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Azactam

Azactam - General Information

A monocyclic beta-lactam antibiotic originally isolated from Chromobacterium violaceum. It is resistant to beta-lactamases and is used in gram-negative infections, especially of the meninges, bladder, and kidneys. It may cause a superinfection with gram-positive organisms.

 

Pharmacology of Azactam

Azactam is a monocyclic beta-lactam antibiotic (a monobactam) originally isolated from Chromobacterium violaceum. Azactam exhibits potent and specific activity in vitro against a wide spectrum of gram-negative aerobic pathogens including Pseudomonas aeruginosa. It has no useful activity against gram-positive bacteria or anaerobes, but has very broad spectrum against gram-negative aerobes, including Pseudomonas aeruginosa. This has given it the nickname "the magic bullet for aerobic gram-negative bacteria". Azactam, unlike the majority of beta-lactam antibiotics, does not induce beta-lactamase activity and its molecular structure confers a high degree of resistance to hydrolysis by beta-lactamases (such as penicillinases and cephalosporinases) produced by most gram-negative and gram-positive pathogens; it is, therefore, usually active against gram-negative aerobic microorganisms that are resistant to antibiotics hydrolyzed by beta-lactamases. It is active against many strains that are multiply-resistant to other antibiotics, such as certain cephalosporins, penicillin, and aminoglycosides. Azactam maintains its antimicrobial activity over a pH range of 6 to 8 in vitro, as well as in the presence of human serum and under anaerobic conditions.

 

Azactam for patients

Patients should be counseled that antibacterial drugs including AZACTAM should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When AZACTAM is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may (1) decrease the effectiveness of the immediate treatment and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by AZACTAM or other antibacterial drugs in the future.

 

Azactam Interactions

No information provided.

 

Azactam Contraindications

This preparation is contraindicated in patients with known hypersensitivity to aztreonam or any other component in the formulation.

 

Additional information about Azactam

Azactam Indication: For the treatment of the following infections caused by susceptible gram-negative microorganisms: urinary tract infections, lower respiratory tract infections, septicemia, skin and skin-structure infections, intra-abdominal infections, and gynecologic infections.
Mechanism Of Action: The bactericidal action of aztreonam results from the inhibition of bacterial cell wall synthesis due to a high affinity of aztreonam for penicillin binding protein 3 (PBP3). By binding to PBP3, aztreonam inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins. It is possible that aztreonam interferes with an autolysin inhibitor.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Aztreonam
Synonyms: AZT
Drug Category: Anti-Bacterial Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Aztreonam: Azactam; Corus 1020; Dynabiotic; Monobactam; Primbactam;
Absorption: Less than 1% absorbed from the gastrointestinal tract following oral administration. Completely absorbed following intramuscular administration.
Toxicity (Overdose): Not Available
Protein Binding: Serum protein binding averaged 56% and is independent of dose. Impaired renal function, 36 to 43%.
Biotransformation: Approximately 6 to 16% metabolized to inactive metabolites by hydrolysis of the beta-lactam bond, resulting in an open-ring compound.
Half Life: The serum half-life of aztreonam averaged 1.7 hours (1.5 to 2.0) in subjects with normal renal function, independent of the dose. In elderly patients and in patients with impaired renal function, the mean serum half-life of aztreonam increased (4.7 to 6 hours and 2.1 hours, respectively).
Dosage Forms of Azactam: Solution Intravenous
Chemical IUPAC Name: (2S,3S)-3-[[(2E)-2-(2-azaniumyl-1,3-thiazol-4-yl)-2-(1-hydroxy-2-methyl-1-oxopropan-2-yl)oxyiminoacetyl]amino]-2-methyl-4-oxoazetidine-1-sulfonate
Chemical Formula: C13H17N5O8S2
Aztreonam on Wikipedia: http://en.wikipedia.org/wiki/Aztreonam
Organisms Affected: Enteric bacteria and other eubacteria