英文药名: Inspra(Eplerenone tabs)
中文药名: 依普利酮片
生产厂家: Pfizer
药品简介
依普利酮(Eplerenone)是一种新型选择性醛固酮受体阻滞剂,与雄激素和黄体酮受体相互作用极小,本品半衰期较长,每日口服1次就可有效的控制高血压,减轻心、脑和肾等靶器官的损害,改善Ⅱ型糖尿病患者微量蛋白尿,而且其副作用发生率与安慰剂相似,耐受良好。依普利酮的面市,对于高血压患者控制高血压、预防与靶器官损害相关的心血管疾病、改善高血压患者的预后等方面均具有重要意义。
适应症
用于治疗高血压。用于提高急性心脏病发作后的充血性心力衰竭患者的生存率(2003年,美国FDA批准的依普利酮新的适应症)。
Generic Name for INSPRA
Eplerenone 25mg, 50mg; tabs.
Legal Classification:
Rx
Pharmacological Class for INSPRA
Aldosterone receptor blocker (mineralocorticoid-selective).
Manufacturer of INSPRA
Pfizer Inc.
Indications for INSPRA
Hypertension.
Other Indications for INSPRA
CHF and arrhythmias
Adult dose for INSPRA
Initially 50mg once daily; may increase after 4 weeks to max 50mg twice daily. Concomitant weak CYP3A4 inhibitors (eg, erythromycin, verapamil, saquinavir, fluconazole): initially 25mg once daily. Adjust based on serum K+ (see literature).
Children's dosing for INSPRA
Not recommended.
Contraindications for INSPRA
Hyperkalemia (serum K+ >5.5mEq/L) at initiation, severe renal impairment (CrCl ≤30mL/min), or concomitant potent CYP3A4 inhibitors (eg, ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir). Type 2 diabetes with microalbuminuria, CrCl<50mL/min, serum creatinine >2mg/dL (males), >1.8mg/dL (females), or concomitant K+ supplements or K+ sparing diuretics.
Warnings/Precautions for INSPRA
Severe hepatic impairment. Renal dysfunction. Monitor serum K+ at baseline, within 1st week, at 1 month after starting and after dose adjustment, then periodically. Elderly. Pregnancy (Cat.B). Nursing mothers: not recommended.
Interactions for INSPRA
CYP3A4 inhibitors (see Contraindications and Dose). NSAIDs may antagonize antihypertensive effects. Angiotensin II receptor blockers, ACEIs increase hyperkalemia risk. Monitor lithium.
Adverse Reactions for INSPRA
Hyperkalemia, dizziness, GI upset, abdominal pain, cough, flu-like symptoms, albuminuria; increased serum creatinine, triglycerides, cholesterol; decreased serum sodium; rare: sex hormone related effects, increased BUN, uric acid, liver enzymes.
How is INSPRA supplied?
Tabs—30, 90
セララ錠25mg/セララ錠50mg/セララ錠100mg
商標名
Selara Tablets
一般名
エプレレノン(Eplerenone)
化学名
9,11α-Epoxy-7α-(methoxycarbonyl)-3-oxo-17α-pregn-4-ene-21,17β-carbolactone
分子式
C24H30O6
分子量
414.49
構造式
性状
白色~黄白色の粉末である。アセトニトリル、ベンジルアルコール又はクロロホルムに溶けやすく、メタノールにやや溶けにくく、エタノール(99.5)に溶けにくく、水に極めて溶けにくい。
包装规格
セララ錠25mg:100錠(PTP)
セララ錠50mg:100錠(PTP)、700錠(PTP)、500錠(瓶)
セララ錠100mg:100錠(PTP
製造販売
ファイザー株式会社
完整处方资料附件:http://www.info.pmda.go.jp/go/pack/2149045F1029_2_01/