Glyburide
The decrease of glyburide in the serum of normal healthy individuals is biphasic;
the terminal half-life is about 10 hours. The major metabolite of glyburide
is the 4-trans-hydroxy derivative. A second metabolite, the 3-cis-hydroxy
derivative, also occurs. These metabolites probably contribute no significant
hypoglycemic action in humans since they are only weakly active (1/400
th and 1/40th as active, respectively, as glyburide) in rabbits. Glyburide
is excreted as metabolites in the bile and urine, approximately 50% by each
route. This dual excretory pathway is qualitatively different from that of other sulfonylureas, which are excreted primarily in the urine.
Metformin hydrochloride
Intravenous single-dose studies in normal subjects demonstrate that metformin
is excreted unchanged in the urine and does not undergo hepatic metabolism
(no metabolites have been identified in humans) nor biliary excretion. Renal
clearance (see Table 1) is approximately 3.5 times greater than creatinine clearance,
which indicates that tubular secretion is the major route of metformin elimination. Following
oral administration, approximately 90% of the absorbed drug is eliminated via
the renal route within the first 24 hours, with a plasma elimination half-life
of approximately 6.2 hours. In blood, the elimination half-life is approximately
17.6 hours, suggesting that the erythrocyte mass may be a compartment of distribution.
Glucovance
Pregnancy
Metabolism and elimination
Patients with type 2 diabetes
Hypoglycemia
Mechanism of action
Metformin hydrochloride
Information for patients
Drug interactions
Overdosage
Glipizide (glucotrol)
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