semaglutide

Action and Spectrum

Actions and Spectrum: 

semaglutide is a medication used to treat type 2 diabetes. It is a glucagon-like peptide-1 (GLP-1) receptor agonist that mimics the action of the natural hormone GLP-1. Here are some of the actions and spectrum of semaglutide: 

• Stimulates insulin secretion: semaglutide stimulates insulin secretion from pancreatic beta cells, which helps to lower blood glucose levels. 
• Reduces glucagon secretion: semaglutide also reduces the secretion of glucagon from pancreatic alpha cells, which helps to lower blood glucose levels. 
• Slows gastric emptying: semaglutide slows down the rate at which food leaves the stomach, which helps to regulate blood glucose levels. 
• Increases satiety: semaglutide increases feelings of fullness and satiety, which can help to reduce food intake and promote weight loss. 
• Lowers A1c: semaglutide has been shown to significantly lower A1c levels in people with type 2 diabetes. 
• Improves cardiovascular outcomes: semaglutide has been shown to reduce the risk of major adverse cardiovascular events in people with type 2 diabetes who have established cardiovascular disease. 
• Reduces body weight: semaglutide has been approved for use as a weight loss medication in people without diabetes. 

Drug Interaction

Adverse Reaction

Adverse drug reactions:   

Frequency defined 

1-10%  

Diarrhea (8.5-8.8%)  

Abdominal pain (5.7-7.3%)  

Abdominal distension (7%)  

Dyspepsia (2.7-3.5%)  

Eructation (1.1-2.7%)  

Flatulence (0.4-1.5%)  

Vomiting (5-9.2%)  

Retinal disorders (6.9%)   

Gastroenteritis viral (4%)   

Hair loss (3%)   

Cholelithiasis (1.6%)  

Hypoglycemia in T2DM (6%)   

Flatulence (6%)  

Constipation (3.1-5%)  

GERD (1.5-1.9%)  

Dyspepsia (9%)   

Gastroenteritis (6%)   

GERD (5%)   

Gastritis (4%)  

Dizziness (8%)   

Eructation (7%)   

Black Box Warning

Black Box Warning: 

The black box warning for semaglutide is related to the risk of thyroid C-cell tumors. C-cells are a type of cell found in the thyroid gland that can become cancerous. semaglutide has been shown to cause an increase in the number of C-cell tumors in rats, and there is a theoretical risk that it could do the same in humans. 

Contraindication / Caution

Contraindication / Caution: 

Contraindications: 

• semaglutide should not be used 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). 
• semaglutide should not be used in patients with hypersensitivity to semaglutide or any of its components. 

Cautions: 

• semaglutide may increase the risk of developing acute pancreatitis. Patients with a history of pancreatitis or gallstones should use semaglutide with caution. 
• semaglutide may cause hypoglycemia (low blood sugar) when used in combination with insulin or other medications that lower blood sugar. 
• semaglutide may cause gastrointestinal adverse effects such as nausea, vomiting, and diarrhea. These symptoms usually resolve on their own but may require discontinuation of the medication in some cases. 
• semaglutide may cause an increase in heart rate. Patients with a history of cardiovascular disease should use semaglutide with caution. 

Pregnancy / Lactation

Pregnancy warnings:     

AU TGA pregnancy category: D
US FDA pregnancy category: Not assigned  

Lactation: 

Excreted into human milk is Unknown 

Pregnancy Categories:       

Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.       

Category B: No evidence shown of risk to the fetus 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 result in humans must take care of potential risks in pregnant women       

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.       

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.       

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

semaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used in the treatment of type 2 diabetes. It works by mimicking the effects of GLP-1, a hormone that is naturally produced in the body in response to food intake, and which helps to regulate blood sugar levels. 

Pharmacodynamics: 

semaglutide binds to the GLP-1 receptor in pancreatic beta cells, leading to increased insulin secretion and decreased glucagon secretion, which results in reduced hepatic glucose production. semaglutide also slows gastric emptying and promotes satiety, which can help to reduce food intake and aid in weight loss. 

Pharmacokinetics: 

Absorption 

semaglutide is administered subcutaneously, and its absorption is slow and prolonged. After subcutaneous injection, the peak concentration is reached after 2-4 days. The absolute bioavailability of semaglutide after subcutaneous administration is approximately 87%. 

Distribution 

semaglutide is extensively distributed in the body, and its volume of distribution is approximately 12.2 L. The plasma protein binding of semaglutide is approximately 99%. 

Metabolism 

semaglutide is metabolized mainly by proteolytic degradation, with the predominant site of metabolism being the kidneys. No significant hepatic metabolism of semaglutide is observed. 

Elimination and Excretion 

semaglutide is eliminated primarily by renal excretion, with approximately 85% of the dose being eliminated unchanged in the urine. The terminal half-life of semaglutide is approximately 1 week. 

Adminstartion

Administration: 

semaglutide is usually administered once a week by subcutaneous injection. The recommended starting dose is 0.25 mg once weekly for the first four weeks, followed by an increase to 0.5 mg once weekly. Depending on the patient’s response, the dose may be further increased to 1 mg once weekly. 

semaglutide should be administered in the abdomen, thigh, or upper arm. The injection site should be rotated to prevent local irritation or tissue damage. 

Before administering semaglutide, it is important to check the patient’s blood glucose levels and ensure that they are stable. semaglutide should not be used in patients with a history of medullary thyroid carcinoma or multiple endocrine neoplasia syndrome type 2. 

Patient Information Leaflet

Patient Information Leaflet    

Generic Name: semaglutide  

Why do we use semaglutide? 

semaglutide is a medication that is primarily used for the treatment of type 2 diabetes. However, it has also been approved by the FDA for the treatment of obesity in adults with a body mass index (BMI) of 30 or greater, or in adults with a BMI of 27 or greater who have at least one weight-related condition, such as high blood pressure, type 2 diabetes, or high cholesterol. 

semaglutide works by mimicking the action of a hormone called glucagon-like peptide-1 (GLP-1), which is released by the gut in response to food intake. GLP-1 promotes feelings of fullness and satiety, which can help reduce food intake and lead to weight loss.