Usage
Liraglutide is prescribed as an adjunct to diet and exercise for:
- Type 2 Diabetes Mellitus: To improve glycemic control in adults and children aged 10 years and older.
- Obesity (Saxenda brand): For chronic weight management in adults and pediatric patients 12 years and older with an initial BMI of ≥ 30 kg/m² (obesity), or ≥ 27 kg/m² to < 30 kg/m² (overweight) with at least one weight-related comorbidity (e.g., dysglycaemia, hypertension, dyslipidaemia, obstructive sleep apnoea).
- Cardiovascular Risk Reduction (Victoza brand): To reduce the risk of major adverse cardiovascular events (cardiovascular death, non-fatal myocardial infarction, or non-fatal stroke) in adults with type 2 diabetes and established cardiovascular disease.
Pharmacological Classification: Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist, also known as an incretin mimetic.
Mechanism of Action: Liraglutide works by mimicking the effects of GLP-1, a naturally occurring hormone that stimulates insulin secretion in a glucose-dependent manner. It also slows gastric emptying, suppresses glucagon secretion, and may reduce appetite and food intake.
Alternate Names
Liraglutide is the generic name. Brand names include:
- Victoza: For type 2 diabetes and cardiovascular risk reduction.
- Saxenda: For chronic weight management.
How It Works
Pharmacodynamics: Liraglutide binds to and activates GLP-1 receptors, leading to increased insulin release, decreased glucagon secretion, delayed gastric emptying, and reduced appetite. These effects contribute to improved glycemic control and weight loss.
Pharmacokinetics: Liraglutide is administered subcutaneously and has a bioavailability of approximately 85%. It has a half-life of around 13 hours, allowing for once-daily administration. Liraglutide is primarily metabolized by dipeptidyl peptidase-4 (DPP-4) and undergoes further degradation. It does not involve CYP450 enzymes. Elimination is primarily through the kidneys.
Mode of Action: Liraglutide acts as a GLP-1 receptor agonist. By binding to these receptors on pancreatic beta-cells, it enhances glucose-stimulated insulin secretion. Simultaneously, it suppresses glucagon release from alpha-cells, further contributing to glycemic control. The effects on gastric emptying and appetite contribute to weight loss.
Receptor Binding: GLP-1 receptor.
Elimination Pathways: Primarily renal excretion following metabolic degradation, not involving CYP450 enzymes.
Dosage
Standard Dosage
Adults:
- Type 2 Diabetes (Victoza): Initial dose is 0.6 mg SC once daily for 1 week. Increase to 1.2 mg SC once daily. If further glycemic control is needed, increase to 1.8 mg SC once daily after at least one week. Maximum dose is 1.8 mg daily.
- Obesity (Saxenda): Initial dose is 0.6 mg SC once daily for 1 week. Increase by 0.6 mg weekly until reaching a maintenance dose of 3 mg SC once daily.
- Cardiovascular Risk Reduction (Victoza): Initial dose is 0.6 mg SC once daily for 1 week. May be increased to 1.2 mg SC once daily, then to 1.8 mg once daily, as needed.
Children:
- Type 2 Diabetes (Victoza, 10 years and older): Initial dose is 0.6 mg SC once daily for 1 week. May be increased in 0.6 mg increments weekly. Maximum dose is 1.8 mg SC once daily.
- Obesity (Saxenda, 12 years and older, >60 kg, BMI ≥ 30 kg/m²): Initial dose 0.6 mg SC once daily for 1 week, then increase by 0.6 mg weekly until reaching 3 mg/day (maintenance dose). If not tolerated, reduce to 2.4 mg/day. Discontinue if 2.4 mg is not tolerated. Dose escalation may take up to 8 weeks. Evaluate BMI change after 12 weeks at the maintenance dose.
Special Cases:
- Elderly Patients: No dose adjustment is generally required based on age alone.
- Patients with Renal Impairment: No dose adjustment required for mild to moderate impairment. Use with caution in severe renal impairment.
- Patients with Hepatic Dysfunction: No dose adjustment is generally recommended. However, use with caution.
- Patients with Comorbid Conditions: Use with caution in patients with gastrointestinal disorders.
Clinical Use Cases
Liraglutide is not typically used in the context of intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dose adjustments are primarily based on tolerability and efficacy for glycemic control or weight loss. Consider renal and hepatic function and comorbid conditions when adjusting the dose.
Side Effects
Common Side Effects
Nausea, vomiting, diarrhea, constipation, headache, dizziness, fatigue, dyspepsia, abdominal pain.
Rare but Serious Side Effects
Pancreatitis, gallbladder disease, renal impairment, severe hypersensitivity reactions (including anaphylaxis), thyroid C-cell tumors (in rodents).
Long-Term Effects
Potential for chronic complications like cholelithiasis, cholecystitis, pancreatitis, and medullary thyroid carcinoma (though primarily observed in animal studies at higher doses).
Adverse Drug Reactions (ADR)
Severe hypersensitivity reactions, acute pancreatitis, and significant renal function changes.
Contraindications
- History of hypersensitivity to liraglutide or any of its components.
- Multiple endocrine neoplasia syndrome type 2 (MEN 2).
- Medullary thyroid carcinoma (MTC).
- Pregnancy.
Drug Interactions
Liraglutide can delay gastric emptying, potentially affecting the absorption of other orally administered drugs. Monitor patients closely when co-administering medications with a narrow therapeutic index.
Pregnancy and Breastfeeding
Pregnancy: Contraindicated. Liraglutide can cross the placenta and has been associated with adverse fetal outcomes in animal studies.
Breastfeeding: Not recommended. It is unknown if liraglutide is excreted in human milk.
Drug Profile Summary
- Mechanism of Action: GLP-1 receptor agonist.
- Side Effects: Nausea, vomiting, diarrhea, pancreatitis (rare).
- Contraindications: Hypersensitivity, MEN 2, MTC, pregnancy.
- Drug Interactions: May delay gastric emptying, affecting absorption of oral medications.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy, not recommended while breastfeeding.
- Dosage: See detailed dosage section above.
- Monitoring Parameters: HbA1c, fasting blood glucose, body weight, blood pressure, renal function.
Popular Combinations
Liraglutide is often used in combination with metformin, sulfonylureas, or thiazolidinediones for the management of type 2 diabetes.
Precautions
- Monitor for gastrointestinal side effects and adjust dosage accordingly.
- Assess renal and hepatic function.
- Evaluate for history of pancreatitis or gallbladder disease.
- Monitor thyroid function.
- Patient education on proper injection technique and storage of the medication.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Liraglutide?
A: See the detailed dosage section above, covering adult, pediatric, and special populations.
Q2: How should Liraglutide be administered?
A: Subcutaneously, once daily, into the abdomen, thigh, or upper arm, irrespective of meals.
Q3: What are the most common side effects of Liraglutide?
A: Nausea, vomiting, diarrhea, and constipation.
Q4: Is Liraglutide safe for use during pregnancy?
A: No, Liraglutide is contraindicated during pregnancy.
Q5: Can Liraglutide be used in patients with renal impairment?
A: Use with caution in patients with severe renal impairment. Dose adjustments may be needed. No dose adjustment is required for mild to moderate impairment.
Q6: What are the potential drug interactions with Liraglutide?
A: Liraglutide may delay the absorption of orally administered drugs.
Q7: What monitoring parameters should be considered for patients on Liraglutide?
A: HbA1c, fasting blood glucose, body weight, blood pressure, and renal function.
Q8: How does Liraglutide compare to other GLP-1 receptor agonists?
A: While they share similar mechanisms of action, individual GLP-1 receptor agonists have different pharmacokinetic properties and side effect profiles. Discuss with your patient which GLP-1 receptor agonist best suits their individual needs.
Q9: What patient education is crucial for Liraglutide?
A: Injection technique, storage, potential side effects, importance of adhering to diet and exercise recommendations, and when to contact their physician.
This information is current as of February 16, 2025. Always consult the latest prescribing information and guidelines.
