Zetia: Targeted Cholesterol Reduction for Better Cardiovascular Health
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Synonyms | |||
Zetia (ezetimibe) is a prescription medication specifically designed to lower elevated levels of low-density lipoprotein (LDL) cholesterol, often referred to as “bad” cholesterol. It operates through a unique mechanism of action, distinct from statins, by selectively inhibiting the absorption of cholesterol in the small intestine. This targeted approach makes it a valuable therapeutic option, both as a monotherapy for patients who cannot tolerate statins and as a complementary agent in combination therapy for those requiring additional LDL-C reduction. By effectively reducing intestinal cholesterol uptake, Zetia directly addresses a key pathway in cholesterol management, contributing to a comprehensive strategy for mitigating cardiovascular risk.
Features
- Active pharmaceutical ingredient: Ezetimibe
- Available in 10 mg oral tablets
- Unique mechanism: selectively inhibits cholesterol absorption at the brush border of the small intestine
- Does not inhibit cholesterol synthesis in the liver or increase bile acid excretion
- Can be taken with or without food, offering dosing flexibility
- Often used in combination with HMG-CoA reductase inhibitors (statins) for additive effect
Benefits
- Significantly reduces LDL-C levels by targeting a complementary pathway to statin therapy
- Provides an effective lipid-lowering option for patients statin-intolerant or with contraindications to statin use
- Lowers non-HDL cholesterol and apolipoprotein B, contributing to comprehensive lipid management
- Demonstrates a favorable safety and tolerability profile in clinical studies
- May help reduce cardiovascular event risk when combined with statin therapy in appropriate patient populations
- Offers convenient once-daily dosing that supports long-term adherence to therapy
Common use
Zetia is primarily indicated as adjunctive therapy to diet for the reduction of elevated total cholesterol, LDL cholesterol, and apolipoprotein B in patients with primary hyperlipidemia, either as monotherapy or in combination with an HMG-CoA reductase inhibitor (statin). It is also indicated for the reduction of elevated sitosterol and campesterol levels in patients with homozygous sitosterolemia. Clinicians frequently prescribe Zetia for patients who have not achieved their LDL-C goals with statin monotherapy alone, or for those who are unable to tolerate effective doses of statins due to muscle-related adverse effects. The medication is typically incorporated into a comprehensive treatment plan that includes therapeutic lifestyle changes, such as a heart-healthy diet and regular physical activity.
Dosage and direction
The recommended dosage of Zetia is 10 mg once daily, administered orally with or without food. When used in combination with a statin, Zetia may be administered simultaneously with the statin, or at any time of day separate from the statin dose. For patients with moderate to severe hepatic impairment, no dosage adjustment is necessary. In patients with renal impairment, including those on hemodialysis, no dosage adjustment is required. The tablet should be swallowed whole and not crushed, chewed, or dissolved. Patients should be advised to take Zetia at approximately the same time each day to maintain consistent therapeutic levels and support medication adherence.
Precautions
Before initiating Zetia therapy, healthcare providers should obtain a complete lipid profile and assess liver function tests. Patients should be advised that Zetia is not a substitute for dietary management of hyperlipidemia and that they should continue their cholesterol-lowering diet during treatment. Regular monitoring of liver enzymes is recommended, particularly when Zetia is used in combination with a statin. Patients should be counseled to report any unexplained muscle pain, tenderness, or weakness promptly, especially if accompanied by fever or malaise. Although rare, there have been reports of myopathy and rhabdomyolysis associated with ezetimibe, particularly when used with statins. Pregnancy and breastfeeding considerations should be discussed, as the safety of Zetia in these populations has not been established.
Contraindications
Zetia is contraindicated in patients with known hypersensitivity to any component of the formulation. The combination of Zetia with a statin is contraindicated in patients with active liver disease or unexplained persistent elevations in hepatic transaminase levels. Additionally, the combination therapy is contraindicated in pregnant and breastfeeding women, as well as in nursing mothers. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency, or glucose-galactose malabsorption should not take Zetia due to the lactose content in the tablet formulation.
Possible side effects
The most commonly reported adverse reactions in clinical trials (occurring in ≥2% of patients and at a rate greater than placebo) included: upper respiratory tract infection, diarrhea, arthralgia, sinusitis, and pain in extremity. Less common but potentially serious side effects may include: elevated liver enzymes, myopathy (muscle pain or weakness), rhabdomyolysis (though rare), hypersensitivity reactions including angioedema and rash, and gastrointestinal disturbances. When used in combination with statins, the side effect profile generally reflects the combined effects of both medications. Patients should be monitored for any signs of hepatic dysfunction or muscle-related symptoms throughout therapy.
Drug interaction
Zetia has no clinically significant interactions with many commonly prescribed medications, including warfarin, digoxin, and oral contraceptives. However, when used concomitantly with cyclosporine, blood levels of both medications may be increased, requiring careful monitoring. Fibrates may increase the risk of cholelithiasis when combined with Zetia, and this combination should generally be avoided unless the potential benefit outweighs the risk. Cholestyramine and other bile acid sequestrants may decrease the absorption of Zetia; therefore, Zetia should be administered at least 2 hours before or 4 hours after administration of a bile acid sequestrant. Clinicians should review all concomitant medications, including over-the-counter products and herbal supplements, before initiating Zetia therapy.
Missed dose
If a dose of Zetia is missed, patients should take it as soon as they remember, unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should not take a double dose to make up for a missed dose. Healthcare providers should educate patients about the importance of consistent dosing while reassuring them that occasional missed doses are unlikely to significantly impact long-term cholesterol management, though consistent adherence is important for optimal therapeutic effect.
Overdose
In the event of overdose, supportive measures should be instituted based on clinical presentation. There is no specific antidote for Zetia overdose. During clinical trials, doses up to 50 mg daily were administered and generally well-tolerated. Given its extensive binding to plasma proteins, Zetia is not expected to be efficiently removed by hemodialysis. In cases of significant overdose, gastric lavage may be considered if performed soon after ingestion. Symptomatic and supportive care should be provided based on the patient’s clinical status, with particular attention to possible gastrointestinal symptoms.
Storage
Zetia tablets should be stored at room temperature, between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). The medication should be kept in its original container with the lid tightly closed to protect from moisture and light. Tablets should be kept out of reach of children and pets. Patients should be advised not to use Zetia beyond the expiration date printed on the packaging and to properly dispose of any unused medication according to local regulations or medication take-back programs.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Zetia is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Individual patient responses to therapy may vary, and treatment decisions should be based on a comprehensive assessment of the patient’s medical history, current health status, and risk factors. Patients should not initiate, discontinue, or change their dosage of Zetia without consulting their healthcare provider. The full prescribing information should be consulted for complete details regarding use, warnings, and precautions.
Reviews
Clinical studies and post-marketing experience have demonstrated Zetia’s efficacy in reducing LDL cholesterol levels by approximately 15-20% as monotherapy and providing additional 20-25% reduction when added to statin therapy. Many clinicians appreciate its unique mechanism of action and favorable safety profile. Patients who are statin-intolerant often report successful cholesterol management with Zetia monotherapy. However, some experts note that while Zetia effectively lowers LDL-C, outcome studies have shown mixed results regarding cardiovascular event reduction compared to statins. The medication continues to be valued as an important tool in the lipid management arsenal, particularly for specific patient populations and as part of combination therapy strategies.