ACULAR

Main information

  • Trade name:
  • ACULAR Eye Drops Solution 0.5 %w/v
  • Dosage:
  • 0.5 %w/v
  • Pharmaceutical form:
  • Eye Drops Solution
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • ACULAR Eye Drops Solution 0.5 %w/v
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PPA1562/037/001
  • Authorization date:
  • 12-11-2010
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Acular0.5%w/vEyeDrops,solution

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Ketorolactrometamol0.5%w/v

Excipients:Benzalkoniumchloride0.01%w/v

Forafulllistofexcipients,seesection6.1

3PHARMACEUTICALFORM

Eyedrops,solution

ProductimportedfromtheUK

Clear,colourlesstopaleyellowaqueoussolution.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Fortheprophylaxisandreductionofinflammationfollowingcataractsurgery.

Acularisindicatedinadults.

4.2Posologyandmethodofadministration

Posology

Post-operativeinflammation:

Onedropinstilledintotheeyethreetimesdailystarting24hoursbeforesurgeryandcontinuingforthreetofourweeks.

Paediatricpopulation

ThereisnorelevantuseofACULARinthepaediatricpopulationintheindication:Fortheprophylaxisandreduction

ofinflammationfollowingcataractsurgery.

Methodofadministration

Ocularuse.

Instilonedropofthesolutionintotheinferiorconjunctivalsacoftheeyetobetreated,whilepullingthelowereyelid

gentlydownwardsandlookingupwards.

4.3Contraindications

Hypersensitivitytotheactivesubstanceoranyoftheexcipients

Thepotentialexistsforcross-sensitivitytoacetylsalicylicacidandothernon-steroidalanti-inflammatory

drugs.ACULAR ®

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4.4Specialwarningsandprecautionsforuse

ItisrecommendedthatACULAR ®

beusedwithcautioninpatientswithknownbleedingtendenciesorwho

arereceivingothermedicationswhichmayprolongbleedingtime.

Incommonwithotheranti-inflammatorydrugs,ACULAR ®

maymasktheusualsignsofinfection.

Allnon-steroidalanti-inflammatorydrugs(NSAIDs)mayslowdownordelaywoundhealing.Concomitantuseof

NSAIDsandtopicalsteroidscanincreasethepotentialforhealingproblems.ConcomitantuseofACULARandtopical

corticosteroidsshouldbeexercisedwithcautioninpatientssusceptibletocornealepithelialbreakdown.

UseoftopicalNSAIDSmayresultinkeratitis.Insomepatients,continueduseoftopicalNSAIDsmayresultin

epithelialbreakdown,cornealthinning,cornealerosion,cornealulcerationorcornealperforation.Theseeventsmaybe

sightthreatening.Patientswithevidenceofcornealepithelialbreakdownshouldimmediatelydiscontinueuseoftopical

NSAIDsandshouldbecloselymonitoredforcornealhealth.

TopicalNSAIDsshouldbeusedwithcautioninpatientswithcomplicatedocularsurgeries,cornealdenervation,

cornealepithelialdefects,diabetesmellitus,ocularsurfacediseases(e.g.dryeyesyndrome),rheumatoidarthritis,or

repeatocularsurgerieswithinashortperiodoftime,astheymaybeatincreasedriskforcornealadverseeventswhich

maybecomesightthreatening.

PostmarketingexperiencewithtopicalNSAIDsalsosuggestthatusemorethan24hourspriortosurgeryoruse

beyond14dayspostsurgerymayincreasepatientriskfortheoccurrenceandseverityofcornealadverseevents.

ThepreservativeinACULAR,benzalkoniumchloridemaycauseeyeirritation.

Contactlensesmustberemovedpriortoapplication,withatleasta15-minutewaitbeforereinsertion.Benzalkonium

chlorideisknowntodiscoloursoftcontactlenses.Contactwithsoftcontactlensesmustbeavoided.

Therehavebeenpost-marketingreportsofbronchospasmorexacerbationofasthmainpatients,whohaveeithera

knownhypersensitivitytoaspirin/non-steroidalanti-inflammatorydrugsorapastmedicalhistoryofasthmaassociated

withtheuseofACULAR,whichmaybecontributory.CautionisrecommendedintheuseofACULARinthese

individuals(seesection4.8).

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Nointeractionstudieshavebeenperformed.

ACULAR ®

hasbeensafelyadministeredwithsystemicandophthalmicmedicationssuchasantibiotics,sedatives,beta

blockers,carbonicanhydraseinhibitors,miotics,mydriaticslocalanaestheticsandcycloplegics.

ACULAR ®

mayslowordelayhealing.Topicalcorticosteroidsarealsoknowntoslowordelayhealing.Concomitant

useoftopicalNSAIDsandtopicalcorticosteroidsmayincreasethepotentialforhealingproblems(seesection4.4).

IfACULAR ®

isusedconcomitantlywithothertopicaleyemedicationstheremustbeanintervalofatleast5minutes

betweenthetwomedications.

4.6Fertility,pregnancyandlactation

Pregnancy

Therearenooralimitedamountofdatafromtheuseofketorolactrometamolinpregnantwomen.Animalstudiesare

insufficientwithrespecttoreproductivetoxicity.ACULARisnotrecommendedduringpregnancyandinwomenof

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Breastfeeding

ACULARshouldnotbeusedduringbreast-feeding.Ketorolactrometamolisexcretedinhumanmilkaftersystemic

administration.

Fertility:

Therearenoadequatedatafromtheuseofketorolactrometamolonfertilityinhumans.

4.7Effectsonabilitytodriveandusemachines

ACULARhasnoornegligibleinfluenceontheabilitytodriveandusemachines.

Transientblurringofvisionmayoccuroninstillationofeyedrops.Donotdriveorusehazardousmachineryunless

visionisclear.

4.8Undesirableeffects

ThemostfrequentadverseeventsreportedwiththeuseofACULARaretransientstingingandburningoninstillation.

Thefrequencyofadversereactionsdocumentedduringclinicaltrialsisgivenbelowandisdefinedasfollows:Very

Common(1/10);Common(1/100to<1/10);Uncommon(1/1,000to<1/100);Rare(1/10,000to<1/1,000);Very

Rare(<1/10,000);NotKnown(cannotbeestimatedfromavailabledata).

Withineachfrequencygrouping,undesirableeffectsarepresentedinorderofdecreasingseriousness:

Immunesystemdisorders

Common: Hypersensitivityincludinglocalisedallergicreactions

Nervoussystemdisorders

Uncommon: Headache

EyeDisorders

VeryCommon: Eyeirritation(includingburningsensation)

Eyepain(includingstinging)

Common

Superficial(punctate)keratitis

Eyeand/oreyelidoedema

Ocularpruritus

Conjunctivalhyperaemia

Eyeinfection

Eyeinflammation

Uncommon: Cornealulcer

Cornealinfiltrates

Blurredand/ordiminishedvision

Eyedryness

Epiphora

Iritis

Notknown: Cornealdamage,e.g.thinning,erosion,epithelialbreakdownandperforation*

Respiratory,thoracicandmediastinaldisorders

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*Occasionalpostmarketingreportsofcornealdamageincludingcornealthinning,cornealerosion,epithelial

breakdownandcornealperforationhavebeenreceived.Theseoccurredmainlyinpatientsusingconcomitanttopical

corticosteroidsand/orwithpredisposingco-morbidity.(seesection4.4).

**Therehavebeenpost-marketingreportsofbronchospasmorexacerbationofasthma,inpatients,whohaveeithera

knownhypersensitivitytoaspirin/non-steroidalanti-inflammatorydrugsorapastmedicalhistoryofasthma,associated

withtheuseofACULARwhichmaybecontributory.

Noneofthetypicaladversereactionsreportedwiththesystemicnon-steroidalanti-inflammatoryagents(including

ketorolactrometamol)havebeenobservedatthedosesusedintopicalophthalmictherapy.

4.9Overdose

Nocaseofoverdosehasbeenreported.Overdoseisunlikelytooccurviatherecommendedmethodofadministration.

Ifaccidentallyingested,drinkfluidstodilute.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacotherapeuticgroup:Anti-inflammatoryagents,non-steroids

ATCcode=S01BC05.

ACULAR(ketorolactrometamol)isanon-steroidalanti-inflammatoryagentdemonstratinganalgesicandanti-

inflammatoryactivity.Itisbelievedtoinhibitthecyclo-oxygenaseenzymeessentialforbiosynthesisofprostaglandins.

ACULARhasbeenshowntoreduceprostaglandinlevelsintheaqueoushumouraftertopicalophthalmic

administration.

Ketorolactrometamolgivensystemicallydoesnotcausepupilconstriction.Resultsfromclinicalstudiesindicatethat

ACULARhasnosignificanteffectonintraocularpressure.

5.2Pharmacokineticproperties

Ketorolactrometamolsolutions(0.1%or0.5%)orvehiclewereinstilledintotheeyesofpatientsapproximately12

hoursand1hourpriortosurgery.Concentrationsofketorolacinaqueoushumoursampledatthetimeofsurgerywere

atthelowerlimitofdetection(40ng/ml)in1patientandbelowthequantitationlimitin7patientsdosedwith0.1%

ketorolactrometamol.Theaverageaqueoushumourlevelofketorolacinpatientstreatedwith0.5%ketorolac

trometamolwas95ng/ml.ConcentrationsofPGEinaqueoushumourwere80pg/ml,40pg/mland28pg/mlin

patientstreatedwithvehicle,0.1%ketorolactrometamoland0.5%ketorolactrometamol,respectively.

Inthe21-daymultipledose(TID)tolerancestudyinhealthysubjects,only1of13subjectshadadetectableplasma

levelpre-dose(0.021µg/ml).Inanothergroupof13subjects,only4subjectsshowedverylowplasmalevelsof

ketorolac(0.011to0.023µg/ml)15minutesaftertheoculardose.

Thus,higherlevelsofketorolacintheaqueoushumourandverylowornodetectableplasmalevelsafterophthalmic

doses,suggestthattheuseofketorolactrometamolbytheophthalmicrouteintreatmentofoculardisordersresultsin

quitelowsystemicabsorptioninpatients.

5.3Preclinicalsafetydata

Non-clinicaldatarevealnospecialhazardforhumansbasedonconventionalstudiesofsafetypharmacology,repeated

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Acute,subacuteandchronicstudiesofACULAR ®

inexperimentalanimalshaveestablishedthesafetyofthedrug.In

addition,octoxinol40wasseparatelyevaluatedforitsocularsafety.ACULAR ®

wasfoundtobenon-irritating,itdid

notdemonstratealocalanaestheticeffect,itdidnotinfluencethehealingofexperimentalcornealwoundsinrabbits,

itdidnotenhancethespreadofexperimentalocularinfectionsofCandidaalbicans,Herpessimplexvirustypeone,

orPseudomonasaeruginosainrabbits,anditdidnotincreasetheocularpressureofnormalrabbiteyes.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Benzalkoniumchloride

Disodiumedetate

Octoxynol40,

Sodiumchloride

Sodiumhydroxideorhydrochloricacid(toadjustpH)

Purifiedwater

6.2Incompatibilities

Notapplicable.

6.3Shelflife

Theshelflifeexpirydateforthisproductshallbethedateshownonthebottleandouterpackageoftheproductonthe

marketinthecountryoforigin.

Usewithin28daysoffirstopening.

6.4Specialprecautionsforstorage

Storebelow25 o

6.5Natureandcontentsofcontainer

Bottlewithdropperapplicator,containingclear,colourlesstoslightlyyellow,sterileophthalmicsolution.Packsize:

5ml.

6.6Specialprecautionsfordisposalandotherhandling

Nospecialrequirements.

Anyunusedproductorwastematerialshouldbedisposedofinaccordancewithlocalrequirements.

7PARALLELPRODUCTAUTHORISATIONHOLDER

LTTPharmaLimited

Unit18,OxleasowRoad

EastMoonMoat

Redditch

WorcestershireB980RE

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8PARALLELPRODUCTAUTHORISATIONNUMBER

PPA1562/37/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:12 th

November2010

10DATEOFREVISIONOFTHETEXT

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