部份中文GLANATEC处方资料(仅供参考)
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
制造商
興和株式会社
完整处方资料附件:
1):http://www.info.pmda.go.jp/go/pack/1319763Q1022_1_05/
2)http://www.120ty.net/bencandy.php?fid=141&aid=27888
青光眼的最强治疗药—GLANATEC ophthalmic solution 0.4%(Ripasudil盐酸盐)
Ripasudil盐酸水合物(Glanatec)是由Kowa Company(兴和株式会社)研发的一种小分子Rho激酶抑制剂药物,用以治疗青光眼和高眼压症。这种药物直接作用于小梁网、增加Schlemm管的外流来达到降低眼压的作用。在这种作用机制下,Repasudil在与其他抗青光眼药物(比如可以增加葡萄膜巩膜外流的前列腺素类似物、以及可以减少房水生成的β受体阻断剂)联合应用的情况下,可进一步增强降眼压的效果。
GLANATEC ophthalmic solution 0.4%
And about, has acquired the manufacturing and marketing approval from the Ministry of Health, Labour and Welfare in date September 26: Kowa Co., Ltd., is a new glaucoma and ocular hypertension treatment "(Ripasujiru hydrochloride hydrate generic name) Guranatekku ® ophthalmic solution 0.4%..
Guranatekku ® ophthalmic solution 0.4%" is a glaucoma and ocular hypertension therapeutic agents which have the world's first mechanism of action, Rho kinase: by inhibiting the (ROCK Rho-associated, coiled-coil containing protein kinase), and fibers meshwork - through the Schlemm's canal and to lower the intraocular pressure by promoting aqueous outflow from the main outlet channel.
There is also the fact that a new mechanism of action of the drug, it is hoped to be a new option for patients that were not sufficient effect is obtained with existing glaucoma treatment.
Brand name : GLANATEC ophthalmic solution 0.4%
Active ingredient: Ripasudil hydrochloride hydrate
Dosage form: colorless to pale yellow limpid ophthalmic solution, (bottle) clear and colorless, (cap) deep green
Print on wrapping:
Effects of this medicine
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.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
•If you are pregnant or breastfeeding.
•If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)
Dosing schedule (How to take this medicine)
•Your dosing schedule prescribed by your doctor is (( to be written by a healthcare professional))
•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.
Precautions while taking this medicine
• Possible adverse reactions to this medicine
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.
Storage conditions and other information
•Keep out of the reach of children. Store away from direct sunlight, heat and moisture.
•Discard the remainder. Do not store them.
Kowa Co., Ltd.External
Published: 11/2014
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.