司美格魯肽(Semaglutide)
Overview
Semaglutide is a potent glucagon-like peptide-1 (GLP-1) receptor agonist. It is indicated for the treatment of type 2 diabetes mellitus to improve glycemic control and reduce the risk of major adverse cardiovascular events. Specific formulations are also approved for chronic weight management.
Mechanism of Action
It acts as a GLP-1 analog, selectively binding to and activating the GLP-1 receptor. This enhances glucose-dependent insulin secretion, inhibits glucagon release, and slows gastric emptying. Furthermore, semaglutide acts centrally in the brain to reduce appetite and food intake, leading to substantial weight loss.
Dosage and Administration
The injectable form is administered subcutaneously once a week. The starting dose is 0.25 mg weekly for 4 weeks, then increased to 0.5 mg weekly. It can be further increased to 1 mg or 2 mg weekly if needed. The oral tablet must be taken once daily on an empty stomach with a small amount of water, waiting at least 30 minutes before eating or taking other medications.
Side Effects
Gastrointestinal issues are very common, particularly nausea, vomiting, diarrhea, abdominal pain, and constipation. These are usually mild to moderate and transient. There is a potential risk of acute pancreatitis, gallbladder disease, and diabetic retinopathy complications.
Contraindications
Like liraglutide, it is contraindicated in patients with a personal or family history of medullary thyroid carcinoma (MTC) or Multiple Endocrine Neoplasia syndrome type 2 (MEN 2). It is also contraindicated in patients with known hypersensitivity to semaglutide.
Pregnancy and Lactation
Semaglutide is contraindicated during pregnancy and should be discontinued at least 2 months before a planned pregnancy due to its long half-life. It is not recommended for use during breastfeeding.
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