英文药名：INHIBACE Tablet（Cilazapril hydrate）

中文药名：西拉普利水合物

生产厂家：中外制药

インヒベース錠0.25／インヒベース錠0.5／インヒベース錠1

治疗类别名称
持续ACE抑制剂
商標名
INHIBACE
一般名
シラザプリル水和物(Cilazapril Hydrate)(JAN)
化学名
(1S,9S)-9-[(1S)-(1-Ethoxycarbonyl-3-phenylpropyl)amino]-10-oxooctahydro-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid monohydrate
構造式

分子式
C22H31N3O5・H2O
分子量
435.51
性　状
白色晶体或结晶性粉末，以黄色。
非常易溶于甲醇，易溶于乙醇（99.5）或乙酸（100），微溶于水。
逐渐成为淡黄色。
熔点
约101℃（分解）
适应病症
○高血圧症
用法用量
原发性高血压：每日1次，每次2.5-5mg，前1-2天从小剂量开始，视病情需要每隔2-4周个别调整剂量，如每日服用5mg仍不能控制血压时。
肾性高血压：由0.5mg或0.25mg开始，每日一次，维持剂量按个体调整。
药效药理
1. 作用机序
本剤被转换为迅速吸收活性代谢Shirazapurirato口服后。 Shirazapurirato是，主要抑制血管紧张素转换存在于血管壁或类似物（ACE）的酶的活性，抑制血管紧张素II，一个血管加压的形成。
抑制血管紧张素II的形成，从外周血管扩张，去甲肾上腺素的血管收缩作用衰减的其他交感神经末梢的去甲肾上腺素释放的抑制，导致醛固酮分泌的抑制，这些被认为以全面的方式提供一个降压动作。另外，这种药物具有产生促进灭活抑制作用的效果及血管舒张血管舒缓激肽的前列腺素，也这些效果被认为向降压效果。
(1) ACE阻害作用
1) Shirazapurirato，在体外，兔肺，抑制ACE的活性制备的人血浆和肺，从猪肾。
2) 在麻醉大鼠，外源性血管紧张素升压反应我有抑制作用。
3) 在自发性高血压大鼠（SHR），它表现出对血清ACE活性的抑制效果，以及各种类型的血管平滑肌ACE活性。
(2) 交感神经活性的抑制作用
1) 在麻醉的狗，它由下肾交感神经刺激血管紧张素I连续输液抑制去甲肾上腺素的释放。
2) 它抑制去甲肾上腺素，这是由脊髓电刺激在脑脊髓破坏大鼠释放的血管平滑肌收缩作用的升压反应。
(3) 激肽失活抑制作用
在肾上腺髓质切除SHR，它增强缓激肽的降血压作用。
2. 降圧作用
(1) 在SHR和2肾1夹肾性高血压大鼠，它产生了持久的降压作用。
(2) 在SHR，观察到的重复给药的降压效果衰减
(3) 在高血压患者（成人），在一次的日常管理，观察用药后的降压超过一小时。
(4) 在高血压患者（成人），在一次的日常管理，但持续超过24小时内显著降压，血压和脉搏的昼夜变化规律没有影响。
包装规格
片剂
0.25mg：100片（PTP）

0.5mg：100片（PTP），500片（PTP，瓶）

1mg：100片（PTP），500片（PTP，瓶），1000片（PTP）

制造厂商
中外制药有限公司
INHIBACE Tablet（Cilazapril hydrate）
INHIBACE Tablet 0.25（インヒベース錠0.25） 
Brand name : INHIBACE Tablet 0.25
　Active ingredient: Cilazapril hydrate
　Dosage form: white tablet (φ: approx. 5.1mm, thickness: approx. 1.9mm)
　Print on wrapping: インヒベース0.25mg
INHIBACE Tablet 0.5（インヒベース錠0.5）
Brand name : INHIBACE Tablet 0.5
　Active ingredient: Cilazapril hydrate
　Dosage form: white tablet (φ: approx. 6.1mm, thickness: approx. 2.7mm)
　Print on wrapping: インヒベース0.5mg
INHIBACE Tablet 1（インヒベース錠1）
Brand name : INHIBACE Tablet 1
　Active ingredient: Cilazapril hydrate
　Dosage form: white tablet (φ: approx. 7.1mm, thickness: approx. 3.1mm)
　Print on wrapping: インヒベース1mg
Effects of this medicine
This medicine lowers blood pressure by suppressing hypertensive substance of angiotensin II. It is usually used to treat hypertension.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you ever experienced any allergic reaction (itch, rash etc.) to any medicine.
If you ever had angioedema.
If you are receiving hemodialysis therapy, or the treatment to clear extra blood cholesterol from the blood (apheresis).
If you are a patient with cirrhosis, renal function disorder, hyperkalemia, or diabetes.
If you are limited your intake of salt.
•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>>
•General dosage regimen: For adults, start with 2 tablets (0.5mg of the active ingredient in terms of anhydride) once a day and increase the dosage little by little. The maximum dosage is 8 tablets (2mg of the active ingredient in terms of anhydride) once a day. However, if you have serious hypertension or you also have renal disorder, start with 1 tablet (0.25mg of the active ingredient in terms of anhydride) once a day. It should be adjusted according to your age and symptoms. Strictly follow the instructions of your doctor/pharmacist.
•Take the missed dose as soon as possible. If it is almost time for the next dose, skip the missed dose and continue yore regular dosing schedule. DO NOT take a double dose to make up for the missed dose.
•If you took too much of this medicine (more than ordered), check with your doctor/pharmacist.
•Do not stop taking this medicine without the instructions of your doctor.
Precautions while taking this medicine
•This medicine may cause dizziness/lightheadedness with decreased blood pressure. Exercise caution to drive a car, operate dangerous machinery, or work at heights.
Possible adverse reactions to this medicine
Common side effects are reported as below. If any of them occurs, check with your doctor/pharmacist: cough, dizziness/vertigo, hypotension, headache, stiff shoulder, discomfort in the throat, rash, pruritus.
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.
•breathlessness, swollen face/tongue/throat [angioedema]
•decreased urinary volume, bloody urine, swollen body/legs/eyes [acute renal failure]
•bad abdominal pain, back/lower-back pain, fever, nausea, vomiting, loss of appetite [pancreatitis]
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 at room temperature (1-30℃), away from direct sunlight and moisture.
•Discard the remainder. Do not store them. Ask the pharmacist how to discard.
Chugai Pharmaceutical Co., Ltd.Internal
Revised: 8/2008
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.
http://www.info.pmda.go.jp/go/pack/2144005F1028_2_12/