Action and Spectrum

Actions and Spectrum: 

exenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist, which means it mimics the action of the hormone GLP-1 to lower blood glucose levels. It has the following actions and spectrum of effects: 

• Stimulates insulin secretion: exenatide stimulates insulin secretion in response to glucose. It binds to GLP-1 receptors on pancreatic beta cells, which triggers the release of insulin. 
• Suppresses glucagon secretion: exenatide also suppresses glucagon secretion from pancreatic alpha cells. Glucagon is a hormone that increases blood glucose levels, so suppressing its secretion helps to lower blood glucose levels. 
• Slows down gastric emptying: exenatide slows down the rate at which food leaves the stomach and enters the small intestine. This delays the absorption of glucose from food, which helps to lower blood glucose levels. 
• Promotes weight loss: exenatide has been shown to promote weight loss in people with type 2 diabetes. This effect is thought to be mediated through its action on GLP-1 receptors in the brain, which leads to reduced appetite and increased feelings of fullness. 
• Improves lipid profiles: exenatide has been shown to improve lipid profiles in people with type 2 diabetes, including reducing triglyceride levels and increasing HDL cholesterol levels. 
• Reduces blood pressure: exenatide has been shown to reduce blood pressure in people with type 2 diabetes, although the mechanism behind this effect is not well understood. 

Drug Interaction

Adverse Reaction

Frequency Defined: 

>10% 

Injection site nodule  

1-10% 

Nausea  

Diarrhea  

Dizziness 

Headache  

Vomiting  

Injection site erythema  

Constipation 

Injection site pruritus

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: 

exenatide is contraindicated in individuals who have a history of severe hypersensitivity reactions to exenatide or to any of its components. 

exenatide should be used with caution in individuals with a history of pancreatitis or a family history of medullary thyroid carcinoma (MTC) as it may increase the risk of developing these conditions. 

exenatide is not recommended for use in individuals with type 1 diabetes or for the treatment of diabetic ketoacidosis. 

exenatide should also be used with caution in individuals with severe gastrointestinal disease, including gastroparesis, as it can slow down gastric emptying and potentially worsen these conditions. 

In addition, exenatide may interact with other medications, so it is important to inform healthcare providers of all medications and supplements being taken before starting treatment with exenatide. 

Pregnancy / Lactation

Pregnancy consideration:  

It is not secure to administer exenatide during pregnancy. 

Breastfeeding warnings:  

No data is available about the excretion of exenatide 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: 

exenatide is a medication used to treat type 2 diabetes. It is a glucagon-like peptide-1 (GLP-1) receptor agonist, which means it mimics the action of GLP-1, a hormone produced in the intestines that sti 

mulates insulin secretion and lowers blood glucose levels. 

exenatide is administered as a subcutaneous injection and has a half-life of approximately 2.4 hours. It stimulates insulin secretion in response to glucose, slows down gastric emptying, and suppresses glucagon secretion, all of which contribute to its blood glucose-lowering effects. 

In addition to its effects on blood glucose levels, exenatide has been shown to promote weight loss, reduce blood pressure, and improve lipid profiles in people with type 2 diabetes. 

exenatide is generally well-tolerated, although some people may experience side effects such as nausea, vomiting, diarrhea, and headache. In rare cases, it may cause pancreatitis or thyroid cancer. 

Pharmacodynamics: 

The pharmacodynamics of exenatide is mainly mediated through its action as a glucagon-like peptide-1 (GLP-1) receptor agonist. exenatide binds to and activates GLP-1 receptors, which are located on pancreatic beta cells, leading to increased insulin secretion in response to glucose. exenatide also suppresses glucagon secretion from pancreatic alpha cells, which helps to further lower blood glucose levels. 

In addition to its effects on pancreatic hormones, exenatide also slows down gastric emptying, which contributes to its blood glucose-lowering effects by delaying the absorption of glucose from food. This effect also contributes to its side effect of nausea, which is more common in the early stages of treatment. 

exenatide has been shown to have other beneficial effects beyond glycemic control, including promoting weight loss, improving lipid profiles, and reducing blood pressure. These effects are thought to be mediated through its action on GLP-1 receptors in other tissues, including the brain and the gastrointestinal tract. 

exenatide has a rapid onset of action, with peak effects observed within two hours of administration. Its effects on insulin secretion and gastric emptying persist for up to 10 hours after administration, which is why it is typically administered twice daily. 

Pharmacokinetics: 

Absorption 

The peak plasma concentration at steady state is 208 pg/mL 

Distribution 

The volume of distribution is 28.3 L 

Elimination and Excretion 

The rate of renal clearance is 9.1 L/hr 

The drug is predominantly excreted in urine 

Adminstartion

Administration: 

exenatide is administered by subcutaneous injection, which means it is injected under the skin. It comes as a pre-filled pen or a vial with a separate needle. 

The recommended dose of exenatide is typically 5 mcg injected twice daily, 60 minutes before the morning and evening meals. After at least one month of treatment, the dose may be increased to 10 mcg injected twice daily, if needed to achieve better glycemic control. 

It is important to follow the instructions for injection provided by the healthcare provider or pharmacist, as the injection technique can affect the absorption and effectiveness of the medication. exenatide should not be administered intravenously or intramuscularly. 

exenatide should be stored in a refrigerator until the expiration date on the label, and the medication should not be used if it has been frozen or exposed to heat or sunlight. Unused medication should be discarded according to local regulations. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: exenatide 

Pronounced: exe-naa-tide 

Why do we use exenatide? 

exenatide is used to treat type 2 diabetes, a condition in which the body becomes resistant to insulin or does not produce enough insulin to regulate blood glucose levels. 

exenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist, which means it mimics the action of the hormone GLP-1 to lower blood glucose levels. By stimulating insulin secretion in response to glucose, slowing down gastric emptying, and suppressing glucagon secretion, exenatide can effectively reduce blood glucose levels in people with type 2 diabetes. 

In addition to its effects on blood glucose levels, exenatide has been shown to promote weight loss, reduce blood pressure, and improve lipid profiles in people with type 2 diabetes. These effects are thought to be mediated through its action on GLP-1 receptors in other tissues, including the brain and the gastrointestinal tract.