Ezetimibe

INTRODUCTION

Indications

Alone or with other agents (HMG CoA reductase inhibitors) in the management of dyslipidemias, including primary hypercholesterolemia, homozygous familial hypercholesterolemia, and homozygous sitosterolemia.

Action

Inhibits absorption of cholesterol in the small intestine. Therapeutic Effects: Lowering of cholesterol, a known risk factor for atherosclerosis.

Adverse Reactions/Side Effects

GI: cholecystitis, cholelithiasis, ↑ hepatic transaminases (with HMG CoA reductase inhibitors), nausea, pancreatitis. Derm: rash. Misc: ANGIOEDEMA.

PHYSICAL THERAPY IMPLICATIONS

Examination and Evaluation

• Monitor signs of angioedema, including rashes, raised patches of red or white skin (welts), burning/itching skin, swelling in the face, and difficulty breathing. Notify physician immediately of these signs.

• Report signs of gallbladder inflammation (cholecystitis) and gallstones (cholelithiasis), including sudden intense pain in the abdomen or right side, bloating, jaundice, loss of appetite, nausea, vomiting, chills, and fever. Report these signs to the physician.

• Be alert for signs of pancreatitis, including upper abdominal pain (especially after eating), indigestion, weight loss, and oily stools. Report these signs to the physician.

Interventions

• Design and implement aerobic exercise and endurance training programs to improve cardiovascular function and help reduce the risk of coronary heart disease.

Patient/Client-Related Instruction

• Remind patients to take medication as directed to control hyperlipidemia even though they are asymptomatic.

• Counsel patients about additional interventions to help control lipid disorders and improve cardiovascular health, including dietary modification, regular exercise, moderation of alcohol consumption, and smoking cessation.

• Instruct patient and family/caregivers to report other troublesome side effects such as severe or prolonged nausea or skin rash.

Pharmacokinetics

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

Distribution: Unknown.

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

Half-life: 22 hr.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Acute liver disease or unexplained laboratory evidence of liver disease (when used with HMG CoA reductase inhibitor); Moderate or severe hepatic insufficiency; Concurrent use of fibrates.

Use Cautiously in: OB: Lactation (use only if benefit to mother outweighs possible risks to infant); OB/Pedi: Pregnancy or children <10 yr (safety not established).

Interactions

Drug-Drug: Effects may be ↓ by cholestyramine or other bile acid sequestrants. Concurrent use of fibrates may ↑ blood levels of ezetimibe and also ↑ the risk of cholelithiasis. Cyclosporine may ↑ ...