ANTIHYPERLIPIDEMIC DRUGS

HMG-CoA reductase inhibitors (statins)

HMG-CoA reductase is an enzyme that is a catalyst in the manufacture of cholesterol.
These drugs either inhibit manufacture of cholesterol or promote breakdown of cholesterol.
Statins are used for hyperlipidemia, primary/secondary prevention
coronary/cardiovascular events
Mild adverse effects; headache, dizziness, insomnia, memory/cognitive impairment,
flatulence, abdominal pain, cramping, N/C, hyperglycemia in NONDIABETIC patients.
Hepatotoxicity, myopathy
C/I in serious liver disorders or during pregnancy/lactation. May increase serum glucose
and HbA1c levels. Caution in pt w/history of alcoholism, nonalcohol related liver disease, acute
infection, hypotension, trauma, endocrine disorders, visual disturbances, myopathy
Rosuvastatin
Higher doses linked to risks for serious muscle toxicity
(myopathy/rhabomyolysis) in pt taking cyclosporine, Asian pt, pt w/severe renal
insufficiency. 5 mg dose is starting dose for pt who do not require aggressive cholesterol
reduction/pt w/predisposing factors of myopathy
Antacids at least 2 hours after giving this medication
Fluvastatin(Lescol)
If prescribed w/bile acid resin, statin given 2 hours before bile acid resin or at
least 4 hours after
Pravastatin(Pravachol)
If prescribed w/bile acid resin, statin given 2 hours before bile acid resin or at
least 4 hours after
Macrolides (erythromycin, clarithromycin), amiodarone, niacin, verapamil
Increase risk of severe myopathy when taken w/statins
Macrolides (erythromycin, clarithromycin), Niacin
Increased risk of rhabdomyolysis
Protease inhibitors elevate plasms levels of statin
Statins w/warfarin increase anticoagulant effect.
Statin drugs have additive effect when used w/bile acid resins; can also
treat hypercholesterolemia that does not respond to single drug regimen.
Always ask about use of herbal products, especially niacin/red yeast. St John’s
wort w/statins cause decrease of statin effectiveness
 Usually statins are taken in the evening/bedtime, avoid grapefruit,
pregnancy category X(do not take during pregnancy), contact HCP if muscle
pain, tenderness, weakness occur
Lovastatin(Altoprev)
No grapefruit, administer w/food at evening meal. Low fat/cholesterol diet,
Simvastatin(Zocor)
No grapefruit, PO preferably in evening
Best measurement for statin-caused liver compromise is fractioned(indirect) bilirubin
levels. If AST levels increase 3x normal, HCP may discontinue statins. Max effect of these
drugs usually evident w/in 4 weeks.
C/I in hepatitis or pregnant
Atorvastatin(Lipitor)
Adverse effects: headache, abdominal pain, rash, myalgia, rhabdomyolysis
Monitor for muscle pain, tenderness, weakness. Take medication at
same time each day, monitor liver function tests.

PCSK9 Inhibitors
PCSK9 is an enzyme that binds w/LDL and prevents it from being removed from the
blood
These inhibitors are monoclonal antibodies that block enzyme process and lower LDL
cholesterol
Alirocumab(Praluent)
Evolocumab(Repatha)
These drugs are given subcutaneously once/twice monthly but
expensive. Can have possible cognitive adverse reactions
New class LDL lowering drugs for pt w/genetic familial hyperlipidemia or if at very high-
risk cardiovascular disease.
Therapy for genetic familial hyperlipidemia begin w/diet mod and statin drugs.

Bile acid resins

Bile is secreted by liver and stored in gallbladder. Bile emulsifies fat/lipids as these
products pass through intestine
Constipation particularly associated w/bile acid resins, may interfere w/digestion of fats
and prevent absorption of fat-soluble vitamins (A,D,E,K) and folic acid; if used for long term
therapy, vitamins A/D may be given in water soluble form/parenterally
 Bile acid resins bind to bile acids to form insoluble substance that cannot be absorbed
by intestine; it is then excreted in feces. Increased loss bile acids=liver uses cholesterol to
manufacture more bile=decrease cholesterol levels
Bile acid resins are used to treat hyperlipidemia, gallstone dissolution in pt where
cholecystectomy is not recommended
Cholestyramine
For pruritus associated w/partial biliary obstruction
Take before meals, take other meds 1 hour before/4 hours after, increase fluid and fiber
intake, know signs/symptoms of bleeding
When taken w/anticoagulants, reduces effect of anticoagulants
When taken w/thyroid hormone, can cause hypothyroidism
Decrease absorption of numerous drugs, given alone or other drugs given 1
hour before or 4 hours after administration of bile acid resins. Restrict fat, cholesterol,
carbohydrates, alcohol
Drugs given w/bile acid resins that decrease level/absorption of drug given
NSAIDs, penicillin G, tetracycline, niacin, digitalis glycosides, furosemide and
thiazide diuretics, glipizide, hydrocortisone, methyldopa, propranolol
General adverse effects include constipation, aggravation of hemorrhoids, abdominal
cramping, flatulence, nausea, increased bleeding tendencies R/T vitamin K
malabsorption, vitamin A/D deficiencies. Pt taking these need to be especially alert for
bleeding tendencies.
Cholestyramine powder
Prescibed dose mixed in 2-6 oz water or noncarbonated beverage and shake
vigorously. Can also be mixed w. highly fluid soups/pulpy fruits(applesauce, crushed
pineapple) do not ingest in dry form. Other drugs 1 hour before or 4-6 hours after
cholestyramine.
Cholestyramine is available combine w artificial sweetener aspartame
for pt w/diabetes or those concerned w/weight gain
C/I in pt w/complete biliary obstruction. Used cautiously in pt w/diabetes, liver, peptic ulcer, or
kidney disease
Colestipol(Colestid)
For primary hypercholesterolemia, pruritis/diarrhea R/T excess bile acids
Interacts w/numerous medications. Teach pt to exercise and quit smoking
Notes:
Take before meals
Colestipol granules
 Dose must be mixed in liquids, soups, cereals, carbonated beverages, pulpy
fruits. Use ~90 mL liquid & slowly stir until ready to drink. Granules will not dissolve.
Drink entire glass, rinse glass w/small amount of water, drink again to ensure all
medication is taken
Colestipol tablets
Swallow whole at one time and w/full glass of fluid, sipping/holding fluid in
mouth can cause tooth discoloration/enamel decay. C/N, abdominal pain, distention
may occur/subside w/continued therapy. Notify HCP if effects become
bothersome/unusual bleeding or brusing occur

Fibric acid derivatives

Fenofibrate(TriCor, Triglide, Antara, Lopid)
Adjunctive treatment for reducing LDLs, total cholesterol, and triglycerides in pt
w/hyperlipidemia
Reduce VLDLs and stimulate catabolism of triglyceride rich lipoproteins,
resulting in decrease plasma triglycerides/cholesterol
Gemfibrozil(Lopid)
For pt w/very high serum triglyceride levels who are at risk for abdominal
pain/pancreatitis and do not respond to dietary mods.
May cause dizziness/blurred vision. Notify HCP if epigastric pain, N/V/D occur
Increases excretion of cholesterol in feces and reduces production of
triglycerides by liver, lowering serum lipid levels.
Caution w/hazardous tasks and gemfibrozil
Cyclosporine w/gemfibrozil may decrease effect cyclosporine
Sulfonylureas w/gemfibrozil may increase hypoglycemic effects
General adverse reactions for fibric acid derivatives include N/VD, GI upset, cholelithiasis,
cholecystitis
C/I in pt w/significant hepatic, renal dysfunction, primary biliary cirrhosis; these drugs may
increase already elevated cholesterol
Drugs that interact with fibric acid derivatives
Anticoagulant effect may be enhanced
HMG-CoA(statins) increase risk of rhabdomyolysis

Miscellaneous/Antihyperlipidemic
Niacin(Niaspan, Niacor)
 Lowers blood lipid levels, used as adjunct therapy for lowering very high serum
triglyceride levels in pt who are at risk for pancreatitis/response to dietary mod is
inadequate
C/I in pt w/active peptic ulcer, hepatic dysfunction, arterial bleeding; used
cautiously w/renal dysfunction, high alcohol consumption, unstable angina, gout
Pt may experience moderate to severe, generalized flushing of skin, warm
sensation, and severe itching/tingling. Tinnitus also may be a concern.
Notify HCP if skin reaction is severe/cause extreme discomfort. Aspirin
(325mg) about 30 minutes before may be administered to reduce adverse
reactions w/niacin
Ezetimibe(Zetia)
Inhibits absorption of cholesterol in small intestine, leading to decreased
cholesterol in liver, typically use in combo w/other antihyperlipidemic/lipid lowering
treatment
Take at least 2 hour before or 4 hours after bile acid sequestrant. Notify HCP if
unusual muscle pain, weakness/tenderness, severe diarrhea, respiratory infections
C/I in pregnant or lactating
General adverse reactions include N/V/D, abdominal pain, severe/generalized flushing of skin,
warm sensation, severe itching/tingling

Notes
Falls R/T dizziness associated w/fibrates and statins.
Statins have been associated w/skeletal muscle effects leading to rhabdomyolysis
Rhabdomyolysis is a rare condition in which muscle damages results in release of muscle
cells contents into bloodstream, can precipitate renal dysfunction or ARF.
Monitor for unexplained muscle pain, muscle tenderness, weakness, especially
if w/fever or malaise. More likely to be observed in Asian pt, initial low starting dose of
rosuvastatin is recommended