Non-Statin Lipid-Lowering Pharmacotherapy Flashcards

What is the primary mechanism of action of ezetimibe?

Answer: Blocks cholesterol absorption at the Niemann-Pick C1-Like 1 (NPC1L1) transporter in the small intestine

Ezetimibe selectively inhibits cholesterol absorption at the brush border of the small intestine by blocking the NPC1L1 transporter, reducing cholesterol delivery to the liver.

Which bile acid sequestrant is FDA-approved for both hypercholesterolemia and as an adjunct treatment for type 2 diabetes?

Answer: Colesevelam

Colesevelam (Welchol) is the only bile acid sequestrant with dual FDA approval for LDL-C lowering and improving glycemic control in adults with type 2 diabetes mellitus.

What is the expected LDL-C reduction with ezetimibe monotherapy?

Answer: 15–25%

Ezetimibe monotherapy typically reduces LDL-C by approximately 15–25%, making it useful as adjunctive therapy rather than a standalone alternative to statins.

Bile acid sequestrants are contraindicated in patients with triglyceride levels exceeding which threshold?

Answer: 400 mg/dL

Bile acid sequestrants can markedly increase triglyceride levels and are contraindicated when fasting triglycerides exceed 400 mg/dL due to the risk of acute pancreatitis.

The IMPROVE-IT trial studied ezetimibe added to simvastatin in patients with recent acute coronary syndrome. What was the primary finding?

Answer: A significant reduction in major adverse cardiovascular events

IMPROVE-IT demonstrated that simvastatin plus ezetimibe significantly reduced the composite primary endpoint of major adverse cardiovascular events compared to simvastatin alone, validating the 'lower is better' hypothesis for LDL-C.

What is the most clinically significant drug interaction concern with bile acid sequestrants?

Answer: They bind and reduce intestinal absorption of many co-administered medications

Bile acid sequestrants are positively charged resins that bind negatively charged molecules in the gut, reducing absorption of many drugs including warfarin, thyroid hormones, and fat-soluble vitamins; other medications should be taken 1 hour before or 4–6 hours after the sequestrant.

Which of the following is NOT classified as a bile acid sequestrant?

Answer: Ezetimibe

Ezetimibe is a selective cholesterol absorption inhibitor acting at the NPC1L1 transporter, not a bile acid sequestrant; cholestyramine, colestipol, and colesevelam are all bile acid-binding resins.