Ceftibuten: An Overview

Abstract

Ceftibuten is an orally active third‐generation cephalosporin that exhibits good microbiologic activity against many gram‐negative and select gram‐positive organisms. It is stable against plasmid‐mediated β‐lactamases, including extended‐spectrum β‐lactamases. Ceftibuten has been shown to be effective in the treatment of upper and lower respiratory tract infections and, although not approved indications, complicated and uncomplicated urinary tract infections in both adults and children. It is readily absorbed (75–90%) after oral administration, with peak serum levels of 17 μg/ml in healthy volunteers. Its half‐life is 2.5 hours in healthy volunteers and is increased in elderly patients to approximately 3.2 hours. Elimination occurs primarily through the kidneys, requiring dosage adjustments to be made when creatinine clearance falls below 50 ml/minute. The drug's safety profile is favorable and similar to that of most other cephalosporins. Based on pharmacokinetic information and clinical trial data, ceftibuten can be dosed once/day for most infections. It is an alternative to other currently available antimicrobial agents in the treatment of indicated upper and lower respiratory tract infections.

A phase I, randomized, double-blind, placebo-controlled, ascending single- and multiple-dose study of the pharmacokinetics, safety, and tolerability of oral ceftibuten in healthy adult subjects

“…Ceftibuten is a cephalosporin antibiotic approved in the USA ( 4 ) for acute exacerbations of chronic bronchitis, acute bacterial otitis media, and pharyngitis/tonsillitis at a dose of 400 mg once-daily for up to 10 days ( 5 – 7 ). The safety profile of ceftibuten is similar to other cephalosporin antibiotics with nausea (4%), headache (3%), diarrhea (3%), dyspepsia (2%) and dizziness, abdominal pain, and vomiting (all 1%) being the most common adverse reactions in the US Food and Drug Administration label ( 8 ).…”

“…The pharmacokinetics (PK) of ceftibuten has been characterized in single- and multiple-dose studies in the range of 25–800 mg ( 9 – 16 ). Previous studies have shown that ceftibuten is very well absorbed after oral administration of doses up to 400 mg, with a bioavailability between 75% and 90% ( 6 , 7 , 13 , 16 ). Maximum plasma concentrations are reached within 2–3 h ( 9 , 12 , 14 ).…”