部分中文CAPTOPRIL R处方资料(仅供参考) 商標名 CAPTOPRIL R 一般名 カプトプリル(Captopril) 化学名 (2S)-1-[(2S)-2-Methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid 分子式 C9H15NO3S 分子量 217.29 融点 105~110℃ 構造式
性状 卡托普利结晶性粉末或白色结晶,有特定的香味或轻微,或不闻,有一种酸酸的味道。它非常易溶于甲醇,易溶于乙醇(99.5),和微溶于水。 操作注意事项 稳定性试验 在正常使用的是什么(铝袋(干燥剂))结果(室温,3年),长期储存试验是玫瑰和包装((干燥剂)和铝枕式包装PTP片)PTP包装,在市场分布是稳定三年已经得到证实。 适应症 用于高血症,也用于对利尿药,洋地黄类治疗无效的心力衰竭患者。 用法用量 视病情或个体差异而定。本品宜在医师指导或监护下服用。常用量:口服25-100mg,一日2-3次,饭前1小时服用。 高血压: 根据其他抗高血压药物的使用情况,血压升高程度及盐限制情况决定用量。如果可能,宜在开始治疗前1周停止服用其他抗高血压药物。一般初剂量25mg,一日2-3次。1-2周内如血压下降不明显,可增至50mg,一日2-3次,如仍未能满意地控制血压,可加服噻嗪类利尿药如氢氨噻嗪25mg,一日一次,以后可每隔1-2周逐步增加利尿药的剂量。以达到抗高血压的常用量。如还需进一步降低血压,可增加本品的剂量至100mg,一日2-3次,本品可与β受体阻滞药合用但降压作用小于两药单独应用的效果。 心力衰竭: 初剂量25mg,一日3次,剂量增至50mg,一日3次后,宜连服2周观察疗效:一般50-100mg,一日3次,临床症状已能得到满意改善,也可与利尿药与洋地黄合并使用。 对近期大量服过利尿药,处于低钠/低血容量,而血压属正常或偏低的患者。 对剂量宜用6.25mg-12.5mg,一日3次。以后通过测试逐步增加至常用量。 任何疑问,请遵医嘱! 禁忌 对本品过敏者禁用。 不良反应 有少数患者服用本品后可能出现以下副反应: 1、1-2%的患者有蛋白尿,其中1/4出现肾病综合症。但多数能在6个月内减少或消失,肾病患者蛋白尿的发生率较高,多尿,无尿及尿频等症状也偶有发现。 2、中性白细胞减少/粒性白细胞缺乏症,多在开始治疗后的3-12周出现。约2周后可恢复正常,其中部份病例并发全身或口腔感染,如红斑狼疮,自身免疫胶原性疾病等。 3、斑丘疹等瘙痒性皮疹或无皮疹性瘙痒,一般反应都较轻微,继续用药可减少,减量或停药后即消失,其中部分患者出现嗜酸性细胞增多,皮疹反应可用抗组胺类药物短期治疗。 4、面部潮红或苍白、四肢、面部、唇、口腔粘膜、舌、声门或喉部等部位的血管性水肿、味觉减退、异常或丧失等反应,应立即告知医生并停药,胃粘膜刺激、恶心、呕吐、腹痛、腹泻、厌食、便闭、口腔溃疡、胃溃疡、失眠、口干、发音困难、感受异常等副反应较为少见。 5、一般心力衰竭患者服药后可能发生血压暂时性降低约20%,并伴有短暂轻微的头昏。以后血压可逐步回复正常。大量服过利尿药引起血容量减少。无机盐过度耗竭的严重心力衰竭患者,可能发生低血压,应停药。 6、可能出现心动过速、胸痛、心悸等症状,心绞痛,心肌梗塞,雷诺氏综合症,充血性心力衰竭等副反应较为少见。 7、肝转氨酶增高,阻塞性黄疸及继发性胆汁郁积等副反应较为少见。 注意事项 1、应告知患者,当发现有血管性水肿症状(如面部、眼、舌、喉、四肢肿胀、吞咽或呼吸困难、声音嘶哑),应立即告知医师,并停药。 2、出现舌,声门或喉部血管性水肿会引起气管阻塞,导致死亡,应立即皮下注射盐酸肾上腺素注射液等药物进行紧急治疗。面部、口腔粘膜、唇、四肢的血管性水肿,一般停药后即可消失,必要时也需药物治疗。 3、肾功能严重减退及自身免疫缺陷的患者慎用。如需使用,应降低初剂量或减少用药次数,以后剂量应缓慢增加,以调节至病人所需的最小有效量。 4、使用过影响白细胞及免疫功能药物患者慎用。 5、应告诫患者,如出现咽痛,发热等感染症状,应及时告知医师。医师应采取措施,防止白细胞下降。 6、对肾功能不良,糖尿病及同时使用保钾利尿剂,补钾或含钾的盐类替代物,及增加血钾的其他的药物的患者服用本品可能引起高钾血症。 7、心力衰竭患者用本品治疗,应避免过量体力活动,要防止过度出汗,腹泻、呕吐等以避免体液减少导致的血压骤降。 8、没有医师指示,不得自行中断或停止治疗。 9、本品用于妊娠13-36周孕妇时,可能引起胎儿损伤甚至死亡,一旦发现妇女妊娠应立即停止使用,哺乳期妇女慎用。 10、儿童在其他药物治疗无效时,方可考虑使用本品。儿童用量可参考成人剂量按体重计算。 11、使用高流量透析膜(如AN69)进行血透病人,如采用本品可能发生过敏样反应,对此类患者及有类似反应的患者应加注意。
http://www.info.pmda.go.jp/go/pack/2144001N1040_1_11/2144001N1040_1_11?view=body GENERIC NAME: captopril BRAND NAME: Capoten DRUG CLASS AND MECHANISM: Captopril is an oral drug and a member of a class of drugs called angiotensin converting enzyme (ACE) inhibitors. ACE inhibitors are used for treating high blood pressure, heart failure, and for preventing kidney failure due to high blood pressure and diabetes. Other ACE inhibitors include enalapril (Vasotec), quinapril (Accupril), ramipril (Altace), fosinopril (Monopril), benazepril (Lotensin), lisinopril (Zestril, Prinivil), moexipril (Univasc) and trandolapril (Mavik). Angiotensin II is a very potent chemical that causes the muscles surrounding blood vessels to contract, thereby narrowing the The narrowing of the vessels increases the pressure within the vessels causing high blood pressure (hypertension). Angiotensin II is formed from angiotensin I in the blood by the enzyme angiotensin converting enzyme or ACE. ACE inhibitors are medications that slow (inhibit) the activity of the enzyme ACE and decrease the production of angiotensin II. As a result, blood vessels enlarge or dilate, and blood pressure is reduced. The lower blood pressure makes it easier for the heart to pump blood and can improve the function of a failing heart. In addition, progression of the blood vessel disease within the kidney caused by high blood pressure or diabetes is slowed. The FDA approved captopril in April 1981. PRESCRIPTION: Yes GENERIC AVAILABLE: Yes PREPARATIONS: Tablets: 12.5, 25, 50, 100 mg STORAGE: Captopril should be stored at room temperature, 15 to 30 C (59 to 86 F) and away from moisture. PRESCRIBED FOR: Captopril is used alone or in combination with other drugs for the treatment of high blood pressure and heart failure. Captopril also is used for improving survival and preventing heart failure and hospitalizations for heart failure after a heart attack. Like other ACE inhibitors, captopril may slow the progression of kidney failure in patients with diabetes or high blood pressure. DOSING: The recommended dose of captopril is 25-150 mg two or three times daily. The maximum dose is 450 mg daily. It should be taken on an empty stomach one hour before or two hours after meals since absorption of captopril is reduced when it is taken with food. DRUG INTERACTIONS: The use of ACE inhibitors with potassium supplements, salt substitutes or diuretics , for example, spironolactone (Aldactone), that increase potassium in the blood may lead to excessive potassium levels (hyperkalemia). Potassium levels should be monitored whenever ACE inhibitors are used in combination with these drugs. There have been reports of increased lithium (Eskalith, Lithobid) levels when lithium is used in combination with ACE inhibitors. The reason for this interaction is not known, but the increased levels may lead to toxicity from lithium. There have been reports that aspirin and other nonsteroidal antiinflammatory drugs (NSAIDs) such as ibuprofen (Advil, Children's Advil/Motrin, Medipren, Motrin, Nuprin, PediaCare Fever, etc.), indomethacin (Indocin, Indocin-SR), and naproxen (Anaprox, Naprelan, Naprosyn, Aleve) may reduce the effects of ACE inhibitors. PREGNANCY: ACE inhibitors, including captopril, can be harmful to the fetus and should not be taken by pregnant women. NURSING MOTHERS: Captopril is secreted in breast milk. Therefore it should be avoided by nursing mothers. SIDE EFFECTS: Captopril generally is well tolerated, and side effects are usually mild and transient. A dry, persistent cough has been reported commonly with the use of captopril and other ACE inhibitors. Coughing resolves after discontinuing the drug. Other side effects include abdominal pain, constipation, diarrhea, rash, dizziness, fatigue, headache, loss of taste, loss of appetite, nausea, vomiting, fainting and numbness or tingling in the hands or feet. Captopril and other ACE inhibitors also may cause kidney failure and increased levels of potassium in the blood. Serious but, fortunately, very rare side effects are liver failure and angioedema (swelling of lips and throat that can obstruct breathing). 药品介绍 本品为卡托普利的白色划痕压制片,具有抗高血压作用,是一种口服有效的特异性竞争型抑制剂。主要作用于肾血管紧张素醛固酮系统(RAA系统)。抑制RAA系统的血管紧张素转换酶(ACE),阻止血管紧张素Ⅰ转换成血管紧张素Ⅱ,并能抑制醛固酮分泌,减少水钠潴留。本品口服吸收迅速,口服治疗剂量1小时后达血药峰浓度胃中食物会减少30-40%的药物吸收,24小时内,95%以上的药物由尿排出,半衰期短于3小时,肾功能损害者会产生药物潴留。高血压患者服用本品后能减少外周动脉阻力,增加或不影响心输出量,增加肾血流量,但不影响肾小球滤过率。一般口服一次剂量后60-90分钟产生最大降压作用。继续服药降压作用增强。约需数周后才能取得最大疗效,本品对立位及卧位患者具有相同的降压效果。体位性低血压及心动过速等反应少见。 对心力衰竭患者,本品能明显降低外周血管阻力,肺毛细血管楔压及肺血管阻力,增加心输出量及运动耐受时间。与安慰剂的对比研究显示,本品对改善运动耐量时间(ETT)的作用无耐受性。 --------------------------------------------------------------- 产地国家: 日本 原产地英文商品名: CAPTOPRIL-R(カプトプリルRカプセル) 18.75mg 100caps 原产地英文药品名: CAPTOPRIL 中文参考商品译名: 卡托普利-R(カプトプリルRカプセル) 18.75毫克/胶囊 100胶囊/盒 中文参考药品译名: 卡托普利 中文参考化合物名称: 1-[(2S)-3- 巯基-2-甲基丙酰]-L脯氨酸 生产厂家英文名: Sawai system Medicines Co. 生产厂家中文名: 泽井制药有限公司
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