CYKLOKAPRON

Main information

  • Trade name:
  • CYKLOKAPRON Solution for Injection 500mg/ 5ml MG/ 5ml
  • Dosage:
  • 500mg/ 5ml MG/ 5ml
  • Pharmaceutical form:
  • Solution for Injection
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • CYKLOKAPRON Solution for Injection 500mg/5ml MG/5ml
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0936/008/002
  • Authorization date:
  • 01-04-1998
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Cyklokapron500mg/5ml,Solutionforinjectionorinfusion.

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Each5mlofthesolutioncontains500mgofTranexamicAcid(100mgperml).

Forafulllistofexcipients,seesection6.1.

3PHARMACEUTICALFORM

Solutionforinjectionorinfusion.

Clear,colourless,aqueoussolution.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Localfibrinolysis

Intheshorttermmanagementofhaemorrhageorriskofhaemorrhageinincreasedfibrinolysisorfibrinogenolysis.

Generalfibrinolysis

Inthemanagementofhaemorrhagecomplicationsinassociationwiththrombolytictherapy.

Inthemanagementofhaemorrhageassociatedwithdisseminatedintravascularcoagulationwithpredominantactivation

offibrinolyticsystem.

4.2Posologyandmethodofadministration

Routeofadministration:Intravenous.

Adultsincludingelderly:

Acuteactivationoffibrinolyticmechanisms

Localfibrinolysis

Uppergastrointestinalhaemorrhage

1.0g(2ampoules)byslowintravenousinjectioneverysixhoursforthefirstthreedaysthen1.0to1.5gorallyevery

sixhoursforafurtherthreetofourdays.

Prostatectomy

1.0gbyslowintravenousinfusioneveryeighthoursforthefirstthreedays;thereafter1gthreetofourtimesdailyuntil

macroscopichaematuriaisnolongerpresent.Asabladderwashout,1gisaddedto1000mlofnormalsalinedailyfor

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Epistaxis

Topicalapplicationmaybemadetothenasalmucosaofpatientssufferingfromepistaxis.1gthreetimesdailymaybe

administeredforsevendayswhererecurrentbleedingisanticipated.

Conisationofthecervix

1.5gthreetimesdaily.

Haemophilia

1.0to1.5gevery8hoursinthemanagementofsurgicalproceduresanddentalextractions.

Generalactivationoffibrinolyticmechanisms:

Neutralisationofthrombolytictherapy

10mg/kgbodyweightbyslowintravenousinjection.

Disseminatedintravascularcoagulation(DIC)

Inpatientswithdisseminatedintravascularcoagulation(DIC)treatmentmustberestrictedtothoseinwhomthereis

predominantactivationofthefibrinolyticsystemwithacutebleeding.Characteristically,thehaematologicalprofile

approximatestothefollowing:reducedeuglobulinclotlysistime;prolongedprothrombintime;reducedplasmalevels

offibrinogen;FactorsVandVIII;fibrinolysinandalpha-2macroglobulin;normalplasmalevelsPandPcomplex,i.e.

factorsII(prothrombin),VIIandX,increasedplasmalevelsoffibrinogendegradationproducts;anormalplatelet

count.Theforegoingpresumesthattheunderlyingdiseasestatedoesnotofitselfmodifythevariouselementsinthis

profile.

Insuchacutecasesasingledoseof1gtranexamicacidisfrequentlysufficienttocontrolbleeding.Thefibrinolytic

activityinthebloodwillbereducedforabout4hoursifrenalfunctionisnormal.Anticoagulationwithheparinshould

beinvestigatedinordertopreventfurtherfibrindeposition.

AdministrationofCyklokaproninDICshouldbeconsideredonlywhenappropriatehaematologicallaboratoryfacilities

andexpertiseareavailable.CyklokapronmustnotbeadministeredinDICwithpredominantactivationofthe

coagulationsystem.

Children’sDosage:

Thisshouldbecalculatedaccordingtobodyweightat25mg/kg/dose.

DosageinRenalInsufficiency:

Inpatientswhererenalfunctionisimpaired,thedosageoftranexamicacidshouldbereducedasshownbelow:

Serumcreatinine Dose Dosefrequency

120-250µmol/l 25 mg/kg Twicedaily

250-500µmol/l 25 mg/kg Every24thhour

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4.3Contraindications

Cyklokaproninjectioniscontraindicatedinpatients

withactivethromboembolicdiseasesuchasdeepveinthrombosis.

Withsubarachnoidhaemorrhage.Thelimitedclinicalexperienceshowsthatreducedriskforprebleedingis

offsetbyanincreaseintherateofcerebralischaemia.

Hypersensitivitytotranexamicacidoranycomponentoftheproduct.

4.4Specialwarningsandprecautionsforuse

Inpatientswithrenalinsufficiency,areductionindosageisrecommended(seeSection4.2,Posologyand

Administration)becauseoftheriskofaccumulation.

Tranexamicacidshouldbeusedwithcautioninhaematuriafromtheupperurinarytract(especiallyinhaemophiliacs),

sinceinafewcasesuretericobstructionhasbeenreported.

Rapidintravenousinjectionmaycausedizzinessand/orhypotension.

Patientswithahighriskofthrombosis(apreviousthromboemboliceventandafamilyhistoryofthromboembolic

disease)shoulduseCyklokapronInjectiononlyifthereisastrongmedicalindicationandunderstrictmedical

supervision.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Noneknown.

4.6Fertility,pregnancyandlactation

Tranexamicacidshouldnotbeusedduringpregnancyandinwomenbreastfeedinginfants,unlessconsideredessential

bythephysician.

4.7Effectsonabilitytodriveandusemachines

Noneknown.

4.8Undesirableeffects

Dose-dependantgastrointestinaldiscomfortifthemostcommonlyreportedundesirableeffect,butisusuallyofamild

andtemporarynature.Allergicskinreactionshavebeenreportedasanuncommon,undesirablesideeffect.

Frequencyofundesirableeffectsatadoseof4g/day

Common(>1/100) GI:Nausea,vomiting,diarrhoea

LessCommon(<1/100) Skin:AllergicSkinreactions

PostMarketingSurveillance:

Rarecasesofadverseeventshavebeenreportedwithuseoftranexamicacid;thromboembolicevents,impairedcolour

visionandothervisualdisturbances.

4.9Overdose

Symptomsmaybenausea,vomiting,orthostaticsymptomsand/orhypotension.Maintainahighfluidintaketo

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5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Tranexamicacidisanantifibrinolyticcompoundwhichisapotentcompetitiveinhibitoroftheactivationoffibrinolysin

toplasmin.Atmuchhigherconcentrationsitisanon-competitiveinhibitorofplasmin.Theinhibitoryeffectof

tranexamicacidinfibrinolysinactivationbyurokinasehasbeenreportedtobe6-100timesandbystreptokinase6-40

timesgreaterthanthatofaminocaproicacid.

Theantifibrinolyticactivityoftranexamicacidisapproximatelytentimesgreaterthanthatofaminocaproicacid.

5.2Pharmacokineticproperties

Tranexamicacidadministeredparenterallyisdistributedinatwocompartmentmodel.Tranexamicacidcrossesthe

placenta,andmayreachonehundredthoftheserumpeakconcentrationinthemilkoflactatingwomen.Tranexamic

acidcrossesthebloodbrainbarrier.

Followingintravenousadministration,thebiologicalhalf-lifeoftranexamicacidhasbeendeterminedtobe1.9hoursto

2.7hours.Approximately90%ofanintravenouslyadministeredtranexamicaciddoseisexcreted,largelyunchanged,

intheurinewithin24hours.Theplasmahalf-lifeisapproximately2hours.

5.3Preclinicalsafetydata

Therearenopreclinicaldataofrelevancetotheprescriberwhichareadditionaltothatalreadyincludedinother

sectionsoftheSummaryofProductCharacteristics.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Waterforinjections.

6.2Incompatibilities

Cyklokapronsolutionforinjectionorinfusionshouldnotbeaddedtobloodfortransfusion,ortoinjectionscontaining

penicillin.

6.3Shelflife

Unopened:3years

Onceopened:Useimmediately.Discardanyunusedportion.Anydilutedproductshouldbeusedimmediately.

6.4Specialprecautionsforstorage

Donotstoreabove25°C.

Forstorageofthedilutedmedicinalproductseesection6.3.,Shelflife.

6.5Natureandcontentsofcontainer

TypeIglass5mland10mlampoules,inpacksizesof10ampoules.

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6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Singleuseonly.

7MARKETINGAUTHORISATIONHOLDER

PharmaciaIreland

9Riverwalk

NationalDigitalPark

CitywestBusinessCampus

Dublin24

8MARKETINGAUTHORISATIONNUMBER

PA0936/008/002

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:01April1983

Dateoflastrenewal:01April2008

10DATEOFREVISIONOFTHETEXT

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