1. 作用机制 Mechanism of Action
中文:
他汀类药物通过抑制羟甲基戊二酰辅酶A(HMG-CoA)还原酶,减少肝脏内胆固醇的合成。
主要机制包括:
降低LDL-C(低密度脂蛋白胆固醇): 通过增加肝脏LDL受体的表达,显著清除循环中的LDL。
升高HDL-C(高密度脂蛋白胆固醇): 轻微提升,有益心血管保护。
降低甘油三酯(TG): 尤其是高TG血症患者效果明显。
English:
Statins inhibit HMG-CoA reductase, the rate-limiting enzyme in hepatic cholesterol biosynthesis.
Key mechanisms include:
LDL-C reduction: Increases hepatic LDL receptor expression, enhancing clearance of circulating LDL.
HDL-C elevation: Slight increase, contributing to cardiovascular protection.
Triglyceride (TG) reduction: Especially effective in patients with hypertriglyceridemia.
2. 适应症 Indications
中文:
原发性高胆固醇血症(如家族性高胆固醇血症)。
动脉粥样硬化性心血管疾病(ASCVD)的一级和二级预防。
混合型高脂血症。
缺血性卒中的长期预防。
English:
Primary hypercholesterolemia (e.g., familial hypercholesterolemia).
Primary and secondary prevention of atherosclerotic cardiovascular disease (ASCVD).
Mixed dyslipidemia.
Long-term prevention of ischemic stroke.
3. 常见药物及特点 Common Statins and Characteristics
药物名称 (Drug) | 剂量范围 (Dose, mg) | LDL-C 降低强度 (LDL-C Reduction) | 半衰期 (Half-Life) | 代谢 (Metabolism) |
---|---|---|---|---|
阿托伐他汀 (Atorvastatin) | 10-80 | 中高强度(30-50%) | 长(14小时) | CYP3A4 |
瑞舒伐他汀 (Rosuvastatin) | 5-40 | 高强度(40-60%) | 长(19小时) | 少量肝代谢 |
辛伐他汀 (Simvastatin) | 10-40 | 中强度(20-40%) | 短(2-3小时) | CYP3A4 |
普伐他汀 (Pravastatin) | 10-40 | 中强度(20-30%) | 短(2小时) | 肝外代谢 |
匹伐他汀 (Pitavastatin) | 1-4 | 中强度(25-40%) | 中(12小时) | CYP2C9 |
洛伐他汀 (Lovastatin) | 20-80 | 低中强度(20-30%) | 短(3小时) | CYP3A4 |
4. 常见副作用 Common Adverse Effects
中文:
肌肉不适(Myopathy): 包括肌痛、肌炎,严重者导致横纹肌溶解。
肝功能异常(Hepatotoxicity): 转氨酶升高,需定期监测肝功能。
糖尿病风险(Diabetes Risk): 可增加2型糖尿病的发生率,尤其在高剂量下。
胃肠道反应(GI Symptoms): 如恶心、腹痛。
English:
Myopathy: Includes myalgia, myositis, and in severe cases, rhabdomyolysis.
Hepatotoxicity: Elevations in transaminases; requires routine liver function monitoring.
Diabetes Risk: Associated with increased risk of type 2 diabetes, especially at high doses.
GI Symptoms: Nausea, abdominal discomfort.
5. 禁忌症和注意事项 Contraindications and Precautions
中文:
活动性肝病或不明原因的肝功能异常。
妊娠和哺乳期(对胎儿有潜在风险)。
与强CYP3A4抑制剂(如克拉霉素、酮康唑)慎用。
English:
Active liver disease or unexplained persistent liver enzyme elevation.
Pregnancy and lactation (potential fetal toxicity).
Caution with strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole).
6. 药物相互作用 Drug Interactions
中文:
与CYP3A4抑制剂(如环孢素、依曲韦林)合用可能增加肌肉毒性风险。
与圣约翰草、苯妥英钠等药物合用可能降低疗效。
English:
Co-administration with CYP3A4 inhibitors (e.g., cyclosporine, erythromycin) may increase the risk of myotoxicity.
Concurrent use with St. John's Wort or phenytoin may reduce statin efficacy.
7. 快速记忆技巧 Rapid Memorization Tips
中文记忆口诀:
“阿瑞辛普洛,匹异降脂酶;肝肌糖孕禁,护心防动脉。”
阿瑞辛普洛匹异:阿托伐他汀、瑞舒伐他汀、辛伐他汀、普伐他汀、洛伐他汀、匹伐他汀、异布他汀。
肝肌糖孕禁:肝损害、肌肉不适、糖代谢异常、孕期禁用。
护心防动脉:主要预防动脉粥样硬化及相关事件。
English Mnemonic:
“AR SPLoRE for Heart – Avoid Liver, Muscle, and Pregnancy Risks.”
A, R, S, P, L, P, R: Atorvastatin, Rosuvastatin, Simvastatin, Pravastatin, Lovastatin, Pitavastatin, and Rare (fluvastatin).
Liver, Muscle, Pregnancy Risks: Key contraindications include liver damage, muscle toxicity, and pregnancy.
请结合经典原文教材阅读!