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Pronunciation |
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(sef
a PYE
rin) |
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U.S. Brand
Names |
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Cefadyl® |
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Generic
Available |
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No |
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Synonyms |
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Cephapirin Sodium |
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Pharmacological Index |
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Antibiotic, Cephalosporin (First Generation) |
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Use |
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Treatment of infections when caused by susceptible strains in respiratory,
genitourinary, gastrointestinal, skin and soft tissue, bone and joint
infections, septicemia; treatment of susceptible gram-positive bacilli and cocci
(never 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 cephapirin 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
<1%: CNS irritation, seizures, fever, rash, urticaria, leukopenia,
thrombocytopenia, increased transaminases
Other reactions with cephalosporins include anaphylaxis, erythema multiforme,
toxic epidermal necrolysis, Stevens-Johnson syndrome, dizziness, fever,
headache, encephalopathy, asterixis, neuromuscular excitability, seizures,
nausea, vomiting, pseudomembranous colitis, decreased hemoglobin,
agranulocytosis, pancytopenia, aplastic anemia, hemolytic anemia, interstitial
nephritis, toxic nephropathy, pain at injection site, vaginitis, angioedema,
cholestasis, hemorrhage, prolonged PT, serum-sickness reactions, 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: High-dose probenecid decreases clearance
Increased toxicity: Aminoglycosides increase nephrotoxic potential
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Stability |
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Reconstituted solution is stable for 24 hours at room temperature and 10 days
when refrigerated; for I.V. infusion in NS or D5W solution is stable
for 24 hours at room temperature, 10 days when refrigerated or 14 days when
frozen; after freezing, thawed solution is stable for 12 hours at room
temperature or 10 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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Distribution: Widely distributed into most body tissues and fluids including
gallbladder, liver, kidneys, bone, sputum, bile, and pleural and synovial
fluids; CSF penetration is poor; crosses the placenta and small amounts appear
in breast milk
Protein binding: 22% to 25%
Metabolism: Partially in the liver, kidney, and plasma to metabolites (50%
active)
Half-life: 36-60 minutes
Time to peak serum concentration: I.M.: Within 30 minutes
Elimination: 60% to 85% excreted as unchanged drug in urine
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Usual Dosage |
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I.M., I.V.:
Adults: 500 mg to 1 g every 6 hours up to 12 g/day
Perioperative prophylaxis: 1-2 g 30 minutes to 1 hour prior to surgery and
every 6 hours as needed for 24 hours following
Dosing interval in renal impairment:
Clcr 10-50 mL/minute: Administer every 6-8 hours
Clcr <10 mL/minute: Administer every 12 hours
Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects:
Administer 1 g every 8 hours |
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Monitoring
Parameters |
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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, false-positive urinary proteins and
steroids |
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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.M. or I.V. 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; obtain specimens for
culture and sensitivity prior to administration of first
dose |
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Dosage Forms |
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Powder for injection, as sodium: 500 mg, 1 g, 2 g, 4 g, 20
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.
Khan AJ and Pryles CV,
"Clinical and Pharmacological Evaluation of Cephapirin Sodium (BL-P-1322) in Infants and Children (Cephapirin in Pediatric Patients),"
Curr Ther Res Clin Exp, 1973, 15(4):198-204.
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