Lipid-Lowering Drugs

Type

Mechanism of Action

Indications

Some Potential Side Effects

Adenosine triphosphate citrate lyase inhibitor

Lowers LDL cholesterol

High LDL cholesterol in people with atherosclerotic cardiovascular disease or familial hypercholesterolemia in people with at least 1 abnormal gene (heterozygous)

Cold or flu-like illness

Gout flare

Pain in back, arms, or legs

Stomach pain

Angiopoietin-like protein 3 inhibitor

Lowers triglycerides, LDL and HDL cholesterol

Familial hypercholesteremia in people who have 2 abnormal genes (are homozygous)

Decreased energy

Dizziness

Influenza-like illness

Nasopharyngitis

Nausea

Pain in legs or arms

Bile acid binder

Bind bile acids in the intestine, causing the acids to be excreted rather than used to make bile and causing the liver to remove more LDL cholesterol from the bloodstream to make bile

High LDL cholesterol

Abdominal pain

Binding of some other drugs (reducing their effectiveness)

Bloating

Constipation

Nausea

Increase in triglyceride level (especially in people with high triglyceride levels)

Cholesterol absorption inhibitor

Decreases cholesterol absorption in the small intestine

High LDL cholesterol

Few serious side effects

Face and lip swelling (very rare)

Loose stools

Muscle aches (very rare)

Fibric acid derivatives

Bezafibrate*

Ciprofibrate*

Increase the breakdown of lipids and speed the removal of VLDL from the bloodstream

May decrease VLDL production by the liver

High triglycerides

Dysbetalipoproteinemia

Possibly high VLDL cholesterol

Abdominal pain

Bloating

Diarrhea

Gallstones

High liver enzyme levels

Muscle aches due to inflammation (myositis)

Nausea

Rash

Microsomal triglyceride transfer protein inhibitor

Inhibits triglyceride secretion

Familial hypercholesteremia in people who have 2 abnormal genes (are homozygous)

Diarrhea

Liver damage

Niacin

Slows removal of HDL

Lowers triglyceride levels

At high doses, decreases production rate of VLDL, which is used to synthesize LDL

High triglycerides

High LDL and VLDL cholesterol

Dysbetalipoproteinemia

Digestive upset

Flushing

Gout

High blood sugar level (hyperglycemia)

High liver enzyme levels

Itching

Ulcers

Omega-3 fatty acids

Omega-3 fatty acids

Lower levels of triglycerides

May decrease production of VLDL

High triglycerides

Belching

Diarrhea

PCSK9 inhibitors

Lowers level of LDL

Familial hypercholesterolemia and for other people at high risk of coronary artery disease

Flu-like symptoms

Rarely, high liver enzyme levels

Skin reactions at injection sites

Lowers level of LDL

Familial hypercholesterolemia and for other people at high risk of coronary artery disease

Flu-like symptoms

Hives

Skin reactions at injection sites

SiRNA targeting PCSK9

Lowers level of LDL

Familial hypercholesterolemia and for other people at high risk of coronary artery disease

Skin reactions at injection sites

Joint pain or stiffness

Statins (HMG-CoA reductase inhibitors)

Block the synthesis of cholesterol, increasing the removal of LDL from the bloodstream

High LDL cholesterol, triglycerides, or both

Bloating

Constipation (mild)

Fatigue

Headache

Loose stools

Rarely, high liver enzyme levels

Rarely, muscle aches due to inflammation (myositis) or degeneration (rhabdomyolysis)

HDL = high density lipoprotein; HMG-CoA = 3-hydroxy-3-methylglutaryl coenzyme A; LDL = low density lipoprotein; PCSK9 = proprotein convertase subtilisin/kexin type 9; SiRNA = small interfering ribonucleic acid; VLDL = very low density lipoprotein.

* Not available in the United States.