Liraglutide
Liraglutide is a once-daily GLP-1 receptor agonist used in adult type 2 diabetes and, under a separate brand name, for chronic weight management. It improves glycaemic control and produces moderate weight reduction.
- Chemical formula
- C172H265N43O51
- CAS number
- 204656-20-2
- ATC code
- A10BJ02
- Molecular weight
- 3751.2 g/mol
- Drug class
- GLP-1 receptor agonist
- Also known as
- NN2211, Liraglutida
What is it?
Liraglutide is a synthetic analogue of human glucagon-like peptide 1 modified with a fatty acid that binds reversibly to albumin, prolonging the half-life to about 13 hours. It was developed by Novo Nordisk and approved for type 2 diabetes in 2010, with a separate brand name later approved for chronic weight management in adults and adolescents. Unlike weekly GLP-1 receptor agonists, liraglutide is administered once daily by subcutaneous injection at the same time of day.
Mechanism of action
Liraglutide binds and activates the GLP-1 receptor in pancreatic beta and alpha cells, the central nervous system and the gastrointestinal tract. The result is glucose-dependent stimulation of insulin secretion, suppression of inappropriate glucagon release, slower gastric emptying and reduced appetite through hypothalamic centres. These actions lower fasting and post-prandial glucose without intrinsic hypoglycaemia risk and produce moderate, gradual weight reduction in many adults.
Pharmacokinetics
After subcutaneous administration, peak plasma concentrations are reached after eight to twelve hours. Albumin binding exceeds 98%. The terminal half-life is approximately 13 hours, supporting once-daily administration with steady state reached within several days. The drug is degraded by ubiquitous peptidases, with no specific organ pathway responsible for clearance, and minimal urinary or faecal elimination of intact peptide. No dose adjustment is required for mild to moderate renal or hepatic impairment.
Indications
Liraglutide is approved in adults with type 2 diabetes mellitus, alone or in combination with other antidiabetic agents, to improve glycaemic control. A second indication, under a separate brand name, is chronic weight management as an adjunct to a reduced-calorie diet and increased physical activity in adults with obesity or with overweight and at least one weight-related comorbidity, and in adolescents from 12 years in some markets. According to the prescribing information, treatment must be initiated and supervised by a clinician.
Safety profile
The most common adverse effects are gastrointestinal: nausea, vomiting, diarrhoea, constipation and abdominal discomfort, generally mild to moderate and most pronounced during the initial dose escalation. Acute pancreatitis, gallbladder disease, injection-site reactions and increased heart rate have been reported. Hypoglycaemia may occur in combination with insulin or sulfonylureas. The product carries a boxed warning regarding thyroid C-cell tumours observed in rodents; medullary thyroid carcinoma and multiple endocrine neoplasia type 2 are contraindications, as is severe gastroparesis.
Products containing this ingredient
Frequently asked questions
How is liraglutide different from semaglutide and dulaglutide? ▾
All three are GLP-1 receptor agonists, but liraglutide is dosed once daily while semaglutide and dulaglutide are dosed once weekly thanks to longer half-lives. Direct trials suggest weekly agents produce somewhat greater glycaemic and weight reductions, while liraglutide allows finer day-to-day flexibility and is approved for paediatric use in some markets. The choice between them is made by the prescriber based on indication, adherence, tolerability and individual response.
How is liraglutide administered? ▾
Liraglutide is given once daily by subcutaneous injection in the abdomen, thigh or upper arm, ideally at the same time of day. According to the prescribing information, the dose is increased gradually over several weeks to limit gastrointestinal adverse effects, until the maintenance dose recommended for the indication is reached. Injection sites should be rotated to prevent lipohypertrophy. Liraglutide can be administered with or without food.
Can liraglutide be used in adolescents? ▾
In some markets, liraglutide is approved for chronic weight management in adolescents aged 12 years and older with obesity, and for type 2 diabetes from age 10 in selected jurisdictions. Use in this population should always be initiated by a specialist clinician within a comprehensive treatment plan that includes diet, physical activity and psychological support. According to the prescribing information, growth and pubertal development should be monitored.
Does liraglutide require refrigeration? ▾
Yes. Unopened pens are stored in a refrigerator between 2°C and 8°C. After first use the pen can be kept at room temperature below a defined limit for the period stated in the leaflet, after which it must be discarded. Freezing damages the peptide. Cold-chain integrity is one reason regulatory agencies caution against purchasing GLP-1 agonists from unverified online sources.
What are the main contraindications for liraglutide? ▾
Personal or family history of medullary thyroid carcinoma, multiple endocrine neoplasia type 2 and known hypersensitivity to liraglutide are formal contraindications. Caution is required in patients with previous pancreatitis, severe gastroparesis or active gallbladder disease, and during pregnancy and breastfeeding. According to the prescribing information, the medical history and current medication list must be reviewed by a clinician before any prescription.
The information on this website is provided for reference and educational purposes only. It does not replace consultation with a qualified healthcare professional.