Mechanism of Action of DPP-4 Inhibitors

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Questions and Answers

Which statement accurately describes the mechanism of action of acarbose and miglitol?

They stimulate insulin release

They cause hypoglycemia when used alone

They increase insulin sensitivity

They delay carbohydrate digestion by inhibiting α-glucosidase enzymes (correct)

What is a notable characteristic of acarbose's pharmacokinetics?

It is excreted unchanged by the kidney

It is metabolized primarily by the liver

It is poorly absorbed and metabolized primarily by intestinal bacteria (correct)

It is well absorbed

Which adverse effect is commonly associated with acarbose and miglitol use?

Weight gain

Insulin resistance

Hypoglycemia

Flatulence (correct)

How do alogliptin, linagliptin, saxagliptin, and sitagliptin differ in their excretion?

They are excreted unchanged by the kidney Signup and view all the answers

Which class of drugs include alogliptin, linagliptin, saxagliptin, and sitagliptin?

Dipeptidyl peptidase-4 (DPP-4) inhibitors Signup and view all the answers

Why are patients with inflammatory bowel disease advised against using acarbose and miglitol?

Due to the risk of exacerbating gastrointestinal adverse effects like diarrhea Signup and view all the answers

What is the mechanism of action of DPP-4 inhibitors in the treatment of diabetes?

Prolonging the activity of incretin hormones like GLP-1 Signup and view all the answers

Which one of the following statements about DPP-4 inhibitors is FALSE?

They can be used in combination with GLP-1 receptor agonists Signup and view all the answers

Which DPP-4 inhibitor is primarily eliminated via the enterohepatic system?

Linagliptin Signup and view all the answers

What is the primary route of elimination for saxagliptin?

Renal excretion Signup and view all the answers

Which of the following is NOT a common adverse effect associated with DPP-4 inhibitors?

Cardiovascular events Signup and view all the answers

What is a rare but serious adverse effect that may occur with the use of DPP-4 inhibitors?

Pancreatitis Signup and view all the answers

What is the mechanism of action of sodium–glucose cotransporter 2 (SGLT2) inhibitors like canagliflozin?

Inhibiting SGLT2 to decrease glucose reabsorption Signup and view all the answers

Why are SGLT2 inhibitors not indicated for the treatment of hypertension?

They may reduce systolic blood pressure Signup and view all the answers

How are drugs like canagliflozin, dapagliflozin, empagliflozin, and ertugliflozin metabolized in the body?

Metabolized by glucuronidation to inactive metabolites Signup and view all the answers

Which of the following should be avoided in patients with renal dysfunction based on the text?

SGLT2 inhibitors like canagliflozin Signup and view all the answers

What cardiovascular risk should be considered when using alogliptin and saxagliptin in patients?

Risk of heart failure hospitalizations Signup and view all the answers

For which of the SGLT2 inhibitors is there an additional indication to reduce cardiovascular death in patients with type 2 diabetes and cardiovascular disease?

Empagliflozin Signup and view all the answers

Study Notes

Mechanism of Action and Pharmacokinetics of Diabetes Medications

Acarbose and miglitol inhibit intestinal alpha-glucosidases, delaying carbohydrate digestion and absorption.
Acarbose has a notable characteristic of being minimally absorbed from the gut, with the majority of the dose being excreted in the feces.

Adverse Effects of Diabetes Medications

Acarbose and miglitol are commonly associated with gastrointestinal adverse effects, such as diarrhea, flatulence, and abdominal pain.
Patients with inflammatory bowel disease are advised against using acarbose and miglitol due to the risk of exacerbating their condition.

DPP-4 Inhibitors

Alogliptin, linagliptin, saxagliptin, and sitagliptin are DPP-4 inhibitors, which work by increasing the levels of active incretin hormones, such as GLP-1 and GIP, to improve glucose tolerance.
The main difference in excretion among DPP-4 inhibitors is that alogliptin is primarily excreted in the urine, linagliptin is primarily excreted in the enterohepatic system, saxagliptin is primarily excreted in the feces, and sitagliptin is primarily excreted in the urine.
A false statement about DPP-4 inhibitors is that they are associated with a high risk of hypoglycemia.
Saxagliptin is primarily eliminated via the enterohepatic system.
The primary route of elimination for saxagliptin is hepatic.
A common adverse effect not associated with DPP-4 inhibitors is weight gain.
A rare but serious adverse effect that may occur with the use of DPP-4 inhibitors is angioedema.

SGLT2 Inhibitors

SGLT2 inhibitors like canagliflozin work by reducing the reabsorption of glucose in the kidney, leading to increased glucose excretion in the urine.
SGLT2 inhibitors are not indicated for the treatment of hypertension, although they may have a secondary effect of lowering blood pressure.
Drugs like canagliflozin, dapagliflozin, empagliflozin, and ertugliflozin are metabolized in the body via UGT1A9 and UGT2B7-mediated glucuronidation.
SGLT2 inhibitors should be avoided in patients with renal dysfunction due to the risk of adverse effects.
A cardiovascular risk to be considered when using alogliptin and saxagliptin in patients is the risk of cardiovascular death and hospitalization for heart failure.
Empagliflozin is the only SGLT2 inhibitor with an additional indication to reduce cardiovascular death in patients with type 2 diabetes and cardiovascular disease.

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Description

Learn about how DPP-4 inhibitors work by inhibiting the enzyme responsible for inactivating incretin hormones, leading to increased insulin release and reduced glucagon secretion. Explore their use as monotherapy or in combination with other diabetes medications.