Version May 2024
| Drug class | Dose range* | Administration | Major side effects and drug interaction potentials |
| Statins | |||
| Atorvastatin | 10 to 80 mg/day | Take any time | Muscle-related (eg, myalgia, myopathy, myositis, rhabdomyolysis); headache; gastrointestinal (eg, nausea, constipation, dyspepsia, diarrhea); sleep disturbance; elevations in hepatocellular enzymes and alkaline phosphatase. Statins are dependent on CYP metabolism and/or transmembrane transporters (eg, OATP, BCRP) for clearance, subjecting them to a significant number of clinically relevant drug interactions. Coadministration of drugs that alter CYP metabolism or drug transporters often requires dose limitations or avoidance. The patient's medication list should be analyzed using a drug interaction database (Lexicomp drug interactions) whenever therapy is adjusted. |
| Fluvastatin | IR: 20 to 80 mg/day | IR: Take in the evening Divide dose twice per day (morning and evening) if dose >40 mg/day | |
| XR: 80 mg/day | XR: Take any time | ||
| Lovastatin | IR: 20 to 80 mg/day | IR: Take once daily with evening meal | |
| XR: 20 to 60 mg/day | XR: Take in the evening | ||
| Pitavastatin | 1 to 4 mg/day | Take any time | |
| Pravastatin | 10 to 80 mg/day | Take in the evening¶ | |
| Rosuvastatin | 5 to 40 mg/day | Take any time | |
| Simvastatin | 10 to 40 mg/day | Take in the evening | |
| Cholesterol absorption inhibitor | |||
| Ezetimibe | 10 mg/day | Take any time | Generally well tolerated; low risk for potential drug interactions. Increased transaminases may be observed with concurrent statin use; however, coadministration is common. |
| PCSK9 inhibitors | |||
| Alirocumab | 75 to 150 mg every 2 weeks or 300 mg every 4 weeks | Administer by subcutaneous injection into thigh, abdomen, or upper arm | Injection site reactions. Low risk for potential drug interactions. |
| Evolocumab | 140 mg every 2 weeks or 420 mg every month Homozygous familial hypercholesterolemia: 420 mg every month to 420 mg every 2 weeks | ||
| Adenosine triphosphate citrate lyase inhibitor | |||
| Bempedoic acid | 180 mg daily | Take any time | Hyperuricemia, acute gouty arthritis; myalgia, muscle spasms, arthralgias; increased aspartate aminotransferase. Potential for significant drug interactions; dose limitations for some statins are recommended during concurrent use. The patient's medication list should be analyzed using a drug interaction database (Lexicomp drug interactions) whenever therapy is adjusted. |
| Fibric acid derivatives | |||
| Fenofibrate | Nanocrystal: 145 mg/day Micronized: 90 to 200 mg/day Nonmicronized: 120 to 160 mg/day Fenofibric acid: 105 to 135 mg/day | Multiple formulations exist with varying dosing and administration Some formulations must be administered with food | Increased serum transaminases, muscle-related (eg, myalgia, myositis, rhabdomyolysis), gastrointestinal (eg, dyspepsia, nausea, bloating, cramping). Potential for significant drug interactions; eg, increased risk of myopathy with statins, enhanced anticoagulant effect of warfarin. Gemfibrozil use with statins is not recommended. The patient's medication list should be analyzed using a drug interaction database (Lexicomp drug interactions) whenever therapy is adjusted. |
| Gemfibrozil | 600 mg twice per day | Take 30 minutes before meals | |
| Bezafibrate (not available in the United States) | Sustained release: 400 mg once daily | Take with or after meals | |
| Bile acid sequestrants | |||
| Cholestyramine | Powder: 4 to 24 g/day | Take within 30 minutes of a meal Administer granules or powder as prepared suspension Do not hold cholestyramine in mouth for prolonged periods (may cause tooth discoloration or enamel decay) Administer other oral medications ≥1 hour before or 4 to 6 hours after bile acid sequestrants | Nausea, bloating, cramping, and constipation; elevations in hepatic transaminases and alkaline phosphatase. Impaired absorption of fat soluble vitamins and coadministered medications. The patient's medication list should be analyzed using a drug interaction database (Lexicomp drug interactions) whenever therapy is adjusted. |
| Colestipol | Granules: 5 to 30 g/day Tablet: 2 to 16 g/day | ||
| Colesevelam | Granules or tablet: 3.75 g/day | ||
| Nicotinic acid (niacin) | IR: 250 mg to 6 g/day | Take with meals | Not recommended for use in most patients due to poor tolerability and lack of efficacy for clinical endpoints. Prostaglandin-mediated cutaneous flushing, headache, warm sensation, and pruritus; hyperpigmentation (particularly in intertriginous regions), acanthosis nigricans, and dry skin; nausea, vomiting, diarrhea; myositis; hyperglycemia, hyperuricemia; hypotension; increased risk of infection. Low risk for potential drug interactions. |
| XR (Niaspan): 0.5 to 2 g/day | Take at bedtime after a low-fat snack or evening meal | ||
IR: immediate release; XR: extended release; PCSK9 inhibitors: proprotein convertase subtilisin kexin type 9 inhibitors; LDL-C: low density lipoprotein cholesterol.
* Dose ranges provided are total daily doses for oral administration (except PCSK9 inhibitors) in adult patients with normal organ function. Statin dose ranges include low-, moderate-, and/or high-intensity LDL-C-lowering therapy, depending on specific statin. For indications and doses, refer to the relevant clinical topic reviews and Lexicomp drug information monographs included within UpToDate.
¶ Per United States labeling, may be taken any time of day; however, UpToDate contributors prefer evening administration due to pravastatin's short half-life.آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟
