21.2 Statins (HMG-CoA Reductase Inhibitors) and PCSK9 Inhibitors
2 min read•june 18, 2024
and are powerful tools in the fight against high cholesterol. These medications work in different ways to lower lipid levels in the blood, reducing the risk of heart disease and stroke.
Understanding how these drugs work is crucial for nurses. We'll look at their mechanisms of action, clinical uses, side effects, and important nursing considerations to help patients get the most benefit from lipid-lowering therapy.
Mechanisms of Action and Effects
Statins and PCSK9 inhibitors lower lipid levels
Statins ( inhibitors)
Block HMG-CoA reductase enzyme involved in rate-limiting step of liver cholesterol synthesis
Decreases liver cholesterol production causing upregulation of on liver cells
Increased LDL receptor expression enhances removal of LDL and VLDL from blood (, )
bind to and inhibit PCSK9 protein
PCSK9 normally binds LDL receptors causing their breakdown and reducing LDL removal
Inhibiting PCSK9 increases available LDL receptors on liver cells
Enhanced LDL receptor expression increases removal of LDL and VLDL from blood (, )
Clinical Use and Efficacy
Indications and effectiveness of statins vs PCSK9 inhibitors
Indications
Statins first-line for primary and secondary prevention of (ASCVD)
PCSK9 inhibitors for or ASCVD patients needing more LDL lowering despite maximum statin dose
Effectiveness
Statins reduce LDL 30-50% and significantly reduce cardiovascular event and mortality risk
PCSK9 inhibitors further lower LDL 50-60% when added to statin
Statin plus PCSK9 inhibitor can reduce LDL up to 75-80%
PCSK9 inhibitors show additional cardiovascular risk reduction when combined with statins
Adverse Effects and Interactions
Common side effects and drug interactions with statins and PCSK9 inhibitors
Statins
Common side effects: muscle pain/weakness, fatigue, digestive issues, headache, elevated liver enzymes
Rare serious side effects: , , liver damage
Drug interactions: increased muscle side effect risk when combined with certain antibiotics, antifungals, fibrates
PCSK9 inhibitors
Generally well-tolerated with few side effects
Most common adverse effect is injection site reactions (pain, redness, itching)
No significant drug interactions identified so far
Nursing Considerations
Key nursing considerations and patient education for lipid-lowering medications
Nursing considerations
Monitor lipid levels and liver function tests regularly
Assess for muscle symptoms and check creatine kinase if muscle symptoms occur
Encourage medication and lifestyle changes
Educate patients to report any adverse effects
Patient education
Emphasize how lipid-lowering medications reduce cardiovascular risk
Discuss importance of taking medications as prescribed and not stopping without consulting provider
Advise reporting any muscle symptoms, unexplained fatigue, yellowing skin/eyes
For PCSK9 inhibitors, teach proper injection technique and medication storage
Key Terms to Review (45)
Adherence: Adherence refers to the extent to which a person's behavior, such as taking medication, following a diet, or executing lifestyle changes, corresponds with the recommendations or instructions provided by their healthcare provider. It is a critical factor in the successful management of various health conditions, including HIV/AIDS and cardiovascular diseases like those treated with statins and PCSK9 inhibitors.
Alirocumab: Alirocumab is a monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), leading to increased clearance of low-density lipoprotein cholesterol (LDL-C) from the bloodstream. It is used as an adjunct to diet and maximally tolerated statin therapy for patients who require additional lipid-lowering treatment.
ALT: ALT, or alanine aminotransferase, is an enzyme found primarily in the liver that is released into the bloodstream when the liver is damaged or inflamed. It is a key biomarker used to assess liver health and function in the context of various medical conditions and drug therapies.
American Heart Association: The American Heart Association (AHA) is a non-profit organization dedicated to fighting cardiovascular diseases and promoting heart health through research, education, and advocacy. It plays a crucial role in setting guidelines for the management of cardiovascular conditions.
AST: AST, or aspartate aminotransferase, is an enzyme found primarily in the liver and heart that is used as a biomarker to assess liver and heart health. It is a key term that is relevant in the context of understanding the mechanisms and effects of various lipid-lowering medications as well as the monitoring of masculinizing hormone therapy.
Atherosclerotic Cardiovascular Disease: Atherosclerotic cardiovascular disease (ASCVD) is a chronic condition characterized by the buildup of fatty deposits, known as plaque, within the walls of the arteries. This gradual narrowing and hardening of the arteries can restrict blood flow to vital organs, leading to an increased risk of heart attack, stroke, and other cardiovascular events.
Atorvastatin: Atorvastatin is a statin medication used to lower cholesterol levels and reduce the risk of cardiovascular disease. It works by inhibiting HMG-CoA reductase, an enzyme involved in cholesterol synthesis in the liver.
Cardiovascular Risk Assessment: Cardiovascular risk assessment is the process of evaluating an individual's likelihood of developing cardiovascular disease, such as heart attack or stroke, based on various risk factors. This assessment is crucial in guiding prevention and management strategies for maintaining cardiovascular health, particularly in the context of statins (HMG-CoA reductase inhibitors) and PCSK9 inhibitors.
Cholesterol Biosynthesis: Cholesterol biosynthesis is the metabolic pathway by which cholesterol is produced from simpler precursor molecules within the body. This process is crucial for maintaining proper cellular function and is closely linked to the regulation of blood cholesterol levels.
Clarithromycin: Clarithromycin is a macrolide antibiotic used to treat various bacterial infections. It is particularly relevant in the context of statins (HMG-CoA reductase inhibitors) and PCSK9 inhibitors, as it can interact with these medications and affect their metabolism and efficacy.
Crestor: Crestor (rosuvastatin) is a statin medication used to lower cholesterol and triglycerides in the blood. It works by inhibiting HMG-CoA reductase, an enzyme involved in the production of cholesterol in the liver.
Cyclosporine: Cyclosporine is an immunosuppressant drug primarily used to prevent organ rejection in transplant patients and to treat various autoimmune disorders. It works by inhibiting the activation and proliferation of T-cells, a critical component of the body's immune response.
Erythromycin: Erythromycin is a macrolide antibiotic used to treat a variety of bacterial infections. It works by inhibiting bacterial protein synthesis, preventing the growth and spread of harmful microorganisms. Erythromycin's versatility makes it an important drug in the treatment of conditions related to calcium channel blockers, statins, ocular anti-inflammatories and anti-infectives, as well as acne drugs.
Evolocumab: Evolocumab is a monoclonal antibody used as an adjunct to diet and maximally tolerated statin therapy to reduce low-density lipoprotein cholesterol (LDL-C). It works by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9), which increases the number of LDL receptors available to clear LDL from the blood.
Familial Hypercholesterolemia: Familial hypercholesterolemia is an inherited genetic disorder characterized by abnormally high levels of low-density lipoprotein (LDL) cholesterol in the blood, leading to an increased risk of early-onset cardiovascular disease. This term is closely related to the topics of lipoprotein and apolipoprotein metabolism, as well as the use of statins and PCSK9 inhibitors to manage this condition.
Fluvastatin XL: Fluvastatin XL is an extended-release form of fluvastatin, a statin medication used to lower cholesterol levels by inhibiting HMG-CoA reductase. It is commonly prescribed for patients with hypercholesterolemia to reduce the risk of cardiovascular disease.
Hepatic Clearance: Hepatic clearance refers to the process by which the liver removes drugs and other substances from the bloodstream, playing a crucial role in the body's ability to metabolize and eliminate these compounds. This term is particularly relevant in the context of understanding the pharmacokinetics and pharmacodynamics of statins, PCSK9 inhibitors, and antitussives.
HMG-CoA Reductase: HMG-CoA reductase is a crucial enzyme involved in the cholesterol biosynthesis pathway. It catalyzes the conversion of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, which is a rate-limiting step in the production of cholesterol within the body. This enzyme plays a central role in the context of statins, a class of medications that inhibit HMG-CoA reductase to lower cholesterol levels, as well as PCSK9 inhibitors, a newer class of drugs that target the PCSK9 protein to indirectly regulate HMG-CoA reductase activity.
Hypercholesterolemia: Hypercholesterolemia refers to the condition of having abnormally high levels of cholesterol in the blood. This elevated cholesterol can contribute to the development of various cardiovascular diseases, making it an important consideration in the context of the topics covered in Chapters 21.2, 21.3, and 21.4.
Inclisiran: Inclisiran is a small interfering RNA (siRNA) drug that targets PCSK9 mRNA, leading to decreased LDL cholesterol levels in the bloodstream. It is used primarily for patients with hypercholesterolemia who are at high risk of cardiovascular events.
LDL Receptors: LDL receptors are cell surface proteins that bind to low-density lipoprotein (LDL) particles, facilitating their uptake and removal from the bloodstream. These receptors play a crucial role in regulating blood cholesterol levels and are a key target for cholesterol-lowering therapies, such as statins and PCSK9 inhibitors.
Leqvio: Leqvio (inclisiran) is a medication that lowers LDL cholesterol levels by inhibiting the synthesis of PCSK9. It is administered as a subcutaneous injection and works in conjunction with statins.
Lescol XL: Lescol XL is an extended-release formulation of fluvastatin, a statin medication used to lower cholesterol levels and reduce the risk of cardiovascular disease. It works by inhibiting HMG-CoA reductase, an enzyme involved in cholesterol synthesis.
Lipid Metabolism: Lipid metabolism refers to the complex biological processes involved in the synthesis, breakdown, and utilization of lipids, which are a diverse group of organic compounds that include fats, oils, waxes, and related molecules. This term is central to understanding the topics of 21.1 Introduction to Lipoprotein and Apolipoproteins, 21.2 Statins (HMG-CoA Reductase Inhibitors) and PCSK9 Inhibitors, and 21.3 Bile Acid Sequestrants, Fibrates, and Niacin, as lipid metabolism plays a crucial role in the regulation of lipid levels and the development of cardiovascular diseases.
Lipitor: Lipitor is the brand name for atorvastatin, a statin medication used to lower cholesterol levels and reduce the risk of cardiovascular disease. It works by inhibiting HMG-CoA reductase, an enzyme involved in cholesterol production in the liver.
Livalo: Livalo is a prescription medication used to lower cholesterol and triglycerides in the blood. It belongs to a class of drugs known as statins, which work by inhibiting HMG-CoA reductase.
Lovastatin: Lovastatin is a statin medication used primarily to lower cholesterol levels and reduce the risk of cardiovascular disease. It works by inhibiting HMG-CoA reductase, an enzyme involved in cholesterol synthesis in the liver.
Monoclonal antibodies: Monoclonal antibodies are laboratory-made molecules that can bind to specific targets, such as antigens on cancer cells. They are used in various therapies, including for cancer and autoimmune diseases.
Monoclonal Antibodies: Monoclonal antibodies are laboratory-produced immune system proteins that are designed to target specific antigens or molecules. They are created by cloning a unique white blood cell, allowing for the mass production of a single, highly specialized antibody that can recognize and bind to a particular target.
Myopathy: Myopathy refers to a group of disorders that primarily affect the muscles, leading to muscle weakness, pain, and impaired function. This term is particularly relevant in the context of various lipid-lowering medications, as certain myopathic conditions can arise as adverse effects of these treatments.
Nasopharyngitis: Nasopharyngitis, also known as the common cold, is an inflammation of the upper respiratory tract that primarily affects the nasal passages and the nasopharynx, the upper part of the throat behind the nose. This condition is commonly caused by viral infections and can occur in the context of various medical treatments, including the use of statins and PCSK9 inhibitors.
PCSK9 inhibitors: PCSK9 inhibitors are a class of drugs that lower LDL cholesterol levels by inhibiting the protein PCSK9, which increases the liver's ability to remove LDL from the blood. They are often used for patients who do not respond adequately to statins or have familial hypercholesterolemia.
PCSK9 Inhibitors: PCSK9 inhibitors are a class of medications that target and inhibit the proprotein convertase subtilisin/kexin type 9 (PCSK9) enzyme, which plays a crucial role in regulating low-density lipoprotein (LDL) cholesterol levels in the body. By inhibiting PCSK9, these drugs effectively lower LDL cholesterol, making them an important therapeutic option for individuals with high cholesterol levels, particularly those who are unable to achieve their target cholesterol goals with traditional treatments like statins.
Pitavastatin: Pitavastatin is a lipid-lowering medication belonging to the statin class, used to reduce cholesterol levels. It works by inhibiting HMG-CoA reductase, an enzyme involved in cholesterol synthesis in the liver.
Pleiotropic effects: Pleiotropic effects are additional, non-lipid lowering benefits provided by certain drugs. In pharmacology, these effects can include anti-inflammatory, antioxidant, and vascular benefits.
Praluent: Praluent (alirocumab) is a monoclonal antibody used to lower LDL cholesterol levels. It belongs to the class of drugs known as PCSK9 inhibitors.
Pravachol: Pravachol is a brand name for pravastatin, a statin medication that lowers cholesterol levels by inhibiting HMG-CoA reductase. It is used to reduce the risk of cardiovascular disease and manage hyperlipidemia.
Pravastatin: Pravastatin is a lipid-lowering medication that belongs to the class of drugs known as statins or HMG-CoA reductase inhibitors. It works by reducing levels of low-density lipoprotein (LDL) cholesterol and triglycerides in the blood while increasing high-density lipoprotein (HDL) cholesterol.
Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9): Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) is a protein that plays a crucial role in regulating the levels of low-density lipoprotein (LDL) cholesterol in the body. PCSK9 is a key player in the context of statins (HMG-CoA reductase inhibitors) and PCSK9 inhibitors, which are important therapeutic options for managing cholesterol levels and reducing the risk of cardiovascular disease.
Repatha: Repatha (evolocumab) is a monoclonal antibody that inhibits PCSK9 and is used to lower LDL cholesterol levels in patients. It is often prescribed for those who have not achieved desired cholesterol levels with statins alone.
Rhabdomyolysis: Rhabdomyolysis is a serious condition that occurs when damaged or destroyed skeletal muscle cells release their contents, including a protein called myoglobin, into the bloodstream. This can lead to various complications and is particularly relevant in the context of certain cholesterol-lowering medications and other drugs that affect lipid metabolism.
Rosuvastatin: Rosuvastatin is a statin medication used to lower cholesterol levels and reduce the risk of cardiovascular diseases. It works by inhibiting the enzyme HMG-CoA reductase, which plays a central role in the production of cholesterol in the liver.
Simvastatin: Simvastatin is a lipid-lowering medication that inhibits the enzyme HMG-CoA reductase, which plays a central role in the production of cholesterol. It is primarily used to lower low-density lipoprotein (LDL) cholesterol levels and reduce cardiovascular risk.
Statins: Statins are a class of medications primarily used to lower cholesterol levels in the blood by inhibiting the enzyme HMG-CoA reductase, a key enzyme involved in the production of cholesterol. They play a crucial role in the management of cardiovascular health by reducing the risk of heart disease and stroke.
Zocor: Zocor, also known as simvastatin, is a lipid-lowering medication that inhibits HMG-CoA reductase. It is primarily used to reduce cholesterol levels and prevent cardiovascular disease.