CATAFLAM

Main information

  • Trade name:
  • CATAFLAM Coated Tablets 25 Milligram
  • Dosage:
  • 25 Milligram
  • Pharmaceutical form:
  • Coated Tablets
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • CATAFLAM Coated Tablets 25 Milligram
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0013/088/001
  • Authorization date:
  • 13-03-1995
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Cataflam25mgCoatedTablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Eachtabletcontains25mgdiclofenacpotassium.

Eachtabletalsocontains45mgsucrose.

Forafulllistofexcipients,seesection6.1.

3PHARMACEUTICALFORM

CoatedTablet(Tablet).

Circular,biconvex,paleredsugarcoatedtabletapproximately7.7mmdiameterimprinted“CG”ononesideand“DD”

ontheother.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Short-termtreatmentofallgradesofpainandinflammationinthefollowingacuteconditions:

Posttraumaticpain,inflammationandswelling,e.g.duetosprains.

Acutemusculo-skeletaldisorderssuchasperiarthritis(forexamplefrozenshoulder),tendonitis,tenosynovitis,

bursitis.

Post-operativepain,inflammationandswelling,e.g.followingdentalororthopaedicsurgery.

Painfuland/orinflammatoryconditionsingynaecology,e.g.primarydysmenorrhoeaoradnexitisandassociated

menorrhagia.

Migraineattacks.

Acutegout.

Painfulsyndromesofthevertebralcolumn.

Non-articularrheumatism.

Asanadjuvantinseverepainfulinflammatoryinfectionsoftheear,noseorthroat,e.g.pharyngotonsillitis,otitis.

Inkeepingwithgeneraltherapeuticprinciples,theunderlyingdiseaseshouldbetreatedwithbasictherapy,as

appropriate.Feveraloneisnotanindication.

4.2Posologyandmethodofadministration

Undesirableeffectsmaybeminimizedbyusingthelowesteffectivedosefortheshortestdurationnecessarytocontrol

symptoms(seesection4.4).

Thetabletsshouldbeswallowedwholewithliquid,preferablybeforemeals,andmustnotbedividedorchewed.

Adults:

Thetotaldailydoseshouldgenerallybedividedin2to3doses.

Inprimarydysmenorrhoea,thedailydoseshouldbeindividuallyadjustedandisgenerally50to150mg.Adoseof50

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maximumof200mg/day.Treatmentshouldbestartedonappearanceofthefirstsymptomsand,dependingonthe

symptomatology,continuedforafewdays.

Inmigraine,aninitialdoseof50mgshouldbetakenatthefirstsignsofanimpendingattack.Incaseswherepainrelief

within2hoursafterthefirstdoseisnotsufficient,afurtherdoseof50mgmaybetaken.Ifneeded,furtherdosesof

50mgmaybetakenatintervalsof4to6hours,notexceedingatotaldoseof200mgperday.

Childrenandadolescents

Cataflamtabletsarenotrecommendedforuseinchildrenandadolescentsbelow14yearsofage;otherformsof

diclofenacsuchasoraldropsorsuppositoriescouldbeusedinthesepatients.Foradolescentsaged14yearsandover,a

dailydoseof75to100mgisusuallysufficient.Thetotaldailydoseshouldgenerallybedividedin2to3doses.

Themaximumdailydoseof150mgshouldnotbeexceeded.

TheuseofCataflam(allforms)inmigraineattackshasnotbeenestablishedinchildrenandadolescents.

Elderly:

AlthoughthepharmacokineticsofCataflamarenotimpairedtoanyclinicallyrelevantextentinelderlypatients,non-

steroidalanti-inflammatorydrugsshouldbeusedwithparticularcautioninolderpatientswhogenerallyaremoreprone

toadversereactions.Inparticular,itisrecommendedthatthelowesteffectivedosagebeusedinfrailelderlypatientsor

thosewithalowbodyweight(seealsoprecautions).Treatmentshouldbereviewedatregularintervalsand

discontinuedifnobenefitisseenorifintoleranceoccurs.

4.3Contraindications

Knownhypersensitivitytotheactivesubstanceortoanyoftheexcipients.

Historyofgastrointestinalbleedingorperforation,relatedtopreviousNSAIDstherapy.Activeorhistoryof

recurrentpepticulcer/haemorrhage(twoormoredistinctepisodesofprovenulcerationorbleeding).

Lasttrimesterofpregnancy(seesection4.6Pregnancyandlactation).

Severehepatic,renalandheartfailure(seesection4.4Specialwarningsandprecautionsforuse).

Likeothernon-steroidalanti-inflammatorydrugs(NSAIDs),Cataflamisalsocontraindicatedinpatientsinwhom

attacksofasthma,urticaria,oracuterhinitisareprecipitatedbyacetylsalicylicacidorotherNSAIDs.

4.4Specialwarningsandprecautionsforuse

Warnings

Gastrointestinalbleeding,orulcerationorperforation,whichcanbefatal,havebeenreportedwithallNSAIDs,

includingdiclofenac,andmayoccuratanytimeduringtreatment,withorwithoutwarningsymptomsoraprevious

historyofseriousgastrointestinalevents.TheelderlyhaveanincreasedfrequencyofadversereactionstoNSAIDs

especiallygastrointestinalbleedingandperforationwhichmaybefatal(seesection4.2Posologyandmethodof

administration).WhengastrointestinalbleedingorulcerationoccurinpatientsreceivingCataflam,themedicinal

productshouldbewithdrawn.

Seriousskinreactions,someofthemfatal,includingexfoliativedermatitis,Stevens-Johnsonsyndromeandtoxic

epidermalnecrolysis,havebeenreportedveryrarelyinassociationwiththeuseofNSAIDs,includingCataflam(see

section4.8Undesirableeffects).Patientsappeartobeatahighestriskofthesereactionsearlyinthecourseoftherapy,

theonsetofthereactionoccurringinthemajorityofcaseswithinthefirstmonthoftreatment.

Cataflamshouldbediscontinuedatthefirstappearanceofskinrash,mucosallesionsoranyothersignof

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AswithotherNSAIDs,allergicreactions,includinganaphylactic/anaphylactoidreactions,canalsooccurinrarecases

withdiclofenacwithoutearlierexposuretothedrug.

LikeotherNSAIDs,Cataflammaymaskthesignsandsymptomsofinfectionduetoitspharmacodynamicproperties.

Theuseofdiclofenacpotassiummayimpairfemalefertilityandisnotrecommendedinwomenattemptingto

conceive.Inwomenwhohavedifficultiesconceivingorwhoareundergoinginvestigationofinfertility,withdrawalof

diclofenacpotassiumshouldbeconsidered.

Precautions

General

Undesirableeffectsmaybeminimisedbyusingthelowesteffectivedosefortheshortestpossibledurationnecessaryto

controlsymptoms(seesection4.2Posology&methodofadministrationandgastrointestinalandcardiovascularrisks

below.)

TheuseofCataflamwithconcomitantNSAIDsincludingcyclooxygenase-2selectiveinhibitorsshouldbeavoideddue

totheabsenceofanyevidencedemonstratingsynergisticbenefitsandthepotentialforadditiveundesirableeffects.

Cautionisindicatedintheelderlyonbasicmedicalgrounds.Inparticular,itisrecommendedthatthelowesteffective

dosebeusedinfrailelderlypatientsorthosewithalowbodyweight.

Cataflamtabletscontainsucroseandthereforearenotrecommendedforpatientswithrarehereditaryproblemsof

fructoseintolerance,glucose-galactosemalabsorptionorsucrase-isomaltaseinsufficiency.

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,includingdiclofenac,closemedicalsurveillanceisimperativeandparticularcautionshouldbe

exercisedwhenprescribingCataflaminpatientswithsymptomsindicativeofgastrointestinal(GI)disorders,orwitha

historysuggestiveofgastricorintestinalulceration,bleedingorperforation(seesection4.8Undesirableeffects).The

riskofGIbleeding,ulcerationorperforationishigherwithincreasingNSAIDdosesinpatientswithahistoryofulcer,

particularlyifcomplicatedwithhaemorrhageorperforation(seesection4.3Contra-indications)andintheelderly.

Thesepatientsshouldcommenceontreatmentonthelowestdoseavailable.

Combinationtherapywithprotectiveagents(e.g.protonpumpinhibitorsormisoprostol)shouldbeconsideredforthese

patients,andalsoforpatientsrequiringconcomitantuseofmedicinalproductscontaininglow-doseacetylsalicylicacid

(ASA)/aspirinorothermedicinalproductslikelytoincreasegastrointestinalrisk(seebelowandsection4.5

Interactionswithothermedicinalproductsandotherformsofinteraction).

PatientswithahistoryofGItoxicity,particularlytheelderly,shouldreportanyunusualabdominalsymptoms

(especiallyGIbleeding)particularlyintheearlystagesoftreatment.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,includingdiclofenac,valuesofoneormoreliverenzymesmayincrease.Duringprolonged

treatmentswithCataflam,regularmonitoringofhepaticfunctionisindicatedasaprecautionarymeasure.Ifabnormal

liverfunctiontestspersistorworsen,ifclinicalsignsorsymptomsconsistentwithliverdiseasedevelop,orifother

manifestationsoccur(e.g.eosinophilia,rash,etc.),Cataflamshouldbediscontinued.Hepatitismayoccurwithuseof

diclofenacwithoutprodromalsymptoms.

CautioniscalledforwhenusingCataflaminpatientswithhepaticporphyria,sinceitmaytriggeranattack.

Renaleffects

AsfluidretentionandoedemahavebeenreportedinassociationwithNSAIDtherapy,includingdiclofenacparticular

cautioniscalledforinpatientswithimpairedcardiacorrenalfunction,historyofhypertension,theelderly,patients

receivingconcomitanttreatmentwithdiureticsormedicinalproductsthatcansignificantlyimpactrenalfunction,and

inthosepatientswithsubstantialextracellularvolumedepletionfromanycause,e.g.beforeoraftermajorsurgery(see

section4.3Contraindications).Monitoringofrenalfunctionisrecommendedasaprecautionarymeasurewhenusing

Cataflaminsuchcases.Discontinuationoftherapyisnormallyfollowedbyrecoverytothepre-treatmentstate.

Haematologicaleffects

UseofCataflamisrecommendedonlyforshort-termtreatment.If,however,Cataflamisusedforaprolongedperiod,

monitoringofthebloodcountisrecommended,aswithotherNSAIDs.

LikeotherNSAIDs,Cataflammaytemporarilyinhibitplateletaggregation.Patientswithdefectsofhaemostasisshould

becarefullymonitored.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

ThefollowinginteractionsincludethoseobservedwithCataflamsugar-coatedtabletsand/orotherpharmaceutical

formsofdiclofenac.

Lithium:Ifusedconcomitantly,diclofenacmayraiseplasmaconcentrationsoflithium.Monitoringoftheserum

lithiumlevelisrecommended.

Digoxin:Ifusedconcomitantly,diclofenacmayraiseplasmaconcentrationsofdigoxin.Monitoringoftheserum

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Diureticsandantihypertensiveagents:LikeotherNSAIDs,concomitantuseofdiclofenacwithdiureticsor

antihypertensiveagents(e.g.beta-blockers,angiotensinconvertingenzyme(ACE)inhibitor)maycauseadecreasein

theirantihypertensiveeffect.Therefore,thecombinationshouldbeadministeredwithcautionandpatients,especially

theelderly,shouldhavetheirbloodpressureperiodicallymonitored.Patientsshouldbeadequatelyhydratedand

considerationshouldbegiventomonitoringofrenalfunctionafterinitiationofconcomitanttherapyandperiodically

thereafter,particularlyfordiureticsandACEinhibitorsduetotheincreasedriskofnephrotoxicity.Concomitant

treatmentwithpotassium-sparingdrugsmaybeassociatedwithincreasedserumpotassiumlevels,whichshould

thereforebemonitoredfrequently(seesection4.4Specialwarningsandprecautionsforuse).

OtherNSAIDsandcorticosteroids:ConcomitantadministrationofdiclofenacandothersystemicNSAIDsor

corticosteroidsmayincreasetheriskofgastrointestinalulcerationorbleeding(seesection4.4Specialwarningand

precautionsforuse).

Anticoagulantsandanti-plateletagents:Cautionisrecommendedsinceconcomitantadministrationcouldincreasethe

riskofgastrointestinalbleeding(seesection4.4Specialwarningsandspecialprecautionsforuse).Althoughclinical

investigationsdonotappeartoindicatethatdiclofenacaffectstheactionofanticoagulants,NSAIDsmayenhancethe

effectsofanti-coagulants,suchaswarfarin(seesection4.4).Therearealsoisolatedreportsofanincreasedriskof

haemorrhageinpatientsreceivingdiclofenacandanticoagulantsconcomitantly.Closemonitoringofsuchpatientsis

thereforerecommended.

Selectiveserotoninreuptakeinhibitors(SSRIs):ConcomitantadministrationofsystemicNSAIDsincludingdiclofenac

andSSRIsmayincreasetheriskofgastrointestinalbleeding(seesection4.4Specialwarningsandprecautionsfor

use).

Antidiabetics:Clinicalstudieshaveshownthatdiclofenaccanbegiventogetherwithoralantidiabeticagentswithout

influencingtheirclinicaleffect.However,therehavebeenisolatedreportsofbothhypoglycaemicandhyperglycaemic

effectsnecessitatingchangesinthedosageoftheantidiabeticagentsduringtreatmentwithdiclofenac.Forthisreason,

monitoringofthebloodglucoselevelisrecommendedasaprecautionarymeasureduringconcomitanttherapy.

Methotrexate:CautionisrecommendedwhenNSAIDs,includingdiclofenacareadministeredlessthan24hoursbefore

oraftertreatmentwithmethotrexate,sincebloodconcentrationsofmethotrexatemayriseandthetoxicityofthis

substancebeincreased.

Ciclosporin:Diclofenac,likeotherNSAIDs,mayincreasethenephrotoxicityofciclosporinduetotheeffectonrenal

prostaglandins.Therefore,itshouldbegivenatdoseslowerthanthosethatwouldbeusedinpatientsnotreceiving

ciclosporin.

Quinoloneantibacterials:therehavebeenisolatedreportsofconvulsionswhichmayhavebeenduetoconcomitantuse

ofquinolonesandNSAIDs.

4.6Fertility,pregnancyandlactation

Pregnancy

Theuseofdiclofenacinpregnantwomenhasnotbeenstudied.Therefore,Cataflamshouldnotbeusedduringthefirst

twotrimestersofpregnancyunlessthepotentialbenefittothemotheroutweighstherisktothefoetus.Aswithother

NSAIDs,useofdiclofenacduringthethirdtrimesterofpregnancyiscontraindicatedowingtothepossibilityofuterine

inertiaand/orprematureclosureoftheductusarteriosus(seesection4.3Contraindications).Animalstudieshavenot

shownanydirectlyorindirectlyharmfuleffectsonpregnancy,embryonal/fetaldevelopment,parturitionorpostnatal

development(seesection5.3Preclinicalsafetydata).

Lactation

LikeotherNSAIDs,diclofenac,passesintothebreastmilk,butinsmallamounts.Therefore,Cataflamshouldnotbe

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Fertility

AswithotherNSAIDs,theuseofCataflammayimpairfemalefertilityandisnotrecommendedinwomenattempting

toconceive.Inwomenwhohavedifficultiesconceivingorwhoareundergoinginvestigationofinfertility,withdrawal

ofCataflamshouldbeconsidered.

4.7Effectsonabilitytodriveandusemachines

Patientswhoexperiencedizziness,vertigo,somnolenceorothercentralnervoussystemdisturbances,includingvisual

disturbances,whiletakingNSAIDsshouldrefrainfromdrivingorusingmachinery.

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,sometimes

fatal,particularlyintheelderly,mayoccur(seesection4.4Specialwarningsandprecautionsforuse).Nausea,vomiting,

diarrhoea,flatulence,constipation,dyspepsia,abdominalpain,melaena,haematemesis,ulcerativestomatitis,exacerbationof

coilitisandCrohn’sdisease(seesection4.4Specialwarningsandprecautionsforuse)havebeenreportedfollowing

administration.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.

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Oedema,hypertensionandcardiacfailurehavebeenreportedinassociationwithNSAIDtreatment.

Clinicaltrialandepidemiologicaldatasuggestthattheuseofdiclofenac,particularlyathighdoses(150mgdaily)and

inlongtermtreatmentmaybeassociatedwithasmallincreasedriskofarterialthromboticevents(forexample

myocardialinfarctionorstroke)(seesection4.4Specialwarningsandprecautionsforuse).

4.9Overdose

Symptoms

disorders

Common: Vertigo.

Veryrare: Tinnitus,hearingimpaired.

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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vomiting,gastrointestinalhaemorrhage,diarrhoea,dizziness,tinnitusorconvulsions.Intheeventofsignificant

poisoning,acuterenalfailureandliverdamagearepossible.

Therapeuticmeasures

ManagementofacutepoisoningwithNSAIDs,includingdiclofenac,consistsessentiallyofsupportivemeasuresand

symptomatictreatment.Supportivemeasuresandsymptomatictreatmentshouldbegivenforcomplicationssuchas

hypotension,renalfailure,convulsions,gastrointestinaldisorder,andrespiratorydepression.

Specialmeasuressuchasforceddiuresis,dialysis,orhaemoperfusionareprobablyunlikelytobehelpfulin

acceleratingtheeliminationofNSAIDs,includingdiclofenac,duetothehighproteinbindingandextensive

metabolism.

Activatedcharcoalmaybeconsideredafteringestionofapotentiallytoxicoverdose,andgastricdecontamination(e.g.

vomiting,gastriclavage)afteringestionofapotentiallylife-threateningoverdose.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacotherapeuticgroup:Anti-inflammatoryandantirheumaticproducts,non-steroids,aceticacidderivativesand

relatedsubstances(NSAID)(ATCcode:M01AB05).

Mechanismofaction

Cataflamcontainsthepotassiumsaltofdiclofenac,anon-steroidalcompoundwithpronounced,analgesic,anti-

inflammatoryandantipyreticproperties.Inhibitionofprostaglandinbiosynthesis,whichhasbeendemonstratedin

experiments,isconsideredfundamentaltoitsmechanismofaction.Prostaglandinsplayamajorroleincausingof

inflammation,pain,andfever.

Cataflamtabletshavearapidonsetofactionwhichmakesthemparticularlysuitableforthetreatmentofacutepainful

andinflammatoryconditions.

Diclofenacpotassiuminvitrodoesnotsuppressproteoglycanbiosynthesisincartilageatconcentrationsequivalentto

thosereachedinhumans.

Pharmacodynamiceffects

Cataflamhasbeenfoundtoexertapronouncedanalgesiceffectinmoderateandseverepain.Inthepresenceof

inflammation,e.g.duetotraumaorfollowingsurgicalinterventions,itrapidlyrelievesbothspontaneouspainandpain

onmovementanddiminishesinflammatoryswellingandwoundoedema.

Clinicalstudieshavealsorevealedthatinprimarydysmenorrohoeatheactivesubstanceiscapableofrelievingthepain

andreducingtheextentofbleeding.

InmigraineattacksCataflamhasbeenshowntobeeffectiveinrelievingtheheadacheandinimprovingthe

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5.2Pharmacokineticproperties

Absorption:

Diclofenacisrapidlyandcompletelyabsorbedfromdiclofenacpotassiumtablets.Theabsorptionsetsinimmediately

afteradministrationandthesameamountisabsorbedasfromanequivalentdoseofdiclofenacsodiumgastro-resistant

tablets.Meanpeakplasmaconcentrationsof3.8µmol/Lareattainedafter20–60minutesafteringestionofonetablet

of50mg.Ingestiontogetherwithfoodhasnoinfluenceontheamountofdiclofenacabsorbedalthoughonsetandrate

ofabsorptionmaybeslightlydelayed.

Theamountabsorbedisinlinearproportiontothesizeofthedose.

Pharmacokineticbehaviourdoesnotchangeafterrepeatedadministration.Noaccumulationoccursprovidedthe

recommendeddosageintervalsareobserved

Distribution:

Theactivesubstanceis99.7%proteinbound,mainlytoalbumin(99.4%).

Diclofenacentersthesynovialfluid,wheremaximumconcentrationsaremeasured2-4hoursafterpeakplasmavalues

havebeenattained.Theapparenthalf-lifeforeliminationfromthesynovialfluidis3-6hours.Twohoursafterreaching

thepeakplasmavalues,concentrationsoftheactivesubstancearealreadyhigherinthesynovialfluidthantheyarein

theplasma,andremainhigherforupto12hours.

Metabolism:

Biotransformationofdiclofenactakesplacepartlybyglucuronidationoftheintactmolecule,butmainlybysingleand

multiplehydroxylationandmethoxylation,resultinginseveralphenolicmetabolites,mostofwhichareconvertedto

glucuronideconjugates.Twophenolicmetabolitesarebiologicallyactive,buttoamuchlesserextentthandiclofenac.

Elimination:

Totalsystemicclearanceofdiclofenacinplasmais263±56mL/min(meanvalue±SD).Theterminalhalf-lifeinplasma

is1-2hours.Fourofthemetabolites,includingthetwoactiveones,alsohaveshortplasmahalf-livesof1-3hours.

About60%oftheadministereddoseisexcretedintheurineastheglucuronideconjugateoftheintactmoleculeandas

metabolites,mostofwhicharealsoconvertedtoglucuronideconjugates.Lessthan1%isexcretedasunchanged

substance.Therestofthedoseiseliminatedasmetabolitesthroughthebileinthefaeces.

Patientswithrenalimpairment:Inpatientssufferingfromrenalimpairment,noaccumulationoftheunchangedactive

substancecanbeinferredfromthesingle-dosekineticswhenapplyingtheusualdosageschedule.Atacreatinine

clearanceof<10mL/min,thecalculatedsteady-stateplasmalevelsofhydroxymetabolitiesareabout4timeshigher

thaninnormalsubjects.However,themetabolitesareultimatelyclearedthroughthebile.

Patientswithhepaticdisease:inpatientswithchronichepatitisornon-decompensatedcirrhosis,thekineticsand

metabolismofdiclofenacarethesameasinpatientswithoutliverdisease.

5.3Preclinicalsafetydata

Preclinicaldatafromacuteandrepeateddosetoxicitystudies,aswellasfromgenotoxicity,mutagenicity,and

carcinogenicitystudieswithdiclofenacrevealednospecifichazardforhumansattheintendedtherapeuticdoses.There

wasnoevidencethatdiclofenachadateratogenicpotentialinmice,ratsorrabbits.

Diclofenachadnoinfluenceonthefertilityoftheparentanimalsinrats.Theprenatal,perinatal,andpostnatal

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6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

TabletCore:

Colloidalanhydroussilica

Calciumphosphate

Magnesiumstearate

Maizestarch

PovidoneK30

Sodiumstarchglycolate(TypeA)

CoatingandPolish:

Microcrystallinecellulose

Dispersedred(redironoxide(E172)andtitaniumdioxide(E171)

Macrogol8000

Sucrose

Povidone

Talc

6.2Incompatibilities

Notapplicable.

6.3ShelfLife

30months

6.4Specialprecautionsforstorage

Donotstoreabove30 °

C.Storeintheoriginalpackage.

6.5Natureandcontentsofcontainer

PVC/PE/PVDCfilmonaluminiumfoilblisterstrips,10tablets/strip.

Packsizes:20or30tablets.

Notallpacksizesmaybemarketed.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements.

7MARKETINGAUTHORISATIONHOLDER

NovartisPharmaceuticalsUKLimited,

FrimleyBusinessPark,

Frimley,

Camberley,

SurreyGU167SR,

Irish Medicines Board

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Date Printed 25/02/2011 CRN 2090979 page number: 10

8MARKETINGAUTHORISATIONNUMBER

PA13/88/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:13March1995

Dateoflastrenewal:25July2008

10DATEOFREVISIONOFTHETEXT

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 25/02/2011 CRN 2090979 page number: 11