DICLOFENAC 50

Main information

  • Trade name:
  • DICLOFENAC 50
  • Dosage:
  • 50 Milligram
  • Pharmaceutical form:
  • Tablets
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • DICLOFENAC 50
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0593/008/005
  • Authorization date:
  • 18-02-2000
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

PartII

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Diclofenac50 mg StadaGastro-resistantTablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Each tabletcontainsdiclofenacsodium50 mg.

Forexcipients, seesection 6.1.

3PHARMACEUTICALFORM

Gastro-resistanttablets.

Light-brown circular, biconvex, gastro-resistanttablets, 8mmx 4.3mm.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Diclofenac50mg StadaGastro-resistantTabletsareindicated forthereliefofallgradesofpain and inflammation in a

rangeofconditions, including:

arthriticconditionssuch asrheumatoid arthritis, osteoarthritis, ankylosing spondylitis, acutegout, psoriatic

arthropathy.

acutemusculo-skeletaldisorderssuch asperiarthritis(e.g. frozen shoulder), tendinitis, tenosynovitis, bursitis.

otherpainfulconditionsresulting fromtraumaincluding fracture, lowback pain, sprains, strains, dislocations,

orthopaedic, dentaland otherminorsurgery.

themanagementofdysmenorrhoeaand associated menorrhagia.

4.2Posologyandmethodofadminstration

Fororaluseonly.

Adults:Therecommendeddoseis75-150 mg daily in two orthreedivided doses, taken wholewith liquid.

Elderly:NSAIDsshould beused with particularcaution in elderly patientswho aremoreproneto adverseevents.The

lowestdosecompatiblewith adequatesafeclinicalcontrolshould beemployed. Seealso Section 4.4.Thelower

strength Diclofenacpreparationsmay thereforebeappropriate.

Children:Therecommendeddoseis1-3 mg/kg daily in divided doses.

Treatmentshould bereviewed atregularintervalsand discontinued ifno benefitisseen.

4.3Contraindications

Patientswith ahistory ofhypersensitivity reactions(e.g.bronchospasm, rhinitis, urticaria)in responseto Diclofenac,

aspirin ornonsteroidalanti-inflammatory drugs.

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4.4Special warningsandspecialprecautionsforuse

Undesirableeffectsmay bereduced by using theminimumeffectivedosefortheshortestpossibleduration.Patients

treated with NSAIDslong-termshould undergo regularmedicalsupervision to monitorforadverseeffects.

Elderly patientsareparticularly susceptibleto theadverseeffectsofNSAIDs.Prolonged useofNSAIDsin theelderly

isnotrecommended. When prolonged therapy isrequired, patientsshould bereviewed regularly.

Gastro-intestinal:Diclofenacshould beused with caution in patientswith ahistory ofpepticulceration or

inflammatory boweldisease.

Gastro-intestinalbleeding orulceration/perforation, haematemesisand melaenain generalhavemoreserious

consequencesin theelderly.They can occuratany timeduring treatmentwith orwithoutwarning symptomsora

previoushistory.In therareinstanceswheregastro-intestinalbleeding orulceration occursin patientsreceiving

Diclofenacthedrug should bewithdrawn.

Hypersensitivityreactions:AswithotherNSAIDs, allergicreactions, including anaphylactic/anaphylactoid

reactions, can also occurwithoutearlierexposureto thedrug.

Renal:Patientswith renal, cardiacorhepaticimpairment, caution isrequired sincetheuseofNSAIDsmay resultin

deteriorationofrenalfunction.Assessmentofrenalfunction should occurpriorto theinitiation oftherapy and

regularlythereafter.

Theimportanceofprostaglandinsinmaintaining renalblood flowshould betaken into accountin patientswith

impaired cardiacorrenalfunction, thosebeing treated with diureticsorrecovering frommajorsurgery.Effectson

renalfunction areusually reversibleon withdrawalofDiclofenac.

Hepatic:Closemedicalsurveillanceisimperativein patientssuffering fromsevereimpairmentofhepaticfunction.If

abnormalliverfunction testspersistorworsen, clinicalsignsorsymptomsconsistentwith liverdiseasedevelop orif

othermanifestationsoccur(eosinophilia, rash), Diclofenacuseshould bediscontinued.Hepatitismay occurwithout

prodromalsymptoms.UseofDiclofenacin patientswith hepaticporphyriamay triggeran attack.

Haematological:AsNSAIDscan interferewith plateletformation, theyshould beused with caution in patientswith

intracranialhaemorrhageand bleeding diathesis.

Patientswith rarehereditary problemsofgalactoseintolerance, theLapp lactasedeficiency orglucose-galactose

malabsorption should nottakethismedicine.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

ItisconsideredunsafetotakeNSAIDsincombinationwithwarfarinorheparinunlessunderdirectmedical

supervision.

Careshould betaken in patientstreated with anyofthefollowing drugsasinteractionshavebeen reported:

Lithium:Decreased eliminationoflithium.

Methotrexate:Decreased eliminationofmethotrexate.Casesofserioustoxicity havebeen reported when

methotrexateand NSAIDsaregiven within24 hoursofeach other.Thisinteraction ismediated through accumulation

ofmethotrexateresulting fromimpairmentofrenalexcretion in thepresenceoftheNSAID.

Cardiacglycosides:NSAIDsmay exacerbatecardiacfailure, reduceGFRand increaseplasmacardiacglycoside

levels.

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OtherNSAIDs:Avoid concomitantuseoftwo ormoreNSAIDs.

Aminoglycosides:Reduction in renalfunction in susceptibleindividualsdecreased elimination ofaminoglycosideand

increased plasmaconcentrations.

Probenecid:Reduction inmetabolismand elimination ofNSAIDand metabolites.

Oralhypoglycaemicagents:Inhibition ofmetabolismofsulphonylureadrugs, prolonged half-lifeand increased risk

ofhypoglycaemia.Clinicalstudieshaveshown thatDiclofenaccan begiven togetherwith oralantidiabeticagents

withoutinfluencing theirclinicaleffect.

Cyclosporin:Increased risk ofnephrotoxicity with NSAIDs.Thismightbemediated through thecombined renal

antiprostaglandin effectsofboth NSAIDsand cyclosporin.

Quinoloneantimicrobials:Convulsionsmay occurdueto an interaction between quinolonesand NSAIDs.Thismay

occurin patientswith orwithoutaprevioushistory ofepilepsy orconvulsions.Therefore, caution should beexercised

when considering theuseofaquinolonein patientswho arealready receiving an NSAID.

Corticosteroids:Increased risk ofgastro-intestinalbleeding.

Diuretics:Reduced diureticeffect.Diureticscan increasetherisk ofnephrotoxicityofNSAIDs.VariousNSAIDs

areliableto inhibittheactivity ofloop-typediureticsin particular.Concomitanttreatmentwith potassium-sparing

diureticsmay beassociated with increased serumpotassiumlevels,henceserumpotassiumshould bemonitored.

4.6Pregnancyandlactation

No teratogeniceffectshavebeen observed in animalstudies.However, dueto lack ofevidenceofsafety, Diclofenac

should notbeprescribed during pregnancy, unlesstherearecompelling reasonsfordoing so.Thelowesteffectivedose

should beused.

Useofprostaglandin synthetaseinhibitorsmay resultin prematureclosureoftheductusarteriosusoruterineinertia;

such drugsarethereforenotrecommended during thelasttrimesterofpregnancy.

Following oraldosesof50mg Diclofenacevery 8 hours, tracesofactivesubstancehavebeen detected in breastmilk,

butin quantitiesso smallthatno undesirableeffectson theinfantareto beexpected.

4.7Effectsonabilitytodriveandusemachines

Patientswhoexperiencedizzinessorothercentralnervoussystemdisturbanceswhiletaking NSAIDsshould refrain

fromdriving oroperating machinery.

4.8Undesirableeffects

Ifseriousside-effectsoccur, Diclofenacshould bewithdrawn.Thefollowing side-effectshavebeen reported:

Frequency estimate:frequent:>10%, occasional:>110%, rare:>0.001%1%, isolated cases:<0.001%.

Gastro-intestinaltract:

Occasional:Epigastricpain, othergastro-intestinaldisorders(e.g. nausea, vomiting, diarrhoea, abdominalcramps,

dyspepsia, flatulence, anorexia).

Rare:Gastro-intestinalbleeding, pepticulcer(with orwithoutbleeding orperforation), bloody diarrhoea.

In isolated cases:Lowergutdisorders(e.g. non-specifichaemorrhagiccolitisand exacerbationsofulcerativecolitisor

Crohn’sproctocolitis), pancreatitis, aphthousstomatitis, glossitis, oesophageallesions, constipation.

Centralnervoussystem:

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Rare:Drowsiness, tiredness.

In isolated cases:Disturbancesofsensation, paraesthesia, memory disturbance, disorientation, disturbanceofvision

(blurred vision, diplopia), impaired hearing, tinnitus, insomnia, irritability, convulsions, depression, anxiety,

nightmares, tremor, psychoticreactions.Tastealteration disorders.

Skin:

Occasional:Rashesorskin eruptions.

Rare:Urticaria.

In isolated cases:Bullouseruptions, eczema, erythemamultiforme, Stevens-Johnson syndrome, Lyell’ssyndrome

(acutetoxicepidermolysis), erythroderma(exfoliativedermatitis), lossofhair, photosensitivity reactions, purpura

including allergicpurpura.

Kidney:

Rare:oedema

In isolated cases:Acuterenalinsufficiency, urinaryabnormalities(e.g. haematuria, proteinuria), interstitialnephritis,

nephroticsyndrome, papillary necrosis.

Liver:

Occasional:Elevation ofserumaminotransferaseenzymes(ALT, AST).

Rare:Liverfunction disordersincluding hepatitis(in isolated casesfulminant)with orwithoutjaundice.

Blood:

In isolated cases:Thrombocytopenia, leucopenia, agranulocytosis, haemolyticanaemia, aplasticanaemia.

Cardiovascularsystem:

Isolated cases:palpitations, chestpain, hypertension, congestiveheartfailure.

Hypersensitivity:

Rare:hypersensitivity reactions(e.g. bronchospasm, anaphylactic/anaphylactoid systemicreactionsincluding

hypotension).

Otherorgansystems:

Isolated cases:Impotence(association with Diclofenacintakeisdoubtful).

4.9Overdose

Managementofacutepoisoning with NSAIDsessentially consistsofsupportiveand symptomaticmeasures. Thereis

no typicalclinicalpictureresulting fromDiclofenacoverdosage.Thetherapeuticmeasuresto betaken are:absorption

should beprevented assoon aspossibleafteroverdosageby meansofgastriclavageand treatmentwith activated

charcoal;supportiveand symptomatictreatmentshould begiven forcomplicationssuch ashypotension, renalfailure,

convulsions,gastro-intestinalirritation, and respiratory depression;specifictherapiessuch asforced diuresisdialysisor

haemoperfusion areprobably ofno help in eliminating NSAIDsdueto theirhigh rateofprotein binding and extensive

metabolism.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacotherapeuticgroup:Anti-inflammatory and antirheumaticproducts, non-steroids, ATCcodeM01 AB05

Diclofenacisanon-steroidalagentwith marked analgesic, anti-pyreticand anti-inflammatory properties. Itisan

inhibitorofcyclo-oxygenase.Diclofenacsodiumin vitrodoesnotsuppressproteoglycan biosynthesisin cartilageat

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5.2Pharmacokineticproperties

Diclofenacsodiumisrapidly absorbed formthegutand issubjectto first-passmetabolism,only 50-60%ofthedrug

reaching thesystemiccirculation in theunchanged form.

Theactivesubstanceismorethan 99%protein bound. Theplasmahalf-lifefortheterminalelimination phaseis1-2

hours.

Diclofenacentersthesynovialfluid, wheremaximumconcentrationsaremeasured 2-4 hoursafterthepeak plasma

valueshavebeen obtained. Theapparenthalf-lifeforelimination formthesynovialfluid is3-6 hours. Two hoursafter

reaching thepeak plasmavalues, concentrationsoftheactivesubstancearealready higherin thesynovialfluid than

they arein theplasma, and they remain higherforup to 12 hours. Diclofenachasalso been detected in thebreastmilk

followingoraladministration (seesection 4.6 Pregnancy and lactation).

Metabolitesinclude4-hydroxy Diclofenac, 5-hydroxy Diclofenac, 3-hydroxy Diclofenacand 4,5-dihydroxy

Diclofenac. Themetabolitesareexcreted in theformofglucuronideand sulphateconjugates. Approximately 60%of

theadministered doseisexcreted viathekidneysin theformofmetabolitesand lessthan 1%in unchanged form. The

remainderofthedoseisexcreted viathebilein metabolised form.

In patientswith impaired renalfunction, no accumulation ofDiclofenachasbeen reported.

5.3Preclinical safetydata

Dog OralLD50:59 mg/kg No toxiceffectsnoted.

MouseOralLD50:125 mg/kg No toxiceffectsnoted.

RatOralLD50:53 mg/kg Behavioural(altered sleep time, ataxia), lungs, thorax orrespiration (respiratory

stimulation).

RabbitOralLD50:157 mg/kg No toxiceffectsnoted.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Tabletcore

Maizestarch

Microcrystallinecellulose

Lactosemonohydrate

PovidoneK30

Colloidalanhydroussilica

Magnesiumstearate

Tabletcoat

Poly (methacrylate, methylmethacrylate)

O-Acetyltriethylcitrate

Hypromellose

Macrogol6000

Macrogol400

Talc

Titaniumdioxide(E171)

Ferricoxidered (E172)

Ferricoxideyellow(E172)

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6.2Incompatibilities

Notapplicable.

6.3ShelfLife

2 years.

6.4Special precautionsforstorage

Do notstoreabove25°C.

6.5Natureandcontentsofcontainer

A1/PVCblisters. Packsizesof20, 50 and 100 tablets.

Notallpack sizesmay bemarketed.

6.6Instructionsforuseandhandling

Swallowwhole. Do notchew.

7MARKETINGAUTHORISATIONHOLDER

StadaArzneimittelAG

Stadastrae2-18

61118 Bad Vilbel

Germany

8MARKETINGAUTHORISATIONNUMBER

PA593/8/5

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation: 18 th

February 2000

Dateoflastrenewal: 18 th

February 2005

10DATEOFREVISIONOFTHETEXT

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