21.3 Bile Acid Sequestrants, Fibrates, and Niacin

3 min readjune 18, 2024

Lowering cholesterol isn't just about . , , and are powerful allies in the fight against high lipids. These meds work in different ways to tackle LDL, triglycerides, and boost good HDL.

Each drug has its quirks. can cause tummy troubles and mess with other meds. Fibrates might make muscles ache. Niacin can make you flush like crazy. But with the right know-how, these side effects can be managed for better heart health.

Bile Acid Sequestrants, Fibrates, and Niacin

Bile acid sequestrants, fibrates, niacin lipid-lowering agents

  • Bile acid sequestrants bind to bile acids in intestine preventing reabsorption primarily lowering (, , )
  • Fibrates activate primarily lowering triglycerides increasing (, )
  • Niacin (vitamin B3, ) inhibits synthesis and release of from liver lowering LDL cholesterol, triglycerides, increasing HDL cholesterol

Bile acid sequestrants, fibrates, niacin reduce lipid levels

  • Bile acid sequestrants bind bile acids in intestine forming insoluble complex excreted in feces reducing bile acid reabsorption causing liver to use more cholesterol to produce new bile acids lowering blood cholesterol levels
  • Fibrates activate PPAR-α nuclear receptor regulating increasing activity enhancing breakdown of triglyceride-rich lipoproteins reducing VLDL production increasing LDL removal from bloodstream
  • Niacin inhibits enzyme synthesizing triglycerides and VLDL in liver decreasing VLDL release reducing LDL formation, increases lipoprotein lipase activity enhancing triglyceride-rich lipoprotein breakdown, reduces HDL catabolism increasing HDL levels

Side effects drug interactions lipid-lowering medications

  • Bile acid sequestrants cause , , nausea, , abdominal discomfort and decrease absorption of other medications (, thyroid hormones, digoxin)
  • Fibrates cause gastrointestinal disturbances, rash, myalgia, fatigue, headache and increase risk of when combined with statins potentiating anticoagulant effects
  • Niacin causes , , gastrointestinal disturbances, hyperglycemia, and potentiates effects of antihypertensives increasing risk of myopathy with statins

Nursing considerations administering bile acid sequestrants, fibrates, niacin

  • Bile acid sequestrants administer with plenty of fluids to minimize gastrointestinal side effects, separate administration from other medications by at least 2 hours, monitor for recommending high-fiber diet and hydration
  • Fibrates assess for signs of myopathy especially when combined with statins, monitor periodically, educate patients about importance of reporting muscle pain or weakness
  • Niacin administer with food to reduce flushing and gastrointestinal side effects, gradually increase dose to minimize side effects, monitor glucose and levels especially in patients with diabetes or , educate patients about management of flushing (taking aspirin before administration)

Patient education plan lipid-lowering drugs

  • Bile acid sequestrants explain mechanism of action and importance of lowering LDL cholesterol, provide strategies to manage constipation (high-fiber diet, adequate hydration), emphasize need to separate administration of other medications
  • Fibrates discuss benefits of lowering triglycerides and increasing HDL cholesterol, advise patients to report any muscle pain, weakness, or dark urine, encourage regular follow-up visits for monitoring liver function and lipid levels
  • Niacin explain multiple lipid-lowering effects, provide strategies to manage flushing (taking aspirin, gradual dose titration), advise patients to report any persistent side effects or worsening of preexisting conditions, emphasize importance of regular glucose and uric acid monitoring

Key Terms to Review (69)

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.
Apolipoprotein C-III: Apolipoprotein C-III (apo C-III) is a protein component of very low-density lipoproteins (VLDLs) and chylomicrons that plays a key role in regulating plasma triglyceride levels. It is an important factor in the context of bile acid sequestrants, fibrates, and niacin, as these therapies can influence apo C-III and thereby affect lipid metabolism.
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.
Atherosclerosis: Atherosclerosis is a chronic inflammatory condition characterized by the buildup of plaque within the arterial walls, leading to the narrowing and hardening of blood vessels. This condition is closely linked to various cardiovascular and cerebrovascular disorders, including intracranial emergencies, hypertension, and angina.
B3 (Niacin): Niacin, also known as Vitamin B3, is a water-soluble vitamin essential for metabolic processes and the health of the nervous system. It is involved in the conversion of nutrients into energy.
Bile Acid Reabsorption Inhibition: Bile acid reabsorption inhibition is a mechanism of action that involves the disruption of the enterohepatic circulation of bile acids, leading to their increased excretion and reduced absorption. This process is central to the therapeutic effects of certain drug classes, including bile acid sequestrants, fibrates, and niacin.
Bile acid sequestrants: Bile acid sequestrants are a class of drugs that bind bile acids in the intestine, preventing their reabsorption. This leads to increased conversion of cholesterol into bile acids, thereby lowering blood cholesterol levels.
Bile Acid Sequestrants: Bile acid sequestrants are a class of medications that bind to bile acids in the intestine, preventing their reabsorption and lowering cholesterol levels in the body. These agents are primarily used to manage high cholesterol and related cardiovascular conditions.
Bilirubin: Bilirubin is a yellow-orange pigment that is produced during the normal breakdown of red blood cells. It is an important component in the context of bile acid sequestrants, fibrates, and niacin, as well as masculinizing hormonal therapy.
Bloating: Bloating refers to a feeling of fullness, tightness, or swelling in the abdomen, often accompanied by gas or discomfort. It is a common symptom that can be associated with various gastrointestinal conditions and can also occur as a side effect of certain medications.
Blood Glucose: Blood glucose refers to the concentration of glucose, the primary sugar found in the bloodstream that serves as the body's main source of energy. It is an essential parameter in maintaining overall health and is closely regulated by various hormones and metabolic processes.
Cardiovascular Disease: Cardiovascular disease (CVD) is a group of disorders that affect the heart and blood vessels, including conditions such as coronary artery disease, heart attack, stroke, and high blood pressure. It is a major cause of morbidity and mortality worldwide, and understanding its relationship to topics like Angiotensin II Receptor Blockers (ARBs) and Bile Acid Sequestrants, Fibrates, and Niacin is crucial for healthcare professionals.
Cholelithiasis: Cholelithiasis is the medical term for the formation of gallstones, which are hard deposits made of cholesterol and other substances that develop in the gallbladder. This condition is closely related to the topics of bile acid sequestrants, fibrates, niacin, and cholesterol absorption inhibitors, as they all play a role in the management or prevention of gallstone formation.
Cholesevelam: Cholesevelam is a bile acid sequestrant used to lower low-density lipoprotein (LDL) cholesterol levels in the blood. It works by binding bile acids in the intestine, preventing their reabsorption.
Cholesteryl Ester Transfer Protein (CETP): Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that facilitates the exchange and transfer of cholesteryl esters and triglycerides between different lipoprotein particles, particularly high-density lipoproteins (HDL) and low-density lipoproteins (LDL). This protein plays a crucial role in the regulation of cholesterol metabolism and distribution within the body.
Cholestyramine: Cholestyramine is a bile acid sequestrant that binds bile acids in the intestine to prevent their reabsorption. It is used primarily to lower cholesterol levels and treat pruritus associated with partial biliary obstruction.
Colesevelam: Colesevelam is a bile acid sequestrant used to lower cholesterol levels in the blood. It works by binding bile acids in the intestine, preventing their reabsorption.
Colestid: Colestid is a bile acid sequestrant used to lower cholesterol levels in the blood. It works by binding bile acids in the intestine, preventing their reabsorption.
Colestipol: Colestipol is a bile acid sequestrant used to lower cholesterol levels in the blood. It binds to bile acids in the intestine, preventing their reabsorption and promoting their excretion.
Constipation: Constipation is a condition characterized by infrequent bowel movements or difficulty in passing stools. It can be a common side effect of opioid medications.
Constipation: Constipation is a common gastrointestinal condition characterized by infrequent or difficult bowel movements, often accompanied by hard, dry stool. This term is particularly relevant in the context of various medication classes, as certain drugs can either cause or alleviate constipation as a side effect or therapeutic effect.
Creatine Kinase: Creatine kinase (CK) is an enzyme found primarily in muscle tissue that catalyzes the reversible conversion of creatine and adenosine triphosphate (ATP) to phosphocreatine and adenosine diphosphate (ADP). This reaction plays a crucial role in the storage and rapid release of energy in muscle cells, making it an important marker for muscle damage or disease.
Diacylglycerol Acyltransferase 2 (DGAT2): Diacylglycerol acyltransferase 2 (DGAT2) is an enzyme that catalyzes the final step in the synthesis of triglycerides, which are the primary storage form of fat in the body. This enzyme plays a crucial role in lipid metabolism and is particularly relevant in the context of bile acid sequestrants, fibrates, and niacin.
Enterohepatic Circulation: Enterohepatic circulation is a physiological process in which substances, such as bile acids, are continuously recycled between the liver and the intestines. This closed-loop system allows for the efficient reabsorption and reuse of these important compounds, rather than their complete elimination from the body.
Extended-Release Niacin: Extended-release niacin, also known as sustained-release or slow-release niacin, is a formulation of the B-complex vitamin niacin (vitamin B3) that is designed to release the active ingredient gradually over an extended period. This extended-release mechanism allows for a more gradual and prolonged increase in niacin levels in the body compared to immediate-release niacin.
Fat-soluble vitamins: Fat-soluble vitamins are vitamins that are absorbed along with fats in the diet and can be stored in the body's fatty tissue. They include vitamins A, D, E, and K.
Fat-Soluble Vitamins: Fat-soluble vitamins are a group of essential nutrients that are absorbed and stored in the body's fatty tissues. Unlike water-soluble vitamins, they can accumulate in the body and have the potential for toxicity if consumed in excess. These vitamins play crucial roles in maintaining overall health and supporting various physiological processes.
Fenofibrate: Fenofibrate is a lipid-lowering medication that primarily targets triglycerides and increases high-density lipoprotein (HDL) levels. It is used to treat hyperlipidemia and hypertriglyceridemia.
Fenofibric acid: Fenofibric acid is the active metabolite of fenofibrate, a fibrate class drug used to reduce cholesterol levels and triglycerides in the blood. It primarily works by activating peroxisome proliferator-activated receptor alpha (PPARα).
Fibrates: Fibrates are a class of lipid-lowering drugs that primarily reduce triglyceride levels and can increase high-density lipoprotein (HDL) cholesterol. They work by activating peroxisome proliferator-activated receptors (PPARs), which regulate lipid metabolism.
Flatulence: Flatulence, commonly known as gas or passing wind, refers to the accumulation and expulsion of gas from the digestive system. This term is particularly relevant in the context of various pharmaceutical agents that can influence the production and expulsion of gas within the body.
Flushing: Flushing is a physiological response characterized by a temporary reddening or warmth of the face, neck, and upper body, often accompanied by a feeling of heat or discomfort. This phenomenon can occur in various contexts, including as a side effect of certain medications or as a result of certain medical conditions.
Gallbladder Disease: Gallbladder disease refers to a range of conditions affecting the gallbladder, a small organ located beneath the liver that stores and concentrates bile, a digestive fluid. These conditions can impact the proper functioning of the gallbladder and the body's ability to effectively utilize bile for digestion, leading to various health issues.
Gemcitabine: Gemcitabine is a nucleoside analog used as chemotherapy. It inhibits DNA synthesis, causing cell death in rapidly dividing cancer cells.
Gemfibrozil: Gemfibrozil is a medication used to reduce cholesterol and triglyceride levels in the blood. It belongs to the class of drugs known as fibrates.
Gout: Gout is a type of inflammatory arthritis caused by the buildup of uric acid crystals in the joints, leading to pain, swelling, and stiffness. It is closely related to the topics of diuretics, bile acid sequestrants, fibrates, niacin, loop diuretics, and thiazide diuretics, as these medications can impact the body's uric acid levels and management of gout.
HDL Cholesterol: HDL (High-Density Lipoprotein) cholesterol is a type of cholesterol that is often referred to as the 'good' cholesterol. It plays a crucial role in the transport and metabolism of lipids within the body, particularly in the context of Bile Acid Sequestrants, Fibrates, and Niacin.
Hepatic Impairment: Hepatic impairment refers to the reduced or compromised functioning of the liver, which can impact the metabolism and clearance of various medications. This term is particularly relevant in the context of opioid agonists and antagonists, bile acid sequestrants, fibrates, niacin, urinary antispasmodics, antimuscarinics, and anticholinergics, as the liver plays a crucial role in the pharmacokinetics and pharmacodynamics of these drug classes.
Hepatotoxicity: Hepatotoxicity is the occurrence of liver damage due to exposure to certain substances, including drugs. It can lead to serious health complications and requires careful monitoring.
Hepatotoxicity: Hepatotoxicity refers to the potential for certain drugs, chemicals, or other substances to cause liver damage or dysfunction. It is a critical consideration in the development and use of various medications and treatments.
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.
Hypertriglyceridemia: Hypertriglyceridemia is a condition characterized by an abnormally high level of triglycerides, a type of fat, in the blood. This metabolic disorder can have significant implications for an individual's cardiovascular health and overall well-being.
Hyperuricemia: Hyperuricemia is a condition characterized by an abnormally high level of uric acid in the blood. It is a key factor in the development of various medical conditions, including gout, kidney stones, and cardiovascular disease. This term is particularly relevant in the context of tuberculosis treatment, diuretic therapy, and the management of lipid disorders.
Immediate-Release: Immediate-release refers to a drug formulation that is designed to release the active pharmaceutical ingredient (API) immediately upon administration, allowing for rapid absorption and onset of action. This term is particularly relevant in the context of bile acid sequestrants, fibrates, and niacin, as the immediate-release properties of these medications can impact their therapeutic effects and pharmacokinetic profiles.
Institute for Safe Medication Practices: The Institute for Safe Medication Practices (ISMP) is a nonprofit organization dedicated to preventing medication errors and ensuring safe medication use. It provides resources, guidelines, and education to healthcare professionals to enhance patient safety.
LDL Cholesterol: LDL (low-density lipoprotein) cholesterol is a type of cholesterol that transports cholesterol particles from the liver to the body's cells. It is often referred to as the 'bad' cholesterol because high levels can contribute to the buildup of plaque in the arteries, increasing the risk of heart disease and stroke.
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.
Lipoprotein Lipase: Lipoprotein lipase is an enzyme responsible for the hydrolysis of triglycerides in lipoproteins, enabling the uptake and utilization of fatty acids by tissues. It plays a crucial role in the metabolism and regulation of lipoproteins, particularly in the context of lipoprotein and apolipoprotein dynamics, as well as the mechanisms of action for bile acid sequestrants, fibrates, and niacin.
Lipoprotein(a): Lipoprotein(a) is a unique type of lipoprotein particle that consists of low-density lipoprotein (LDL) cholesterol bound to a large glycoprotein called apolipoprotein(a). It is considered an independent risk factor for cardiovascular disease due to its ability to promote atherosclerosis and thrombosis.
Liver Function Tests: Liver function tests (LFTs) are a group of blood tests that provide information about the state of a person's liver. These tests measure the levels of certain enzymes and proteins in the blood, which can indicate liver damage or disease.
Lopid: Lopid, also known as gemfibrozil, is a medication used to lower lipid levels in the blood. It primarily reduces triglycerides and increases high-density lipoprotein (HDL) cholesterol.
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.
Niacin: Niacin, also known as vitamin B3, is an essential nutrient that plays a crucial role in various metabolic processes within the body. It is involved in the conversion of food into energy and the maintenance of healthy skin, nerves, and digestive system.
Nicotinic Acid: Nicotinic acid, also known as niacin, is a water-soluble B-complex vitamin that plays a crucial role in various metabolic processes within the body. It is an essential nutrient that can be obtained through dietary sources or supplementation, and it has particular relevance in the context of bile acid sequestrants, fibrates, and niacin therapy.
Oral Anticoagulants: Oral anticoagulants are a class of medications that work to prevent the formation of blood clots by interfering with the body's natural clotting mechanisms. They are commonly prescribed to patients at risk of developing blood clots, such as those with atrial fibrillation, deep vein thrombosis, or recent surgery.
Pediatric clients: Pediatric clients are children and adolescents who require medical care, including pharmacological treatments. Special considerations must be made for their unique physiological and developmental needs.
Peroxisome Proliferator-Activated Receptor Alpha (PPAR-α): Peroxisome proliferator-activated receptor alpha (PPAR-α) is a nuclear receptor that plays a crucial role in regulating lipid and glucose metabolism. It is a key player in the mechanisms of action for several classes of drugs, including bile acid sequestrants, fibrates, and niacin.
Pregnancy: Pregnancy is the period during which a fertilized egg develops into a fetus inside the uterus. It typically lasts around 40 weeks from the last menstrual period to childbirth.
Pregnancy: Pregnancy is the state of carrying a developing embryo or fetus within the female body. It is a crucial life event that involves significant physiological, hormonal, and metabolic changes in the mother's body to support the growth and development of the unborn child. Understanding the implications of pregnancy is essential in the context of various medical fields, including pharmacology, obstetrics, and gynecology.
Pruritus: Pruritus is an unpleasant, irritating sensation that provokes the desire to scratch. It is a common symptom associated with various medical conditions and can significantly impact a person's quality of life.
Questran: Questran, also known as cholestyramine, is a bile acid sequestrant used to lower cholesterol levels in the blood. It works by binding bile acids in the intestine, preventing their reabsorption.
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.
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.
Sustained-Release: Sustained-release, also known as extended-release or controlled-release, refers to drug formulations designed to release the active pharmaceutical ingredient(s) at a predetermined rate and duration to maintain a consistent therapeutic effect in the body over an extended period of time.
Tricor: Tricor is a brand name for fenofibrate, a medication used to reduce cholesterol levels, particularly triglycerides. It works by increasing the natural enzyme that breaks down fats in the blood.
Uric Acid: Uric acid is a waste product produced by the breakdown of purines, which are compounds found in certain foods and are also produced naturally in the body. It is primarily filtered out of the bloodstream by the kidneys and excreted through urine. Uric acid levels can impact various aspects of health, including the topics of bile acid sequestrants, fibrates, and niacin.
VLDL: VLDL, or very low-density lipoprotein, is a type of lipoprotein that transports triglycerides and cholesterol from the liver to peripheral tissues in the body. It plays a crucial role in lipid metabolism and is closely related to the topics of lipoprotein and apolipoprotein structure, as well as the mechanisms of action of bile acid sequestrants, fibrates, and niacin.
Warfarin: Warfarin is an anticoagulant medication used to prevent and treat blood clots. It works by inhibiting the production of certain clotting factors, thereby reducing the body's ability to form blood clots. Warfarin is a crucial drug in the context of pharmacology, interdisciplinary teams, nursing practice, drug administration, anticoagulant therapy, and hormonal therapy.
Welchol: Welchol (colesevelam) is a bile acid sequestrant used to lower LDL cholesterol levels in the blood. It works by binding bile acids in the intestine, preventing their reabsorption and promoting their excretion.
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