Hyperlipidemia or high cholesterol is a condition where excessive amounts of lipids (fats) accumulate in the blood. This can increase the risks of cardiovascular diseases like heart attack and stroke. Lifestyle modifications like dietary changes and exercise can help control cholesterol levels to some extent. However, medications are often required to bring cholesterol values down to the recommended levels. Let us look at the different classes of antihyperlipidemic or lipid lowering drugs available.

Statins

Statins are considered as first-line drugs for treatment of hypercholesterolemia. They work by inhibiting an enzyme called HMG-CoA reductase which is involved in cholesterol synthesis in the liver. Some common statins available include atorvastatin, rosuvastatin, simvastatin, pravastatin, etc. Statins are highly effective in lowering LDL or bad cholesterol by around 50% on average. They also modestly lower triglyceride levels and cause a small rise in HDL or good cholesterol. Statins have proved cardiovascular benefits and are the most widely prescribed antihyperlipidemic medications worldwide. Side effects of statins include muscle pain, liver dysfunction but are generally well-tolerated.

PCSK9 Inhibitors

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors are a newer class of injectable drugs for treatment of hypercholesterolemia. PCSK9 binds to LDL receptors on liver cells and promotes their degradation, thereby increasing LDL levels. PCSK9 inhibitors like alirocumab, evolocumab directly bind and inhibit PCSK9 leading to more LDL receptors on surface of liver cells, enhanced clearance of LDL from blood and substantial reduction in LDL levels by around 60%. These powerful drugs are used as add-on therapy for patients not achieving optimal LDL goals with high intensity statin and other agents or those who are statin-intolerant.

Bile acid sequestrants

Bile acid sequestrants are oral non-statin drugs which bind to bile acids in gut and promote their elimination. This enhances clearance of cholesterol from liver via upregulation of LDL receptors which lowers circulating LDL levels. Common bile acid sequestrants used are cholestyramine, colestipol and colesevelam. They are moderately effective in reducing LDL by around 15-25% and can also modestly lower triglyceride levels. Side effects include constipation and interference with absorption of other drugs when taken simultaneously.

Fibrates

Fibrates act by activating peroxisome proliferator-activated receptor alpha (PPAR-α) receptors leading to reduced hepatic triglyceride synthesis and increased breakdown of triglyceride-rich lipoproteins. They primarily lower triglyceride levels by around 30-50% and modestly increase HDL cholesterol levels by 5-15%. Common fibrates used are fenofibrate, gemfibrozil and bezafibrate. They have proven benefits in reducing cardiovascular risk in patients with high triglyceride levels and low HDL. Side effects can include gastrointestinal upset and gallbladder disease.

Niacin

Niacin or nicotinic acid is one of the oldest lipid lowering agents used for alternative of Antihyperlipidemic Drugs. It effectively lowers LDL, triglyceride levels and markedly increases HDL cholesterol levels by 15-30% when used in high doses. Niacin works through various mechanisms but its primary action is inhibition of lipolysis in adipose tissue. It was previously a commonly used drug but its use has reduced now due to risk of side effects like flushing, hyperglycemia and hepatotoxicity with high doses required for optimal lipid effects. Extended release preparations are better tolerated.

Ezetimibe

Ezetimibe is a relatively new drug which lowers cholesterol by inhibiting cholesterol absorption from intestine. It works by blocking the Niemann-Pick C1-like 1 protein which transports cholesterol across intestinal wall. Ezetimibe effectively lowers LDL levels by around 15-20% when used alone or in combination with statins. It is generally well-tolerated and can be useful as adjunct therapy in patients requiring additional LDL lowering or those who cannot tolerate higher potency statins.

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