Erythromycin phosphate powder lyophilisate injection vial 100mg N1
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Active ingredients
Erythromycin
Release form
Lyophilisate
Composition
1 bottle contains: Active substance: erythromycin phosphate (in terms of erythromycin) - 100 mg.
Pharmacological effect
An antibiotic group macrolides. It has a bacteriostatic effect. However, in high doses in relation to sensitive microorganisms has a bactericidal effect. Erythromycin reversibly binds to the ribosomes of bacteria, thereby inhibiting protein synthesis. Active against gram-positive bacteria: Staphylococcus spp. (strains producing and not producing penicillinase), Streptococcus spp. (including Streptococcus pneumoniae); Gram-negative bacteria: Neisseria gonorrhoeae, Haemophilus influenzae, Bordetella pertussis, Brucella spp., Legionella spp., Bacillus anthracis, Corynebacterium diphtheriae; anaerobic bacteria: Clostridium spp. Erythromycin is also active against Mycoplasma spp., Chlamydia spp., Spirochaetaceae, Rickettsia spp. Gram-negative rods are resistant to erythromycin, including Escherichia coli, Pseudomonas aeruginosa, Shigella spp., Salmonella spp.
Pharmacokinetics
Reversibly binding to the 50S subunit of ribosomes in its donor part, it blocks the synthesis of proteins of sensitive microbial cells, since violates the process of translocation and the formation of peptide bonds between amino acid molecules. It is well absorbed from the gastrointestinal tract, gastric contents and acidic medium slow down the absorption process. Cmax is 0.8–4 mcg / ml and is reached 2–3 hours after enteral and 20 minutes after i.v. Communication with plasma proteins is variable. It penetrates well into the body cavities (in pleural, peritoneal and synovial fluids, the concentration is 15–30% of that in the blood), and in muscle tissue, prostate gland and seminal fluid is detected in concentrations equal to plasma. Diffuses into poorly supplied organs and tissues (the concentration in the middle ear is 50% of that found in the blood). Through intact BBB practically does not penetrate; passes through the placental barrier and is secreted into breast milk. T1 / 2 is 1–1.2 hours. It is subjected to biotransformation in the liver with the formation of inactive metabolites. Excreted mainly with bile, with 20–30% in active form and 2–8% in urine. With the on / in the introduction of urine displays up to 12-15%.
Indications
Severe forms of bacterial infections caused by susceptible pathogens: diphtheria (including bacteriocarrier), whooping cough, trachoma, brucellosis, legionnaires' disease, erythrasma, listeriosis, scarlet fever, amebic dysentery, gonorrhea, urinary infections in pregnant women,caused by Chlamydia trachomatis; Primary syphilis (in patients allergic to penicillins); Infections of the upper respiratory tract (tonsillitis, otitis, sinusitis); Biliary tract infections (cholecystitis); Infections of the upper and lower respiratory tract (tracheitis, bronchitis, pneumonia); infections of skin and soft tissues (infected wounds, bedsores, II-III burns, trophic ulcers). Prevention of infectious complications during therapeutic and diagnostic procedures (including preoperative preparation of the intestine, dental interventions, endoscopy) in patients with heart defects .Gastroparesis (including gastroparesis after vagotomy surgery, diabetic gastroparesis and gastroparesis associated with progressive systemic sclerosis)
Contraindications
Hypersensitivity to erythromycin, other components of the drug and other macrolides; significant hearing loss; Simultaneous use of terfenadine, astemizole, pimozide, ergotamine, dihydroergotamine, Children's age up to 14 years, breastfeeding period.
Precautionary measures
The use of erythromycin containing benzene for intravenous injection has sometimes been accompanied by the development of fatal Gasping syndrome in children, as well as acute drug hepatitis in adults and children.
Use during pregnancy and lactation
The use of the drug during pregnancy is possible in the case when the intended benefit to the mother outweighs the potential risk to the fetus. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.
Dosage and administration
Intravenously slowly (within 3-5 minutes) or drip. Preferably, and more safely, intravenous drip. A single dose of the drug for adults is 0.2 g, daily - 0.6 g. In case of 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 age, body weight and severity of infection, 30-50 microns / kg / day (for 2-4 injections); children of the first 3 months of life - 20-40 microns / kg / day. In case of severe infections, the dose may be doubled. For intravenous injection, the drug is dissolved in water for injection or 0.9% sodium chloride solution at the rate of 5 mg per 1 ml of solvent.For intravenous drip, dissolved in 0.9% sodium chloride solution or 5% dextrose solution to a concentration of 1 mg / ml and injected at a rate of 60-80 drops / minute. Intravenous administered for 5-6 days (before the onset of a distinct therapeutic effect) with the subsequent transition to oral administration. With good tolerance and the absence of phlebitis and periphlebitis, the course of intravenous administration can be extended to 2 weeks (no more). In case of renal failure there is no need to adjust the dose of the drug.
Side effects
On the part of the gastrointestinal tract: nausea, vomiting, gastralgia, abdominal pain, tenesmus, diarrhea, dysbacteriosis, rarely - oral candidiasis, pseudomembranous enterocolitis, abnormal liver function, cholestatic jaundice, increased activity of hepatic transaminases, pancreatitis. In newborns receiving erythromycin, high risk of pyloric stenosis. On the part of the 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, prolongation of the QT interval on the ECG, flicker and / or atrial flutter (in patients with a prolonged QT interval on an ECG). Allergic reactions: urticaria, skin rash, eosinophilia, rarely anaphylactic shock. Local reactions: phlebitis at the site of intravenous administration.
Overdose
Symptoms: abnormal liver function, up to acute liver failure, and hearing loss. Treatment: gastric lavage, forced diuresis, hemo-and peritoneal dialysis. Constant monitoring of vital functions (ECG, electrolyte composition of blood) is performed.
Interaction with other drugs
Erythromycin is incompatible with lincomycin, clindamycin and chloramphenicol because of the antagonism of the ryhm. (penicillins, cephalosporins, carbapenems). With simultaneous use of Erythromycin with theophylline, the concentration of the latter increases. and simultaneous application of drugs, of which the metabolism in the liver (carbamazepine, valproic acid, hexobarbital, phenytoin, alfentanil, disopyramide, lovastatin, bromocriptine) can increase the concentration of these drugs in plasma, becauseErythromycin is an inhibitor of liver microsomal enzymes. Erythromycin enhances cyclosporine nephrotoxicity (especially in patients with concomitant renal failure). Erythromycin reduces the clearance of triazolam and midazolam, and therefore may enhance the pharmacological effects of these benzodiazepines. vasoconstriction with the development of spasms, dysesthesia. Erythromycin slows down the excretion and enhances the effects of lprednisolone, felodipine and coumarin row anticoagulants. If co-administered with lovastatin, rhabdomyolysis may develop. Erythromycin increases the bioavailability of digoxin and reduces the effectiveness of hormonal contraception.
special instructions
With long-term therapy, it is necessary to monitor the laboratory parameters of liver function. Symptoms of cholestatic jaundice may develop several days after the start of therapy, but the risk of development increases after 7-14 days of continuous therapy. The likelihood of ototoxic effect is higher in patients with renal and / or hepatic insufficiency, as well as in elderly patients. May interfere with the determination of catecholamines in the urine and the activity of hepatic transaminases in the blood (colorimetric determination using definilhydrazine). You can not drink milk or dairy products. In numerous clinical studies, the antral and duodenal prokinetic effect of erythromycin has been proven. The use of the drug does not affect the management of vehicles and the maintenance of machines and mechanisms that require concentration of attention.