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盐酸利哌酸盐水合物
治疗类别名称
Rho激酶抑制剂
青光眼和高眼压症的治疗剂
批准上市日期：2014年12月
商標名
GLANATEC ophthalmic solution 0.4％
一般名 
リパスジル塩酸塩水和物（Ripasudil Hydrochloride Hydrate） 
化学名 
4-Fluoro-5-｛［（2S）-2-methyl-1,4-diazepan-1-yl］sulfonyl｝isoquinoline monohydrochloride dihydrate 
構造式

 

分子式 
C15H18FN3O2S・HCl・2H2O 
分子量 
395.88 
融点 
約255℃（分解） 
性状 
这是至淡黄色粉末白色。易溶于二甲基亚砜，微溶于水，乙醇（99.5）微溶。
分配系数（log P）
-2.33（PH2）， - 2.13（在pH4）， - 1.25（pH为6）， - 0.155（pH8的），0.812（pH为10），1.16（pH12的）
[1辛醇/ BR缓冲（25±1℃）]
薬効薬理
1. 眼圧下降作用
该Ripasujiru盐酸盐水合物滴眼液0.0625至0.5％，兔，当一个从0.1到猴的0.4％施用单一滴注，观察到浓度依赖性眼压效果。
2. 作用机序
降眼压Ripasujiru的效果的机制的基础上，激酶抑制作用 - 房水外流促进从穿过施累姆氏管的主要流动路径已经建议。
(1)Ripasujiru表明对人ROCK-1和ROCK-2同种型的Rho激酶（体外）的选择性抑制作用。
(2)当这种药物滴注单家兔房水的流出率显著增加相比，在给药组。
(3)当该试剂滴入单兔，并没有影响到葡萄膜巩膜流和水的生产量。
适应症：
青光眼，高眼压症
用法与用量
每日两次，一次1滴
包装规格
滴眼液0.4％
5毫升×5瓶
5毫升×10瓶
5毫升×30瓶

Description

This medicine inhibits Rho kinase and promotes drainage of aqueous humor from main outflow. It consequently decreases intraocular pressure.
It is usually used to treat glaucoma and ocular hypertension when other medicines for glaucoma have insufficient effect or can not be used.

Presentation

5mL

Feature

colorless to pale yellow limpid ophthalmic solution,
(bottle) clear and colorless, (cap) deep green

Active Ingredients

Ripasudil hydrochloride hydrate

Effect/Efficacy

This medicine inhibits Rho kinase and promotes drainage of aqueous humor from main outflow. It consequently decreases intraocular pressure.
It is usually used to treat glaucoma and ocular hypertension when other medicines for glaucoma have insufficient effect or can not be used.

Usage/Dosage

In general, apply 1 drop at a time, twice a day. Strictly follow the instructions.
Apply the medicine so as not to touch the eye directly with the eyedropper tip.
If you need to use other eye drops at the same time, wait more than 5 minutes.
Avoid applying the medicine when you are wearing soft contact lens.
If you miss a dose, apply the missed dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. You should never apply two doses at one time.
If you accidentally apply more than your prescribed dose, consult with your doctor or pharmacist.
Do not stop applying this medicine unless your doctor instructs you to do so.

Cautions

The most commonly reported adverse reactions include conjunctival congestion, conjunctival inflammation, blepharitis and eye irritation. If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
No pertinent entries.
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.

Contraindication

The most commonly reported adverse reactions include conjunctival congestion, conjunctival inflammation, blepharitis and eye irritation. If any of these symptoms occur, consult with your doctor or pharmacist.