Cardiovascular System

Hyperlipidemia: Treatments

Anisha ValliLeave a comment
  • The goal of hyperlipidemia treatment is to prevent atherosclerosis and other cardiovascular diseases, and, in the case of hypertriglyceridemia, to prevent pancreatitis.
  • Prevention and treatment of hyperlipidemia comprises lifestyle modifications that promote cardiovascular health, including a low-fat diet, increased physical activity, weight loss, and avoidance of cigarette smoking.
  • When those measures are not enough, medications can be prescribed.

Anti-hyperlipidemia Drugs:

Statins

  • HMG-CoA reductase inhibitors; they upregulate hepatic LDL receptors, which lowers serum levels of LDL.
  • Statins can reduce LDL levels by 20-60%, and reduce triglyceride levels as well.
  • Adverse effects include myalgia and myositis; some statins are associated with increased risk of diabetes.
  • Statins are contraindicated in liver disease, and can interact with several drugs, including warfarin.
  • Statins are a mainstay treatment of hyperlipidemia and have been shown to reduce the risk of cardiovascular disease and reduce the progression and mortality from atherosclerotic cardiovascular disease (ASCVD).

Cholesterol absorption inhibitors

  • These drugs, which include ezetimibe, are the most commonly used non-statin drugs.
  • They block the intestinal absorption of cholesterol and upregulate hepatic LDL receptors.
  • Cholesterol absorption inhibitors reduce LDL and Apolipoprotein B; these drugs are often used in combination with statins to produce additional reductions in LDL.
  • They are generally well-tolerated, though diarrhea is common, and can be used when statins are contraindicated or in conjunction with statins.

PCSK9 inhibitors (proprotein convertease subtilsin-kexin type 9 inhibitors)

  • Block PCSK9 from binding with LDL receptors, which allows more LDL binding and, therefore, clearance.
  • These drugs reduce LDL levels 50-70%.
  • They are administered via injection, which can lead to inflammation at the injection site.
  • The need for self-injection and refrigeration can be prohibitive for some individuals.

Fibric acid derivatives

  • Also called fibrates.
  • Reduce synthesis of triglycerides and VLDL.
  • These drugs can reduce triglycerides by 20-35%, and can increase HDL levels by up to 20%.
    – Recall that HDL are the “good” lipoproteins with anti-atherogenic properties.
  • Common side effects include gastrointestinal upset and cholelithiasis (formation of gallstones); when taken in conjunction with statins, they may exacerbate myopathy.
  • Fibrates my increase serum creatinine levels, but this is not necessarily indicative of renal dysfunction.

Niacin

  • Nicotinic acid reduces hepatic synthesis of LDL and VLDL.
  • Can reduce LDL by 10-25%; triglycerides by 20-30%, and may increase HDL by 10-40%.
  • Side effects include flushing and abdominal issues; more rarely, patients experience hepatotoxicity or atrial fibrillation.
  • Increased uric acid levels may cause gout.

Bile acid sequestrants

  • Bind bile acids and prevent their reabsorption in the intestine; ultimately, this induces LDL receptor upregulation.
  • These drugs can reduce LDL by 15-25%.
  • Possible side effects include increased serum triglycerides, as well as constipation and bloating; they also impair intestinal absorption of other drugs, vitamins, and folic acid.
    – Unfortunately, gastrointestinal issues may reduce drug adherence.

ASCVD risk and the use of statins.

  • ASCVD is an umbrella term that includes:
    Coronary heart disease (for example, heart attack, coronary artery stenosis)
    Cerebrovascular disease (for example, transient ischemic attack, ischemic stroke)
    Peripheral artery disease
    Aortic atherosclerotic disease.
  • Factors that enhance a patient’s risk of ASCVD include a family history of ASCVD, metabolic and inflammatory disorders, preeclampsia, inclusion in certain populations, and, abnormal biomarkers.

Guidelines for Statin use

  • Indicate that primary prevention comprises heart-healthy lifestyles, though clinicians and their patients should be aware of and consider the patient’s risks of ASCVD.
  • ASCVD risk profiles guide the use of statins: http://tools.acc.org/ASCVD-Risk-Estimator-Plus/
  • Patients with ASCVD can be given high-intensity statins with the goal of a 50% or greater reduction in LDL.
    – If LDL remains elevated, non-statins, such as cholesterol absorption inhibitors, can be added.
  • Patients with hypercholesterolemia can also use high-intensity statins, with the additional of non-statins if LDL isn’t reduced by at least 50%.
  • Patients with diabetes and LDL levels greater than 70 mg/dL can prescribed moderate or high-intensity statins, depending on their ASCVD risk.
  • Patients with 10-year ASCVD risk scores between 7.5% and 19.9% are classified as “intermediate risk”; these patients can be prescribed moderate-intensity statins.
  • Be aware that other factors, including age, are also included in the guidelines.

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