Liraglutide is an injection for the treatment of Diabetes. They are Incretin mimetics and act by stimulating the pancreas to stimulate the right amount of insulin when there is a blood sugar spike.
When did FDA approve the drug? 23rd Dec 2014
Commonly marketed under the brand name of Victoza
Mode of administration: Injection of 3 ml pre-filled pen containing 18 mg of liraglutide
It is not injected intravenously or intramuscularly. Administeration of the injection subcutaneously on the abdomen, thigh, or arms is recommended.
It is produced by recombinant DNA technology as human glucagon-like peptide-1(GLP-1) using yeast as a host.
Indications:
- Adjunct Therapy: Insufficiently controlled type 2 diabetes mellitus + diet and exercise
- Mono therapy: when they tolerate or contraindicate metformin
- Treatment of Diabetes along with other medicines
Who should not take the medicine?
- Patients with type 1 diabetes
- Patients with Diabetic ketoacidosis
- Patients with heart failure
- Patients with Inflammatory Bowel Syndrome
Adverse reactions include hypoglycemia, cholecystitis, pancreatitis, and reactions at the site of injection
Mechanism of Action
It is an analog of GLP-1 and is almost 97% similar to human GLP-1 in its sequence. It binds and activates the GLP-1 receptor, which is a target for native GLP-1. Once it is administered, it acts based on three mechanisms:
- Self-association resulting in a slow absorption
- Binding to albumin
- Higher enzymatic stability to DPP-4, resulting in a long half-life in the plasma
Once it binds to the GLP-1 receptor, it leads to an increase in a secondary messenger called cyclic AMP (cAMP). Liraglutide helps in the efficient stimulation of insulin secretion keeping in mind the glucose levels. It also reduces high glucagon secretion. Upon a spike in glucose, insulin secretion is stimulated and glucagon is inhibited. This entire mechanism of blood glucose reduction slightly delays gastric emptying. The overall result is a decrease in body weight and body mass index.
The above information is given in the spmc of the drug.
Current research on Liraglutide
Liraglutide and Cardiaometabolic Health
Liraglutide led to reduced Neprolysin activity in people who were maintaining weight loss. This suggests the benefits of this medication on cardiometabolic health
Liraglutide and Deliriums
Patients experiencing Delirium have altered attention, consciousness, and cognition. This results in an overall reduction in focus and attention. Deliriums are common in patients who have just had cardiac surgery. These deliriums are mainly due to neuro-inflammation. Recent research suggests that Liraglutide helps [prevent neuroinflammation and preserves the structural integrity of the synapse.
Liraglutide and Cardiomyopathy
Diabetic patients have hyperglycemia (high glucose levels in the blood). This results in apoptosis and inflammation caused due to oxidative stress. All these factors contribute to the development of Cardiomyopathy. Liraglutide helps reduce the effects of cardiomyopathy due to four of its properties: antioxidant, anti-glycemic, antiapoptotic, and anti-inflammatory properties.
Liraglutide and adverse gastrointestinal effects
GLP1 agonists such as liraglutide, especially when used for weight loss can result in adverse gastrointestinal effects like irritable bowel syndrome and pancreatitis. Although these adverse effects are rare according to the spmc of the drug, it is important to consider this effect especially when taken for weight loss.
Liraglutide and Intragastric balloon
Intragastric Baloon is used to give a feeling of fullness and aids in weight loss. It is made of silicone and is filled with saline. Recent research has shown that Liraglutide when taken along with the Intragastric balloon made weight loss faster.
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