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Pronunciation |
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(oks
a SIL
in) |
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U.S. Brand
Names |
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Bactocill® |
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Generic
Available |
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Yes |
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Synonyms |
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Methylphenyl Isoxazolyl Penicillin; Oxacillin Sodium |
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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
Staphylococcus |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to oxacillin or other penicillins or any
component |
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Warnings/Precautions |
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Elimination rate will be slow in neonates; modify dosage in patients with
renal impairment and in the elderly; use with caution in patients with
cephalosporin hypersensitivity |
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Adverse
Reactions |
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1% to 10%: Gastrointestinal: Nausea, diarrhea
<1%: Fever, rash, vomiting, eosinophilia, leukopenia, neutropenia,
thrombocytopenia, agranulocytosis, hepatotoxicity, increased AST, hematuria,
acute interstitial nephritis, serum sickness-like 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; effects of
penicillins may be impaired by tetracycline
Increased effect: Disulfiram, probenecid may increase penicillin levels,
increased effect of anticoagulants are possible with large I.V. doses
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Stability |
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Reconstituted parenteral solution is stable for 3 days at room temperature
and 7 days when refrigerated; for I.V. infusion in NS or D5W,
solution is stable for 24 hours at room temperature |
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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: Oral: 35% to 67%
Distribution: Into bile, synovial and pleural fluids, bronchial secretions;
also distributes to peritoneal and pericardial fluids; crosses the placenta and
appears in breast milk; penetrates the blood-brain barrier only when meninges
are inflamed
Metabolism: In the liver to active metabolites
Half-life: Children 1 week to 2 years: 0.9-1.8 hours; Adults: 23-60 minutes
(prolonged with reduced renal function and in neonates)
Time to peak serum concentration: Oral: Within 2 hours; I.M.: Within 30-60
minutes
Elimination: By kidneys and to small degree the bile as parent drug and
metabolites |
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Usual Dosage |
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Neonates: I.M., I.V.:
Postnatal age <7 days:
<2000 g: 25 mg/kg/dose every 12 hours
>2000 g: 25 mg/kg/dose every 8 hours
Postnatal age >7 days:
<1200 g: 25 mg/kg/dose every 12 hours
1200-2000 g: 30 mg/kg/dose every 8 hours
>2000 g: 37.5 mg/kg/dose every 6 hours
Infants and Children:
Oral: 50-100 mg/kg/day divided every 6 hours
I.M., I.V.: 150-200 mg/kg/day in divided doses every 6 hours; maximum dose:
12 g/day
Adults:
Oral: 500-1000 mg every 4-6 hours for at least 5 days
I.M., I.V.: 250 mg to 2 g/dose every 4-6 hours
Dosing adjustment in renal impairment: Clcr <10
mL/minute: Use lower range of the usual dosage
Hemodialysis: Not dialyzable (0% to 5%) |
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Dietary
Considerations |
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Should be administered orally on an empty stomach 1 hour before meals or 2
hours after meals; presence of food decreases GI absorption of
oxacillin |
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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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May interfere with urinary glucose tests using cupric sulfate (Benedict's
solution, Clinitest®); may inactivate aminoglycosides
in vitro; false-positive urinary and serum proteins |
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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 development of oral
candidiasis |
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Patient
Information |
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Take at regular intervals around-the-clock, preferably on empty stomach with
a 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, difficulty breathing, or
skin rash. Notify prescriber if condition does not respond to
treatment. |
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Nursing
Implications |
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Administer around-the-clock rather than 4 times/day, 3 times/day, etc, (ie,
12-6-12-6, not 9-1-5-9) to promote less variation in peak and trough serum
levels; I.M. injections should be administered deep into a large muscle mass
such as the gluteus maximus; can be administered by I.V. push over 10 minutes at
a maximum concentration of 100 mg/mL or by I.V. intermittent infusion over 15-30
minutes at a final concentration less than or equal to 40 mg/mL
Monitor periodic CBC, urinalysis, BUN, serum creatinine, AST and ALT
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Dosage Forms |
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Capsule, as sodium: 250 mg, 500 mg
Powder:
For injection, as sodium: 250 mg, 500 mg, 1 g, 2 g, 4 g, 10 g
For oral solution, as sodium: 250 mg/5 mL (100 mL) |
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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.
Olans RN and Weiner LB, "Reversible Oxacillin Hepatotoxicity," J
Pediatr, 1976, 89(5):835-8.
Prober CG, Stevenson DK, and Benitz WE,
"The Use of Antibiotics in Neonates Weighing Less Than 1200 Grams," Pediatr
Infect Dis J, 1990, 9(2):111-21.
Wright AJ, "The Penicillins," Mayo Clin Proc, 1999, 74(3):290-307.
Yoshikawa TT, "Antimicrobial Therapy for the Elderly Patient," J Am
Geriatr Soc, 1990, 38(12):1353-72.
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