Aztreonam

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Aztreonam
Systematic (IUPAC) name
3-[2-(2-azaniumyl-1,3-thiazol-4-yl)-2-(1-hydroxy-2-
methyl-1-oxo-propan-2-yl)oxyimino- acetyl]amino-2-methyl-4-oxo-azetidine-1-sulfonate
Identifiers
CAS number 78110-38-0
ATC code J01DF01
PubChem 54116
DrugBank APRD00815
Chemical data
Formula C13H17N5O8S2 
Mol. mass 435.435 g/mol
Pharmacokinetic data
Bioavailability 100% (IM)
Protein binding 56%
Metabolism hepatic (minor %)
Half life 1.7 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

B1 (Au), B (U.S.)

Legal status

℞-only (U.S.)

Routes Intravenous and intramuscular

Aztreonam (Azactam®) is a synthetic monocyclic beta-lactam antibiotic (a monobactam) originally isolated from Chromobacterium violaceum. It was approved by the FDA in 1986. It is resistant to some beta-lactamases, but is inactivated by extended-spectrum beta-lactamases.

Contents

[edit] Mechanism of action

Aztreonam is similar in action to penicillin. It inhibits mucopeptide synthesis in the bacterial cell wall. It has a very high affinity for penicillin-binding protein 3 (PBP-3) and mild affinity for PBP-1a. Aztreonam binds the penicillin-binding proteins of gram-positive and anaerobic bacteria very poorly and is largely ineffective against them.[1] Aztreonam is bactericidal but less so than some of the cephalosporins.

[edit] Indications

Aztreonam has strong activity against susceptible gram-negative bacteria, including Pseudomonas aeruginosa. It has no useful activity against gram-positive bacteria or anaerobes. It is known to be effective against a wide range of bacteria including Citrobacter, Enterobacter, E coli, Haemophilus, Klebsiella, Proteus, and Serratia species.[2]

[edit] Administration

Aztreonam must be administered intravenously, as the compound is poorly absorbed when given via the oral route.

[edit] Common adverse effects

Reported side-effects include injection site reactions, rash, and rarely toxic epidermal necrolysis. Gastrointestinal side effects generally include diarrhea and nausea and vomiting. There may be drug-induced eosinophilia. There is limited cross-reactivity between aztreonam and other beta-lactam antibiotics, and it is generally considered safe to admininister aztreonam to patients with hypersensitivity (allergies) to penicillins.[1]

Aztreonam is considered Pregnancy category B.

[edit] References

  1. ^ a b (2006) AHFS DRUG INFORMATION® 2006, 2006 ed, American Society of Health-System Pharmacists. 
  2. ^ (2006) Mosby's Drug Consult 2006, 16 ed, Mosby, Inc.. 


[edit] External link


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