BETOPTIC

Main information

  • Trade name:
  • BETOPTIC 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:
  • BETOPTIC Eye Drops Solution 0.5 %w/v
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PPA1447/039/001
  • Authorization date:
  • 25-02-2011
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Betoptic0.5%w/v,EyeDrops,Solution.

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Betaxolol0.5%w/v(ashydrochloride)

Excipients-ContainsBenzalkoniumChloride

Forafulllistofexcipients,seesection6.1.

3PHARMACEUTICALFORM

Eyedropssolution

ProductimportedfromGreece:

Aclear,colourlesstopaleyellowsterile,eyedropssolution

4CLINICALPARTICULARS

4.1TherapeuticIndications

Betopticisindicatedforthereductionofelevatedintraocularpressureinpatientswithocularhypertensionandchronic

openangleglaucoma.

4.2Posologyandmethodofadministration

Adults(includingtheelderly)

Theusualdoseisonedroptobeinstilledintotheaffectedeye(s)twicedaily.

Children

Betopticisnotrecommendedforuseinchildren.

4.3Contraindications

Hypersensitivitytotheactivesubstanceortoanyoftheexcipients.

Betopticiscontraindicatedinpatientswithsinusbradycardia,greaterthanafirstdegreeatrioventricularblock,

cardiogenicshockorpatientswithuncontrolledcongestivecardiacfailure.

4.4Specialwarningsandprecautionsforuse

Topicallyappliedbeta-blockerscanbesystemicallyresorbed.Consequently,thesameundesirableeffectscanappearas

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Followingmeasuresare,afterapplicationoftheeyedrops,usefultoreducesystemicresorption:

Keeptheeyelidclosedfor2minutes.

Closethelacrimalductwiththefingerfor2minutes.

Ophthalmicbetaxololhasbeenshowntohaveaminoreffectonheartrateandbloodpressureinclinicalstudies.

Cautionshouldbeusedintreatingpatientswithahistoryofcardiacfailureorheartblock.TreatmentwithBetoptic

shouldbediscontinuedatthefirstsignsofcardiacfailure.

DiabetesMellitus

Beta-adrenergicblockingagentsshouldbeadministeredwithcautioninpatientssubjecttospontaneoushypoglycemia

ortodiabeticpatients(especiallythosewithlabilediabetes)whoarereceivinginsulinororalhypoglycemicagents.

Beta-adrenergicreceptorblockingagentsmaymaskthesignsandsymptomsofacutehypoglycemia.

Thyrotoxicosis

Beta-adrenergicblockingagentsmaymaskcertainclinicalsigns(e.g.tachycardia)orhyperthyroidism.Patients

suspectedofdevelopingthyrotoxicosisshouldbemanagedcarefullytoavoidabruptwithdrawalofbeta-adrenergic

blockingagents,whichmightprecipitateathyroidstorm.

Majorsurgery

Considerationmaybegiventothegradualwithdrawalofbeta-adrenergicblockingagentspriortogeneralanesthesia,

becauseofthereducedabilityofthehearttorespondtobeta-adrenergicallymediatedsympatheticreflexstimuli.

Pulmonary

Betaxololisacardioselectivebeta-blocker,andtheophthalmicadministrationhasproducedonlyminimaleffectsin

patientswithobstructiveairwaysdisease.However,wheezing,bronchospasmanddyspnoeahaveoccurredinsome

patients.Althoughrechallengeofsomepatientswithophthalmicbetaxololhasnotadverselyaffectedpulmonary

functiontestresults,thepossibilityofadversepulmonaryeffectsinpatientssensitivetobeta-blockerscannotberuled

out.Cautionshouldbeexercisedinthetreatmentofpatientswithexcessiverestrictionofpulmonaryfunction.

Theriskofinducingbronchospasmmustbeappreciatedinpatientswithsymptomaticorpoorlycontrolledasthmaor

obstructiveairwaydiseases.Appropriateprecautions,includingconsiderationofalternativeglaucomatherapies,should

betaken.

Myasthenia

Beta-adrenergicblockadehasbeenreportedtopotentiatemuscleweaknessconsistentwithcertainmyasthenic

symptoms(e.g.diplopia,ptosis,generalizedweakness).Beta-adrenergicblockadehasbeenreportedtounmaskor

worsensymptomsassociatedwithmyastheniagravis.

Ocular

Inpatientswithangle-closureglaucoma,theimmediatetreatmentobjectiveistoreopentheanglebyconstrictionofthe

pupilwithamioticagent.Betaxololhaslittleornoeffectonthepupil.WhenBetopticisusedtoreduceelevated

intraocularpressureinangle-closureglaucoma,itshouldbeusedwithamioticandnotalone.

Limitedclinicalexperiencesuggeststhattheproductissuitableforuseinaphakicpatients.

Betopticshouldnotbeappliedwhilewearingcontactlenses;lensesshouldnotbeinsertedfor15minutesafter

instillationofproduct.

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4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Eachinteractionthatisassociatedwithsystematicallyadministeredbetablockerscan,inprinciple,appearwiththeuse

ofbetablockereyedrops.

Patientswhoarereceivingabeta-adrenergicblockingagentorallyBetopticshouldbeobservedforpotentialadditive

effecteitherontheintraocularpressureorontheknownsystemiceffectsofbetablockade.Orallyadministeredbeta-

adrenergicblockingagentsreducecardiacoutputinhealthysubjectsandpatientswithheartdiseases.Inpatientswith

severeimpairmentofmyocardialfunction,beta-adrenergicreceptorantagonistsmayinhibitthesympatheticstimulatory

effectnecessarytomaintainadequatecardiacfunction.

Becauseofpossibleadditiveeffects,andespeciallytheproductionofhypotensionand/orbradycardia,close

observationofthepatientisrecommendedwhenabetablockerisadministeredwithotherproductswithsimilar

cardiovasculareffectsorcatecholamine-depletingdrugssuchasreserpine.

Betaxololisanadrenergicblockingagent;therefore,cautionshouldbeexercisedinpatientsusingconcomitant

adrenergicpsychotropicdrugs.

AlthoughBetopticusedalonehaslittleornoeffectonpupilsize,mydriasisresultingfromconcomitanttherapywith

Betopticandadrenalinehasbeenreportedoccasionally.

Ifsupplementaryeyepreparationsaretobeused,thepatientshouldwait15minutesbetweenthetwoapplications.

4.6Fertility,pregnancyandlactation

Pregnancy

Therearenoadequateandwell-controlledstudiesinpregnantwomen.Postimplantationloss,butnoteratogenicity,was

seeninanimalsadministeredbetaxololatdosesgreatlyinexcessofthoseoccurringwithBetopticEyeDrops(see

section5.3).Asthepotentialriskforhumansisunknown,itisrecommendedtouseBetopticduringpregnancyonlyif

clearlynecessary.

Lactation

ItisnotknownwhetherBetaxololHCIisexcretedinhumanmilk.Becausemanydrugsareexcretedinhumanmilk,

cautionshouldbeexercisedwhenBetopticisadministeredtonursingwomen.

4.7Effectsonabilitytodriveandusemachines

TheinstillationofBetopticmaytemporarilyimpairvision.Ifblurredvisionoccursatinstillation,thepatientmustwait

untilthevisionclearsbeforedrivingorusingmachinery.

4.8Undesirableeffects

Themostfrequentlyoccurringundesirableeffectsareeyediscomfort,irritationandhyperaemiafollowinginstillation.

Systemicreactionsfollowingtopicaladministrationofbetaxololhavebeenrarelyreported.

Thefollowingundesirableeffectshavebeenobserved:

Psychiatricdisorders

Rare(>1/10,000to1/1000):Depression.

Nervoussystemdisorders

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Eyedisorders

Common(>1/100to1/10):Oculardiscomfort,eyeirritation,ocularhyperaemia.

Uncommon(>1/1000to1/100):Eyepruritus,abnormalsensationineye,visionblurred,photophobia,lacrimation

increased.

Rare(>1/10,000to1/1000):Eyeallergy,punctuatekeratis,ptosis,madarosis,keratoconjunctivissicca.

Cardiacdisorders

Rare(>1/10,000to1/1000):Bradycardia.

Respiratory,thoraricandmediastinaldisorders

Rare(>1/10,000to1/1000):Dyspnosea,asthma.

Skinandsubcutaneoustissuedisorders

Rare(>1/10,000to1/1000):Alopecia.

Musculoskeletalandconnectivetissuedisorders

Rare(>1/10,000to1/1000):Muscularweakness,myalgia.

Sincetopicallyappliedbeta-adrenergicblockingagentsmaybeabsorbedsystemically,adversereactionsfoundwith

systemicadministrationofbeta-1-adrenergicblockingagentsmayoccurwithtopicaladministration(seesection4.4

SpecialWarnings).

Thesemayincludebradycardia,aslowedAV~conductionorincreaseofanexistingAV~block,hypotension,heart

failure,coldandcyanoticextremities,Raynaudphenomenon,paraesthesiaoftheextremities,increaseofanexisting

intermittentclaudication,fatigue,headaches,impairedvision,hallucinations,psychoses,confusion,impotence,

dizziness,sleepdisturbances,depression,nightmares,gastro-intestinalproblems,nausea,vomiting,diarrhoea,

bronchospasminpatientswithbronchialasthmaorahistoryofasthmaticcomplaints,disorderoftheskinespecially

rash,anddryeyes.Betablockersmaymaskthesymptomsofthyrotoxicosisorhypoglycaemia.AnincreaseinAnti

NuclearAntibodies(ANA)hasbeenseen;itsclinicalrelevanceisunclear.

4.9Overdose

AtopicaloverdoseofBetopticmaybeflushedfromtheeye(s)withlukewarmtapwater.

Treatmentofasuspectedoverdoseoraccidentalingestionissymptomaticandsupportive.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Ophthalmologicals:AntiglaucomaPreparation&Miotics.

ATCCode:SO1ED02

Betaxolol,acardioselective(beta-1-adrenergic)receptorblockingagent,doesnothavesignificantmembrane-

stabilizing(localanaesthetic)activityandisdevoidofintrinsicsympathomimeticaction.Orallyadministeredbeta-

adrenergicblockingagentsreducecardiacoutputinhealthysubjectsandpatientswithheartdisease.Inpatientswith

severeimpairmentofmyocardialfunction,beta-adrenergicreceptorantagonistsmayinhibitthesympathetic

stimulatoryeffectnecessarytomaintainadequatecardiacfunction.

BetaxololhasnosignificanteffectonpulmonaryfunctionasmeasuredbyForcedExpiratoryVolumeinonesecond

(FEV

).ForcedVitalcapacity(FVC),FEV

/FVCandnoevidenceofcardiovascularbeta-adrenergic-blockadeduring

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Wheninstilledintheeye,Betaxololhastheactionofreducingelevatedaswellasnormalintraocularpressure(IOP),

whetherornotaccompaniedbyglaucoma.OphthalmicBetaxololhaslittleornoeffectontheconstrictionofthepupil

minimaleffectonpulmonaryandcardiovascularparameters.

ElevatedIOPpresentsamajorriskfactoringlaucomatousfieldloss.ThehigherthelevelofIOP,thegreaterthe

likelihoodofopticnervedamageandvisualfieldloss.Betaxololhastheactionofreducingelevatedaswellasnormal

intraocularpressure,andthemechanismofocularhypotensiveactionappearstobeareductionofaqueoushumour

productionasdemonstratedbytonographyandaqueousfluorophotometry.

5.2Pharmacokineticproperties

Followingtopicaladministration,Betaxololisabsorbedsystemically.Plasmaconcentrationsofapproximately0.2

ng/mlweredetectedfollowingadministrationofBetopticSSuspension.(Holloetal.,IOVS,vol47,no1,pp235-240,

2006).

Betaxololishighlylipophilicwhichresultsingoodpermeationofthecornea,allowinghighintraocularlevelsofthe

drug.Betaxololischaracterisedbyitsgoodoralabsorption,lowfirstpasslossandarelativelylonghalf-lifeofapprox

16-22hours.Theeliminationofbetaxololisprimarilybytherenalratherthanfaecalroute.Themajormetabolic

pathwaysyieldtwocarboxylicacidformsplusunchangedbetaxololintheurine(approx.16%oftheadministered

dose).

5.3Preclinicalsafetydata

Reproduction,teratologyandperi-andpostnatalstudiesconductedwithorallyadministeredbetaxololHCIinratsand

rabbitsshowedevidenceofdrug-relatedpost-implantationlossinrabbitsandratsatdoselevelsabove12mg/kgand

128mg/kg,respectively.BetaxololHCIwasnotshowntobeteratogenic,however,therewerenootheradverseeffects

onreproductionatsubtoxicdoselevels.

Nootherpreclinicalfindingswereseenthatareofrelevancetotheprescriber.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Disodiumedetate

SodiumChloride

BenzalkoniumChloride

SodiumHydroxide(forpHadjustment)

Hydrochloricacid(forpHadjustment)

PurifiedWater

6.2Incompatibilities

Notapplicable.

6.3Shelflife

Theshelf-lifeexpirydateofthisproductisthedateshownonthebottleandoutercartonoftheproductonthemarket

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6.4Specialprecautionsforstorage

Donotstoreabove25 °

Keepintheoutercartoninordertoprotectfromlight.

Discardremainingcontents4weeksafterfirstopening

6.5Natureandcontentsofcontainer

Overlabelledbottlecontaining5mlofsolution

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements

7PARALLELPRODUCTAUTHORISATIONHOLDER

G&ALicensingLimited

Ballymurray

CoRoscommon

Ireland

8PARALLELPRODUCTAUTHORISATIONNUMBER

PPA1447/39/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:25thFebruary2011

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