Look Up > Drugs > Cloxacillin
Cloxacillin
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
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
(kloks a SIL in)

U.S. Brand Names
Cloxapen®; Tegopen®

Generic Available

Yes


Canadian Brand Names
Apo®-Cloxi; Novo-Cloxin; Nu-Cloxi; Orbenin®; Taro-Cloxacillin®

Synonyms
Cloxacillin Sodium

Pharmacological Index

Antibiotic, Penicillin


Use

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


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to cloxacillin or any component, or penicillins


Warnings/Precautions

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


Adverse Reactions

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


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

Increased effect: Disulfiram, probenecid may increase penicillin levels, increased effect of anticoagulants


Stability

Refrigerate oral solution after reconstitution; discard after 14 days; stable for 3 days 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: ~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


Usual Dosage

Oral:

Children (>20 kg) and Adults: 250-500 mg every 6 hours

Hemodialysis: Not dialyzable (0% to 5%)


Dietary Considerations

Should be taken 1 hour before or 2 hours after meals with water


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 urine and serum proteins; false-positive in uric acid, urinary steroids


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

Rare reports of agranulocytosis; 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 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.


Nursing Implications

Monitor CBC with differential, urinalysis, BUN, serum creatinine, and liver enzymes


Dosage Forms

Capsule, as sodium: 250 mg, 500 mg

Powder for oral suspension, as sodium: 125 mg/5 mL (100 mL, 200 mL)


References

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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