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Aztreonam



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 (trade name 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.

Additional recommended knowledge

Contents

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.

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]

Administration

Aztreonam must be administered intravenously, as the compound is poorly absorbed when given via the oral route. Phase III trials are currently in progress to measure its delivery in inhaled form, using an ultrasonic nebulizer.

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.

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.. 


 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Aztreonam". A list of authors is available in Wikipedia.
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