7.9 Antilipemic Medications V2

Andrea Sullivan Degenhardt

7.9 Antilipemic Medications V2

Pharmacological treatment for managing dyslipidemia for the prevention of cardiovascular disease begins with screening individuals that includes age, health issues, family history, lifestyle factors, and lab work (Canadian Cardiovascular Society, 2021). Review unit 7.2 Conditions and Disorders related to Perfusion, Dyslipidemia.

Antilipemic agents are used to treat hyperlipidemia and dyslipidemia that may lead to additional health problems such as stroke, myocardial infarction, angina, and heart failure. The risk of atherosclerosis and coronary artery disease is directly related to increased levels of low-density lipoproteins (LDLs). If LDL levels decrease, this can slow the progression of atherosclerosis.

If after lifestyle changes are not successful at improving cholesterol levels, anti-lipemic meds are initiated. This therapy is long term and should be used in adjunct with a healthy diet and exercise regime. Some of the meds are used primarily to lower low-density lipoproteins (LDLs), some for lowering triglycerides, and others can help raise high density lipoproteins (HDLs).

Statins are often the first medication to be started and depending on the response, other cholesterol lowering meds will be added.

Treatment Guidelines

Cholesterol screening done every 5 years for adults 40-75 years of age (earlier if risk factors for CAD). Labs include total cholesterol, LDL, HDL, triglycerides (TG).
Identity high risk factors, including lifestyle and health issues (diabetes, family history of CAD).

Non- pharmacological interventions: diet, exercise, weight control, smoking cessation

LDL not lowered with diet, exercise, lifestyle changes → drug therapy is initiated along with ongoing lifestyle modifications

Drug Therapy: HMB-CoA reductase inhibitors “statins” →reduce LDLs
If ineffective, and depending on ongoing blood work, add on:

Bile-acid sequestrants – cholestyramine, colestipol and colesevelam (reduce LDLs)

Cholesterol absorption inhibitors – Ezetimibe (reduce LDLs)

Along with the above, may add on drugs to raise HDL. Ie. Fibrates (lower TG, increase HDL)

To learn more about these interventions go to the 2021 Canadian Cardiac Society Dyslipidemia Guidelines and Resources, go to the following link: https://ccs.ca/guideline/2021-lipids/

In this unit, we will cover the following classes of meds:

HMG-CoA Reductase Inhibitors (statins),
Bile Acid Sequestrants,
Fibrates,
Niacin,
Cholesterol Absorption Inhibitors.

HMG-CoA Reductase Inhibitors (statins)

HMG-CoA reductase inhibitors, more commonly known as statins, are the first line treatment to manage dyslipidemias and prevent cardiovascular disease. There are a number of meds in this class, including atorvastatin, lovastatin and simvastatin, that all differ in potency, metabolism and potential for side effects. For example, atorvastatin is more potent with higher ability to lower LDLs, whereas rosuvastatin is more hydrophilic with fewer muscle related side effects. Based on the client profile including age, risk factors and lab values, the prescriber will determine the most appropriate statin. Statins need to be used along with dietary and lifestyle modifications.

Atorvastatin will be our prototype medication.

Mechanism of Action

Atorvastatin inhibits HMG-CoA reductase and cholesterol synthesis, which reduces LDL (low density lipoprotein).Statins decrease cholesterol production in the liver by preventing HMG-CoA conversion to mevalonate. HMG-CoA is a rate limiting enzyme in cholesterol synthesis. When this enzyme is reduced, cholesterol production is decreased, resulting in hepatocytes making more HMG-CoA reductase (restoring cholesterol synthesis) and increasing the number of LDL receptors in the liver. With more LDL receptors, the liver can remove more LDLs from the blood (McIver & Siddique, 2025).

Along with lowering LDL levels, statins also decrease the production of very low density lipoproteins (VLDLs), resulting in lower VLDL levels and triglyceride levels. Statins also increase HDLs levels (Rosenjack Burchum & Rosenthal, 2019).

7.9a Mechanism of action of the different anti-lipemic medications (Sheila Odubote/TRU Open Press) CC BY-NC-SA

Indications for Use

This medication is used for hyperlipidemia and the prevention of cardiovascular disease. It primarily lowers LDLs, but also has an effect on lowering triglycerides and increasing HDLs. Statins decrease the risk of CV disease, such as myocardial infarction, stroke, revascularization procedures, and angina. It is also prescribed for type 2 diabetics who have multiple risk factors to lower their CV risk (McIver & Siddique, 2025). Other effects include anti-inflammatory, anti-oxidant (helps protect cells from damage) and anti-proliferative (inhibits growth and division of cells) effects. They also have anti-inflammatory effects and improve endothelial dysfunction and vascular remodelling, helping to stabilize atherosclerotic plaques and reducing thrombosis. The extent of these other actions in improving CV health is less clear, and statins continue to be used for mostly for the reduction of lipid levels (Feingold, 2024).

Pharmacokinetics
Statins are rapidly absorbed after administration, with peak effect in 1-2 hours. It has extensive first pass effect. It is metabolized in the liver via CYP3A4 and CYP3A5. It is excreted in the bile.

Nursing Considerations

Administration: oral. Take at same time each day, with or without food.

For most statins, it is advised to take statins at bedtime as endogenous cholesterol synthesis occurs during fasting at night.

Atorvastatin has a long half life, so taking the med at any time of the day is acceptable, but need to be consistent with taking it at the same time.

Labs: liver enzymes (AST/AST), creatine kinase (CK), lipid profile. Labs are drawn before therapy, 6 months after initiation and then every 5-12 months. Blood glucose levels drawn prior to therapy and regularly, depending on risk for diabetes.

Renal function: Renal function is not a concern with atorvastatin. Other statins would require a dose reduction if severe renal impairment, such as lovastatin or simvastatin.

Do not use with clients who have hepatic disease.

Pregnancy: contraindicated with clients who are pregnant or breastfeeding. If planning on becoming pregnant, stop statins three months prior to becoming pregnant.

Pediatrics: Do not give to clients under 10 years of age.

Use caution with older adult due to increased risk for myopathy.

Drug Interactions:

Depending on the statin, drug interactions can be a concern due to effects with CYP3A4 metabolism. There are many meds that can interact with statins. If the client is on many other meds, atorvastatin may not be ideal as drugs that inhibit CYP3A4 will increase atorvastatin levels. In this case, other statins would be prescribed such as rosuvastatin. Drug interactions can occur with certain antibiotics, antifungals, calcium channel blockers, leading to higher statin levels and more risk for adverse effects.

Avoid grapefruit juice as it deactivates CYP3A4, leading to risk of serious adverse effects such as myopathies and elevated blood sugar levels.

Adverse/Side Effects

Generally well-tolerated with side effects uncommon. Most side effects are transient.

Side effects: headache, nausea, constipation, dyspepsia.

Adverse effects:

Myopathy: injury to muscle tissue occurs in 5-10% of clients. Clients experience muscle aches, tenderness or weakness and can be diffuse or localized. Myositis (muscle inflammation) is rare, leading to elevated CK and potassium levels. Rarely, this can lead to rhabdomyolysis.
Rhabdomyolysis is a condition in which damaged skeletal muscle breaks down rapidly, causing muscle pain and weakness. Labs show elevated myoglobin and marked elevation of CK which can cause renal impairment due to CK plugging up glomeruli. Symptoms include renal impairment and a characteristic tea-coloured urine (DailyMed, 2025). Increased risk of myopathy are the older adult, low vitamin D and coenzyme Q levels, high doses of statins, concurrent use of fibrates and those with multiple health disorders.
Hyperglycemia: may increase blood sugar levels due to increasing insulin resistance or impairing insulin secretion in the beta cells. Risk of developing diabetes type 2 in pre-diabetic clients. Can raise H1C and random glucose levels.

Client Teaching

Clients should take the prescribed medication as directed and do not double up missed doses.
Avoid or limit consumption of grapefruit juice during drug therapy.
Continue with dietary and lifestyle modifications.
Inform client if they experience any muscle pain, tenderness, or weakness, these should be reported to the healthcare provider.
When obtaining a prescription, ensure that their prescribed statin is not substituted for a different statin.
If you plan to become pregnant, inform your health care provider. Statins are avoided during pregnancy.
Inform prescriber is planning on taking any OTC medications, herbal supplements or vitamins as they may interact with the med.

Vallerand & Sanoski (2024)

Downloadable file (.docx): Atorvastatin Medical Card

Fibric Acid Derivatives (Fibrates)

Gemfibrozil, is a fibrate used to treat hypercholesterolemia and mixed dyslipidemia. It is used mostly to lower triglyceride levels, but can also raise HDL levels. It has no effect on LDL levels. They are used less often due to higher risk of adverse effects when used with other antilipemic meds. As with all the antilipemic meds, dietary and lifestyle factors should be implemented. Other fibrates are fenofibrate and fenofibric acid.