Indications
Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist. It is used alongside diet and exercise to improve glycemic control in adults and in children aged 10 years and older who have type 2 diabetes mellitus. It is also used to reduce the risk of major adverse cardiovascular events in adults who have type 2 diabetes mellitus and established cardiovascular disease. Victoza, a brand of liraglutide, is a GLP-1 receptor agonist with the same uses. It is given as an adjunct to diet and exercise to improve glycemic control in adults and pediatric patients aged 10 years and older with type 2 diabetes mellitus, and to reduce the risk of major adverse cardiovascular events in adults with type 2 diabetes mellitus and established cardiovascular disease. Limitations of use: liraglutide is not for the treatment of type 1 diabetes mellitus. It should not be coadministered with other liraglutide-containing products.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Liraglutide is an acylated human Glucagon-Like Peptide-1 (GLP-1) receptor agonist. Its amino acid sequence is 97% homologous to endogenous human GLP-1(7-37), which makes up <20% of the total endogenous GLP-1 in circulation. Like GLP-1(7-37), liraglutide activates the GLP-1 receptor, a membrane-bound cell-surface receptor in pancreatic beta cells that is coupled to adenylyl cyclase by the stimulatory G-protein, Gs. This raises intracellular cyclic AMP (cAMP), and insulin is released when glucose concentrations are elevated. The insulin secretion subsides as blood glucose falls and approaches euglycemia. Liraglutide also decreases glucagon secretion in a glucose-dependent manner, and a delay in gastric emptying is part of how it lowers blood glucose.
GLP-1(7-37) has a half-life of 1.5 to 2 minutes, because the ubiquitous endogenous enzymes dipeptidyl peptidase IV (DPP-IV) and neutral endopeptidases (NEP) break it down. Liraglutide, unlike native GLP-1, is stable against metabolic degradation by both peptidases, and after subcutaneous administration its plasma half-life is 13 hours. This pharmacokinetic profile makes it suitable for once daily administration. It results from self-association that delays absorption, plasma protein binding, and stability against metabolic degradation by DPP-IV and NEP.
Pregnancy & Breastfeeding
Liraglutide must not be used during pregnancy. Weight loss gives a pregnant woman no benefit, and the medicine may harm the baby. There are no data on liraglutide in pregnant women, so the risk of major birth defects and miscarriage is not known. If a patient wants to become pregnant, or if pregnancy occurs, liraglutide treatment should be stopped.
For breastfeeding, there are no data on whether liraglutide passes into human milk, what it does to a breastfed infant, or whether it affects milk production. It was found in the milk of lactating rats. The doctor and the mother should weigh the developmental and health benefits of breastfeeding against the mother's clinical need for liraglutide. They should also consider any possible adverse effects on the breastfed infant, whether from the medicine or from the mother's underlying condition.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.