Pharmacology Exam 2

Atorvastatin

High-intensity statin (can lower by >50%)

Lowers LDL

Rosuvastatin

High-intensity statin

lowers LDL

Simvastatin

moderate-intensity statin

lowers LDL

Pravastatin

moderate-intensity statin

lowers LDL

Statins mechanism

Inhibits HMG-CoA reductase, decreases cholesterol synthesis and causes increased LDL-R and more LDL clearance from blood (small improvement in HDL and TG)

pleiotropic effects: decreased inflammation, plaque stabilization

Statin adverse effects

elevates liver enzymes

increase T2D incidence

Pregnancy category X

myopathy

*rhabdomyolysis- rare, breakdown of muscle causing kidney failure or death

alirocumab

PCSK9 inhibitor

monoclonal antibodies that bind PCSK9 and prevent degradation. causes LDL clearance from blood

usually used in conjunction with statins

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evolocumab

PCSK9 inhibitor

monoclonal antibodies that bind PCSK9 and prevent degradation. causes LDL clearance from blood

usually used in conjunction with statins

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ezetimibe

lowers LDL by blocking an intestinal cholesterol transporter

reduces absorption of dietary and biliary cholesterol

bempedoic acid

Inhibits ATP citrate lyase, lowers acetyl co-a (cholesterol precursor) in liver cells.

decreases cholesterol synthesis, increased LDL receptor expression, increased LDL clearance.

usually used in addition to statins or for those who cannot tolerate statins.

Fenofibrate

fibric acid derivative

PPAR-alpha activation causes decreased VLDL production, increased HDL.

used for hypertriglyceridemia

omega-3-acid ethyl esters

mix of EPA and DHA, uncertain mechanism but significantly lowers triglycerides, anti-inflammatory.

icosapent ethyl

purified EPA, significantly lowers triglycerides, anti-inflammatory