TY - JOUR
T1 - Dose-dependent effects of glyburide on insulin secretion and glucose uptake in humans
AU - Groop, Leif C.
AU - Barzilai, Nir
AU - Ratheiser, Klaus
AU - Luzi, Livio
AU - Wåhlin-Boll, Elisabeth
AU - Melander, Arne
AU - DeFronzo, Ralph A.
PY - 1991/8
Y1 - 1991/8
N2 - Objective: To examine the relationship between plasma glyburide concentrations (0, 50, 100, 200, 400, and 800 nM) and the insulin response and glucose metabolism during euglycemic (4.6 ± 0.1 mM) and hyperglycemic (11.6 ± 0.2 mM) conditions. Research Design and Methods: Nine healthy subjects participated in the study. Steady-state plasma glyburide concentrations were achieved by primed continuous intravenous infusion of glyburide. Results: During both euglycemia and hyperglycemia, glyburide enhanced insulin secretion and glucose disposal only to drug levels of 100-200 nM corresponding to an oral dose ≤10 mg. Conclusions: The data suggest that glyburide (and probably other sulfonylureas) operates within a narrow range of plasma concentrations (50-200 nM), which can be achieved with very low doses of the drug. It remains to be shown whether the threshold of maximal effect also in clinical practice is achieved with lower sulfonylurea doses than that currently used.
AB - Objective: To examine the relationship between plasma glyburide concentrations (0, 50, 100, 200, 400, and 800 nM) and the insulin response and glucose metabolism during euglycemic (4.6 ± 0.1 mM) and hyperglycemic (11.6 ± 0.2 mM) conditions. Research Design and Methods: Nine healthy subjects participated in the study. Steady-state plasma glyburide concentrations were achieved by primed continuous intravenous infusion of glyburide. Results: During both euglycemia and hyperglycemia, glyburide enhanced insulin secretion and glucose disposal only to drug levels of 100-200 nM corresponding to an oral dose ≤10 mg. Conclusions: The data suggest that glyburide (and probably other sulfonylureas) operates within a narrow range of plasma concentrations (50-200 nM), which can be achieved with very low doses of the drug. It remains to be shown whether the threshold of maximal effect also in clinical practice is achieved with lower sulfonylurea doses than that currently used.
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U2 - 10.2337/diacare.14.8.724
DO - 10.2337/diacare.14.8.724
M3 - Article
C2 - 1954808
AN - SCOPUS:0025883121
SN - 0149-5992
VL - 14
SP - 724
EP - 727
JO - Diabetes care
JF - Diabetes care
IS - 8
ER -