Erythromycin - instructions for use, dose, side effects, contraindications

Bacteriostatic antibiotic from the group of macrolides, reversibly binds to 50S subunit of ribosomes, which disrupts the formation of peptide bonds between amino acid molecules and blocks the synthesis of proteins of microorganisms (does not affect the synthesis of nucleic acids). When used in high doses depending on the type of pathogen can exhibit bactericidal action.

Sensitive include microorganisms, whose growth is delayed at an antibiotic concentration of less than 0.5 mg / l, moderately sensitive - 1-6 mg / l, stable - 6-8 mg / l.

The spectrum of action includes:

Gram-positive microorganisms: Staphylococcus spp., producing and not producing penicillinase, incl. Staphylococcus aureus; Streptococcus spp. (incl. Streptococcus pneumoniae, Streptococcus pyogenes), alpha-hemolytic streptococcus (groups Viridans), Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium minutissimum;

gram-negative microorganisms: Neisseria gonorrhoeae, Haemophilus influenzae, Campylobacter jejuni, Bordetella pertussis, Brucella spp., Legionella spp., incl. Legionella pneumophila and other microorganisms: Mycoplasma spp. (at t.h. Mycoplasma pneumoniae), Chlamydia spp. (at t.h. Chlamydia trachomatis), Treponema spp., Rickettsia spp., Entamoeba histolytica, Listeria monocytogenes.

The drug is stable gram-negative rods: Escherichia coli, Pseudomonas aeruginosa, and Shigella spp., Salmonella spp., Bacteroides fragilis, Enterobacter spp. and etc.

Pharmacokinetics:

The time to reach the maximum concentration after intravenous administration is 20 min. The connection with plasma proteins is 70-90%. Bioavailability is 30-65%. In the body it is distributed unevenly. In large quantities, it accumulates in the liver, spleen, kidneys. In bile and urine, the concentration is ten times higher than that in plasma. It penetrates well into the tissues of the lungs, lymph nodes, exudate of the middle ear, secretion of the prostate gland, sperm, pleural cavity, ascitic and synovial fluid. The milk of lactating women contains 50% of the concentration in the plasma. Poorly penetrates the blood-brain barrier into the cerebrospinal fluid (concentration is 10% of the concentration of the drug in the plasma). In inflammatory processes in the membranes of the brain, their permeability for erythromycin increases somewhat.

Like other macrolides, erythromycin is able to penetrate into cells, including cells of the immune system, while creating very high intracellular concentrations: the concentration of antibiotic in alveolar macrophages is 9-23 times, and in neutrophils it is 4-24 times higher than its levels in the extracellular fluid. However, intracellular concentrations of erythromycin are unstable, and after drug discontinuation they decrease rather quickly. It penetrates the placental barrier and enters the blood of the fetus, where its content reaches 5-20% of the content in the mother's plasma.

With intravenous injection of the drug to newborns, its high concentrations in the blood (on average about 13 μg / ml) are maintained longer than in older children. The process of reducing the concentration has a distinct biphasic character: in the first 2 hours it decreases significantly faster than in the next 10 hours.

Metabolised in the liver (more than 90%), partially with the formation of inactive metabolites. In the metabolism of the drug, isozymes participate CYP₃_A₄, CYP₃_A₅ and CYP₃_A₇, of which it is an inhibitor.

The half-life is 1.4-2 hours, with anuria 4-6 hours. Excretion with bile is 20-30% unchanged, with kidneys (unchanged) after intravenous administration - 12-15%.

Indications:

Bacterial infections caused by susceptible pathogens: diphtheria (including bacteriocarriers), whooping cough, trachoma, brucellosis, legionnaires, erythrasma, listeriosis, scarlet fever, amoebic dysentery, gonorrhea; genitourinary infections in pregnant women caused by Chlamydia trachomatis; primary syphilis (in patients with penicillin allergy), an infection with ENT organs (tonsillitis, otitis, sinusitis); bile duct infection (cholecystitis); infections of the upper and lower respiratory tract (tracheitis, bronchitis, pneumonia); infections of the skin and soft tissues (infected wounds, bedsores, burns II-III st, trophic ulcers).

Prevention of infectious complications in medical and diagnostic procedures (including preoperative intestinal preparation, dental interventions, endoscopy, in patients with heart defects).

Gastroparesis (including gastroparesis after vagotomy, diabetic gastroparesis and gastroparesis, associated with progressive systemic sclerosis).

Contraindications:

Hypersensitivity, significant hearing loss, simultaneous reception of terfenadine or astemizole, lactation.

Carefully:

Arrhythmias (in the anamnesis), lengthening of the interval QT, jaundice (history), hepatic and / or renal insufficiency, pregnancy.

Pregnancy and lactation:

The use of the drug in pregnancy is possible only in those cases when the intended use for the mother exceeds the potential risk to the fetus.

If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

Dosing and Administration:

Intravenously slowly (within 3-5 minutes) or drip. Preferably, and more safely, the intravenous drip of the preparation.

A single dose of the drug for adults is 0.2 g, daily 0.6 g. In severe infection, the daily dose can be increased to 1 g, then the drug is administered 4 times a day (every 6 hours). Children from 4 months to 18 years, depending on the age, body weight and severity of infection - 30-50 mg / kg / day (for 2-4 injection); children of the first 3 months of life - 20-40 mg / kg / day. In case of severe infections, the dose can be doubled.

For intravenous fluid administration, the drug is dissolved in water for injection or 0.9% solution of sodium chloride at a rate of 5 mg per 1 ml of solvent.

For intravenous drip infusion, dissolve in a 0.9% sodium chloride solution or 5% dextrose solution to a concentration of 1 mg / ml and inject at a rate of 60-80 cap / min.Intravenously injected for 5-6 days (before the onset of a distinct therapeutic effect) with a subsequent transition to oral administration.

With good tolerability and absence of phlebitis and periflebit, the course of intravenous administration can be prolonged up to 2 weeks (no more).

With renal failure, there is no need to adjust the dose of the drug.

Side effects:

From the gastrointestinal tract: nausea, vomiting, gastralgia, abdominal pain, tenesmus, diarrhea, dysbacteriosis, rarely - candidiasis of the oral cavity, pseudomembranous enterocolitis, impaired liver function, cholestatic jaundice, increased activity of "liver" transaminases, pancreatitis.

In newborns receiving erythromycin, the risk of pyloric stenosis is high.

From the organs of hearing: ototoxicity: hearing loss and / or tinnitus (when used in high doses - more than 4 g / day, usually reversible).

From the cardiovascular system: rarely - tachycardia, lengthening of the interval QT on ECG, flicker and / or atrial flutter (in patients with an elongated interval QT on the ECG).

Allergic reactions: urticaria, skin rash, eosinophilia, rarely anaphylactic shock.

Local reactions: phlebitis at the site of intravenous administration.

Overdose:

Symptoms: nausea, diarrhea, discomfort in the stomach; dizziness (especially in patients with hepatic or renal insufficiency); a violation of the liver, up to acute liver failure, rarely - hearing impairment.

Treatment: careful monitoring of the state of the respiratory system (if necessary - carrying out artificial ventilation of the lungs), acid-base state and electrolyte metabolism, ECG. It is necessary to carry out symptomatic therapy. Hemodialysis, peritoneal dialysis and forced diuresis are ineffective.

Interaction:

Reduces the bactericidal action of beta-lactam antibiotics (penicillins, cephalosporins, carbopenems). Increases the concentration of theophylline.

Intravenous introduction of erythromycin increases the effect of ethanol (acceleration of gastric emptying and reduction of the duration of action of ethanol dehydrogenase in the gastric mucosa).

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

Reduces the clearance of triazolam and midazolam,in connection with which it can enhance the pharmacological effects of benzodiazepines.

Slows down the elimination (increases the effect) of methylprednisolone, felodipine and anticoagulants of the coumarin series.

When co-administered with lovastatin, the risk of rhabdomyolysis increases.

Increases the bioavailability of digoxin.

Reduces the effectiveness of hormonal contraception.

Drugs that block tubular secretion, prolong the half-life of erythromycin.

When taken concomitantly with drugs that are metabolized in the liver (carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, disopyramide, lovastatin, bromocriptine), the concentration of these drugs in plasma can be increased (it is an inhibitor of microsomal liver enzymes).

With the simultaneous administration with terfenadine or astemizole, it is possible to develop arrhythmia (scintillation and fluttering of the ventricles, ventricular tachycardia, up to a fatal outcome), with dihydroergotamine or unhydrogenated ergot alkaloids - vasoconstriction to spasm, dysesthesia.

Incompatible with lincomycin, clindamycin and chloramphenicol (antagonism).

Special instructions:

With prolonged therapy, it is necessary to monitor the laboratory parameters of liver function.

Symptoms of cholestatic jaundice can develop a few days after the initiation of therapy, but the risk rises after 7-14 days of continuous therapy.

The likelihood of developing an ototoxic effect is higher in patients with renal and / or hepatic insufficiency, as well as in elderly patients.

Some resistant strains Haemophilus influenzae are sensitive to the simultaneous administration of erythromycin and sulfonamides.

May interfere with the determination of catecholamines in the urine and the activity of "liver" transaminases in the blood (colorimetric determination with diphenylhydrazine).

Form release / dosage:Lyophilizate for the preparation of a solution for intravenous administration, 100 mg and 200 mg.

Packaging:

100 mg of the preparation in 10 ml vials; 200 mg - in bottles with a capacity of 20 ml.

1, 5 or 10 bottles with instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000664 / 01

Date of registration:01.10.2007

The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp30.09.2015

Illustrated instructions

Instructions

Erythromycin (Erythromycin)