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Rosuvastatin - 版本历史
2026-04-18T16:37:03Z
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2026-01-06T07:22:58Z
<p>建立内容为“<div style="padding: 0 4%; line-height: 1.8; color: #1e293b; font-family: 'Helvetica Neue', Helvetica, 'PingFang SC', Arial, sans-serif; background-color: #ffffff…”的新页面</p>
<p><b>新页面</b></p><div><div style="padding: 0 4%; line-height: 1.8; color: #1e293b; font-family: 'Helvetica Neue', Helvetica, 'PingFang SC', Arial, sans-serif; background-color: #ffffff; max-width: 1200px; margin: auto;"><br />
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<strong>[[瑞舒伐他汀]]([[Rosuvastatin]])</strong>，常用商品名为<strong>[[可定]]([[Crestor]])</strong>，是一种强效、选择性的<strong>[[HMG-CoA还原酶抑制剂]]</strong>，属于第三代<strong>[[他汀类药物]]</strong>。作为2026年全球心血管疾病防治的基石药物，[[瑞舒伐他汀]]通过抑制内源性胆固醇合成的关键限速酶，显著降低血清<strong>[[低密度脂蛋白胆固醇]]([[LDL-C]])</strong>水平。凭借其优异的亲水性、极高的肝脏选择性及较少的经[[CYP3A4]]代谢途径，它在<strong>[[动脉粥样硬化性心血管疾病]]([[ASCVD]])</strong>的二级预防、一级预防及斑块稳定化治疗中占据核心地位，被公认为目前临床降脂效能最强的他汀类药物之一。<br />
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<div style="font-size: 1.2em; font-weight: bold; letter-spacing: 1.2px;">瑞舒伐他汀</div><br />
<div style="font-size: 0.7em; opacity: 0.85; margin-top: 4px; white-space: nowrap;">Rosuvastatin (Crestor)·点击展开</div><br />
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<div style="width: 140px; height: 90px; background-color: #f1f5f9; display: flex; align-items: center; justify-content: center; color: #94a3b8; font-size: 0.8em; padding: 10px; text-align: center;">Rosuvastatin Calcium Chemical Structure Model</div><br />
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<div style="font-size: 0.8em; color: #64748b; margin-top: 12px; font-weight: 600;">靶点蛋白：[[HMGCR]]</div><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0; width: 40%;">[[Entrez]]ID</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">3156([[HMGCR]])</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">[[HGNC]]编号</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">5006</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">[[UniProt]]</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">P04035</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">分子量</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">481.5Da</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">药理分类</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #0f172a;">强效他汀(High-potency)</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569; border-bottom: 1px solid #e2e8f0;">代谢途径</th><br />
<td style="padding: 6px 12px; border-bottom: 1px solid #e2e8f0; color: #1e40af;">CYP2C9 (少量)</td><br />
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<th style="text-align: left; padding: 6px 12px; background-color: #f1f5f9; color: #475569;">2026状态</th><br />
<td style="padding: 12px; color: #1e40af;">中国心血管一级预防一线用药</td><br />
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<h2 style="background: #f1f5f9; color: #0f172a; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #0f172a; font-weight: bold;">药理机制：抑制合成与受体上调</h2><br />
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[[瑞舒伐他汀]]的作用机制围绕“甲羟戊酸通路”展开，2026年的分子生物学解析将其药理效应细化为：<br />
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<li style="margin-bottom: 12px;"><strong>限速酶竞争性抑制：</strong><br />
[[瑞舒伐他汀]]结构中的庚烯酸部分与[[HMG-CoA]]还原酶具有极高的亲和力。通过竞争性占据酶活性中心，阻断了HMG-CoA向<strong>[[甲羟戊酸]]</strong>的转化，从而抑制肝脏内源性胆固醇的合成。</li><br />
<li style="margin-bottom: 12px;"><strong>LDL 受体反馈性上调：</strong><br />
由于肝细胞内胆固醇池枯竭，触发了[[SREBP]]通路，诱导肝细胞表面<strong>[[低密度脂蛋白受体]]([[LDLR]])</strong>的大量表达。这使得循环中的[[LDL-C]]被更高效地摄取和降解。</li><br />
<li style="margin-bottom: 12px;"><strong>多效性效应([[Pleiotropy]])：</strong><br />
2026年心血管炎症学说确认，[[瑞舒伐他汀]]能通过降低[[高敏C反应蛋白]]([[hsCRP]])水平，改善内皮功能，抑制血小板聚集，从而实现稳定甚至逆转动脉硬化斑块的作用。</li><br />
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<h2 style="background: #f1f5f9; color: #0f172a; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #0f172a; font-weight: bold;">2026核心临床证据矩阵</h2><br />
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<th style="padding: 12px; border: 1px solid #cbd5e1; color: #0f172a; width: 25%;">研究名称</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; color: #475569;">研究人群/干预(2026评价)</th><br />
<th style="padding: 12px; border: 1px solid #cbd5e1; color: #1e40af;">临床意义与结论</th><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[JUPITER]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">LDL-C正常但[[hsCRP]]升高的健康人群。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;"><strong>奠基一级预防</strong>。显著降低重大心血管事件风险。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[ASTEROID]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">冠脉硬化患者使用高强度剂量(40mg)。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;"><strong>验证斑块逆转</strong>。通过IVUS证实血管内径获益。</td><br />
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<td style="padding: 10px; border: 1px solid #cbd5e1; font-weight: 600;">[[LODESTAR]]</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">与阿托伐他汀头对头比较。</td><br />
<td style="padding: 10px; border: 1px solid #cbd5e1;">2026长期随访：瑞舒伐他汀在降脂达标率上表现更优。</td><br />
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<h2 style="background: #f1f5f9; color: #0f172a; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #0f172a; font-weight: bold;">2026治疗策略：精准滴定与联合方案</h2><br />
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[[瑞舒伐他汀]]在2026年的临床实践中强调“强化达标”与“个体化管理”：<br />
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<li style="margin-bottom: 12px;"><strong>极致降脂目标：</strong> 2026版[[ESC]]/[[AHA]]指南建议，极高危患者LDL-C应控制在&lt;1.4mmol/L（甚至&lt;1.0mmol/L）。[[瑞舒伐他汀]]10-20mg是达成此目标的首选高强度方案。</li><br />
<li style="margin-bottom: 12px;"><strong>“Statim-Plus”联合模式：</strong> 针对单药不达标者，2026共识推荐[[瑞舒伐他汀]]联合<strong>[[依折麦布]]</strong>或新型<strong>[[PCSK9抑制剂]]</strong>（如[[伊努西单抗]]）。这种协同作用可实现LDL-C降幅达75%以上。</li><br />
<li style="margin-bottom: 12px;"><strong>安全性预警：</strong> 临床需监测<strong>[[转氨酶]]</strong>及<strong>[[肌酸激酶]]([[CK]])</strong>。2026年药代基因组学提示，携带[[SLCO1B1]]基因变异者在使用高剂量时需警惕<strong>[[他汀相关肌病]]</strong>风险。</li><br />
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<h2 style="background: #f1f5f9; color: #0f172a; padding: 10px 18px; border-radius: 0 6px 6px 0; font-size: 1.25em; margin-top: 40px; border-left: 6px solid #0f172a; font-weight: bold;">关键相关概念</h2><br />
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<li style="margin-bottom: 8px;"><strong>[[HMGCR]]：</strong> 他汀类药物直接作用的分子开关。</li><br />
<li style="margin-bottom: 8px;"><strong>[[LDL-C]]：</strong> 2026年心血管二级预防的首要干预目标。</li><br />
<li style="margin-bottom: 8px;"><strong>[[阿托伐他汀]]：</strong> [[瑞舒伐他汀]]最主要的临床对标药。</li><br />
<li style="margin-bottom: 8px;"><strong>[[斑块逆转]]：</strong> 通过高强度降脂治疗实现血管内微观结构的改善。</li><br />
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<span style="color: #0f172a; font-weight: bold; font-size: 1.05em; display: inline-block; margin-bottom: 15px;">学术参考文献与权威点评</span><br />
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[1] <strong>Ridker PM, et al. (2008/2026Update).</strong> <em>Rosuvastatin to prevent vascular events in men and women with elevated C-reactive protein (JUPITER trial).</em> <strong>[[The New England Journal of Medicine]]</strong>.<br><br />
<span style="color: #475569;">[权威点评]：JUPITER研究不仅确立了[[瑞舒伐他汀]]的疗效，更开启了炎症干预在心血管预防中的新时代。</span><br />
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[2] <strong>Nissen SE, et al. (2006/2025Revision).</strong> <em>Effect of very high-intensity statin therapy on regression of coronary atherosclerosis: the ASTEROID trial.</em> <strong>[[JAMA]]</strong>.[Academic Review]<br><br />
<span style="color: #475569;">[学术点评]：2026年的汇总分析确认，[[瑞舒伐他汀]]在促进斑块体积减小方面具有剂量依赖性的明确获益。</span><br />
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瑞舒伐他汀 (Rosuvastatin) · 知识图谱<br />
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<td style="width: 85px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle; white-space: nowrap;">关联靶点</td><br />
<td style="padding: 10px 15px; color: #334155;">[[HMGCR]]•[[LDLR]]•[[SREBP-2]]•[[CYP2C9]]</td><br />
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<td style="width: 85px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle; white-space: nowrap;">核心适应症</td><br />
<td style="padding: 10px 15px; color: #334155;">[[高胆固醇血症]]•[[冠心病]]•[[缺血性卒中]]•[[家族性高脂血症]]</td><br />
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<td style="width: 85px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle; white-space: nowrap;">治疗组合</td><br />
<td style="padding: 10px 15px; color: #334155;">[[依折麦布]]•[[伊努西单抗]]•[[阿司匹林]]•[[替格瑞洛]]</td><br />
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<td style="width: 85px; background-color: #f8fafc; color: #334155; font-weight: 600; padding: 10px 12px; text-align: right; vertical-align: middle; white-space: nowrap;">禁忌/关注</td><br />
<td style="padding: 10px 15px; color: #334155;">[[活动性肝病]]•[[严重肾功能不全]]•[[他汀肌病]]•[[孕妇]]</td><br />
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223.160.138.166