• Primary hyperlipidemia, including heterozygous familial hypercholesterolemia (as monotherapy [in adults only] or in combination with a statin).
• Mixed hyperlipidemia (in combination with fenofibrate).
• Homozygous familial hypercholesterolemia (in combination with a statin and other low-density lipoprotein cholesterol [LDL-C] lowering therapies).
• Familial sitosterolemia.

Contraindicated in:

• Hypersensitivity
• When a statin, fenofibrate, or other LDL-C lowering therapy is contraindicated (when used in combination with statin, fenofibrate, or other LDL-C lowering therapy)
• Moderate or severe hepatic impairment.

Use Cautiously in:

• OB: Safety not established in pregnancy
• Lactation: Safety not established in breastfeeding
• Pedi: Children <10 yr (safety and effectiveness not established).

Derm: rash.

GI: ↑liver enzymes, cholecystitis, cholelithiasis, nausea, pancreatitis.

MS: myopathy, RHABDOMYOLYSIS.
Misc: ANGIOEDEMA.

Drug-Drug:

• Effects may be ↓ by cholestyramine or other bile acid sequestrants.
• Concurrent use of fibrates may ↑ levels and the risk of cholelithiasis.
• Cyclosporine may ↑ levels.
• May ↑ risk of rhabdomyolysis when used with HMG CoA-reductase inhibitors.

(Generic available)

• Tablets: 10 mg;
• In combination with: rosuvastatin (Roszet); simvastatin (Vytorin); see Appendix [not included in this PDA edition].

• PO (Adults): 10 mg once daily.

Zetia

• Inhibits absorption of cholesterol in the small intestine.

• Reduction of LDL-C concentrations.
• Reduction of sitosterol and campesterol concentrations.

Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: cholesterol absorption inhibitors

Absorption: Following absorption, rapidly converted to ezetimibe-glucuronide, which is active. Bioavailability is variable.

Distribution: Unknown.

Metabolism/Excretion: Undergoes enterohepatic recycling, mostly eliminated in feces, minimal renal excretion.

Half-life: 22 hr.

Ezetrol

• Instruct patient to take ezetimibe as directed, at the same time each day, even if feeling well. Take missed doses as soon as remembered, but do not take more than 1 dose/day. Medication helps control but does not cure elevated serum cholesterol levels. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of change.
• Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking. Ezetimibe does not assist with weight loss.
• Instruct patient to notify health care professional if unexplained muscle pain, tenderness, or weakness occur. Risk may increase when used with HMG-CoA reductase inhibitors.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any other Rx, OTC, or herbal products.
• Advise patient to notify health care professional of medication regimen prior to treatment or surgery.
• Advise females of reproductive potential to notify health care professional promptly if pregnancy is planned or suspected or if breastfeeding. If regimen includes HMG-CoA reductase inhibitors, they are contraindicated in pregnancy.
• Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.

e-ZET-i-mibe