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Cefuroxime

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From Pharmacopedia
Cefuroxime (axetil oral, sodium IV)
Ceftin (oral), Zinacef (IV)

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Titration strategies

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Summary
Common uses
Acute otitis media0, Acute bacterial sinusitis0, Streptococcal pharyngitis0, Community-acquired pneumonia (mild outpatient)0, Lyme disease (alternative to doxycycline)0, Uncomplicated gonorrhea (with azithromycin, historical; ceftriaxone now preferred)0
Pharmacy
Starting dose
250-500 mg PO BID × 7-14 days; IV 1.5 g q8h for serious infections
Preparations
125, 250, 500 mg tablets; 125 mg/5 mL, 250 mg/5 mL suspension; 750 mg, 1.5 g IV vials
US FDA Max
1 g/d (oral); 6 g/d (IV)
Pharmacology
Routes
Oral, IV, IM
Onset
Hours
Duration
8-12 hours
Half-life
~1.5 hours[1]
Bioavailability
~37% (oral, as axetil prodrug; food modestly improves absorption)[1]
Pregnancy
Generally considered safe in pregnancy.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Cefuroxime axetil is a prodrug hydrolyzed by intestinal esterases to cefuroxime; like all β-lactams it binds penicillin-binding proteins (PBPs) and inhibits transpeptidation of peptidoglycan cross-links, producing bactericidal cell wall destabilization.0 Second-generation cephalosporin spectrum: improved gram-negative activity relative to first-generation cephalexin while retaining gram-positive activity and adding some β-lactamase stability. Cefuroxime crosses the blood-brain barrier sufficiently for Lyme disease but not reliably for bacterial meningitis (where third-generation agents are preferred)[1].

References

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  1. 1.0 1.1 1.2 FDA Prescribing Information, Ceftin (cefuroxime axetil), GSK, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050605s039lbl.pdf