Pharmacology
Summary
PCSK9 inhibitors, such as alirocumab and evolocumab, are drugs most commonly used as 2nd and 3rd line adjunctive agents in the management of hypercholesterolemia. These monoclonal antibodies act by neutralizing the PCSK9 protein, a critical regulator of LDL receptors on hepatocytes. When PCSK9 function is inhibited, the density of LDL receptors on hepatocytes increases, leading to increased clearance of circulating LDL cholesterol. PCSK9 inhibitors are essential for secondary prevention in high-risk patients, especially those who haven't achieved cholesterol targets with maximal statin therapy. Their efficacy is highlighted in conditions like familial hypercholesterolemia. Adverse effects of PCSK9 inhibitors include injection site reactions and respiratory side effects such as nasopharyngitis, influenza, and URTIs.
Lesson Outline
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FAQs
PCSK9 inhibitors, as therapeutic monoclonal antibodies, specifically target and neutralize the PCSK9 protein. PCSK9 is known to degrade LDL receptors on hepatocytes. By counteracting PCSK9, these medications increase LDL receptor density on hepatocytes, increasing the clearance of circulating LDL cholesterol and effectively reducing serum cholesterol.
Alirocumab and evolocumab are often prescribe for hypercholesterolemia, and are recommended as 2nd or 3rd line add-on therapy for secondary prevention for patients who have not met their cholesterol goals despite maximal statin therapy Their notable efficacy is observed in cases of familial hypercholesterolemia, as well as in patients with atherosclerotic cardiovascular disease not adequately controlled with statins.
PCSK9 inhibitors stand out in cardiovascular management due to their potent LDL cholesterol-reducing effect. Elevated LDL cholesterol contributes to atherosclerotic plaque buildup, a precursor to major cardiovascular events such as heart attacks and strokes. By enhancing LDL cholesterol clearance, PCSK9 inhibitors substantially diminish associated cardiovascular risks.
While PCSK9 inhibitors are generally well-tolerated, they are not devoid of side effects. Since they are delivered subcutaneously, patients may experience injection site reactions, marked by redness, itchiness, or swelling. Systemic effects can include respiratory symptoms such as nasopharyngitis, influence, and URTIs..
PCSK9 inhibitors are administered subcutaneously. The dosing frequency varies by the specific agent and patient condition. For instance, Evolocumab can be given either every two weeks or monthly, while Alirocumab is typically a biweekly administration. Always adhere to a clinician's guidance on dosing regimen.
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