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All about: Ezetimibe/Simvastatin

Big Image Pronouncation: (ezz-ET-ih-mibe/SIM-vah-STAT-in)
Class: Antihyperlipidemic combination

Trade Names:
Vytorin 10/10
- Tablets 10 mg ezetimibe/10 mg simvastatin

Trade Names:
Vytorin 10/20
- Tablets 10 mg ezetimibe/20 mg simvastatin

Trade Names:
Vytorin 10/40
- Tablets 10 mg ezetimibe/40 mg simvastatin

Trade Names:
Vytorin 10/80
- Tablets 10 mg ezetimibe/80 mg simvastatin

Mechanism of Action

Pharmacology

Ezetimibe

Inhibits absorption of cholesterol by the small intestine.

Simvastatin

Increases rate at which body removes cholesterol from blood and reduces production of cholesterol by inhibiting enzyme that catalyzes early rate-limiting step in cholesterol synthesis.

Indications and Usage

Adjunctive treatment to diet for reduction of elevated total-cholesterol, LDL cholesterol, triglycerides, non-HDL cholesterol, and apolipoprotein B (Apo B), and to increase HDL cholesterol in patients with primary hypercholesterolemia or mixed hyperlipidemia; as an adjunct to other lipid-lowering treatment for the reduction of total cholesterol and LDL cholesterol in patients with homozygous familial hypercholesterolemia.

Contraindications

Active liver disease or unexplained persistent elevations in serum transaminases; pregnancy and lactation; hypersensitivity to any component of the product.

Dosage and Administration

Primary Hypercholesterolemia
Adults

PO Dosage range is 10 mg ezetimibe/10 mg simvastatin through 10/80 mg daily. Start with 10/20 mg daily. Lipid levels may be analyzed after 2 or more wk and dosage adjusted. For patients requiring a large reduction in LDL cholesterol (greater than 55%), therapy may be started at 10/40 mg daily.

Homozygous Familial Hypercholesterolemia
Adults

PO 10/40 mg daily or 10/80 mg daily in the evening. Use as an adjunct to other lipid lowering treatments.

General Advice

Administer without regard to meals. Administer with food if GI upset occurs.

Storage/Stability

Store tablets at controlled room temperature (68° to 77°F).

Drug Interactions

Amiodarone, verapamil

Risk of myopathy/rhabdomyolysis may be increased. Dose of ezetimibe/simvastatin should not exceed 10/20 mg daily.

Bile acid sequestrant (eg, cholestyramine)

Ezetimibe concentrations may be reduced, decreasing the therapeutic effect. Give at least 2 h before or 4 h after the bile acid sequestrant.

Cyclosporine

Exposure to ezetimibe may be increased, especially in patients with severe renal insufficiency. Dose of ezetimibe/simvastatin should not exceed 10/10 mg daily.

Digoxin

Digoxin plasma concentrations may be slightly elevated.

Fibrates (eg, fenofibrate, gemfibrozil)

Ezetimibe concentrations may be increased.

Potent inhibitors of CYP3A4 (eg, clarithromycin, cyclosporine, erythromycin, HIV protease inhibitors, itraconazole, ketoconazole, nefazodone, large quantities of grapefruit juice [greater than 1 quart daily])

May reduce the elimination of simvastatin, increasing the risk of myopathy.

Propranolol

Simvastatin peak plasma concentrations may be reduced.

Warfarin

The anticoagulant effect, as measured by the INR, may be modestly potentiated.

Laboratory Test Interactions

None well documented.

Adverse Reactions

The incidence stated for the following adverse reaction were reported with Vytorin (ezetimibe/simvastatin) administration. Adverse reactions occurring with administration of either ezetimibe or simvastatin can be found listed in their respective monographs.

CNS

Headache (7%).

Musculoskeletal

Myalgia (4%); pain in extremity (2%).

Pulmonary

Upper respiratory tract infection (4%).

Miscellaneous

Influenza (3%).

Precautions

Monitor

Lipid levels

Ensure that lipid levels are measured before therapy is started, at least 2 wk after starting ezetimibe/simvastatin therapy or changing the dose, and then periodically thereafter.


Pregnancy

Category X .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hepatic Function

Use is not recommended in patients with moderate or severe hepatic insufficiency.

Hepatotoxicity

Ensure that serum transaminases are determined before starting therapy and periodically thereafter as clinically indicated. For patient being titrated to 10/80 mg dose, ensure that transaminases are determined before titration, 3 mo after titration to 10/80 mg dose, and periodically thereafter (eg, every 6 mo) for first year of treatment. If elevated serum transaminase levels develop during treatment, repeat levels more frequently. If transaminase levels rise to 3 times upper limit of normal or greater and persist, notify health care provider. Be prepared to discontinue therapy.

Liver dysfunction

Use with caution in patients who consume substantial quantities of alcohol or who have history of liver disease. Marked, persistent increases in serum transaminases can occur.

Rhabdomyolysis

Ensure that therapy is temporarily withheld in patient with an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (eg, sepsis, hypotension, major surgery).

Secondary causes of hyperlipidemia

Rule out or treat secondary causes of hyperlipidemia before starting treatment.

Skeletal muscle effects

Rhabdomyolysis with renal dysfunction secondary to myoglobinuria has occurred with statin administration. Consider myopathy in any patient with diffuse myalgias, muscle tenderness or weakness, or marked CPK elevation.

Patient Information

  • Explain name, dose, action, potential side effects of medication, and LDL-C goal.
  • Advise patient that dose of medication may change, based on results of cholesterol blood tests, in an effort to reach LDL-C goal.
  • Review other substances (eg, grapefruit juice) and medications (eg, potent CYP3A4 inhibitors, fibrates) that should not be taken with this medication.
  • Advise patient to take prescribed dose once daily in the evening without regard to meals, but to take with food if stomach upset occurs.
  • Advise patient that if a dose is missed to take as soon as remembered but to never take more than 1 dose of medicine a day.
  • Caution patient not to change the dose or stop taking unless advised by health care provider.
  • Advise patient that drug helps control, but does not cure, cholesterol abnormality and to continue taking drug as prescribed when LDL-C goal has been met.
  • Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
  • Advise patient who is also taking a bile acid sequestrant (eg, cholestyramine) to take the ezetimibe/simvastatin at least 2 h before or 4 h after the sequestrant.
  • Instruct patient to immediately notify health care provider if experiencing any unexplained muscle pain, tenderness, and/or weakness, or if they note any other unusual feelings.
  • Emphasize to patient importance of other modalities on cholesterol control: dietary changes (reduced saturated fat intake, increase soluble fiber intake), weight control, regular exercise, smoking cessation.
  • Advise women of childbearing potential to use effective contraception during treatment with ezetimibe/simvastatin.

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