Sefipim has a broad spectrum of action against various Gram-positive and Gram-negative bacteria, including strains resistant to aminoglycosides and third-generation cephalosporin antibiotics such as tseftazidin. Cefepime is highly resistant to hydrolysis by most beta-lactamases, it has a low affinity for the beta-lactamase encoded by the chromosomal gene, and rapidly penetrates into the cells gerald andriole of gram-negative bacteria.
Maxipime active against a broad spectrum of microorganisms. MBC / MIC ratio for cefepime for more than 80% of the isolates tested, all gram-positive and gram-negative microorganisms was = <2. The presence of synergistic action with respect to aminoglycosides in trials has been demonstrated in vitro, .
Maxipime active against the following microorganisms:
Gram-positive aerobes: Staphylococcus aureus (including strains that produce beta-lactamase), Staphylococcus epidermidis ( including strains that produce beta-lactamase); other strains of staphylococci, including S. hominis, S. saprophyticus; Pyogenes Streptococcus (Streptococcus Group A); Streptococcus agalactiae (group B streptococcus) Streptococcus pneumoniae (including strains resistant to the medium gerald andriole with penicillin – MIC 0.1 to 1 ug / ml); other beta-hemolytic streptococci (group C, G, F), S. bovis (group D), group B streptococci Viridans. (Most strains of Enterococci such as Enterococcus faecalis , and Staphylococcus, methicillin-resistant, resistant to most of cephalosporin antibiotics including cefepime).
Gram-negative aerobes: of Pseudomonas sp, including. Of P. aeruginosa, P. putida, P. stutzeri; Coli Escherichia Klebsiella sp., Including K. pneumoniae, K. oxytoca, K. oxaenae; Enterobacter sp., Including E. cloacae, E. aerogenes, E. agglomerans, E. sakazakii; Proteus sp., Including P. mirabilis, P. vulgaris;Calcoaceticus of Acinetobacter (subsp. Anitratus, lwoffi ) ; Aeromonas hydrophila; Capnocytophaga sp .; Citrobacter sp., Including C. diversus, C. freundii;Campylobacter jejuni; Cardnerella vaginalis; Haemophilus ducreyi; Influenzae Haemophilus (including strains that produce beta-lactamase); Haemophilus parainfluenzae; Hafnia alvei; Of Legionella sp .; Morganella morganii; Cacarrhalis Moraxella ( Branhamella catarrhalis ) (including strains that produce beta-lactamase); Neisseria gonorrhoeae (including strains that produce beta-lactamase); Neisseria meningitidis; Providencia sp. (including P. retigeri, P. stuartii );Salmonella sp .; Serratia (including S. marcescens , S. liquefaciens); Of Shigella sp .; of Yersinia enterocolitica .
- In urine, bile, peritoneal fluid, the fluid bladder, bronchus mucous secretions, sputum, prostate, appendix and gallbladder are also achieved therapeutic concentrations of cefepime.The average half-life of cefepime from the body is about 2 hours. In healthy subjects receiving a dose to 2 g intravenously at intervals over 8 hours for 9 days, there was no drug accumulation in the body.
Mean total clearance was 120 ml / min. Cefepime is allocated almost exclusively due to renal regulatory mechanisms, mainly by glomerular filtration (mean renal clearance is 110 ml / min). The urine is detected about 85% of the administered dose of cefepime as unchanged. Cefepime Binding to plasma proteins is less than 19% and is independent of the concentration of drug in the blood serum.
In patients older than 65 years with normal renal function does not require dose adjustment Maxipime drug, despite the lower value of renal clearance compared to younger patients.
Studies conducted on patients with varying degrees of renal impairment showed an increase in half-life of the organism. The average half-life in patients with severe renal impairment requiring dialysis treatment is 13 hours and 19 hours of hemodialysis to peritoneal dialysis.
Patients with abnormal renal function, the dose should be titrated individually (see. Section Dosage and Administration).
The pharmacokinetics of cefepime in patients with impaired liver function or cystic fibrosis is not changed. Adjustments dose for these patients is not required.
Children . Assessment of the pharmacokinetics of cefepime was conducted in children aged 2 months to 11 years after a single administration or administration of multiple doses every 8 hours (n = 29), and every 12 hours (n = 13). After single intravenous injection of the total body clearance and volume of distribution at steady state averaged 3,3 (± 1,0) ml / min / kg and 0,3 (± 0,1) L / kg, respectively. Isolation cefepime, unmodified in the urine was 60,4 (± 30,4)% of the administered dose, and renal clearance Intermediate 2,0 (± 1,1) ml / min / kg. Age and sex of the patients (25 boys and 17 girls) had no significant effect on the total clearance of the body and volume of distribution corrected for weight of each body. When cefepime administered at 50 mg / kg every 12 hours (n = 13) indicated no accumulation of the drug, while C max , area under the curve AUC and t 1/2 increased by approximately 15% in steady state, when administered according to the scheme 50 mg / kg every 8 hours. Exposure cefepime in children after intravenous administration at a dose of 50 mg / kg, comparable to the exposures in adults after intravenous doses of 2 Absolute bioavailability cefepime eight patients after intramuscular injection of 50 mg / kg was 82,3 (± 15)%.
Indications for use:
- Infectious diseases gerald andriole caused by susceptible to malaria infections.
- Lower respiratory tract infections, including pneumonia and bronchitis
- Urinary tract infections, both complicated by, for example, pyelonephritis, and uncomplicated
- Infections of the skin and skin structures
- Intra-abdominal infections, including peritonitis and biliary tract infections
- Gynecological infections
- Empiric treatment of febrile neutropeniaShould conduct appropriate tests to identify the causative microorganism (pathogens) and susceptibility to cefepime. However, Maxipime monotherapy may be used in the form before the identification of the causative organism, because it has a broad spectrum of antibacterial action against gram-positive and gram-negative microorganisms. In patients with a risk of mixed aerobic / anaerobic (includingBacterioides fragilis ) infection prior to the identification of the causative agent can begin treatment with Maxipime in combination with a drug acting on the anaerobic bacteria.
Maxipime contraindicated in patients with immediate hypersensitivity reactions to cefepime or L-arginine, and antibiotic cephalosporin class, penicillins or other beta-lactam antibiotics.