Erythromycin

General characteristics. Structure:

International and chemical names: erythromycin; (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-4-[(2,6-дидеокси-3-С-метил-3-О-метил-a-L-рибо-гексопиранозил) - oks] -14-этил-7,12,13-тригидрокси-3,5,7,9,11,13-гексаметил-6 - [[3,4,6-тридеокси-3-диметиламино-b-D-ксило-гексопиранозил] - oks] - oksatsiklotetradekan-2,10-dion (erythromycin A); main physical and chemical properties: tablets of a round form, color, white, almost white or white with a yellowish shade, with a biconvex surface. Scarcely noticeable impregnations are allowed; structure: 1 tablet contains erythromycin in terms of 1000 mkg/mg (PIECE/mg) and anhydrous substance - 100 mg; excipients: potato starch, calcium stearate, aerosil.

Pharmacological properties:

Pharmacodynamics. Erythromycin – a makrolidny antibiotic of bacteriostatic action. In big concentration and in relation to highly sensitive microorganisms can have bactericidal effect. Gets through a cellular membrane of bacteria and reversibly contacts subunit 50S of bacterial ribosomes; brakes a translocation of peptides from the acceptor site of a ribosome to donor, interfering with further synthesis of protein.
It is active in relation to gram-positive bacteria: Streptococcus pyogenes, Streptococcus viridans, Streptococcus pneumoniae, Staphylococcus aureus, Corynebacterium diphtheriae, Corynebacterium minutissimum, Listeria monocytogenes; to gram-negative bacteria: Bordetella pertussis, Legionella pneumophila, some strains of Haemophilus influenzae, Mycoplasma pneumoniae, and also in relation to Entaemoeba hystolitica, Chlamydia trachomatis, Treponema pallidum.
Gram-negative sticks are steady against effect of erythromycin: intestinal, pyocyanic, and also shigellas, salmonellas.

Pharmacokinetics. It is soaked up in a digestive tract, at the same time the speed of absorption depends on specific features of an organism. Bioavailability makes 30 – 65%. The maximum concentration in blood is noted in 2 hours after reception. It is distributed in the majority of fabrics and liquids of an organism, gets through a placental barrier and into breast milk.
Linkng with proteins of plasma makes 70 – 90%. It is metabolized in a liver, partially with formation of inactive metabolites. A considerable part of erythromycin is brought out of an organism with bile and only 2 – 5% in steady-state condition with urine. An elimination half-life – 1,4 – 2 hours at normal function of kidneys.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug, including pneumonia, pneumopleuritis, bronchoectatic disease in aggravation stages, septic states, an ugly face, mastitis, osteomyelitis, peritonitis, purulent otitis and other pyoinflammatory processes; diphtheria, whooping cough, trachoma, brucellosis, scarlet fever; gonorrhea, syphilis at patients with hypersensitivity to drugs of a penicillinic row; other infections caused by the microorganisms steady against penicillin, tetracyclines, chloramphenicol, streptomycin.

Route of administration and doses:

Establish individually, depending on localization and weight of course of an infection, sensitivity of the activator.
Appoint inside for 1 – 1,5 hour to or in 2 – 3 hours after food. The adult on 200 – 500 mg 4 times a day; the highest single dose – 500 mg, daily – 2 g. To children from 3 to 6 years – 500 – 700 mg a day; from 6 to 8 years – 700 mg a day; from 8 to 14 years – to 1 g a day, having divided a daily dose into 4 receptions; at the age of more than 14 years – in a dose for adults. A course of treatment – 5 - 14 days, after disappearance of symptoms of a disease apply on an extent of 2 days.

Features of use:

With care appoint at abnormal liver functions and kidneys. When performing long therapy by Erythromycin or at reception of high doses of drug it is necessary to control indicators of function of a liver.
Symptoms of cholestatic jaundice can develop after 7 – 14 days of continuous therapy by Erythromycin. Patients with a partial hearing loss in the anamnesis can have an increased risk of its further loss, especially if patients are people of advanced age and have a renal failure or a liver and receive high doses of Erythromycin.
At prolonged use of Erythromycin development of stability of microorganisms to drug and to other antibiotics macroleads is possible.
There are no references that Eritromitsin can negatively influence psychomotor reactions at the drivers and people working with the equipment.
The drugs increasing acidity of a gastric juice and acid drinks inactivate erythromycin.
Erythromycin cannot be washed down with milk and dairy products.
At purpose of Erythromycin during pregnancy it is necessary to estimate possible advantage for mother and potential risk for a fruit. In case of need appointments during a lactation it is necessary to resolve an issue of the feeding termination by a breast.

Side effects:

From the alimentary system nausea, vomiting, pain in epigastriums, cholestatic jaundice are possible;
from sense bodys: decrease in hearing and/or a sonitus which disappears after drug withdrawal;
allergic reactions: skin rash, small tortoiseshell, acute anaphylaxis; the effects caused by chemotherapeutic action: oral cavity candidiasis, vagina candidiasis.

Interaction with other medicines:

Simultaneous use of Erythromycin and lincomycin or chloramphenicol weakens their action.
Erythromycin increases concentration of theophylline, Aminophyllinum, carbamazepine, caffeine in a blood plasma, thereby increasing risk of their toxic action.
Simultaneous use of Erythromycin and digoxin causes increase in level of digoxin in a blood plasma.
Erythromycin oppresses ergotamine metabolism, strengthening the vasospasm connected with ergotamine.
At the simultaneous use of Erythromycin and other drugs possessing hepatotoxic or ototoksichesky action the risk of hepatotoxic or ototoksichesky action amplifies.
At simultaneous use of a lovastatin and Erythromycin the risk of an acute necrosis of skeletal muscles which can usually develop after the end of treatment by Erythromycin can increase.
At simultaneous use of midazolam or a triazolam and Erythromycin the clearance of these drugs can decrease owing to what the pharmacological effect of midazolam and a triazolam amplifies.
Strengthening of effect of anticoagulants at their simultaneous use with Erythromycin is described. This effect is more expressed at people of advanced age.
Drug increases concentration of cyclosporine in a blood plasma and can increase risk of development of nephrotoxic action.
Effect of Erythromycin amplifies in a combination with streptocides and tetracyclines.

Contraindications:

Hypersensitivity to erythromycin and macroleads, the expressed abnormal liver functions, children up to 3 years.

Overdose:

Symptoms: nausea, vomiting, diarrhea and feeling of discomfort in a stomach; an abnormal liver function, up to an acute liver failure; a hearing loss, a sonitus, dizziness (especially at patients with a renal or liver failure).
Treatment: use of absorbent carbon, careful control of a condition of breath (in case of need – carrying out IVL), acid-base equilibrium and electrolytic exchange.
The gastric lavage is effective at reception of the dose exceeding an average therapeutic dose by 5 times. The hemodialysis, peritoneal dialysis and an artificial diuresis are ineffective.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature not above 25 °C.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 20 tablets in a blister strip packaging.