注射用兰索拉唑
注射用右兰索拉唑-详细说明书与重点
注射用右兰索拉理［成份］:本品活性成份为右兰索拉哗。
化学名称：(R)2［I［3-甲基4(222-三氟氧基)2此基］:甲基］:亚硫酷基］:-IH-苯并咪化学结构式。
分子式:C16H14F3N3O2S ,分子量:369.36。
辅料:葡甲胺、甘露醇、氢氧化钠。
［规格］：20mg o［用法用量］：静脉滴注:通常成年人一次20mg ,一日2次，疗程不超过5天。
一旦患者可以口服药物，应改为口服用药。
临用前将瓶中内容物用5mL0.9%氯化钠注射液溶解，再用IOOLO.9%氧化钠注射液释，一日2次，静脉滴注，推荐给药时间不少于30分钟。
使用时注意：1.经本品治疗的前3日内达到止血效果的，应改用口服用药，不可无限制静脉给药。
临床试验中，本品目前尚无超过6天的用药经验。
2.本品临床试验中未入选Forrestla级喷射样出血者。
对于内镜下见喷射样出血、活动性渗血、血管裸露等高危人群，建议参考临床诊治指南首先考虑进行内镜止血。
3.本品仅用于静脉滴注。
溶解后应尽快使用，勿保存。
避免与0.9%氯化钠注射液以外的液体和其他药物混合静滴。
4.使用本品时应使用专用的输液器，不得与其他药物共用。
万不得已需要通过其他药物的输液器侧管给予本品时应停止输注其他药物，并在本品给药之前和之后用0.9%氯化钠注射液冲管。
5.本品静消使用时应配有孔径为1.2um的过滤器，以便去除输液过程中可能产生的沉淀物。
这些沉淀物有可能引起小血管栓塞而产生严重后果。
［适应症］：用于口服疗法不适用的伴有出血的胃、十二指肠溃疡。
6禁忌症］：1.对本品中任何成份过敏的患者禁止使用本品。
2.正在使用硫酸阿扎那韦、盐酸利匹韦林的患者禁止使用本品。
［注意事项］：L以下患者慎重用药。
（1）有药物过敏症既往史的患者。
（2）肝功能障碍的患者（因本药的代谢、排泄延迟）。
2 .本品治疗可能会掩盖消化道肿瘤的症状，应排除恶性肿瘤后方可用药。
3 .本品治疗时密切观察病情，治疗无效时应改用其它疗法。
注射用兰索拉唑与奥硝唑氯化钠注射液存在配伍禁忌
滴／ ａ ｒ ｉ ｎ ， 第 三次 速 度较 慢 ， 为２ ５滴／ ｍ ｉ ｎ左 右 。滴 注 速 度 快时 两种 液体 尚未 充 分反 应 ， 前 一 种 液 体 即滴 注 完
毕， 或 发生反 应 量 少 变化 不 明显 。滴 注 速 度 慢 时 两 种
参 考 文 献
１ 卢艳华． 兰索拉唑治疗 ｌ Ｏ Ｏ例 消 化 性 溃 疡 疗 效 分 析 ［ Ｊ ］ ．北 方 药 学 ，
２ ｏ １ ３， （ ７ ） ： １ ２ ３
黄色， ５ ｍ ｉ ｎ后 变 为深 黄 色 ， ２ ｈ后 变 成 黄色 ， ２ ４ ｈ后 仍 为黄 色液 体 。此 实验 经三个 样 品量 在 同等 条 件 同时 展
制 剂 ， 本 药在 胃黏膜 壁细胞 酸 性环境 下 转变 为活 性
液各 ５ ｍ ｌ 液体加 以混合 ， 主要 是 考 虑 到 前 液 尚 未 输
后 液加 入时 最 大 可 能 的混 合 量 。经 三次 同等 条 件 型的代谢 物， 与 质子泵 的 ｓ Ｈ基结 合 ， 抑 制 该 酶 的 活 完 ， 性， 从而 能抑 制 胃酸 的分 泌 ， Ｉ ｌ ｆ ｉ ｉ 床上 广 泛用 于 与 酸相 关 同时展 开实 验 ， 结 果一 致 ， 由此判 断 注射 用 兰索 拉唑 与 ０ ． ５ ％ 奥硝 唑氯 化 钠 注 射 液存 在 配伍 禁 忌 。经 文献 检 胃病和幽门螺旋杆菌感染的治疗 。奥硝唑是第三代硝
嘱， 患者 滴 注注 射用 兰索 拉 唑 ３ ０ ｍ ｇ ／ ｄ （ 山东 罗欣 药 业 液 体有 充 分 的 时 间发 生 反 应 ， 故 发 现 输 液 管 变 成 淡 股 份有 限公 司 ） 溶于 氯化 钠 注射 液 １ ０ ０ ｍ ｌ 中， ０ ． ５ ％ 奥 黄色 。
兰索拉唑
恶心呕吐防治历程
5-HT3受体拮抗剂上市历史
分代
英文名
通用中文名 （商品名）
研发与上市公 司
首次上 市时间
上市国家
国内 上市时间
Ondansetron 昂丹司琼 ( 枢复宁) 葛兰素史克
1991
英美
1995
Granisetron 格拉司琼 (凯特瑞)
罗氏
1994
美国
1996
第1代
短效5HT3受体 拮抗剂
欧丽（帕洛诺司琼） 简介
恶心、呕吐——最令癌症患者恐惧的经历
Rank 1 2 3
19831 呕吐 恶心 脱发
4 担心临床的处理
5
处理所需要的时 间
19932 恶心 持续疲倦 脱发 影响家庭
呕吐
19973 恶心 脱发 呕吐 持续疲倦
注射
19994 恶心 脱发 持续疲倦 呕吐
味觉的改变
10%~20%的患因害怕不良反应而拒绝化疗Βιβλιοθήκη 迟发性呕吐 Delayed
化疗 24 hours
Chemotherapy-Induced Nausea and Vomiting (CINV):化疗导致的恶心呕吐
延迟性CINV的发生率和严重性被普遍低估
70% 60% 50% 40% 30% 20% 10%
医生预测 实际发生
HEC 60%
34%33%
欧丽半衰期长达40h，远高于第1代5- 5-HT3受体拮抗剂 欧丽与5-HT3受体的亲和力较其他5-HT3受体拮抗剂至少高30-100倍
欧丽优势1
受体亲和力强：欧丽与5-HT3受体的亲和力较其他5-HT3受 体拮抗剂至少高30-100倍
化合物 帕洛诺司琼
注射用兰索拉唑与复方甘草酸单铵注射液存在配伍禁忌
注射用兰索拉唑与复方甘草酸单铵注射液存在配伍禁忌发表时间：2020-07-10T06:11:51.586Z 来源：《航空军医》2020年5期作者：王亚铎[导读]（陆军第81集团医院河北张家口 075000）注射用兰索拉唑（30 mg）是一种抑制胃酸分泌药，性状为白色或类白色疏松块状物或粉末，适用于各种类型的腐蚀性食道炎治疗，如反流性食管炎、胃溃疡、十二指肠溃疡等。
脱氧核苷酸钠注射液复方甘草酸单铵注射液（5ml）为复方制剂，适用于急、慢性肝炎、药物中毒、食物中毒、药物过敏等。
在临床工作中发现，注射用兰索拉唑与复方甘草酸单铵注射液存在配伍禁忌，现报道如下；1临床资料患者，男，57 岁，2019 年10 月因慢性乙型肝炎、胃溃疡收入院，遵医嘱予0．9% 氯化钠注射液100 ml 中加入注射用兰索拉唑30 mg 静脉滴注治疗，滴注过程通畅，后又予5% 葡萄糖注射液250 ml 中加入复方甘草酸单铵注射液5ml 静脉滴注，发现在同一静脉通路的两组液体混合时，在莫非氏滴管中会出现白色絮状物，输液管中出现浑浊现象。
见状立即停止输液，更换液体及输液管并报告医生，续输0．9% 氯化钠注射液100 ml，监测患者生命体征，患者无不良反应发生。
2 实验方法及结果为进一步证实注射用兰索拉唑与复方甘草酸单铵注射液是否存在配伍禁忌，随即我们做了配伍实验，用0．9% 氯化钠注射液10 ml 将注射用兰索拉唑30 mg 充分溶解取2 ml，与复方甘草酸单铵注射液2 ml 混合，随即出现白色浑浊现象，静置20 min 无变化，重复几次实验均出现相同的反应。
临床应用及实验均表明注射用兰索拉唑与复方甘草酸单铵注射液存在配伍禁忌，两者不能同时使用。
3 讨论经查阅《306 种注射剂临床配伍应用检索表》及药品说明书，未注明注射用兰索拉唑与脱氧核苷酸钠复方甘草酸单铵注射液存在配伍禁忌，因此，医护人员在临床中使用上述两种药物时，应间隔给药，可在两种药物输注间歇时用生理盐水冲洗输液管，减慢输液速度，观察患者的反应，避免两种药物直接接触而发生反应，给患者造成不良后果，确保临床用药安全。
兰索拉唑针的作用
兰索拉唑针的作用关于《兰索拉唑针的作用》，是我们特意为大家整理的，希望对大家有所帮助。
临床医学上一般用兰索拉唑针医治十二指肠溃疡。
实际上兰索拉唑针归属于典型性的质子泵缓聚剂，一般状况下如果是成年人建议24钟头内开展2次给药，一次为30mg，根据兰索拉唑针可以非常大水平的抑制胃酸代谢，有利于推动病况康复治疗。
那麼除开这种兰索拉唑针还有哪些功效呢?注射用兰索拉唑，适用范围为用以内服治疗法不适合的伴随流血的十二指肠溃疡。
适用范围用以内服治疗法不适合的伴随流血的十二指肠溃疡。
药理学毒理学药用价值：兰索拉唑归属于质子泵缓聚剂。
本药遍布于胃黏膜壁细胞的酸碱性自然环境后，变化为有特异性的类化合物。
这类类化合物与存有于酸转化成位置的H ，K -ATP酶的巯基融合，根据抑止H ，K -ATP酶的特异性而抑止酸代谢。
兰索拉唑抑制胃酸代谢功效呈使用量依赖感，药后24钟头内对基本和刺激性造成的胃液代谢均有抑制效果。
身心健康成年人1次30Mg，一日2次静脉给药，由此可见持续的胃液代谢抑制效果。
有报导在酸碱性标准下，血液凝结与血小板聚集遭受非常大危害。
血液凝结所产生的游离脂肪酸，在酸碱性标准下可被胃蛋白酶融解。
本药根据上升胃内pH值而改进血液凝结与血小板聚集作用，抑止胃蛋白酶的特异性而充分发挥抑止流血的功效。
此外，在酸碱性标准下，胃的损害黏膜的修补遭受抑止，本药根据抑止酸代谢进而胃内pH值升高，推动损害黏膜的修补。
毒理学科学研究：基因遗传毒副作用：Ames实验。
大白鼠肝脏程序流程外DNA 生成实验及其小白鼠微核试验、大白鼠骨髓细胞染色体畸变实验結果均为呈阴性。
身体之外人网织红细胞染色体畸变试验結果为呈阳性。
生殖毒副作用：大白鼠和家兔静脉给与兰索拉唑使用量达30Mg/kg/天(按体表面积测算等同于人临床医学强烈推荐使用量的8倍和16倍)，未发觉对生育能力和试管胚胎有欠佳影响。
致癌物质科学研究：SD大鼠持续24月内服兰索拉唑5-150Mg/kg/天(按体表面积测算等同于休重为5KG病人的临床医学强烈推荐使用量30Mg/d的1～40倍)，数据显示兰索拉唑以使用量依靠方法引起肠胃嗜铬样(ECL)体细胞增生和良好ECL细胞瘤;受试小动物胃上皮细胞出現肠上皮细胞化的发病率提升。
注射用兰索拉唑与舒血宁注射液存在配伍禁忌
注射用兰索拉唑与舒血宁注射液存在配伍禁忌作者：吴青佩来源：《护理实践与研究》 2014年第5期吴青佩doi:10.3969/j.issn.1672-9676.2014.05.044注射用兰索拉唑为白色或类白色疏松块状物或粉末，主要成分为兰索拉唑，属于质子泵抑制剂，主要作用是抑制胃酸分泌，用于口服疗法不适用的伴有出血的十二指肠溃疡，规格：30 mg/支。
舒血宁注射液为黄色澄明液体，主要成分为银杏叶。
功能与主治：扩张血管、改善微循环，用于缺血性心脑血管疾病、冠心病、心绞痛、脑栓塞、脑血管痉挛等。
规格：2 ml/支。
笔者临床发现此两种药液序贯输入时发生变色。
现报道如下。
1临床资料患者，女，70岁，主因无明显诱因出现头晕伴视物旋转 1 d 以椎基底动脉供血不足于2013年9月4日收住院。
患者曾于2012年5月查胃镜诊断为反流性食管炎、疣状胃炎后长期口服奥美拉唑肠溶胶囊20 mg，1次/d。
此次住院后医嘱停奥美拉唑肠溶胶囊口服，给予0.9%氯化钠注射液100 ml+注射用兰索拉唑30 mg静脉输入，1次/d;5%葡萄糖注射液250 ml+舒血宁注射液20 ml静脉输入，1次/d。
临床输液时当0.9%氯化钠注射液100 ml+注射用兰索拉唑30 mg静滴完毕，更换舒血宁组液后输液器滴壶内即刻变为黄绿色澄明液体，立即更换输液器，并更换0.9%氯化钠注射液100 ml冲管15 min后再次更换舒血宁组液继续静脉输入，观察患者30 min无不良反应。
2实验方法与结果笔者用20 ml注射器先后抽取0.9%氯化钠注射液100 ml+注射用兰索拉唑30 mg组液10 ml、5%葡萄糖注射液250 ml+舒血宁注射液20 ml组液10 ml，当注射器内两种药液混合后立刻变为黄绿色，将其静置24 h后观察仍为黄绿色，无混浊、沉淀、絮状物生成，此实验证明注射用兰索拉唑与舒血宁注射液之间存在配伍禁忌。
3小结查阅注射用兰索拉唑说明书上注明与硫酸阿扎那韦存在配伍禁忌，无与其他药物之间相关配伍禁忌的说明。
注射用兰索拉唑说明书(美国)
O N H NS CH 2 N H 3C2CF 3 (No. 3954)PRV0509 R6May 2009PREVACID ® I.V.(lansoprazole)for Injection30 mg/vialR x onlyDESCRIPTIONThe active ingredient in PREVACID I.V. (lansoprazole) for Injection is a substituted benzimidazole, 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl] methyl] sulfinyl] benzimidazole, a compound that inhibits gastric acid secretion. Its empirical formula is C 16H 14F 3N 3O 2S with a molecular weight of 369.37. PREVACID has the following structure:Lansoprazole is a white to brownish-white odorless crystalline powder which melts withdecomposition at approximately 166°C. Lansoprazole is freely soluble in dimethylformamide; soluble in methanol; sparingly soluble in ethanol; slightly soluble in ethyl acetate, dichloromethane and acetonitrile; very slightly soluble in ether; and practically insoluble in hexane and water.Lansoprazole is stable when exposed to light for up to two months. The rate of degradation of the compound in aqueous solution increases with decreasing pH.PREVACID I.V. for Injection contains 30 mg of the active ingredient lansoprazole, 60 mgmannitol, 10 mg meglumine, and 3.45 mg sodium hydroxide and is supplied as a sterile, lyophilized powder for I.V. (intravenous) use. The solution of PREVACID I.V. for Injection has a pH ofapproximately 11 following the first reconstitution with Sterile Water for Injection, USP, andapproximately 10.2, 10.0, or 9.5 after further dilution with either 0.9% Sodium Chloride Injection, USP, Lactated Ringer’s Injection, USP, or 5% Dextrose Injection, USP, respectively.CLINICAL PHARMACOLOGYPharmacokinetics and MetabolismFollowing the administration of 30 mg of lansoprazole by intravenous infusion over 30 minutes to healthy subjects, plasma concentrations of lansoprazole declined exponentially with a mean (+ standard deviation) terminal elimination half-life of 1.3 (± 0.5) hours. The mean peak plasma concentration of lansoprazole (C max) was 1705 (± 292) ng/mL and the mean area under the plasma concentration versus time curve (AUC) was 3192 (± 1745) ng⋅h/mL. The absolute bioavailability of lansoprazole following oral administration is over 80%, and C max and AUC of lansoprazole are approximately proportional in doses from 15 mg to 60 mg after single oral administration. The pharmacokinetics of lansoprazole did not change with time after 7-day once daily repeated oral or intravenous administration of 30 mg lansoprazole.DistributionThe apparent volume of distribution of lansoprazole is approximately 15.7 (± 1.9) L, distributing mainly in extracellular fluid. Lansoprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 0.05 to 5.0 µg/mL.MetabolismLansoprazole is extensively metabolized in the liver. Two metabolites have been identified in measurable quantities in plasma (the hydroxylated sulfinyl and sulfone derivatives of lansoprazole). These metabolites have very little or no antisecretory activity. Lansoprazole is thought to be transformed into two active species which inhibit acid secretion by blocking the proton pump [(H+,K+)-ATPase enzyme system] at the secretory surface of the gastric parietal cell. The two active species are not present in the systemic circulation. The plasma elimination half-life of lansoprazole is less than 2 hours while the acid inhibitory effect lasts more than 24 hours. Therefore, the plasma elimination half-life of lansoprazole does not reflect its duration of suppression of gastric acid secretion. EliminationFollowing an intravenous dose of lansoprazole, the mean clearance was 11.1 (± 3.8) L/h. Following single-dose oral administration of lansoprazole, virtually no unchanged lansoprazole was excreted in the urine. In one study, after a single oral dose of 14C-lansoprazole, approximately one-third of the administered radiation was excreted in the urine and two-thirds was recovered in the feces. This implies a significant biliary excretion of the lansoprazole metabolites.Special PopulationsGeriatric UseFollowing oral administration, the clearance of lansoprazole is decreased in the elderly, with elimination half-life increased approximately 50% to 100%. Because the mean half-life in the elderly remains between 1.9 to 2.9 hours, repeated once daily dosing does not result in accumulation of lansoprazole. Peak plasma levels were not increased in the elderly. No intravenous dosage adjustment is needed.Pediatric UseThe pharmacokinetics of intravenous lansoprazole have not been studied in pediatric patients. For further information, please see the PREVACID package insert for the oral formulations.GenderThe pharmacokinetic data of intravenous lansoprazole in females is limited; however, in a study with oral lansoprazole comparing 12 male and 6 female human subjects who received lansoprazole, no gender differences were found in pharmacokinetics and intragastric pH results. No intravenous dosage adjustment is needed (also refer to Use in Women).Renal InsufficiencyIn patients with severe renal insufficiency, plasma protein binding decreased by 1.0%-1.5% after oral administration of 60 mg of lansoprazole. Patients with renal insufficiency had a shortened elimination half-life and decreased total AUC (free and bound). The AUC for free lansoprazole in plasma, however, was not related to the degree of renal impairment; and the C max and T max (time to reach the maximum concentration) were not different than the C max and T max from subjects with normal renal function. No intravenous dosage adjustment is necessary in patients with renal insufficiency. Hepatic InsufficiencyIn patients with various degrees of chronic hepatic disease, the mean plasma half-life of lansoprazole was prolonged from 1.5 hours to 3.2-7.2 hours after oral administration. An increase in the mean AUC of up to 500% was observed at steady state in hepatically-impaired patients compared to healthy subjects. Intravenous dose reduction in patients with severe hepatic disease should be considered. RaceThe pooled mean pharmacokinetic parameters of orally administered lansoprazole from twelve U.S. Phase 1 studies (N=513) were compared to the mean pharmacokinetic parameters from two Asianstudies (N=20). The mean AUCs of lansoprazole in Asian subjects were approximately twice those seen in pooled U.S. data; however, the inter-individual variability was high. The C max values were comparable. Information for intravenous dosing is not available.PharmacodynamicsMechanism of ActionPREVACID (lansoprazole) belongs to a class of antisecretory compounds, the substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the (H+, K+) -ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the parietal cell, lansoprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated gastric acid secretion for at least 24 hours irrespective of the stimulus. Lansoprazole does not exhibit anticholinergic or histamine type-2 antagonist activity.Antisecretory ActivityAcid OutputAn open-label, single-center, two period study was conducted to evaluate the pharmacodynamics of 30 mg of intravenous lansoprazole and 30 mg of oral lansoprazole in 29 healthy subjects. The primary pharmacodynamic endpoints were pentagastrin stimulated maximum acid output (MAO) and basal acid output (BAO). Subjects received oral lansoprazole for 7 days in Period 1 and then were immediately switched to intravenous lansoprazole for 7 days in Period 2. MAO and BAO were measured at baseline and 21 hours following the last oral dose and the last intravenous dose of lansoprazole. This study demonstrated that 7 days of oral lansoprazole followed by 7 days of intravenous lansoprazole administration significantly suppressed gastric acid output as compared with baseline. Seven days of 30 mg of intravenous lansoprazole was equivalent to 30 mg of oral lansoprazole in the ability to maintain gastric acid output suppression (Table 1).Table 1: Acid Output (mEq/hr)PREVACID 30 mgBaseline After 7 Days ofOral Dosing After 7 Days of I.V. DosingMaximum Acid Output (Median) 11.26n=27 4.76*n=285.13*n=28Basal Acid Output (Median) 1.42n=28 0.42*n=280.27*n=28* Significantly (p ≤ 0.05) less acid output as compared to baseline.24-Hour Intragastric pHA multiple-dose study was conducted in 36 healthy subjects comparing the pharmacokinetics and pharmacodynamics of lansoprazole after intravenous administration and oral administration. During the first-hour post-dosing interval, intravenous lansoprazole resulted in significantly higher mean intragastric pH than did oral lansoprazole. There were no statistically significant differences between oral and intravenous regimens in 24-hour mean intragastric pH for the percentage of time that the intragastric pH was above 3 and 4 after 1-day or 5-day once daily repeated administration of 30 mg lansoprazole. Gastric acid suppression was maintained throughout each treatment period. The pharmacodynamic results are summarized in Table 2.Table 2: Mean Antisecretory Effects after Single and Multiple Daily DosingParameter BaselineValuePREVACID30 mg daily Orallyx 5 days30 mg I.V. Infusion daily x5 DaysDay 1 Day 5 Day 1 Day 5Mean 24-Hour pH Mean first hour pH % Time Gastric pH>3 % Time Gastric pH>4 3.334.4445.2731.074.752.7474.0867.185.254.7983.9277.614.864.64*78.3670.515.365.91*85.5479.68*Significantly (p≤ 0.05) higher than the oral lansoprazoleRefer to CLINICAL PHARMACOLOGY for pharmacokinetic results.Enterochromaffin-like (ECL) Cell EffectsDuring lifetime exposure of rats with up to 150 mg/kg/day of lansoprazole dosed orally seven days per week, marked hypergastrinemia was observed followed by ECL cell proliferation and formation of carcinoid tumors, especially in female rats (refer to PRECAUTIONS, Carcinogenesis, Mutagenesis, Impairment of Fertility).Gastric biopsy specimens from the body of the stomach from approximately 150 patients treated continuously with lansoprazole for at least one year did not show evidence of ECL cell effects similar to those seen in rat studies. Longer term data are needed to rule out the possibility of an increased risk of the development of gastric tumors in patients receiving long-term therapy with lansoprazole. Other Gastric Effects In HumansLansoprazole did not significantly affect mucosal blood flow in the fundus of the stomach. Due to the normal physiologic effect caused by the inhibition of gastric acid secretion, a decrease of about 17% in blood flow in the antrum, pylorus, and duodenal bulb was seen. Lansoprazole significantly slowed the gastric emptying of digestible solids. Lansoprazole increased serum pepsinogen levels and decreased pepsin activity under basal conditions and in response to meal stimulation or insulin injection. As with other agents that elevate intragastric pH, increases in gastric pH were associated with increases in nitrate-reducing bacteria and elevation of nitrite concentration in gastric juice in patients with gastric ulcer. No significant increase in nitrosamine concentrations was observed.Serum Gastrin EffectsIn over 2,100 patients, median fasting serum gastrin levels increased 50% to 100% from baseline but remained within normal range after treatment with 15 to 60 mg of oral lansoprazole. These elevations reached a plateau within two months of therapy and returned to pretreatment levels within four weeks after discontinuation of therapy.Endocrine EffectsHuman studies for up to one year have not detected any clinically significant effects on the endocrine system. Hormones studied include testosterone, luteinizing hormone (LH), follicle stimulating hormone (FSH), sex hormone binding globulin (SHBG), dehydroepiandrosterone sulfate (DHEA-S), prolactin, cortisol, estradiol, insulin, aldosterone, parathormone, glucagon, thyroid stimulating hormone (TSH), triiodothyronine (T3), thyroxine (T4), and somatotropic hormone (STH). Lansoprazole in oral doses of 15 to 60 mg for up to one year had no clinically significant effect on sexual function. In addition, lansoprazole in oral doses of 15 to 60 mg for two to eight weeks had no clinically significant effect on thyroid function.In 24-month carcinogenicity studies in Sprague-Dawley rats with daily lansoprazole dosages up to 150 mg/kg, proliferative changes in the Leydig cells of the testes, including benign neoplasm, were increased compared to control rates; these findings are rat specific.Other EffectsNo systemic effects of lansoprazole on the central nervous system, lymphoid, hematopoietic, renal, hepatic, cardiovascular or respiratory systems have been found in humans. Among 56 patients who had extensive baseline eye evaluations, no visual toxicity was observed after lansoprazole treatment (up to 180 mg/day) for up to 58 months.After lifetime lansoprazole exposure in rats, focal pancreatic atrophy, diffuse lymphoid hyperplasia in the thymus and spontaneous retinal atrophy were seen.CLINICAL STUDIESErosive EsophagitisA multicenter, double-blind, two-period placebo-controlled, pharmacodynamic study was conductedto assess the ability of PREVACID I.V. for Injection to maintain gastric acid suppression in patients switched from the oral dosage form of lansoprazole to the intravenous dosage form. Erosive esophagitis patients (n=87; 18 to 78 years of age; 28 female; 69 Caucasian/non-Hispanic, 14 Hispanic, 3 African-American, and 1 Native American) received 30 mg of oral lansoprazole for 7 days in Period 1. Patients were then immediately switched to receive either 30 mg of intravenous lansoprazole or intravenous placebo (normal saline) for 7 days in Period 2. MAO and BAO were determined 21 hours following the last dose of oral medication and the last dose of intravenous administration. MAO was calculated from two hours of continuous collection of gastric contents following a subcutaneous injection of 6.0 μg/kg of pentagastrin. BAO was calculated from one hour of continuous collection of gastric contents.This study demonstrated that, after seven days of repeated oral administration followed by 7 days of intravenous administration, the oral and intravenous dosage forms of PREVACID were similar in their ability to suppress MAO and BAO in patients with erosive esophagitis (refer to Table 3). Also, patients receiving oral PREVACID, who were switched to intravenous placebo, experienced a significant increase in acid output within 48 hours of their last oral dose.Table 3: Acid Output (mEq/h) in Erosive Esophagitis PatientsPREVACID Oral PREVACID I.V. Placebo I.V.(last oral dose) (last I.V. dose) (last I.V. dose)Maximum Acid Output (Median) 7.16n=807.64n=5626.90**n=17Basal Acid Output (Median) 0.77n=810.51n=553.19*n=16*, ** Significantly different from PREVACID I.V. at p=0.005 and p<0.001 levels, respectivelyINDICATIONS AND USAGEWhen patients are unable to take the oral formulations, PREVACID I.V. for Injection is indicated as an alternative for the short-term treatment (up to 7 days) of all grades of erosive esophagitis. Once the patient is able to take medications orally, therapy can be switched to an oral formulation of PREVACID for a total of 6 to 8 weeks. The safety and efficacy of PREVACID I.V. for Injection as an initial treatment of erosive esophagitis have not been demonstrated. Refer to full prescribing information for the oral formulations of PREVACID.CONTRAINDICATIONSPREVACID I.V. for Injection is contraindicated in patients with known severe hypersensitivity to any component of the formulation.PRECAUTIONSGeneralSymptomatic response to therapy with lansoprazole does not preclude the presence of gastric malignancy.Treatment with PREVACID I.V. for Injection should be discontinued as soon as the patient is able to resume treatment with PREVACID oral formulations.Drug InteractionsLansoprazole is metabolized through the cytochrome P450 system, specifically through the CYP3A and CYP2C19 isozymes. Studies have shown that lansoprazole does not have clinically significant interactions with other drugs metabolized by the cytochrome P450 system, such as warfarin, antipyrine, indomethacin, ibuprofen, phenytoin, propranolol, prednisone, diazepam, or clarithromycin in healthy subjects. These compounds are metabolized through various cytochrome P450 isozymes including CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A. When lansoprazole was administered concomitantly with theophylline (CYP1A2, CYP3A), a minor increase (10%) in the clearance of theophylline was seen. Because of the small magnitude and the direction of the effect on theophylline clearance, this interaction is unlikely to be of clinical concern. Nonetheless, individual patients may require additional titration of their theophylline dosage when lansoprazole is started or stopped to ensure clinically effective blood levels.In a study of healthy subjects neither the pharmacokinetics of warfarin enantiomers nor prothrombin time were affected following single or multiple 60 mg doses of lansoprazole. However, there have been reports of increased International Normalized Ratio (INR) and prothrombin time in patients receiving proton pump inhibitors, including lansoprazole, and warfarin concomitantly. Increases in INR and prothrombin time may lead to abnormal bleeding and even death. Patients treated with proton pump inhibitors and warfarin concomitantly may need to be monitored for increases in INR and prothrombin time.Concomitant administration of lansoprazole and tacrolimus may increase whole blood levels of tacrolimus, especially in transplant patients who are intermediate or poor metabolizers of CYP2C19.Lansoprazole causes a profound and long-lasting inhibition of gastric acid secretion; therefore, it is theoretically possible that lansoprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (eg, ketoconazole, ampicillin esters, iron salts, digoxin). Carcinogenesis, Mutagenesis, Impairment of FertilityIn two 24-month carcinogenicity studies, Sprague-Dawley rats were treated with oral lansoprazole doses of 5 to 150 mg/kg/day - about 1 to 40 times the exposure on a body surface (mg/m2) basis of a 50-kg person of average height [1.46 m2 body surface area (BSA)] given the recommended human dose of 30 mg/day. Lansoprazole produced dose-related gastric enterochromaffin-like (ECL) cell hyperplasia and ECL cell carcinoids in both male and female rats. It also increased the incidence of intestinal metaplasia of the gastric epithelium in both sexes. In male rats, lansoprazole produced a dose-related increase of testicular interstitial cell adenomas. The incidence of these adenomas in rats receiving doses of 15 to 150 mg/kg/day (4 to 40 times the recommended human dose based on BSA) exceeded the low background incidence (range = 1.4 to 10%) for this strain of rat.In a 24-month carcinogenicity study, CD-1 mice were treated orally with doses of 15 to600 mg/kg/day, 2 to 80 times the recommended human dose based on BSA. Lansoprazole produced a dose-related increased incidence of gastric ECL cell hyperplasia. It also produced an increased incidence of liver tumors (hepatocellular adenoma plus carcinoma). The tumor incidences in male mice treated with 300 and 600 mg/kg/day (40 to 80 times the recommended human dose based on BSA) and female mice treated with 150 to 600 mg/kg/day (20 to 80 times the recommended human dose based on BSA) exceeded the ranges of background incidences in historical controls for this strainof mice. Lansoprazole treatment produced adenoma of rete testis in male mice receiving 75 to600 mg/kg/day (10 to 80 times the recommended human dose based on BSA).A 26-week p53 (+/-) transgenic mouse carcinogenicity study was not positive.Lansoprazole was not genotoxic in the Ames test, the ex vivo rat hepatocyte unscheduled DNA synthesis (UDS) test, the in vivo mouse micronucleus test, or the rat bone marrow cell chromosomal aberration test. It was positive in in vitro human lymphocyte chromosomal aberration assays.Lansoprazole at intravenous doses of up to 30 mg/kg/day (approximately 8 times the recommended human dose based on BSA) was found to have no effect on fertility and reproductive performance in male and female rats.Pregnancy: Teratogenic EffectsPregnancy Category BTeratology studies have been conducted in rats and rabbits using intravenous lansoprazole doses of up to 30 mg/kg/day (approximately 8 times in rats and 16 times in rabbits of the recommended human dose based on BSA). Treatment with lansoprazole did not result in any impairment of fertility or harm to the fetus.However, there are no adequate and well-controlled studies in pregnant women using the intravenous route. Because animal reproduction studies are not always predicative of human response, PREVACID I.V. for Injection should be used during pregnancy only if clearly needed.Nursing MothersLansoprazole or its metabolites are excreted in the milk of rats. It is not known whether lansoprazole is excreted in human milk. Because many drugs are excreted in human milk, because of the potential for serious adverse reactions in nursing infants from lansoprazole, and because of the potential for tumorigenicity shown for lansoprazole in rodent carcinogenicity studies, a decision should be made whether to discontinue nursing or to discontinue PREVACID I.V. for Injection, taking into accountthe importance of PREVACID I.V. for Injection to the mother.Pediatric UseThe safety and effectiveness of PREVACID I.V. for Injection have not been established for pediatric patients. For further information, please see the PREVACID package insert for the oral formulations.Use in WomenAmong intravenous PREVACID treated subjects, similar percentages of adverse events were reported in males and females.Over 4,000 women were treated with oral PREVACID. Ulcer healing rates in females were similar to those in males. The incidence rates of adverse events in females were also similar to those seen in males.Use in Geriatric PatientsData in elderly patients administered intravenous lansoprazole is limited; however, with oral lansoprazole, ulcer healing rates in elderly patients are similar to those in a younger age group. The incidence rates of PREVACID-associated adverse events and laboratory test abnormalities are similar to those seen in younger patients. For geriatric patients, dosage and administration of PREVACID need not be altered for a particular indication.ADVERSE REACTIONSClinical Safety Experience with PREVACID I.V. for InjectionMore than 1,000 patients and subjects have participated in domestic and foreign clinical trials. Treatment with PREVACID I.V. for Injection was well-tolerated.In four U.S. trials involving 161 subjects exposed to PREVACID I.V. for Injection, the following treatment-related adverse events were reported in >1% of subjects: headache (1.0%), injection site pain (1.0%), injection site reaction (1.0%) and nausea (1.3%). Treatment-related adverse events occurring in less than 1% of subjects included abdominal pain, vasodilatation, diarrhea, dyspepsia, vomiting, dizziness, paresthesia, rash, and taste perversion. No additional adverse drug reactions were reported with the intravenous formulation that had not been reported previously with the oral formulations.Clinical Safety Experience with Oral Formulations of PREVACIDWorldwide, over 10,000 patients have been treated with oral PREVACID in Phase 2 or Phase3 clinical trials involving various dosages and durations of treatment. In general, PREVACID treatment has been well-tolerated in both short-term and long-term trials.The following adverse events were reported by the treating physician to have a possible or probable relationship to drug in 1% or more of PREVACID-treated patients and occurred at a greater rate in PREVACID-treated patients than placebo-treated patients in Table 4.Table 4: Incidence of Possibly or Probably Treatment-Related Adverse Events in Short-Term,Placebo-Controlled PREVACID StudiesBody System/Adverse Event PREVACIDOral(N= 2768)%Placebo(N= 1023)%Body as a WholeAbdominal Pain Digestive SystemConstipation DiarrheaNausea 2.11.03.81.31.20.42.31.2Headache was also seen at greater than 1% incidence but was more common on placebo. The incidence of diarrhea was similar between patients who received placebo and patients who received 15 mg and 30 mg of PREVACID, but higher in the patients who received 60 mg of PREVACID (2.9%, 1.4%, 4.2%, and 7.4%, respectively).Additional adverse experiences occurring in less than 1% of patients or subjects who received PREVACID in domestic trials are shown below:Body as a Whole - abdomen enlarged, allergic reaction, asthenia, back pain, candidiasis, carcinoma, chest pain (not otherwise specified), chills, edema, fever, flu syndrome, halitosis, infection (not otherwise specified), malaise, neck pain, neck rigidity, pain, pelvic pain; Cardiovascular System - angina, arrhythmia, bradycardia, cerebrovascular accident/cerebral infarction, hypertension/ hypotension, migraine, myocardial infarction, palpitations, shock (circulatory failure), syncope, tachycardia, vasodilation; Digestive System - abnormal stools, anorexia, bezoar, cardiospasm, cholelithiasis, colitis, dry mouth, dyspepsia, dysphagia, enteritis, eructation, esophageal stenosis, esophageal ulcer, esophagitis, fecal discoloration, flatulence, gastric nodules/fundic gland polyps, gastritis, gastroenteritis, gastrointestinal anomaly, gastrointestinal disorder, gastrointestinal hemorrhage, glossitis, gum hemorrhage, hematemesis, increased appetite, increased salivation, melena, mouth ulceration, nausea and vomiting, nausea and vomiting and diarrhea, gastrointestinal moniliasis, rectal disorder, rectal hemorrhage, stomatitis, tenesmus, thirst, tongue disorder, ulcerative colitis, ulcerative stomatitis; Endocrine System - diabetes mellitus, goiter, hypothyroidism; Hemic and Lymphatic System - anemia, hemolysis, lymphadenopathy; Metabolic and Nutritional Disorders -avitaminosis, gout, dehydration, hyperglycemia/hypoglycemia, peripheral edema, weight gain/loss; Musculoskeletal System - arthralgia, arthritis, bone disorder, joint disorder, leg cramps,musculoskeletal pain, myalgia, myasthenia, ptosis, synovitis; Nervous System - abnormal dreams, agitation, amnesia, anxiety, apathy, confusion, convulsion, dementia, depersonalization, depression, diplopia, dizziness, emotional lability, hallucinations, hemiplegia, hostility aggravated, hyperkinesia, hypertonia, hypesthesia, insomnia, libido decreased/increased, nervousness, neurosis, paresthesia, sleep disorder, somnolence, thinking abnormality, tremor, vertigo; Respiratory System - asthma, bronchitis, cough increased, dyspnea, epistaxis, hemoptysis, hiccup, laryngeal neoplasia, lung fibrosis, pharyngitis, pleural disorder, pneumonia, respiratory disorder, upper respiratoryinflammation/infection, rhinitis, sinusitis, stridor; Skin and Appendages -acne, alopecia, contact dermatitis, dry skin, fixed eruption, hair disorder, maculopapular rash, nail disorder, pruritus, rash, skin carcinoma, skin disorder, sweating, urticaria; Special Senses -abnormal vision, amblyopia, blepharitis, blurred vision, cataract, conjunctivitis, deafness, dry eyes, ear/eye disorder, eye pain, glaucoma, otitis media, parosmia, photophobia, retinal degeneration/disorder, taste loss, taste perversion, tinnitus, visual field defect; Urogenital System - abnormal menses, breast enlargement, breast pain, breast tenderness, dysmenorrhea, dysuria, gynecomastia, impotence, kidney calculus, kidney pain, leukorrhea, menorrhagia, menstrual disorder, penis disorder, polyuria, testis disorder, urethral pain, urinary frequency, urinary retention, urinary tract infection, urinary urgency, urination impaired, vaginitis.PostmarketingAdditional adverse experiences have been reported since oral PREVACID has been marketed. The majority of these cases are foreign-sourced and a relationship to PREVACID has not been established. Because these events were reported voluntarily from a population of unknown size, estimates of frequency cannot be made. These events are listed below by COSTART body system.Body as a Whole –anaphylactic/anaphylactoid reactions; Digestive System - hepatotoxicity, pancreatitis, vomiting; Hemic and Lymphatic System - agranulocytosis, aplastic anemia, hemolytic anemia, leukopenia, neutropenia, pancytopenia, thrombocytopenia, and thrombotic thrombocytopenic purpura; Musculoskeletal System – myositis; Skin and Appendages – severe dermatologic reactions including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (some fatal); Special Senses -speech disorder; Urogenital System – interstitial nephritis, urinary retention.。
兰索拉唑说明书 - 常州四药
通用名称：注射用兰索拉唑英文名称：Lansoprazole for Injection汉语拼音：Zhusheyong Lansuolazuo【成份】本品主要成份为兰索拉唑，化学名称为2-[[[3-甲基-4-（2,2,2-三氟乙氧基）-2-吡啶基]甲基]亚硫酰基]苯并咪唑。
分子式：C16H14F3N3O2S分子量：369.37辅料为：甘露醇、聚乙二醇400、氢氧化钠。
【性状】本品为白色或类白色疏松块状物或粉末。
【适应症】用于口服疗法不适用的伴有出血的十二指肠溃疡。
【规格】30mg【用法用量】静脉滴注。
通常成年人每次30mg，一日2次，疗程不超过7天。
一旦患者可以口服药物，应改换为兰索拉唑口服剂型。
临用前将瓶中内容物用5毫升灭菌注射用水溶解，再用100毫升0.9%氯化钠注射液稀释，静脉滴注，推荐给药时间不少于30min。
使用时注意：(1)本品静滴使用时应配有孔径为1.2μm的过滤器，以便去除输液过程中可能产生的沉淀物。
这些沉淀物有可能引起小血管栓塞而产生严重后果。
(2)在喷出性或涌出性大量出血、血管暴露等危险性大的情况下，应先采用内窥镜下止血措施。
(3)本品仅用于静脉滴注。
溶解后应尽快使用，勿保存。
避免与0.9% 氯化钠注射液以外的液体和其他药物混合静滴。
(4)经本品治疗的前3日内达到止血效果的，应改用口服用药，不可无限制静脉给药。
【不良反应】国内临床研究中，本品一日2次，每次30mg静脉滴注，5天疗程。
109例受试者中发生7例(6.25%)不良反应，分别是白细胞减少、过敏、药疹和头晕。
国外上市后超过1000名患者使用注射用兰索拉唑后有较好的耐受性。
在美国4个临床试验中有161名患者使用注射用兰索拉唑，超过1% 的不良反应有恶心(1.3%)、头痛(1%)、注射部位痛感(1%)；低于1% 的不良反应有腹痛、腹泻、消化不良、呕吐、头晕、感觉异常、味觉异常、皮疹和血管扩张。
未见与口服给药不同的不良反应。
日本221例受试者使用注射用兰索拉唑的临床研究资料报道，发生31例(14.0%)临床实验室检查值异常，主要为丙氨酸氨基转移氨酶(ALT)升高(6.2%)、天门冬氨酸氨基转移酶(AST)升高(5.7%)、乳酸脱氢酶(LDH)升高(2.0%)、γ-谷氨酰转移酶(γ-GGT)升高(1.5%)等。
- 1、下载文档前请自行甄别文档内容的完整性，平台不提供额外的编辑、内容补充、找答案等附加服务。
- 2、"仅部分预览"的文档,不可在线预览部分如存在完整性等问题,可反馈申请退款(可完整预览的文档不适用该条件!)。
- 3、如文档侵犯您的权益，请联系客服反馈,我们会尽快为您处理(人工客服工作时间：9:00-18:30)。
产品简介：通用名：注射用兰索拉唑
商品名：奥维加
英文名：lansoprazole for Injection
汉语拼音：Zhusheyong Lansuolazuo
主要成分及化学名称为：2-[[[3-甲基-4-（2,2,2-三氟乙氧基）-2-吡啶基]甲基]亚磺酰基-1H-苯并咪唑]
化学结构式：
分子式：C16H14F3N3O2S
分子量：369.36
辅料为甘露醇，用适量氢氧化钠调节PH值。
【性状】本品为白色或类白色疏松块状物及粉末。
【适应症】用于口服疗法不适用的伴有出血的十二指肠溃疡。
【规格】30mg。
【用法用量】
静脉滴注：通常成年人一次30mg，用0.9%氯化钠注射液100ml 溶解后，一日2次，推荐静滴时间30分钟，疗程不超过7天。
使用时注意：
（1）本品配有孔径1.2um的过滤输液器。
（2）在喷出性或涌出性大量出血、血管暴露等危险性大的情况下，应该采用内窥镜下止血措施。
（3）本品仅用于静脉滴注。
溶解后应尽快使用，勿保存。
避免与0.9%氯化钠注射液以外的液体和其他药物混合静滴。
【不良反应】国内临床研究中，本品一日2次，每次30mg 静脉滴注，5天疗程。
127例受试者中发生4例（3.64%）不良反应，主要是白细胞减少（1.82%）、转氨酶轻度升高（0.91%）和皮疹（0.91%）。
白细胞减少者一周后复查正常，转氨酶轻度升高者十天后复查正常。
国外上市后超过1000名患者使用注射用兰索拉唑后有较好的耐受性，在美国4个临床试验中有161名患者使用注射用兰索拉唑，超过1%的不良反应有恶心(1.3%)，头痛(1.0%),注射部位痛感(1.0%)；低于1%的不良反应有腹痛、腹泻、消化不良、呕吐、头晕、感觉异常、味觉异常、皮疹和血管扩张。
未见与口服给药不同的不良反应。
【包装】1瓶/盒。