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Oxacillin
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Test Interactions
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(oks a SIL in)

U.S. Brand Names
Bactocill®

Generic Available

Yes


Synonyms
Methylphenyl Isoxazolyl Penicillin; Oxacillin Sodium

Pharmacological Index

Antibiotic, Penicillin


Use

Treatment of infections such as osteomyelitis, septicemia, endocarditis, and CNS infections caused by susceptible strains of Staphylococcus


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to oxacillin or other penicillins or any component


Warnings/Precautions

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


Adverse Reactions

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


Overdosage/Toxicology

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


Drug Interactions

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


Stability

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


Mechanism of Action

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.


Pharmacodynamics/Kinetics

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


Usual Dosage

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%)


Dietary Considerations

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


Monitoring Parameters

Observe for signs and symptoms of anaphylaxis during first dose


Test Interactions

May interfere with urinary glucose tests using cupric sulfate (Benedict's solution, Clinitest®); may inactivate aminoglycosides in vitro; false-positive urinary and serum proteins


Mental Health: Effects on Mental Status

Penicillins reported to cause apprehension, illusions, hallucinations, depersonalization, agitation, insomnia, and encephalopathy


Mental Health: Effects on Psychiatric Treatment

May cause neutropenia; use caution with clozapine and carbamazepine


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

Prolonged use of penicillins may lead to development of oral candidiasis


Patient Information

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.


Nursing Implications

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


Dosage Forms

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)


References

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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