Erythromycin

General characteristics. Structure:

Active agent: erythromycin (in terms of active agent) - 500 mg. Excipients: one thousand povidone-12,6 (polyvinylpirrolidone low-molecular medical 12600 ± 2700) - 18,9 mg, кросповидон (коллидон TsL, коллидон CL-M) - 27,0 mg, calcium stearate - 8,28 mg, polysorbate 80 (twin-80) - 0,18 mg, talc - 20,7 mg, potato starch - 324,94 mg. Structure of a cover: целлацефат (atsetilftaliltsellyuloza) - 32,4 mg, titanium dioxide (titanium dioxide) - 1,6 mg, castor-bean trees ordinary seeds oil (castor oil) - 6,0 mg.

Pharmacological properties:

Pharmacodynamics. A 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, to moderately sensitive - 1-6 mg/l, to steady - more than 6 mg/l belong to sensitive. The wide range of antimicrobic effect of erythromycin includes: gram-positive microorganisms: Staphylococcus spp., the producing and not producing penicillinases, including Staphylococcus aureus (except strains, resistant to Methicillinum - MRSA); Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. viridans groups); Bacillus anthracis, Corynebacterium diphtheriae, Corynebacterium minutissimum, Listeria monocytogenes; gram-negative microorganisms: Bordetella pertussis, Campylobacter jejuni, Legionella spp. (including Legionella pneumophila), Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae; Haemophilus influenzae (some strains can be steady against erythromycin, but are sensitive to other makrolidny antibiotics); other microorganisms: Chlamydia spp. (including Chlamydia trachomatis), Mycoplasma spp. (including Mycoplasma pneumoniae), Ureaplasma urealyticum, Treponema spp., Propionibacterium acnes, Entamoeba histolytica. Gram-negative sticks are steady against erythromycin: Escherichia coli and other representatives of the Enterobacteriaceae family (Klebsiella spp., Proteus spp., Salmonella spp., Shigella spp. and others); Pseudomonas aeruginosa; Acinetobacter spp. and other nonfermentative bacteriums, and also anaerobic bacteria (Bacteroides spp., including Bacteroides fragilis), metitsillinrezistentny strains of Staphylococcus aureus (MRSA) and enterococci of Enterococcus spp., mycobacteria. Is an agonist of receptors of a motilin. Accelerates evacuation of gastric contents due to increase in amplitude of reduction of the gatekeeper and improvement of antral and duodenal coordination, has pro-kinetic properties.

Pharmacokinetics. Absorption - high. Meal does not exert impact on the peroral forms of erythromycin in the form of the basis covered with a film kishechnorastvorimy cover. Time of achievement of the maximum concentration in a blood plasma after reception of tablets inside - 2-4 h, communication with proteins - 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 of erythromycin 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 (GEB), into cerebrospinal fluid (SMZh) (concentration makes 10% of the content of erythromycin in plasma). At inflammatory processes their permeability for erythromycin increases in brain covers a little. Gets through a placental barrier and comes to fruit blood where its contents reaches 5-20% of content in mother's plasma. 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 erythromycin. An elimination half-life (T1/2) - 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 intake - 2-5%.

Indications to use:

The bacterial infections caused by activators, sensitive to erythromycin: - infections of ENT organs (laryngitis, pharyngitis, tonsillitis, sinusitis, outside and average otitises); - lower respiratory tract infections (tracheitis, bronchitis, pneumonia); - infections of skin and soft tissues (pustulous diseases of skin, including contaminated wounds, decubituses, burns of the II-III Art., trophic ulcers); - infections of biliary tract (cholecystitis); - 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); - gonorrhea; - scarlet fever, legionellosis (disease of legionaries), listeriosis, trachoma; Prevention of exacerbations of a streptococcal infection (tonsillitis, pharyngitis) at patients with rheumatism. Prevention of an infectious endocarditis at dental interventions and ENT organs operations at patients with risk factors (heart diseases, the fitted a prosthesis valves, etc.). Erythromycin is a reserve antibiotic at an allergy to penicillin and other antibiotics of group of penicillin, and also to other beta lactams.

Route of administration and doses:

Inside. To take a pill in 1-2 hours prior to food or in 2-3 hours after food. Tablets cannot be divided and chewed. Adults and teenagers are more senior than 14 years: usual doses at the majority of infections: a single dose - 500 mg, a daily dose - 1000-2000 mg (1-2 g). Erythromycin 4 times a day accept, an interval between receptions - 6 hours. At a daily dose of erythromycin no more than 1 g/days - are possible administration of drug 2 times a day (on 500 mg each 12 hours). At heavy infections the daily dose of erythromycin can be increased to 4 g (4000 mg). The maximum daily dose of erythromycin for the adult - 4 g (4000 mg). Course of treatment - 5-14 days, after disappearance of symptoms continue treatment within 2 days. Treatment of streptococcal infections of various localization (including a tonzillofaringita) - has to continue not less than 10 days. At urinogenital chlamydial infections during pregnancy - on 500 mg 4 times a day within not less than 7 days or (at bad portability of such dose) - on 500 mg 2 times a day in 12 hours within not less than 14 days. At uncomplicated clamidiosis (urethral, endocervical or rectal) at intolerance of tetracycline antibiotics - the adult on 500 mg 4 times a day within not less than 7 days. Treatment of primary syphilis - the course dose is equal to 30-40 g treatment duration - 10-15 days, frequency rate of reception - 4 times a day. It is more preferable to begin treatment with intravenous administration, with the subsequent transition to peroral forms. At gonorrhea - on 500 mg of each 6 h within 3 days, further on 500 mg each 12 h within 7 days. At scarlet fever - in usual doses, a course of treatment - not less than 10 days. At legionellosis (a disease of legionaries) - in the daily dose of 2-4 g/days divided into 4 receptions (on 500-1000 mg 4 times a day) before disappearance of clinical symptomatology of a disease (but not less than 14 days). At listeriosis - on 500 mg 2-4 times a day not less than 7 days, causal treatment is carried out till 6-7th day of normal temperature, and at severe forms - up to 14-21st day. Prevention of exacerbations of a streptococcal infection (tonsillitis, pharyngitis) at patients with rheumatism of adults - on 500 mg 2-4 times a day, course duration - not less than 10 days. Prevention of an infectious endocarditis at patients with heart diseases at dental interventions and ENT organs operations - the adult on 1 g (1000 mg) for 1-2 h prior to a medical or diagnostic procedure, further on 500 mg each 6 h, only 8 receptions.

Features of use:

At long therapy it is necessary to exercise control of laboratory indicators of function of a liver. Symptoms of cholestatic jaundice can develop in several days after the beginning of therapy, however the risk of development increases after 7-14 days of continuous therapy. The probability of development of ototoksichesky effect is higher at patients with a renal and/or liver failure, and also at elderly patients. Can interfere with definition of catecholamines in urine and activity of "hepatic" transaminases in blood (colorimetric definition by means of a definilgidrazin). It is impossible to wash down with milk or dairy products. In numerous clinical trials the antral and duodenal pro-kinetic effect of erythromycin was proved. Use of drug does not exert impact on control of vehicles and on service of the cars and mechanisms demanding concentration of attention.

Side effects:

Allergic reactions: small tortoiseshell, other forms of skin rash, eosinophilia, acute anaphylaxis. From the alimentary system: nausea, vomiting, gastralgia, abdominal pain, tenesmus, diarrhea, dysbacteriosis, oral cavity candidiasis, pseudomembranous colitis, abnormal liver function, cholestatic jaundice, increase in activity of "hepatic" transaminases, pancreatitis. From an acoustic organ: ototoxicity - decrease in hearing and/or a sonitus (at use in high doses - more than 4 g/days, are usually reversible). From cardiovascular system: tachycardia, lengthening of an interval of Q-T on the electrocardiogram, blinking and/or an atrial flutter (patients with the extended interval have Q-T on the electrocardiogram). If any of the side effects specified in the instruction are aggravated, or you noticed any other side effects which are not specified in the instruction, report about it to the doctor.

Interaction with other medicines:

Reduces bactericidal action beta лактамных antibiotics (penicillin, cephalosporins, karbapenema). Increases concentration of theophylline.
Increases nephrotoxicity of cyclosporine (especially at patients with the accompanying renal failure).
Reduces clearance of a triazolam and midazolam in this connection can strengthen pharmacological effects of benzodiazepines.
Slows down elimination (strengthens effect) Methylprednisolonum, a felodipin and anticoagulants of a coumarinic row.
At combined use with lovastatiny the risk of development of a rabdomioliz increases.
Increases bioavailability of digoxin.
Reduces efficiency of hormonal contraception.
The Medicines (M) blocking canalicular secretion extend erythromycin T1/2.
At combined use with HP which metabolism is carried out in a liver by system of P450 cytochrome (carbamazepine, valproic acid, hexobarbital, Phenytoinum, alfentanil, Disopyramidum, ловастатин, Bromocriptinum) concentration of these HP in plasma can increase (as erythromycin is inhibitor of microsomal enzymes of a liver).
At combined use with terfenadiny or astemizoly development of arrhythmia (blinking and trembling of ventricles, ventricular tachycardia is possible, up to death), with dihydroergotamine or not hydrogenated ergot alkaloids - vasoconstriction up to a full spasm, a dizesteziya.
If you accept other drugs, it is necessary to consult with the doctor.

Contraindications:

Hypersensitivity to erythromycin, other components of drug and other macroleads; considerable decrease in hearing; a concomitant use of a terfenadin, an astemizol, Pimozidum, ergotamine, dihydroergotamine, children's age up to 14 years, the breastfeeding period. 
Use at pregnancy Use of erythromycin at pregnancy is possible only in that case when the expected advantage for mother exceeds potential risk for a fruit. In the period of a lactation in connection with a possibility of penetration into breast milk it is necessary to refrain from feeding by a breast at erythromycin use.

Overdose:

Symptoms: the abnormal liver function, up to an acute liver failure, is rare a hearing disorder.
Treatment: absorbent carbon, careful control of a condition of respiratory system (if necessary - carrying out artificial ventilation of the lungs), an acid-base state and electrolytic exchange, the electrocardiogram.
The gastric lavage is effective at reception of the dose fivefold exceeding average therapeutic.
The hemodialysis, peritoneal dialysis and artificial diuresis are inefficient.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the places unavailable to children. 
Period of validity 3 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

10 pieces - planimetric strip packagings (1) - packs cardboard
10 pieces - planimetric strip packagings (2) - packs cardboard