Pharmacokinetic disposition of 14C-glyburide in patients with varying renal function.
The pharmacokinetics of 14C-labeled glyburide were studied in 13 men with varying degrees of renal impairment. Patients received a single, 5 mg oral dose of glyburide as a solution (10 microCi/ml/mg) after a high-carbohydrate breakfast. Serial plasma and breath samples were collected for 48 hours and urine and feces were collected for 5 to 7 days. Patients with normal to moderately impaired renal function (creatinine clearance [CLCR] of 29 to 131 ml/min/1.7 m2) had glyburide plasma t1/2 values of 2.0 to 5.0 hours, with no relationship between CLCR and glyburide clearance. One subject with severe renal impairment (CLCR = 5 ml/min/1.7 m2) had decreased glyburide clearance that resulted in a t1/2 of 11 hours. The elimination of metabolites was more dependent on renal status but was only significantly affected in the patient with severe renal impairment.
Pearson
J G
JG
Antal
E J
EJ
Raehl
C L
CL
Gorsch
H K
HK
Craig
W A
WA
Albert
K S
KS
Welling
P G
PG
D000042:Absorption; D000284:Administration, Oral; D000328:Adult; D000368:Aged; D001944:Breath Tests; D002250:Carbon Radioisotopes; D002851:Chromatography, High Pressure Liquid; D003404:Creatinine / Q000032:analysis; D005243:Feces / Q000032:analysis; D005905:Glyburide / Q000097:blood / Q000378:metabolism* / Q000652:urine; D006801:Humans; D007668:Kidney / Q000378:metabolism; D007674:Kidney Diseases / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D008875:Middle Aged
D002250:Carbon Radioisotopes; D003404:Creatinine; D005905:Glyburide