Prescribing Focus:

Statins for the Management of Hyperlipidemia

Introduction
It is estimated that 102.2 million adults in the US have total blood cholesterol values of 200 mg/dL,
with about 35.7 million having levels 240 mg/dL, signicantly increasing the risk for cardiovascular
events (CV) in these patients.
1
Statinsor HMG-CoA reductase inhibitorshave demonstrated the ability
to reduce the risk of adverse CV events in diverse patient populations. This Prescribing Focus ofers
recommendations for the management of hyperlipidemia with statin therapy to decrease morbidity and
mortality in your patients with CV risk.
Lipoprotein Prole Testing in Adults
2
The National Cholesterol Education Program Adult Treatment Panel III (NCEP ATP III) recommends a
fasting lipoprotein prole test, including LDL-C screening every 5 years in all low-risk adults age 20 and
over. For those with diabetes or coronary heart disease, annual testing is recommended with an LDL-C
goal of <100 mg/dL. Measuring lipoprotein levels will help guide treatment and selection of appropriate
cholesterol-lowering drug therapies.
Use of Statins for Hyperlipidemia
2
The NCEP ATP III guideline recommends treatment of high blood cholesterol in adults, based on low-
density lipoprotein cholesterol (LDL-C) levels and a patients absolute risk for cardiovascular disease.
Both short-term (10-year) risk and long-term risk must be considered for treatment decisions. Those
with existing CHD, or CHD risk equivalent, are at the highest risk and require stringent LDL-C control.
For the full summary of the NCEP ATP III guideline for the management of hyperlipidemia, please visit
http://www.nhlbi.nih.gov/guidelines/cholesterol/atp3_rpt.htm.
The American Diabetes Association also encourages an aggressive treatment of diabetic dyslipidemia to
reduce the risk of cardiovascular disease (CVD). Statins should be the rst-line consideration for therapy.
A cholesterol absorption inhibitor or a resin, niacin, or fenobrate may be added if necessary to reach
the LDL-C goal or in the case of statin intolerance.
Selecting a Statin for Your Patient
4
There are diferent factors to consider when selecting the appropriate statin for your patient, including:
The extent of each statins ability to lower LDL-C levels and raise HDL-C levels (Table 1)
Drug interactions between statins and your patients concurrent drug therapy (Table 2). With the
exception of pravastatin, all other statins undergo microsomal metabolism by the cytochrome
P450 isoenzyme systems. About half of all medications currently available in clinical practice are
metabolized by CYP3A4.
4

Your patients prescription drug coverage. Some statins may be subject to prior authorizations
or step therapy edits.
Table 1. Relative Lipid-Lowering Efcacy of Statins Mean Changes from Baseline (%)
4
The results in the table are derived from various clinical trials. Therefore, any direct comparisons of
the lipid-lowering efects of each medication should take into account the diferences in trial design,
endpoints and patient demographics.
Drug Name and Dosage LDL-C HDL-C TG
Altoprev (lovastatin, extended-release)
20 mg QD -30 +12 -13
40 mg (QD or divided BID) -35 +13 -10
60 mg (QD or divided BID) -40 +12 -25
Crestor (rosuvastatin)
5 mg QD -28 to 45 +3 to 13 -21 to 35
10 mg QD -45 to 52 +8 to 14 -10 to 37
20 mg QD -31 to 55 +8 to 22 -23 to 37
40 mg QD -43 to 63 +10 to 17 -28 to 43
Lescol (uvastatin)
20 mg QPM -22 to 25 +2 to 6 -12 to 17
40 mg QPM -24 to 31 +4 to 8 -14 to 20
40 mg BID (80 mg) -34 to 36 +4 to 9 -18 to 23
Lescol XL (uvastatin, extended-release)
80 mg QPM -33 to 38 +7 to 11 -19 to 25
Lipitor (atorvastatin)
10 mg QD -27 to 39 +6 to 14 -17 to 41
20 mg QD -30 to 43 +9 to 11 -26 to 39
40 mg QD -50 +6 -29
80 mg QD -41 to 60 +5 to 7.5 -37 to 53
*Generic available
Drug Name and Dosage LDL-C HDL-C TG
Livalo (pitavastatin)
1 mg QD -32 +8 -15
2 mg QD -36 +7 -19
4 mg QD -43 +5 -18
Mevacor (lovastatin)*
10 mg QD -21 +5 -10
20 mg (QD or divided BID) -24 to 28 +6 to 8 -7 to 10
40 mg (QD or divided BID) -30 to 34 +2 to 9 -6 to 21
80 mg (QD or divided BID) - 40 to 42 +8 to 10 -19 to 27
Niaspan (niacin, extended release)
1000 mg QPM -5 +18 -21
1500 mg QPM -12 +20 -13
2000 mg QPM -14 +22 -28
Pravachol (pravastatin)*
10 mg QD -22 +7 -15
20 mg QD -26 to 32 +1 to 2 -10 to 11
40 mg QD -21 to 41 +5 to 14 -12 to 24
80 mg QD -37 +3 -19
Zocor (simvastatin)*
5 mg QD -26 +10 -12
10 mg QD -30 +12 -15
20 mg QD -38 +8 -19
40 mg QD -28 to 50 +7 to 13 -8 to 41
80 mg QD -36 to 51 +7 to 16 -24 to 38
*Generic available
Drug Name and Dosage LDL-C HDL-C TG
Combination Products
Advicor (niacin ER/lovastatin)
2000 mg/40 mg QHS
-47 (women)
-34 (men)
+ 33 (women)
+24 (men)
-48 (women)
-35 (men)
Caduet (amlodipine/atorvastatin)
2.5 mg/10 mg N/A N/A N/A
2.5 mg/20mg N/A N/A N/A
2.5 mg/40mg N/A N/A N/A
5 mg/10 mg -39 N/A N/A
5 mg/20mg -42 N/A N/A
5 mg/40mg -45 N/A N/A
5 mg/80mg -48 N/A N/A
10mg/10 mg -37 N/A N/A
10mg/20mg -39 N/A N/A
10mg/40mg -43 N/A N/A
10mg/80mg -49 N/A N/A
Simcor (niacin ER/simvastatin)
1000mg/20mg QPM -12 21 -27
2000mg/20mg QPM -14 29 -38
1000mg/40mg QPM -7 15 -23
2000mg/40mg QPM -5 24 -32
Vytorin (ezetimibe/simvastatin)
10 mg/10 mg QD -45 +8 -23
10 mg/20 mg QD -52 +10 -24
10 mg/40 mg QD -55 +6 -23
10 mg/80 mg QD -60 +6 -31
N/A = Not available *Generic available
Note: The information above is provided for your reference only. Not all products listed may be included
in the health plan's formulary. Please call your patient's health plan to inquire about the formulary status
of the desired statin medication or for more benet information.
Table 2. Myopathy and Rhabdomyolysis Drug-Drug Interactions
4,5
The risk of myopathy with statins is increased when used in combination with drugs listed in Table 2
below. These interactions range from moderate to severe in nature. Please refer to the package inserts
for the full range of drug interactions associated with each statin.
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a
Crestor dose should not exceed 5 mg/day
b
Crestor dose should not exceed 10 mg/day
c
Lovastatin dose should not exceed 40 mg/day
d
Lovastatin dose should not exceed 20 mg/day
e
Simvastatin dose should not exceed 10 mg/day
f
Use with simvastatin is contraindicated
g
Simvastatin dose should not exceed 20 mg/day
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Pitavastatin dose should not exceed 1 mg/day
i
Pitavastatin dose should not exceed 2 mg/day
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Niacin ( 1g/day) x x x x x
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Amlodipine x
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Verapamil x x x
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Grapefruit Juice
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a
Crestor dose should not exceed 5 mg/day
b
Crestor dose should not exceed 10 mg/day
c
Lovastatin dose should not exceed 40 mg/day
d
Lovastatin dose should not exceed 20 mg/day
e
Simvastatin dose should not exceed 10 mg/day
f
Use with simvastatin is contraindicated
g
Simvastatin dose should not exceed 20 mg/day
h
Pitavastatin dose should not exceed 1 mg/day
i
Pitavastatin dose should not exceed 2 mg/day
Some of the common adverse efects associated with statins include headache, constipation and
abdominal pain. Statins are contraindicated in patients with acute liver disease or unexplained persistent
elevations of serum transaminases. They are also contraindicated during pregnancy (Category X). All
statins have the potential to cause persistent elevations in serum transaminases. Liver function tests
should be performed prior to initiation of statin therapy, particularly in patients with a history of liver
disease, and when otherwise clinically indicated.
Summary of Recommendations
Proper disease management will help reduce the risk and burden of coronary heart disease and
maximize your patients overall well-being. Please consider a lipoprotein prole test or statin therapy
in your patient as clinically appropriate for the management of hyperlipidemia.
References:
1. Cholesterol Statistics. American Heart Association Web site. http://www.americanheart.org/presenter.jhtml?identifer=4506.
Accessed February 19, 2010.
2. Third report of the National Cholesterol Education Program (NCEP) expert panel on detection, evaluation, and treatment of high
blood cholesterol in adults (ATP III Final Report). National Heart, Lung, and Blood Institute, National Institutes of Health Web site.
http://www.nhlbi.nih.gov/guidelines/cholesterol/atp3_rpt.htm. Accessed November 29, 2010.
3. American Diabetes Association. Standards of medical care in diabetes 2010. Diabetes Care. 2010;33(suppl 1):S11-S61.
4. Micromedex Web site. http://www.thomsonhc.com/ Accessed November 29, 2010.
5. FDA News Release. FDA announces new safety recommendations for high-dose simvastatin. United States Food and Drug
Administration web site. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm258338.htm. Accessed June 8, 2011.
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