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Pronunciation |
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(AZ
tree oh
nam) |
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U.S. Brand
Names |
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Azactam® |
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Generic
Available |
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No |
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Synonyms |
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Azthreonam |
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Pharmacological Index |
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Antibiotic, Miscellaneous |
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Use |
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Treatment of patients with urinary tract infections, lower respiratory tract
infections, septicemia, skin/skin structure infections, intra-abdominal
infections, and gynecological infections caused by susceptible gram-negative
bacilli; often useful in patients with allergies to penicillins or
cephalosporins |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to aztreonam or any component |
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Warnings/Precautions |
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Rare cross-allergenicity to penicillins and cephalosporins; requires dosing
adjustment in renal impairment |
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Adverse
Reactions |
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1% to 10%:
Dermatologic: Rash
Gastrointestinal: Diarrhea, nausea, vomiting
Local: Thrombophlebitis, pain at injection site
<1%: Hypotension, seizures, confusion, headache, vertigo, insomnia,
dizziness, fever, breast tenderness, pseudomembranous colitis, aphthous ulcer,
abnormal taste, halitosis, numb tongue, vaginitis, hepatitis, jaundice, elevated
liver enzymes, thrombocytopenia, eosinophilia, leukopenia, neutropenia, myalgia,
weakness, diplopia, tinnitus, sneezing, anaphylaxis |
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Overdosage/Toxicology |
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Symptoms of overdose include seizures
If necessary, dialysis can reduce the drug concentration in the blood
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Drug
Interactions |
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Avoid antibiotics that induce beta-lactamase production (cefoxitin,
imipenem) |
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Stability |
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Reconstituted solutions are colorless to light yellow straw and may turn pink
upon standing without affecting potency; use reconstituted solutions and I.V.
solutions (in NS and D5W) within 48 hours if kept at room temperature
or 7 days if kept in refrigerator |
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Mechanism of
Action |
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Inhibits bacterial cell wall synthesis by binding to one or more of the
penicillin binding proteins (PBPs); which in turn inhibits the final
transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus
inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing
activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while
cell wall assembly is arrested. Monobactam structure makes cross-allergenicity
with beta-lactams unlikely. |
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Pharmacodynamics/Kinetics |
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Absorption: I.M.: Well absorbed; I.M. and I.V. doses produce comparable serum
concentrations
Distribution: Relative diffusion of antimicrobial agents from blood into
cerebrospinal fluid (CSF): Good only with inflammation (exceeds usual MICs);
widely distributed to most body fluids and tissues including breast milk;
crosses placenta
Vd: Neonates: 0.26-0.36 L/kg; Children: 0.2-0.29 L/kg; Adults: 0.2
L/kg
Ratio of CSF to blood level (%): Inflamed meninges: 8-40; Normal meninges: ~1
Protein binding: 56%
Metabolism: Partial
Half-life:
Neonates: <7 days, less than or equal to 2.5 kg: 5.5-9.9 hours; <7
days, >2.5 kg: 2.6 hours; 1 week to 1 month: 2.4 hours
Children 2 months to 12 years: 1.7 hours
Adults: Normal renal function: 1.7-2.9 hours
End-stage renal disease: 6-8 hours
Time to peak: Within 60 minutes (I.M., I.V. push) and 90 minutes (I.V.
infusion)
Elimination: 60% to 70% excreted unchanged in urine and partially in feces
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Usual Dosage |
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Neonates: I.M., I.V.:
Postnatal age less than or equal to 7 days:
<2000 g: 30 mg/kg/dose every 12 hours
>2000 g: 30 mg/kg/dose every 8 hours
Postnatal age >7 days:
<1200 g: 30 mg/kg/dose every 12 hours
1200-2000 g: 30 mg/kg/dose every 8 hours
>2000 g: 30 mg/kg/dose every 6 hours
Children >1 month: I.M., I.V.: 90-120 mg/kg/day divided every 6-8 hours
Cystic fibrosis: 50 mg/kg/dose every 6-8 hours (ie, up to 200 mg/kg/day);
maximum: 6-8 g/day
Adults:
Urinary tract infection: I.M., I.V.: 500 mg to 1 g every 8-12 hours
Moderately severe systemic infections: 1 g I.V. or I.M. or 2 g I.V. every
8-12 hours
Severe systemic or life-threatening infections (especially caused by
Pseudomonas aeruginosa): I.V.: 2 g every 6-8 hours; maximum: 8 g/day
Dosing adjustment in renal impairment: Adults:
Clcr >50 mL/minute: 500 mg to 1 g every 6-8 hours
Clcr 10-50 mL/minute: 50% to 75% of usual dose given at the usual
interval
Clcr <10 mL/minute: 25% of usual dosage given at the usual
interval
Hemodialysis: Moderately dialyzable (20% to 50%); administer dose
postdialysis or supplemental dose of 500 mg after dialysis
Peritoneal dialysis: Administer as for Clcr <10 mL/minute
Continuous arteriovenous or venovenous hemofiltration (CAVH/CAVHD): Dose as
for Clcr 10-50 mL/minute |
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Monitoring
Parameters |
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Periodic liver function test; monitor for signs of anaphylaxis during first
dose |
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Test
Interactions |
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May interfere with urine glucose tests containing cupric sulfate (Benedict's
solution, Clinitest®) |
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Mental Health: Effects
on Mental Status |
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May rarely produce confusion |
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Mental Health:
Effects on Psychiatric
Treatment |
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Rarely produces leukopenia and neutropenia; use caution with clozapine and
carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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This medication can only be administered I.M. or I.V. You may experience
nausea or GI distress. Frequent mouth care, frequent small meals, sucking
lozenges, or chewing gum may help relieve these symptoms. May cause false
readings with urine glucose testing. Diabetics should use alternate means of
monitoring glucose. Report any unrelieved diarrhea or vomiting, pain at
injection sites, unresolved fever, unhealed or new sores in mouth or vagina,
vaginal discharge, or acute onset of respiratory difficulty. Breast-feeding
precautions: Consult prescriber if breast-feeding. |
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Nursing
Implications |
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Administer by IVP over 3-5 minutes at a maximum concentration of 66 mg/mL or
by intermittent infusion over 20-60 minutes at a final concentration not to
exceed 20 mg/mL |
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Dosage Forms |
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Powder for injection: 500 mg (15 mL, 100 mL); 1 g (15 mL, 100 mL); 2 g (15
mL, 100 mL) |
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References |
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Bosso JA and Black PG,
"The Use of Aztreonam in Pediatric Patients: A Review," Pharmacotherapy,
1991, 11(1):20-5.
Brogden RN and Heel RC,
"Aztreonam. A Review of Its Antibacterial Activity, Pharmacokinetic Properties and Therapeutic Use,"
Drugs, 1986, 31(2):96-130.
Creasey WA, Platt TB, Frantz M, et al,
"Pharmacokinetics of Aztreonam in Elderly Male Volunteers," Br J Clin
Pharmacol, 1985, 19:233-7.
Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med,
1988, 318(7):419-26 and 318(8):490-500.
Hellinger WC and Brewer NS,
"Carbapenems and Monobactams: Imipenem, Meropenem, and Aztreonam," Mayo Clin
Proc, 1999, 74(4):420-34.
Johnson DH and Cunha BA, "Aztreonam," Med Clin North Am, 1995,
79(4):733-43.
Settler FR, Schramm M, Swabb EA,
"Safety of Aztreonam and SQ 26,992 in Elderly Patients With Renal Insufficiency,"
Rev Infect Dis, 1985, (Suppl 4):5622.
Stutman HR, Chartrand SA, Tolentino T, et al,
"Aztreonam Therapy for Serious Gram-Negative Infections in Children," Am J
Dis Child, 1986, 140(11):1147-51. |
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