Chemical Properties
Exenatide acetate is White Solid
Uses
Application of exenatide
acetate causes an increase in acinar cAMP without stimulating amylase release. As an incretin mimetic, exenatide
acetate acts as agonist of the glucagon-like peptide-1 (GLP-1) receptor. As GLP-1, though with prolonged activity, exenatide
acetate augments the postprandial production of insulin and suppresses secretion of glucagon. For this reason, exenatide
acetate has found use as a medication of diabetes II.
Uses
A 39-amino acid peptide originally isolated from the salivary glands of the Gila monster (Heloderma suspectum), differs from exendin-3 only in two positions close to the N-terminus. Application of exenatide causes an increase in acinar cAMP without stimulating amylase release. As an incretin mimetic, exenatide acts as agonist of the glucagon-like peptide-1 (GLP-1) receptor. As GLP-1, though with prolonged activity, exenatide augments the postprandial production of insulin and suppresses secretion of glucagon. For this reason, exenatide has found use as a medication of diabetes II.
Clinical Use
39-peptide known as an incretin mimetic;
an agonist of glucagon-like peptide-1,
used adjunctively in type II diabetes
mellitus.
Drug interactions
Potentially hazardous interactions with other drugs
Anticoagulants: possibly enhances anticoagulant
effect of warfarin.
Other nephrotoxins: avoid concomitant use.
Metabolism
Exenatide is eliminated through the kidneys by
glomerular filtration followed by proteolytic degradation.
Description
Exenatide is a single, non-glycosylated, peptide containing 39 amino acids and having a molecular mass of 4186.6 Dalton. Exenatide has the empirical formula C
184H
282N
50O
60S.
Background
Exenatide Derived from the saliva of the gila monster, is a 39 amino acid peptide that mimics the GLP-1 incretin, an insulin secretagogue with glucoregulatory effects. Typical responses to exenatide include improvements in the initial rapid release of endogenous insulin, suppression of glucagon release by the pancreas, regulation of gastric empyting, and reduced appetite - all of which function to lower blood glucose. Exenatide is self-regulating in that it lowers blood sugar when levels are elevated but does not continue to lower blood sugar when levels return to normal, unlike with sulfonylureas or insulins.
