liraglutide

Action and Spectrum

Actions and Spectrum: 

liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist that mimics the action of the naturally occurring hormone GLP-1. GLP-1 stimulates insulin secretion from pancreatic beta cells, decreases glucagon secretion from pancreatic alpha cells, slows gastric emptying, and reduces food intake by increasing feelings of fullness. 

liraglutide is a long-acting GLP-1 receptor agonist that binds to and activates the GLP-1 receptor on pancreatic beta cells, leading to increased insulin secretion and reduced glucagon secretion. These actions result in lower blood sugar levels in patients with type 2 diabetes. In addition, liraglutide slows down the rate at which food leaves the stomach, which can help reduce appetite and promote weight loss. 

liraglutide has also been shown to have cardiovascular benefits. It has been shown to reduce the risk of major adverse cardiovascular events in patients with type 2 diabetes and established cardiovascular disease or multiple cardiovascular risk factors. 

Drug Interaction

Adverse Reaction

Frequency Defined 

>10% 

Nausea  

Diarrhea  

Hypoglycemia 

Headache 

Vomiting 

Constipation 

1-10% 

Reactions on injection site 

Antiliraglutide antibodies 

Constipation 

Dyspepsia  

Fatigue  

Dizziness  

Abdominal pain  

Upper abdominal pain  

Eructation  

Urinary tract infection  

Flatulence  

Viral gastroenteritis  

Injection site erythema  

Injection site reaction  

Abdominal distension  

Insomnia  

Dry mouth  

Gastroesophageal reflux disease  

Gastroenteritis  

Increased lipase  

Asthenia  

Anxiety 

<1%: 

UTI 

Urticaria 

Dizziness 

Sinusitis 

Hypertension 

Back pain 

Nasopharyngitis 

Pancreatitis 

Thyroid C-cell hyperplasia 

Hypoglycemia 

Black Box Warning

Black Box Warning: 

There is a risk of thyroid C-cell tumors due to liraglutide. 

The drug is contraindicated in people who have history of MTC (medullary thyroid carcinoma). 

And, in patients with multiple type 2 endocrine neoplasia syndrome. 

MTC patients treated with liraglutide, should get their serum calcitonin monitored. 

Contraindication / Caution

Contraindication/Caution: 

liraglutide has several contraindications and precautions that should be taken into consideration before prescribing the medication. These include: 

• Pancreatitis: liraglutide should be used with caution in patients with a history of pancreatitis, as the medication may increase the risk of developing pancreatitis. 
• Renal impairment: liraglutide should be used with caution in patients with renal impairment, as the medication is eliminated primarily by the kidneys. 
• Gastrointestinal disease: liraglutide should be used with caution in patients with a history of gastrointestinal disease, such as gastroparesis, as the medication may slow down gastric emptying. 
• Thyroid disease: liraglutide should be used with caution in patients with a history of thyroid disease, as the medication may affect thyroid function. 
• Pregnancy and breastfeeding: liraglutide are not recommended for use during pregnancy or breastfeeding. 

Pregnancy / Lactation

Pregnancy consideration:  

It is not secure to administer liraglutide during pregnancy. 

Breastfeeding warnings:  

No data is available about the excretion of liraglutide in human breastmilk. Avoid using in lactating women. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

liraglutide is administered by subcutaneous injection once daily, at any time of the day, with or without food. The injection should be given in the abdomen, thigh, or upper arm. The exact dose and administration instructions may vary depending on the patient’s individual needs, medical history, and response to treatment. 

The initial dose of liraglutide is usually 0.6 mg/day, which is increased to 1.2 mg/day after one week. After an additional week, the dose may be increased to the maintenance dose of 1.8 mg/day, if necessary, to achieve optimal glycemic control. 

liraglutide should not be mixed with other insulins or solutions, and it should not be administered intravenously or intramuscularly. Patients should be instructed on proper injection technique and how to rotate injection sites to minimize the risk of injection site reactions. 

Pharmacodynamics: 

liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist that mimics the action of the naturally occurring hormone GLP-1. GLP-1 stimulates insulin secretion from pancreatic beta cells, decreases glucagon secretion from pancreatic alpha cells, slows gastric emptying, and reduces food intake by increasing feelings of fullness. 

liraglutide is a long-acting GLP-1 receptor agonist that binds to and activates the GLP-1 receptor on pancreatic beta cells, leading to increased insulin secretion and reduced glucagon secretion. These actions result in lower blood sugar levels in patients with type 2 diabetes. In addition, liraglutide slows down the rate at which food leaves the stomach, which can help reduce appetite and promote weight loss. 

liraglutide has also been shown to have cardiovascular benefits. It has been shown to reduce the risk of major adverse cardiovascular events in patients with type 2 diabetes and established cardiovascular disease or multiple cardiovascular risk factors. 

Pharmacokinetics: 

Absorption 

The peak plasma concentration is achieved in 11 hours (for Saxenda) 

The peak plasma concentration is 35 ng/mL (for Victoza) 

The area under the curve is 960 ng·hr/mL (for Victoza) 

Average steady state concentration over 24 hours is 128 ng/mL (at 1.8 mg dose) 

The absolute bioavailability is 55% 

Distribution 

The protein bound is more than 98% 

The volume of distribution is 13 L (for Victoza); and 20-25 L (for Saxenda); 0.07 L/kg (for intravenous) 

Metabolism 

The drug is endogenously metabolized to large proteins. No specific route is mentioned. 

Elimination 

The half-life is 13 hours 

Mean apparent clearance rate is 1.2 L/hr (for Victoza) and 0.9-1.4 L/hr (for Saxenda) 

The drug is excreted 5% in feces and 6% in urine 

Adminstartion

Administration: 

liraglutide is administered by subcutaneous injection once daily, at any time of the day, with or without food. The injection should be given in the abdomen, thigh, or upper arm. The exact dose and administration instructions may vary depending on the patient’s needs, medical history, and response to treatment. 

The initial dose of liraglutide is usually 0.6 mg/day, which is increased to 1.2 mg/day after one week. After an additional week, the dose may be increased to the maintenance dose of 1.8 mg/day, if necessary, to achieve optimal glycemic control. 

liraglutide should not be mixed with other insulins or solutions and should not be administered intravenously or intramuscularly. Patients should be instructed on proper injection techniques and how to rotate injection sites to minimize the risk of injection site reactions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: liraglutide 

Pronounced: LIR-a-GLOO-tide 

Why do we use liraglutide? 

liraglutide is a medication used to treat type 2 diabetes. It is a glucagon-like peptide-1 (GLP-1) receptor agonist, which mimics the action of GLP-1, a hormone produced by the intestines that stimulates insulin secretion and reduces glucose production by the liver. liraglutide also slows down the rate at which food leaves the stomach, which can help reduce appetite and promote weight loss. 

liraglutide is typically used as an adjunct to diet and exercise to improve blood sugar control in patients with type 2 diabetes who have not achieved adequate glycemic control with other medications, such as metformin, sulfonylureas, or insulin. It is also approved for use with basal insulin to help lower blood sugar levels in adults with type 2 diabetes who have not achieved adequate glycemic control with basal insulin alone.