Objective: To review the pharmocology, pharmacokinetics, dosing guidelines,
adverse effects, drug interactions, and clinical efficacy of nateglinide.
Data Source: Primary and review articles regarding nateglinide were identif
ied by MEDLINE search (from 1966 to January 2001); abstracts were identifie
d through the Institute for Scientific Information Web of Science (from 199
5 to January 2001) and the American Diabetes Association; additional inform
ation was obtained from the nateglinide product information.
Study Selection/Data Extraction: All articles and meeting abstracts identif
ied from the data source were evaluated and all information deemed relevant
was included in this review. Much of the information was from abstracts or
the product labeling, since few clinical studies have been published in th
e medical literature.
Data Synthesis: Nateglinide is a novel nonsulfonylurea oral antidiabetic ag
ent that stimulates insulin secretion from the pancreas. It has a rapid ons
et and short duration of action, allowing administration before a meal to r
educe postprandial hyperglycemia. Improvement in glycemic control with nate
glinide monotherapy has been demonstrated in patients not previously treate
d with antidiabetic medications. Greater improvement in glycemic control wa
s observed when nateglinide was administered in combination with metformin.
Conclusions: Nateglinide is similar to repaglinide, but has a quicker onset
of action, quicker reversal, and does not usually require dosage titration
. Based on the pharmacodynamics of nateglinide and repaglinide, nateglinide
produces a more rapid postprandial increase in insulin secretion, and its
duration of response is shorter than that of repaglinide. The risk of posta
bsorptive hypoglycemia should be lower than with either sulfonylureas or re
paglinide.