Ertapenem J instructions for use of the drug

Pharmacological properties

Pharmacodynamics.
mechanism of action. ertapenem inhibits bacterial cell wall synthesis by binding ertapenem to penicillin binding proteins (PBPs). in escherichia coli it has a very strong degree of binding to psb 2 and 3. Mechanism of resistance. For strains considered susceptible to ertapenem, resistance was infrequently observed during observational studies in Europe. Some of the resistant strains have demonstrated resistance to other antibacterial drugs of the carbapenem class. Ertapenem is resistant to hydrolysis by beta-lactamases, including penicillinases, cephalosporinases and extended-spectrum beta-lactamases, but not metallo-beta-lactamases.

Staphylococci and enterococci resistant to methicillin are resistant to ertapenem due to insensitivity of the target penicillin-binding proteins; P. aeruginosa and other non-fermenting bacteria are usually resistant, probably due to limited penetration and active efflux from the cell.

Resistance from pathogens belonging to the family Enterobacteriaceae is rare, and ertapenem is generally active against extended-spectrum beta-lactamases. However, resistance may occur if extended spectrum beta-lactamases are present or other potent beta-lactamases (eg, AmpC type) exhibit reduced permeability due to loss of one or more outer membrane proteins or have active efflux. Resistance may also result from the acquisition of significant carbapenem hydrolyzing activity by beta-lactamases (particularly metallo-beta-lactamases of the IMP and VIM type or the KPC type), but this is a rare occurrence.

The mechanism of action of ertapenem differs from that of other classes of antibiotics, namely quinolones, aminoglycosides, macrolides and tetracyclines. There is no targeted cross-resistance between ertapenem and these substances. However, microorganisms can suppress resistance to more than one class of antibacterial drugs if the mechanism exhibits or includes the possibility of impermeability to certain compounds and/or the efflux pump.

Limit points. The MIK (microbial inhibitory concentration) breakpoints established by the European Committee on Antimicrobial Susceptibility Testing (EUCAST) are:

• Enterobacteriaceae: sensitive 0.5 mg/l and resistant 1 mg/l;
• Streptococcus groups A, B, C, G: sensitive 0.5 mg/l and resistant 0.5 mg/l;
• Streptococcus pneumoniae: sensitive 0.5 mg/l and resistant 0.5 mg/l;
• Haemophilus influenzae: sensitive 0.5 mg/l and resistant 0.5 mg/l;
• M. catarrhalis: sensitive 0.5 mg/l and resistant 0.5 mg/l;
• anaerobic gram-negative microorganisms: sensitive 1 mg/l and resistant 1 mg/l;
• breakpoints not associated with any strain: sensitive 0.5 mg/L and resistant 1 mg/L.

Note: Staphylococci resistant to methicillin are also resistant to ertapenem.

Local MIK limit points, if any, should also be taken into account.

Sensitivity of microorganisms. The prevalence of acquired resistance in individual species may vary over time and across geographic regions, and information on local resistance patterns is therefore very useful, especially in the treatment of severe infections. Localized outbreaks of infections caused by organisms resistant to carbopenems have been described in the European Union. The information provided below provides only approximate indications of the sensitivity of microorganisms to ertapenem.

Moderately sensitive strains

Aerobic gram-positive microorganisms: methicillin-resistant staphylococci (including Staphylococcus aureus)*, Streptococcus agalactiae*, Streptococcus pneumoniae*,**, Streptococcus pyogenes.

Anaerobic gram-negative microorganisms: Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli*, Haemophilus influenzae*, Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae*, Moraxella catarrhalis*, Morganella morganii, Proteus mirabilis*, Proteus vulgaris, Serratia marcescens .

Anaerobic microorganisms: Bacteroides fragilis and other species of the B. fragilis group*, Clostridium strains (except C. difficile)*, Eubacterium strains*, Fusobacterium strains*, Peptostreptococcus strains*, Porphyromonas asaccharolytica*, Prevotella strains*.

Strains for which acquired resistance may be a problem: methicillin-resistant staphylococci***.

Highly sensitive organisms

Aerobic gram-positive microorganisms: Corynebacterium jeikeium; enterococci, including Enterococcus faecalis and Enterococcus faecium.

Anaerobic gram-negative microorganisms: Aeromonas strains, Acinetobacter strains, Burkholderia cepacia, Pseudomonas aeruginosa, Stenotrophomonas maltophilia.

Anaerobic microorganisms: Lactobacillus strains.

Others: Chlamydia strains, Mycoplasma strains, Rickettsia strains, Legionella strains.

*Satisfactory activity was observed in clinical studies.

**The effectiveness of Invanz for the treatment of community-acquired pneumonia caused by penicillin-sensitive Streptococcus pneumoniae has not been established.

***Frequency of acquired resistance 50%. Methicillin-resistant staphylococci (including MRSA) are always susceptible to beta-lactams.

Efficiency research in pediatric practice. Randomized comparative multicenter studies involving patients aged 3 months to 17 years assessed the safety and effectiveness of ertapenem in pediatric practice.

The ratio of patients who experienced a positive clinical effect after treatment and patients who continued treatment are presented in Table 1.

Table 1

*9 patients in the ertapenem group (7 patients with NPC and 2 patients

Product description certified by the manufacturer Merck Sharp Laboratories and Dome Chibre

.
Verified
Sevryukov Alexander Viktorovich

Release form, packaging and composition of the drug Ertapenem J

Lyophilisate for preparing a solution for intravenous and intramuscular administration

in the form of a lyophilized powder or porous mass of white or yellowish-white color; the reconstituted solution should be clear, colorless or light yellow.

Excipients

: sodium bicarbonate - 203 mg, sodium hydroxide qs to pH 6.5-8.5.

1 g - Colorless glass bottles with a capacity of 20 ml (1) - cardboard packs. 1 g - Colorless glass bottles with a capacity of 20 ml (5) - plastic trays (1) - cardboard packs.

Note!

Description of the drug Invanz Liof. d/r-ra d/in. 1g fl. No. 1 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

Indications for use

Treatment of severe and moderate infectious and inflammatory diseases caused by sensitive strains of microorganisms (including for initial empirical antibacterial therapy until the pathogens are identified): infections of the abdominal cavity; infections of the skin and subcutaneous tissue, including infections of the lower extremities in diabetes mellitus (“diabetic” foot); community-acquired pneumonia; infections of the urinary system (including pyelonephritis); acute infections of the pelvic organs (including postpartum endomyometritis, septic abortion and postoperative gynecological infections); bacterial septicemia.

Side effect

From the side of the central nervous system:

often - headache; rarely - dizziness, drowsiness, insomnia, convulsions, confusion.

From the digestive system:

often - diarrhea, nausea, vomiting;
rarely - candidiasis of the oral mucosa, constipation, belching with sour contents, pseudomembranous colitis (often manifested by diarrhea) caused by uncontrolled proliferation of Clostridium difficile ,
dry mouth, dyspepsia, anorexia.

From the cardiovascular system:

rarely - decreased blood pressure.

From the respiratory system:

rarely - dyspnea.

Dermatological reactions:

often - rash; rarely - erythema, itching.

From the body as a whole:

rarely - abdominal pain, taste disturbance, weakness/fatigue, candidiasis, swelling, fever, chest pain.

Local reactions:

often - post-infusion phlebitis/thrombophlebitis.

From the genital organs

: vaginal itching.

From the laboratory parameters:

often - increased ALT, AST, alkaline phosphatase, increased platelet count; rarely - an increase in direct, indirect and total bilirubin, an increase in the number of eosinophils and monocytes, an increase in partial thromboplastin time, creatinine and blood glucose levels, a decrease in the number of segmented neutrophils and leukocytes, a decrease in hematocrit, hemoglobin and platelet count; bacteriuria, increased serum urea nitrogen levels, the number of epithelial cells in the urine, and the number of erythrocytes in the urine.

Other:

rarely - allergic reactions, general malaise, fungal infections.

Directions for use and doses

The method of administration and dosage regimen of a particular drug depend on its release form and other factors. The optimal dosage regimen is determined by the doctor. The compliance of the dosage form of a particular drug with the indications for use and dosage regimen should be strictly observed.

Administered by intravenous infusion or intramuscular injection. When administered intravenously, the infusion duration should be 30 minutes. IM administration may be an alternative to IV infusion.

The average daily dose of the drug for adults is 1 g, the frequency of administration is 1 time/day.

The usual duration of therapy is from 3 to 14 days, depending on the severity of the disease and the type of microorganisms. If there are clinical indications, a transition to subsequent adequate oral antimicrobial therapy is acceptable.

In patients with CC>30 ml/min/1.73 m2, no dosage adjustment is required. In patients with severe renal impairment (creatinine clearance≤30 ml/min/1.73 m2), including those on hemodialysis, the recommended dose is 500 mg/day.

Patients on hemodialysis who received ertapenem at a dose of 500 mg/day in the next 6 hours before the hemodialysis session should receive an additional 150 mg of ertapenem after the session. If ertapenem is administered more than 6 hours before hemodialysis, no additional dose is required. There are currently no recommendations for patients undergoing peritoneal dialysis or hemofiltration.

special instructions

Serious (even fatal) anaphylactic reactions have been reported in patients treated with beta-lactam antibiotics. These reactions are more likely in individuals with a history of multivalent allergies (in particular, individuals with hypersensitivity to penicillin often develop severe hypersensitivity reactions when treated with other beta-lactam antibiotics). Before starting to use ertapenem, you should check for a history of indications of previous hypersensitivity reactions to other allergens (especially to penicillins, cephalosporins and other beta-lactam antibiotics). If an allergic reaction occurs, ertapenem should be discontinued immediately. When using ertapenem (like many antibacterial agents ) the development of pseudomembranous colitis (the main cause of which is a toxin produced by Clostridium difficile) is possible, which should be kept in mind when severe diarrhea occurs in patients receiving antibacterial therapy. When administered intramuscularly, avoid accidental penetration of ertapenem into a blood vessel. Use in pediatrics

Because The safety and effectiveness of ertapenem in pediatrics have not been studied, and its use in children and adolescents under 18 years of age is not recommended.