Contents

1- Abstract 

2- Introduction (What are Antihyperlipidemic agents?)

3- History of antihyperlipidemic agents 

4- Types  of antihyperlipidemic agents 

5- Mechanism of action

6- Uses 

7- Side effects

8- Pharmacokinetics 

•  Absorption 

• Distribution

•  Metabolism 

• Excretion 

9- Interaction of Antihyperlipidimic druds

• Drug-drug interaction 

• Drug-food interaction

10- Condition to treat

4- Types  of antihyperlipidemic agents

Statins

 PCSK9 inhibitors

• PCSK9 inhibitors attach to a particular liver cell surface protein, which results in lowered LDL (“bad”) cholesterol. You can take this class of drug with statins. A provider can inject PCSK9 inhibitors for you. They’re usually for people at high risk of heart disease who haven’t been able to lower their cholesterol enough in other ways.

Fibric acid derivatives (fibrates)

• Fibric acid derivatives are antihyperlipidemics that reduce blood lipid (fat) levels, especially triglycerides. Your body creates triglycerides (fats) from food when you consume calories but don’t burn them. Fibric acid derivatives may also increase the level of HDL, the “good” cholesterol, while lowering liver production of LDL, the “bad” cholesterol. People who have severe kidney disease or liver disease shouldn’t take fibrates.

Bile acid sequestrants (bile acid resins)

• This class of cholesterol medication works inside your intestine by attaching to bile, a greenish fluid made of cholesterol your liver produces to digest food. The binding process means that less cholesterol is available in your body. Resins decrease LDL cholesterol and give a slight boost to HDL cholesterol levels.

Selective cholesterol absorption inhibitors (ezetimibe)

• This class of antihyperlipidemic works in your intestine to stop your body from absorbing cholesterol. These inhibitors reduce LDL cholesterol, but may also reduce triglycerides and increase HDL, or “good,” cholesterol. You can combine them with statins.

Nicotinic acid

• Nicotinic acid, or niacin, is a B-complex vitamin. You can get over-the-counter (OTC) versions of this, but some versions are prescription-only. Niacin decreases LDL cholesterol and triglycerides and increases HDL. If you have gout or severe liver disease, you shouldn’t take niacin.

Omega-3 fatty acid esters and polyunsaturated fatty acids (PUFAs)

• People often call these antihyperlipidemics fish oils. They use them to lower triglycerides. Some products are available over the counter, while others need a prescription (like ethyl eicosapentaenoic acid). Fish oils might interfere with other medications, and some people are allergic to fish and shellfish. Fish oils aren’t for everyone, so talk to a provider before taking them.

Adenosine triphosphate-citric lyase (ACL) inhibitors (bempedoic acid)

• Bempedoic acid works in your liver to slow down cholesterol production. You should take it with statin medications, but you’ll need to limit your dosage if you take it with simvastatin or pravastatin.

5- Mechanism of action

This drug group increases the cell absorption of LDL by blocking the enzyme (HMG-CoA reductase) regulating the rate-limiting step in the synthesis of cholesterol. With this alteration in fat metabolism, HDL increases slightly. Drugs under this classification are chemically-modified compounds from the products of fungi. watch the following to learn more.

6- Uses

Antihyperlipidemic drugs help you improve your cholesterol levels by:

• Decrease your LDL cholesterol.

• Decrease your VLDL cholesterol.

• Decrease your triglyceride level.

• Increase your HDL cholesterol.

• Reduce your risk of heart attack and stroke.

8- Pharmacokinetics 

kinetics properties of other anti hyperlipidemic agents (gemfibrozil) include: 

• Absorption:

  • Gemfibrozil is absorbed from the gastrointestinal tract.

* In healthy volunteers, a 900mg oral dose of gemfibrozil has a Cmax of 46±16μg/mL with a Tmax of 2.2±1.1h

* . In patients with chronic renal failure, gemfibrozil has a Cmax of  13.8±11.1μg/mL with a Tmax of 2.3±1.0h

* In patients with liver disease, gemfibrozil has a Cmax of 23.0±10.3μg/mL with a Tmax of 2.6±1.7h.

• Distribution:

 • The volume of distribution of gemfibrozil is estimated to be 0.8L/kg.

* Gemfibrozil is 99% protein bound.

* It is 98.6% bound to serum albumin, 0.8% bound to erythrocytes, and 0.8% unbound.

* There is negligible binding to alpha-1-acid glycoprotein.

•  Metabolism :

 • Gemfibrozil undergoes hydroxylation at the 5'-methyl and 4' positions to form the M1 and M2 metabolites respectively.

* Gemfibrozil also undergoes O-glucuronidation to form gemfibrozil 1-beta glucuronide, an inhibitor of CYP2C8.

* This O-glucuronidation is primarily mediated by UGT2B7, but also by UGT1A1, UGT1A3, UGT1A9, UGT2B4, UGT2B17.

• Excretion :

 • Approximately 70% of a dose of gemfibrozil is eliminated in the urine.

* The majority of a dose is eliminated as a glucuronide conjugate and <2% is elimiinated as the unmetabolized drug.

* 6% of a dose is eliminated in the feces.

9- Interaction of Antihyperlipidimic druds

• Drug-drug interaction 

Antihyperlipidemic medications can interact with various drugs, including:

1. Statins: Interactions with drugs like fibrates, some antibiotics, and antifungals can increase the risk of muscle damage.

2. Bile Acid Sequestrants: These can bind with other medications, reducing their absorption. It's advisable to take other medications either an hour before or four to six hours after taking bile acid sequestrants.

3. Niacin: It may increase the risk of muscle damage when combined with statins.

4. Ezetimibe: When combined with statins, it can increase the risk of liver damage.

• Drug-food interaction

• Food interaction of antihyperlipidemic drug :

1. Grapefruit juice: Grapefruit juice can increase the levels of some statins in the blood, potentially leading to side effects.

2. High-fat meals: Consuming high-fat meals may decrease the absorption of some statins, so it's generally advised to take them with food but not necessarily high-fat meals.

3. Alcohol: Drinking alcohol while taking fibrates or niacin can increase the risk of liver problems.

4. High-fiber foods: Fiber-rich foods can bind to bile acid sequestrants, potentially reducing their effectiveness.