奥美拉唑说明书.doc

奥美拉唑说明.doc 注射用奥美拉唑说明书 【 药品名称 】 注射用奥美拉唑钠 【 英文名称 】 Omeprazole Sodium for Injection 【 药品别名 】 奥克? 本品主要成份为:奥美拉唑钠，其化学名称为:5-甲氧基-2-,[(4-甲氧基-3, 5-二甲基-2-吡啶基)-甲基]-亚磺酰基,-1H-苯并咪唑钠盐一水合物。 【 性状 】 本品为白色疏松块状物或粉末，专用溶剂为无色的透明液体。 【 药理毒理 】 本品为胃壁细胞质子泵抑制剂，能特异性地抑制壁细胞顶端膜构成的分泌性微管和胞浆内的管状泡上的H+、K+-ATP酶，从而有效地抑制胃酸的分泌。由于H+、K+-ATP酶是壁细胞泌酸的最后一个过程，故本品抑酸能力强大。它不仅能非竞争性抑制促胃液素、组胺、胆碱及食物、刺激迷走神经等引起的胃酸分泌，而且能抑制不受胆碱或H2受体阻断剂影响的部分基础胃酸分泌，对H2受体拮抗剂不能抑制的由二丁基环腺苷酸(DCAMP)刺激引起的胃酸分泌也有强而持久的抑制作用。本品对胃蛋白酶分泌也有抑制作用，对胃黏膜血流量改变不明显，也不影响体温、胃腔温度、动脉血压、静脉血红蛋白、动脉氧分压、二氧化碳分压及动脉血pH。 【 药代动力学 】 静脉注射本品后，体内分布在肝、肾、胃、十二指肠、甲状腺等组织，分布容积为0.19,0.48L/kg，与细胞外液体积相当。T1/2为0.5,1小时，慢性肝病患者为3小时。本品主要在肝脏中经细胞色素P450代谢，代谢产物主要为硫醚、砜和羟基衍生物。对胃酸的分泌无作用，代谢完全，仅少数以原形排泄。约有80%的代谢物经肾排出，部分(18,23%)随粪便排出。有肠肝循环过程，血浆蛋白结合率高，达95%左右。肾衰患者对本品的清除无明显变化，肝功能受损者清除半衰期可有延长。 【 适应症 】 主要用于:(1)消化性溃疡出血、吻合口溃疡出血。(2)应激状态时并发的急性胃黏膜损害，和非甾体类抗炎药引起的急性胃黏膜损伤;(3)亦常用于预防重症疾病(如脑出血、严重创伤等)胃手术后预防再出血等;(4)全身麻醉或大手术后以及衰弱昏迷患者防止胃酸反流合并吸入性肺炎。 【 用法用量 】 静脉推注。一次40mg(一瓶冻干粉),每日1,2次。临用前将10ml专用溶剂注入冻干粉小瓶内，禁止用其它溶剂溶解。本品溶解后必须在2小时内使用，推注时间为2.5~4分钟。 【 不良反应 】 偶可见有一过性的轻度恶心、腹泻、腹痛、感觉异常、头晕或头痛等，但不影响治疗。 【 禁忌 】 对本品过敏者禁用。 【 】 1.本品抑制胃酸分泌的作用强，时间长，故应用本品时不宜同时再服用其它抗酸剂或抑酸剂。为防止抑酸过分，在一般消化性溃疡等病时，不建议大剂量长期应用(卓-艾综合征例外)。 2. 因本品能显著升高胃内pH，可能影响许多药物的吸收。 3.肾功能受损者不须调整剂量;肝功能受损者需要酌情减量。 4.治疗胃溃疡时应排除胃癌后才能使用本品，以免延误诊断和治疗。 5.动物实验中，长期大量使用本品后，观察到高胃泌素血症及继发胃ECL-细胞增大和良性肿瘤的发生，这种变化在应用其它抑酸剂及施行胃大部切除术后亦可出现。 【 孕妇及哺乳期妇女用药 】 尽管动物实验未发现本品对妊娠期和哺乳期有不良作用，或对胎儿有毒性或致畸作用，但建议妊娠期和哺乳期妇女尽可能不用。 【 儿童用药 】 目前尚无儿童使用本品的经验。 【 老年患者用药 】 老年患者无需调整剂量。 【 药物相互作用 】 1.本品可延长地西泮、苯妥英钠及其他经肝氧代谢药物的药效，如本品与苯妥英钠合用，则需小心监测病情，且苯妥英钠应酌情减量。 2.与经细胞色素P450酶系统代谢的药物(如华法林)可能有相互作用。 【 药物过量 】 临床试验中，本品静脉给药一天累积剂量达270mg和三天达650mg，并未出现剂量相关性不良反应。 【 规格 】 奥美拉唑钠42.6mg，相当于奥美拉唑40mg。 The Package Insert of Omeprazole Sodium for Injection [Drug name] Common name: Omeprazole Sodium for Injection Chinese Pinyin: Zhu Sheyong Aomeilazuona Ingredients: Omeprazole Sodium, whose chemical name is 5-methoxy-2-{[4-methoxy-3, 5-dimethyl-2-pyridyl-methyl]-sulphony}-1H-benzimidazolesodrum salt-Hydrate Molecular Formula: C17H18N3NaO3S-H2O Molecular Weight: 385.41 [Description] White loose lump or powder, the specific solvent is achromatic transparent liquid. [Pharmacology & toxicology] This product is a proton pump inhibitor of parietal cell. It effectively inhibits the secretion of gastric acid by imposing specific inhibiting effect on the proton pump of the tubular reside of cytoplasm and secretory canaliculus which are formed by arpical membrane of parietal cell. As the proton pump is involved in the last process when gastric -.cid is secreted by parietal cell, it displays strong and non-competitive potency against the secretion of gastric acid caused by pepsin, histamine, choline, food and stimulation of vagus nerve. Also, it has immense effect on part of the basic secretion of gastric acid which process is free of the impact of choline and H2-receptor blocker. Besides, it has a lasting and powerful inhibiting effect on the acid secretion stimulated by Dibutylcyclic adenosine monophosphate (DcAMP) which process cannot be inhibited by H2-receptor antagonist. Additionally, it can inhibit the secretion of pepsin while showing little impact on the blood flow of mucous membrane, as well as body temperature, the temperature of gastral cavity, arterial blood pressure, venous hemoglobin, arterial partial pressure of oxygen, the partial pressure of carbon dioxide and PH of arterial blood. [Pharmacokinetics] When injected intravenously, the drug is distributed among the tissues of liver, kidney, stomach, duodenum and thyroid gland with its distribution volume at 0.19-0.48 L/Kg, equivalent to the volume of extracelluar fluid. Its half life is 0.5-1 hour and 3 hours for chronic hepatopath. Most of its metabolic processes take place in the liver by cytochrome P450. its metabolites are mainly thioether, salphone and hydroxyl derivate, which have no effect on the secretion of gastric acid and its complete metabolism eaves very small percentage of the drug excreted in its original shape. About 80% of metabolites are excreted by kidney while another 18%~20% along with feces. It has high affinity rate for plasma protein which reaches 95% and enterohepatic circulation. There is no evident change in drug elimination for patients with renal failure while the half-life of elimination may be prolonged for the patients who are suffering from impairment of liver function. [Indication] 1. hemorrhage of peptic ulcer and marginal ulcer 2. Impairment of acute gastric mucous membrane complicated in the stress state, or triggered by non-steroids anti-inflammatory agents. 3. Prevention of rehemorrhage after operation for glare disease, e.g. cerebral hemorrhage, severe trauma. 4. Prevention of regurgitation of gastric acid reflux associated aspiratory pneumonia for patients who have gone through general anesthesia or major operation or who are in hypothetic narcosis. [Dosage and usage] This injection is administered by intravenous injection. It should be given to the patience once or twice per day and 40mg for each time. Inject 10 ml special solvent into vials for lyophilized powder before administrating, other solvent excluded. The drug must be used in 2 hours after distribution and the time of bolus should be no less than 20 minutes. [Adverse reaction] Slight nausea, diarrhea, bellyache, paraesthesia, swirl and headache may occur occasionally but the treatment will not be affected. [Contradiction] Do not administer this product to those who are hypersensitive to it. [Precautions] 1. As this has long and powerful inhibiting effect on the secretion of gastric acid, it is not appropriate to use it along with other anti-acid agents or acid –inhibiting agents. It is recommended that this product should not be used at a high dosage over a long period of time for the ordinary digestive ulcer except Zollinger-Ellison Syndrome. 2. It may affect the absorption of medicines because of its significant effect on raising PH in stomach. 3. Adjustment of dosages is not necessary for patients with impaired renal function but reduction in dosage is necessary for those with impaired liver function. 4. The possibility of Carcinoma Ventriculi must be precluded before administering this for the treatment of gastric ulcer in case any delay in diagnosis and treatment may occur. 5. The zoopery revealed that high-dosage and chronic administering of this drug, hypergastrinemia, secondary gastric ECL-cell inflation and benign tumor are observed which also occur after using other administration of other anti-acid agents and operations of partial gastrectomy. [Usage during the pregnancy and suckling period] t is recommended that women in pregnancy and lactation avoid this product, although no adverse reaction related to pregnancy and lactation and no toxicity and teratogenesis for fetus are found in zoopery. [Usage for children] The experience of administration for children is limited. [Drug interaction] 1. The effect of this drug is prolonged when administered along with diazepam, phenytoinum and other drugs metabolized via liver. For instance, when used with phenytoinum, patients’ condition should be monitored with great care and less phenytoinum should be used according to the condition of the patients. 2. Interaction may be involved when used with drugs metabolized via cytochrome P450 enzyme system, such as warfarin. [Over dosage] According to the clinical trial, no dosage-related adverse reaction arises when the drug is administered intravenously 270mg in one day or 650 in three days. [Specification] 40mg [Storage] preserved in well closed containers, and stored in a cool and dry place [Package] This product should be packaged in glass tube antibiotic vial with closure made of butyl rubber for pharmaceutical use. [Registered number of approval] state drug permit Doc(SDPD) H [ validity] 24 months