Summary of the Major Approved Drugs Used for the Treatment of Dyslipidemia
| Drug | Major Indications | Starting Dose | Maximal Dose | Mechanism | Common Side Effects |
|---|---|---|---|---|---|
| HMG-CoA reductase inhibitors (statins) | Elevated LDL-C; increased CV risk | ↓Cholesterol synthesis, ↑Hepatic LDL receptors, ↓VLDL production | Myalgias, arthralgias, elevated transaminases, dyspepsia | ||
| Lovastatin | 20-40 mg daily | 80 mg daily | |||
| Pravastatin | 40-80 mg daily | 80 mg daily | |||
| Simvastatin | 20-40 mg daily | 80 mg daily | |||
| Fluvastatin | 20-40 mg daily | 80 mg daily | |||
| Atorvastatin | 20-40 mg daily | 80 mg daily | |||
Pitavastatin | 5-20 mg daily 1-2 mg daily | 40 mg daily 4 mg daily | |||
| Cholesterol absorption inhibitor | Elevated LDL-C | ↓Cholesterol absorption, ↑ LDL receptors | Elevated transaminases | ||
| Ezetimibe | 10 mg daily | 10 mg daily | |||
| Bile acid sequestrants | Elevated LDL-C | ↑Bile acid excretion and ↑ LDL receptors | Bloating, constipation, elevated triglycerides | ||
| Cholestyramine | 4 g daily | 32 g daily | |||
5 g daily 3750 mg daily | 40 g daily 4375 mg daily | ||||
MTP inhibitor Lomitapide | HoFH |
5 mg daily |
60 mg daily | ↓VLDL production | Nausea, diarrhea, increased hepatic fat |
apoB inhibitor Mipomersen | HoFH |
200 mg SC weekly |
200 mg SC weekly | ↓VLDL production | Injection site reactions, flu-like symptoms, increased hepatic fat |
Immediate-release Sustained-release Extended-release | Elevated LDL-C, elevated TG |
100 mg tid 250 mg bid 500 mg qhs |
1 g tid 1.5 g bid 2 g qhs | ↓VLDL production | Cutaneous flushing, GI upset, elevated glucose, uric acid, and elevated liver function tests |
Fibric acid derivatives | Elevated TG |
600 mg bid 145 mg qd |
600 mg bid 145 mg qd | ↑LPL, ↓ VLDL synthesis | Dyspepsia, myalgia, gallstones, elevated transaminases |
Omega-3 fatty acids Omega-3 acid ethyl esters | Elevated TG | 4 g daily | 4 g daily | ↑TG catabolism | Dyspepsia, fishy odor to breath |
| Icosapent ethyl | 4 g daily | 4 g daily |
Abbreviations: CV, cardiovascular; HDL-C, high-density lipoprotein cholesterol; HoFH, homozygous familial hypercholesterolemia; LDL-C, LDL-cholesterol; LPL, lipoprotein lipase; MTP, microsomal triglyceride transfer protein; TG, triglyceride; VLDL, very-low-density lipoprotein.