Instructions for use ERYTHROMYCIN

Compound

Description:

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

Pharmacotherapeutic group: antibiotic - macrolide.

ATX code:

J01FA01

Pharmachologic effect:

Pharmacodynamics

A bacteriostatic antibiotic from the macrolide group, reversibly binds to the 50S subunit of bacterial ribosomes, blocks protein synthesis, prevents the growth and reproduction of bacteria (does not affect the synthesis of nucleic acids). In high doses it can have a bactericidal effect. The spectrum of activity includes gram-positive (Staphylococcus spp., producing and non-producing penicillinase, 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-negatives are resistant to erythromycin: Escherichia coli, Pseudomonas aeruginosa, as well as Shigella spp., Salmonella spp. and others. The sensitive group includes microorganisms whose growth is delayed at an antibiotic concentration of less than 0.5 mg/l, moderately sensitive - 1-6 mg/l, moderately resistant and resistant - 6-8 mg/l.

Pharmacokinetics

Absorption is high. Eating does not affect the absorption of erythromycin enteric-coated tablets. The maximum concentration (Cmax) is reached after 2-4 hours. Communication with plasma proteins is 70-90%.

Bioavailability - 30-65%. 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. Penetrates well into the tissues of the lungs, lymph nodes, middle ear, prostate secretions, sperm, pleural cavity, ascitic and synovial fluid. In the milk of lactating women, the concentration of erythromycin is 50% of the serum concentration. Penetrates poorly through the blood-brain barrier. During inflammatory processes in the meninges, their permeability to erythromycin increases slightly. Penetrates through the placental barrier.

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

Erythromycin tablet p/o intestinal solution. 250 mg 10 pcs

Pharmacological group:

Antibiotic, macrolide.
Pharmacodynamics:
Bacteriostatic antibiotic from the macrolide group. Reversibly binds to the 50S subunit of ribosomes, which disrupts the formation of peptide bonds between amino acid molecules and blocks the synthesis of microbial proteins (does not affect the synthesis of nucleic acids). When used in high doses, depending on the type of pathogen, it can exhibit a bactericidal effect. Microorganisms whose growth is delayed at an antibiotic concentration of less than 0.5 mg/l are classified as sensitive, 1-6 mg/l as moderately sensitive, and more than 6 mg/l as resistant. The wide spectrum of antimicrobial action of erythromycin includes: gram-positive microorganisms: Staphylococcus spp., producing and non-producing penicillinase, incl. Staphylococcus aureus (except methicillin-resistant strains - MRSA); Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. 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; 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. Gram-negative bacilli are resistant to erythromycin: Escherichia coli and other representatives of the Enterobacteriaceae family (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 of Staphylococcus aureus (MRSA) and Enterococcus spp., mycobacteria. It is a motilin receptor agonist. Accelerates the evacuation of gastric contents by increasing the amplitude of pyloric contraction and improving antral-duodenal coordination, and has prokinetic properties.

Pharmacokinetics:

Absorption is high. Food intake has no effect on enteric film-coated oral forms of erythromycin base. The time to reach the maximum concentration in the blood plasma after taking the tablets orally is 2-4 hours, the connection with proteins is 70-90%. Bioavailability - 30-65%. 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 that in plasma. Penetrates well into the tissues of the lungs, lymph nodes, middle ear exudate, prostate secretions, sperm, pleural cavity, ascitic and synovial fluid. The milk of lactating women contains 50% of the plasma concentration. It penetrates poorly through the blood-brain barrier (BBB) ​​and into the cerebrospinal fluid (CSF) (the concentration is 10% of the drug content in plasma). During inflammatory processes in the membranes of the brain, their permeability to erythromycin increases slightly. 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. Metabolized in the liver (more than 90%), partially with the formation of inactive metabolites. The metabolism of erythromycin involves the isoenzymes CYP3A4, CYP3A5 and CYP3A7, of which it is an inhibitor. The half-life (T1/2) is 1.4-2 hours, with anuria - 4-6 hours. Excretion with bile - 20-30% unchanged, by the kidneys (unchanged) after oral administration - 2-5%.

Indications for use

Infectious and inflammatory diseases caused by sensitive microflora: diphtheria (including bacterial carriage), whooping cough (including prevention), trachoma, brucellosis, Legionnaires' disease, erythrasma, listeriosis, scarlet fever, amoebic dysentery, gonorrhea; genitourinary infections in pregnant women caused by Chlamydia trachomatis; uncomplicated chlamydia in adults (with localization in the lower genitourinary tract and rectum), with intolerance or ineffectiveness of tetracyclines, etc.; infections of the ENT organs (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 (adolescent acne, infected wounds, bedsores, stage II burns, trophic ulcers), infections of the conjunctiva.

Infections caused by streptococci (tonsillitis, pharyngitis).

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

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

Erythromycin – granules, lyophilisate, powder, suppositories

Orally (tablets, capsules, oral suspension, granules or powder for the preparation of oral suspension), intravenously (lyophilisate for the preparation of solution for injection), rectally (suppositories).

IV slowly (over 3-5 minutes) or drip. All doses of the drug are given based on calculations based on the basis.

A single dose for adults and adolescents over 14 years of age is 0.25-0.5 g, daily - 1-2 g. The interval between administration is 6 hours. In case of severe infections, the daily dose can be increased to 4 g. For intravenous jet administration, the drug is dissolved in water for injection or 0.9% NaCl solution at the rate of 5 mg per 1 ml of solvent.

For intravenous drip administration, the drug is dissolved in a 0.9% NaCl solution or a 5% dextrose solution to a concentration of 1 mg/ml and administered at a rate of 60-80 drops/min. It is administered intravenously for 5-6 days (until a clear therapeutic effect occurs), followed by a transition to oral administration. With good tolerability and the absence of phlebitis and periphlebitis, the course of intravenous administration can be extended to 2 weeks (no more).

Orally (the regimen for taking the drug and eating is determined by the dosage form and its resistance to the effects of gastric juice), the average daily dose for adults is 1-2 g in 2-4 doses, the maximum daily dose is 4 g. Children from 4 months to 18 years depending on age, body weight and severity of infection - 30-50 mg/kg/day in 2-4 doses; for children in the first 3 months of life - 20-40 mg/kg/day. In case of severe infections, the dose may be doubled.

For the treatment of diphtheria carriage - 0.25 g 2 times a day.

The course dose for the treatment of primary syphilis is 30-40 g, the duration of treatment is 10-15 days.

For amoebic dysentery, adults - 0.25 g 4 times a day, children - 30-50 mg/kg/day; Course duration is 10-14 days.

For legionellosis - 0.5-1 g 4 times a day for 14 days.

For gonorrhea - 0.5 g every 6 hours for 3 days, then 0.25 g every 6 hours for 7 days.

For gastroparesis - orally (for the treatment of gastroparesis, a drug for intravenous use is more preferable), 0.15-0.25 g 30 minutes before meals 3 times a day.

For preoperative bowel preparation to prevent infectious complications - orally, 1 g 19 hours, 18 hours and 9 hours before surgery (3 g in total).

For the prevention of streptococcal infections (for tonsillitis, pharyngitis) adults - 20-50 mg/kg/day, 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 and 20 mg/kg for children, 1 hour before a treatment or diagnostic procedure, then 0.5 g for adults and 10 mg/kg for children, again after 6 h.

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

For conjunctivitis of newborns - 50 mg/kg/day suspension in 4 divided doses for at least 2 weeks.

For pneumonia in children - 50 mg/kg/day suspension in 4 divided doses for at least 3 weeks.

For genitourinary infections during pregnancy - 0.5 g 4 times a day for at least 7 days or (if this dose is poorly tolerated) 0.25 g 4 times a day for at least 14 days.

In adults, with uncomplicated chlamydia and intolerance to tetracyclines - 0.5 g 4 times a day for at least 7 days.

Rectally: children aged 1 to 3 years - 0.4 g / day, from 3 to 6 years - 0.5-0.75 g / day, 6-8 years - up to 1 g / day. The daily dose is divided into 4-6 parts and administered every 4-6 hours.

Directions for use and dosage:

Inside.

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

For the treatment of diphtheria carriage - 250 mg 2 times a day.

For amoebic dysentery in adults - 250 mg 4 times a day, course duration - 10-14 days.

For legionellosis - 500-1000 mg 4 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, adults - 20-50 mg/kg/day, 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 treatment or diagnostic procedure, then 0.5 g for adults again after 6 hours.

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

For genitourinary infections during pregnancy - 500 mg 4 times a day for 7 days or (if tolerated) - 250 mg 4 times a day for 14 days.

In adults, with uncomplicated chlamydia and intolerance to tetracyclines - 500 mg 4 times a day for at least 7 days.

Instructions for use "Erythromycin"

The tablets are taken orally with a small amount of water. The dosage is determined by the doctor. Recommendations for techniques depend on age:

1. Adults and children over 14 years old - at a time you can take from 250 to 500 mg in terms of the active substance, the maximum daily amount is 2 g. Tablets are taken no more than once every 6 hours. If the disease manifests itself in severe form, the maximum daily dosage is increased to 4 g.
2. Children from 4 months to 17 years inclusive take the drug at a rate of 30-50 mg of active substance per 1 kg of body. This is the maximum daily amount, which is divided into several (up to 4) doses.
3. If the tablets are prescribed to patients with heart disease or septic endocarditis, the daily dosage for an adult is 500 mg for an adult. Children with the same diseases are advised to take no more than 10 mg of the active drug per 1 kg of body.
4. For the treatment of gonorrhea - 3 times a day, 500 mg per dose. Treatment is carried out in this mode for the first 3 days, and starting from 4 days - 250 mg also 3 times a day.
5. For the treatment of whooping cough, the daily dosage is 40-50 mg per 1 kg of body. This is the maximum daily amount. Therapy lasts from 5 to 14 days.
6. For the treatment of uncomplicated chlamydia, take 500 mg at a time (total amount - 4 times a day). The minimum course is 7 days, further - as necessary and in agreement with the doctor.

Side effect

From the digestive system: nausea, vomiting, gastralgia, abdominal pain, tenesmus, diarrhea, dysbacteriosis, rarely - oral candidiasis, pseudomembranous enterocolitis, liver dysfunction, cholestatic jaundice, increased activity of “liver” transaminases, pancreatitis.

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

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

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

Interaction with other drugs

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

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 benzodiazepines.

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

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

When taken simultaneously with terfenadine or astemizole - the possibility of developing arrhythmia, with dihydroergotamine or non-hydrogenated ergot alkaloids - vasoconstriction to spasm, dysesthesia.

Incompatible with chloramphenicol (antagonism).

When co-administered with lovastatin, rhabdomyolysis increases.

Erythromycin

Reduces the bactericidal effect (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 may lead to subtherapeutic concentrations of erythromycin and a decrease in its effect.

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 benzodiazepines.

Slows down the elimination (increases the effect) of mestilprednisolone, felodipine and coumarin anticoagulants.

When used together with lovastatin and other HMB-CoA reductase inhibitors, the risk of developing rhabdomyolysis increases.

Increases the bioavailability of digoxin.

Reduces the effectiveness of hormonal contraception.

Medicines that block tubular secretion prolong T1/2 of erythromycin.

Since erythromycin is an isoenzyme inhibitor and a CYP3A substrate, when taken simultaneously with drugs that are metabolized in the liver (acenocoumarol, astemizole, cilostazol, cyclosporine, dihydroergotamine, ergotamine, omeprazole, quinidine, rifabutin, tacrolimus, terfenadine, vinblastine, carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, disopyramide, lovastatin, bromocriptine, antifungals such as fluconazole, ketoconazole and itraconazole), the plasma concentrations of these drugs may increase.

Drugs that are inducers of CYP3A4 isoenzymes (such as rifampicin, phenytoin, carbamazepine, phenobarbital, St. John's wort) can induce the metabolism of erythromycin, which can lead to subtherapeutic concentrations of erythromycin and a decrease 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, arrhythmia (ventricular fibrillation and flutter), ventricular tachycardia of the “pirouette” type, cardiac arrest, and even death may develop.

Protease inhibitors inhibit the metabolism of erythromycin; monitoring of the concentration of erythromycin in blood plasma is necessary.

When used simultaneously with terfenadine or astemizole, arrhythmia may develop (ventricular fibrillation and flutter, ventricular tachycardia, even death), with dihydroergotamine or dihydrogenated ergot alkaloids - vasoconstriction up to complete spasm, dysesthesia.

Concomitant use 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 can lead to a prolongation of the QTc interval, and the development of arrhythmia (ventricular fibrillation and flutter), ventricular tachycardia of the “pirouette” type is possible.

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.

With concomitant use of erythromycin, the toxicity of colchinitis increases.

If you are taking other medications, you should consult your doctor.

special instructions

Due to the possibility of passage into breast milk, breastfeeding should be discontinued when erythromycin is prescribed.

During long-term therapy, it is necessary to monitor laboratory parameters of liver function.

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 liver failure, as well as in elderly patients.

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

May interfere with the determination of catecholamines in urine and the activity of “liver” transaminases in the blood (colorimetric determination using definylhydrazine).

Erythromycin, 250 mg, enteric-coated tablets, 10 pcs.

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

Reduces the bactericidal effect (antagonism) of betalactam antibiotics (penicillins, cephalosporins, carbapenems), lincomycin, clindamycin, chloramphenicol, streptomycin, tetracyclines, colistin.

When taken simultaneously with drugs that are metabolized in the liver (theophylline, carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, disopyramide, lovastatin, bromocriptine), the concentration of these drugs in plasma may increase (it is an inhibitor of microsomal liver enzymes).

When interacting with theophylline, 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 decrease in its effect.

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 benzodiazepines.

When taken simultaneously with terfenadine or astemizole - the possibility of developing arrhythmia, with dihydroergotamine or non-hydrogenated ergot alkaloids - vasoconstriction to spasm, dysesthesia.

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

When co-administered 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.

When taken simultaneously with drugs that are metabolized in the liver (acenocoumarol, astemizole, cilostazol, cyclosporine, dihydroergotamine, ergotamine, omeprazole, quinidine, rifabutin, tacrolimus, terfenadine, vinblastine and antifungal drugs such as fluconazole, ketoconazole and itraconazole) in plasma the concentration of these drugs increases.

Concomitant use of erythromycin with ergotamine is associated with a risk of acute toxicity, manifested by vasospasm, ischemia of the limbs and other organs, including the central nervous system. Therefore, erythromycin is contraindicated in patients taking ergotamine.

When taken simultaneously with erythromycin, an increase in the level of cisapride is possible, which can lead to a prolongation of the QTc interval, the development of arrhythmia (ventricular fibrillation and flutter), and ventricular tachycardia of the “pirouette” type.

When taken together with verapamil and other slow calcium channel blockers, hypotension, bradyarrhythmia and lactic acidosis are observed.

Drugs that are inducers of CYP3A4 isoenzymes (such as rifampicin, phenytoin, carbamazepine, phenobarbital, St. John's wort) can induce the metabolism of erythromycin, which can lead to subtherapeutic concentrations of erythromycin and a decrease in its effect. The interaction persists for 2 weeks after discontinuation of treatment with CYP3A4 inducers.

The interaction of erythromycin with colchicine can increase toxicity and leads to a significant increase in the concentration of the latter in the blood plasma due to the ability of erythromycin to inhibit CYP3A4.

Erythromycin alters the metabolism of mizolastine.

When taken together with pimozide, arrhythmia (ventricular fibrillation and flutter), ventricular tachycardia of the “pirouette” type, cardiac arrest, and even death may develop.

Protease inhibitors: inhibit the metabolism of erythromycin; monitoring of plasma erythromycin concentrations is necessary.

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.