Pharmacology of Statins and Gemfibrozil

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

What is the maximum recommended dose of simvastatin?

80 mg (correct)

40 mg

100 mg

60 mg

Which statin is primarily metabolized by CYP3A4?

Pitavastatin

Atorvastatin

Lovastatin (correct)

Rosuvastatin

What is the effect of atorvastatin on triglyceride (TG) levels?

No effect on TGs

Reduces TGs by 10–20%

Increases TGs by 15–20%

Reduces TGs by 25–35% (correct)

What is the plasma half-life of rosuvastatin?

18–24 hours Signup and view all the answers

Which statin is considered the most potent and recently introduced?

Pitavastatin Signup and view all the answers

When are most statins recommended to be taken for maximum effectiveness?

At bedtime Signup and view all the answers

What is a common side effect of using pitavastatin in conjunction with gemfibrozil?

Decreased clearance of pitavastatin Signup and view all the answers

Which statin shows a greater rise in HDL-CH when low?

Simvastatin Signup and view all the answers

What is the primary elimination route for gemfibrozil?

Urine Signup and view all the answers

Which of the following is a common adverse effect of gemfibrozil?

Eosinophilia Signup and view all the answers

What is the recommended dosage of gemfibrozil for patients with raised triglyceride levels?

600 mg twice daily Signup and view all the answers

Which condition is contraindicated for the use of gemfibrozil?

Pregnancy Signup and view all the answers

What differentiates bezafibrate from gemfibrozil in terms of side effects?

No increase in rhabdomyolysis with statin Signup and view all the answers

Which of the following is a significant difference in pharmacokinetics between gemfibrozil and fenofibrate?

Fenofibrate has a longer elimination half-life Signup and view all the answers

Which condition is most likely to require a dose adjustment when prescribing gemfibrozil?

Elderly patients Signup and view all the answers

What is the mechanism of action of gemfibrozil concerning lipid levels?

Lowers triglyceride levels Signup and view all the answers

What is one of the proposed mechanisms by which statins exert their antiatherosclerotic action?

Suppression of macrophage mediated inflammation Signup and view all the answers

What percentage decrease in LDL cholesterol can statins generally achieve?

20–50% Signup and view all the answers

How do statins improve endothelial function?

By increasing nitric oxide production Signup and view all the answers

What effect do statins have on HDL cholesterol levels?

Increase by 10–15% Signup and view all the answers

What other medication appears to reduce VLDL secretion by the liver?

Gemfibrozil Signup and view all the answers

Which condition may be effectively treated with bezafibrate?

Type III hyperlipoproteinaemia Signup and view all the answers

The increase in HDL cholesterol from statins is partly due to which process?

Transfer of surface lipid components from catabolized VLDL Signup and view all the answers

What is a notable side effect observed with prolonged use of statins in certain patients?

Increase in LDL cholesterol Signup and view all the answers

What is a recommended method to minimize the risk of statin myopathy?

Starting with a low dose and gradually increasing Signup and view all the answers

Which of the following is a role of laropiprant when combined with nicotinic acid?

Minimizes flushing without lowering lipid levels Signup and view all the answers

What effect does nicotinic acid have on triglycerides and VLDL levels?

Decreases triglycerides and VLDL rapidly Signup and view all the answers

What severe side effect is associated with the use of high doses of nicotinic acid?

Serious liver damage Signup and view all the answers

Which of the following describes a common side effect of high doses of nicotinic acid?

Flushing and dyspepsia Signup and view all the answers

What is the typical effect of fenofibrate on cholesterol levels?

Reduces triglyceride and VLDL levels Signup and view all the answers

In what situation should nicotinic acid not be used?

In cases of liver dysfunction Signup and view all the answers

What is the main mechanism by which nicotinic acid raises HDL cholesterol?

By decreasing the rate of HDL catabolism Signup and view all the answers

What is the primary indication for long-term use of nicotinic acid?

To control pancreatitis related to severe hypertriglyceridaemia Signup and view all the answers

Which adverse effect is most commonly associated with high doses of nicotinic acid?

Reversible hepatic dysfunction Signup and view all the answers

What percentage decrease in LDL cholesterol levels is typically observed with the use of Ezetimibe?

15-20% Signup and view all the answers

Which of the following statements about CETP inhibitors is true?

They increase the exchange of cholesteryl esters with triglycerides. Signup and view all the answers

What is a significant effect of combining statin and niacin therapy?

Greater reduction in carotid IMT Signup and view all the answers

Which condition limits the use of nicotinic acid in treatment?

Presence of high-risk cases only Signup and view all the answers

What is the typical recommended maintenance dose limit for nicotinic acid?

2 g/day Signup and view all the answers

What is an effect of Ezetimibe on cholesterol absorption?

It inhibits intestinal absorption of cholesterol. Signup and view all the answers

What was the outcome of the clinical trial involving torcetrapib?

It was found to increase cardiovascular events. Signup and view all the answers

What is the primary mechanism by which ezetimibe lowers cholesterol levels?

By undergoing enterohepatic circulation after conjugation. Signup and view all the answers

What effect does raising plasma cholesterol (CH) have on coronary artery disease (CAD) risk?

The higher the CH level, the greater the risk of CAD. Signup and view all the answers

What is the main limitation of ezetimibe when used alone?

It cannot lower LDL-CH levels beyond 15-20%. Signup and view all the answers

What might be a potential therapeutic value of CETP inhibitors?

Further research is being conducted to assess their efficacy. Signup and view all the answers

What is the significance of the combination therapy involving ezetimibe and a low dose of statin?

It offers similar LDL-CH lowering as high doses of statins. Signup and view all the answers

What is the plasma half-life of ezetimibe as stated?

22 hours Signup and view all the answers

What has substantial evidence confirmed regarding lowering LDL-CH?

It leads to a reduction in cardiovascular morbidity and mortality. Signup and view all the answers

Study Notes

Types of Primary Hyperlipoproteinemia

Type I: Familial lipoprotein lipase deficiency, very rare occurrence. Elevated chylomicrons, and increased triglycerides.
Type Ila: Familial hypercholesterolemia, less common. Elevated LDL cholesterol
Type Ilb: Polygenic hypercholesterolemia, most common. Elevated LDL cholesterol.
Type III: Familial dysbetalipoproteinemia, rare. Elevated IDL and chylomicron remnants, high levels of both LDL and Triglycerides.
Type IV: Hypertriglyceridemia, common. Elevated VLDL
Type V: Familial combined hyperlipidemia, less common. Elevated VLDL and LDL, high levels of both Triglycerides and Cholesterol.

Classification of Hypolipidemic Drugs

HMG-CoA reductase inhibitors (Statins): Lower cholesterol synthesis. Examples include lovastatin, simvastatin, atorvastatin, rosuvastatin.
Bile acid sequestrants (Resins): Reduce cholesterol absorption. Examples include cholestyramine, colestipol.
Lipoprotein lipase activators (Fibrates): Increase breakdown and reduce production of VLDL. Examples include gemfibrozil, bezafibrate, fenofibrate.
Nicotinic acid: Lowers VLDL, TG and increases HDL.
Sterol absorption inhibitors: Ezetimibe inhibits cholesterol absorption.

HMG-CoA Reductase Inhibitors (Statins)

Statins are potent and well-tolerated hypolipidemics.
They inhibit HMG-CoA reductase, reducing cholesterol synthesis: significantly lowering LDL.
Statins cause compensatory increase in LDL receptors on liver cells, leading to increased uptake and catabolism of LDL and IDL.
Statins are effective in lowering LDL-C, lowering TG levels, and slightly increasing HDL-C.
Statin efficacy is dose-dependent, with maximum LDL-C reductions seen with higher doses.

Studying That Suits You

Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

Description

Test your knowledge on the pharmacology of statins and gemfibrozil with this quiz. Questions cover dosage recommendations, metabolism, effects on cholesterol levels, and side effects associated with these medications. Perfect for students studying pharmacology or healthcare professionals looking to refresh their knowledge.