Composition
Active ingredient: erythromycin (based on the Active ingredient) – 250 mg. Auxiliary substances: potato starch, calcium stearate, povidone (low molecular weight medical polyvinylpyrrolidone 12600±2700), polysorbate-80 (twin-80).
Pharmacological action
A bacteriostatic antibiotic from the macrolide group, reversibly binds to the 50S ribosomal subunit in its donor part, 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, it may have a bactericidal effect. The spectrum of action includes gram-positive (Staphylococcus spp., producing and not producing penicillinase, including Staphylococcus aureus; Streptococcus spp. 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., Entamoeba histolytica, Listeria monocytogenes. Gram-negative bacilli are resistant: Escherichia coli, Pseudomonas aeruginosa, as well as Shigella spp., Salmonella spp., etc. The sensitive group includes microorganisms whose growth is delayed at an antibiotic concentration of less than 0.5 mg/l, medium – sensitive – 1 – 6 mg/l, moderately resistant and resistant – 6-8 mg/l. Pharmacokineticabsorption is high. Food intake does not affect oral forms of Erythromycin in the form of a base coated with an enteric coating. The maximum concentration (Cmax) is reached after oral use in 2-4 hours. Plasma protein binding is 70-90%. Bioavailability – 30-65%. It is distributed unevenly in the body. It accumulates in large amounts in the liver, spleen, and kidneys. In bile and urine, the concentration is ten times higher than in plasma. It penetrates well into the tissues of the lungs, lymph nodes, middle ear exudate, prostate secretions, semen, pleural cavity, ascitic and synovial fluids. The milk of lactating women contains 50% of the plasma concentration. Poorly penetrates through the blood-brain barrier, into the spinal fluid (its concentration is 10% of the drug content in plasma). With inflammatory processes in the meninges, their permeability to Erythromycin increases slightly. Penetrates through the placental barrier and enters the blood of the fetus, where its content reaches 5-20% of the content in the mother’s plasma. It is metabolized in the liver (more than 90%), partly with the formation of inactive metabolites. Half-life (T1 / 2) – 1.4-2 hours, with anuria-4-6 hours. Excretion with bile-20-30% unchanged, kidneys (unchanged) after oral use-2-5%.
Indications
-Bacterial infections caused by sensitive microflora: diphtheria (including bacterial carrier), whooping cough (including prevention), trachoma, brucellosis, legionnaires ‘ disease, erythrasma, listeriosis, scarlet fever, amoebic dysentery, gonorrhea; conjunctivitis of newborns, pneumonia in children, genitourinary infections in pregnant women caused by Chlamydia trachomatis. Primary syphilis (in patients allergic to penicillins), uncomplicated chlamydia in adults (with localization in the lower genitourinary tract and rectum) with intolerance or ineffectiveness of tetracyclines, etc. ; – infections of ENT organs (tonsillitis, otitis media, sinusitis);- biliary tract infections (cholecystitis);- upper and lower respiratory tract infections (tracheitis, bronchitis, pneumonia);- skin and soft tissue infections (pustular skin diseases, including juvenile acne, infected wounds, bedsores, burns of II-III st, trophic ulcers);- infections of the eye mucosa;- prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with rheumatism. Prevention of infectious complications in medical and diagnostic procedures (including preoperative bowel preparation, dental interventions, endoscopy, in patients with heart defects).
Contraindications
Hypersensitivity, hearing loss, concomitant use of terfenadine or astemizole, children under 3 years of age, lactation. With caution, arrhythmias( in the anamnesis), prolongation of the QT interval, jaundice (in the anamnesis), hepatic and/or renal failure.
Side effects
Hypersensitivity reactions: allergic skin reactions (urticaria, other forms of rash), eosinophilia, rarely-anaphylactic shock. Nausea, vomiting, gastralgia, tenesmus, abdominal pain, diarrhea, dysbiosis, rarely oral candidiasis, pseudomembranous enterocolitis (both during and after treatment), liver dysfunction, cholestatic jaundice, increased activity of “hepatic” transaminases, pancreatitis, hearing loss and/or tinnitus (when using high doses – more than 4 g/day, hearing loss after discontinuation of the drug is usually reversible). Rarely-tachycardia, prolongation of the QT interval on the ECG, ventricular arrhythmias, including ventricular tachycardia (such as “pirouette”), in patients with an extended QT interval. Overdose symptoms: impaired liver function, up to acute liver failure, hearing loss. Treatment: activated charcoal, careful monitoring of the respiratory system. Gastric lavage is effective when taking a dose five times higher than the average therapeutic dose. Hemodialysis, peritoneal dialysis, and forced diuresis are ineffective.
Interaction
Drugs that block tubular secretion extend the half-life of Erythromycin. Incompatible with lincomycin, clindamycin and chloramphenicol (antagonism). Reduces the bactericidal effect of beta-lactam antibiotics (penicillins, cephalosporins, carbopenems). When taken concomitantly with drugs that are metabolized in the liver (theophylline, carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanyl, disopyramide, lovastatin, bromocriptine), the concentration of these drugs in plasma may increase (it is an inhibitor of microsomal liver enzymes). Increases the nephrotoxicity of cyclosporine (especially in patients with concomitant renal insufficiency). 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 arrhythmia, with dihydroergotamine or non-hydrogenated ergot alkaloids – vasoconstriction to spasm, dysesthesia. Slows down the elimination (enhances the effect) of methylprednisolone, felodipine and coumarin anticoagulants. When co-administered with lovastatin, rhabdomyolysis increases. Increases the bioavailability of digoxin.
How to take, course of use and dosage
Inside. 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 use is 6 hours. In severe infections, the daily dose can be increased to 4 g. Children from 3 to 14 years of age, depending on age, body weight and severity of infection – 30 – 50 mg/kg/day in 2 – 4 doses. In case of severe infections, the dose may be doubled. For the treatment of diphtheria carriers – 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; the course duration is 10-14 days. With 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 preoperative bowel preparation to prevent infectious complications – inside,1 g for 19 hours,18 hours and 9 hours before the operation (total of 3 g). For the prevention of streptococcal infection (with tonsillitis, pharyngitis), adults – 20-50 mg / kg / day, children-20-30 mg / kg/day, the course duration is 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 the treatment or diagnostic procedure, then 0.5 g for adults and 10 mg / kg for children, again after 6 hours. For whooping cough – 40-50 mg / kg / day for 5-14 days. For pneumonia in children – 50 mg / kg / day in 4 doses, for at least 3 weeks. For urogenital infections during pregnancy-0.5 g 4 times a day for at least 7 days or (if such a dose is poorly tolerated) – 0.25 g 4 times a day for at least 14 days. In adults with uncomplicated chlamydia and tetracycline intolerance-0.5 g 4 times a day for at least 7 days.
Special instructions
Due to the possibility of penetration into breast milk, you should refrain from breast-feeding when prescribing Erythromycin. With long-term therapy, it is necessary to monitor laboratory parameters of liver function. Symptoms of cholestatic jaundice may develop a few days after the start of therapy, but the risk increases after 7-14 days of continuous therapy. The probability of developing an ototoxic effect is higher in patients with renal and hepatic insufficiency, as well as in elderly patients. Some resistant strains of Haemophilus influenzae are sensitive to simultaneous use of erythromycin and sulfonamides. It may interfere with the determination of catecholamines in the urine and the activity of “hepatic” transaminases in the blood (colorimetric determination using definylhydrazine).
Storage conditions
List B. Store in a dry place at room temperature.
Shelf life
2 years
Active ingredient
Erythromycin
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Purpose
Pregnant women as prescribed by a doctor, Adults as prescribed by a doctor, Children as prescribed by a doctor, Children over 3 years of age
Indications
Infectious diseases, Sore throat, Purulent wounds, Chlamydia, Biliary tract infections, Pharyngitis, Bronchitis, Tracheitis, Eye Infections, Sinusitis, Pyoderma, Tonsillitis, Pneumonia, Cholecystitis, Urinary Tract Infections, Sinusitis, Whooping Cough, Acne
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Side effects of Erythromycin pills 250mg, 10pcs.
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