What is the brand name for ezetimibe (Zetia)?

Brand Name for Ezetimibe

The brand name for ezetimibe is Zetia. 1, 2

Medication Overview

Ezetimibe (Zetia) is a cholesterol absorption inhibitor that works by:

• Selectively inhibiting intestinal uptake of cholesterol at the brush border of the small intestine
• Binding to the Niemann-Pick C1 Like 1 (NPC1L1) protein, which prevents cholesterol absorption
• Reducing both dietary and biliary cholesterol absorption without affecting absorption of fat-soluble vitamins or triglycerides 2

Clinical Efficacy

Ezetimibe provides significant lipid-lowering benefits:

• As monotherapy: Reduces LDL cholesterol by approximately 15-20% 1
• As add-on to statin therapy: Provides an additional 25% reduction in LDL-C 2
• In the IMPROVE-IT trial, adding ezetimibe to statin therapy demonstrated cardiovascular benefit, especially among patients with type 2 diabetes 3

Pharmacokinetic Properties

• Rapidly absorbed after oral administration and extensively metabolized (>80%) to the pharmacologically active ezetimibe-glucuronide
• Maximum concentrations reached 1-2 hours after administration
• Terminal half-life of approximately 22 hours
• Can be administered once daily (10 mg) without regard to food or time of day 4
• Undergoes enterohepatic recirculation which ensures repeated delivery to the intestinal site of action while limiting peripheral exposure 2

Clinical Applications

Ezetimibe is commonly used in:

1. Patients who need modest LDL-C reductions (15-20%)
2. Patients intolerant to statins or other lipid-lowering medications
3. Combination therapy with statins when:
   • Patients cannot tolerate high-dose statins
   • Additional LDL-C reduction is needed despite maximum statin doses 1, 3
4. Patients with statin-associated muscle symptoms, as a non-statin alternative 3

Safety Profile

Ezetimibe is generally well-tolerated:

• Adverse event profile similar to placebo when used as monotherapy
• No significant effects on major drug metabolizing enzymes (CYP450), reducing potential drug interactions
• Most common side effects include mild gastrointestinal discomfort 3, 4

Important Drug Interactions

• No clinically significant interactions with most commonly prescribed medications
• Should be administered several hours apart from bile acid sequestrants (like colestyramine) to avoid reduced bioavailability
• Caution advised when co-administered with cyclosporine 4

Ezetimibe represents an important option in the lipid management armamentarium, particularly for patients who cannot achieve LDL-C goals with statins alone or who experience statin intolerance.