DICLOFENAC 100 MG PROLONGED RELEASE TABLETS

Main information

  • Trade name:
  • DICLOFENAC 100 MG PROLONGED RELEASE TABLETS
  • Dosage:
  • 100 Milligram
  • Pharmaceutical form:
  • Tablets
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • DICLOFENAC 100 MG PROLONGED RELEASE TABLETS
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0476/010/001
  • Authorization date:
  • 05-09-1997
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

PartII

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Diclofenac100 mg Prolonged ReleaseTablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

DiclofenacSodium100 mg

Forexcipients, see6.1

3PHARMACEUTICALFORM

Prolonged releasetablet.

White, circular, biconvex tablets, diameter12.0 mmwithaGreek Deltasymbolembossed on oneside.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Reliefofallgradesofpain and inflammation in conditionssuch as:

arthriticconditions:rheumatoid arthritis, ankylosing spondylitis, acutegout, psoriaticarthropathy.

(ii) acutemusculo-skeletaldisorderssuch asperiarthritis(forexamplefrozen shoulder), tendinitis, tenosynovitis,

bursitis.

(iii) otherpainfulconditionsresulting fromtrauma, including fracture, lowback pain, sprains, bruises, strains,

dislocations, orthopaedic, dentaland otherminorsurgery.

Dysmenorrhoeaand associated menorrhagia.

Forthesymptomatictreatmentofosteoarthritis.

4.2Posologyandmethodofadminstration

Dosage

Routeofadministration:oral.

Adults:Onetabletdaily, taken wholewith liquid, preferably atmealtimes.

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

lowesteffectivedosageofdiclofenaccompatiblewith adequatesafeclinicalcontrolshould beemployed.(Seealso

Specialwarning and precautions, Section 4.4).

Treatmentshould bereviewed atregularintervalsand discontinued ifno benefitisseen orintoleranceoccurs.

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4.3Contraindications

Patientswith activeorsuspected pepticulceration, pepticulcerdiseaseorgastro-intestinalbleeding.

Previoussensitivity to diclofenacorotheringredientsofthepreparation.

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

Retard 100 mg Tablets, aspirin orothernon-steroidalanti-inflammatory drugs.

4.4Special warningsandspecialprecautionsforuse

Undesirableeffectsmay bereduced by using theminimumeffectivedosefortheshortestpossibleduration.Patients

treated with NSAIDslong-termshould undergo regularmedicalsupervision to monitorforadverseevents.

Gastro-intestinal:DiclofenacRetard 100 mg Tabletsshould beused with caution in patientswith ahistory ofpeptic

ulceration ofinflammatory disease.Patientswith ulcerativecolitisorCrohn’sdisease, bleeding diathesisor

haematologicalabnormalitiesshould also betreated with caution.In therareinstanceswheregastro-intestinalbleeding

orulceration occursin patientsreceiving diclofenacthedrugsshould bewithdrawn.

Hypersensitivityreactions:Aswithothernon-steroidalanti-inflammatory drugs, allergicreactions, including

anaphylactic/anaphylactoid reactions, can also occurwithoutearlierexposureto thedrug.

Renal:In 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 renal

function areusually reversibleon withdrawalofdiclofenac.

Hepatic:Closemedicalsurveillanceisimperativein patientssuffering fromsevereimpairmentofhepaticfunction. If

abnormalliverfunction testspersistorworsen, clinicalsignsorsymptomsconsistentwith liverdiseasedevelop orif

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

prodromalsymptoms. Useofdiclofenacin patientswith hepaticporphyriamay triggeran attack.

Haematological:AsNSAIDscan interferewith plateletfunction, they should beused with caution in patientswith

intracranialhaemorrhageand bleeding diathesis(seeanticoagulantsin‘drug interaction’).

Long-termtreatment:Allpatientswho arereceiving non-steroidalanti-inflammatory agentsshould bemonitored asa

precautionary measuree.g. renalfunction, hepaticfunction (elevation ofliverenzymesmay occur)and blood counts.

Elderly patientsareparticularly susceptibleto adverseeffectsofNSAIDs.Prolonged useofNSAIDsin theelderly is

notrecommended.Whereprolonged therapy isrequired, patientsshouldbereviewed regularly.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Itisconsidered unsafeto takeNSAIDsin combinationwith Warfarin orheparin unlessunderdirectmedical

supervision.

Careshould betaken in patientstreated with anyofthefollowing drugsasinteractionshavebeen reported.

Anti-hypertensives:reduced anti-hypertensiveeffect.

Diuretics:reduced diureticeffect.Diureticscan increasetherisk ofnephrotoxicityofNSAIDs.

Cardiacglycosides:NSAIDsmay exacerbatecardiacfailure, reduceGFRand increaseplasmacardiacglycoside

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Lithium:decreased elimination oflithium.

Methotrexate:decreased elimination ofmethotrexate.

Cyclosporin:increased risk ofnephrotoxicity with NSAIDs.

OtherNSAIDS:avoid concomitantuseoftwo ormoreNSAIDs.

Corticosteroids:increased risk ofgastrointestinalbleeding.

Aminoglycosides:reduction in renalfunction in susceptibleindividuals, decreasedelimination ofaminoglycosideand

increased plasmaconcentrations.

Probenecid:reduction in metabolismand elimination ofNSAIDand metabolites.

Oralhypoglycaemicagents:inhibition ofmetabolismofsulphonylureadrugs, prolonged half-lifeand increased risk

ofhypoglycaemia.

4.6Pregnancyandlactation

Although animalstudieshavenotdemonstrated teratogeniceffects, diclofenacshould notbeprescribed during

pregnancy, unlesstherearecompelling reasonsfordoing so. Thelowesteffectivedosageshould beused.

Useofprostaglandin synthetaseinhibitorsduring thethird trimesterofpregnancy may resultin prematureclosureof

theductusarteriosusoruterineinertiaand should thereforebeavoided.

Following oraladministration ofdiclofenac, tracesofactivesubstancehavebeen detected in breastmilk in trace

quantitiesunlikely to haveany undesirableeffectson theinfant.

4.7Effectsonabilitytodriveandusemachines

Patientswhoexperiencedizzinessorothercentralnervoussystemdisturbanceswhiletaking NSAIDsshould refrain

fromdriving oroperating machinery.

4.8Undesirableeffects

Ifseriousside-effectsoccur, diclofenacshould bewithdrawn.

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:

Occasional:Headache, dizziness,orvertigo.

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.

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

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

including allergicpurpura.

Kidney:

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.

Otherorgansystems:

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

hypotension).

Isolated cases:Impotence(association with diclofenacintakeisdoubtful), palpitation,chestpain, hypertension.

4.9Overdose

Managementofacutepoisoning with NSAIDsessentially consistsofsupportiveand symptomaticmeasures. Thereis

no typicalclinicalpictureresulting fromdiclofenacoverdosage.

Thefollowing therapeuticmeasuresmay betaken:

1. Absorption should beprevented assoon aspossibleafteroverdosageby meansofgastriclavageandtreatmentwith

activated charcoal;

2. Supportiveand symptomatictreatmentforcomplicationssuch ashypotension, renalfailure, convulsions, gastro-

intestinalirritation, and respiratory depression.

Specifictherapiessuch asforced diuresis,dialysisorhaemoperfusion areunlikely to beofhelp ineliminating NSAIDs

dueto theirhigh rateofproteinbinding and extensivemetabolism.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

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

inhibitorofcyclo-oxygenase. Diclofenacsodiumin vitro doesnotsuppressproteoglycan biosynthesisin cartilageat

concentrationsequivalentto theconcentrationsreached in human beings.

5.2Pharmacokineticproperties

Diclofenacsodiumisrapidly absorbed fromthegutand 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 fromthesynovialfluid 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

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Metabolitesinclude4-hydroxy diclofenac, 5-hydroxy diclofenac, 3-hydroxy diclofenacand 4,5-dihydroxy diclofenac.

Themetabolitesareexcreted in theformofglucuronideand sulphateconjugates. Approximately 60%ofthe

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

remainderofthedoseisexcreted viathebilein metabolised form.

In patientswith impaired renalfunction, no accumulation ofdiclofenachasbeen reported.

5.3Preclinical safetydata

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Hydrogenated vegetableoil

Lactose

Magnesiumstearate

Povidone

Talc

6.2Incompatibilities

Notapplicable.

6.3ShelfLife

2 years.

6.4Special precautionsforstorage

Do notstoreabove25°C.

6.5Natureandcontentsofcontainer

Blisterpacks(A1/PVC), PP-containerwith LDPEcap (Securitainer), HDPE-containerwith LDPEcap (Scanstar).

Pack sizes:28, 30, 56, 100 tablets.

6.6Instructionsforuseandhandling

None.

7MARKETINGAUTHORISATIONHOLDER

Olinka(UK)Limited

38/40, ChamberlayneRoad

London

NW10 3JE

OralLD50: 59 mg/kg No toxiceffectsnoted

Mouse OralLD50: 125 mg/kg No toxiceffectsnoted

OralLD50: 53 mg/kg Behavioural(altered sleep time, ataxia),

Lungs, thorax orrespiration (respiratory stimulation)

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8MARKETINGAUTHORISATIONNUMBER

PA476/10/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation: 5 th

September1997

Dateoflastrenewal:5 th

September2002

10DATEOFREVISIONOFTHETEXT

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Date Issued 11/11/2005 CRN 2016774 page number: 6