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aztreonam (Azactam)
Tradename: Azactam.
Indications:
1) treatment for bacterial infections due to susceptible organisms
2) treatment of patients with documented multidrug-resistant aerobic gram-negative infection in which aminoglycoside & beta-lactamase is contraindicated
3) used for treatment of
a) urogenital infections
1] urinary tract infection
2] gynecologic infections
a] pelvic inflammatory disease
b] endometritis
b) lower respiratory tract infection,
c) septicemia
d) skin or soft tissue infection
1] skin infections
2] skin structure infections
e) intra-abdominal infections
- bacterial peritonitis
Dosage:
1) urinary tract infection: 500 mg IV/IM every 8-12 hours
2) severe systemic infection: 2 g IV every 6-8 hours
3) maximum dose: 8 g/day
4) pediatrics: 30 mg/kg every 6-8 hours.
Dosage adjustment in renal failure:
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) < 1% absorbed from GI tract
2) IM: well absorbed
3) rapidly & widely distributed to body tissues
a) good CSF penetration
b) crosses placenta
4) peak serum concentration within 60 minutes
5) protein binding 56%
6) 60-70% excreted unchanged in the urine
7) partially excreted in the feces
8) elimination 1/2life 1.3-2.2 hours (6-8 hours ESRD)
Antimicrobial activity:
Gram negative
- 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:
1) not common (1-10%)
- thrombophlebitis, pain at site of injection, diarrhea, nausea/vomiting, rash
2) 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,
3) 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
Interactions
drug interactions
General
monobactam (monobactam antibiotic)
Properties
MISC-INFO: elimination route KIDNEY
1/2life 1.3-2.2 HOURS
protein-binding 56%
pregnancy-category B
safety in lactation ?
Database Correlations
PUBCHEM correlations
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