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|Erythromycin 500 mg|
270 pills - 500 mg
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|Erythromycin 250 mg|
270 pills - 250 mg
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Pharmacological action of Erythromycin
Instructions for medical use approved by the Pharmacological Committee of the Ministry of Health of the Russian Federation
Bacteriostatic antibiotic from the macrolide group, reversibly binds to the 50S ribosome subunit in its donor part, which disrupts the formation of peptide bonds between amino acid molecules and blocks the synthesis of proteins of microorganisms (does not affect the synthesis nucleic acids). When used in high doses, it can show bactericidal action. The spectrum of action includes gram-positive (Staphylococcus spp., Producing and non-producing penicillinase, including Staphylococcus aureus; Streptococcus spp. (Including Streptococcus pneumoniae, Streptococcus pyogenes), alpha-hemolytic streptococcus Bacillus), groups 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.
Resistant gram-negative bacilli: Escherichia coli, Pseudomonas aeruginosa, as well as Shigella spp., Salmonella spp. other. The sensitive group includes microorganisms, the growth of which 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.
Absorption - high. Food intake has no effect on oral forms of erythromycin in the form of a base, coated with an enteric coating. Cmax is achieved after oral administration in 2-4 hours. The connection with plasma proteins is 70-90%.
Bioavailability is 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 ten times higher than the concentration 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 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 content in the mother's plasma.
It is metabolized in the liver (more than 90%), partially with the formation of inactive metabolites. 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%.
Indications of the drug Erythromycin
Bacterial infections caused by sensitive microflora:
diphtheria (including the carrier of bacteria);
whooping cough (including prevention);
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 urogenital tract and rectum) with intolerance or ineffectiveness of tetracyclines;
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 (pustular skin diseases, including juvenile acne, infected wounds, bedsores, burns of the II-III degree, trophic ulcers);
infections of the mucous membrane of the eyes;
prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with rheumatism;
prevention of infectious complications during medical and diagnostic procedures (including preoperative bowel preparation, dental interventions, endoscopy, in patients with heart defects).
Dosing regimen of Erythromycin
A single dose fordose adults and adolescents over 14 years old is 250-500 mg, the dailyis 1-2 g. The interval between doses is 6 hours. In severe infections, the daily dose can be increased to 4 g.
Children from 4 months to 18 years old, in depending on age, body weight and severity of infection - 30-50 mg / kg / day in 2-4 doses; children of the first 3 months of life - 20-40 mg / kg / day. For more severe infections, the dose may be doubled.
For the treatment of diphtheria carriage - 250 mg 2 times / day. The course dose for the treatment of primary syphilis is 30-40 g, the duration of treatment is 10-15 days.
With amoebic dysentery adults - 250 mg 4 times / day, children - 30-50 mg / kg / day; course duration - 10-14 days.
With legionellosis - 500 mg-1 g 4 times / day for 14 days.
With gonorrhea - 500 mg every 6 hours for 3 days, then 250 mg every 6 hours for 7 days.
For preoperative bowel preparation in order to prevent infectious complications - by mouth, 1 g for 19 hours, 18 hours and 9 hours before the operation (only 3 g).
For the prevention of streptococcal infection (with tonsillitis, pharyngitis), adults - 20-50 mg / kg / day, children - 20-30 mg / kg / day, the duration of the course 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 a medical or diagnostic procedure, then 500 mg for adults and 10 mg / kg for children, again after 6 hours
with whooping cough - 40-50 mg / kg / day for 5-14 days. With pneumonia in children - 50 mg / kg / day in 4 divided doses, for at least 3 weeks. For genitourinary infections during pregnancy - 500 mg 4 times / day for at least 7 days, or (with poor tolerance of such a dose) - 250 mg 4 times / day for at least 14 days.
In adults, with uncomplicated chlamydia and tetracyclines intolerance - 500 mg 4 times / day for at least 7 days.
Contraindications to the use of
concomitant use of terfenadine or astemizole;
With care: arrhythmias (in history); prolongation of the QT interval; jaundice (history); liver failure; renal failure.
Application during pregnancy and lactation
Due to the possibility of penetration into breast milk, you should refrain from breastfeeding while taking erythromycin.
Application for violations of liver function
Contraindicated in liver failure.
Application for impaired renal function
Contraindicated in renal failure.
Application in children
Children from 4 months to 18 years old, depending on age, body weight and severity of infection - 30-50 mg / kg / day in 2-4 doses; children of the first 3 months of life - 20-40 mg / kg / day. For more severe infections, the dose may be doubled.
Use in elderly patients The
likelihood of developing an ototoxic effect is higher in elderly patients.
With long-term therapy, it is necessary to monitor laboratory parameters 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 hepatic insufficiency, as well as in elderly patients.
Some resistant strains of Haemophilus influenzae are susceptible to co-administration of erythromycin and sulfonamides.
May interfere with the determination of catecholamines in the urine and the activity of hepatic transaminases in the blood (colorimetric determination using definilhydrazine).
Symptoms: impaired liver function, up to acute liver failure, hearing loss.
Treatment: activated carbon, careful monitoring of the state of the respiratory system. Gastric lavage is effective when taking a dose that is five times the average therapeutic dose. Hemodialysis, peritoneal dialysis, forced diuresis are ineffective.
Drugs that block tubular secretion lengthen the T1/2 of erythromycin.
Incompatible with lincomycin, clindamycin and chloramphenicol (antagonism).
Reduces the bactericidal effect of beta-lactam antibiotics (penicillins, cephalosporins, carbopenems).
When taken simultaneously with drugs 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 liver microsomal enzymes).
Enhances 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 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 taken together with lovastatin, rhabdomyolysis is enhanced.
Increases the bioavailability of digoxin.
Reduces the effectiveness of hormonal contraception.
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 drug withdrawal is usually reversible).
Rarely - tachycardia, prolongation of the QT interval on the ECG, ventricular arrhythmias, including ventricular tachycardia ("pirouette" type) in patients with an extended QT interval.