Avibactam (formerly NXL104, AVE1330A) is a β-lactamase non-synthetic β-lactam inhibitor that inhibits the activity of Ambler class A and C beta-lactamase enzymes and certain Ambler class D. This review summarizes the available data for
ceftazidime published avibactam including the relevant chemistry, mechanisms of action and resistance, microbiology, pharmacokinetics, pharmacodynamics and efficacy and safety data from animal and human studies. Although not a β-lactam, the chemical structure of avibactam resembles parts of the cephem bicyclic ring system has been shown and avibactam covalently attached to ß-lactamases connect. Very little is known about the potential for resistance to avibactam choose. Adding a strong avibactam (4-1024 times the minimum inhibitory concentration reduction [MIC]) improves the activity of ceftazidime against most Enterobacteriaceae species, depending on the presence or absence of the β-lactamase enzyme (s). Against Pseudomonas aeruginosa, adding avibactam improves ceftazidime activity (MIC ~ reduction four times). Limited data suggest that adding avibactam not enhance the activity of ceftazidime against Acinetobacter species or most anaerobic bacteria (exceptions: .. Bacteroides fragilis, Clostridium perfringens, Prevotella spp and Porphyromonas spp). The pharmacokinetics of avibactam follow a two-compartment model and do not seem to be affected by concomitant administration of ceftazidime. The maximum concentration of drug in plasma (C (max)) and the area under the plasma concentration-time curve (AUC) between avibactam increase linearly with doses of 50 mg to 2000 mg. The mean volume of distribution and half-life of 22 L (~ 0.3 L / kg) and ~ 2 hours, changed, are similar to ceftazidime. How avibactam ceftazidime is mainly excreted by the kidneys, and the clearance was correlated with creatinine clearance. The pharmacodynamic data suggest that ceftazidime quickly avibactam bactericidal against Gram-negative β-lactamase producing bacteria which are not inhibited by ceftazidime alone.Clinical studies to date have reported that ceftazidime avibactam is as effective as the standard treatment for carbapenem complicated intra-abdominal infection is and complicated urinary tract infections, including caused by gram-negative resistant cephalosporin isolates the infection. The safety and tolerability of ceftazidime avibactam was reported in three Phase I pharmacokinetic studies and two Phase II clinical trials. Ceftazidime avibactam seems date.In statements reported in healthy volunteers and patients to the hospital to be met with few serious adverse effects associated with drug well tolerated treatment is avibactam the ceftazidime spectrum to expand against ß-lactamase producing Gram-negative bacilli. The exact ceftazidime avibactam roles will be defined by the efficacy and safety data from other clinical trials. possible future roles for ceftazidime avibactam include treatment of suspected or documented infections caused by gram negative bacilli resistant to producing extended-spectrum beta-lactamase carbapenemases (ESBL) Klebsiella pneumoniae (CCP) and / or AmpC ß-lactamases. In addition, ceftazidime avibactam used in combination (with metronidazole) used on suspicion of polymicrobial infections. Finally, the increase of the activity of ceftazidime against P. aeruginosa is avibactam may be beneficial clinical P. aeruginosa infections with suspected or documented in patients.
