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

core composition: active substance: erythromycin 117.0 mg or 292.4 mg (based on the active substance) 100.0 mg or 250.0 mg; Excipients: lactose monohydrate-30.0 mg or 67.5 mg; povidone K17 5.0 mg or 11.2 mg; polysorbate-80 - 4.0 mg or 9.0 mg; magnesium stearate 2.0 mg or 4.5 mg; potato starch to obtain a core tablet with a mass of 200.0 mg or 450.0 mg;

shell composition: Excipients: copolymer of methacrylic acid and ethylacridate [1: 1] - 5.7 mg or 13.5 mg; titanium dioxide - 1.8 mg or 3.3 mg; talc - 3.3 mg or 7.6 mg; Macrogol-4000 - 1.2 mg or 2.6 mg.

Description:

Tablets are white or white with a grayish shade of color, biconvex form.

Pharmacotherapeutic group:antibiotic-macrolide

ATX: & nbsp

S.01.A.A.17 Erythromycin

J.01.F.A.01 Erythromycin

Pharmacodynamics:

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 - more than 6 mg / l.

The spectrum of action includes Gram-positive microorganisms: Staphylococcus spp., producing and non-producing penicillinase, including Staphylococcus aureus; Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes), Streptococcus spp. groups viridans, Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium minutissimum;

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

The drug is stable gram-negative rods: Escherichia coli (and other members of the family Enterobacteriaceae), Pseudomonas aeruginosa and Acinetobacter spp. and other non-fermenting bacteria, as well as anaerobic bacteria (Bacteroides spp.), including Bacteroides fragilis.

Is a receptor agonist motilin. Accelerates the evacuation of gastric contents by increasing the amplitude of contraction of the pylorus and improving the antral-duodenal coordination, possesses prokinetic properties.

Pharmacokinetics:

Absorption is high. The ingestion of food does not affect the absorption of oral forms of erythromycin in the form of a base, covered with a film intestine-soluble membrane.

Time to reach the maximum concentration in the blood plasma after taking the tablets inside - 2-4 hours, the connection with plasma proteins - 70-90%. Bioavailability - 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, ascites and synovial fluid. The milk of lactating women contains 50% of the concentration in the plasma. Poorly penetrates the blood-brain barrier (BBB), into the cerebrospinal fluid (CSF) (the concentration is 10% of the erythromycin content in the plasma). In inflammatory processes in the membranes of the brain, their permeability for erythromycin increases somewhat. 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.

Metabolised in the liver (more than 90%), partially with the formation of inactive metabolites. In the metabolism of erythromycin, isozymes participate CYP3A4, CYP3A5 and CYP3A7, the inhibitor of which it is.The half-life (T_1/2) - 1,4-2 hours, with anuria 4-6 hours. Excretion with bile - 20-30% unchanged, kidney (unchanged) after ingestion - 2-5%.

Indications:

Bacterial infections caused by susceptible pathogens: diphtheria (including bacteriocarrier), whooping cough (including prophylaxis), trachoma, brucellosis, erythrasma, listeriosis, scarlet fever, amoebic dysentery, gonorrhea; genitourinary infections in pregnant women caused by Chlamydia trachomatis; primary syphilis (in patients with penicillin allergy), uncomplicated chlamydia in adults (with localization in the lower sections of the urogenital tract and rectum) with intolerance or inefficiency of tetracyclines, etc .; infection of the ENT organs (tonsillitis, otitis media, sinusitis); bile duct infection (cholecystitis); infections of the upper and lower respiratory tract (tracheitis, bronchitis, pneumonia, including caused by Legionella spp.).

Prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with rheumatism.

Prophylaxis of infective endocarditis in dental interventions in patients with risk factors (heart defects, prosthetic valves, etc.).

It is an antibiotic reserve for allergies to penicillin.

Contraindications:

Hypersensitivity, significant hearing loss, simultaneous reception of terfenadine or astemizole, children under 14 years old, the period of breastfeeding.

Simultaneous administration of pimozide, cisapride.

Carefully:

Arrhythmias (in the anamnesis), lengthening of the interval Q-T, jaundice, including history, hepatic and / or renal insufficiency.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the expected benefit for the mother exceeds the potential risk to the fetus and the baby.

During lactation due to the possibility of penetration into breast milk, one should refrain from breastfeeding while prescribing erythromycin.

Dosing and Administration:

Inside. The tablet can not be divided and chewed.

The dose depends on clinical and microbiological studies, as well as on the general condition of the patient.

The average single dose for adults and adolescents over the age of 14 is 0.25-0.5 g, the average daily intake is 1-2 g. The interval between doses is 6 h. In severe infections, the daily dose can be increased to 4 g.

For the treatment of diphtheria carriage - 0.25 g 2 times a day. Erythromycin it is necessary to take at least 2-3 days after the disappearance of the symptoms of the disease.

The course dose for the treatment of primary syphilis (in patients with an allergy to penicillins) is 30-40 g, the duration of treatment is 10-15 days. Treatment for this indication begins with intravenous administration of the drug, and then switch to oral forms.

With amoebic dysentery - 0.25 g 4 times a day, the duration of treatment - 10-14 days.

For the treatment of infections of the upper and lower respiratory tract (tracheitis, bronchitis, including caused by Legionella spp.) - 0.5-1 g 4 times a day for 14 days.

With gonorrhea - 0.5 g every 6 hours for 3 days, then 0.25 g every 6 hours for 7 days.

In uncomplicated chlamydia in adults (with localization in the lower sections of the urogenital tract and rectum) with intolerance or

inefficiency of tetracyclines, etc. - 0.5 g 4 times a day for at least 7 days.

For the prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with rheumatism - 0.25-0.5 g 4 times a day, the course duration - not less than 10 days.

For the prevention of infectious endocarditis in dental interventions in patients with risk factors (heart defects, prosthetic valves, etc.) - 1 g per hour before the therapeutic or diagnostic procedure,then 0.5 g, again after 6 hours.

For the rest of the indications, the recommended single dose is 0.25-0.5 g, the daily dose is 1-2 g. The interval between doses is 6 hours. Erythromycin it is necessary to take at least 2-3 days after the disappearance of the symptoms of the disease.

Side effects:

From the digestive system: nausea, vomiting, gastralgia, abdominal pain, tenesmus, diarrhea, dysbacteriosis, candidiasis of the oral mucosa, pseudomembranous colitis, impaired liver function, cholestatic jaundice, increased activity of "liver" transaminases, pancreatitis.

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

From the cardiovascular system: tachycardia, lengthening interval Q-T on an electrocardiogram, flicker and / or atrial flutter (in patients with an elongated interval Q-T on an electrocardiogram); Ventricular arrhythmias, including ventricular tachycardia and torsade des pointes (syndrome of an elongated interval Q-T).

From the nervous system: convulsions.

Allergic reactions: urticaria, other forms of skin rash (erythema multiforme, Stevens-Johnson syndrome, Lyell syndrome), eosinophilia, anaphylactic shock.

Overdose:

Symptoms: a violation of the liver, up to acute liver failure, rarely - hearing impairment.

Treatment: Activated carbon, careful monitoring of the condition respiratory system (if necessary - carrying out artificial ventilation legrams), acid-base state and electrolyte balance, electrocardiogram.

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:

Reduces the bactericidal action of beta-lactam antibiotics

(penicillins, cephalosporins, carbapenems).

Incompatible with lincomycin, clindamycin and chloramphenicol (antagonism).

Increases the concentration of theophylline in the blood.

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

Reduces the clearance of triazolam and midazolam, in connection with what may enhance the pharmacological effects of benzodiazepines.

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

When combined with lovastatin and other inhibitors of HMG-CoA reductase is increasedrisk of rhabdomyolysis.

Increases the bioavailability of digoxin.

Reduces the effectiveness of hormonal contraception.

Drugs (drugs), blocking tubular secretion, extend T_1/2 erythromycin.

As erythromycin is an inhibitor of isoenzymes and a substrate CYP3A, then with simultaneous admission with drugs, the metabolism of which is carried out in the liver (carbamazepine, valproic acid, hexobarbital, phenytoin, alfetanyl, disopyramide, lovastatin, bromocriptine), the concentration of these drugs in the plasma can increase.

With the simultaneous reception with terfenadine or astemizole, the development of arrhythmia (scintillation and fluttering of the ventricles, ventricular tachycardia, up to a fatal outcome), with dihydroergotamine or dihydrated ergot alkaloids - vasoconstriction to spasm, dysesthesia.

Simultaneous reception of erythromycin with sildenafil can lead to a moderate increase in the maximum concentration of sildenafil in the blood.

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 start of 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 / or hepatic insufficiency, as well as in elderly patients.

May interfere with the determination of catecholamine content in the urine and the activity of "hepatic" transaminases in the blood (colorimetric determination with the help of de-nylhydrazine).

Do not drink milk or dairy products.

In numerous clinical trials, the antrum and duodenal prokinetic effect of erythromycin was demonstrated.

Effect on the ability to drive transp. cf. and fur:During treatment, care should be taken when driving a car and when engaging in other potentially hazardous activities requiring special attention and quick reactions.

Form release / dosage:

Intestine-soluble tablets shell, 100 mg or 250 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 20 tablets in a jar of polymer materials.

2 contour mesh packages with instructions for medical use are placed in a pack of cardboard.

100 cans of polymer materials with an equal number of instructions for medical use are placed in a group package (for hospitals).

Storage conditions:

Store in a dry place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:PL-000211

Date of registration:15.02.2011

Date of cancellation:2016-02-15

The owner of the registration certificate:AVEKSIMA, JSC AVEKSIMA, JSC Russia

Manufacturer: & nbsp

IRBITSK HFZ, OJSC Russia

Information update date: & nbsp29.09.2015

Illustrated instructions

Instructions

Erythromycin (Erythromycin)