Liraglutide is a GLP-1 analog used in the management of type 2 diabetes mellitus and prevention of cardiovascular complications associated with diabetes.
Victoza, a formulation of liraglutide used in diabetes, intended for weight loss, is indicated as an adjunct to diet and exercise to improve glycemic control in patients ≥10 years old with type 2 diabetes mellitus. It is also indicated to reduce the risk of major adverse cardiovascular events in adult patients with type 2 diabetes and established cardiovascular disease.
Liraglutide is also available in combination with insulin degludec as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus.
Liraglutide is made by attaching a C-16 fatty acid (palmitic acid) with a glutamic acid spacer on the remaining lysine residue at position 26 of the peptide precursor. Liraglutide was granted FDA approval on January 25, 2010.
Liraglutide is a once-daily GLP-1 derivative for the treatment of type 2 diabetes. The prolonged action of liraglutide is achieved by attaching a fatty acid molecule at position 26 of the GLP-1 molecule, enabling it to bind reversibly to albumin within the subcutaneous tissue and bloodstream and be released slowly over time.
Binding with albumin results in slower degradation and reduced elimination of liraglutide from the circulation by the kidneys compared to GLP-1. The effect of liraglutide is the increased secretion of insulin and decreased secretion of glucagon in response to glucose as well as slower gastric emptying.
Liraglutide also does not adversely affect glucagon secretion in response to low blood sugar.
Liraglutide is an acylated synthetic glucagon-like peptide-1 analog. Liraglutide is an agonist of the glucagon-like peptide-1 receptor which is coupled to adenylate cyclaseLabel. The increase in cyclic AMP stimulates the glucose dependant release of insulin, inhibits the glucose dependant release of glucagon, and slows gastric emptying to increase control of blood sugar.
Metabolism: Liraglutide is less sensitive to metabolism than the endogenous GLP-1 and so is more slowly metabolized by dipeptidyl peptidase-4 and neutral endopeptidase to various smaller polypeptides which have not all been structurally determined. A portion of Liraglutide may be completely metabolized to carbon dioxide and water.
Absorption: Bioavailability of liraglutide after subcutaneous injection is approximately 55% and maximum concentrations are reached after 11.7 hours.
Route of elimination: 6% excreted in urine and 5% excreted in feces.
Half life: Terminal half life of 13 hours.
All medicines may cause side effects, but many people have no, or minor, side effects.Some medical conditions may interact with Liraglutide.
Tell your doctor or pharmacist if you have any medical conditions.
There is no clinical significance of race or ethnicity on the safety or efficacy of liraglutide. Geriatric patients do not experience clinically significant differences in pharmacokinetics though patients at an especially advanced age may be more susceptible to adverse effects. Female patients have reduced clearance of liraglutide but no dose adjustment is necessary. The risk and benefit of liraglutide in pregnancy must be weighed before prescribing.
This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider.
