vildagliptin

Action and Spectrum

Actions and spectrum:

vildagliptin is an oral antidiabetic medication that belongs to the class of dipeptidyl peptidase-4 inhibitors. Its main action is to inhibit the enzyme DPP-4, which is responsible for breaking down incretin hormones like glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). By inhibiting DPP-4, vildagliptin increases the levels of GLP-1 and GIP, leading to enhanced insulin secretion from the pancreas and reduced glucagon release. This results in improved glucose control and regulation of blood sugar levels with type 2 diabetes.

The spectrum of vildagliptin’s action is primarily focused on its effect on glucose metabolism in patients with type 2 diabetes, helping to lower blood sugar levels and improve glycemic control.

Drug Interaction

Adverse Reaction

Frequency not defined

Headache

Upper respiratory tract infection

Dizziness

Nausea & vomiting

abdominal pain

Asthenia

Anaphylactic reactions

Hepatitis

Nasopharyngitis

Hypoglycemia

Tremor

Rash

Increased liver enzymes

Angioedema

Bullous pemphigoid

Black Box Warning

Black Box Warning:

There were no black box warnings is associated with vildagliptin.

Contraindication / Caution

Contraindication/Caution:

Contraindication:

• Hypersensitivity: vildagliptin should not be used in individuals who have a known hypersensitivity or allergy to vildagliptin or any of its components.
• Type 1 Diabetes: vildagliptin is not used for the treatment of type 1 diabetes, as it is ineffective in this condition.
• Diabetic Ketoacidosis: vildagliptin should not be used in individuals with diabetic ketoacidosis, a serious complication of uncontrolled diabetes.
• Severe Hepatic Impairment: vildagliptin is contraindicated in patients with severe hepatic impairment because its metabolism relies on the liver.

Caution:

• Pancreatitis: vildagliptin should be used with caution in individuals with a history of pancreatitis, as there have been rare reports of pancreatitis occurring with the use of DPP-4 inhibitors, which includes vildagliptin.
• Hypoglycemia: vildagliptin, when used in combination with other antidiabetic medications like insulin or sulfonylureas, can increase the risk of hypoglycemia (low blood sugar). Caution is needed, especially in patients at higher risk of hypoglycemia, such as those with renal impairment or the elderly.
• Liver Function: vildagliptin is metabolized in the liver, so caution is advised in patients with liver impairment. Dosage adjustments may be necessary in individuals with moderate to severe hepatic impairment.
• Heart Failure: Some studies have suggested an association between DPP-4 inhibitors, including vildagliptin, and heart failure. Patients with a history of heart failure or at risk for heart failure should be monitored closely while on vildagliptin.
• Renal Function: vildagliptin is primarily excreted through the kidneys. Caution is recommended in patients with renal impairment, and dosage adjustments may be necessary based on renal function.
• Pregnancy and Breastfeeding: vildagliptin use during pregnancy and breastfeeding is not well-established.

Comorbidities:

• Hypertension: Diabetes and hypertension often coexist, and both conditions can exacerbate each other, increasing the risk of cardiovascular complications.
• Dyslipidemia: Many individuals with type 2 diabetes also have dyslipidemia, characterized by abnormal levels of cholesterol & triglycerides thereby increases the risk of cardiovascular disease.
• Obesity: It is a risk factor for developing type 2 diabetes, and it often occurs alongside the condition. Managing weight is crucial in diabetes management.
• Cardiovascular disease: Diabetes is a risk factor for heart disease, heart attack & stroke.
• Chronic Kidney Disease (CKD): Diabetes is one of the leading causes of chronic kidney disease. When diabetes is not well-controlled, it can lead to kidney damage over time.
• Retinopathy: Diabetes can affect the eyes and lead to diabetic retinopathy, which can result in vision impairment or blindness if left untreated.
• Peripheral Neuropathy: Diabetes-related nerve damage, known as peripheral neuropathy, can cause tingling, numbness, or pain in the extremities.
• Non-Alcoholic Fatty Liver Disease (NAFLD): There is a higher prevalence of NAFLD in patients with diabetes, especially those with uncontrolled blood sugar levels.

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: B

Lactation: excreted into human milk: unknown

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:

vildagliptin is an oral antidiabetic medication belonging to the class of dipeptidyl peptidase-4 (DPP-4) inhibitors. It works by inhibiting the DPP-4 enzyme, which plays a role in the breakdown of incretin hormones like GLP-1 (glucagon-like peptide-1). Incretins are essential in regulating blood sugar levels by increasing insulin secretion and reducing glucagon release, thereby lowering blood glucose levels. By inhibiting DPP-4, vildagliptin prolongs the activity of these incretins, leading to enhanced insulin production and reduced glucose output from the liver. This mechanism of action improves glycemic control in patients with type 2 diabetes. vildagliptin does not stimulate insulin secretion in the absence of elevated blood sugar levels, reducing the risk of hypoglycemia.

Pharmacodynamics:

• GLP-1 Action: GLP-1 enhances insulin secretion from pancreatic beta cells due to the increased blood glucose levels. It also suppresses glucagon release from pancreatic alpha cells, which reduces glucose production by the liver. These combined actions lead to a decrease in blood glucose levels.
• GIP Action: GIP also stimulates insulin release in response to meals, further contributing to the control of postprandial glucose levels.
• Insulin Sensitivity: vildagliptin may also improve insulin sensitivity in peripheral tissues, leading to increased glucose uptake and utilization.
• HbA1c Reduction: By promoting insulin release and reducing glucagon secretion, vildagliptin effectively lowers HbA1c levels.
• Preservation of Beta Cell Function: In addition to its effects on glycemic control, vildagliptin has shown potential in preserving beta cell function, thereby supporting long-term diabetes management.
• No Hypoglycemia Risk: vildagliptin’s mechanism of action is glucose-dependent, which means it only stimulates insulin secretion when blood glucose levels are increased, reducing the risk of hypoglycemia when compared with other antidiabetic medications.

Pharmacokinetics:

Absorption

vildagliptin is rapidly absorbed from the gastrointestinal tract after oral administration. Its absolute bioavailability is approximately 85%.

Distribution

vildagliptin has a moderate volume of distribution, indicating that it distributes throughout the body tissues. It binds extensively to plasma proteins, primarily to albumin.

Metabolism

vildagliptin undergoes limited hepatic metabolism via hydrolysis to form an inactive metabolite (LAY151) and is not extensively metabolized by the liver.

Elimination and excretion

vildagliptin is primarily eliminated renally, with the majority (approximately 85%) of the dose excreted unchanged in the urine. The remaining portion of the drug is excreted in the feces. The elimination half-life (t½) of vildagliptin is short, ranging from 1.5 to 2.5 hours.

Adminstartion

Administration:

vildagliptin is available as oral tablets and should be administered by mouth. The typical recommended dose for adults with type 2 diabetes is usually 50 mg twice daily. It can be taken with or without food, as food intake does not significantly affect its absorption or bioavailability. However, it is essential to follow the specific dosing instructions or as mentioned on the medication label. vildagliptin should not be used to treat type 1 diabetes or diabetic ketoacidosis.

Patient Information Leaflet

Patient information leaflet

Generic Name: vildagliptin

Pronounced: (vil-da-GLIP-tin)

Why do we use vildagliptin?

vildagliptin is used in the treatment of type 2 diabetes mellitus. It is typically prescribed to help control blood sugar levels in patients with this condition. vildagliptin is classified as an oral antidiabetic drug that belongs to the class of dipeptidyl peptidase-4 (DPP-4) inhibitors. vildagliptin helps to improve glycemic control & reduces the risk of associated complications with uncontrolled diabetes. vildagliptin is often used in combination with other antidiabetic medications or as a monotherapy, depending on the individual patient’s needs and medical history. As with any medication, it should be used under the guidance of a healthcare professional.