Statins Indication & Mechanism SE’s/AE’s Drug (Brand) High Med.
Low Interactions Notes
Intensity Intensity Intensity 3A4 2C9 PGP P1B1 P1B3
Indicated for reduction of Myalgias: caused by Ca2+ Atorvastatin 40-80 10-20 - X - X X - First consideration:
elevated LDL cholesterol. sparks, leading to muscle cell (Lipitor) High Intensity: Expected >50%
apoptosis. Research Rosuvastatin 20-40 5-10 - - X - X X reduction in LDL
Inhibition of HMG CoA- indicates exercise can reduce (Crestor) Med Intensity: Expected 30-
reductase. statin associated myalgias. Simvastatin - 20-40 10 X - X X - 50% reduction in LDL
LDL receptor activation to New onset diabetes: (Zocor) Low Intensity: Expected <30%
increase hepatic molecular level changes to Lovastatin - - 20 X - X - - reduction in LDL.
cholesterol uptake. pancreatic beta cells, muscle (Mevacor) Secondary: Interactions,
cells, and adipose cells Pravastatin - 40-80 10-20 - - - X X coverage/cost
reduces insulin secretion and (Pravachol) Most statins are dosed once
sensitivity, respectively. Pitavastatin - 2-4 - - * - X X daily, but new research
Teratogenic (Livalo) introduces the possibility of
Cognitive dysfunction intermittent dosing.
Non-Statins Indication & Mechanism SE’s/AE’s Drug (Brand) Efficacy Interactions Notes
Cholesterol Sterol transporter Flatulence, bloating Ezetimibe 10mg QD May increase concentration of Per the IMPROVE-IT trial,
Uptake inhibitor, reduces Avoid in hepatic impairment (Zetia) Mild to moderate reduction in OATP1B1 and OAT P1B3 ezetimibe has CV event
Inhibitors cholesterol intake. May contribute or cholesterol. Varies depending substrates. Reduced absorption benefit to high risk groups
exacerbate statin-induced on diet. when taken in within 2h of BAS only in combination with
myalgias statin.
Per the EWTOPIA 75 trial,
patients over age 75 received
significant benefit from
addition of ezetimibe to
regimen (caution: open-label
trial).
Bile Acid Indicated for lowering Acidosis Cholestyramine 7%, 28% (4g, 28g respectively) Bile acid sequestrants reduce Some formulations are
Sequestrant LDL-C Bleeding d/t (Prevalight) [Powder dissolved in drink] absorption of many oral drugs reconstituted into liquid from
s hypoprothrombinemia (vit K Colestipol 12%, 24% (4g, 16g) (including ezetimibe). powder. Taken one or
Bile acids are made from deficiency) (Colestid) [Large tablet] Caution when used with blood multiple times daily.
cholesterol. Loss of bile Constipation Colesevelam 15%, 18% (3.8g, 4.3g) thinners, esp. warfarin
acids d/t sequestrants Hypothyroidism (in theory) (Welchol) [Powder packet, tablet] Also used for IBS-D;
increases conversion of cholestatic pruritis;
LDL to bile acid
PPAR-α RA Indicated for lowering Hepatotoxicity (Monitor LFT) Gemfibrozil Indicated for most severe Strong CYP2C8 inhibitor TG reduction not necessarily
total triglycerides; little to Myopathy (Lopid) hypertriglyceridemia Some OATP1B1/B3 inhibition indicated with better
no LDL lowering Cholelithiasis Fenofibrate Weak CYP2C9 inhibitor outcomes
(Triglide May increase hypoglycemic
events w/ SU’s
Niacin Decreases VLDL and LDL; Hepatotoxic Niacin Primarily increases HDL. Increased SAM’s No longer recommended
increases HDL (most Hyperuricemia (avoid in (Niaspan) Modest LDL lowering effect. Reduced absorption w/ BAS except in patients with
effective) those with gout) TG>500 or special situations
Can reduce TG’s where patients are unable to
Reduced glucose tolerate preferred agents
sensitivity/tolerance
Ω-3-Acid Decreases TG synthesis Fishy taste / burps Icosapent Ethyl While Vascepa claims to not Aspirin and other blood thinners Generic and OTC formulations
Ethyl Esters Increased bleed risk (Vascepa) [EPA raise LDL, other drugs in this may be considered, but
Possible contribution to only] category may increase LDL and content of EPA+DHA needs to
atrial fibrillation Fish oil total cholesterol. This is most be specified
Ω-3-Acid Ethyl significant with Lovaza, which Inexpensive
Esters has the highest TG reduction in **Caution in patients with fish
(Lovaza) class but also the highest LDL allergy**
increase in class.
PCSK9i Indicated for lowering Very LDL low LDL Evolucumab 40%+ reduction in LDL. May increase SAM’s Costly
LDL-C Muscle pain (Repatha) No specific interactions listed per Needs to be injected
(hypercholesterolemia, Injection-site reactions Alirocumab lexicomp Twice or once monthly
familial and statin- (Praluent)
unresponsive) Inclisiran
(Praluent)
Antibody which targets
LDL-receptor degrading
protein
Bempedoic Indicated for lowering Hyperuricemia Bempedoic Mild to moderate reduction in Increases blood statin Available alone or in
Acid LDL-C, especially for Anemia Acid LDL (similar to ezetimibe) concentration (esp. simvastatin, combination with ezetimibe.
those with inadequate Limb pain (Nexletol) pravastatin) Approved in 2020 as a first-in-
response to statin class therapy by FDA, but yet
therapy. to be included on guidelines
due to its novelty.
Adenosine triphosphate-
citrate lyase blocker
(upstream of HMGCoA)
Determining appropriate antihyperlipidemic therapy:
- ASCVD Risk
- Age
- Comorbidity (specifically diabetes for statins)
- Primary vs secondary heart attack prevention
- LDL level and goal
- TG level
For almost all patients, statins will be the first line agent. They are effective, relatively safe, and inexpensive. Counseling will focus on understanding signs of myalgias (intense muscle pains, intense
urine discoloration; labs include creatinine kinase levels)
HDL below 40 mg/dL considered a negative risk factor for heart disease. HDL>60 desired.
LDL goal <70
Red Yeast rice is an unregulated supplement containing a compound related to lovastatin. Patients taking red yeast rice are consuming an unknown amount of active compound and should ideally
us a statin medication instead. Using cholesterol lowering medications with red yeast rice may increase likelihood of SAM’s.
TG’s usually not as high a concern as LDL. TG>500 require pharmacologic therapy.
