Cholesterol-lowering medications are a key therapeutic approach to regulate lipid metabolism in the blood, primarily targeting low-density lipoprotein cholesterol (LDL-C, commonly known as "bad cholesterol"). These drugs reduce blood cholesterol levels through various mechanisms to decrease the risk of atherosclerosis, myocardial infarction, and stroke. Treatment goals are usually set based on individual patient risk factors (such as age, family history, diabetes, etc.) with specific LDL-C target values, combined with lifestyle modifications for optimal results.
Currently, there are five main categories of cholesterol-lowering drugs: statins, ezetimibe, PCSK9 inhibitors, niacin, and bile acid sequestrants. Statins are the most common, working by inhibiting HMG-CoA reductase in the liver to suppress cholesterol synthesis; ezetimibe inhibits intestinal cholesterol absorption. PCSK9 inhibitors are monoclonal antibodies that enhance LDL receptor availability to promote cholesterol clearance. Different mechanisms can be combined to enhance lipid-lowering effects.
Suitable for primary hypercholesterolemia (such as familial hypercholesterolemia) and secondary hypercholesterolemia (caused by hypothyroidism, kidney disease, etc.). Common scenarios include patients at high risk for cardiovascular disease, those with a history of myocardial infarction or stroke, and patients with high cholesterol unmanageable by diet alone. Some drugs, like PCSK9 inhibitors, are approved for severe familial hypercholesterolemia.
Most statins are oral capsules or tablets taken once daily, with some requiring administration in the evening to enhance efficacy. Ezetimibe is taken once daily orally, while PCSK9 inhibitors are administered via subcutaneous injection every two weeks or monthly. Dosages are adjusted based on patient age and liver/kidney function; for example, statins are contraindicated in severe liver impairment. Physicians regularly monitor blood lipid levels to adjust treatment plans.
Statins may cause muscle discomfort (such as myalgia, elevated creatine phosphokinase), and in severe cases, rhabdomyolysis. Close monitoring of liver function and muscle symptoms is essential. Ezetimibe may cause gastrointestinal discomfort; PCSK9 inhibitors might lead to injection site redness or swelling. Some patients using niacin may experience flushing or hyperglycemia. Long-term statin use may affect liver enzymes, requiring periodic testing.
Contraindications include active liver disease, pregnancy, and breastfeeding (which may affect the fetus or infant). Patients on statins should avoid grapefruit juice (which can increase drug levels). Those with a history of muscle disease or severe liver dysfunction should not use statins. Baseline liver function and creatine kinase tests are necessary before starting therapy, with follow-up every 3-6 months to monitor blood lipids and liver function.
Statins may interact with certain antibiotics (e.g., erythromycin), antifungal agents (e.g., ketoconazole), potentially increasing muscle toxicity risk. Combining with warfarin may enhance anticoagulant effects. Patients on cyclosporine post-renal transplant should avoid high doses of statins. When using PCSK9 inhibitors, inform your doctor if you are on immunosuppressants or anticoagulants.
Multiple large clinical trials (such as IMPROVE-IT, FOURIER) show that combining statins with ezetimibe can further reduce cardiovascular risk by 10%. PCSK9 inhibitors demonstrated LDL-C reductions of up to 60% in the ODYSSEY trial. Therapeutic effects are usually seen within 4-12 weeks, with ongoing monitoring of non-HDL cholesterol and apolipoprotein B levels.
Non-pharmacological treatments include the Mediterranean diet (low saturated fat, high fiber), regular aerobic exercise, and weight management. Other drug options include omega-3 fatty acid supplements (for high triglycerides) and fibrates (for hyperlipidemia). When oral medications are unsuitable, subcutaneous PCSK9 inhibitors or intestinal cholesterol absorption inhibitors can be considered. Patients should work with their physicians to evaluate drug tolerability and lifestyle modifications to choose the most appropriate plan.
It is recommended to take medications at a fixed time to maintain stable drug levels, such as taking statins after dinner to reduce gastrointestinal discomfort. A low-fat, high-fiber diet should be followed, avoiding high-cholesterol foods (such as organ meats and fried foods), and increasing intake of deep-sea fish and nuts to enhance treatment effectiveness.
Could muscle soreness be related to cholesterol-lowering drugs?Yes, statins can occasionally cause muscle pain or weakness, and in severe cases, elevated creatine kinase levels. If symptoms persist or worsen, stop the medication immediately and consult your doctor. Dose adjustments or switching to other drugs (such as PCSK9 inhibitors) may be necessary, with regular monitoring of creatine kinase levels.
Is regular liver function testing necessary during treatment?Yes, some medications may affect liver function, especially during initial treatment. Liver enzymes (ALT/AST) should be checked every 3-6 months initially. If abnormal, medication should be paused and evaluated. Even with normal results, ongoing monitoring is recommended to prevent long-term liver burden.
What interactions should I be aware of when combining with other medications?Certain antibiotics (e.g., macrolides), immunosuppressants (e.g., cyclosporine), or antifungal drugs may increase statin blood levels, raising the risk of muscle or liver issues. Always inform your healthcare provider of all medications and supplements you are taking, including herbal products, to adjust dosages if necessary.
If my cholesterol levels are within target, can I reduce the medication dosage on my own?No, do not adjust the dosage yourself. Even if cholesterol levels are controlled, continued medication is necessary to maintain arterial health. Sudden reduction may cause rebound increases and elevate cardiovascular risk. Any dosage changes should be evaluated and approved by your healthcare provider, with ongoing lipid monitoring and risk assessment.
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