Eritromitsina

General characteristics. Structure:

Active agent: Erythromycin phosphate (in terms of erythromycin) - 100 mg, 200 mg.

Pharmacological properties:

The bacteriostatic antibiotic from group of macroleads, reversibly communicates with 50S in subunit of ribosomes that breaks formation of peptide bonds between molecules of amino acids and blocks protein synthesis of microorganisms (does not influence synthesis of nucleic acids). At use in high doses depending on a type of the activator can show bactericidal action. Microorganisms which growth is late at concentration of an antibiotic less than 0.5 mg/l, moderately sensitive - 1-6 mg/l, steady - 6-8 mg/l belong to sensitive. The action spectrum includes: gram-positive microorganisms: Staphylococcus spp., the producing and not producing penicillinases, including Staphylococcus aureus; Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes), alpha and hemolitic streptococcus (Viridans groups), Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium minutissimum; gram-negative microorganisms: Neisseria gonorrhoeae, Haemophilus influenzae, Campylobacter jejuni, Bordetella pertussis, Brucella spp., Legionella spp., including Legionella pneumophila, etc. microorganisms: Mycoplasma spp. (including Mycoplasma pneumoniae), Chlamydia spp. (including Chlamydia trachomatis), Treponema spp., Rickettsia spp., Entamoeba histolytica, Listeria monocytogenes. Gram-negative sticks are steady against drug: Escherichia coli, Pseudomonas aeruginosa, and also Shigella spp., Salmonella spp., Bacteroides fragilis, Enterobacter spp., etc. 

Pharmacokinetics. Time of achievement of the maximum concentration after intravenous administration - 20 min. Communication with proteins of plasma - 70-90%. Bioavailability - 30-65%. In an organism it is distributed unevenly. In large numbers collects in a liver, a spleen, kidneys. In bile and urine concentration in tens of times exceeds that in plasma. Well gets into tissues of lungs, lymph nodes, exudate of a middle ear, a prostate secret, sperm, a pleural cavity, ascitic and synovial liquids. Milk of the feeding women contains 50% of concentration in plasma. Badly gets through a blood-brain barrier, into cerebrospinal fluid (concentration makes 10% of concentration of drug in plasma). At inflammatory processes their permeability for erythromycin increases in brain covers a little. As well as other macroleads, erythromycin it is capable to get in cells including in cells of immune system, creating at the same time very high intracellular concentration: concentration of an antibiotic in alveolar macrophages at 9-23 time, and in neutrophils at 4-24 time exceed its levels in extracellular liquid. However, intracellular concentration of erythromycin are unstable, and after drug withdrawal they quickly enough decrease. Gets through a placental barrier and comes to fruit blood where its contents reaches 5-20% of content in mother's plasma. At intravenous administration of drug by the newborn high concentration it in blood (on average about 13 mkg/ml) are maintained is longer, than at children of more advanced age. Process of decrease in concentration has clear two-phase character: in the first 2 hours it decreases much quicker than in the next 10 hours. It is metabolized in a liver (more than 90%), partially with formation of inactive metabolites. Isoenzymes of CYP3A4, CYP3A5 and CYP3A7 which inhibitor it is participate in metabolism of drug. An elimination half-life - 1.4-2 h, at an anury - 4-6 h. Removal with bile - 20-30% in not changed look, kidneys (in not changed look) after intravenous administration - 12-15%.

Indications to use:

Treatment of severe forms of the bacterial infections caused by sensitive microflora when administration of drug is inside ineffective or impossible when it is necessary to create quickly in blood high concentration of an antibiotic, including at the following diseases:

— diphtheria (including diphtheritic carriage);

— whooping cough (including prevention of a disease at the persons put risk of infection);

— trachoma;

— brucellosis;

— disease of legionaries;

— scarlet fever;

— amoebic dysentery;

— gonorrhea;

— conjunctivitis of newborns;

— the pneumonia at children caused by Chlamydia trachomatis;

— the urinogenital infections at pregnant women caused by Chlamydia trachomatis;

— uncomplicated clamidiosis at adults (with localization in lower parts of urinogenital ways and a rectum) at intolerance or inefficiency of tetracyclines;

— primary syphilis (at patients with an allergy to penicillin);

— infections of ENT organs (tonsillitis, otitis, sinusitis);

— infections of biliary tract (cholecystitis);

— infections of upper and lower respiratory tracts (tracheitis, bronchitis, pneumonia);

— infections of skin and soft tissues.

Prevention of infectious complications at medical and diagnostic procedures (including dental interventions, endoscopy) at patients with heart diseases.

Is a reserve antibiotic for treatment of the bacterial infections caused by strains of gram-positive activators (in particular, stafilokokkam), steady against penicillin.

Route of administration and doses:

Intravenously slowly (within 3-5 min.) or kapelno. Preferably and more safely intravenous drop administration of drug. The single dose of drug for adults makes 0,2 g, daily - 0,6 g. At the heavy course of an infection the daily dose can be increased to 1 g, then the drug is administered 4 times a day (every 6 hours). To children from 4 months to 18 years depending on age, body weight and weight of an infection - till 30-50 мк/кг/сут (for 2-4 introductions); to children of the first 3 months of life - 20-40 мк/кг/сут. In case of heavy infections the dose can be doubled. For intravenous jet administration drug is dissolved in water for injections or 0.9% chloride sodium solution at the rate of 5 mg on 1 ml of solvent. For intravenous drop administration dissolve in 0.9% solution of sodium of chloride or 5% dextrose solution to concentration of 1 mg/ml and enter with a speed of 60-80 of cap/min. Intravenously enter within 5-6 days (before clear therapeutic effect) with the subsequent transition to oral administration. At good tolerance and absence of phlebitis and a periphlebitis it is possible to prolong a course of intravenous administration up to 2 weeks (no more). At a renal failure there is no need of dose adjustment of drug.

Features of use:

With care apply at abnormal liver functions and/or kidneys.

The drugs increasing acidity of a gastric juice and acid drinks inactivate erythromycin.

Side effects:

From the alimentary system: an abnormal liver function, increase in activity of hepatic transaminases, nausea, vomiting, tenesmus, diarrhea, abdominal pains, cholestatic jaundice, a pseudomembranous coloenteritis (both during treatment, and after the termination).

From an acoustic organ: decrease in hearing and/or a sonitus (ototoxicity after cancellation is usually reversible).

Allergic reactions: urticaria, skin rash, eosinophilia, acute anaphylaxis.

From cardiovascular system: tachycardia, blinking and/or an atrial flutter (patients with the extended interval have QT on an ECG).

Interaction with other medicines:

Erythromycin phosphate is incompatible with lincomycin, clindamycin and chloramphenicol because of antagonism of action.

At a concomitant use with terfenadiny or astemizoly the risk of development of arrhythmia increases.

At simultaneous use of Erythromycin of phosphate with the drugs blocking canalicular secretion the erythromycin elimination half-life is extended.

Erythromycin phosphate reduces bactericidal action beta лактамных antibiotics (penicillin, cephalosporins, karbapenema).

At simultaneous use of Erythromycin of phosphate with theophylline concentration of the last increases.

At simultaneous use with drugs which metabolism is carried out in a liver (carbamazepine, valproic acid, hexobarbital, Phenytoinum, alfentanit, Disopyramidum, ловастатин, Bromocriptinum), concentration of these drugs in plasma since erythromycin is inhibitor of microsomal enzymes of a liver can increase.

Erythromycin phosphate increases nephrotoxicity of cyclosporine (especially at patients with the accompanying renal failure).

Erythromycin phosphate reduces clearance of a triazolam and midazolam in this connection can strengthen pharmacological effects of these benzodiazepines.

At simultaneous use of Erythromycin of phosphate with dihydroergotamine or not hydrogenated alkaloids of an ergot vasoconstriction with development of spasms, dizesteziya is noted.

Erythromycin phosphate slows down removal and strengthens effects of Methylprednisolonum, felodipin and anticoagulants of a coumarinic row.

At joint appointment with lovastatiny development of a rabdomioliz is possible.

Erythromycin phosphate increases bioavailability of digoxin and reduces efficiency of hormonal contraception.

Contraindications:

— jaundice (in the anamnesis);

— liver and/or renal failure;

— concomitant use of a terfenadin or astemizol;

— hypersensitivity to drug components.

 

ERYTHROMYCIN drug use PHOSPHATE at pregnancy and feeding by a breast
If necessary use of drug at pregnancy it is necessary to estimate estimated advantage for mother and potential risk for a fruit.

In need of use in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

 

Use at abnormal liver functions
It is contraindicated at a liver failure.

 

Use at renal failures
It is contraindicated at a renal failure.

 

Use for children
To children of all age groups drug appoint in a daily dose 20 mg/kg (in 2-3 receptions).

Overdose:

Symptoms: nausea, diarrhea, discomfort in a stomach, acute pancreatitis, dizziness (especially at patients with a liver or renal failure).

Treatment: careful control of a condition of respiratory system (if necessary - carrying out IVL), acid-base balance and electrolytic exchange. The hemodialysis, peritoneal dialysis, an artificial diuresis are ineffective.

Storage conditions:

List B. Drug should be stored in dry, protected from light and the place, unavailable to children, at a temperature from 15 °C to 25 °C. A period of validity - 4 years.

Issue conditions:

According to the recipe

Packaging:

1 bottle with the lyophilized powder for preparation of injection solution contains mg erythromycin 100 or 200; in a cardboard pack 10 or in a box of 50 bottles.