Classes
DEA Class; Rx
Common Brand Names; Vytorin
- Lipid-Lowering Agents, Statins;
- HMG-CoA Reductase Inhibitors
Description
Oral antilipemic combination of a potent cholesterol absorption inhibitor (ezetimibe) and HMG-CoA reductase inhibitor (simvastatin); results in synergistic cholesterol-lowering effects; 10—80 mg of simvastatin with ezetimibe achieves LDL reductions of approximately > 51%
Used for primary hypercholesterolemia or mixed hyperlipidemia; also effective for homozygous familial hypercholesterolemia
Myopathy, including rhabdomyolysis, is greater in patients receiving 80 mg/day of simvastatin compared to lower doses or other statin therapies; therefore, 10/80 mg dose is restricted to patients who have taken 10/80 mg/day chronically (e.g. >= 12 months) without evidence of myopathy
Indications
Indicated for the treatment of primary heterozygous familial hypercholesterolemia and nonfamilial hypercholesterolemia or mixed hyperlipoproteinemia as an adjunct to diet to reduce total-C, LDL-C, Apo B, triglycerides, and non-HDL-C and to increase HDL-C.
Contraindications
Hypersensitivity to either component
Active liver disease, or unexplained elevated transaminases
Women who are pregnant or may become pregnant
Lactation
Concomitant administration with strong CYP3A4 inhibitors (eg, itraconazole, ketoconazole, erythromycin, clarithromycin, posaconazole, voriconazole, HIV protease inhibitors, nefazodone, cobicistat), fibrates (including gemfibrozil), cyclosporine, and danazol
Adverse Effects
- Headache (6.8%)
- Upper respiratory tract infection (3.9%)
- Myalgia (3.5%)
- Increased ALT (4%)
- Influenza (2.6%)
- Pain in extremity (2.3%)
- Erectile dysfunction
- Interstitial lung disease
- Rare reports of cognitive impairment (eg, memory loss, forgetfulness, amnesia, memory impairment, confusion) associated with statin use
Warnings
Discontinue if markedly elevated CPK levels occur or myopathy is diagnosed or suspected
Increased HbA1c and fasting serum glucose levels reported with HMG-CoA reductase inhibitors
Avoid use in severe renal impairment
High potential for drug interactions
Pregnancy and Lactation
Contraindicated in women who are or may become pregnant
Lipid lowering drugs offer no benefit during pregnancy, because cholesterol and cholesterol derivatives are needed for normal fetal development
Unknown if simvastatin excreted in human milk; because a small amount of another drug in this class is excreted in human milk and because of the potential for serious adverse reactions in nursing infants, women taking simvastatin should not breastfeed
Maximum Dosage
10 mg/day PO ezetimibe and 40 mg/day PO simvastatin for most patients; 80 mg/day PO simvastatin for patients already taking 80 mg/day chronically without evidence of myopathy.
10 mg/day PO ezetimibe and 40 mg/day PO simvastatin for most patients; 80 mg/day PO simvastatin for patients already taking 80 mg/day chronically without evidence of myopathy.
10 mg/day PO ezetimibe and 40 mg/day PO simvastatin.
>= 10 years: 10 mg/day PO ezetimibe and 40 mg/day PO simvastatin.
< 10 years: Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Simvastatin/ezetimibe
tablet
- 10mg/10mg
- 10mg/20mg
- 10mg/40mg
- 10mg/80mg
