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Pronunciation |
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(kloks
a SIL
in) |
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U.S. Brand
Names |
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Cloxapen®;
Tegopen® |
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Generic
Available |
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Yes |
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Canadian Brand
Names |
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Apo®-Cloxi; Novo-Cloxin; Nu-Cloxi;
Orbenin®; Taro-Cloxacillin® |
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Synonyms |
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Cloxacillin Sodium |
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Pharmacological Index |
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Antibiotic, Penicillin |
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Use |
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Dental: Treatment of susceptible orofacial infections, notably
penicillinase-producing staphylococci
Medical: Treatment of susceptible bacterial infections, notably
penicillinase-producing staphylococci causing respiratory tract, skin and skin
structure, bone and joint, urinary tract infections |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to cloxacillin or any component, or
penicillins |
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Warnings/Precautions |
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Monitor PT if patient concurrently on warfarin, elimination of drug is slow
in renally impaired; use with caution in patients allergic to cephalosporins due
to a low incidence of cross-hypersensitivity |
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Adverse
Reactions |
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1% to 10%: Gastrointestinal: Nausea, diarrhea, abdominal pain
<1%: Fever, seizures with extremely high doses and/or renal failure, rash
(maculopapular to exfoliative), vomiting, pseudomembranous colitis, vaginitis,
eosinophilia, leukopenia, neutropenia, thrombocytopenia, agranulocytosis,
anemia, hemolytic anemia, prolonged PT, hepatotoxicity, transient elevated LFTs,
hematuria, interstitial nephritis, increased BUN/creatinine, serum sickness-like
reactions, hypersensitivity |
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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
Increased effect: Disulfiram, probenecid may increase penicillin levels,
increased effect of anticoagulants |
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Stability |
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Refrigerate oral solution after reconstitution; discard after 14 days; stable
for 3 days 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: ~50%
Distribution: Crosses the placenta; appears in breast milk; distributed
widely to most body fluids and bone; penetration into cells, into the eye, and
across normal meninges is poor; inflammation increased amount that crosses the
blood-brain barrier
Protein binding: 90% to 98%
Metabolism: Significant in the liver to active and inactive metabolites
Half-life: 0.5-1.5 hours (prolonged with renal impairment and in neonates)
Time to peak serum concentration: Oral: Within 0.5-2 hours
Elimination: In urine and through bile |
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Usual Dosage |
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Oral:
Children (>20 kg) and Adults: 250-500 mg every 6 hours
Hemodialysis: Not dialyzable (0% to 5%) |
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Dietary
Considerations |
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Should be taken 1 hour before or 2 hours after meals with
water |
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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 urine and serum proteins; false-positive in uric
acid, urinary steroids |
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Mental Health: Effects
on Mental Status |
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Penicillins have been reported to cause apprehension, illusions, agitation,
insomnia, depersonalization, and encephalopathy |
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Mental Health:
Effects on Psychiatric
Treatment |
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Rare reports of agranulocytosis; 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 1 hour before or 2 hours after meals with water. Finish all medication;
do not skip doses. Take around-the-clock. 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. Immediately report any signs or
symptoms of anaphylactic reactions (eg, chills, fever, wheezing, tightness in
chest), excessive GI side effects, or signs or symptoms of opportunistic
infection (eg, white spots or sores in mouth, vaginal discharge or sores, fever,
fatigue, unhealed sores or wounds). Breast-feeding precautions: Inform
prescriber if breast-feeding. |
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Nursing
Implications |
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Monitor CBC with differential, urinalysis, BUN, serum creatinine, and liver
enzymes |
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Dosage Forms |
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Capsule, as sodium: 250 mg, 500 mg
Powder for oral suspension, as sodium: 125 mg/5 mL (100 mL, 200 mL)
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References |
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Bluhm G, Jacobson B, Julander I, et al,
"Antibiotic Prophylaxis in Pacemaker Surgery - A Prospective Study," Scand J
Thorac Cardiovasc Surg, 1984, 18(3):227-34.
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.
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