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 and myopathy ↑transaminases, ↑diabetes risk | ||
| 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 | |||
5-20 mg daily | 40 mg daily | ||||
1-2 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 | 40 g daily | ||||
3750 mg daily | 4375 mg daily | ||||
PCSK9 inhibitors | Elevated LDL-C | ↓PCSK9 activity, | Injection site reactions | ||
| 140 mg SQ q 2 weeks | 420 mg SQ q 1 month (hoFH) | ↑LDL receptors | ||
75 mg SQ q 2 weeks | 150 mg SQ q 2 weeks | ||||
MTP inhibitor | HoFH | 5 mg daily | 60 mg daily | ↓VLDL production | Nausea, diarrhea, increased hepatic fat |
ApoB inhibitor | HoFH | 200 mg SC weekly | 200 mg SC weekly | ↓VLDL production | Injection site reactions, flu-like symptoms, increased hepatic fat |
Fibric acid derivatives | Elevated TG | ↑LPL, ↓ VLDL synthesis | Dyspepsia, myalgia, gallstones, elevated transaminases | ||
600 mg bid | 600 mg bid | ||||
145 mg qd | 145 mg qd | ||||
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: GI, gastrointestinal; HDL-C, high-density lipoprotein cholesterol; HoFH, homozygous familial hypercholesterolemia; LDL, low-density lipoprotein; LDL-C, LDL-cholesterol; LPL, lipoprotein lipase; TG, triglyceride; VLDL, very-low-density lipoprotein.