利拉魯肽(Liraglutide)
Overview
Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist. It is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes. A separate, higher-dose formulation is approved for weight management in overweight or obese individuals.
Mechanism of Action
Liraglutide mimics the action of the endogenous incretin hormone GLP-1. It binds to and activates the GLP-1 receptor, leading to glucose-dependent stimulation of insulin secretion, suppression of inappropriate glucagon secretion, and a delay in gastric emptying. These actions collectively lower fasting and postprandial blood glucose and promote satiety.
Dosage and Administration
For type 2 diabetes, the starting dose is 0.6 mg injected subcutaneously once daily for one week to improve gastrointestinal tolerance. The dose is then increased to 1.2 mg daily, and up to a maximum of 1.8 mg daily if needed. It can be administered at any time of day, independent of meals.
Side Effects
Gastrointestinal adverse reactions are the most common, including nausea, vomiting, diarrhea, and constipation, which often decrease over time. It may increase the risk of gallbladder disease and acute pancreatitis. Hypoglycemia risk is low unless combined with an insulin secretagogue.
Contraindications
It is contraindicated in patients with a personal or family history of medullary thyroid carcinoma (MTC) or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2). It should not be used in patients with prior severe hypersensitivity to liraglutide.
Pregnancy and Lactation
Liraglutide should not be used during pregnancy, as weight loss offers no potential benefit to a pregnant woman and may cause fetal harm. It should be discontinued if pregnancy is recognized. Breastfeeding is not recommended.
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