52．洛赛克
出处：按学科分类—医药、卫生 军事医学科学出版社《临床常用进口药物手册》第288页（7442字）
【中文释文】：
40mg静脉注射剂(奥美拉唑——阿斯特拉)
洛赛克静脉注射剂：一个硬纸盒内，装有一瓶冻干物质和一支安瓿溶媒。每小瓶含有奥美拉唑钠42．6mg，相当于奥美拉唑40mg，以及调整pH值用的氢氧化钠适量。一支安瓿有10ml溶剂。
〔说明〕
洛赛克(奥美拉唑)借助高选择性的作用机制来降低胃酸的分泌，它对胃壁细胞中的酶H+K+-ATP酶会产生与剂量大小有关的抑制作用。由于此一特殊机制，抑制形成胃酸的最后步骤，因此可有效地抑制基础胃酸及因刺激而产生的胃酸分泌。奥美拉唑对乙酰胆碱受体或组织胺受体不产生任何作用，而且除了已知对酸分泌的作用外，临床上并无其他明显的药代动力学作用。本药作用迅速，且1天1次的剂量对胃酸的分泌可达到可逆性的控制。
〔用途和适应证〕
下列病症无法以口服药物有效治疗时的取代方法：十二指肠溃疡、胃溃疡、返流性食管炎及Zollinger-Ellison症。
〔禁忌证〕
使用洛赛克尚无任何禁忌证。
〔注意事项〕
当怀疑是胃溃疡，而有恶化的可能时，应立即就医，因给予治疗会减轻其症状而延误诊断。
〔孕妇及授乳期妇女的使用〕
如其他的新药，除非必要，洛赛克不应用于怀孕及授乳期的妇女。动物实验中尚无任何证据显示在怀孕及授乳期的动物使用洛赛克会产生胎儿毒性或致畸胎作用。
〔副作用〕
人对洛赛克的耐受性良好，一些临床报告有恶心、头痛、腹泻、便秘及胀气等症状，但相当少见，另有一些病人则有皮肤潮红现象。通常这些症状都是短暂而轻微的，且和治疗没有一定的关联。
〔剂量及用法〕
对于重症病人，口服疗法不适用时，可静脉注射，推荐剂量为洛赛克40mg每天静脉注射1次，胃内酸度立即下降，24h内平均下降90%。
对Zollinger-Ellison综合征病人给药剂量须视个体状况加以调整，或者增高剂量，或者增加给药频率。把本品附带的10ml溶剂完全抽出，然后注入冻干奥美拉唑的小瓶内，溶解后即成静脉注射液，并应在4h内使用。其他溶剂一概不应使用。
洛赛克溶液只供静脉注射用，不应加进其他液体内作静脉点滴输注用。重组后，注射液应缓慢注射，至少2．5min以上，最大注射速率为4ml／min。
〔肝肾功能不全者〕
有肾功能和肝功能障碍的病人亦无须调整剂量。
〔儿童〕
目前尚无儿童使用洛赛克的经验。
〔老年人〕
老年人使用洛赛克并不需要调整剂量。
〔配伍禁忌〕
除本品附带的溶剂外，其他溶剂不得使用。
〔相互作用〕
洛赛克会延长地西泮，华法林及苯妥英等由肝脏氧化代谢的药物的排出，如果病人同时服用华法林或苯妥英，则华法林和苯妥英应予减量，并加以监测。但是，同时以20mg／d的洛赛克治疗，苯妥英的血药浓度并不受影响。与普萘洛尔、美替洛尔、茶碱、利多卡因或奎尼丁并用无相互作用产生。但如合用其他经由细胞色素P450酶系统代谢的药物，仍可能产生相互作用。与制酸剂合用未见相互作用发生。
〔用药过量〕
目前尚无人体使用过量的资料，亦无法提供过量特别的疗法。单一静脉注射剂量达到80mg的量，耐受性非常好。静脉注射剂量达200mg／d和每3d达520mg，不会产生副作用。
〔贮存条件〕
避光于25℃或25℃以下保存。
〔生产厂家〕
瑞典阿斯特拉公司
【外文释文】：
(omeprazole-Astra)
For intravenous injection only
Losec．i．v injection：Combination pack consisting of one vial and one ampoule：Each vial contains omeprazole sodium 42．6 mg equivalent to omeprazole 40 mg and sodium hydroxide q．s．for pH adjustment(pH 12)．Each ampoule contains 10 ml of solvent for reconstitution．
Description
Losec(omeprazole)reduces gastric acid secretion through a highly selective mechanism of action．It produces specific dose dependent inhibition of the enzyme H′，K′-ATPase(the‘proton pump′)in the parietal cell．As this action inhibits the final stage of gastric acid formation，there is effective inhibition of both basal and stimulated acid secretion irrespective of the stimulus to acid formation．Omeparazole has no effect on acetylcholine or histamine receptors and no clinically significant pharmacodynamic effects have been observed other than those explained by the effect of omeprazole on acid secretion．The onset of action is rapid and reversible control of gastric acid secretion is achieved with once daily dosing．
Use／Indications
Losec i．v．injection is indicated for alternative use to oral medication in：duodenal ulcer，gastric ulcer，reflux oesophagitis，Zollinger-Ellison syndrome．
Contraindications
There are no known contraindications to the use of losec．
Precautions
When gastric ulcer is suspected，the possibility of malignancy should be excluded as treatment may alleviate symptoms and delay diagnosis．
Use in pregnancy and lactation
As with all new drugs，losec should not be given during pregnancy and lactation unless its use is considered essential．Animal studies have not shown evidence of any hazard from the administration of losec during pregnancy and lactation and there is no evidence of foetal toxicity or teratogenic effect．
Adverse reactions
Losec is well tolerated．The following events have been reported，but in the great majority of cases a consistent relationship between these events and treatment with omeprazole has not bee established．
Headache，diarrhoea，constipation，abdominal pain，nausea／vomiting and flatulence have been reported at a frequency＞1%by patients treated with omeprazole in clinical trials．
Furthermor，the following events have been reported from marketed use of losec：
Rarely：Rash，urticaria and／or pruritus，dizziness，paraesthesia，somnolence，insomnia，vertigo and malaise．
In isolated cases：Arthralgia，muscular weakness，myalgia，reversible mental confusion，agitation，depression and hallucination(predominantly in severely ill patients)，stomatitis and gastrointestinal candidiasis，increased liver enzymes with or without increased bilirubin values，gynecomastia，leukpenia，thrombocytopenia，peripheral oedema，blurred vision and taste perversion．
Dosage and administration
Losec 40 mg intravenous administration once daily is recommended where oral medication is inappropriate，e．g．in severely ill patients．This produces an immediate decrease in intragastric acidity and a mean decrease over 24 hours of approximatily 90%．
In Zollinger-Ellison syndrome the dosage should be individually adjusted，and higher，more frequent dosing may be indicated．
The i．v．solution is obtained by reconstitution of the lyophilized omeprazole using the solvent provided，and should be used within 4 hours of reconstitution、No other solvent should be used．
Losec solution should be used for i．v．injection only and should not be added to solutions for i．v．infusion．After reconstitution the injection shoud be given slowly over a period of at least 2．5 minutes to a maximum rate of 4 ml per minute．
Impaired renal and liver function
Dose adjustment in patients with impaired renal or liver function is not required．
Children
There is no experience with losec in children．
Elderly
No dose adjustment is necessary in the elderly．
Incompatibilities
Reconstitute using only solvent provided．No other solvents should be used．
Interactions
Losec can prolong the dimination of diazepam，warfarin and phenytoin，drugs that are metabolised by oxidation in the liver．Monitoring of patients also receiving warfarin or phenytioin is recommended and a reduction of the dose of phenytion and warfarin may be necessary．However，concomitant treatment with losec 20 mg daily did not change the blood concentration of phenytion in patients on continuonus treatment with phenytoin．No interaction with propranolol，metoprolol，theophylline，lidocaine or quinidine has been found，but interactions with other drugs also metabolised via the cytochrome P450 enzyme system cannot be excluded．No interaction with concomitantly administered antacids has been found．
Overdosage
There is no information available on the effects of overdosage in man and specific recommendations for treatment cannot be given．
Single i．v．doses of up to 80 mg have been well tolerated．I．V．doses of up to 200 mg on a single day and up to 520 mg over a three day period have been given without adverse effects．
Storage conditions
Protect from light．Store at or below 25℃。
Manufacturer
ASTRA，Sweden．