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【药品名称】西拉普利片
【商品名称】抑平舒
【英文名称】GILAZAPRIL TABLETS
【拼音名称】XILAPULI PIAN
【药品类别】抗高血压药
【性 状】薄膜衣片，为粉红色刻痕片，除去薄膜衣后显白色。
【药理毒理】本品为血管紧张素转换酶抑制剂，口服吸收转化为药理活性的西拉普利拉，它使血管紧张素Ⅰ不能转换为血管紧张素Ⅱ，并使血浆肾素活性增高、醛固酮分泌减少，从而使血管舒张、血管阻力降低而产生降压作用。
药代动力学： 西拉普利能有效被吸收并迅速地被转化为具有药理活性的西拉普利拉。进食后服用会轻微减慢和降低其吸收率，但并不影响疗效。根据尿液回收资料分析，口服抑平舒后的西拉普利拉的生物利用度约为60%。用药后两小时内达到血药峰浓度，浓度与剂量有直接关系。每日一次服用后，西拉普利拉的有效半衰期为9小时，并以原形从肾脏排除。肾功能不全病人，当肌酐清除率降低时，药物清除率也随之降低，故这类病人的西拉普利拉的血药浓度比肾功能正常的病人要高些。肾功能完全丧失者，肾脏失去清除能力，但可通过血液透析使西拉普利和西拉普利拉的血药浓度减低至一定范围之内。肾功能正常的老年病人，其西拉普利拉血药浓度要比年轻病人高40%，药物清除率要较之低20%。中度到重度肝硬化病人的药代动力学改变和老年病人相似。慢性心力衰竭病人的西拉普利拉清除率与肌酐清除率密切相关。所以剂量必需按照病人的肾功能进行调整(见特殊用药指导)。
适应症 用于治疗各种程度原发性高血压和肾性高血压，也可与洋地黄和(或)利尿剂合用作为治疗慢性心力衰竭的辅助药物。
【用法用量】：口服：每日一次，餐前或餐后服药均可。应在每天的同一时间内服药。
【特殊剂量指导】：
1.原发性高血压：通常剂量范围是2.5～5.0mg，每日一次。推荐的起始剂量为1mg片剂，每日一次。起始剂量很少能达到所需的疗效，应根据每个病人的血压情况分别调整剂量。如每日一次5mg仍不能控制血压时，则可加用非潴钾利尿药以增强其降压效果。
2.肾性高血压：与原发性高血压相比，血管紧张素转换酶抑制剂能更显著地减低肾性高血压。所以治疗肾性高血压时，起始剂量应为0.5mg或0.25mg，每日一次。维持剂量应按个体调整。
3.服用利尿剂的高血压病人：在用治疗前2～3天，应停用利尿剂以减少可能发生的症状性低血压。但如需要，以后可再恢复使用。这类病人的推荐起始剂量为0.5mg，每日一次。
4.慢性心力衰竭：可与洋地黄和(或)利尿剂联合使用，作为治疗慢性心力衰竭病人的辅助药物，起始剂量应以0.5mg，每日一次，并在严格的医生指导下进行。可根据耐受情况及临床状况将剂量增加至1mg，每日一次的最大维持剂量。此外，若需要把维持剂量调整至1～2.5mg之间，应根据病人的反应、临床状况及耐受性而进行调整。通常最大剂量为5mg，每日一次。临床试验结果证明，慢性心力衰竭病人的西拉普利拉清除率与肌酐清除率相互关联，因此慢性心力衰竭和肾功能不全病人应按肾功能不全一节所推荐的剂量用药。根据肾功能不全病人的肌酐清除率，而减少剂量，下面是推荐的用药方案：肌酐清除率 起始剂量 最大剂量 ＞40ml/min 1mg每日一次 5mg每日一次 10～4ml/min 0.5mg每日一次 2.5mg每日一次＞10ml/min 根据血压情况 0.25～0.5mg 每周1～2次需要血液透析的病人，应在不进行透析的日子服用，剂量应根据血压情况调整。如同其它血管紧张素转换酶抑制剂一样，使用高流量聚丙烯腈膜透析时会产生过敏反应，要避免这种情况，就应改用其它降压药，或是改换透析膜种类。
5.肝硬化：在极少情况下肝硬化病人需服用。由于可能会导致严重的低血压，故必须以0.5mg或0.25mg每日一次的起始剂量谨慎用药。
6.老年人：以每日0.5mg片剂作为起始剂量进行治疗，并根据不同病人的耐受性、疗效及临床状况以1～2.5mg的维持剂量用药。
7.儿童：由于尚未定出对儿童的药物效能及安全范围，故尚无法推荐儿童服用方案。
【不良反应】：最常报道的不良反应是头痛与头晕。其它发生率少于2%的不良反应包括乏力，低血压、消化不良、恶心、皮疹和干咳。大多数不良反应是短暂性的，轻度或中度，无需中止用药。服用慢性心力衰竭病人最常报道的不良反应是头晕及咳嗽。特异性反应：与其它血管紧张素转换酶抑制剂一样，罕有血管神经性水肿的报道。但由于此症可能伴有喉头水肿，故一旦波及面部、口唇、舌、声带和(或) 喉头时，必须立刻停用并进行适当治疗。某些病人中有血红蛋白、红细胞压积和(或)白细胞计数降低的报告，但尚无病例证明与本品有明确关系。
禁忌症 禁用于对该药或其它血管紧张素转换酶抑制剂过敏或患有腹水的病人。由于动物试验中发现血管紧张素转换酶抑制剂具有胚胎毒性，故禁用于妊娠期妇女。已发现其它类型的血管紧张素转换酶抑制剂与妊娠期羊水过少以及新生儿低血压和无尿有关。
【注意事项】：
1.禁用于主动脉瓣狭窄或心脏流出道阻塞病人。
2.症状性低血压：
(1)用血管紧张素转换酶抑制剂治疗偶见症状性低血压的报告。特别是因呕吐、腹泻，先已服用利尿剂、低钠饮食或血透后腹水低钠或低血容量的病人。
(2)急性低血压病人必须平卧休息，必要时静脉滴注生理盐水或扩容剂。血容量恢复后，也可以继续治疗，但如低血压持续存在，则应减少剂量或中止用药。 (3)慢性心力衰竭病人用可能会导致血压显著降低，但在以0.5mg的起始剂量的临床试验中，用药后未发现症状性低血压。
3.肾功能不全病人使用时，可根据病人的肌酐清除率而减少剂量。与其它血管紧张素转换酶抑制剂一样，用于单侧或双侧肾动脉狭窄病人时，可能会使尿素氮和血肌酐增加，这些改变通常能随着中止用药和(或)给予利尿剂治疗而恢复。
4.外科麻醉：血管紧张素转换酶抑制剂与具有降压作用的外科麻醉剂合用时，能导致动脉性低血压，发生这种情况时，则应以静脉输液法扩大血容量。无效时，应静脉滴注血管紧张素Ⅱ。
5.过敏样反应：虽然过敏样反应机理尚未确立，但已有临床显示，病人在服用血管紧张素转换酶抑制剂期间(包括西拉普利)，若使用高流量多丙烯腈膜继续血透、血过滤或LDL分离性输血，可导致过敏性反应或过敏样反应，包括危及生命的休克。故正在接受血管紧张素转换酶抑制剂的病人一定要避免以上各种治疗。
6.此外，若病人在服用血管紧张素转换酶抑制剂期间，同时接受用黄蜂或蜜蜂毒液作脱敏治疗，可能发生过敏性反应。因此，在接受脱敏治疗前一定要停止服用西拉普利，在这种情况下，不可用β-阻断剂来代替西拉普利。
【孕妇及哺乳期妇女用药】：
尚不明确本品是否能进入人类乳汁中，但由于动物资料显示少量小鼠乳汁含有西拉普利拉，故哺乳期妇女不应使用本品。
【老年患者用药】：
对使用大剂量利尿剂的老年慢性心力衰竭病人开始使用应严格按推荐的 0.5mg起始剂量用药。
药物相互作用】：
1.本品已与地高辛、硝酸盐类、速尿、噻唑类,口服抗糖尿病药物以及H2受体阻断剂等合用过,未见有地高辛浓度增高及其它具有临床意义的药物相互作用。但当本品与其它降压药物合用时可能会引起相加作用。
2.本品与潴钾利尿剂合用，可引起血钾增高，特别是在肾功能不全者。
3.和其它血管紧张素转换酶抑制剂一样，与非甾体抗炎药物合用时，可能会降低本品的降压作用。在使用非甾体抗炎药物之前使用本品的病人则不发生以上情况。
【贮藏】：遮光，密闭保存。
【原产地英文商品名】VASCACE(Inhibace Equivalent)2.5MG/TABLET,28 TABLETS
【原产地英文药品名】Cilazapril
【中文参考商品译名】抑平舒 - 2.5毫克/片，28片/瓶
【中文参考药品译名】西拉普利
【生产厂家中文参考译名】罗氏
【生产厂家英文名】ROCHE
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【原产地英文商品名】ZAPRIL(Inhibace Italy) 2.5mg/tab 28tabs/bottle
【原产地英文药品名】CILAZAPRIL
【中文参考商品译名】ZAPRIL(意大利抑平舒)2.5毫克/片 28片/瓶
【中文参考药品译名】西拉普利
Vascace (cilazapril)
How does it work?
Vascace tablets contain the active ingredient cilazapril, which is a type of medicine called an ACE inhibitor.
ACE inhibitors work by blocking the action of a compound in the body called angiotensin converting enzyme (ACE). Normally ACE produces another compound called angiotensin II, as part of the body's natural control of blood pressure. Angiotensin II causes blood vessels to constrict and narrow, which increases the pressure within the blood vessels.
As cilazapril blocks the action of ACE, it reduces the production of angiotensin II. This means that the blood vessels are allowed to relax and widen. The overall effect of this is a drop in blood pressure, hence cilazapril can be used to lower high blood pressure.
The reduced pressure within the blood vessels means that the heart doesn't have to work as hard to pump the blood around the body. This means that ACE inhibitors such as cilazapril can also be used to improve the symptoms of heart failure, where the heart is not pumping as efficiently as it should be.
What is it used for?
High blood pressure with no known cause (essential hypertension).
Heart failure.
Warning!
Some people may experience dizziness caused by low blood pressure in the first few days of taking this medicine and in particular the first dose. For this reason, the first dose should preferably be taken at bedtime. Your doctor may want you to take the first dose of this medicine under medical supervision in hospital if you are aged over 70 years, have low blood pressure, low levels of fluids or salt in your blood (eg due to dehydration), severe or unstable heart failure, kidney problems, or are taking high doses of diuretic medicines, multiple diuretic medicines, or certain other medicines that dilate your blood vessels.
If you feel dizzy during treatment this can be relieved by lying down until the symptoms pass. If affected you should avoid performing potentially hazardous tasks such as driving or operating machinary. If you frequently feel dizzy you should let your doctor know, as your dose of this medicine may need reducing.
Alcohol may enhance the blood pressure lowering effect of this medicine, which can increase dizziness and may increase the risk of fainting.
ACE inhibitors can sometimes cause an allergic reaction called angioedema. Stop taking this medicine and consult your doctor immediately if you experience difficulty breathing or swallowing, or swelling of your face, lips, tongue, throat, hands, feet or ankles while taking this medicine. This type of allergic reaction has been reported more frequently in people of Afro-Caribbean origin.
Your blood pressure, kidney function and the amount of potassium in your blood should be regularly monitored while you are taking this medicine.
Use with caution in
Elderly people.
Decreased liver function.
Decreased kidney function.
Narrowing of the arteries that supply blood to the kidneys (renal artery stenosis).
People with hardening of the arteries (athersclerosis), eg in the heart (cardiovascular disease), brain (cerebrovascular disease) or legs (peripheral vascular disease).
People with low fluid volume or salt levels in the body, eg due to diuretic therapy, low-sodium diet, diarrhoea or vomiting.
People taking other medicines for high blood pressure, particularly diuretics (see end of factsheet).
Narrowing of the main artery of the body (aortic stenosis).
Heart disease characterised by thickening of the internal heart muscle and a blockage inside the heart (hypertrophic obstructive cardiomyopathy).
Severe heart failure.
Diabetes.
Diseases affecting connective tissue, eg scleroderma, systemic lupus erythematosus or rheumatoid arthritis (collagen vascular diseases).
People with kidney failure requiring a certain type of haemodialysis (high-flux membrane).
People receiving therapy to remove certain types of fat from the blood using a machine (LDL apheresis).
People undergoing therapy to decrease allergy to bee or wasp stings (desensitisation).
Not to be used in
Allergy to other ACE inhibitor medicines.
History of swelling of the lips, face or tongue (angioedema) caused by previous use of an ACE inhibitor medicine.
People with fluid accumulation in the abdomen (ascites).
Pregnancy.
Breastfeeding.
Rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption (Vascace tablets contain lactose).
This medicine is not recommended for children.
This medicine should not be used if you are allergic to one or any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy.
If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately.
Pregnancy and breastfeeding
Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding providing the benefits to the mother outweigh the risks to the unborn baby. Always inform your doctor if you are pregnant or planning a pregnancy, before using any medicine.
This medicine must not be used during pregnancy as it may be harmful to the developing baby. Seek further medical advice from your doctor. If you get pregnant while taking this medicine, stop taking it and consult your doctor immediately.
It is not known if this medicine passes into breast milk. The manufacturer states that it should not be taken by women who are breastfeeding. Seek further medical advice from your doctor.
Side effects
Medicines and their possible side effects can affect individual people in different ways. The following are some of the side effects that are known to be associated with this medicine. Just because a side effect is stated here does not mean that all people using this medicine will experience that or any side effect.
Headache.
Dizziness.
Dry cough.
Fatigue.
Low blood pressure (hypotension).
Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
Rash.
Alteration in taste.
Increased heart rate (tachcardia).
Awareness of your heart beat (palpitations).
Chest pain.
Increased sensitivity of the skin the sunlight (photosensitivity).
Hair loss.
Shortness of breath.
Inflammation of the sinuses or lining of the nose (sinusitis/rhinitis).
Inflammation of the pancreas (pancreatitis).
Severe swelling of lips, face, tongue or throat (angioedema - see warning above).
Problems with kidney function.
Disturbances in the normal levels of blood cells in the blood (tell you doctor if you get a sore throat, mouth ulcers, high temperature (fever), or feel tired or generally unwell while taking this medicine).
Problems with liver function, including jaundice or hepatitis (consult your doctor promptly if you develop unexplained itching, yellowing of the skin or eyes, unusually dark urine, nausea and vomiting, abdominal pains, loss of appetite or flu-like symptoms while taking this medicine).
The side effects listed above may not include all of the side effects reported by the medicine's manufacturer.
For more information about any other possible risks associated with this medicine, please read the information provided with the medicine or consult your doctor or pharmacist.
How can this medicine affect other medicines?
It is important to tell your doctor or pharmacist what medicines you are already taking, including those bought without a prescription and herbal medicines, before you start treatment with this medicine. Similarly, check with your doctor or pharmacist before taking any new medicines while taking this one, to ensure that the combination is safe.
Cilazapril has an additive effect with other medicines that decrease blood pressure, particularly other medicines used to treat high blood pressure (antihypertensives). In people taking antihypertensive medicines it may cause a large drop in blood pressure with the first dose, particularly in people taking diuretic medicines such as furosemide. This may cause dizziness, which can usually be relieved by lying down until the symptoms pass. If you are taking a diuretic medicine, your doctor may reduce your dose or ask you to stop taking it for a few days before starting cilazapril. This is to prevent your blood pressure from dropping too low. If you frequently feel dizzy while taking this medicine in combination with other blood pressure lowering medicines you should let your doctor know, as your doses may need adjusting. Other medicines that decrease blood pressure include the following:
other ACE inhibitors, eg captopril
aldesleukin
alpha-blockers such as prazosin
alprostadil
angiotensin II receptor antagonists such as losartan
antipsychotics
benzodiazepines, eg temazepam, diazepam
baclofen
beta-blockers such as propranolol
calcium-channel blockers such as verapamil, nifedipine
clonidine
diazoxide
diuretics, eg furosemide, bendroflumethiazide
dopamine agonists, eg bromocriptine, apomorphine
hydralazine
levodopa
MAOI antidepressants, eg phenelzine
methyldopa
minoxidil
moxonidine
moxisylyte
nicorandil
nitrates, eg glyceryl trinitrate
tizanidine.
Non-steroidal anti-inflammatory drugs (NSAIDs, eg indometacin, aspirin, diclofenac, ibuprofen) may reduce the blood pressure lowering effect of cilazapril, and may increase the risk of a decline in kidney function. You should avoid taking this type of painkiller unless recommended by your doctor.
There may be a risk of raised potassium levels in the blood (hyperkalaemia) if any of the following medicines are taken with cilazapril, hence these are not normally recommended for use in combination with cilazapril. If you are taking any of the following with this medicine you should have regular blood tests to monitor the amount of potassium in your blood:
angiotensin II receptor antagonists, eg losartan
ciclosporin
drospirenone
epoetin (this may also oppose the blood pressure lowering effect of enalapril)
heparin
potassium-containing salt substitutes (eg Lo-Salt)
potassium salts, eg potassium citrate for cystitis
potassium-sparing diuretics (eg spironolactone, triamterene, amiloride)
potassium supplements.
Cilazapril may increase the blood level of the medicine lithium and for this reason, it is not normally recommended for people taking lithium. People taking this medicine in combination with lithium should have the level of lithium in their blood closely monitored.
Cilazapril may possibly enhance the blood sugar lowering effect of insulin and oral antidiabetic medicines, and so could increase the risk of low blood sugar (hypoglycaemia). People with diabetes should therefore carefully monitor their blood sugar while taking this medicine, particularly in the first few weeks of treatment.
There may be an increased risk of a drop in the normal numbers of white blood cells in the blood if this medicine is taken in combination with any of the following medicines:
allopurinol
azathioprine
immunosuppressant therapy
procainamide.
If you are taking any of these in combination with this medicine, you should have regular blood tests to monitor the levels of your blood cells in your blood, particularly if you also have any kidney problems or diseases affecting connective tissue, eg scleroderma, systemic lupus erythematosus or rheumatoid arthritis (collagen vascular diseases). Tell your doctor if you experience any signs of infection, such as fever, sore throat or mouth ulcers, as these could be signs of problems with your white blood cells.
Other medicines containing the same active ingredient
There are currently no other medicines available in the UK that contain cilazapril as the active ingredient. | 
