CATAFLAM SACHETS

Main information

  • Trade name:
  • CATAFLAM SACHETS
  • Dosage:
  • 50 Milligram
  • Pharmaceutical form:
  • Powder for Oral Solution
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • CATAFLAM SACHETS
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0013/088/003
  • Authorization date:
  • 14-07-2006
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

CataflamSachets50mgPowderforOralSolution.

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Theactiveingredientispotassium[o-(2,6-dichlorophenyl)-amino]-phenyl-acetate

(diclofenacpotassium)

Onesachetcontains50mgdiclofenacpotassium

Thesachetalsocontains50mgaspartame(E951)

Forafulllistofexcipients,seesection6.1

3PHARMACEUTICALFORM

Powderfororalsolution.

Whitetolightyellowpowderfororalsolution.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Short-termtreatmentofallgradesofpainandinflammationinthefollowingacuteconditions:

Post-traumaticpain,inflammationandswelling,e.g.duetosprains.

Acutemusculo-skeletaldisorderssuchasperiarthritis(forexamplefrozenshoulder).

Postoperativepain,inflammationandswelling,e.g.followingdentalororthopaedicsurgery.

Painfuland/orinflammatoryconditionsingynaecology,e.g.primarydysmenorrhoeaoradnexitisandassociated

menorrhagia.

Migraineattacks.

Painfulsyndromesofthevertebralcolumn.

Non-articularrheumatism.

Asanadjuvantinseverepainfulinflammatoryinfectionsoftheear,nose,orthroat,e.g.pharyngotonsillitis,

otitis.Inkeepingwithgeneraltherapeuticprinciples,theunderlyingdiseaseshouldbetreatedwithbasictherapy,

asappropriate.Feveraloneisnotanindication.

4.2Posologyandmethodofadministration

Undesirableeffectsmaybeminimisedbyusingthelowesteffectivedosefortheshortestdurationnecessarytocontrolsymptoms

(seesection4.4).

Thecontentsofthesachetshouldbedissolvedwithstirringinaglassofnatural(non-carbonated)water.Thesolution

mayremainslightlyopalescent,butthisshouldnotinfluencetheefficacyofthepreparation.Thesolutionshouldbe

swallowedpreferablybeforemeals.

Adults

Therecommendedinitialdosageis100to150mg.Inmildercases50to100mgdailyareusuallysufficient.

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Inprimarydysmenorrhoea,thedailydosageshouldbeindividuallyadjustedandisgenerally50to150mg.Initiallya

doseof50to100mgshouldbegivenand,ifnecessary,increasedoverthecourseofseveralmenstrualcyclesuptoa

maximumof200mg/day.Treatmentshouldbestartedonappearanceofthefirstsymptomsand,dependingonthe

symptomatology,continuedforafewdays.

Inmigraineaninitialdoseof50mgshouldbetakenatthefirstsignsofanimpendingattack.Incaseswherepainrelief

within2hoursafterthefirstdoseisnotsufficient,afurtherdoseof50mgmaybetaken.Ifneeded,furtherdosesof

50mgmaybetakenatintervalsof4to6hours,notexceedingatotaldoseof200mgperday.

Childrenandadolescents

Cataflam50mgpowderfororalsolutionisnotrecommendedforuseinchildrenandadolescentsbelow14yearsofage.

Fortreatmentinchildrenandadolescentsbelow14yearsofage,oraldropsandsuppositoriesofdiclofenac12.5mgare

available.

Foradolescentsaged14yearsandover,50to100mgdailyareusuallysufficient,givenas1to2divideddoses.

Themaximumdailydoseof150mgshouldnotbeexceeded.

TheuseofCataflam50mgpowderfororalsolutioninmigraineattackshasnotbeenestablishedinchildrenand

adolescents.

4.3Contraindications

Knownhypersensitivitytotheactivesubstanceortoanyoftheexcipients.

Historyofgastrointestinalbleedingorperforation,relatedtopreviousNSAIDstherapy.Activeorhistoryof

recurrentpepticulcer/haemorrhage(twoormoredistinctepisodesofprovenulcerationorbleeding).

Lasttrimesterofpregnancy(seesection4.6Pregnancyandlactation).

Severehepatic,renalor heart failure(seesection4.4Specialwarningsandprecautionsforuse).

Likeothernon-steroidalanti-inflammatorydrugs(NSAIDs),Cataflamisalsocontraindicatedinpatientsin

whomattacksofasthma,urticaria,oracuterhinitisareprecipitatedbyacetylsalicylicacidorotherNSAIDs.

4.4Specialwarningsandprecautionsforuse

Warnings

Gastrointestinalbleeding,ulcerationorperforation,whichcanbefatal,hasbeenreportedwithallNSAIDsandmay

occuratanytimeduringtreatment,withorwithoutwarningsymptomsoraprevioushistoryofseriousgastrointestinal

events.TheelderlyhaveanincreasedfrequencyofadversereactionstoNSAIDsespeciallygastrointestinalbleeding

andperforationwhichmaybefatal(seesection4.2Posologyandmethodofadministration).Whengastrointestinal

bleedingorulcerationoccursinpatientsreceivingCataflam,themedicinalproductshouldbewithdrawn.

Seriousskinreaction,someofthemfatal,includingexfoliativedermatitis,Stevens-Johnsonsyndromeandtoxic

epidermalnecrolysis,havebeenreportedveryrarelyinassociationwiththeuseofNSAIDs,includingCataflam(see

section4.8Undesirableeffects).Patientsappeartobeatahighestriskofthesereactionsearlyinthecourseoftherapy,

theonsetofthereactionoccurringinthemajorityofcaseswithinthefirstmonthoftreatment.

Cataflamshouldbediscontinuedatthefirstappearanceofskinrash,mucosallesionsoranyothersignof

hypersensitivity.

AswithotherNSAIDs,allergicreactions,includinganaphylactic/anaphylactoidreactions,canalsooccurinrarecases

withoutearlierexposuretothedrugdiclofenac.

LikeotherNSAIDs,Cataflammaymaskthesignsandsymptomsofinfectionduetoitspharmacodynamicproperties.

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womenwhohavedifficultiesconceivingorwhoareundergoinginvestigationofinfertility,withdrawlofdiclofenac

sodiumshouldbeconsidered.

Precautions

General

Undesirableeffectsmaybeminimisedbyusingthelowesteffectivedosefortheshortestpossibledurationnecessaryto

controlsymptoms(seesection4.2Posology&methodofadministration)andgastrointestinalandcardiovascularrisks

below.

TheuseofCataflamwithconcomitantNSAIDsincludingcyclooxygenase-2selectiveinhibitorsshouldbeavoideddue

totheabsenceofanyevidencedemonstratingsynergisticbenefitsandthepotentialforadditiveundesirableeffects.

Cautionisindicatedintheelderlyonbasicmedicalgrounds.Inparticular,itisrecommendedthatthelowesteffective

dosagebeusedinfrailelderlypatientsorthosewithalowbodyweight.

Pre-existingasthma

Inpatientswithasthma,seasonalallergicrhinitis,swellingofthenasalmucosa(i.e.nasalpolyps),chronicobstructive

pulmonarydiseasesorchronicinfectionsoftherespiratorytract(especiallyiflinkedtoallergicrhinitis-likesymptoms),

reactionsonNSAIDslikeasthmaexacerbations(so-calledintolerancetoanalgesics/analgesics-asthma),Quincke’s

oedemaorurticariaaremorefrequentthaninotherpatients.Therefore,specialprecautionisrecommendedinsuch

patients(readinessforemergency).Thisisapplicableaswellforpatientswhoareallergictoothersubstances,e.g.with

skinreactions,pruritusorurticaria.

Gastrointestinaleffects

AswithallNSAIDs,closemedicalsurveillanceisimperativeandparticularcautionshouldbeexercisedwhen

prescribingCataflaminpatientswithsymptomsindicativeofgastrointestinal(GI)disorders,orwithahistory

suggestiveofgastricorintestinalulceration,bleedingorperforation(seesection4.8Undesirableeffects).Theriskof

GIbleeding,ulcerationorperforationishigherwithincreasingNSAIDdosesinpatientswithahistoryofulcer,

particularlyifcomplicatedwithhaemorrhageorperforation(seesection4.3Contra-indications)andintheelderly.

Thesepatientsshouldcommencetreatmentonthelowestdoseavailable.

Combinationtherapywithprotectiveagents(e.g.protonpumpinhibitorsormisoprostol)shouldbeconsideredforthese

patients,andalsoforpatientsrequiringconcomitantuseofmedicinalproductscontaininglow-doseacetylsalicylicacid

(ASA)/aspirinorothermedicinalproductslikelytoincreasegastrointestinalrisk(seebelowandsection4.5

Interactionswithothermedicinalproductsandotherformsofinteractions).

PatientswithahistoryofGItoxicity,particularlytheelderly,shouldreportanyunusualabdominalsymptoms

(especiallyGIbleeding)particularlyintheinitialstagesoftreatment.Cautionisrecommendedinpatientsreceiving

concomitantmedicationswhichcouldincreasetheriskofulcerationorbleeding,suchasoralcorticosteroids,

anticoagulantssuchaswarfarin,anti-plateletagentssuchasaspirinorselectiveserotonin-reuptakeinhibitors(see

section4.5Interactionwithothermedicinalproductsandotherformsofinteraction).

NSAIDsshouldbegivenwithcaretopatientswithahistoryofgastrointestinaldisease(ulcerativecolitisorCrohn’s

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Cardiovascularandcerebrovasculareffects

Appropriatemonitoringandadvicearerequiredforpatientswithahistoryofhypertensionand/ormildtomoderate

congestiveheartfailureasfluidretentionandoedemahavebeenreportedinassociationwithNSAIDtherapy.

Clinicaltrialandepidemiologicaldatasuggestthattheuseofdiclofenac,particularlyathighdoses(150mgdaily)and

inlongtermtreatmentmaybeassociatedwithasmallincreasedriskofarterialthromboticevents(forexample

myocardialinfarctionorstroke).

Patientswithuncontrolledhypertension,congestiveheartfailure,establishedischaemicheartdisease,peripheral

arterialdisease,and/orcerebrovasculardiseaseshouldonlybetreatedwithdiclofenacaftercarefulconsideration.

Similarconsiderationshouldbemadebeforeinitiatinglonger-termtreatmentofpatientswithriskfactorsfor

cardiovascularevents(e.g.hypertension,hyperlipidaemia,diabetesmellitus,smoking).

Hepaticeffects

ClosemedicalsurveillanceisrequiredwhenprescribingCataflamtopatientswithimpairedhepaticfunction,astheir

conditionmaybeexacerbated.

AswithotherNSAIDs,valuesofoneormoreliverenzymesmayincrease.DuringprolongedtreatmentswithCataflam,

regularmonitoringofhepaticfunctionisindicatedasaprecautionarymeasure.Ifabnormalliverfunctiontestspersist

orworsen,ifclinicalsignsorsymptomsconsistentwithliverdiseasedevelop,orifothermanifestationsoccur(e.g.

eosinophilia,rash,etc.),Cataflamshouldbediscontinued.Hepatitismayoccurwithoutprodromalsymptoms.

CautioniscalledforwhenusingCataflamonpatientswithhepaticporphyria,sinceitmaytriggeranattack.

Renaleffects

AsfluidretentionandoedemahavebeenreportedinassociationwithNSAIDtherapy,historyofhypertension,the

elderly,patientsreceivingconcomitanttreatmentbeingtreatedwithdiureticsormedicinalproductsthatcan

significantlyimpactrenalfunction,andinthosepatientswithsubstantialextracellularvolumedepletionfromany

cause,e.g.beforeoraftermajorsurgery(seesection4.3Contraindications).Monitoringofrenalfunctionis

recommendedasaprecautionarymeasurewhenusingCataflaminsuchcases.Discontinuationoftherapyisusually

followedbyrecoverytothepre-treatmentstate.

Haematologicaleffects

UseofCataflamisrecommendedonlyforshort-termtreatment.IfhoweverCataflamisusedforaprolongedperiod,as

withotherNSAIDs,monitoringofthebloodcountisrecommended.

LikeotherNSAIDs,Cataflammaytemporarilyinhibitplateletaggregation.Patientswithdefectsofhaemostasisshould

becarefullymonitored.

Cataflam50mgpowderfororalsolutioncontainsaspartame,asourceofphenylalaninewhichmaybeharmfulfor

patientswithphenylketonuria.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

(Includinginteractionsobservedwithotherdosageformsofdiclofenacpotassiumanddiclofenacsodium).

Lithium:Ifusedconcomitantly,diclofenacmayincreaseplasmaconcentrationsoflithium.Monitoringoftheserum

lithiumlevelisrecommended.

Digoxin:Ifusedconcomitantly,diclofenacmayraiseplasmaconcentrationsofdigoxin.Monitoringoftheserum

digoxinlevelisrecommended.

Diureticsandantihypertensiveagents:LikeotherNSAIDs,concomitantuseofdiclofenacwithdiureticsor

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theirantihypertensiveeffect.Therefore,thecombinationshouldbeadministeredwithcautionandpatients,especially

theelderly,shouldhavetheirbloodpressureperiodicallymonitored.

Patientsshouldbeadequatelyhydratedandconsiderationshouldbegiventomonitoringofrenalfunctionafter

initiationofconcomitanttherapyandperiodicallythereafter,particularlyfordiureticsandACEinhibitorsduetothe

increasedriskofnephrotoxicity.

Concomitanttreatmentwithpotassium-sparingdiureticsmaybeassociatedwithincreasedserumpotassiumlevels,

whichshouldthereforebemonitoredfrequently(seesection4.4Specialwarningsandprecautionsforuse).

Anticoagulants:Althoughclinicalinvestigationsdonotappeartoindicatethatdiclofenacaffectstheactionof

anticoagulants, NSAIDsmayenhancetheeffectsofanti-coagulants,suchaswarfarin(seesection4.4.). Therearealsoisolated

reportsofanincreasedriskofhaemorrhageinpatientsreceivingdiclofenacandanticoagulantsconcomitantly.Close

monitoringofsuchpatientsisthereforerecommended.

Selectiveserotoninreuptakeinhibitors(SSRIs):ConcomitantadministrationofsystemicNSAIDsandSSRIsmay

increasetheriskofgastrointestinalbleeding(seesection4.4Specialwarningandprecautionsforuse).

Antidiabetics:Clinicalstudieshaveshownthatdiclofenaccanbegiventogetherwithoralantidiabeticagentswithout

influencingtheirclinicaleffect.However,isolatedtherehavebeenisolatedreportsofbothhypoglycaemicand

hyperglycaemiceffectsnecessitatingchangesinthedosageoftheantidiabeticagentsduringtreatmentwithdiclofenac.

Forthisreason,monitoringofthebloodglucoselevelisrecommendedasaprecautionarymeasureduringconcomitant

therapy.

Methotrexate:CautionisrecommendedwhenNSAIDsareadministeredlessthan24hoursbeforeoraftertreatment

withmethotrexate,sincebloodconcentrationsofmethotrexatemayriseandthetoxicityofthissubstancebeincreased.

Ciclosporin:Diclofenac,likeotherNSAIDs,mayincreasethenephrotoxicityofciclosporinduetotheeffectonrenal

prostaglandins.Therefore,itshouldbegivenatdoseslowerthanthosethatwouldbeusedinpatientsnotreceiving

ciclosporin.

Quinoloneantibacterials:Therehavebeenisolatedreportsofconvulsionswhichmayhavebeenduetoconcomitant

useofquinolonesandNSAIDs.

OtherNSAIDsandCorticosteroids:ConcomitantadministrationofdiclofenacandothersystemicNSAIDsororal

corticosteroidsmayincreasetheriskofgastrointestinalulcerationorbleeding(seesection4.4Specialwarningsand

precautionsforuse).

4.6Pregnancyandlactation

Pregnancy

Theuseofdiclofenacinpregnantwomenhasnotbeenstudied.Therefore,Cataflamshouldnotbeusedduringthefirst

twotrimestersofpregnancyunlessthepotentialbenefittothemotheroutweighstherisktothefoetus.Aswithother

NSAIDs,useduringthethirdtrimesterofpregnancyiscontraindicatedowingtothepossibilityofuterineinertiaand/or

prematureclosureoftheductusarteriosus(seesection4.3Contraindications).Animalstudieshavenotshownany

directlyorindirectlyharmfuleffectsonpregnancy,embryonal/fetaldevelopment,parturitionorpostnataldevelopment

(seesection5.3Preclinicalsafetydata).

Lactation

LikeotherNSAIDs,diclofenac,passesintothebreastmilk,insmallamounts.Therefore,Cataflamshouldnotbe

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Fertility

AswithotherNSAIDs,theuseofCataflammayimpairfemalefertilityandisnotrecommendedinwomenattempting

toconceive.Inwomenwhohavedifficultiesconceivingorwhoareundergoinginvestigationofinfertility,withdrawal

ofCataflamshouldbeconsidered.

4.7Effectsonabilitytodriveandusemachines

Patientsexperiencingdizziness,vertigo,somnolenceorothercentralnervoussystemdisturbanceswhiletaking

Cataflamincludingvisualdisturbances,shouldnotdriveoroperatemachines.

4.8Undesirableeffects

Adversereactions(Table1)arerankedunderheadingoffrequency,themostfrequentfirst,usingthefollowing

convention:common( ≥1/100,<1/10);uncommon(≥1/1,000,<1/100);rare(≥1/10,000,<1/1,000);veryrare(<

1/10,000).

Themostcommonlyobservedadverseeventsaregastrointestinalinnature.Pepticulcers,perforationorGIbleeding,

sometimesfatal,particularlyintheelderly,mayoccur(seesection4.4Specialwarningsandprecautionsforuse).

Nausea,vomiting,diarrhoea,flatulence,constipation,dyspepsia,abdominalpain,melaena,haematemesis,ulcerative

stomatitis,exacerbationofcolitisandCrohn’sdisease(seesection4.4Specialwarningsandprecautionsforuse)have

beenreportedfollowingadministration.Lessfrequently,gastritishasbeenobserved.

ThefollowingtableofundesirableeffectsincludethosereportedwithCataflamsugarcoatedtabletsand/orother

pharmaceuticalformsofdiclofenac,witheithershort-termorlong-termuse.

Table1

Bloodandlymphatic

systemdisorders

Veryrare: Thrombocytopenialeucopenia,anaemia(includinghaemolyticanaemiaandaplastic

anaemia),agranulocytosis.

Immunesystemdisorder

Rare: Hypersensitivity,anaphylacticandanaphylactoidreactions(includinghypotension

andshock)

Veryrare: Angioneuroticoedema(includingfaceoedema).

Psychiatricdisorders:

Veryrare: Disorientation,depression,insomnia,nightmare,irritability,psychoticdisorder.

Nervoussystemdisorders

Common: Headache,dizziness,

Rare: Somnolence,

Veryrare: Paraesthesias,memoryimpairment,convulsion,anxiety,Tremor,asepticmeningitis,

tastedisturbances,cerebrovascularaccident.

Eyedisorders

Veryrare: Visualdisturbance,visionblurred,diplopia.

Earandlabyrinth

disorders

Common: Vertigo.

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Oedema,hypertensionandcardiacfailurehavebeenreportedinassociationwithNSAIDtreatment.

Clinicaltrialandepidemiologicaldatasuggestthattheuseofdiclofenac,particularlyathighdoses(150mgdaily)and

inlongtermtreatmentmaybeassociatedwithasmallincreasedriskofarterialthromboticevents(forexample

myocardialinfarctionorstroke)(seesection4.4Specialwarningsandprecautionsforuse).

4.9Overdose

Symptoms

Thereisnotypicalclinicalpictureresultingfromdiclofenacoverdosage.Overdosagecancausesymptomssuchas

vomiting,gastrointestinalhaemorrhage,diarrhoea,dizziness,tinnitusorconvulsions.Intheeventofsignificant

Cardiacdisorders:

Veryrare: Palpitations,chestpain,cardiacfailure,myocardialinfarction

Vasculardisorders

Veryrare: hypertension,vasculitis.

Respiratory,thoracicand

mediastinaldisoders:

Rare: Asthma(includingdyspnoea).

Veryrare: Pneumonitis.

Gastrointestinaldisorders

Common: Nausea,vomiting,diarrhoea,dyspepsia,abdominalpain,flatulence,anorexia.

Rare: Gastritis,gastrointestinalhaemorrhage,haematemesis,diarrhoeahaemorrhagic,

melaena,gastrointestinalulcer(withorwithoutbleedingorperforation).

Veryrare: Colitis(includinghaemorrhagiccolitisandexacerbationofulcerativecolitisor

Crohn’sdisease),constipationstomatitis,glossitis,oesophagealdisorder,diaphragm-

likeintestinalstrictures,pancreatitis.

Hepatobiliarydisorders

Common: Transaminasesincreased.

Rare: Hepatitis,jaundice,liverdisorder.

Veryrare: Fulminanthepatitis,hepaticnecrosis,hepaticfailure

Skinandsubcutaneous

tissuedisorders

Common: Rash.

Rare: Urticaria.

Veryrare: Bullouseruptions,eczema,erythema,erythemamultiforme,Stevens-Johnson

syndrome,toxicepidermalnecroylsis(Lyell’ssyndrome),dermatitisexfoliativeloss

ofhair,photosensitivityreaction,purpura,allergicpurpura,pruritus.

Renalandurinary

disorders

Veryrare: Acuterenalfailurehaematuria,proteinuria,nephriticsyndrome,interstitialnephritis,

renalpapillarynecrosis.

Generaldisordersand

administrationsite

conditions

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Therapeuticmeasures

ManagementofacutepoisoningwithNSAIDSconsistsessentiallyofsupportivemeasuresandsymptomatictreatment.

Supportivemeasuresandsymptomatictreatmentshouldbegivenforcomplicationssuchashypotension,renalfailure,

convulsions,gastrointestinaldisorder,andrespiratorydepression.

Specialmeasuressuchasforceddiuresis,dialysis,orhaemoperfusionareprobablyunlikelytobehelpfulin

acceleratingtheeliminationofNSAIDsbecauseoftheirhighproteinbindingrateandextensivemetabolism.

Activatedcharcoalmaybeconsideredafteringestionofapotentiallytoxicoverdose,andgastricdecontamination(e.g.

vomiting,gastriclavage)afteringestionofapotentiallylife-threateningoverdose.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacotherapeuticgroup:Anti-inflammatoryandantirheumaticproducts,non-steroidsaceticacidderivativesand

relatedsubstances(NSAID)(ATCcode:M01AB05).

Mechanismofaction

Cataflamsachetscontainthepotassiumsaltofdiclofenac,anon-steroidalcompoundwithpronouncedanalgesic,anti-

inflammatory,andantipyreticproperties.

Cataflamsachetshavearapidonsetofaction,whichmakesitparticularlysuitableforthetreatmentofacutepainfuland

inflammatoryconditions.Inhibitionofprostaglandinbiosynthesis,whichhasbeendemonstratedinexperiments,is

consideredtobefundamentaltoitsmechanismofaction.Prostaglandinsplayamajorroleincausinginflammation,

pain,andfever.

Diclofenacpotassiuminvitrodoesnotsuppressproteoglycanbiosynthesisincartilageatconcentrationsequivalentto

theconcentrationsreachedinhumans.

Pharmacodynamiceffects

Cataflamsachetshavebeenfoundtoexertapronouncedanalgesiceffectinmoderateandseverepain.Inthepresence

ofinflammation,e.g.duetotraumaorfollowingsurgicalinterventions,itrapidlyrelievesbothspontaneouspainand

painonmovementanddiminishesinflammatoryswellingandwoundoedema.Clinicalstudieshavealsorevealedthat

inprimarydysmenorrhoeatheactivesubstanceiscapableofrelievingthepainandreducingtheextentofbleeding.In

migraineattacksCataflamsachetshavebeenshowntobeeffectiveinrelievingtheheadacheandinimprovingthe

accompanyingsymptomsnauseaandvomiting.

5.2Pharmacokineticproperties

Absorption

Diclofenacisrapidlyandcompletelyabsorbedfromdiclofenacpotassium.Meanpeakplasmaconcentrationsof5.5

micromol/Lareattainedafter5-20minutesafteringestionofonesachetof50mg.

Ingestiontogetherwithfoodisexpectedtohavenoinfluenceontheamountofdiclofenacabsorbedalthoughonsetand

rateofabsorptionmaybeslightlydelayed.

Theamountabsorbedisinlinearproportiontothesizeofthedose.

Sinceabouthalfofdiclofenacismetabolizedduringitsfirstpassagethroughtheliver("firstpass"effect),thearea

undertheconcentrationcurve(AUC)isabouthalfaslargefollowingoralorrectaladministrationasitisfollowinga

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Pharmacokineticbehaviourdoesnotchangeafterrepeatedadministration.Noaccumulationoccursprovidedthe

recommendeddosageintervalsareobserved.

Distribution

99.7%ofdiclofenacbindstoserumproteins,mainlytoalbumin(99.4%).Theapparentvolumeofdistribution

calculatedis0.12-0.17L/kg.

Diclofenacentersthesynovialfluid,wheremaximumconcentrationsaremeasured2-4hoursafterpeakplasmavalues

havebeenreached.Theapparenthalf-lifeforeliminationfromthesynovialfluidis3-6hours.Twohoursafterreaching

peakplasmalevels,concentrationsoftheactivesubstancearealreadyhigherinthesynovialfluidthanintheplasma,

andtheyremainhigherforupto12hours.

Biotransformation

Biotransformationofdiclofenactakesplacepartlybyglucuronidationoftheintactmolecule,butmainlybysingleand

multiplehydroxylationandmethoxylation,resultinginseveralphenolicmetabolites(3'-hydroxy-,4'-hydroxy-,5-

hydroxy-,4',5-dihydroxy-,and3'-hydroxy-4'-methoxy-diclofenac),mostofwhichareconvertedtoglucuronide

conjugates.Twoofthesephenolicmetabolitesarebiologicallyactive,buttoamuchlesserextentthandiclofenac.

Elimination

Totalsystemicclearanceofdiclofenacfromplasmais263±56mL/min(meanvalue±SD).Theterminalhalf-lifein

plasmais1-2hours.Fourofthemetabolites,includingthetwoactiveones,alsohaveshortplasmahalf-livesof1-3

hours.Onemetabolite,3'-hydroxy-4'-methoxy-diclofenac,hasamuchlongerplasmahalf-life.However,thismetabolite

isvirtuallyinactive.

About60%oftheadministereddoseisexcretedintheurineastheglucuronideconjugateoftheintactmoleculeandas

metabolites,mostofwhicharealsoconvertedtoglucuronideconjugates.Lessthan1%isexcretedasunchanged

substance.Therestofthedoseiseliminatedasmetabolitesthroughthebileinthefaeces.

Characteristicsinpatients

Norelevantage-dependentdifferencesinthedrug'sabsorption,metabolism,orexcretionhavebeenobserved.

Inpatientssufferingfromrenalimpairment,noaccumulationoftheunchangedactivesubstancecanbeinferredfrom

thesingle-dosekineticswhenapplyingtheusualdosageschedule.Atacreatinineclearanceoflessthan10mL/min,the

calculatedsteady-stateplasmalevelsofthehydroxymetabolitesareabout4timeshigherthaninnormalsubjects.

However,themetabolitesareultimatelyclearedthroughthebile.

Inpatientswithchronichepatitisornon-decompensatedcirrhosis,thekineticsandmetabolismofdiclofenacarethe

sameasinpatientswithoutliverdisease.

5.3Preclinicalsafetydata

Preclinicaldataformacuteandrepeateddosetoxicitystudies,aswellasfromgenotoxicity,mutagenicity,and

carcinogenicitystudieswithdiclofenacrevealednospecifichazardforhumansattheintendedtherapeuticdoses.There

wasnoevidencethediclofenachadateratogenicpotentialinmice,ratsorrabbits.

Diclofenachadnoinfluenceonthefertilityoftheparentanimalsinrats.Theprenatal,perinatal,andpostnatal

developmentoftheoffspringwasnotaffected.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Potassiumhydrogencarbonate

Mannitol

Aspartame

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Glyceryldibehenate

Mintflavour

Aniseflavour

6.2Incompatibilities

Intheabsenceofcompatibilitystudies,thismedicinalproductmustnotbemixedwithanythingotherthanwater.

6.3ShelfLife

2years.

6.4Specialprecautionsforstorage

Donotstoreabove25 °

Storeintheoriginalpackageinordertoprotectfrommoisture.

6.5Natureandcontentsofcontainer

Sachetconsistingofcoupledpaper/aluminium/polyethylene,hermeticallysealedinfourdirectionsThreesachetsarepackagedin

onecarton.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements

7MARKETINGAUTHORISATIONHOLDER

NovartisPharmaceuticalsUKLimited

FrimleyBusinessPark

Frimley,Camberley

Surrey,GU167SR

8MARKETINGAUTHORISATIONNUMBER

PA0013/088/003

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:14July2006

Dateoflastauthorisation:25July2008

10DATEOFREVISIONOFTHETEXT

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 26/10/2010 CRN 2049740 page number: 10