Questions and Answers
What do HMG-CoA Reductase Inhibitors lower?
What is the biggest side effect of antilipemic drugs?
Myopathy
All antilipemic drugs have generic names that end in what?
Statin
What are antilipemics primarily effective for?
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What is the mechanism of action for antilipemics?
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What are the therapeutic uses for antilipemics?
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List some contraindications for antilipemics.
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Name some adverse effects of antilipemics.
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What can interact with antilipemics?
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Which antilipemic carries the biggest risk for rhabdomylosis?
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What condition can all antilipemics potentially cause in the eyes?
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What are bile acid sequestrants now considered in cholesterol management?
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List the three available agents of bile acid sequestrants.
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What do bile acid sequestrants primarily treat?
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What is the mechanism of action for bile acid sequestrants?
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Name some contraindications for bile acid sequestrants.
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List some adverse effects of bile acid sequestrants.
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What medications can interact with bile acid sequestrants?
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What is the bile acid sequestrant of choice?
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What is a characteristic of Cholestyramine (Questran)?
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What is Colestipol (Colestid) primarily used for?
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What is Niacin (Nicotinic acid) used for?
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What are some adverse effects of Niacin?
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What preparations does Niacin come in?
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What are fibric acid derivatives primarily used for?
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What are Gemfibrozil (Lopid) and Fenofibrate (Tricor) used for?
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What does Ezetimibe (Zetia) do?
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Study Notes
Antilipemic Drugs Overview
- Antilipemic drugs primarily reduce LDL cholesterol and total cholesterol levels.
- They can also increase HDL and decrease triglycerides in some patients.
HMG-CoA Reductase Inhibitors
- Commonly known as statins; all generic names end in "statin."
- Mechanism of action involves blocking HMG-CoA reductase, decreasing cholesterol synthesis and increasing LDL receptor numbers in the liver.
Side Effects and Risks
- The most significant side effect is myopathy; liver toxicity is also a concern.
- Regular liver function tests (AST/ALT) are recommended.
- All antilipemics may cause cataracts.
Therapeutic Uses
- Indicated for hyperlipidemia, primary and secondary prevention of cardiovascular events, post-myocardial infarction therapy, and protecting diabetics from myocardial infarction.
Contraindications
- Includes drug allergies, pregnancy (category X), and liver disease.
Adverse Effects
- Common issues include GI upset, headaches, rash, insomnia, and constipation.
Drug Interactions
- Increased risk of myopathy when used with other lipid-lowering drugs.
- Statin levels can be elevated by drugs that inhibit CYP3A3 and grapefruit juice.
Bile Acid Sequestrants
- Second-line agents used alongside statins; examples include colesevelam, cholestyramine, and colestipol.
- These agents interfere with bile acid reabsorption, necessitating greater cholesterol use for bile acid synthesis.
Contraindications and Adverse Effects of Bile Acid Sequestrants
- Contraindicated in individuals with biliary or bowel obstruction and phenylketonuria (PKU).
- Side effects are generally limited to the GI tract, including constipation, bloating, nausea, and indigestion.
Specific Bile Acid Sequestrants
- Colesevelam is the preferred choice available in powder form; taken with food.
- Cholestyramine, also a powder, can decrease vitamin K levels and affect bleeding when combined with anticoagulants like Coumadin.
- Colestipol is available in tablet form and should also be taken with food.
Niacin
- Primarily used to treat triglyceride levels in patients at risk for pancreatitis and to improve HDL levels.
- Side effects include flushing, gastrointestinal upset, liver toxicity, and hyperglycemia.
Preparations and Forms of Niacin
- Available in immediate release, timed-release, and extended-release formulations; over-the-counter doses typically do not cause adverse effects.
Fibric Acid Derivatives
- Considered as third-line drugs for lipid management, specifically effective in reducing triglycerides and raising HDLs.
Gemfibrozil and Fenofibrate
- Gemfibrozil is administered 600 mg twice daily, taken 30 minutes before meals; similarly, fenofibrate has analogous actions.
- Adverse effects can include gallstones, myopathy, and liver toxicity.
- Both drugs interact with warfarin and statins, increasing bleeding risk and myopathy, respectively.
Ezetimibe
- Works by inhibiting dietary cholesterol absorption; used as adjunct therapy with dietary modifications.
- Interacts with fibrates and bile acid sequestrants and is generally well tolerated; standard dosage is 10 mg per day.
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Description
This quiz provides an overview of antilipemic drugs, focusing on their mechanisms of action, therapeutic uses, and potential side effects. It covers HMG-CoA reductase inhibitors (statins), indications for use, and important contraindications to consider. Test your knowledge on lipid-lowering therapies and their impact on cardiovascular health.
