HMG-CoA Reductase Inhibitors (Statins)

HMG-CoA Reductase Inhibitors (Statins)

• Statins are oral medications used to lower cholesterol levels
• They work by inhibiting HMG-CoA reductase, a key enzyme in cholesterol synthesis
• Atorvastatin, Fluvastatin, Rosuvastatin, Lovastatin, Simvastatin, Pitavastatin, and Pravastatin are examples of statins.
• Some statins are prodrugs, meaning they are inactive until metabolized in the body
• Active forms of statins are inhibitors, meaning they block the production of cholesterol
• Statins increase LDL receptors in the liver, effectively removing LDL cholesterol from the blood.
• Statins are generally well-tolerated but should be avoided by those with certain conditions like pregnancy, liver disease, and heavy alcohol consumption.

Drug Interactions

• Statins can interact with other medications.
• Grapefruit juice can inhibit the metabolism of some statins, potentially increasing their levels in the blood.
• Some statins should not be taken with fibrates (Gemfibrozil).
• Certain azoles or macrolides should be used cautiously with statins

Bile Acid Binding Resins

• These resins are used to lower cholesterol levels by binding bile acids in the intestine, preventing their reabsorption and stimulating the liver to produce more bile acids from cholesterol.
• Examples include Colestipol and Cholestyramine.
• These medications may cause gastrointestinal discomfort, such as heartburn, diarrhea, and bloating.
• They should be taken before meals.
• Interaction with fat soluble vitamins such as vitamin K may be reduced.

Fibrates

• Fibrates (e.g., Gemfibrozil, Fenofibrate) are used to lower triglycerides and raise HDL cholesterol.
• They work by activating PPAR-α receptors, which affect lipid metabolism.
• These drugs may cause myopathy and interact with other drugs.
• Fenofibrate is usually better tolerated compared to gemfibrozil.

Sterol Absorption Inhibitors

• These drugs (e.g., Ezetimibe) work by inhibiting the absorption of cholesterol from the intestines.
• They are often used in combination with statins for a more significant reduction in LDL cholesterol.

PCSK9 Inhibitors (Monoclonal Antibodies)

• These are used to lower LDL cholesterol by reducing LDL receptor degradation.
• They are given via injection (subcutaneous).
• Examples include Evolocumab (brand name Repatha) and Alirocumab (brand name Praluent).
• They are used to treat high cholesterol, especially in patients with a severe form of hypercholesterolemia, those with an inadequate response to other lipid-lowering agents, or with other factors such as diabetes that might increase risk of cardiovascular events

Niacin (Nicotinic Acid)

• A vitamin that can also lower cholesterol levels.
• It reduces the production of VLDL and increases HDL levels, effectively improving lipid profile.
• Common side effects include flushing, and should be administered carefully with patient monitoring.

Fish Oil (Omega-3 Fatty Acids)

• Primarily used to reduce triglycerides.
• May improve blood lipid profile, in particular, lowering triglycerides.
• May cause side effects like increased bleeding and should be used with caution by patients taking blood thinners.