Erythromycin, 250 mg 20 pcs

Pharmacotherapeutic group

Macrolide antibiotic

ATX code: S01AA17

Pharmacodynamics:

Bacteriostatic antibiotic of the macrolide group. It binds irreversibly to 50S subunit of ribosomes which disrupts formation of peptide bonds between amino acid molecules and blocks protein synthesis in microorganisms (it does not affect synthesis of nucleic acids). When used in high doses depending on the type of pathogen it may show bactericidal effect.

Sensitive microorganisms are those which inhibit their growth at antibiotic concentration below 05 mg/l, moderately sensitive – 1-6 mg/l, resistant – more than 6 mg/l.

The broad spectrum of antimicrobial action of erythromycin includes:

Gram-positive microorganisms: Staphylococcus spp. producing and non-producing penicillinase including Staphylococcus aureus (except strains resistant to methicillin – MRSA); Streptococcus spp.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.

Eritromycin is resistant to Gram-negative bacilli: Escherichia coli and other members of the family Enterobacteriaceae (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. It accelerates the evacuation of gastric contents by increasing the amplitude of contraction of the pylorus and improving the antral-duodenal coordination has prokinetic properties.

Pharmacokinetics:

The absorption is high. Food intake has no effect on oral forms of erythromycin as base coated with a film-coated enteric-soluble coating.

Time to reach maximum concentration in blood plasma after oral administration – 2-4 hours Protein binding – 70-90%. Bioavailability is 30-65%. The drug is not evenly distributed in the body. Large amounts are accumulated in the liver, spleen and kidneys. The concentration in bile and urine is ten times higher than in plasma. It penetrates well into lung lymph node tissue, middle ear exudate, prostate secretion, sperm pleural cavity, ascitic and synovial fluid.

In milk of lactating women contains 50% of the concentration in plasma. It poorly penetrates through the blood-brain barrier (BBB) into the cerebrospinal fluid (CSF) (the concentration is 10% of the drug concentration in plasma). In inflammatory processes in the brain membranes their permeability to erythromycin increases slightly. It penetrates through the placental barrier and enters the fetal bloodstream where its content reaches 5-20% of the plasma content in the mother.

It is metabolized in the liver (more than 90%) partially with the formation of inactive metabolites. CYP3A4 CYP3A5 and CYP3A7 isoenzymes are involved in the metabolism of erythromycin. The elimination half-life (T1/2) is 14-2 h with anuria – 4-6 h. Excretion with bile – 20-30% unchanged by kidneys (unchanged) after oral administration – 2-5%.

Indications

Bacterial infections caused by susceptible pathogens:

– ENT organ infections (laryngitis pharyngitis tonsillitis sinusitis external and middle otitis media);

– lower respiratory tract infections (tracheitis bronchitis pneumonia);

– skin and soft tissue infections (pustular skin diseases including.Infections of the skin and soft tissues (pustular skin diseases including juvenile acne infected wounds decubitus burns II-III stage. trophic ulcers);

– biliary tract infections (cholecystitis);

– urogenital infections in pregnant women caused by Chlamydia trachomatis;

– uncomplicated chlamydia in adults (with localization in the lower urinary tract and rectum) when tetracyclines are intolerant or ineffective;

– primary syphilis (in patients allergic to penicillins);

– gonorrhea;

– diphtheria (including bacteriocytosis).

– diphtheria (including bacteriocarriage) whooping cough (including prevention) scarlatina trachoma legionellosis (legionnaire’s disease) erythrax listeriosis amebic dysentery;

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

Prevention of infectious endocarditis during dental and ENT operations in patients with risk factors (heart defects, prosthetic valves, etc.).

Eritromycin is the antibiotic of choice for allergies to penicillin and other antibiotics of the penicillin group as well as other beta-lactams.

Active ingredient

Composition

Composition per 1 tablet:

Composition of the core:

active ingredient: erythromycin (in terms of active ingredient) – 250 mg;

excipients: povidone-12.6 thousand. (polyvinylpyrrolidone low molecular weight medical 12600±2700) – 9.45 mg, crospovidone (collidone CL-M) – 13.5 mg, calcium stearate – 4.14 mg, talc – 10.35 mg, potato starch – to the weight of the core 450 mg.

The composition of the shell: cellulose (acetyl phthalyl cellulose) – 16.2 mg, titanium dioxide (titanium dioxide – 0.8 mg), castor oil 3.0 mg.

How to take, the dosage

Ingestion. Take the tablet 1-2 hours before a meal or 2-3 hours after a meal.

The tablet should not be divided and chewed.

Adults and adolescents over 14 years of age: usual doses for most infections: single dose is 250-500 mg daily dose is 1000-2000 mg (1-2 g). Erythromycin is taken 4 times a day with an interval of 6 hours between doses. If daily dose of Erythromycin is less than 1 g/day, it is possible to take the drug twice a day (500 mg every 12 hours).

In severe infections, the daily dose of Erythromycin may be increased to 4 g (4000 mg). The maximum daily dose of Erythromycin for adults is 4 g (4000 mg).

The course of treatment is 5-14 days after symptoms have disappeared, treatment is continued for another 2 days.

The treatment of streptococcal infections of various localizations (including tonsillitis and pharyngitis) should be continued for at least 10 days.

In case of juvenile acne – 250 mg 2 times a day simultaneously with local therapy, then after 1 month from the beginning of treatment depending on the condition the dose can be reduced to 250 mg once a day.

In genitourinary chlamydial infections during pregnancy, 500 mg 4 times daily for at least 7 days or (if this dose is poorly tolerated) 250 mg 4 times daily (or 500 mg 2 times daily 12 hours apart) for at least 14 days.

In uncomplicated chlamydia (urethral endocervical or rectal) with intolerance to tetracycline antibiotics, adults – 500 mg 4 times daily for at least 7 days.

Interaction

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

Incompatible with lincomycin clindamycin and chloramphenicol (antagonism).

Increases theophylline concentration.

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

Decreases clearance of triazolam and midazolam and therefore may increase the pharmacological effects of benzodiazepines.

Co-use with lovastatin simvastatin and other statins increases the risk of rhabdomyolysis.

Increases the bioavailability of digoxin.

Decreases the effectiveness of hormonal contraception.

Medicinal products (drugs) that block tubular secretion prolong the T1/2 of erythromycin.

When used concomitantly with drugs metabolized in the liver by the cytochrome P450 system (carbamazepine valproic acid hexobarbital phenytoin alfentanil disopyramide lovastatin bromocriptine) plasma concentrations of these drugs may be increased (because erythromycin is an inhibitor of microsomal liver enzymes).

If combined with terfenadine or astemizole, arrhythmias (ventricular fibrillation and torsade de pointes up to fatal) with dihydroergotamine or unhydrogenated ergot alkaloids – vasoconstriction up to complete dysesthesia.

Special Instructions

Laboratory measures of liver function should be monitored during long-term therapy.

The symptoms of cholestatic jaundice may develop within a few days after the start of therapy; however, the risk of development increases after 7-14 days of continuous therapy. The likelihood of ototoxic effects is higher in patients with renal and/or hepatic impairment and in elderly patients.

May interfere with the determination of catecholamines in the urine and “hepatic” transaminase activity in the blood (colorimetric determination with definyl hydrazine).

Do not drink milk or dairy products.

The antral and duodenal prokinetic effects of erythromycin have been proven in numerous clinical studies.

The use of the drug has no effect on driving and operating machines and mechanisms requiring concentration.

Contraindications

Hypersensitivity to erythromycin and other macrolides; significant hearing loss; concomitant use of terfenadine astemizole pimozide ergotamine dihydroergotamine children under 14 years of age breast-feeding period.

Arrhythmias (history) prolonged Q-T interval jaundice (including history) hepatic and/or renal failure.

If you have any of the above conditions, be sure to consult your doctor before taking the drug.

Side effects

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

Digestive system disorders: nausea vomiting gastralgia abdominal pain tenesmus diarrhea dysbacteriosis oral candidiasis pseudomembranous colitis liver function disorders cholestatic jaundice increased activity of “liver” transaminases pancreatitis.

Hearing organ: ototoxicity – decreased hearing and/or tinnitus (when used in high doses – more than 4 g/day usually reversible).

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

If any of the side effects listed in the instructions worsen, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms: impairment of liver function up to acute liver failure rarely hearing impairment.

Treatment: activated charcoal careful monitoring of the respiratory system (if necessary – performing artificial ventilation) acid-base state and electrolyte metabolism electrocardiogram.

Gastric lavage is effective if the dose is five times the average therapeutic dose.

Hemodialysis peritoneal dialysis and forced diuresis are ineffective.

Pregnancy use

The use of Erythromycin in pregnancy is possible only when the expected benefits to the mother exceed the potential risk to the fetus.

In lactation during lactation due to the possibility of penetration into the breast milk, Erythromycin should be refrained from breastfeeding.

Similarities