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
Antihyperlipidemic agents promote reduction of lipid levels in the blood. Some antihyperlipidemic agents aim to lower the levels of low-density lipoprotein (LDL) cholesterol, some reduce triglyceride levels, and some help raise the high-density lipoprotein (HDL) cholesterol. By reducing the LDL cholesterol, they can prevent both the primary and secondary symptoms of coronary heart disease.
Antihyperlipidemic drugs have been developed since the late 1950s. Useful drugs among them include the fibrate series and the statin (HMG-CoA reductase inhibitor) series.
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 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.
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.
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, 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.
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.
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.
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.
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.
Pain, including muscle pain (myalgia) and back pain.
Swelling at the drug injection site.
Flu-like or cold-like symptoms.
Constipation or diarrhea and Weight loss.
Bloating, belching or vomiting.
Stomachache, headache or backache.
Muscle pain and weakness.
Sore throat and Stuffy nose.
Constipation or diarrhea.
-Weight loss.
-Belching and Bloating.
-Nausea and vomiting and Stomach pain.
Diarrhea and Fatigue.
Joint pain.
Flushing of your face and upper body.
Taking niacin with meals may make this better. You might have less flushing if you take aspirin about 30 minutes before taking niacin.
Skin issues, such as itching or tingling.
Headache, Coughing and Stomach upset.
Increased blood sugar.
Belching and Skin issues like rash or itching.
Gas and Fishy taste.
Slower blood clotting after a cut.
Upper respiratory infection.
Stomach, back or muscle pain and tendon injury.
Increased levels of uric acid.
kinetics properties of other anti hyperlipidemic agents (gemfibrozil) include:
• 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.
• 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.
• 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.
• 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.
Antihyperlipidemic medications can interact with various drugs, including:
Statins: Interactions with drugs like fibrates, some antibiotics, and antifungals can increase the risk of muscle damage.
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.
Niacin: It may increase the risk of muscle damage when combined with statins.
Ezetimibe: When combined with statins, it can increase the risk of liver damage.
Food interaction of antihyperlipidemic drug :
Grapefruit juice: Grapefruit juice can increase the levels of some statins in the blood, potentially leading to side effects.
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.
Alcohol: Drinking alcohol while taking fibrates or niacin can increase the risk of liver problems.
High-fiber foods: Fiber-rich foods can bind to bile acid sequestrants, potentially reducing their effectiveness.
Antihyperlipidemic agents are commonly used to treat conditions such as hyperlipidemia, which is characterized by elevated levels of lipids in the blood, including cholesterol and triglycerides. These agents are also prescribed to manage conditions like atherosclerosis, coronary artery disease, and other cardiovascular disorders.
In addition to the conditions mentioned earlier, antihyperlipidemic agents may also be used to treat familial hypercholesterolemia, which is an inherited disorder characterized by high levels of LDL cholesterol, as well as other lipid disorders such as mixed hyperlipidemia and dyslipidemia.
Certainly! Antihyperlipidemic agents are also prescribed as preventive measures for individuals at high risk of developing cardiovascular diseases, such as those with a family history of heart disease, smokers, individuals with obesity or diabetes, and those with hypertension. Additionally, they may be used in combination with lifestyle modifications like diet and exercise to manage lipid levels and reduce the risk of cardiovascular events.
Antihyperlipidemic agents can also be used in certain cases to prevent or manage complications associated with conditions like pancreatitis, which can be triggered by high levels of triglycerides in the blood. Furthermore, they may have potential therapeutic benefits in other conditions such as non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome, where abnormal lipid metabolism plays a significant role in the pathology of the disease.