The penetration of ceftibuten into the respiratory tract.
OBJECTIVE
To determine the penetration of ceftibuten into various respiratory tissues and fluids.


METHODS
Single-dose, open-label, pharmacokinetic study.


METHODS
Veterans Administration Medical Center.


METHODS
Twelve hospitalized men aged 34 to 75 years with a variety of noninfectious pulmonary symptoms/diseases.


METHODS
Patients received a single oral dose of ceftibuten, 200 mg, prior to undergoing diagnostic fiberoptic bronchoscopy. Plasma samples for the determination of ceftibuten concentrations were collected pretreatment and up to 12 h postdosing. Nasal secretions, tracheal secretions, BAL fluid, and lung tissue from a biopsy were obtained at bronchoscopy from 2 to 7 h postdosing.


RESULTS
Mean pharmacokinetic parameters for ceftibuten in plasma were the following: maximum observed plasma concentration (Cmax), 8.77 microg/mL; time to reach Cmax, 2.2 h; area under the plasma concentration-time curve extraploated to infinity, 49.21 microg/h/mL; and terminal elimination half-life, 3.17 h. These parameters were similar to those obtained in studies using healthy volunteers. Mean penetration of ceftibuten into nasal, tracheal, and bronchial secretions was 47%, 50%, and 30%, respectively. Mean penetration into BAL fluid was 81%, whereas penetration into lung tissue was 39%. No patient experienced any adverse effects related to ceftibuten.


CONCLUSIONS
Ceftibuten penetrates well into various tissues and fluids of the upper and lower respiratory tracts. The results support the activity of ceftibuten in the treatment of upper and lower respiratory tract infections.
Krumpe
P
P
Department of Pulmonary Medicine, VA Medical Center, Reno, NV 89520, USA.
Lin
C C
CC
Radwanski
E
E
Cayen
M N
MN
Affrime
M B
MB
D000328:Adult; D000368:Aged; D001992:Bronchoalveolar Lavage Fluid; D001999:Bronchoscopy; D000077722:Ceftibuten; D002511:Cephalosporins / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D008875:Middle Aged; D012137:Respiratory System / Q000378:metabolism*; D012140:Respiratory Tract Diseases / Q000378:metabolism*; D014018:Tissue Distribution
D002511:Cephalosporins; D000077722:Ceftibuten