Lipid-Lowering Medications

atorvastatin

Lipitor

colesevelam

Welchol

ezetimibe

Zetia

fenofibrate

Antara, Fenoglide, Lipofen, Lofibra, Tricor, Trilipix

gemfibrozil

Lopid

lovastatin

Altoprev, Mevacor

niacin

Niaspan, Slo-Niacin

omega-3-ethyl esters

Lovaza, Vascepa

pravastatin

Pravachol

rosuvastatin

Crestor

simvastatin

Zocor

HMG-CoA reductase inhibitor (statins) indications

1. hyperlipidemia (excess fats/lipid in blood)

2. primary/secondary prevention of atherosclerotic cardiovascular disease

3. familial hypercholesterolemia (high LDL)

HMG-CoA (statins) mechanism of action

_____ reductase inhibitors completely inhibit conversion of ______ to mevalonate (this is an early rate-limiting step in cholesterol synthesis)

• results in increased LDL receptors, which bind and remove circulating LDL cholesterol

HMG-CoA (statins) major contraindications

• breastfeeding

• active liver disease

HMG-CoA (statins) black box warnings

none

HMG-CoA (statins) ADRs (common)

• myopathy (muscle weakness/stiffness)

• diarrhea

HMG-CoA (statins) ADRs (rare but serious)

• rhabdomyolysis (breakdown of muscles)

• hepatotoxicity (liver toxicity)

HMG-CoA (statins) key counseling points

• this drug will lower your bad cholesterol (LDL, TG) and raise good cholesterol (HDL)

• contact your doctor if you develop muscle pain

cholesterol absorption inhibitor (ezetimibe/Zetia) indications

1. hyperlipidemia (excess fats/lipids in blood)

2. familial hypercholesterolemia (high LDL)

cholesterol absorption inhibitor (ezetimibe/Zetia) mechanism of action

inhibits absorption of cholesterol at the brush border of small intestine

cholesterol absorption inhibitor (ezetimibe/Zetia) major contraindications

• gallbladder disease

  • severe hepatic dysfunction

cholesterol absorption inhibitor (ezetimibe/Zetia) black box warnings

none

cholesterol absorption inhibitor (ezetimibe/Zetia) ADRs (common)

none

cholesterol absorption inhibitor (ezetimibe/Zetia) ADRs (rare but serious)

• rhabdomyolysis (breakdown of muscles)

• hepatotoxicity (liver toxicity)

cholesterol absorption inhibitor (ezetimibe/Zetia) key counseling points

• this drug will lower your bad cholesterol (LDL, TG) and raise good cholesterol (HDL)

• contact your doctor if you develop muscle pain

bile acid sequestrant (colesevelam/Welchol) indications

1. hyperlipidemia (excess fats/lipid in blood)

bile acid sequestrant (colesevelam/Welchol) mechanism of action

this drug binds with bile acids in the intestine, forming an insoluble complex that is excreted in feces

bile acid sequestrant (colesevelam/Welchol) major contraindications

• history of bowel obstruction

• high triglycerides (>500 mg/dL)

• hypertriglyceridemia-induced pancreatitis

bile acid sequestrant (colesevelam/Welchol) black box warnings

none

bile acid sequestrant (colesevelam/Welchol) ADRs (common)

• constipation

bile acid sequestrant (colesevelam/Welchol) ADRs (rare but serious)

• pancreatitis

• bowel obstruction

bile acid sequestrant (colesevelam/Welchol) key counseling points

• this medication is used to lower cholesterol levels

• take w/ food

• take w/ liquid

  • packet/granules: mix w/ 120 to 240 mL of water, stir, and drink

  • tablets: swallow w/ liquid

fibric acids

fenofibrate (Antara, Fenoglide)

gemfibrozil (Lopid)

fibric acids indications

1. hyperlipidemia (excess fats/lipids in blood)

2. hypertriglyceridemia (high triglycerides in blood)

fibric acids mechanism of action

the derivatives of this drug activate peroxisome proliferator-activated receptor α (PPARα), which activates lipoprotein lipase / eliminates triglycerides from plasma

fibric acids major contraindications

gallbladder disease

fibric acids black box warnings

none

fibric acids ADRs (common)

increased transaminases (distressed liver)

fibric acids ADRs (rare but serious)

• rhabdomyolysis (breakdown of muscles, especially when combined with a statin)

• hepatotoxicity (liver toxicity)

fibric acids key counseling points

• this is used to lower bad cholesterol (LDL, TG) and raise good cholesterol (HDL)

• this medication comes in many formulations, some require administration with food (fenofibrate/Fenoglide, Antara)

• contact your doctor if you develop muscle pain

antilipemic (niacin/Niaspan) indications

1. hyperlipidemia (excess fats/lipid in blood)

antilipemic (niacin/Niaspan) mechanism of action

not well-defined

May involve partial inhibition of release of free fatty acids from adipose tissue

antilipemic (niacin/Niaspan) major contraindications

• severe hepatic dysfunction

• peptic ulcer disease

antilipemic (niacin/Niaspan) black box warnings

none

antilipemic (niacin/Niaspan) ADRs (common)

• flushing (must slowly titrate up to target dose)

  • avoiding alcohol and spicy foods may help

  • taking aspirin 30 minutes before may help

• headache

antilipemic (niacin/Niaspan) ADRs (rare but serious)

• rhabdomyolysis (breakdown of muscles)

• hepatotoxicity (liver toxicity)

antilipemic (niacin/Niaspan) key counseling points

• this medication is used to lower cholesterol levels

• you will start at a low dose and slowly increase over time to decrease side effects

• to decrease flushing, avoid alcohol and spicy food while on this medication

omega-3-ethyl-esters (Lovaza/Vascepa) indications

1. hyperlipidemia (excess fats/lipids in blood)

2. hypertriglyceridemia (high triglycerides in blood)

omega-3-ethyl-esters (Lovaza/Vascepa) mechanism of action

reduction in hepatic production of triglyceride-rich very low-density lipoproteins

omega-3-ethyl-esters (Lovaza/Vascepa) major contraindications

hypersensitivity to drug, fish, or shellfish

omega-3-ethyl-esters (Lovaza/Vascepa) black box warnings

none

omega-3-ethyl-esters (Lovaza/Vascepa) ADRs (common)

• diarrhea

• “fishy” breath, burping, change in taste

omega-3-ethyl-esters (Lovaza/Vascepa) ADRs (rare but serious)

elevated LFTs (stressed liver cells)

omega-3-ethyl-esters (Lovaza/Vascepa) key counseling points

• this is used to lower bad cholesterol (LDL, TG)

• take w/ food