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Pronunciation
(dye kloks a SIL in)
Generic Available (U.S.)
Yes
Index Terms
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment of systemic infections such as pneumonia, skin and soft tissue infections, and osteomyelitis caused by penicillinase-producing staphylococci
Use: Dental
Treatment of susceptible orofacial infections (notably penicillinase-producing staphylococci)
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse events have not been observed in animal studies; therefore, dicloxacillin is classified as pregnancy category B. Dicloxacillin crosses the placenta. Teratogenic effects have not been reported with dicloxacillin, but adequate and well-controlled studies of dicloxacillin have not been completed in pregnant women. Other penicillins are considered safe for use in pregnancy.
Lactation
Excretion in breast milk unknown/use caution
Breast-Feeding Considerations
It is not known if dicloxacillin crosses into human milk. The manufacturer recommends that caution be exercised when administering dicloxacillin to nursing women. Other penicillins distribute into human milk and are considered safe for use during breast-feeding. Nondose-related effects could include modification of bowel flora.
Contraindications
Hypersensitivity to dicloxacillin, penicillin, or any component of the formulation
Warnings/Precautions
Concerns related to adverse effects:
• Anaphylactoid/hypersensitivity reactions: Serious and occasionally severe or fatal hypersensitivity (anaphylactoid) reactions have been reported in patients on penicillin therapy, especially with a history of beta-lactam hypersensitivity, history of sensitivity to multiple allergens, or previous IgE-mediated reactions (eg, anaphylaxis, angioedema, urticaria). Use with caution in asthmatic patients.
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis.
Concurrent drug therapy issues:
• Warfarin: Monitor PT if patient is concurrently on warfarin.
Special populations:
• Neonates: Use with caution in neonates; elimination of drug is slow.
Adverse Reactions
1% to 10%: Gastrointestinal: Nausea, diarrhea, abdominal pain
<1%: Agranulocytosis, anemia, BUN/creatinine increased, eosinophilia, fever, hematuria, hemolytic anemia, hepatotoxicity, hypersensitivity, interstitial nephritis, leukopenia, LFTs increased (transient), neutropenia, prolonged PT, pseudomembranous colitis, rash (maculopapular to exfoliative), seizure with extremely high doses and/or renal failure, serum sickness-like reactions, thrombocytopenia, vaginitis, vomiting
Metabolism/Transport Effects
Induces CYP3A4 (weak/moderate)
Drug Interactions
ARIPiprazole: CYP3A4 Inducers may decrease the serum concentration of ARIPiprazole. Management: Double aripiprazole dose when initiating concomitant therapy with a CYP3A4 inducer (e.g., carbamazepine). Monitor response and adjust aripiprazole dose as clinically indicated. If CYP3A4 inducer is discontinued, reduce aripiprazole dose to 10-15 mg/day. Risk D: Consider therapy modification
Axitinib: CYP3A4 Inducers (Weakly to Moderately Effective) may decrease the serum concentration of Axitinib. Risk X: Avoid combination
BCG: Antibiotics may diminish the therapeutic effect of BCG. Risk X: Avoid combination
Fusidic Acid: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification
Methotrexate: Penicillins may decrease the excretion of Methotrexate. Risk C: Monitor therapy
Mycophenolate: Penicillins may decrease serum concentrations of the active metabolite(s) of Mycophenolate. This effect appears to be the result of impaired enterohepatic recirculation. Risk C: Monitor therapy
Probenecid: May increase the serum concentration of Penicillins. Risk C: Monitor therapy
Saxagliptin: CYP3A4 Inducers may decrease the serum concentration of Saxagliptin. Risk C: Monitor therapy
Tetracycline Derivatives: May diminish the therapeutic effect of Penicillins. Risk D: Consider therapy modification
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 24 hours after cessation of antibacterial agents. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Dicloxacillin may diminish the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Vitamin K Antagonists (eg, warfarin): Penicillins may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Food: Food decreases drug absorption rate and serum concentration. Management: Administer around-the-clock on an empty stomach with a large glass of water 1 hour before or 2 hours after meals.
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: 35% to 76%; rate and extent reduced by food
Distribution: Throughout body with highest concentrations in kidney and liver; CSF penetration is low
Protein binding: 96%
Half-life elimination: 0.6-0.8 hour; slightly prolonged with renal impairment
Time to peak, serum: 0.5-2 hours
Excretion: Feces; urine (56% to 70% as unchanged drug); prolonged in neonates
Dosage
Usual dosage range:
Newborns: Use not recommended
Children <40 kg: Oral: 12.5-100 mg/kg/day divided every 6 hours
Children >40 kg: Oral: 125-250 mg every 6 hours
Adults: Oral: 125-1000 mg every 6 hours
Indication-specific dosing:
Children: Oral:
Furunculosis: 25-50 mg/kg/day divided every 6 hours
Osteomyelitis: 50-100 mg/kg/day in divided doses every 6 hours
Adults: Oral:
Erysipelas, furunculosis, mastitis, otitis externa, septic bursitis, skin abscess: 500 mg every 6 hours
Impetigo: 250 mg every 6 hours
Prosthetic joint (long-term suppression therapy): 250 mg twice daily
Staphylococcus aureus,
methicillin susceptible infection if no I.V. access: 500-1000 mg every 6-8 hours
Dosage adjustment in renal impairment: Not necessary
Hemodialysis: Not dialyzable (0% to 5%); supplemental dosage not necessary
Peritoneal dialysis: Supplemental dosage not necessary
Continuous arteriovenous or venovenous hemofiltration: Supplemental dosage not necessary
Dental Usual Dosing
Susceptible orofacial infections: Children >40 kg and Adults: 125-250 mg every 6 hours
Administration: Oral
Administer 1 hour before or 2 hours after meals. Administer around-the-clock to promote less variation in peak and trough serum levels.
Monitoring Parameters
Monitor prothrombin time if patient concurrently on warfarin; monitor for signs of anaphylaxis during first dose
Test Interactions
False-positive urine and serum proteins; false-positive in uric acid, urinary steroids; may interfere with urinary glucose tests using cupric sulfate (Benedict's solution, Clinitest®); may inactivate aminoglycosides in vitro
Dietary Considerations
Administer on an empty stomach 1 hour before or 2 hours after meals. Some products may contain sodium.
Patient Education
Take medication with a large glass of water 1 hour before or 2 hours after meals. Take at regular intervals around-the-clock. May cause some gastric distress and diarrhea. Report fever, vaginal itching, persistent diarrhea, sores in the mouth, loose foul-smelling stools, yellowing of skin or eyes, or change in color of urine or stool.
Geriatric Considerations
No dosage adjustment for renal function is necessary.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Prolonged use of penicillins may lead to development of oral candidiasis.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Penicillins have been reported to cause apprehension, illusions, agitation, insomnia, depersonalization, and encephalopathy
Mental Health: Effects on Psychiatric Treatment
Rarely may cause agranulocytosis; use caution with clozapine and carbamazepine
Nursing: Physical Assessment/Monitoring
Assess allergy history prior to beginning therapy.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, oral: 250 mg, 500 mg
Pricing: U.S. (www.drugstore.com)
Capsules (Dicloxacillin Sodium)
250 mg (30): $18.99
500 mg (30): $24.99
References
Donowitz GR and Mandell GL, “Beta-Lactam Antibiotics,” N Engl J Med, 1988, 318(7):419-26 and 318(8):490-500.
Pacifici GM, Viani A, Taddeucci-Brunelli G, et al, “Plasma Protein Binding of Dicloxacillin: Effects of Age and Diseases,” Int J Clin Pharmacol Ther Toxicol, 1987, 25(11):622-6.
Wright AJ, “The Penicillins,” Mayo Clin Proc, 1999, 74(3):290-307.
International Brand Names
Lexi-Comp.com
Last full review/revision March 2012
Content last modified March 2012
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