Statins^A1,A2

Atorvastatin (Lipitor)

Fluvastatin

Lovastatin

Pitavastatin (Livalo)

Pravastatin (Pravachol)

Rosuvastatin (Crestor)

Simvastatin (Zocor)

Active liver disease and pregnancy

Generally better tolerated than other agents

Myopathies occur in < 1% of patients; increased incidence when used with fibrates

Rhabdomyolysis occurs in < 0.2% of patients

Liver function test results greater than three times the upper limit of normal occur in < 2% of patients

NNH = 255 for four years to cause one case of diabetes mellitus

Primary prevention: NNT = 56 for five years to prevent one major atherosclerotic cardiovascular disease event

Secondary prevention: NNT = 61 for five years to prevent one death

Most statins are taken once daily at bedtime

Ezetimibe (Zetia)^A3,A4

Ezetimibe/simvastatin (Vytorin)

No serious safety concerns with ezetimibe monotherapy, but it should be avoided in those with active liver disease when combined with a statin (e.g., Vytorin)

Well tolerated as monotherapy; adverse effects similar to placebo

Arthralgias and myalgias are more common when combined with a statin

Primary prevention: lacks clinical outcome data

Secondary prevention: NNT = 58 for six years to prevent one nonfatal myocardial infarction when combined with a moderate-intensity statin

Monotherapy reduces LDL-C by 18%

Taken once daily

No known effect on absorption of other medications

Ezetimibe may increase concentrations of cyclosporine (Sandimmune); closely monitor cyclosporine concentrations in patients taking both medications

Bile acid sequestrants^A5

Cholestyramine (Questran)

Colesevelam (Welchol)

Colestipol (Colestid)

Complete biliary or bowel obstruction

Constipation, nausea, and bloating are common, leading to poor adherence in most patients

May increase triglyceride level; use with caution when triglyceride level > 200 mg per dL (2.3 mmol per L)

Primary or secondary prevention: no effect on all-cause mortality

Reduces LDL-C by 15% to 30%

Many drug interactions; separate from warfarin (Coumadin), digoxin, and amiodarone by at least two hours

PCSK9 inhibitors^A6–A8

Alirocumab (Praluent)

Evolocumab (Repatha)

Serious hypersensitivity to any component of the formulation

No difference in serious adverse events when compared with placebo

Injection site reaction occurs in 6% to 7%

Associated with reduced risk of mortality (NNT = 246 to 1,354), myocardial infarction (NNT = 136 to 1,442), and lipid profile compared with no PCSK9 therapy in adults with hypercholesterolemia

Alirocumab: 75 mg subcutaneously once every two weeks (150 mg subcutaneously once every two weeks if LDL-C response is inadequate)

Evolocumab: 140 mg subcutaneously once every two weeks or 420 mg subcutaneously once monthly

Fibrates^A5,A9,A10

Gemfibrozil (Lopid)

Multiple prescription preparations of fenofibrate are available

Severe hepatic or renal disease

Gastrointestinal upset, rash, and abdominal pain are common

Decreased renal function and myopathies are rare

Increases risk of gallstones in 1% to 2%

Primary or secondary prevention: no effect on all-cause mortality

Lowers LDL-C and triglycerides by 5% to 20% and 20% to 50%, respectively

Increases HDL-C by 10% to 35%

Gemfibrozil: twice daily before meals

Micronized fenofibrate tablets and capsules should be taken with food

Nicotinic acid (niacin)^A5,A10-A12

Multiple OTC preparations

Multiple controlled-release prescription products

Severe peptic ulcer disease, chronic liver disease, and severe gout

Flushing is common; may be reduced with aspirin pretreatment

Discontinuation is common (one in 20 patients)

May increase uric acid and glucose levels

Increased risk of serious adverse events with niacin/laropiprant* vs. placebo:

Bleeding (NNH = 71)

Infection (NNH = 71)

New-onset diabetes mellitus (NNH = 71)

Gastrointestinal event (NNH = 100)

Musculoskeletal event (NNH = 142)

Dermatologic event (NNH = 333)

Primary or secondary prevention: no effect on all-cause mortality

Improves cholesterol levels when combined with statins

Primarily increases HDL-C by 15% to 35%

Taken twice daily with food

OTC preparations may be less effective but have fewer adverse effects

Omega-3 fatty acids^A13,A14

Multiple OTC preparations

Lovaza

Vascepa

Use with caution in patients with fish allergy

Dyspepsia, burping, and fishy taste more common

Primary and secondary prevention: no effect on all-cause mortality

Two to four prescription capsules taken once or twice daily based on preparation†

OTC preparations may require multiple capsules to achieve doses used in clinical trials