INSULIN SECRETAGOGUE: D-PHENYLALANINE DERIVATIVE
Nateglinide, aD-phenylalanine
derivative, is the latest insulinsecretagogue to become clinically available.
Nateglinide stimulates very rapid and transient release of insulin from beta
cells through closure of the ATP-sensitive K+ channel. It also
partially restores initial insulin release in response to an intravenous
glucose toler-ance test. This may be a significant advantage of the drug
because type 2 diabetes is associated with loss of this initial insulin
response. The restoration of more normal insulin secretion may suppress
glucagon release early in the meal and result in less endogenous or hepatic
glucose production. Nateglinide may have a special role in the treatment of
individuals with isolated post-prandial hyperglycemia, but it has minimal
effect on overnight or fasting glucose levels. Nateglinide is efficacious when
given alone or in combination with nonsecretagogue oral agents (such as
met-formin). In contrast to other insulin secretagogues, dose titration is not
required.
Nateglinide is
ingested just before meals. It is absorbed within 20 minutes after oral
administration with a time to peak concen-tration of less than 1 hour and is
metabolized in the liver by CYP2C9 and CYP3A4 with a half-life of about 1 hour.
The over-all duration of action is about 4 hours. Nateglinide amplifies the
insulin secretory response to a glucose load, but it has a markedly diminished
effect in the presence of normoglycemia. The incidence of hypoglycemia with
nateglinide may be the lowest of all the secretagogues, and nateglinide has the
advantage of being safe in those with very reduced renal function.
Related Topics
Privacy Policy, Terms and Conditions, DMCA Policy and Compliant
Copyright © 2018-2026 BrainKart.com; All Rights Reserved. Developed by Therithal info, Chennai.