: dysbiosis, oral candidiasis, pseudomembranous colitis (both during and after treatment).

Application during pregnancy and lactation

If necessary, use during pregnancy should evaluate the intended benefit to the mother and the potential risk to the fetus.

If necessary, use during lactation should decide on the termination of breastfeeding.

Application for violations of liver function

Contraindicated in liver failure.

Application for impaired renal function

Contraindicated in renal failure.

Application in children

Contraindicated for oral administration in children 3 years old or up to 14 years old, depending on the dosage form used.

Use in elderly patients

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

special instructions

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

With prolonged therapy, it is necessary to monitor the indicators of liver function.

Symptoms of cholestatic jaundice may develop several days after starting 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.

May interfere with the determination of catecholamines in the urine and the activity of hepatic transaminases in the blood.

Do not drink milk or dairy products.

In numerous clinical studies, the antral and duodenal prokinetic effect of erythromycin has been proven.

Drug interactions

Erythromycin is incompatible with lincomycin, clindamycin and chloramphenicol due to its antagonistic action.

When taken simultaneously with terfenadine or astemizole, the risk of arrhythmias increases.

With simultaneous use with drugs that block tubular secretion, the T1 / 2 of erythromycin is lengthened.

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

With simultaneous use with theophylline, its concentration in plasma increases.

With simultaneous use with drugs, the metabolism of which 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.

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

Reduces the clearance of triazolam and midazolam, and therefore may enhance the pharmacological effects of these benzodiazepines.

With simultaneous use with dihydroergotamine or non-hydrogenated ergot alkaloids, vasoconstriction is noted with the development of spasms, dysesthesia.

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

When used together with lovastatin, rhabdomyolysis may develop.

Erythromycin increases the bioavailability of digoxin and decreases the effectiveness of hormonal contraception.