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Pronunciation |
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(naf
SIL
in) |
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U.S. Brand
Names |
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Nafcil™ Injection; Nallpen®
Injection; Unipen® Injection; Unipen®
Oral |
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Generic
Available |
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Yes |
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Synonyms |
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Ethoxynaphthamido Penicillin Sodium; Nafcillin Sodium; Sodium
Nafcillin |
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Pharmacological Index |
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Antibiotic, Penicillin |
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Use |
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Treatment of infections such as osteomyelitis, septicemia, endocarditis, and
CNS infections caused by susceptible strains of staphylococci
species |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to nafcillin or any component or
penicillins |
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Warnings/Precautions |
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Extravasation of I.V. infusions should be avoided; modification of dosage is
necessary in patients with both severe renal and hepatic impairment; elimination
rate will be slow in neonates; use with caution in patients with cephalosporin
hypersensitivity |
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Adverse
Reactions |
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Percentage unknown: Fever, pain, rash, nausea, diarrhea, neutropenia,
thrombophlebitis; oxacillin (less likely to cause phlebitis) is often preferred
in pediatric patients, acute interstitial nephritis, hypersensitivity
reactions |
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Overdosage/Toxicology |
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Symptoms of penicillin overdose include neuromuscular hypersensitivity
(agitation, hallucinations, asterixis, encephalopathy, confusion, and seizures)
and electrolyte imbalance with potassium or sodium salts, especially in renal
failure
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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Decreased effect: Efficacy of oral contraceptives may be reduced;
warfarin/anticoagulants
Increased effect: Disulfiram, probenecid may increase penicillin levels
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Stability |
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Refrigerate oral solution after reconstitution; discard after 7 days;
reconstituted parenteral solution is stable for 3 days at room temperature and 7
days when refrigerated or 12 weeks when frozen; for I.V. infusion in NS or
D5W, solution is stable for 24 hours at room temperature and 96 hours
when refrigerated |
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Mechanism of
Action |
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Interferes with bacterial cell wall synthesis during active multiplication,
causing cell wall death and resultant bactericidal activity against susceptible
bacteria |
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Pharmacodynamics/Kinetics |
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Absorption: Oral: Poor and erratic
Distribution: Widely distributed; CSF penetration is poor but enhanced by
meningeal inflammation; crosses the placenta
Metabolism: Primarily in the liver; it undergoes enterohepatic circulation
Half-life:
Neonates: <3 weeks: 2.2-5.5 hours; 4-9 weeks: 1.2-2.3 hours
Children 3 months to 14 years: 0.75-1.9 hours
Adults: 30 minutes to 1.5 hours, with normal renal and hepatic function
Time to peak serum concentration: Oral: Within 2 hours; I.M.: Within 30-60
minutes
Elimination: Primarily eliminated in bile, 10% to 30% in urine as unchanged
drug; undergoes enterohepatic recycling |
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Usual Dosage |
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Neonates:
<2000 g, <7 days: 50 mg/kg/day divided every 12 hours
<2000 g, >7 days: 75 mg/kg/day divided every 8 hours
>2000 g, <7 days: 50 mg/kg/day divided every 8 hours
>2000 g, >7 days: 75 mg/kg/day divided every 6 hours
Children:
Oral: 25-50 mg/kg/day in 4 divided doses
I.M.: 25 mg/kg twice daily
I.V.:
Mild to moderate infections: 50-100 mg/kg/day in divided doses every 6 hours
Severe infections: 100-200 mg/kg/day in divided doses every 4-6 hours
Maximum dose: 12 g/day
Adults:
Oral: 250-500 mg (up to 1 g) every 4-6 hours
I.M.: 500 mg every 4-6 hours
I.V.: 500-2000 mg every 4-6 hours
Dosing adjustment in renal impairment: Not necessary
Dialysis: Not dialyzable (0% to 5%) via hemodialysis; supplemental dosage not
necessary with hemo- or peritoneal dialysis or continuous arteriovenous or
venovenous hemofiltration (CAVH/CAVHD) |
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Dietary
Considerations |
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Should be administered on an empty stomach, as there is decreased absorption
with food |
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Monitoring
Parameters |
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Periodic CBC, urinalysis, BUN, serum creatinine, AST and ALT; observe for
signs and symptoms of anaphylaxis during first dose |
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Test
Interactions |
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Positive Coombs' test (direct), false-positive urinary and serum proteins;
may inactivate aminoglycosides in vitro |
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Mental Health: Effects
on Mental Status |
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Penicillins reported to cause apprehension, illusions, hallucinations,
depersonalization, agitation, insomnia, and encephalopathy |
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Mental Health:
Effects on Psychiatric
Treatment |
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May 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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Prolonged use of penicillins may lead to the development of oral
candidiasis |
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Patient
Information |
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Oral: Take at regular intervals around-the-clock, preferably on and empty
stomach with full glass of water. Take complete course of treatment as
prescribed. You may experience nausea or vomiting; small frequent meals and good
mouth care may help. If diabetic, drug may cause false tests with
Clinitest® urine glucose monitoring; use of glucose
oxidase methods (Clinistix®) or serum glucose monitoring
is preferable. This drug may interfere with oral contraceptives; an alternate
form of birth control should be used. Report persistent fever, sore throat,
sores in mouth, diarrhea, unusual bleeding or bruising. Report difficulty
breathing or skin rash. Notify prescriber if condition does not respond to
treatment. Breast-feeding precautions: Consult prescriber if
breast-feeding. |
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Nursing
Implications |
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Extravasation: Use cold packs
Hyaluronidase (Wydase®): Add 1 mL NS to 150 unit vial
to make 150 units/mL of concentration; mix 0.1 mL of above with 0.9 mL NS in 1
mL syringe to make final concentration = 15 units/mL |
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Dosage Forms |
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Capsule, as sodium: 250 mg
Powder for injection, as sodium: 500 mg, 1 g, 2 g, 4 g, 10 g
Solution, as sodium: 250 mg/5 mL (100 mL)
Tablet, as sodium: 500 mg |
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References |
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Banner W Jr, Gooch WM 3d, Burckart G, et al,
"Pharmacokinetics of Nafcillin in Infants With Low Birth Weights," Antimicrob
Agents Chemother, 1980, 17(4):691-4.
Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med,
1988, 318(7):419-26 and 318(8):490-500.
Wright AJ, "The Penicillins," Mayo Clin Proc, 1999, 74(3):290-307.
Zenk KE, Dungy CL, and Greene CR,
"Nafcillin Extravasation Injury: Use of Hyaluronidase as an Antidote," Am J
Dis Child, 1981, 135(12):1113-4.
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