Ezetimibe – Cholesterol Absorption Inhibitor

 

Ezetimibe is a lipid-lowering agent that reduces cholesterol absorption in the intestine. Learn about its mechanism of action, uses, dosage, brand names, price, side effects, and contraindications.

Table of Contents:

1. Introduction  

2. Mechanism of Action  

3. Pharmacokinetics & Dynamics  

4. Indications & Drug of Choice  

5. Contraindications  

6. Side Effects  

7. Drug Interactions  

8. Dosage  

9. Brand Names  

10. Price  

11. Conclusion  

1. Introduction:

*Ezetimibe* is a *lipid-lowering medication* used to manage *hypercholesterolemia*. It works by *blocking intestinal absorption of cholesterol*, making it effective alone or in combination with statins for improving lipid profiles.

2. Mechanism of Action:

Ezetimibe selectively inhibits the *Niemann-Pick C1-Like 1 (NPC1L1)* transporter in the small intestine. This reduces the absorption of dietary and biliary cholesterol, leading to:

- ↓ Total cholesterol

- ↓ LDL-C (bad cholesterol)  

- Slight ↑ HDL-C (good cholesterol)

3. Pharmacokinetics & Dynamics:

| Absorption          | Rapid oral absorption  

| Bioavailability     | ~35–60%  

| Peak Plasma Time    | 1–2 hours  

| Half-Life           | ~22 hours  

| Metabolism          | Liver (glucuronidation)  

| Excretion           | Feces (~80%), urine (~11%)  

4. Indications & Drug of Choice:

- *Primary hyperlipidemia* (alone or with statins)

- *Familial hypercholesterolemia*

- *Sitosterolemia (rare lipid disorder)*

- *Alternative for statin-intolerant patients*

Drug of Choice: 

As add-on therapy to statins when LDL goals are not met or in statin-intolerant individuals.

5. Contraindications:

- Active liver disease (when used with statins)  

- Hypersensitivity to ezetimibe  

- Pregnancy & lactation (if used with statins)

6. Side Effects:

- Headache  

- Diarrhea  

- Myalgia  

- Fatigue  

- Elevated liver enzymes (with statins)  

- Rare: Rhabdomyolysis (when combined with statins)

7. Drug Interactions:

- *Statins:* ↑ risk of liver enzyme elevation  

- *Fibrates (especially gemfibrozil):* ↑ risk of gallstones

- *Bile acid sequestrants:* Reduce ezetimibe absorption (space doses)  

- *Cyclosporine:* May increase ezetimibe levels

8. Dosage:

- *Adult dose:* 10 mg once daily  

- *Pediatric use (≥10 years):* 10 mg once daily  

- *No dose adjustment* needed in mild-to-moderate renal or hepatic impairment (caution in severe hepatic dysfunction)

9. Brand Names:

 

- *Zetia* (USA)  

- *Ezedoc*  

- *Ezeday*  

- *Lipirex EZ*  

- *Ezita*  

- *Ezentia*

10. Price:

- *USA:* 8–15 per tablet (brand),1–3 (generic)  

- *India/Pakistan:* Rs. 15–40 per 10 mg tablet (generic)  

11. Conclusion:

*Ezetimibe* is a well-tolerated, effective lipid-lowering agent that complements statins in managing *dyslipidemia*. It provides a valuable option in statin-intolerant patients or when LDL-C goals are not achieved with statins alone. Monitoring liver function is advised when combined with other lipid-lowering therapies.