Improvement of glucose tolerance by nateglinide occurs through enhancement of early phase insulin secretion

Uto, Yuko; Teno, Shinichi; Iwamoto, Yasuhiko; Omori, Yasue; Takizawa, Takao

doi:10.1053/meta.2002.29008

Cited by 12 publications

(4 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Secretory responsiveness was enhanced only at very high glucose concentration (30 m M ), making the effects of nateglinide very similar to other insulinotropic drugs such as sulphonylureas and repaglinide ( Hu et al ., 2001 ). These insulinotropic effects of nateglinide were mediated in non‐depolarized cells, and reflect the interaction of the drug with B‐cell K ATP channels ( Hansen et al ., 2002 ; Hu, 2002 ), producing a secretory response which likely underlies the restoration of early‐phase insulin secretion associated with nateglinide ( Hollander et al ., 2001 ; Uto et al ., 2002 ).…”

Section: Discussionmentioning

confidence: 99%

Acute and long‐term effects of nateglinide on insulin secretory pathways

Ball¹,

Flatt²,

McClenaghan³

2004

British J Pharmacology

View full text Add to dashboard Cite

1 Acute and chronic effects of the insulinotropic drug nateglinide upon insulin release were examined in the BRIN-BD11 cell line. 2 Nateglinide (10-400 mM) stimulated a concentration-dependent increase (Po0.05-Po0.001) in insulin release at a non-stimulatory (1.1 mM) glucose concentration. The insulinotropic response to 200 mM nateglinide was increased at 30 mM (Po0.01), but not 5.6-16.7 mM glucose concentrations. 3 In depolarized cells, nateglinide (50-200 mM) evoked K ATP channel-independent insulin secretion (Po0.05-Po0.001) in the absence and presence of 5.6-30.0 mM glucose (Po0.001). 4 Exposure for 18 h to 100 mM nateglinide abolished the acute insulinotropic effects of 200 mM nateglinide, tolbutamide or glibenclamide, but had no effect upon the insulinotropic effect of 200 mM efaroxan. 5 While 18 h exposure to 100 mM nateglinide did not affect basal insulin release or insulin release in the presence of 16.7 mM glucose, 25 mM forskolin or 10 nM PMA, significant inhibition of the insulinotropic effects of 20 mM leucine and 20 mM arginine were observed. 6 These data show that nateglinide stimulates both K ATP channel-dependent and-independent insulin secretion. The maintained insulinotropic effects of this drug with increasing glucose concentrations support the antihyperglycaemic actions of nateglinide in Type II diabetes. 7 Studies of the long-term effects of nateglinide indicate that nateglinide shares signalling pathways with sulphonylureas, but not the imidazoline efaroxan. This may be significant when considering a nateglinide treatment regimen, particularly in patients previously treated with sulphonylurea.

show abstract

Section: Discussionmentioning

confidence: 99%

Acute and long‐term effects of nateglinide on insulin secretory pathways

Ball¹,

Flatt²,

McClenaghan³

2004

British J Pharmacology

View full text Add to dashboard Cite

show abstract

“…No accumulation of the medication has been observed after 1 week at a dose of 120 mg three times a day [20]. Different studies have been performed with nateglinide in Europe [21], in North America [12,[22][23][24], and in Japan [25,26]; the present study is the only one that has been performed in patients recruited from five Latin American countries.…”

Section: Discussionmentioning

confidence: 81%

“…It has also been established that the early insulin secretion contributes more effectively than the total insulin secretion to the improvement of postprandial hyperglycemia in type 2 DM patients [26].…”

Section: Discussionmentioning

confidence: 99%

Evaluation of the Effects of Nateglinide on Postprandial Glycemia in Patients with Type 2 Diabetes mellitus: A Multicenter, Multinational, Non-Randomized, Non-Controlled Latin American Study

Islas-Andrade¹,

Revilla-Monsalve²,

Hurtado³

et al. 2003

Pharmacology

View full text Add to dashboard Cite

One hundred and sixteen Latin American type 2 diabetic patients previously only on a diet were enrolled in this multicenter, multinational, nonrandomized, noncontrolled study. Only 109 completed the study. After 8 weeks of treatment with 120 mg of nateglinide, administered prior to each meal, the postprandial (2 h) glucose concentration decreased to 85.11 ± 5.65 mg/dl (p < 0.0001), and HbA_1c values decreased to 1.06 ± 0.10% (p < 0.0001). No response differences were detected in relation to age, gender, or ethnicity, but we did encounter a better response in recently diagnosed patients (≤1 year). No serious adverse events were observed. We can, therefore, conclude that nateglinide is a well-tolerated, safe, and effective insulinotropic agent.

show abstract

“…Findings from such pre‐clinical studies have been confirmed in healthy volunteers 15 and in patients with type 2 diabetes 16,36,37 . Figure 4 depicts the results from one such study performed in newly diagnosed obese patients with type 2 diabetes.…”

Section: Mechanistic Studiesmentioning

confidence: 77%

Nateglinide (Starlix®): Update on a New Antidiabetic Agent

Dunning

2003

Int J Clinical Practice

View full text Add to dashboard Cite

SUMMARYNateglinide is a new oral antidiabetic agent that stimulates insulin release promptly after its pre‐meal administration in a strongly glucose‐dependent fashion. Because its insulinotropic effects are short in duration, nateglinide specifically targets postprandial hyperglycaemia with a low potential to elicit hypoglycaemia or sustained hyperinsulinaemia. Nateglinide has an excellent safety and tolerability profile, and its efficacy in reducing HbA1c in monotherapy (120 mg before meals) is comparable to that of metformin, sulphonylureas, thiazolidinediones or acarbose (−0.5 to −1.5%). When combined with metformin, which primarily reduces fasting glucose levels, nateglinide's effects are additive. In our clinical experience, nateglinide is a particularly good therapeutic option in newly diagnosed, treatment‐naive patients; elderly patients in whom hypoglycaemia is a concern; patients with kidney failure or mild hepatic impairment; patients taking low‐dose sulphonylureas who encounter problems with hypoglycaemia; and patients failing to achieve adequate glycaemic control on metformin or thiazolidinedione monotherapy.

show abstract

Improvement of glucose tolerance by nateglinide occurs through enhancement of early phase insulin secretion

Cited by 12 publications

References 0 publications

Acute and long‐term effects of nateglinide on insulin secretory pathways

Acute and long‐term effects of nateglinide on insulin secretory pathways

Evaluation of the Effects of Nateglinide on Postprandial Glycemia in Patients with Type 2 Diabetes mellitus: A Multicenter, Multinational, Non-Randomized, Non-Controlled Latin American Study

Nateglinide (Starlix®): Update on a New Antidiabetic Agent

Contact Info

Product

Resources

About