Pharmacology of Statins and Gemfibrozil

<p>18–24 hours (A)</p> Signup and view all the answers

<p>Pitavastatin (D)</p> Signup and view all the answers

<p>At bedtime (A)</p> Signup and view all the answers

<p>Decreased clearance of pitavastatin (B)</p> Signup and view all the answers

<p>Simvastatin (A)</p> Signup and view all the answers

<p>Urine (B)</p> Signup and view all the answers

<p>Eosinophilia (B)</p> Signup and view all the answers

<p>600 mg twice daily (C)</p> Signup and view all the answers

<p>Pregnancy (A)</p> Signup and view all the answers

<p>No increase in rhabdomyolysis with statin (A)</p> Signup and view all the answers

<p>Fenofibrate has a longer elimination half-life (B)</p> Signup and view all the answers

<p>Elderly patients (B)</p> Signup and view all the answers

<p>Lowers triglyceride levels (D)</p> Signup and view all the answers

<p>Suppression of macrophage mediated inflammation (A)</p> Signup and view all the answers

<p>20–50% (A), 10–15% (C)</p> Signup and view all the answers

<p>By increasing nitric oxide production (C)</p> Signup and view all the answers

<p>Increase by 10–15% (B)</p> Signup and view all the answers

<p>Gemfibrozil (B)</p> Signup and view all the answers

<p>Type III hyperlipoproteinaemia (A)</p> Signup and view all the answers

<p>Transfer of surface lipid components from catabolized VLDL (B)</p> Signup and view all the answers

<p>Increase in LDL cholesterol (C)</p> Signup and view all the answers

<p>Starting with a low dose and gradually increasing (B)</p> Signup and view all the answers

<p>Minimizes flushing without lowering lipid levels (C)</p> Signup and view all the answers

<p>Decreases triglycerides and VLDL rapidly (B)</p> Signup and view all the answers

<p>Serious liver damage (C)</p> Signup and view all the answers

<p>Flushing and dyspepsia (C)</p> Signup and view all the answers

<p>Reduces triglyceride and VLDL levels (D)</p> Signup and view all the answers

<p>In cases of liver dysfunction (C)</p> Signup and view all the answers

<p>By decreasing the rate of HDL catabolism (B)</p> Signup and view all the answers

<p>To control pancreatitis related to severe hypertriglyceridaemia (D)</p> Signup and view all the answers

<p>Reversible hepatic dysfunction (A)</p> Signup and view all the answers

<p>15-20% (B)</p> Signup and view all the answers

<p>They increase the exchange of cholesteryl esters with triglycerides. (B)</p> Signup and view all the answers

<p>Greater reduction in carotid IMT (D)</p> Signup and view all the answers

<p>Presence of high-risk cases only (C)</p> Signup and view all the answers

<p>2 g/day (A)</p> Signup and view all the answers

<p>It inhibits intestinal absorption of cholesterol. (C)</p> Signup and view all the answers

<p>It was found to increase cardiovascular events. (D)</p> Signup and view all the answers

<p>By undergoing enterohepatic circulation after conjugation. (A)</p> Signup and view all the answers

<p>The higher the CH level, the greater the risk of CAD. (B)</p> Signup and view all the answers

<p>It cannot lower LDL-CH levels beyond 15-20%. (D)</p> Signup and view all the answers

<p>Further research is being conducted to assess their efficacy. (C)</p> Signup and view all the answers

<p>It offers similar LDL-CH lowering as high doses of statins. (C)</p> Signup and view all the answers

<p>22 hours (C)</p> Signup and view all the answers

<p>It leads to a reduction in cardiovascular morbidity and mortality. (D)</p> Signup and view all the answers

A class of drugs that lower cholesterol by inhibiting the enzyme HMG-CoA reductase, which is involved in cholesterol synthesis.

The time it takes for the concentration of a drug in the body to reduce by half.

A type of enzyme that metabolizes many drugs, including statins.

A type of lipid often referred to as 'good' cholesterol, which can help remove bad cholesterol from the body.

A type of lipid often referred to as 'bad' cholesterol, which can accumulate in the arteries and contribute to heart disease.

A specific type of statin that is commonly used with a long half-life, often given at bedtime.

The maximum effect a drug can have, regardless of the dose.

A class of drugs that are often used to lower high triglycerides levels.

Statins are a group of drugs that lower cholesterol levels by inhibiting an enzyme called HMG-CoA reductase, which is involved in cholesterol synthesis.

Statins can reduce the risk of heart disease by improving blood vessel function, stabilizing plaques in arteries, and reducing inflammation.

Fibrates are a class of drugs that lower triglyceride levels by stimulating an enzyme called lipoprotein lipase, which breaks down triglycerides.

Fibrates can also increase HDL (good) cholesterol levels by promoting the transfer of lipid components from VLDL to HDL.

Fibrates are particularly effective in treating type III hyperlipoproteinemia, a rare genetic disorder characterized by high levels of both cholesterol and triglycerides.

Gemfibrozil and bezafibrate can change the composition of LDL cholesterol, shifting small, dense LDL particles (which are more likely to cause atherosclerosis) to larger, less dense particles.

Statins are typically the first choice drugs for managing high cholesterol levels.

Fibrates are used primarily for treating high triglyceride levels, especially when they are high enough to increase the risk of pancreatitis.

An oral medication used to decrease high triglyceride levels, it is well-absorbed, undergoes metabolism in the liver, and gets eliminated through urine.

A common side effect of Gemfibrozil that can cause discomfort in the upper stomach area, particularly after eating.

A combination of Gemfibrozil and Statins may increase the risk of muscle breakdown, a serious condition. This risk is especially high in elderly patients or those with kidney problems.

A fibrate medication that has a longer lasting effect in the body, making it ideal for controlling cholesterol levels.

Fenofibrate can be combined with statins to help lower harmful LDL ('bad') cholesterol levels, without necessarily increasing the risk of muscle breakdown.

Although rare, Fenofibrate can cause inflammation of the liver (Hepatitis) and muscle breakdown (Rhabdomyolysis).

Fibrates, like Gemfibrozil and Fenofibrate, are primarily used to lower high triglyceride levels, but they also have an impact on cholesterol levels.

Nicotinic acid is a B vitamin that acts as a lipid-lowering agent, independent of its vitamin function. It effectively reduces triglycerides and VLDL cholesterol levels, and also promotes a modest decrease in LDL and total cholesterol.

Nicotinic acid is highly effective at increasing HDL cholesterol levels, possibly by slowing down the breakdown of HDL particles. This makes it a valuable medication for improving cholesterol profiles.

Nicotinic acid has the potential to cause flushing, a skin reddening similar to sunburn, due to its effects on prostaglandin synthesis. This side effect can be minimized by taking nicotinic acid with a meal, starting with lower doses, and gradually increasing the dose as needed.

Laropiprant is a drug specifically developed to block the prostaglandin pathway responsible for flushing. It's often used in combination with nicotinic acid to minimize flushing discomfort. It does not have any lipid-lowering properties on its own.

Nicotinic acid can cause unpleasant gastrointestinal symptoms like dyspepsia, vomiting, and diarrhea. These side effects are most prominent when full doses are taken.

Long-term use of nicotinic acid can lead to liver issues, including dysfunction and jaundice. This makes monitoring liver function essential during treatment. Nicotinic acid is contraindicated in patients with pre-existing liver problems.

Nicotinic acid can cause an increase in blood sugar levels and may even trigger diabetes in some individuals. It's important to carefully consider its use in patients with diabetes or impaired glucose tolerance.

Both fibrates and niacin can effectively reduce triglyceride levels and raise HDL cholesterol levels. However, fibrates typically don't have the same potential for raising HDL cholesterol levels as niacin.

Nicotinic acid, a B vitamin, dilates blood vessels in the skin, causing flushing, warmth, and itching. These effects are more pronounced with higher doses.

Nicotinic acid is a medication used to lower high cholesterol levels, especially when combined with other treatments. It's most effective for individuals who are at high risk of heart disease.

Nicotinic acid can lower the risk of heart attacks and further coronary events in patients who have already experienced a heart attack.

Nicotinic acid is primarily indicated to control pancreatitis related to extremely high triglyceride levels, particularly in individuals with certain genetic conditions.

Nicotinic acid can sometimes be used to lower high cholesterol levels, but its use is restricted to high-risk cases due to potential side effects.

Ezetimibe is a medication that works by reducing the absorption of cholesterol from the gut, both dietary and from bile. It targets a specific protein in the intestinal wall.

Ezetimibe is often used in combination with statins to further lower cholesterol and improve heart health. It's a valuable addition for those who need more significant cholesterol reduction.

Ezetimibe is generally well-tolerated, with few side effects. However, some patients may experience reversible liver function changes or rare cases of muscle problems.

Ezetimibe works by blocking the absorption of cholesterol from the small intestine, primarily through a mechanism called Niemann-Pick C1-like 1 (NPC1L1) inhibition.

Ezetimibe is often used in combination with statins to achieve better cholesterol reduction than either drug alone. This approach is particularly effective when statins alone aren't enough to reach target cholesterol levels.

Ezetimibe is a weak cholesterol-lowering drug when used alone, achieving limited LDL-C reduction beyond 15-20%. Increasing the dose does not significantly increase its effectiveness.

Torcetrapib is a drug that inhibits cholesteryl ester transfer protein (CETP), which helps move cholesterol from high-density lipoprotein (HDL) to low-density lipoprotein (LDL). It was initially believed to be promising, but a large clinical trial demonstrated an increased risk of cardiovascular events.

Despite the setbacks with torcetrapib, researchers continue to investigate whether other CETP inhibitors could be effective and safe therapies. However, the results so far are uncertain, and the therapeutic value of this class of drugs is currently doubtful.

High cholesterol levels are a major risk factor for coronary artery disease (CAD). The higher the cholesterol level, the greater the risk of developing CAD.

Numerous studies have confirmed that lowering LDL-cholesterol levels, especially when they are high, significantly reduces the risk of cardiovascular mortality and morbidity.

Recent studies like the HPS (2002) and ASCOT-LLA (2003) have shown that using statins prophylactically (preventively) in patients with CAD or hypertension, even those with average or lower cholesterol levels, lowers the risk of coronary events and strokes.