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Pronunciation |
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(SEF
ra
deen) |
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U.S. Brand
Names |
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Velosef® |
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Generic
Available |
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Yes |
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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; 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 cephradine, 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%: Rash, nausea, vomiting, pseudomembranous colitis, increased BUN,
increased creatinine
Other reactions with cephalosporins include anaphylaxis, erythema multiforme,
toxic epidermal necrolysis, Stevens-Johnson syndrome, dizziness, fever,
headache, encephalopathy, asterixis, neuromuscular excitability, seizures,
neutropenia, leukopenia, agranulocytosis, pancytopenia, aplastic anemia,
hemolytic anemia, interstitial nephritis, toxic nephropathy, 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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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: Well absorbed
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 appears in breast milk
Protein binding: 18% to 20%
Half-life: 1-2 hours
Time to peak serum concentration: Oral: Within 1-2 hours
Elimination: ~80% to 90% unchanged drug is recovered in urine within 6 hours
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Usual Dosage |
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Oral:
Adults: 250-500 mg every 6-12 hours
Dosing adjustment in renal impairment: Adults:
Clcr 10-50 mL/minute: 250 mg every 6 hours
Clcr <10 mL/minute: 125 mg every 6 hours |
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Dietary
Considerations |
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May administer with food to decrease GI distress; however there is delayed
absorption |
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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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Oral: Take as directed, at regular intervals around-the-clock (with or
without food). Chilling oral suspension improves flavor (do not freeze).
Complete full course of medication, even if you feel better. 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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Administer around-the-clock to promote less variation in peak and trough
serum levels; I.M. doses should be administered deep into a large muscle mass
(ie, gluteus maximus)
Stability: Reconstituted solution is stable for 2 hours at room temperature
and 24 hours when refrigerated; for I.V. infusion in normal saline or
D5W solution is stable for 10 hours at room temperature, 48 hours
when refrigerated or 6 weeks when frozen; after freezing, thawed solution is
stable for 10 hours at room temperature or 48 hours when refrigerated
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Dosage Forms |
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Capsule: 250 mg, 500 mg
Powder for injection: 250 mg, 500 mg, 1 g, 2 g, (in ready-to-use infusion
bottles)
Powder for oral suspension: 125 mg/5 mL (5 mL, 100 mL, 200 mL); 250 mg/5 mL
(5 mL, 100 mL, 200 mL) |
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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.
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.
Smith GH, "Oral Cephalosporins in Perspective," DICP, 1990,
24(1):45-51.
Wise R, "The Pharmacokinetics of the Oral Cephalosporins - A Review," J
Antimicrob Chemother, 1990, 26(Suppl E):13-20.
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