Cloxacillin

Pronunciation

(kloks a SIL in)

Synonyms

Cloxacillin Sodium

Generic Available

Yes

Canadian Brand Names

Apo-Cloxi®; Novo-Cloxin; Nu-Cloxi; Riva-Cloxacillin

Use

Treatment of susceptible bacterial infections, notably penicillinase-producing staphylococci causing respiratory tract, skin and skin structure, bone and joint, urinary tract infections

Use - Dental

Treatment of susceptible orofacial infections (notably penicillinase-producing staphylococci)

Restrictions

Not available in U.S.

Pregnancy Risk Factor

Lactation

Excretion in breast milk unknown

Contraindications

Hypersensitivity to cloxacillin, any component of the formulation, 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, seizure 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

Methotrexate: Penicillins may increase the exposure to methotrexate during concurrent therapy; monitor.

Oral contraceptives: Anecdotal reports suggesting decreased contraceptive efficacy with penicillins have been refuted by more rigorous scientific and clinical data.

Probenecid, disulfiram: May increase levels of penicillins (cloxacillin)

Warfarin: Effects of warfarin may be increased

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: Widely to most body fluids and bone; penetration into cells, into eye, and across normal meninges is poor; crosses placenta; enters breast milk; inflammation increases amount that crosses blood-brain barrier

Protein binding: 90% to 98%

Metabolism: Extensively hepatic to active and inactive metabolites

Half-life elimination: 0.5-1.5 hours; prolonged with renal impairment and in neonates

Time to peak, serum: 0.5-2 hours

Excretion: Urine and feces

Dosage

Oral:

Children >1 month (<20 kg): 50-100 mg/kg/day in divided doses every 6 hours; up to a maximum of 4 g/day

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

Hemodialysis: Not dialyzable (0% to 5%)

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

Dietary Considerations

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

Sodium content of 250 mg capsule: 13.8 mg (0.6 mEq)

Sodium content of suspension 5 mL of 125 mg/5 mL: 11 mg (0.48 mEq)

Patient Education

Take 1 hour before or 2 hours after meals with water. Finish all medication; do not skip doses. Take around-the-clock. If you have diabetes, drug may cause false test results with Clinitest® urine glucose monitoring; use of glucose oxidase methods (Clinistix®) or serum glucose monitoring is preferable. 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 precaution: Inform prescriber if breast-feeding.

Nursing Implications

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

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

Rare reports of agranulocytosis; use caution with clozapine and carbamazepine

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.

International Brand Names

Apo-Cloxi® (CA); Cloxacilina® (CL); Cloxam® (TH); Cloxapen® (CL); Cloxgen® (TH); Navaclox® (BD); Novo-Cloxin (CA); Nu-Cloxi (CA); Omniclox® (BD); Orbenil® (IL); Orbenin® (HR, KW, LU, SI, TH); Riva-Cloxacillin (CA); T-Clox® (BD); Theraclox® (TH); Ultraxin® (BG, JO, KW, LB, MA, MY, SY); Vaclox ® (TH)

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