Ertapenem - instructions for use, doses, side effects, contraindications

Clinical and pharmacological group: & nbsp

Antibiotics

Included in the formulation

Invenza®

lyophilizate for injections

Merck Sharp and Dohm-Shibre Laboratories France

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

АТХ:

J.01.D.H Carbapenems

J.01.D.H.03 Ertapenem

Pharmacodynamics:

The antibiotic from the carbapenem group is 1-β methyl carbapenem, a long-acting beta-lactam antibiotic for parenteral administration. Has a bactericidal effect due to inhibition of bacterial cell wall synthesis and binding to penicillin-binding proteins. Violates the synthesis of peptidoglycan-biopolymer - the main component of the cell wall of bacteria. Inhibits the peptidoglycan trespeptidase, inhibits the activity of the endogenous inhibitor, which leads to activation of murein hydrolase, which cleaves peptidoglycan. Effective against fissile bacteria, in the walls of which the synthesis of peptidoglycan occurs.

Has a wide range of antibacterial action. Has a bactericidal effect against gram-negative bacteria: Acinetobacter spp., Moraxella catarrhalis, Citrobacter spp. (including Citrobacter freundii, Citrobacter diversus, Citrobacter amalonaticas), Enterobacter spp., Escherichia coli, Haemophilus influenzae, Klebsiella spp. (including Klebsiella pneumoniae), Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Pseudomonas spp. (at tth number Pseudomonas aeruginosa, Pseudomonas maltophila), Salmonella spp., Serratia spp. (including Serratia marcescens); and gram-positive bacteria: Staphylococcus aureus, Staphylococcus epidermidis (coagulase-negative strains), Staphylococcus saprophyticus, Streptococcus agalactiae (group B), Streptococcus bovis, Enterococcus faecalis, Streptococcus pneumoniae, Streptococcus pyogenes (group A, beta-hemolytic), Streptococcus viridans; anaerobic bacteria: Bacteroides spp., including Bacteroides fragilis group (Bacteroides fragilis, Bacteroides vulgatus, Bacteroides thetaiotaomicronron, Bacteroides ovatus, Bacteroides distasonis), and non-Bacteroides fragilis (beta-melanogenic), Clostridium spp. (including Clostridium perfiingens, Clostridium difficile, Clostridium sporogenes, Clostridium ramosum, Clostridium bifermentans), Eubacterium spp., Fusobacterium spp. (including Fusobacterium nucleatum and Fusobacterium necrophorum), Peptococcus spp., Peptostreptococcus spp., Veillonella spp.

Resistant to the action of most β-lactamases (penicillinase, cephalosporinase and extended-spectrum β-lactamase, except for metal-β-lactamases).

Pharmacokinetics:

After intramuscular injection is well absorbed, bioavailability is about 92%, the maximum concentrationin blood plasma is achieved after 2 hours. The connection with plasma proteins is 95%. About 6% undergoes biotransformation in the liver with the formation of an inactive metabolite. About 80% is excreted by the kidneys (38% - unchanged, about 37% - in the form of a metabolite), 10% - through the intestine. Half-lifeis 4 hours.

Indications:

It is used to treat infectious diseases caused by pathogens that are sensitive to the drug: septicemia, peritonitis, urinary tract infections.

Severe and moderate infections caused by susceptible strains of microorganisms: bone and connective tissue, skin and subcutaneous tissue, lower respiratory tract, community acquired pneumonia, urinary tract infections, acute pelvic infection, bacterial septicemia.

ICD-10

I.A30-A49.A40 Streptococcal septicemia

I.A30-A49.A41 Other septicemia

X.J10-J18.J15 Bacterial pneumonia, not elsewhere classified

X.J40-J47.J42 Chronic bronchitis, unspecified

X.J20-J22.J20 Acute bronchitis

XI.K65-K67.K65.0 Acute peritonitis

XI.K80-K87.K81.0 Acute cholecystitis

XI.K80-K87.K81.1 Chronic cholecystitis

XI.K80-K87.K83.0 Cholangitis

XII.L00-L08.L01 Impetigo

XII.L00-L08.L02 Abscess of skin, boil and carbuncle

XII.L00-L08.L03 Phlegmon

XII.L00-L08.L08.0 Pyoderma

XIII.M00-M03.M00 Pyogenic arthritis

XIII.M86-M90.M86 Osteomyelitis

XIV.N10-N16.N11.9 Chronic tubulointerstitial nephritis, unspecified

XIV.N10-N16.N10 Acute tubulointerstitial nephritis

XIV.N10-N16.N15.1 Abscess of kidney and adrenal tissue

XIV.N30-N39.N30 Cystitis

XIV.N30-N39.N34 Urethritis and urethral syndrome

XIV.N40-N51.N41 Inflammatory diseases of the prostate

XIV.N70-N77.N70 Salpingitis and oophoritis

XIV.N70-N77.N71 Inflammatory diseases of the uterus, except the cervix

XXI.Z20-Z29.Z29.2 Another type of preventive chemotherapy

Contraindications:

Hypersensitivity (including other β-lactam antibiotics), Children's age is up to 3 months. When using lidocaine hydrochloride as a solvent for intramuscular injection: hypersensitivity to amide local anesthetics,severe arterial hypotension, violation of intracardiac conduction.

Carefully:

Pregnancy, lactation.

Pregnancy and lactation:

Recommendations for FDA - Category B. It is used in pregnancy and lactation.

Dosing and Administration:

Use in children

Intramuscularly on a 1-2% solution of lidocaine with a preliminary skin test for tolerability.

At the age of 3 months to 12 years: 15 mg / kg per day in 2 admission (but not more than 1 g per day).

Children over 12 years: 1 g 1 time per day.

Dosing and Administration

Intramuscularly (1-2% solution of lidocaine), intravenously drip (for 30 minutes) 1 g per day once.

Side effects:

Frequent (1-10%): headache, postinfusion phlebitis / thrombophlebitis, diarrhea, nausea, vomiting.

Rare (0.1-1%): dizziness, weakness / fatigue, drowsiness, insomnia, convulsions, confusion; a decrease in blood pressure; dyspnea; Candidiasis of the oral mucosa, pseudomembranous colitis caused by Clostridium difficile (often manifested by diarrhea), dry mouth, indigestion (including constipation, belching of acid contents), anorexia, abdominal pain, perversion of taste; skin rash, itching of the skin; vaginal candidiasis (vaginal itching), swelling, fever, chest pain.

Allergic and anaphylactic reactions (more often in people who have a history of polyvalent allergies, including penicillin and others β-lactam antibiotics), superinfection.

Changes in laboratory indicators (often - increased activity of ALT, ACT, alkaline phosphatase and thrombocytosis), less often - increased direct, indirect and total bilirubin, partial thromboplastin time, eosinophilia, monocytosis, hypercreatininaemia and hyperglycemia; reduction in the number of segmented neutrophils and leukopenia, a decrease in hematocrit and hemoglobin, thrombocytopenia; bacteriuria, increased urea nitrogen in the serum, epithelial cells in the urine, erythrocyturia.

Overdose:

Symptoms: nausea, vomiting, diarrhea, neuromuscular excitability, convulsive attacks.

Treatment: symptomatic, hemodialysis.

Interaction:

Do not use in solutions containing dextrose.

When co-administered with drugs that block tubular secretion, correction of the dosing regimen is not required.

Does not affect the metabolism of xenobiotics, mediated by six major isoenzymes of cytochrome P450: CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4.

Special instructions:

Before applying ertapenem, a skin test is required for sensitivity in view of the high likelihood of polyvalent allergy in persons with hypersensitivity to penicillins and cephalosporins.

When intramuscular introduction, it is necessary to avoid accidental insertion into a blood vessel.

Possible development of pseudomembranous colitis, the severity of which can vary from mild to life-threatening, so it is necessary to keep in mind the possibility of its development in patients with diarrhea.

Instructions

Ertapenem (Ertapenemum)