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Urology Mar 1993Aztreonam is the first monobactam and is unique among beta-lactam antibiotics for its spectrum of activity that is exclusively active against gram-negative aerobic... (Review)
Review
Aztreonam is the first monobactam and is unique among beta-lactam antibiotics for its spectrum of activity that is exclusively active against gram-negative aerobic bacteria. Broad clinical experience with this agent supports its use in the treatment of adults with severe or complicated urologic infections. Aztreonam may be safely used in patients with penicillin allergy. With a spectrum of activity that is comparable to the aminoglycosides but without the potential for ototoxicity or nephrotoxicity, aztreonam represents a rational choice of therapy for treatment of systemic urinary tract infections due to susceptible organisms.
Topics: Aztreonam; Gram-Negative Aerobic Bacteria; Gram-Negative Bacterial Infections; Humans; Urinary Tract Infections
PubMed: 8442309
DOI: 10.1016/0090-4295(93)90568-u -
Obstetrics and Gynecology Clinics of... Sep 1992Aztreonam is a synthetic monobactam antibiotic that has excellent activity against aerobic gram-negative bacilli. It can be used as a single agent for the treatment of... (Review)
Review
Aztreonam is a synthetic monobactam antibiotic that has excellent activity against aerobic gram-negative bacilli. It can be used as a single agent for the treatment of upper urinary tract infections caused by organisms resistant to the cephalosporins and ampicillin. It also can be administered in combination with a drug such as clindamycin for treatment of pelvic inflammatory disease or postoperative pelvic infections.
Topics: Aztreonam; Bacterial Infections; Costs and Cost Analysis; Female; Genital Diseases, Female; Humans; Pregnancy; Pregnancy Complications, Infectious; Urinary Tract Infections
PubMed: 1436929
DOI: No ID Found -
Infection Control and Hospital... Sep 1990Aztreonam, the first commercially available monobactam, has a wide range of activity against aerobic gram-negative bacilli. It can be administered two to three hours... (Review)
Review
Aztreonam, the first commercially available monobactam, has a wide range of activity against aerobic gram-negative bacilli. It can be administered two to three hours daily because its half-life is 1.6 to 2 hours. Excellent blood and tissue concentrations are attained. The MIC of aztreonam against most Enterobacteriaceae is less than or equal to 2 micrograms/ml and against P aeruginosa less than or equal to 16 micrograms g/ml. Aztreonam has been used in a wide array of infections of the urinary tract and respiratory tract, blood, intra-abdominal and gynecologic infections and infections of the skin, bones and joints. As empiric therapy, aztreonam is usually combined with another antimicrobial agent active against anaerobes and/or aerobic gram-positive cocci until culture results are available. One exception is empiric therapy for gram-negative urinary tract infections in which aztreonam can be used initially as monotherapy against susceptible gram-negative pathogens. In general, the efficacy of aztreonam is equal or superior to that of the aminoglycosides. Adverse reactions to aztreonam are unusual, and it as been shown to be a poor hapten, permitting its administration to patients with proven allergy to the penicillins and cephalosporins. Aztreonam is a useful addition to the available antibiotics for treatment of gram-negative infections.
Topics: Aztreonam; Bacterial Infections; Gram-Negative Bacteria; Humans
PubMed: 2230052
DOI: 10.1086/646216 -
American Family Physician Oct 1988New beta lactams and the quinolone class of antibiotics represent major improvements in the therapy of moderate to severe infections. These newer antibiotics have an... (Review)
Review
New beta lactams and the quinolone class of antibiotics represent major improvements in the therapy of moderate to severe infections. These newer antibiotics have an extended spectrum of antimicrobial activity, excellent pharmacokinetic properties and low toxicity. The beta lactams include carbapenems, represented by imipenem-cilastatin, and monobactams, represented by aztreonam. Norfloxacin and ciprofloxacin are potent quinolones.
Topics: 4-Quinolones; Anti-Bacterial Agents; Anti-Infective Agents; Cilastatin; Cilastatin, Imipenem Drug Combination; Drug Combinations; Humans; Imipenem; Monobactams
PubMed: 3051970
DOI: No ID Found -
The Journal of Allergy and Clinical... Apr 2020Limited population-based data on penicillin-, carbapenem-, monobactam-, and clindamycin-associated reported adverse reactions exist.
BACKGROUND
Limited population-based data on penicillin-, carbapenem-, monobactam-, and clindamycin-associated reported adverse reactions exist.
OBJECTIVE
To collect data on penicillin, carbapenem, monobactam, and clindamycin usage and associated adverse reactions.
METHODS
Data from January 1, 2009, to December 31, 2017, in Kaiser Permanente Southern California were collected.
RESULTS
There were 6,144,422 unique individuals, mean age 33.6 ± 21.1 years, 52.2% females, with at least 1 health care visit during the 9-year study interval, for a total of 37,387,313 patient-years of follow-up. This population was exposed to 5,617,402 courses of oral penicillins, 370,478 courses of parenteral penicillins, 59,645 courses of parenteral carbapenems or monobactams, 817,232 courses of oral clindamycin, and 215,880 courses of parenteral clindamycin. New penicillin allergies were reported more commonly after parenteral (0.85%) compared with oral (0.74%) exposures (P < .0001). There were 22 cases (1 in 255,320) of oral penicillin-associated anaphylaxis and 3 cases (1 in 123,792) of parenteral penicillin-associated anaphylaxis (P < .001). There were 2 clindamycin-associated anaphylaxis cases, 1 (1 in 817,232) oral and 1 (1 in 215,880) parenteral. There were 2 (1 in 2,993,940) penicillin-associated serious cutaneous adverse reaction (SCAR) cases, but both also had co-trimoxazole coexposure within 45 days. There was 1 (1 in 1,033,112) clindamycin-associated SCAR. Clostridioides difficile infection was more common after parenteral exposures, and with extended-spectrum penicillins, beta-lactamase combinations, carbapenems, monobactam, and clindamycin exposures compared with oral penicillins or clindamycin.
CONCLUSIONS
Only 1 of 1543 (0.065%) oral and 1 of 1030 (0.097%) parenteral penicillin-associated allergy reports were confirmed to be anaphylaxis. C. difficile was more common after parenteral versus oral penicillin, carbapenem, monobactam, and clindamycin exposures, and with broader spectrum antibiotic exposures.
Topics: Adolescent; Adult; Anti-Bacterial Agents; Carbapenems; Child; Clindamycin; Clostridioides difficile; Drug Hypersensitivity; Female; Humans; Male; Middle Aged; Monobactams; Penicillins; Retrospective Studies; Young Adult
PubMed: 31821919
DOI: 10.1016/j.jaip.2019.11.035 -
Nature Reviews. Drug Discovery May 2010In February 2010, aztreonam for inhalation solution (Cayston; Gilead) - an inhalable formulation of the monobactam antibiotic aztreonam and lysine - was approved by the...
In February 2010, aztreonam for inhalation solution (Cayston; Gilead) - an inhalable formulation of the monobactam antibiotic aztreonam and lysine - was approved by the US FDA to improve respiratory symptoms in patients with cystic fibrosis infected with Pseudomonas aeruginosa.
Topics: Administration, Inhalation; Anti-Bacterial Agents; Aztreonam; Cystic Fibrosis; Drug Discovery; Humans; Lysine; Pseudomonas Infections; Pseudomonas aeruginosa; Treatment Outcome
PubMed: 20431562
DOI: 10.1038/nrd3170 -
Bioorganic & Medicinal Chemistry Letters Feb 2018Metallo-β-lactamases (MBLs), such as New Delhi metallo-β-lactamase (NDM-1) have spread world-wide and present a serious threat. Expression of MBLs confers resistance...
Metallo-β-lactamases (MBLs), such as New Delhi metallo-β-lactamase (NDM-1) have spread world-wide and present a serious threat. Expression of MBLs confers resistance in Gram-negative bacteria to all classes of β-lactam antibiotics, with the exception of monobactams, which are intrinsically stable to MBLs. However, existing first generation monobactam drugs like aztreonam have limited clinical utility against MBL-expressing strains because they are impacted by serine β-lactamases (SBLs), which are often co-expressed in clinical isolates. Here, we optimized novel monobactams for stability against SBLs, which led to the identification of LYS228 (compound 31). LYS228 is potent in the presence of all classes of β-lactamases and shows potent activity against carbapenem-resistant isolates of Enterobacteriaceae (CRE).
Topics: Animals; Anti-Bacterial Agents; Aztreonam; Bacterial Proteins; CHO Cells; Carbapenem-Resistant Enterobacteriaceae; Cricetulus; Drug Stability; Escherichia coli; Female; Humans; Meropenem; Mice; Microbial Sensitivity Tests; Molecular Structure; Monobactams; Pseudomonas aeruginosa; Receptors, GABA-A; Seizures; Structure-Activity Relationship; Thienamycins; beta-Lactam Resistance; beta-Lactamases
PubMed: 29336873
DOI: 10.1016/j.bmcl.2018.01.006 -
Bioorganic & Medicinal Chemistry Letters Sep 2012Novel siderophore-linked monobactams with in vitro and in vivo anti-microbial activity against MDR Gram-negative pathogens are described.
Novel siderophore-linked monobactams with in vitro and in vivo anti-microbial activity against MDR Gram-negative pathogens are described.
Topics: Animals; Binding Sites; Blood Proteins; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Resistance, Multiple, Bacterial; Gram-Negative Bacteria; Gram-Negative Bacterial Infections; Humans; Mice; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Monobactams; Rats; Structure-Activity Relationship
PubMed: 22892121
DOI: 10.1016/j.bmcl.2012.07.005 -
Indian Pediatrics Apr 2004Aztreonam belongs to the monobactam group of naturally occurring antibiotic compounds characterized by a monocycling ring structure. Aztreonam is the first monobactam...
Aztreonam belongs to the monobactam group of naturally occurring antibiotic compounds characterized by a monocycling ring structure. Aztreonam is the first monobactam that has been approved for use in pediatric medicine by US FDA in the year 1998.
Topics: Anti-Bacterial Agents; Aztreonam; Child; Humans
PubMed: 15123864
DOI: No ID Found -
Bioorganic Chemistry Jan 2020Based on the structural characteristics of aztreonam (AZN) and its target PBP3, a series of new monobactam derivatives bearing various substituents on oxime residue were...
Based on the structural characteristics of aztreonam (AZN) and its target PBP3, a series of new monobactam derivatives bearing various substituents on oxime residue were prepared and evaluated for their antibacterial activities against susceptible and resistant Gram-negative bacteria. Among them, compounds 8p and 8r displayed moderate potency with MIC values of 0.125-32 μg/mL against most tested Gram-negative strains, comparable to AZN. Meanwhile, the combination of 8p and 8r with avibactam as a β-lactamases inhibitor, in a ratio of 1:16, showed a promising synergistic effect against both ESBLs- and NDM-1-producing K. pneumoniae, with significantly reduced MIC values up to 8-fold and >256-fold respectively. Furthermore, both of them demonstrated excellent safety profiles both in vitro and in vivo. The results provided powerful information for further structural optimization of monobactam antibiotics to fight β-lactamase-producing resistant Gram-negative bacteria.
Topics: Anti-Bacterial Agents; Dose-Response Relationship, Drug; Escherichia coli; Klebsiella pneumoniae; Microbial Sensitivity Tests; Molecular Structure; Monobactams; Oximes; Structure-Activity Relationship
PubMed: 31831161
DOI: 10.1016/j.bioorg.2019.103487