GLP-1 Receptor Agonists
Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) are a class of drugs used in the management of:
- Type 2 diabetes mellitus
- Obesity and overweight
- Cardiovascular risk reduction
They mimic the action of the GLP-1 hormone, enhancing glucose-dependent insulin secretion and reducing appetite.
🧬 Mechanism of Action
- Stimulates insulin secretion (glucose-dependent)
- Inhibits glucagon release
- Slows gastric emptying
- Promotes satiety via CNS pathways
💊 Examples of GLP-1 RAs
| Generic Name | Brand Name(s) | Dosing Frequency |
|---|---|---|
| Exenatide | Byetta / Bydureon | BID / Weekly |
| Liraglutide | Victoza / Saxenda | Daily |
| Dulaglutide | Trulicity | Weekly |
| Semaglutide | Ozempic / Wegovy | Weekly |
| Tirzepatide * | Mounjaro | Weekly |
- Tirzepatide is a dual GLP-1/GIP receptor agonist.
📈 Clinical Indications
- Type 2 diabetes mellitus (T2DM)
- Reduces HbA1c with low hypoglycemia risk
- Obesity and overweight (with or without T2DM)
- Significant weight loss, especially with semaglutide and tirzepatide
- Cardiovascular risk reduction
- CV benefit shown with liraglutide, dulaglutide, and semaglutide in high-risk patients
⚠️ Common Side Effects
- Nausea, vomiting, diarrhea, constipation
- Gallbladder disease
- Pancreatitis (rare but serious)
- Injection site reactions
❌ Contraindications
- Personal/family history of medullary thyroid carcinoma (MTC)
- MEN type 2 syndrome
- History of pancreatitis (use with caution)
🔬 Ongoing Research
- Non-alcoholic steatohepatitis (NASH)
- Cognitive and neurodegenerative disease modulation
- Multi-agonist therapies (dual/triple incretin agonists)