奥美拉唑说明书

1、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】OmeprazoleSodiumforInjection【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）-甲基卜亚磺酰基-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

2、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0.190.48L/kg,与细胞外液体积相当。T1/2为0.51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

3、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（1823%）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（瓶冻干粉），每日12次。临用前将10ml专用溶剂注入冻干粉小瓶内，禁止用其它溶

4、剂溶解。本品溶解后必须在2小时内使用，推注时间为2.54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。【注意事项】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）。因本品能显著升高胃内pH，可能影响许多药物的吸收。肾功能受损者不须调整剂量；肝功能受损者需要酌情减量。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。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

5、，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,并未岀现剂量相关性不良反应。【规格】奥美拉唑钠4

6、2.6mg,相当于奥美拉唑40mg。ThePackageInsertofOmeprazoleSodiumforInjectionDrugnameCommonname:OmeprazoleSodiumforInjectionChinesePinyin:ZhuSheyongAomeilazuonaIngredients:OmeprazoleSodium,whosechemicalnameis5-methoxy-2-4-methoxy-3,5-dimethyl-2-pyridyl-methyl-sulphony-1H-benzimidazolesodrumsalt-HydrateMolecularF

7、ormula:C17H18N3NaO3S-H2OMolecularWeight:385.41DescriptionWhitelooselumporpowder,thespecificsolventisachromatictransparentliquid.Pharmacology&toxicologyThisproductisaprotonpumpinhibitorofparietalcell.Iteffectivelyinhibitsthesecretionofgastricacidbyimposingspecificinhibitingeffectontheprotonpumpofthet

8、ubularresideofcytoplasmandsecretorycanaliculuswhichareformedbyarpicalmembraneofparietalcell.Astheprotonpumpisinvolvedinthelastprocesswhengastric-.cidissecretedbyparietalcell,itdisplaysstrongandnon-competitivepotencyagainstthesecretionofgastricacidcausedbypepsin,histamine,choline,foodandstimulationof

9、vagusnerve.Also,ithasimmenseeffectonpartofthebasicsecretionofgastricacidwhichprocessisfreeoftheimpactofcholineandH2-receptorblocker.Besides,ithasalastingandpowerfulinhibitingeffectontheacidsecretionstimulatedbyDibutylcyclicadenosinemonophosphate(DcAMP)whichprocesscannotbeinhibitedbyH2-receptorantago

10、nist.Additionally,itcaninhibitthesecretionofpepsinwhileshowinglittleimpactonthebloodflowofmucousmembrane,aswellasbodytemperature,thetemperatureofgastralcavity,arterialbloodpressure,venoushemoglobin,arterialpartialpressureofoxygen,thepartialpressureofcarbondioxideandPHofarterialblood.Pharmacokinetics

11、Wheninjectedintravenously,thedrugisdistributedamongthetissuesofliver,kidney,stomach,duodenumandthyroidglandwithitsdistributionvolumeat0.19-0.48L/Kg,equivalenttothevolumeofextracelluarfluid.Itshalflifeis0.5-1hourand3hoursforchronichepatopath.MostofitsmetabolicprocessestakeplaceintheliverbycytochromeP

12、450.itsmetabolitesaremainlythioether,salphoneandhydroxylderivate,whichhavenoeffectonthesecretionofgastricacidanditscompletemetabolismeavesverysmallpercentageofthedrugexcretedinitsoriginalshape.About80%ofmetabolitesareexcretedbykidneywhileanother18%20%alongwithfeces.Ithashighaffinityrateforplasmaprot

13、einwhichreaches95%andenterohepaticcirculation.Thereisnoevidentchangeindrugeliminationforpatientswithrenalfailurewhilethehalf-lifeofeliminationmaybeprolongedforthepatientswhoaresufferingfromimpairmentofliverfunction.IndicationhemorrhageofpepticulcerandmarginalulcerImpairmentofacutegastricmucousmembra

14、necomplicatedinthestressstate,ortriggeredbynon-steroidsanti-inflammatoryagents.Preventionofrehemorrhageafteroperationforglaredisease,e.g.cerebralhemorrhage,severetrauma.Preventionofregurgitationofgastricacidrefluxassociatedaspiratorypneumoniaforpatientswhohavegonethroughgeneralanesthesiaormajoropera

15、tionorwhoareinhypotheticnarcosis.DosageandusageThisinjectionisadministeredbyintravenousinjection.Itshouldbegiventothepatienceonceortwiceperdayand40mgforeachtime.Inject10mlspecialsolventintovialsforlyophilizedpowderbeforeadministrating,othersolventexcluded.Thedrugmustbeusedin2hoursafterdistributionan

16、dthetimeofbolusshouldbenolessthan20minutes.AdversereactionSlightnausea,diarrhea,bellyache,paraesthesia,swirlandheadachemayoccuroccasionallybutthetreatmentwillnotbeaffected.ContradictionDonotadministerthisproducttothosewhoarehypersensitivetoit.PrecautionsAsthishaslongandpowerfulinhibitingeffectonthes

17、ecretionofgastricacid,itisnotappropriatetouseitalongwithotheranti-acidagentsoracid-inhibitingagents.ItisrecommendedthatthisproductshouldnotbeusedatahighdosageoveralongperiodoftimefortheordinarydigestiveulcerexceptZollinger-EllisonSyndrome.Itmayaffecttheabsorptionofmedicinesbecauseofitssignificanteff

18、ectonraisingPHinstomach.Adjustmentofdosagesisnotnecessaryforpatientswithimpairedrenalfunctionbutreductionindosageisnecessaryforthosewithimpairedliverfunction.ThepossibilityofCarcinomaVentriculimustbeprecludedbeforeadministeringthisforthetreatmentofgastriculcerincaseanydelayindiagnosisandtreatmentmay

19、occur.Thezooperyrevealedthathigh-dosageandchronicadministeringofthisdrug,hypergastrinemia,secondarygastricECL-cellinflationandbenigntumorareobservedwhichalsooccurafterusingotheradministrationofotheranti-acidagentsandoperationsofpartialgastrectomy.Usageduringthepregnancyandsucklingperiodtisrecommende

20、dthatwomeninpregnancyandlactationavoidthisproduct,althoughnoadversereactionrelatedtopregnancyandlactationandnotoxicityandteratogenesisforfetusarefoundinzoopery.UsageforchildrenTheexperienceofadministrationforchildrenislimited.DruginteractionTheeffectofthisdrugisprolongedwhenadministeredalongwithdiazepam,phenytoinumandotherdrug