exenatide subdermal implant

Action and Spectrum

Actions and Spectrum: 

exenatide subdermal implant is a medication used to treat type 2 diabetes. It is a long-acting form of exenatide, a glucagon-like peptide-1 receptor agonist (GLP-1 RA). The subdermal implant is a small device placed under the skin and continuously releases exenatide over an extended period. 

Action: 

• GLP-1 Receptor Agonism: exenatide subdermal implant works by activating the GLP-1 receptors in the body. GLP-1 receptors exist in various tissues, including the pancreas, liver, and brain. Activating these receptors leads to several physiological effects that help manage blood sugar levels. 
• Glucose Regulation: By activating GLP-1 receptors, exenatide subdermal implant enhances glucose-dependent insulin secretion from pancreatic beta cells. It also inhibits glucagon secretion, which reduces the production of glucose by the liver. These actions help to regulate blood sugar levels and reduce post-meal hyperglycemia. 
• Delayed Gastric Emptying: exenatide slows down the stomach’s rate of emptying, resulting in a prolonged feeling of fullness after meals. This effect can contribute to weight loss or maintenance in individuals with type 2 diabetes. 
• Appetite Suppression: exenatide can reduce appetite and food intake by acting on the central nervous system, specifically the hypothalamus. This effect can also support weight management. 

Spectrum: The exenatide subdermal implant provides extended and sustained release of exenatide, allowing for once-weekly dosing. It offers a more convenient treatment option than daily injections of short-acting GLP-1 receptor agonists. 

• Long Duration of Action: The implant releases exenatide continuously over an extended period, maintaining therapeutic levels in the body. This prolonged-release allows for once-weekly administration, reducing the frequency of injections and improving patient adherence. 
• Consistent Blood Sugar Control: The sustained release of exenatide helps maintain stable blood sugar levels throughout the week. This can result in improved glycemic control, reduced variability in glucose levels, and a lower risk of hypoglycemia. 
• Weight Management: exenatide has been associated with weight loss or maintenance in individuals with type 2 diabetes. The subdermal implant’s extended action can contribute to sustained effects on appetite suppression and delayed gastric emptying, which may support weight management efforts. 
• Convenience: The once-weekly dosing schedule of the subdermal implant offers convenience and potentially improves treatment adherence compared to more frequent injections.

Drug Interaction

Adverse Reaction

Pending

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

Here are some potential contraindications: 

• Hypersensitivity: exenatide subdermal implant may be contraindicated in individuals with known hypersensitivity/allergic reaction to exenatide or its components. Hypersensitivity reactions can range from mild skin reactions to severe anaphylaxis. 
• Medullary Thyroid Carcinoma (MTC): exenatide subdermal implant may be contraindicated in individuals with a personal or family history of MTC (medullary thyroid carcinoma) or in patients with MEN 2 (multiple endocrine neoplasia syndrome type 2). In animal studies, exenatide has been associated with developing thyroid C-cell tumors, including MTC. 
• Pancreatitis: exenatide subdermal implant may be contraindicated in individuals with a history of pancreatitis or a known risk factor. exenatide has been associated with an increased risk of pancreatitis, including severe and necrotizing forms. 
• Diabetic Ketoacidosis (DKA): exenatide subdermal implant may be contraindicated in individuals with a current/previous history of diabetic ketoacidosis. Use caution when initiating or continuing exenatide treatment in patients with known risk factors for DKA. 

Caution 

Here are some potential cautions: 

• Hypoglycemia: exenatide subdermal implant, like other medications used to treat diabetes, may cause hypoglycemia (low blood sugar). Individuals should be educated about the signs and symptoms of hypoglycemia and how to manage it, including appropriate adjustments in their antidiabetic medications, meal planning, and physical activity. 
• Renal Impairment: Caution may be warranted in patients with renal impairment or end-stage renal disease. exenatide is primarily eliminated through renal clearance, and dosage adjustment may be necessary for individuals with impaired kidney function. 
• Gastrointestinal Disorders: exenatide can cause gastrointestinal adverse effects, such as nausea, vomiting, diarrhea, and constipation. Individuals with a history of gastrointestinal disorders, such as gastroparesis, may require careful monitoring or adjustment of their treatment plan. 
• Thyroid Abnormalities: exenatide may affect thyroid function, including alterations in thyroid hormone levels. Close monitoring of thyroid function is recommended in patients with known thyroid disease or those receiving concomitant medications that may affect thyroid function. 
• Injection Site Reactions: As an exenatide subdermal implant involves a subdermal insertion, it is crucial to be cautious of potential injection site reactions, such as redness, swelling, itching, or pain at the implant site. Patients should be instructed on proper site care and advised to report any persistent or severe injection site reactions to their healthcare provider. 
• Pregnancy and Breastfeeding: The safety of exenatide subdermal implant during pregnancy and breastfeeding is not well established. It is key to consult with a healthcare professional if you are in pregnant condition, planning to become pregnant, or breastfeeding, as alternative treatment options may be considered. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not Known. 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data 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: 

exenatide subdermal implant is a medication used to treat type 2 diabetes. It is a long-acting form of exenatide, a glucagon-like peptide-1 receptor agonist (GLP-1 RA). Here is an overview of the pharmacology of exenatide subdermal implant: 

exenatide subdermal implant works by activating the GLP-1 receptors in the body. GLP-1 receptors are primarily located in the pancreas, liver, and brain. Activating these receptors leads to several physiological effects that help manage blood sugar levels. 

Pharmacodynamics: 

Mechanism of action: exenatide subdermal implant is a medication used to treat type 2 diabetes. It works through action similar to other formulations of exenatide, a glucagon-like peptide-1 receptor agonist (GLP-1 RA). Here is an overview of the mechanism of action of exenatide subdermal implant: 

• GLP-1 Receptor Activation: exenatide subdermal implant activates the GLP-1 receptors located on various cells in the body, including pancreatic beta cells, liver cells, and brain cells. 
• Glucose-Dependent Insulin Secretion: exenatide subdermal implant stimulates insulin release by activating GLP-1 receptors on pancreatic beta cells. Importantly, this insulin secretion is glucose-dependent, meaning it occurs in response to enhanced blood glucose levels and also helps to balance the blood sugar levels and prevent excessive postprandial (after-meal) glucose spikes. 
• Inhibition of Glucagon Secretion: exenatide subdermal implant also inhibits the release of glucagon, a hormone produced by pancreatic alpha cells. Glucagon typically promotes the production of glucose by the liver. By reducing glucagon secretion, the exenatide subdermal implant helps to lower blood glucose levels by decreasing the liver’s glucose output. 
• Delayed Gastric Emptying: exenatide subdermal implant slows down the speed that the stomach empties, leading to a prolonged feeling of fullness and decreased appetite. This effect can contribute to weight loss or management in individuals with type 2 diabetes. 

Pharmacokinetics: 

Absorption 

exenatide subdermal implant is designed to provide continuous and extended release of exenatide. The implant releases the medication slowly, allowing gradual absorption into the systemic circulation. 

Distribution 

exenatide is extensively distributed throughout the body. 

Metabolism 

exenatide undergoes extensive enzymatic degradation, primarily through proteolytic cleavage and enzymatic degradation by peptidases. The metabolism of exenatide occurs predominantly in the kidney, plasma, and tissues. 

Elimination and Excretion 

exenatide is eliminated primarily by renal clearance. After administration, exenatide undergoes degradation into smaller peptides and amino acids. The intact exenatide and its metabolites are primarily excreted through the kidneys. 

Adminstartion

Administration: 

exenatide subdermal implant is a medication used to treat type 2 diabetes. Here is a general overview of the administration of the exenatide subdermal implant. However, it’s important to note that specific instructions may vary based on the product’s formulation and the prescribing information. Therefore, it’s crucial to follow the instructions provided by your healthcare professional or the specific product labeling. Here are some general guidelines: 

• Implant Placement: A healthcare professional typically places The exenatide subdermal implant under the skin, usually in the abdominal area. The exact placement location may vary, and your healthcare provider should determine it. 
• Local Anesthesia: Depending on the specific product and the healthcare provider’s preference, local anesthesia may be used to numb the local area where the implant will be inserted. This can help minimize discomfort during the procedure. 
• Implant Insertion: The implant is inserted under the skin using a specialized delivery system once the area is prepared. The delivery system ensures that the implant is placed correctly and secured. 
• Post-Placement Care: After the implant is inserted, your physician will provide instruction on how to care for the implant site. This might include keeping the area clean and dry, avoiding strenuous activities that could disrupt the implant, and following specific guidelines for wound care. 
• Follow-Up Visits: Regular follow-up visits with your healthcare provider are important to monitor the effectiveness of the treatment, assess any side effects or complications, and also make any necessary adjustments to your diabetes management plan. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: exenatide subdermal implant 

Pronounced: [ ex-EN-a-tide ] 

Why do we use exenatide subdermal implant? 

exenatide subdermal implant is a medication used to treat type 2 diabetes. It generally belongs to a class of drugs known as the GLP-1 RAs (glucagon-like peptide-1 receptor agonists). The subdermal implant provides continuous and extended release of exenatide, allowing for once-weekly dosing. Here are the primary uses of exenatide subdermal implants: 

• Glycemic Control: exenatide subdermal implant improves glycemic control in individuals with type 2 diabetes. It helps regulate blood sugar levels by enhancing glucose-dependent insulin secretion from pancreatic beta cells. It also inhibits glucagon secretion, which reduces the production of glucose by the liver. These actions can help lower fasting and postprandial (after-meal) blood glucose levels. 
• Weight Management: exenatide subdermal implant has been associated with weight loss or maintenance in individuals with type 2 diabetes. It achieves this effect through various mechanisms, including appetite suppression, delayed gastric emptying (slowing down the rate at which the stomach empties), and increased feelings of fullness after meals. These actions can support efforts to manage body weight in individuals with type 2 diabetes.