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Pronunciation |
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(sef
A zoe
lin) |
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U.S. Brand
Names |
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Ancef®; Kefzol®;
Zolicef® |
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Generic
Available |
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Yes |
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Synonyms |
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Cefazolin Sodium |
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Pharmacological Index |
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Antibiotic, Cephalosporin (First Generation) |
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Use |
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Dental: Alternative antibiotic for prevention of bacterial endocarditis when
parenteral administration is needed. Individuals allergic to amoxicillin
(penicillins) may receive cefazolin provided they have not had an immediate,
local, or systemic IgE-mediated anaphylactic allergic reaction to penicillin.
Alternate antibiotic for premedication in patients not allergic to penicillin
who may be at potential increased risk of hematogenous total joint infection
when parenteral administration is needed.
Medical: Treatment of gram-positive bacilli and cocci (except enterococcus);
some gram-negative bacilli including E. coli, Proteus, and
Klebsiella may be susceptible |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to cefazolin sodium, 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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1% to 10%:
Gastrointestinal: Diarrhea
Local: Pain at injection site
<1%: Anaphylaxis, rash, pruritus, Stevens-Johnson syndrome, oral
candidiasis, nausea, vomiting, abdominal cramps, anorexia, pseudomembranous
colitis, eosinophilia, neutropenia, leukopenia, thrombocytopenia,
thrombocytosis, elevated transaminases, phlebitis, vaginitis, fever, seizures
Other reactions with cephalosporins include toxic epidermal necrolysis,
abdominal pain, cholestasis, superinfection, renal dysfunction, toxic
nephropathy, aplastic anemia, hemolytic anemia, hemorrhage, prolonged
prothrombin time, pancytopenia |
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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: High-dose probenecid decreases clearance
Increased toxicity: Aminoglycosides increase nephrotoxic potential
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Stability |
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Store intact vials at room temperature and protect from temperatures
exceeding 40°C
Reconstituted solutions of cefazolin are light yellow to yellow
Protection from light is recommended for the powder and for the reconstituted
solutions
Reconstituted solutions are stable for 24 hours at room temperature and 10
days under refrigeration
Stability of parenteral admixture at room temperature
(25°C): 48 hours
Stability of parenteral admixture at refrigeration temperature
(4°C): 14 days
Standard diluent: 1 g/50 mL D5W; 2 g/50 mL D5W
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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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Distribution: Widely distributed into most body tissues and fluids including
gallbladder, liver, kidneys, bone, sputum, bile, pleural and synovial fluids;
CSF penetration is poor; crosses the placenta and small amounts appear in breast
milk
Protein binding: 74% to 86%
Metabolism: Hepatic is minimal
Half-life: 90-150 minutes (prolonged with renal impairment)
Time to peak serum concentration: I.M.: Within 0.5-2 hours
Elimination: 80% to 100% is excreted unchanged in urine |
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Usual Dosage |
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I.M., I.V.:
Adults: 250 mg to 2 g every 6-12 (usually 8) hours, depending on severity of
infection; maximum dose: 12 g/day
Dosing adjustment in renal impairment:
Clcr 10-30 mL/minute: Administer every 12 hours
Clcr <10 mL/minute: Administer every 24 hours
Hemodialysis: Moderately dialyzable (20% to 50%); administer dose
postdialysis or administer supplemental dose of 0.5-1 g after dialysis
Peritoneal dialysis: Administer 0.5 g every 12 hours
Continuous arteriovenous or venovenous hemofiltration (CAVH/CAVHD): Dose as
for Clcr 10-30 mL/minute; removes 30 mg of cefazolin per liter of
filtrate per day |
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Monitoring
Parameters |
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Renal function periodically when used in combination with other nephrotoxic
drugs, hepatic function tests, CBC; monitor for signs 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. 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; observe for signs and
symptoms of anaphylaxis during first dose |
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Dosage Forms |
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Infusion, premixed, as sodium, in D5W (frozen)
(Ancef®): 500 mg (50 mL); 1 g (50 mL)
Injection, as sodium (Kefzol®): 500 mg, 1 g
Powder for injection, as sodium (Ancef®,
Zolicef®): 250 mg, 500 mg, 1 g, 5 g, 10 g, 20 g
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References |
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"Advisory Statement. Antibiotic Prophylaxis for Dental Patients With Total Joint Replacements. American Dental Association; American Academy of Orthopedic Surgeons,"
J Am Dent Assoc, 1997, 128(7):1004-8.
Dajani AS, Taubert KA, Wilson WW, et al,
"Prevention of Bacterial Endocarditis. Recommendations by the American Heart Association,"
JAMA, 1997, 277(22):1794-801.
Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med,
1988, 318(7):419-26 and 318(8):490-500.
Gentry LO, Zeluff BJ, and Cooley DA,
"Antibiotic Prophylaxis in Open-Heart Surgery: A Comparison of Cefamandole, Cefuroxime, and Cefazolin,"
Ann Thorac Surg, 1988, 46(2):167-71.
Gustaferro CA and Steckelberg JM,
"Cephalosporin Antimicrobial Agents and Related Compounds," Mayo Clin
Proc, 1991, 66(10):1064-73.
Marshall WF and Blair JE, "The Cephalosporins," Mayo Clin Proc, 1999,
74(2):187-95.
Peterson CD, Lake KD, Arom KV, et al,
"Antibiotic Prophylaxis in Open-Heart Surgery Patients: Comparison of Cefamandole and Cefuroxime,"
Drug Intell Clin Pharm, 1987, 21(9):728-32.
Pickering LK, O'Connor DM, Anderson D, et al,
"Clinical and Pharmacologic Evaluation of Cefazolin in Children," J Infect
Dis, 1973, 128(Suppl):S407-1.
Robinson DC, Cookson TL, and Grisafe JA,
"Concentration Guidelines for Parenteral Antibiotics in Fluid-Restricted Patients,"
Drug Intell Clin Pharm, 1987, 21(12):985-9.
Simon VC, Malerczyk V, Tenschert B, et al,
"Die Geriatrische Pharmakologie von Cefazolin, Cefradin, und Sulfisomidin,"
Arzneim Forsch, 1976, 26(7):1377-82.
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