Safety Recommendations

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Summary of Statin Safety Recommendations

Class I
"1. To maximize the safety of statins, selection of the appropriate statin and dose in men and nonpregnant/nonnursing women should be based on patient characteristics, level of ASCVD* risk, and potential for adverse effects.
Moderate-intensity statin therapy should be used in individuals in whom high-intensity statin therapy would otherwise be recommended when characteristics predisposing them to statin-associated adverse effects are present. Characteristic predisposing individuals to statin adverse effects include, but are not limited to[1][2][3][4][5][6][7][8][9][10]:
  • Multiple or serious comorbidities, including impaired renal or hepatic function
  • History of previous statin intolerance or muscle disorders
  • Unexplained ALT elevations > 3 times ULN
  • Patient characteristics or concomitant use of drugs affecting statin metabolism
  • > 75 years of age

Additional characteristics that may modify the decision to use higher statin intensities may include, but are not limited to:

"2. Baseline measurement of hepatic transaminase levels (ALT) should be performed before initiating statin therapy.[1][7][8] (Level of Evidence: B)"
"3. Individuals receiving statin therapy should be evaluated for new-onset diabetes mellitus according to the current diabetes screening guidelines.[11] Those who develop diabetes mellitus during statin therapy should be encouraged to adhere to a heart healthy dietary pattern, engage in physical activity, achieve and maintain a healthy body weight, cease tobacco use, and continue statin therapy to reduce their risk of ASCVD events.[12](Level of Evidence: B)"
Class III
"1. CK should not be routinely measured in individuals receiving statin therapy.[13][4][5][6][9][10](Level of Evidence: A)"
"2. It may be harmful to initiate simvastatin at 80 mg daily or increase the dose of simvastatin to 80 mg daily.[14][9](Level of Evidence: A)"
Class IIa
"1. Baseline measurement of CK is reasonable for individuals believed to be at increased risk for adverse muscle events based on a personal or family history of statin intolerance or muscle disease, clinical presentation, or concomitant drug therapy that might increase the risk for myopathy. (Level of Evidence: C)"
"2. During statin therapy, it is reasonable to measure CK in individuals with muscle symptoms, including pain, tenderness, stiffness, cramping, weakness, or generalized fatigue.(Level of Evidence: C)"
"3. During statin therapy, it is reasonable to measure hepatic function if symptoms suggesting hepatotoxicity arise (e.g., unusual fatigue or weakness, loss of appetite, abdominal pain, dark-colored urine or yellowing of the skin or sclera).

(Level of Evidence: C)"

"4. For individuals taking any dose of statins, it is reasonable to use caution in individuals >75 years of age, as well as in individuals that are taking concomitant medications that alter drug metabolism, taking multiple drugs, or taking drugs for conditions that require complex medication regimens (e.g., those who have undergone solid organ transplantation or are receiving treatment for HIV). A review of the manufacturer’s prescribing information may be useful before initiating any cholesterol-lowering drug.(Level of Evidence: C)"
"5. It is reasonable to evaluate and treat muscle symptoms, including pain, tenderness, stiffness, cramping, weakness, or fatigue, in statin-treated patients according to the following management algorithm:
  • To avoid unnecessary discontinuation of statins, obtain a history of prior or current muscle symptoms to establish a baseline before initiating statin therapy.
  • If unexplained severe muscle symptoms or fatigue develop during statin therapy, promptly discontinue the statin and address the possibility of rhabdomyolysis by evaluating CK, creatinine, and a urinalysis for myoglobinuria.
  • If mild to moderate muscle symptoms develop during statin therapy:
    • Discontinue the statin until the symptoms can be evaluated.
    • Evaluate the patient for other conditions that might increase the risk for muscle symptoms (e.g., hypothyroidism, reduced renal or hepatic function, rheumatologic disorders such as polymyalgia rheumatica, steroid myopathy, vitamin D deficiency, or primary muscle diseases.)
    • If muscle symptoms resolve, and if no contraindication exists, give the patient the original or a lower dose of the same statin to establish a causal relationship between the muscle symptoms and statin therapy.
    • If a causal relationship exists, discontinue the original statin. Once muscle symptoms resolve, use a low dose of a different statin.
    • Once a low dose of a statin is tolerated, gradually increase the dose as tolerated.
    • If, after 2 months without statin treatment, muscle symptoms or elevated CK levels do not resolve completely, consider other causes of muscle symptoms listed above.
    • If persistent muscle symptoms are determined to arise from a condition unrelated to statin therapy, or if the predisposing condition has been treated, resume statin therapy at the original dose. (Level of Evidence: B)"
Class IIb
"1. Decreasing the statin dose may be considered when 2 consecutive values of LDL–C levels are <40 mg/dL.[13](Level of Evidence: C)"
"2. For individuals presenting with a confusional state or memory impairment while on statin therapy, it may be reasonable to evaluate the patient for nonstatin causes, such as exposure to other drugs, as well as for systemic and neuropsychiatric causes, in addition to the possibility of adverse effects associated with statin drug therapy.(Level of Evidence: C)"

Summary of Nonstatin Safety Recommendations

Safety of Niacin

Class I
"1. Baseline hepatic transaminases, fasting blood glucose or hemoglobin A1c, and uric acid should be obtained before initiating niacin, and again during up-titration to a maintenance dose and every 6 months thereafter.(Level of Evidence: B)[4]"
"2. In individuals with adverse effects from niacin, the potential for ASCVD benefits and the potential for adverse effects should be reconsidered before reinitiating niacin therapy.(Level of Evidence: B)"
Class III
"1. Niacin should not be used if:
  • Hepatic transaminase elevations are higher than 2 to 3 times ULN.[15]
  • Persistent severe cutaneous symptoms, persistent hyperglycemia, acute gout or unexplained abdominal pain or gastrointestinal symptoms occur.[15]
  • New-onset atrial fibrillation or weight loss occurs.[16](Level of Evidence: B)"
Class IIa
"1. To reduce the frequency and severity of adverse cutaneous symptoms, it is reasonable to:
  • Start niacin at a low dose and titrate to a higher dose over a period of weeks as tolerated.
  • Take niacin with food or premedicating with aspirin 325 mg 30 minutes before niacin dosing to alleviate flushing symptoms.
  • If an extended-release preparation is used, increase the dose of extended-release niacin from 500 mg to a maximum of 2,000 mg/day over 4 to 8 weeks, with the dose of extended-release niacin increasing not more than weekly.
  • If immediate-release niacin is chosen, start at a dose of 100 mg 3 times daily and up-titrate to 3 g/day, divided into 2 or 3 doses.(Level of Evidence: C)"
"2. It is reasonable to use BAS with caution if baseline triglyceride levels are 250 to 299 mg/dL, and evaluate a fasting lipid panel in 4 to 6 weeks after initiation. Discontinue the BAS if triglycerides exceed 400 mg/dL. (Level of Evidence: C)"

Safety of BAS

Class III
"1. BAS should not be used in individuals with baseline fasting triglyceride levels ≥300 mg/dL or type III hyperlipoproteinemia, because severe triglyceride elevations might occur. (A fasting lipid panel should be obtained before BAS is initiated, 3 months after initiation, and every 6 to 12 months thereafter.)[17](Level of Evidence: B)"
Class IIa
"1. It is reasonable to use BAS with caution if baseline triglyceride levels are 250 to 299 mg/dL, and evaluate a fasting lipid panel in 4 to 6 weeks after initiation. Discontinue the BAS if triglycerides exceed 400 mg/dL.(Level of Evidence: C)"

Safety of Cholesterol-Absorption Inhibitors

Class IIa
"1. It is reasonable to obtain baseline hepatic transaminases before initiating ezetimibe. When ezetimibe is coadministered with a statin, monitor transaminase levels as clinically indicated, and discontinue ezetimibe if persistent ALT elevations >3 times ULN occur.[18][19][20] (Level of Evidence: B)"

Safety of Fibrates

Class I
"1. Renal status should be evaluated before fenofibrate initiation, within 3 months after initiation, and every 6 months thereafter. Assess renal safety with both a serum creatinine level and an eGFR based on creatinine. (Level of Evidence: B)"
Class III
"1. Gemfibrozil should not be initiated in patients on statin therapy because of an increased risk for muscle symptoms and rhabdomyolysis.[1](Level of Evidence: B)"
"2.Fenofibrate should not be used if moderate or severe renal impairment, defined as eGFR <30 mL/min per 1.73 m2, is present.(Level of Evidence: B)"
"3.If eGFR is between 30 and 59 mL/min per 1.73 m2, the dose of fenofibrate should not exceed 54 mg/day.(Level of Evidence: B)"
"4.If, during follow-up, the eGFR decreases persistently to ≤30 mL/min per 1.73 m2, fenofibrate should be discontinued. (Level of Evidence: B)"
Class IIb
"1. Fenofibrate may be considered concomitantly with a low- or moderate-intensity statin only if the benefits from ASCVD risk reduction or triglyceride lowering when triglycerides are >500 mg/dL, are judged to outweigh the potential risk for adverse effects.(Level of Evidence: C)"

Safety of Omaga-3 Fatty Acids

Class IIa
"1. If EPA and/or DHA are used for the management of severe hypertriglyceridemia, defined as triglycerides ≥500 mg/dL, it is reasonable to evaluate the patient for gastrointestinal disturbances, skin changes, and bleeding. (Level of Evidence: B)"

"*Based on the presence of clinical ASCVD, diabetes mellitus, LDL–C >190 mg/dL, or level of estimated 10-year ASCVD risk.

†Individuals with elevated ALT levels (usually >1.5 or 2 times ULN) were excluded from RCT participation. Unexplained ALT >3 times ULN is a contraindication to statin therapy as listed in manufacturer’s prescribing information.

‡Statins use is associated with a very modest excess risk of new onset diabetes in RCTs and meta-analyses of RCTs (i.e., 0.1 excess case per 100 individuals treated 1 year with moderate-intensity statin therapy and 0.3 excess cases per 100 individuals treated for 1 year with high-intensity statin therapy. The increased risk of new onset diabetes appears to be confined to those with risk factors for diabetes. These individuals are also at higher risk of ASCVD due to these risk factors. Therefore, if a statin-treated individual develops diabetes as detected by current diabetes screening guidelines, they should be counseled to adhere to a heart healthy dietary pattern, engage in physical activity, achieve and maintain a healthy body weight, cease tobacco use, and continue statin therapy to reduce their risk of ASCVD events."

References

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