aztreonam (Azactam)
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Introduction
Tradename: Azactam.
Indications
- treatment for bacterial infections due to susceptible organisms
- treatment of patients with documented multidrug-resistant aerobic gram-negative infection in which aminoglycoside & beta-lactamase is contraindicated
- used for treatment of
Dosage
- urinary tract infection: 500 mg IV/IM every 8-12 hours
- severe systemic infection: 2 g IV every 6-8 hours
- maximum dose: 8 g/day
- pediatrics: 30 mg/kg every 6-8 hours.
Dosage adjustment in renal failure
Table
| creatinine clearance | dosage |
|---|---|
| 10-30 mL/min* | 50% of usual dose at usual interval |
| < 10 mL/min# | 25% of usual dose at usual interval |
* same dose for continuous arteriovenous hemofiltration
# 0.5 mg after hemodialysis
Pharmacokinetics
- < 1% absorbed from GI tract
- IM: well absorbed
- rapidly & widely distributed to body tissues
- peak serum concentration within 60 minutes
- protein binding 56%
- 60-70% excreted unchanged in the urine
- partially excreted in the feces
- elimination 1/2life 1.3-2.2 hours (6-8 hours ESRD)
elimination via kidney
1/2life = 1.3-2.2 hours
protein binding = 56 %
Antimicrobial activity
- Neisseria gonorrhoeae
- Neisseria meningitidis
- Moraxella catarrhalis
- Haemophilus influenzae
- Escherichia coli
- Klebsiella species
- Enterobacter species
- Serratia species
- Salmonella species
- Shigella species
- Proteus mirabilis
- Proteus vulgaris
- Providencia species
- Morganella species
- Citrobacter species
- Aeromonas species
- Pseudomonas aeruginosa
- Yersinia enterocolitica
- Pasteurella multocida
Adverse effects
- not common (1-10%)
- thrombophlebitis, pain at site of injection, diarrhea, nausea/vomiting, rash
- uncommon (< 1%)
- hypotension, seizures, confusion, anaphylaxis, hepatitis, jaundice, headache, vertigo, insomnia, dizziness, tinnitus, diplopia, numb tongue, mouth ulcer, altered taste, sneezing, halitosis, vaginitis, breast tenderness, weakness, muscular aches, fever, pseudomembranous colitis, thrombocytopenia, eosinophilia, leukopenia, neutropenia,
- other:
- hypersentitivity
- no cross-allerginicity with beta-lactam antibiotics
- generally well tolerated
Mechanism of action
- monocyclic beta-lactam compound isolated from Chromobacterium violaceum
- nteracts with penicillin-binding proteins of susceptible organisms & induces formation of long filamentous bacterial structures
- resistant to beta-lactamases produced by most gram-positive bacteria
Notes
- the antimicrobial activity of aztreonam differs from those of other beta lactam antibiotics & more closely resembles that of an aminoglycoside
- patients who are allergic to penicillins & cephalosporins appear not to react to aztreonam
More general terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill pg 1092
- ↑ Harrison's Principles of Internal Medicine, 13th ed. Companion Handbook. Isselbacher et al (eds), McGraw-Hill Inc. NY, 1995, pg 163
- ↑ Sanford Guide to antimicrobial therapy 1997
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ Department of Veterans Affairs, VA National Formulary
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=54116
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=54117
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2274
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5287725
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=124105