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Pronunciation |
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(sef
MET a
zole) |
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U.S. Brand
Names |
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Zefazone® |
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Generic
Available |
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No |
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Synonyms |
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Cefmetazole Sodium |
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Pharmacological Index |
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Antibiotic, Cephalosporin (Second Generation) |
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Use |
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Second generation cephalosporin, useful for susceptible aerobic and anaerobic
gram-positive and gram-negative bacteria; surgical prophylaxis, specifically
colorectal and OB-GYN |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to cefmetazole or any component or
cephalosporins |
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Warnings/Precautions |
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Modify dosage in patients with severe renal impairment; prolonged use may
result in superinfection; use with caution in patients with a history of
penicillin allergy especially IgE-mediated reactions (eg, anaphylaxis,
urticaria); may cause antibiotic-associated colitis or colitis secondary to
C. difficile |
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Adverse
Reactions |
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Contains MTT side chain which may lead to increased risk of
hypoprothrombinemia and bleeding.
Dermatologic: Rash
Gastrointestinal: Diarrhea
<1%: Pain at injection site, phlebitis, pseudomembranous colitis,
epigastric pain, candidiasis, bleeding, shock, hypotension, headache, hot
flashes, dyspnea, epistaxis, respiratory distress, fever, vaginitis
Other reactions with cephalosporins include anaphylaxis, seizures, toxic
epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome, renal
dysfunction, interstitial nephritis, toxic nephropathy, cholestasis, aplastic
anemia, hemolytic anemia, hemorrhage, pancytopenia, neutropenia,
agranulocytosis, colitis, superinfection |
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Overdosage/Toxicology |
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Symptoms of overdose include neuromuscular hypersensitivity, convulsions
especially with renal insufficiency; many beta-lactam antibiotics have the
potential to cause neuromuscular hyperirritability or seizures
Hemodialysis may be helpful to aid in the removal of the drug from the blood,
otherwise most treatment is supportive or symptom directed.
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Drug
Interactions |
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Increased effect: Probenecid may decrease cephalosporin elimination
Increased toxicity: Furosemide, aminoglycosides may be a possible additive to
nephrotoxicity |
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Stability |
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Reconstituted solution and I.V. infusion in NS or D5W solution are
stable for 24 hours at room temperature, 7 days when refrigerated, or 6 weeks
when frozen; after freezing, thawed solution is stable for 24 hours at room
temperature or 7 days when refrigerated |
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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. |
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Pharmacodynamics/Kinetics |
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Absorption: I.M.: Well absorbed
Distribution: Widely distributed
Protein binding: 65%
Metabolism: <15%
Half-life: 72 minutes
Elimination: Renal |
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Usual Dosage |
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Adults: I.V.:
Prophylaxis: 2 g 30-90 minutes before surgery or 1 g 30-90 minutes
before surgery; repeat 8 and 16 hours later
Dosing interval in renal impairment:
Clcr 50-90 mL/minute: Administer every 12 hours
Clcr 10-50 mL/minute: Administer every 16-24 hours
Clcr <10 mL/minute: Administer every 48 hours
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Monitoring
Parameters |
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Monitor prothrombin times; observe for signs and symptoms of anaphylaxis
during first dose |
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Test
Interactions |
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Positive direct Coombs', false-positive urinary glucose test using cupric
sulfate (Benedict's solution, Clinitest®, Fehling's
solution), false-positive serum or urine creatinine with
Jaffé reaction |
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Mental Health: Effects
on Mental Status |
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May cause nervousness; case reports of euphoria, delusion, illusions, and
depersonalization with cephalosporins |
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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause 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 drug is administered I.V. or I.M. Drink 2-3 L fluid/day. Avoid alcohol
during therapy and for 72 hours after last dose (may cause severe
disulfiram-like reactions). If diarrhea occurs, yogurt or buttermilk may help.
May cause false-positive test with Clinitest®; use another
form of testing. May interfere with oral contraceptives; additional
contraceptive measures are necessary. Report severe, unresolved diarrhea;
vaginal itching or drainage; sores in mouth; blood, pus, or mucus in stool or
urine; easy bleeding or bruising; unusual fever or chills; rash; or respiratory
difficulty. Breast-feeding precautions: Consult prescriber if
breast-feeding. |
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Nursing
Implications |
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Do not admix with aminoglycosides in same bottle/bag |
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Dosage Forms |
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Powder for injection, as sodium: 1 g, 2 g |
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References |
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Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med,
1988, 318(7):419-26 and 318(8):490-500.
Donowitz GR and Mandell GL, "Drug Therapy. Beta-Lactam Antibiotics (1)," N
Engl J Med, 1988, 318(7):419-26.
Donowitz GR and Mandell GL, "Drug Therapy. Beta-Lactam Antibiotics (2)," N
Engl J Med, 1988, 318(8):490-500.
Jones RN,
"Review of the In vitro Spectrum and Characteristics of Cefmetazole (CS-1170),"
J Antimicrob Chemother, 1989, 23(Suppl D):1-12.
Marshall WF and Blair JE, "The Cephalosporins," Mayo Clin Proc, 1999,
74(2):187-95.
Plouffe JF,
"Cefmetazole Versus Cefoxitin in Prevention of Infections After Abdominal Surgery,"
J Antimicrob Chemother, 1989, 23(Suppl D):85-8.
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