降血脂 (statin) Primary hyperlipidemia or mixed dyslipidemia.
原發性高膽固醇血症及混合型血脂異常
藥理
Pitavastatin competitively inhibits HMG-CoA reductase, which is a rate-determining enzyme involved with biosynthesis of cholesterol, in a manner of competition with the substrate so that it inhibits cholesterol synthesis in the liver. As a result, the expression of LDL-receptors followed by the uptake of LDL from blood to liver is accelerated and then the plasma TC decreases.
藥動學
Bioavailability: 51%, plasma protein binding: 99%, primarily albumin and alpha 1-acid glycoprotein; the primary route of pitavastatin metabolism is glucuronidation via liver glucuronosyltransferases (UGT1A3 and UGT2B7); Elimination Half-life: 11-12 hrs.
禁忌症
Known hypersensitivity to product components; Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels; Women who are pregnant or may become pregnant; Nursing mothers; Co-administration with cyclosporine.
懷孕分類
X
哺乳分類
Contraindication
副作用
Myalgia, back pain, diarrhea, constipation, myasthenia gravis, and pain in extremity.
劑量和給藥方法
Initial, 2 mg ORALLY daily; MAX 4 mg daily; dosage range 1 to 4 mg daily; assess lipid levels 4 weeks after dose initiation or titration; taken with or without food, at any time of day.
小兒調整劑量
腎功能調整劑量
Dose adjustments according to GFR:
Moderate to severe renal impairment (GFR 15~59 mL/min/1.73 m2) as well as ESRD on H/D: Starting dose of 1 mg once daily and maximum dose of 2 mg once daily.