ACULAR

Main information

  • Trade name:
  • ACULAR Eye Drops Solution 0.5 Per Cent
  • Dosage:
  • 0.5 Per Cent
  • Pharmaceutical form:
  • Eye Drops Solution
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • ACULAR Eye Drops Solution 0.5 Per Cent
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PPA1447/019/001
  • Authorization date:
  • 14-11-2008
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

ACULAR0.5%w/vEyedrops,solution

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Ketorolactrometamol5mg/ml.

Excipients:Benzalkoniumchloride0.1mg/ml.

Forafulllistofexcipients,seeSection6.1

3PHARMACEUTICALFORM

EyeDrops,Solution.

ProductimportedfromFrance:

Clear,colourlesstopaleyellowaqueoussolution.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Fortheprophylaxisandreductionofinflammationfollowingcataractsurgery.

ACULARisindicatedinadults.

4.2Posologyandmethodofadministration

Posology

Post-operativeinflammation:

Onedropinstilledintotheeyethreetimesdailystarting24hoursbeforesurgeryandcontinuingforthreetofourweeks.

PaediatricPopulation

ThereisnorelevantuseofACULARinthepaediatricpopulationintheindication:Fortheprophylaxisandreduction

ofinflammationfollowingcataractsurgery.

Methodofadministration

Ocularuse.

Instilonedropofthesolutionintotheinferiorconjunctivalsacoftheeyetobetreated,whilepullingthelowereyelid

gentlydownwardsandlookingupwards.

4.3Contraindications

Hypersensitivitytotheactivesubstanceortoanyoftheexcipients.

Thepotentialexistsforcross-sensitivitytoacetylsalicylicacidandothernon-steroidalanti-inflammatorydrugs.

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4.4Specialwarningsandprecautionsforuse

ItisrecommendedthatACULARbeusedwithcautioninpatientswithknownbleedingtendenciesorwhoare

receivingothermedicationswhichmayprolongbleedingtime.

Incommonwithotheranti-inflammatorydrugs,ACULARmaymasktheusualsignsofinfection.

Allnon-steroidalanti-inflammmatorydrugs(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,benzalkoniumchloride,maycauseeyeirritation.Contactlensesmustberemovedprior

toapplication,withatleasta15minutewaitbeforereinsertion.Benzalkoniumchlorideisknowntodiscoloursoft

contactlenses.Contactwithsoftcontactlensesmustbeavoided.

Therehavebeenpostmarketingreportsofbronchospasmsorexacerbationofasthmainparients,whohaveeithera

knownhypersensitivitytoaspirin/non-steroidalanti-inflammatorydrugsorapastmedicalhistoryofasthmaassociated

withtheuseofACULAR,whichmaybecontributory.CautionisrecommendedintheuseofACULARinthese

individuals(seesection4.8).

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Nointeractionstudieshavebeenperformed.

ACULARhasbeensafelyadministeredwithsystemicandophthalmicmedicationssuchasantibiotics,sedatives,beta

blockers,carbonicanhydraseinhibitors,miotics,mydriaticslocalanaestheticandcycloplegics.

ACULARmayslowordelayhealing.Topicalcorticosteroidsarealsoknowntoslowordelayhealing.Concomitant

useoftopicalNSAIDsandtopicalcorticosteroidsmayincreasethepotentialforhealingproblems(seesection4.4).

IfACULARisusedconcomitantlywithothertopicaleyemedicationstheremustbeanintervalofatleast5minutes

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4.6Fertility,pregnancyandlactation

Pregnancy

Therearenooralimitedamountofdatafromtheuseofketorolactrometamolinpregnantwomen.Animalstudiesare

insufficientwithrespecttoreproductivetoxicity.ACULARisnotrecommendedduringpregnancyandinwomaenof

childbearingpotentialnotusingcontraception.

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);

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

Withineachprequencygrouping,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/ordiminished

Eyedryness

Epiphora

Iritis

NotKnown Cornealdamage,e.g.thinning,erosion,epithelialbreakdownandperforation*

Respiratory,thoracicandmediastinaldisorders

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Occasionalpostmarketingreportsofcornealdamageincludingcornealthinning,cornealerosion,epithelialbreakdownandcorneal

perforationhavebeenreceived.Theseoccurredmainlyinpatientsusingconcomitanttopicalcorticosteroidsand/orwithpredisposingco-

morbidity(seesection4.4).

**Therehavebeenpost-marketingreportsofbrochospasmorexacerbationofasthma,inpatients,whohaveeitheraknownhypersensitivityto

aspirin/non-steroidalanti-inflammatorydrugsorapastmedicalhistoryofasthma,associatedwiththeuseofACULARwhichmaybe

contributory.

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-inflammatory

activity.Itisbelievedtoinhibitthecyclo-oxygenaseenzymeessentialforbiosynthesisofprostaglandins.ACULARhasbeen

showntoreduceprostaglandinlevelsintheaqueoushumouraftertopicalophthalmicadministration.

Ketorolactrometamolgivensystemicallydoesnotcausepupilconstriction.ResultsfromclinicalstudiesindicatethatACULAR

hasnosignificanteffectonintraocularpressure.

5.2Pharmacokineticproperties

Ketorolactrometamolsolutions(0.1%or0.5%)orvehiclewereinstilledintotheeyesofpatientsapproximately12hoursand1

hourpriortosurgery.Concentrationsofketorolacinaqueoushumoursampledatthetimeofsurgerywereatthelowerlimitof

detection(40ng/ml)in1patientandbelowthequantitationlimitin7patientsdosedwith0.1%ketorolactrometamol.Theaverage

aqueoushumourlevelofketorolacinpatientstreatedwith0.5%ketorolactrometamolwas95ng/ml.ConcentrationsofPGE2in

aqueoushumourwere80pg/ml,40pg/mland28pg/mlinpatientstreatedwithvehicle,0.1%ketorolactrometamoland0.5%

ketorolactrometamol,respectively.

Inthe21-daymultipledose(TID)tolerancestudyinhealthysubjects,only1of13subjectshadadetectableplasmalevelpre-dose

(0.021g/ml).Inanothergroupof13subjects,only4subjectsshowedverylowplasmalevelsofketorolac(0.011to0.023g/ml)15

minutesaftertheoculardose.

Thus,higherlevelsofketorolacintheaqueoushumourandverylowornodetectableplasmalevelsafterophthalmicdoses,

suggestthattheuseofketorolactrometamolbytheophthalmicrouteintreatmentofoculardisordersresultsinquitelowsystemic

absorptioninpatients.

5.3Preclinicalsafetydata

Non-clinicaldatarevealnospecialhazardforhumansbasedonconventionalstudiesofsafetypharmacology,repeated

dosetoxicity,genotoxicity,carcinogenicpotential,toxicitytoreproductionanddevevlopment.

Acute,subacuteandchronicstudiesofACULARinexperimentalanimalshaveestablishedthesafetyofthedrug.In

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demonstratealocalanaestheticeffect,itdidnotinfluencethehealingofexperimentalcornealwoundsinrabbits,itdid

notenhancethespreadofexperimentalocularinfectionsofCandidaalbicans,Herpessimplexvirustypeone,or

Pseudomonasaeruginosainrabbits,anditdidnotincreasetheocularpressureofnormalrabbiteyes.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Sodiumchloride

DisodiumEdetate

Octoxinol

Benzalkoniumchloride

Sodiumhydroxideorhydrochloricacid(dilute),toadjustpHto7.4-7.8

Purifiedwater

6.2Incompatibilities

Notapplicable.

6.3Shelflife

Theshelf-lifeexpirydateofthisproductshallbethedateshownonthecontainerandouterpackageoftheproductonthemarket

inthecountryoforigin.

Usewithin15daysoffirstopening.

6.4Specialprecautionsforstorage

Storebelow25 o

6.5Natureandcontentsofcontainer

Dropperbottles(withdropperlids)containing5mlofsolution.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements.

Anyunusedproductorwastematerialshouldbedisposedofinaccordancewithlocalrequirements.

7PARALLELPRODUCTAUTHORISATIONHOLDER

G&ALicensingLimited

Ballymurray

Co.Roscommon

Ireland

8PARALLELPRODUCTAUTHORISATIONNUMBER

PPA1447/19/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

DateofFirstAuthorisation:14 th

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10DATEOFREVISIONOFTHETEXT

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