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- W2064757739 abstract "Persistent hypoglycemia is a serious condition that is frequently reported in patients undergoing sulfonylurea treatment, often necessitating hospitalization in the event of overdose. Somatostatin is a regulatory hormone with a broad range of physiological actions that include the inhibition of insulin and glucagon secretion, predominantly via activation of the somatostatin receptor subtypes sstr<sub>5</sub> and sstr<sub>2</sub>, respectively. Previous studies have demonstrated that octreotide, a potent somatostatin analogue with high affinity for sstr<sub>2</sub> and moderate affinity for sstr<sub>5</sub>, significantly increases serum glucose levels and prevents recurrence of hypoglycemic episodes in patients with sulfonylurea-induced hypoglycemia. Pasireotide (SOM230) is a multireceptor-targeted somatostatin analogue with a 39-, 30- and 5-fold higher binding affinity for sstr<sub>5</sub>, sstr<sub>1</sub> and sstr<sub>3</sub>, respectively, and a slightly lower (0.4-fold) affinity for sstr<sub>2</sub> compared with octreotide. This study evaluated the effects of pasireotide and octreotide in rats with glyburide-induced hypoglycemia. In fasted rats, pasireotide (10 and 30 µg/kg) prevented glyburide-induced hypoglycemia in a dose-dependent manner for up to 6 h. Qualitatively similar results were observed in non-fasted rats. However, the antihypoglycemic effect of pasireotide was stronger in non-fasted rats, resulting in transient hyperglycemia. In contrast to pasireotide, octreotide 10 µg/kg did not prevent glyburide-induced hypoglycemia in fasted and non-fasted rats, while octreotide 30 µg/kg resulted in small but significant increases in blood glucose at 3 h post-dose only. These findings suggest that pasireotide could have a more potent effect than octreotide in the management of patients with severe hypoglycemia caused by hyperinsulinemia." @default.
- W2064757739 created "2016-06-24" @default.
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- W2064757739 date "2015-02-06" @default.
- W2064757739 modified "2023-09-27" @default.
- W2064757739 title "Pasireotide (SOM230) Prevents Sulfonylurea-induced Hypoglycemia in Rats" @default.
- W2064757739 doi "https://doi.org/10.1055/s-0034-1398552" @default.
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