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

It binds to the 50S-subunit of ribosomes and blocks the synthesis of proteins of sensitive microbial cells, as it disrupts the process of translocation and formation of peptide bonds between amino acid molecules. It penetrates into cells and creates a high intracellular concentration. Has a bacteriostatic effect, in high concentrations can have a bactericidal effect.

The spectrum of action includes Gram-positive (Staphylococcus spp., producing and not producing penicillinase, including Staphylococcus aureus, Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes), alpha-hemolytic streptococcus (groups Viridans), Bacillus anthracis, 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. (at including Mycoplasma pneumoniae), Chlamydia spp. (at including Chlamydia trachomatis), Treponema spp., Rickettsia spp., Entamoeba histolytica, Listeria monocytogenes.

Sustainable gram-negative sticks: Escherichia coli, Pseudomonas aeruginosa, a also Shigella spp., Salmonella spp. and others.

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.

Pharmacokinetics:

Nestoek in an acidic environment, therefore, is used in the form of coated tablets. Well absorbed from the digestive tract; gastric contents slow the absorption process. FROM_max in blood plasma is achieved after 1.5-3 hours after ingestion and 20 minutes after intravenous administration. Connection with proteins plasma is 79-90%. 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 tens of times higher than the concentration in the 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. In the milk of lactating women, 50% of the plasma concentrations are contained. Poorly penetrates the blood-brain barrier. 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.

Undergoes biotransformation in the liver (more than 90%) with the formation of inactive metabolites. Half-life is 1.4-2 hours, with anuria 4-6 hours. Excreted mainly with bile (20-30% unchanged) and 2-8% of the kidneys.

Indications:

Streptococcal, staphylococcal and mycoplasmal infections, angina, acute sinusitis, pneumonia, legionnaires' disease, endocarditis, enteritis, osteomyelitis, chlamydia, syphilis.

ICD-10

I.A30-A49.A36.9 Diphtheria, unspecified

I.A30-A49.A38 Scarlet fever

I.A30-A49.A41.9 Septicemia, unspecified

I.A30-A49.A49.0 Staphylococcal infection, unspecified

I.A30-A49.A49.1 Streptococcal infection, unspecified

I.A30-A49.A49.3 Infection caused by mycoplasma, unspecified

X.J00-J06.J03.9 Acute tonsillitis, unspecified

X.J10-J18.J18 Pneumonia without clarification of the pathogen

X.J40-J47.J47 Bronchoectasia

XII.L00-L08.L08.0 Pyoderma

Contraindications:

Hepatic or renal failure, individual intolerance.

Carefully:

Dysfunction of the liver, obstruction of the bile duct, arrhythmia (in the anamnesis), lengthening of the interval PQ, lactation period.

Pregnancy and lactation:

Recommendations for FDA - Category B.

Not recommended. Use in pregnant and lactating women only if the expected benefit exceeds potential harm.In connection with the possibility of penetration into breast milk, it is necessary to refrain from breast-feeding while treating erythromycin.

Dosing and Administration:

Inside for 1 hour before meals. Adults on 200-400 mg 4 times a day every 6 hours, if necessary, increase the dose to 4 g per day; children: 30-40 mg / kg per day, in 2-4 admission.

Outwardly, on the affected skin 2 times a day, with eye diseases ointment is placed in the lower or upper eyelid 3-5 times a day.

Side effects:

Nausea, vomiting, diarrhea, candidiasis of the mucous membranes of the gastrointestinal tract, vagina. Allergic reactions.

Overdose:

Symptoms: violations of liver function up to acute liver failure, hearing loss.

Treatment is symptomatic.

Interaction:

Incompatible with lincomycin, clindamycin and chloramphenicol (antagonism). Reduces the bactericidal action of beta-lactam antibiotics (penicillins, cephalosporins, carbapenems).

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

It is an inhibitor of microsomal liver enzymes, so it can increase the concentration in the blood of drugs whose biotransformation carried out in the liver (carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, disopyramide, lovastatin, bromocriptine).

Increases the nephrotoxicity of cyclosporine (especially in patients with concomitant renal failure). Reduces the clearance of triazolam and midazolam, and therefore can enhance the pharmacological effects of benzodiazepines.

When taken concomitantly with terfenadine or astemizole - the possibility of arrhythmia (scintillation and fluttering of the ventricles, ventricular tachycardia, up to the fatal outcome), with dihydroergotamine or unhydrogenated ergot alkaloids - narrowing of the vessels to spasm, dysesthesia.

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

With a joint appointment with lovastatin increases rhabdomyolysis.

Reduces the effectiveness of hormonal contraception.

Special instructions:

Before the application of erythromycin, it is necessary to determine the sensitivity of the isolated pathogen to the antibiotic.Treatment can begin before the results of the antibioticogram.Esli antibioticogram does not confirm the sensitivity of the selected pathogen to erythromycin, the replacement of the drug

There are no data on the negative effect of the drug on the ability to drive vehicles and maintain moving mechanical devices.

The probability of development of ototoxic effect is higher in patients with renal and hepatic insufficiency, and in old age.

Instructions

Erythromycin (Erythromycinum)