中文药名: 奈必洛尔片

英文药名: Bystolic (Nebivolol Tablets)

介绍

奈比洛尔为β-阻段剂系列高血压治疗药物的新成员。12月17日，FDA宣布批准抗高血压新药奈比洛尔(nebivolol，Bystolic)上市。奈比洛尔为β-阻段剂系列高血压治疗药物的新成员。在美国，成年人高血压发病率约为1/3。高血压平时没有特别症状，但可导致中风、心衰、心脏病发作、肾衰竭甚至死亡的风险，因此常被称作隐行杀手。奈比洛尔为患者控制血压提供了新选择。
适应症
具有血管扩张活性的选择性β1肾上腺素受体拮抗剂，无内源性产感神经活性。用于轻至中度高血压病人的治疗，亦可用于心绞痛和充血性心力衰竭的治疗。
规格
片剂，2.5mg; 5mg/片。
用法用量
一日一次，一次一片，肝肾功能不全及老年人可适当减量。
任何疑问，请遵医嘱！
不良反应

本品不良反应较少，最常见的有头痛、眩晕、乏力、感觉异常、便秘、腹泻等。这些不良反应通常是一过性的，很少因此而停药。本品不引起体位性低血压，很少诱发心衰或引起严重缓慢性心律失常。
 
原产地英文商品名:
BYSTOLIC 2.5mg/tablet 30tablets/box
原产地英文药品名:
NEBIVOLOL HCL
中文参考商品译名:
BYSTOLIC 2.5毫克/片 30片/盒
中文参考药品译名:
盐酸奈必洛尔

BYSTOLIC

Indication(s):

Hypertension, alone or with other antihypertensives.

Pharmacology:

Nebivolol is a once-daily β-adrenergic blocking agent that, at doses up to 10mg, is primarily β₁-selective. In poor metabolizers (those with reduced activity of CYP2D6) and at higher doses, however, it may inhibit β₂ adrenergic receptors as well. β₂ blockade may lead to bronchoconstrictive effects. Nebivolol does not have intrinsic sympathomimetic effects or membrane stabilizing activity at therapeutic doses. It has several active metabolites which are the product of glucuronidation and hydroxylation by the oxidative enzyme CYP2D6.

Clinical Trials:

Three double-blind, placebo-controlled, 12-week studies were conducted to demonstrate the effectiveness of nebivolol as monotherapy in the treatment of hypertension. Two of these trials studied 1716 patients in the general hypertensive population (26% non-Caucasian) and a third studied 300 Black (African-American) patients. Another study, which enrolled 669 patients, evaluated the effect of adding nebivolol to a background anti-hypertensive regimen of up to two other agents, including ACEIs, ARBs, and thiazide diuretics. In each study, nebivolol was shown to be effective in lowering both systolic and diastolic BP. Effectiveness was established in Black patients, but as monotherapy the magnitude of effect was somewhat less than in Caucasians. The BP-lowering effect was seen at 2 weeks after starting therapy and was maintained over the 24-hour dosing interval.

Legal Classification:

Rx

Adults:

≥18yrs: initially 5mg once daily. Individualize; may increase at 2-week intervals; max 40mg/day. Severe renal or moderate hepatic impairment: initially 2.5mg once daily.

Children:

<18yrs: not recommended.

Contraindication(s):

Severe hepatic impairment (Child-Pugh >B). Severe bradycardia. 2nd- or 3rd degree AV block. Cardiogenic shock. Overt heart failure. Sick sinus syndrome (unless paced).

Warnings/Precautions:

CHF. Angina. Recent MI. Bronchospastic disease. Diabetes. Hyperthyroidism. Severe renal impairment. Moderate hepatic impairment. Avoid abrupt cessation (taper over 1–2 weeks). Surgery. Peripheral vascular disease. Pheochromocytoma. Pregnancy (Cat.C). Nursing mothers: not recommended.

Interaction(s):

Caution with phenylalkylamine and benzothiazepine calcium channel blockers (eg, verapamil, diltiazem), antiarrhythmics (eg disopyramide), digoxin, reserpine, guanethidine; monitor. May be potentiated by CYP2D6 inhibitors (eg, quinidine, propafenone, paroxetine, fluoxetine); may need to reduce dose. If on both nebivolol and clonidine, discontinue nebivolol before tapering clonidine. May block epinephrine.

Adverse Reaction(s):

Headache, fatigue, dizziness, GI upset.

How Supplied:

Tabs—30, 100

FDA未批准Bystolic治疗慢性心衰竭

Forest Labs宣布，美国FDA并未批准Bystolic(R) (nebivolol)治疗慢性心衰竭(CHF)。
奈比洛尔为β-阻段剂系列高血压治疗药物的新成员。12月17日，FDA宣布批准抗高血压新药奈比洛尔(nebivolol，Bystolic)上市。奈比洛尔为β-阻段剂系列高血压治疗药物的新成员。 在美国，成年人高血压发病率约为1/3。高血压平时没有特别症状，但可导致中风、心衰、心脏病发作、肾衰竭甚至死亡的风险，因此常被称作隐行杀手。奈比洛尔为患者控制血压提供了新选择。

3项持续3个月以上的随机双盲多中心安慰剂对照的临床研究评价了奈比洛尔的疗效和安全性。 第4项安慰剂对照研究中，服用其它2种降压药物后降压效果不充分的患者，再接受本品治疗，达到了良好的效果。4项临床研究中总共超过2000例患者服用奈比洛尔，其药效与同类β-阻段剂药物的药效相当。 临床研究中，奈比洛尔最常见不良反应为头疼、疲劳、头晕和腹泻。
Bystolic由北卡罗莱纳州的Mylan Bertek制药公司开发，纽约Forest Laboratories公司负责奈比洛尔的销售