What it's for (Indications)
- Liraglutide is used to control blood glucose levels in adults with type 2 diabetes mellitus, as an adjunct to diet and exercise.
- It is also indicated to reduce the risk of major adverse cardiovascular events in adults with type 2 diabetes mellitus and established cardiovascular disease.
- Additionally, it is used for chronic weight management in obese or overweight adults with at least one weight-related comorbidity, in conjunction with a reduced-calorie diet and increased physical activity.
Dosage Information
| Type | Guideline |
|---|---|
| Standard | Liraglutide is administered as a subcutaneous injection once daily in the abdomen, thigh, or upper arm, without regard to meal timing. Injection sites should be rotated. The recommended target maintenance dose is 3 mg daily. Dosing should be initiated at 0.6 mg per day for one week, with weekly dose increases in 0.6 mg increments until the target dose of 3 mg is reached. For pediatric patients, dose escalation may take up to 8 weeks, and if 3 mg is not tolerated, the dose may be reduced to 2.4 mg daily or to the previous tolerated level during escalation. Adult patients with type 2 diabetes should monitor blood glucose levels before and during treatment. Prior to initiation, patients should be trained on proper injection technique. Consult a healthcare provider for storage instructions. |
Safety & Warnings
Common Side Effects
- Common side effects include nausea, diarrhea, constipation, vomiting, headache, dizziness, low blood glucose levels (especially when used with concomitant anti-diabetic therapy), gastrointestinal disturbances, fatigue, fever, toothache, anorexia, and injection site reactions.
- More serious potential side effects include acute gallbladder disease, increased heart rate, acute pancreatitis, acute kidney injury due to volume depletion, severe gastrointestinal adverse reactions, serious hypersensitivity reactions (including anaphylaxis and angioedema), and potential for suicidal behavior and ideation.
Serious Warnings
- Black Box Warning: WARNING: RISK OF THYROID C-CELL TUMORS. Liraglutide causes dose-dependent and treatment-duration-dependent thyroid C-cell tumors at clinically relevant exposures in both genders of rats and mice. It is unknown whether liraglutide causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans, as the human relevance of liraglutide-induced rodent thyroid C-cell tumors has not been determined.
- Patients should be counselled on the potential risk of **Thyroid C-cell Tumors**; consult a doctor if you or anyone in your family has ever had thyroid cancer, or if you feel a lump or swelling in your neck, difficulty swallowing, or shortness of breath.
- **Acute Pancreatitis** has been reported; monitor for persistent severe abdominal pain.
- **Acute Gallbladder Disease** (e.
- g.
- , cholelithiasis, cholecystitis) can occur.
- There is an increased risk of **Hypoglycemia** when used concomitantly with insulin or insulin secretagogues; adult type 2 diabetes patients should monitor blood glucose.
- Liraglutide can cause an **Increased Heart Rate**.
- **Acute Kidney Injury** due to volume depletion, possibly from severe gastrointestinal reactions, has been reported; caution should be exercised in patients with pre-existing kidney problems.
- **Severe Gastrointestinal Adverse Reactions** may lead to dehydration and acute kidney injury; patients with pre-existing stomach problems should consult their doctor.
- **Serious Hypersensitivity Reactions**, including anaphylaxis and angioedema, have been reported.
- **Suicidal Behavior and Ideation** have been reported with GLP-1 receptor agonists; patients should be monitored for depression or suicidal thoughts.
- There is a potential for **Pulmonary Aspiration** during general anesthesia or deep sedation due to delayed gastric emptying.
- **Pregnancy and Lactation**: Liraglutide is contraindicated in pregnant females and research suggests avoidance during breastfeeding; consult a doctor.
- **Driving**: Avoid driving if symptoms like dizziness or low blood glucose impair ability.
How it Works (Mechanism of Action)
Liraglutide is an acylated human GLP-1 receptor agonist with 97% amino acid sequence homology to endogenous human GLP-1(7-37). It binds to and activates the GLP-1 receptor, a cell-surface receptor coupled to adenylyl cyclase activation through the stimulatory G-protein, Gs. Unlike native GLP-1, liraglutide is stable against metabolic degradation by dipeptidyl peptidase 4 (DPP-4) and neutral endopeptidases (NEP), resulting in a prolonged plasma half-life of 13 hours, suitable for once-daily administration. This action contributes to the physiological regulation of appetite and calorie intake.