制造商：
科瓦和莉莉
药理分类：
HMG - CoA还原酶抑制剂
活性成分（补）：
匹伐他汀1毫克，2毫克，4毫克;标签。
指示（补）：
配合饮食：为了降低升高的总- C中，低密度脂蛋白胆固醇，载脂蛋白B和甘油三酯，并提高原发性高脂血症和混合性高血脂高密度脂蛋白胆固醇。
药理作用：
匹伐他汀竞争性地抑制HMG - CoA还原酶，这种酶能够控制内源性胆固醇的合成速率。在肝摄取低密度脂蛋白的血液和血浆中总胆固醇降低这个结果。此外，抑制胆固醇的合成降低极低密度脂蛋白（VLDL的）的水平。
临床试验：
一个剂量范围研究匹伐他汀疗效比较（1，2，每日4毫克）251例原发性高脂血症患者服用安慰剂。在12个星期，匹伐他汀显着降低血浆LDL - C水平，TC，TG和ApoB水平较安慰剂。在HDL - C增加横渡剂量范围变量。
匹伐他汀进行了比较，在一宗涉及817例原发性高脂血症或多于12星期混合性高血脂患者的研究阿托伐他汀。匹伐他汀2毫克和4mg是不逊于阿托伐他汀10毫克和20毫克，分别为中低密度脂蛋白胆固醇的平均百分比变化。
匹伐他汀是比较辛伐他汀对843例原发性高脂血症或超过12周，混合性高血脂的病人。匹伐他汀2毫克和4mg是不逊于辛伐他汀20毫克和40毫克，分别为中低密度脂蛋白胆固醇的平均百分比变化。
在为期12周的平行组研究中，匹伐他汀进行了比较，在942例原发性高脂血症或混合性高血脂老年患者普伐他汀。匹伐他汀一，二，4mg/day显着降低LDL - C水平相比，普伐他汀10，20和40mg/day分别。
在为期12周，涉及351≥2冠心病和高脂血症或混合性高血脂的主要危险因素的患者的研究中，匹伐他汀4mg的被证明是不逊于在LDL - C的平均百分比变化辛伐他汀40毫克。
匹伐他汀4mg的是比较在一个涉及410例2型糖尿病合并血脂异常患者的研究和阿托伐他汀20毫克。两个治疗组没有统计学差异对于LDL - C水平，但不自卑不适合匹伐他汀成立。
法律分类：
接收
成人：
最初2毫克，每天一次，4周后可能会增加至最大4毫克，每日一次。中度肾功能损害（肌酐清除率30至<60mL/min，或终末期肾病血液透析）：1毫克，每日一次，最大2毫克，每天一次。伴随红霉素：最大1毫克每天。伴随利福平：最大2毫克每天。
儿童：
不推荐。
禁忌（补）：
活动性肝病。原因不明的，持续的血清转氨酶升高。严重肾功能损害（肌酐清除率<30mL/min无透析）。伴随环孢素或洛匹那韦/利托那韦。妊娠（部件十）。哺乳的母亲。
警告/注意事项：
肌病的危险因素（如肾功能不全，甲状腺功能不足治疗，年龄> 65岁，伴随贝特类药物，降脂修改烟酸）。监测肝功能（治疗前，12周后开始或增加剂量，然后定期）：降低剂量或停止，如果血清转氨酶水平≥3xULN坚持。摄入大量酒精。如果停止或肌病发生CK水平明显升高;暂停，如果发展到肾功能衰竭继发横纹肌溶解症倾向的发展（如败血症，低血压，脱水，外伤，癫痫，严重的内分泌，代谢或电解质紊乱）。
互动（补）：
Potentiated环孢素，可能洛匹那韦/利托那韦（见禁忌）。贝特类，烟酸增加肌病的风险（考虑减少剂量匹伐他汀）。红霉素，利福平Potentiated（见成人剂量）。监测华法林。
不良反应（补）：
肌肉疼痛，背部/下肢疼痛，胃肠不适，便秘，肌酸磷酸激酶升高，转氨酶，碱性磷酸酶，胆红素，葡萄糖，肌肉病变，肾功能不全，过敏反应横纹肌溶解症。
如何提供：
制表- 90
最后更新：
2010年6月24日
Manufacturer:
Kowa and Lilly
Pharmacological Class:
HMG-CoA reductase inhibitor
Active Ingredient(s):
Pitavastatin 1mg, 2mg, 4mg; tabs.
Indication(s):
Adjunct to diet: To reduce elevated total-C, LDL-C, ApoB, and TG, and to increase HDL-C in primary hyperlipidemia and mixed dyslipidemia.
Pharmacology:
Pitavastatin competitively inhibits HMG-CoA reductase, an enzyme that controls the rate of endogenous cholesterol synthesis. This results in the hepatic uptake of LDL from the blood and a decrease in plasma total cholesterol. Also, the inhibition of cholesterol biosynthesis reduces the levels of very low density lipoproteins (VLDL).
Clinical Trials:
A dose-ranging study compared the efficacy of pitavastatin (1, 2, and 4mg per day) to placebo in 251 patients with primary hyperlipidemia. At 12 weeks, pitavastatin significantly reduced plasma LDL-C, TC, TG and ApoB compared to placebo. Increases in HDL-C were variable across the dosage range.
Pitavastatin was compared to atorvastatin in a study involving 817 patients with primary hyperlipidemia or mixed dyslipidemia over 12 weeks. Pitavastatin 2mg and 4mg was non-inferior to atorvastatin 10mg and 20mg, respectively, for mean percent change in LDL-C.
Pitavastatin was compared to simvastatin in 843 patients with primary hyperlipidemia or mixed dyslipidemia over 12 weeks. Pitavastatin 2mg and 4mg was non-inferior to simvastatin 20mg and 40mg, respectively, for mean percent change in LDL-C.
In a 12-week parallel-group study, pitavastatin was compared to pravastatin in 942 elderly patients with primary hyperlipidemia or mixed dyslipidemia. Pitavastatin 1, 2, and 4mg/day significantly reduced LDL-C compared to pravastatin 10, 20, and 40mg/day, respectively.
In a 12-week study involving 351 patients with ≥2 risk factors for coronary heart disease and primary hyperlipidemia or mixed dyslipidemia, pitavastatin 4mg was shown to be non-inferior to simvastatin 40mg for mean percent change in LDL-C.
Pitavastatin 4mg was compared to atorvastatin 20mg in a study involving 410 patients with type 2 diabetes and combined dyslipidemia. The two treatment groups were not statistically different regarding LDL-C, but non-inferiority was not established for pitavastatin.
Legal Classification:
Rx
Adults:
Initially 2mg once daily; may increase after 4 weeks to max 4mg once daily. Moderate renal impairment (CrCl 30 to <60mL/min, or ESRD with hemodialysis): 1mg once daily; max 2mg once daily. Concomitant erythromycin: max 1mg daily. Concomitant rifampin: max 2mg daily.
Children:
Not recommended.
Contraindication(s):
Active liver disease. Unexplained, persistent elevated serum transaminases. Severe renal impairment (CrCl <30mL/min without dialysis). Concomitant cyclosporine or lopinavir/ritonavir. Pregnancy (Cat. X). Nursing mothers.
Warnings/Precautions:
Risk factors for myopathy (eg, renal impairment, inadequately treated hypothyroidism, age >65 years, concomitant fibrates, lipid-modifying niacin). Monitor liver function (before therapy, at 12 weeks after starting or dose increase, then periodically): reduce dose or discontinue if serum transaminase levels ≥3xULN persist. Substantial alcohol ingestion. Discontinue if myopathy or markedly elevated CK levels occur; suspend if a predisposition to development of renal failure secondary to rhabdomyolysis develops (eg, sepsis, hypotension, dehydration, trauma, seizures; severe endocrine, metabolic, or electrolyte disorders).
Interaction(s):
Potentiated by cyclosporine, possibly lopinavir/ritonavir (see Contraindications). Fibrates, niacin increase myopathy risk (consider reducing pitavastatin dose). Potentiated by erythromycin, rifampin (see Adult dose). Monitor warfarin.
Adverse Reaction(s):
Myalgia, back/extremity pain, GI upset, constipation, elevated creatine phosphokinase, transaminases, alkaline phosphatase, bilirubin, glucose; myopathy, rhabdomyolysis with renal dysfunction, hypersensitivity reactions.
How Supplied:
Tabs—90