BETOPTIC 0.5 %w/v Eye Drops Solution

Ireland - English - HPRA (Health Products Regulatory Authority)

Buy It Now

Active ingredient:
BETAXOLOL HYDROCHLORIDE
Available from:
G & A Licensing Limited
INN (International Name):
BETAXOLOL HYDROCHLORIDE
Dosage:
0.5 %w/v
Pharmaceutical form:
Eye Drops Solution
Prescription type:
Product subject to prescription which may be renewed (B)
Authorization status:
Withdrawn
Authorization number:
PPA1447/039/001
Authorization date:
2013-02-27

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

Whenusingnasolacrimalocclusionorclosingtheeyelidsfor2minutes,thesystemicabsorptionisreduced.Thismay

resultinadecreaseinsystemicsideeffectsandanincreaseinlocalactivity.

Adults(includingtheelderly)

Theusualdoseisonedroptobeinstilledintotheaffectedeye(s)twicedaily.

Children

Betopticisnotrecommendedforuseinchildren.

4.3Contraindications

Hypersensitivitytotheactivesubstance(substances),ortoanyoftheexcipients.

Reactiveairwaydiseaseincludingseverebronchialasthmaorahistoryofseverebronchialasthma,severechronic

obstructivepulmonarydisease.

Sinusbradycardia,sicksinussyndromesino-atrialblock,secondorthirddegreeatrioventricularblocknotcontrolled

withpace-maker.Overtcardiacfailure,cardiogenicshock.

4.4Specialwarningsandprecautionsforuse

LikeothertopicallyappliedophthalmicagentsBetaxololisabsorbedsystemically.Duetobetaadrenergiccomponent,

Betaxolol,thesametypesofcardiovascular,pulmonaryandotheradversereactionsseenwithsystemicbeta-adrenergic

blockingagentsmayoccur.IncidenceofsystemicADRsaftertopicalophthalmicadministrationislowerthanfor

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 16/05/2012 CRN 2113391 page number: 1

ContainsBenzalkoniumchloridewhichmaycauseeyeirritation.

Topicallyappliedbeta-blockerscanbesystemicallyresorbed.Consequently,thesameundesirableeffectscanappearas

withsystemicallyadministeredbeta-blockers.

Followingmeasuresare,afterapplicationoftheeyedropsusefultoreducesyatemicresorption:

Keeptheeyelidclosedfor2minutes.

Closethelacrimalductwiththefingerfor2minutes.

Opthalmicbetaxololhasbeenshowntohaveaminoreffectonheartrateandbloodpressureinclinicalstudies.Caution

shouldbeusedintreatingpatientswithahistoryofcardiacfailureorheartblock.TreatmentwithBetopticshouldbe

discontinuedatthefirstsignsofcardiacfailure.

Cardiacdisorders

Inpatientswithcardiovasculardiseases(e.g.coronaryheartdisease,Prinzmetal'sanginaandcardiacfailure)and

hypotensiontherapywithbeta-blockersshouldbecriticallyassessedandthetherapywithotheractivesubstances

shouldbeconsidered.Patientswithcardiovasculardiseasesshouldbewatchedforsignsofdeteriorationofthese

diseasesandofadversereactions.

Duetoitsnegativeeffectonconductiontime,beta-blockersshouldonlybegivenwithcautiontopatientswithfirst

degreeheartblock.

Vasculardisorders

Patientswithsevereperipheralcirculatorydisturbance/disorders(i.e.severeformsofRaynaud’sdiseaseorRaynaud’s

syndrome)shouldbetreatedwithcaution.

Respiratorydisorders

Respiratoryreactions,includingdeathduetobronchospasminpatientswithasthmahavebeenreportedfollowing

administrationofsomeophthalmicbeta-blockers.

Patientswithmild/moderatebronchialasthma,ahistoryofmild/moderatebronchialasthmaor,mild/moderatechronic

obstructivepulmonarydisease(COPD)shouldbetreatedwithcaution.

Hypoglycaemia/diabetes

Beta-blockersshouldbeadministeredwithcautioninpatientssubjecttospontaneoushypoglycaemiaortopatientswith

labilediabetes,asbeta-blockersmaymaskthesignsandsymptomsofacutehypoglycaemia.

Beta-blockersmayalsomaskthesignsofhyperthyroidism.

Cornealdiseases

Ophthalmic-blockersmayinducedrynessofeyes.Patientswithcornealdiseasesshouldbetreatedwithcaution.

Otherbeta-blockingagents

Theeffectonintra-ocularpressureortheknowneffectsofsystemicbeta-blockademaybepotentiatedwhenBetaxolol

isgiventothepatientsalreadyreceivingasystemicbeta-blockingagent.Theresponseofthesepatientsshouldbe

closelyobserved.Theuseof

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 16/05/2012 CRN 2113391 page number: 2

Anaphylacticreactions

Whiletakingbeta-blockers,patientswithhistoryofatopyorahistoryofsevereanaphylacticreactiontoavarietyof

allergensmaybemorereactivetorepeatedchallengewithsuchallergensandunresponsivetotheusualdoseof

adrenalineusedtotreatanaphylacticreactions.

Choroidaldetachment

Choroidaldetachmenthasbeenreportedwithadministrationofaqueoussuppressanttherapy(e.g.timolol,

acetazolamide)afterfiltrationprocedures.

Surgicalanaesthesia

-blockingophthalmologicalpreparationsmayblocksystemic-agonisteffectse.g.ofadrenaline.The

anaesthesiologistshouldbeinformedwhenthepatientisreceivingBetaxolol.

DiabetesMellitus

Beta-adrenergicblockingagentsshouldbeadministeredwithcautioninpatientssubjecttospontaneoushypoglycemia

ortodiabeticpatients(especiallythosewithlabilediabetes)whoarereceivinginsulinororalhypoglycemicagents.

Beta-adrenergicreceptorblockingagentsmaymaskthesignsandsymptomsofacutehypoglycemia.

Thyrotoxicosis

Beta-adrenergicblockingagentsmaymaskceratinclinicalsigns(e.g.,tachycardia)ofhypothyroidism.Patients

suspectedofdevelopingthyrotoxicosisshouldbemanagedcarefullytoavoidabruptwithdrawalofbeta-adrenergic

blockingagents,whichmightprecipitateathyroidstorm.

MajorSurgery

Considerationmaybegiventothegradualwithdrawalofbeta-adrenergicblockingagentspriortogeneralanestrhesia

becauseofthereducedabilitytothehearttorespondtobeta-adrenergicallymediatedsympatheticreflexstimuli.

Pulmonary

Betaxololisacardioselectivebeta-blocker,andtheophthalmicadministrationhasproducedonlyminimaleffectsin

patientswithobstructiveairwaysdisease.However,wheezing,bronchospasmanddyspnoeahaveoccurredinsome

patients.Althoughrechanllengesofsomepatientswithophthalmicbetaxololhasnotadverselyaffectedpulmonary

functiontestresults,thepossibilityofadversepulmonaryeffectsinpatientssensitivetobeta-blockerscannotberuled

out.CautionshouldbeexercisedIthetreatmentofpatientswithexcessiverestrictionofpulmonaryfunction.

Theriskofinducingbronchospasmmustbeappreciatedinpatientswithsymptomaticorpoorlycontrolledasthmaor

obstructiveairwaydiseases.Appropriateprecautions,includingconsiderationofalternativeglaucomatherapies,should

betaken.

Myastenia

Beta-adnrenergicblockadehasbeenreportedtopotentiatemuscleweaknessconsistentwithcertainmyasthenic

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

worsensymptomsassociatedwithmyastheniagravis.

Ocular

Inpatientswithangle-closureglaucoma,theimmediatetreatmentobjectiveistoreopentheanglebyconstrictionofthe

pupilwithamioticagent.Betaxololhasalittleornoeffectonthepupil.WhenBetopticisusedtoreduceelevated

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 16/05/2012 CRN 2113391 page number: 3

Limitedclinicalexperiencesuggeststhattheproductissuitablefortheuseinaphakicpatients.

Betopticshouldnotbeappliedwhilewearingcontactlenses;lensesshouldnotbeinsertedfor15minuteafter

instillationofproduct.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Eachinteractionthatisassociatedwithsystemicallyadministeredbetablockerscan,inprinciple,appearwiththeuseof

betablockereyedrops.

Patientswhoarereceivingabeta-adrenergicblockingagentorallyandBetopticshouldbeobservedforpotential

additiveeffecteitherontheintraocularpressureorontheknownsystemiceffectsofbetablockade.Orallyadministered

beta-adrenergicblockingagentsreducecardiacoutputinhealthysubjectsandpatientswithheartdisease.Inpatients

withsevereimpairmentofmyocardialfunction,beta-adrenergicreceptorantagonistmayinhibitthesymphatetic

stimulatoryeffectnecessarytomaintainadequatecardiacfunction.

NospecificdruginteractionstudieshavebeenperformedwithBetaxolol.

Thereisapotentialforadditiveeffectsresultinginhypertensionand/ormarkedbradycardiawhenopthalmicbeta-

blockersisadministeredconcomitantlywithoralcalciumchannelblockers,beta-adrenergicblockingagents,

antiarrhythmics(includingamiodarone),digitalisglycosides,parasympathomimetics,guanethidine.

Betaxololisanadrenergicblockingagent;therefore,cautionshouldbeexercisedinpatientsusingconcomitant

adrenergicpsychotropicdrugs.

AlthoughBetopticusedalonehaslittleornoeffectonpupilsize,Mydriasisresultingfromconcomitantuseof

ophthalmicbeta-blockersandadrenaline(epinephrine)hasbeenreportedoccasionally.

Ifsupplementaryeyepreparationsaretobeused,thepatientshouldwait15minutesbetweenthetwoapplications.

4.6Fertility,pregnancyandlactation

Pregnancy

TherearenoadequatedatafortheuseofBetaxololinpregnantwomen.Betaxololshouldnotbeusedduringpregnancy

unlessclearlynecessary.Toreducethesystemicabsorption,see4.2.

Epidemiologicalstudieshavenotrevealedmalformativeeffectsbutshowariskforintrauterinegrowthretardation

whenbeta-blockersareadministeredbytheoralroute.Inaddition,signsandsymptomsofbeta-blockade(e.g.

bradycardia,hypotension,respiratorydistressand

hypoglycaemia)havebeenobservedintheneonatewhenbeta-blockershavebeenadministereduntildelivery.If

Betopticisadministereduntildelivery,theneonateshouldbecarefullymonitoredduringthefirstdaysoflife.

Lactation

Beta-blockersareexcretedinbreastmilk.However,attherapeuticdosesofbetaxololineyedropsitisnotlikelythat

sufficientamountswouldbepresentinbreastmilktoproduceclinicalsymptomsofbeta-blockadeintheinfant.To

reducethesystemicabsorption,see4.2.

4.7Effectsonabilitytodriveandusemachines

TheinstillationofBetopticmaytemporarilyimpairvision.Ifblurredvisionoccursatinstallation,thepatientmustwait

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 16/05/2012 CRN 2113391 page number: 4

4.8Undesirableeffects

Likeothertopicallyappliedophthalmicdrugs,Betaxololisabsorbedintothesystemiccirculation.Thismaycause

similarundesirableeffectsasseenwithsystemicbeta-blockingagents.IncidenceofsystemicADRsaftertopical

ophthalmicadministrationislowerthanforsystemicadministration.Listedadversereactionsincludereactionsseen

withintheclassofophthalmicbeta-blockers.

Themostfrequentlyoccurringundesirableeffectsareeyediscomfort,irritationandhyperaemiafollowinginstillation.

SystemicreactionsfollowingtopicaladministrationofBetaxololhavebeenrarelyreported.

Thefollowingundesirableeffectshavebeenobserved:

Psychiatricdisorders

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

NervousSystemDisorders

Rare(>1/10,000to1/1000):Headache,insomnia

Eyedisorders

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

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

increased

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

Cardiacdisorders

Rare(>1/10000to1/1000):Bradycardia

Respiratory.Thoraricandmediastinaldisorders

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

SkinandSubcutaneousTissuedisorders

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

Musculosketalandconnectivetissuedisorders

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

Additionaladversereactionshavebeenseenwithophthalmicbeta-blockersandmaypotentiallyoccurwithBetoptic:

Immunesystemdisorders:

Systemicallergicreactionsincludingangioedema,urticaria,localizedandgeneralizedrash,pruritus,anaphylactic

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 16/05/2012 CRN 2113391 page number: 5

Metabolismandnutritiondisorders:

Hypoglycaemia.

Psychiatricdisorders:

Insomnia,depression,nightmares,memoryloss.

Nervoussystemdisorders:

Syncope,cerebrovascularaccident,cerebralischemia,increasesinsignsandsymptomsofmyastheniagravis,dizziness,

paraesthesia,andheadache.

Eyedisorders:

Signsandsymptomsofocularirritation(e.g.burning,stinging,itching,tearing,redness),blepharitis,keratitis,blurred

visionandchoroidaldetachmentfollowingfiltrationsurgery(see4.4Specialwarningsandspecialprecautionsforuse).

decreasedcornealsensitivity,dryeyes,cornealerosionptosis,diplopia.

Cardiacdisorders:

Bradycardia,chestpain,palpitations,oedema,arrhythmia,congestiveheartfailure,atrioventricularblock,cardiac

arrest,cardiacfailure.

Vasculardisorders:

Hypotension,Raynaud'sphenomenon,coldhandsandfeet.

Respiratory,thoracic,andmediastinaldisorders:

Bronchospasm(predominantlyinpatientswithpre-existingbronchospasticdisease),dyspnoea,cough.

Gastrointestinaldisorders:

Dysgeusia,nausea,dyspepsia,diarrhoea,drymouth,abdominalpain,vomiting.

Skinandsubcutaneoustissuedisorders:

Alopecia,psoriasiformrashorexacerbationofpsoriasis,skinrash.

Musculoskeletalandconnectivetissuedisorders:

Myalgia.

Reproductivesystemandbreastdisorders:

Sexualdysfunction,decreasedlibido.

Generaldisordersandadministrationsiteconditions:

Asthenia/fatigue.

Sincetopicallyappliedbeta-adrenergicblockingagentsmaybeabsorbedsystematically,adversereactionsfoundwith

systemicadministrationofbeta,-adrenergicblockingagentsmayoccurwithtopicaladministration(seesection4.4

Specialwarnings).

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 16/05/2012 CRN 2113391 page number: 6

failure,coldandcyanoticextremeties,Raynaudphenomenon,parasthesiaoftheextremities,increasedofanexisting

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

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

brochospasminpatientswithbronchialasthmaorahistoryofasthmaticcomplaints,disorderoftheskin,especially

rash,anddryeyes.Betablockersmaymaskthesymptomsofthyrotoxicosisorhypoglycemia.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

exercisewasobserved.

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

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 16/05/2012 CRN 2113391 page number: 7

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

inthecountryoforigin.

6.4Specialprecautionsforstorage

Donotstoreabove25 °

Keepintheoutercartoninordertoprotectfromlight.

Discardremainingcontents4weeksafterfirstopening

6.5Natureandcontentsofcontainer

Overlabelledbottlecontaining5mlofsolution

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements

7PARALLELPRODUCTAUTHORISATIONHOLDER

G&ALicensingLimited

Ballymurray

CoRoscommon

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 16/05/2012 CRN 2113391 page number: 8

8PARALLELPRODUCTAUTHORISATIONNUMBER

PPA1447/39/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:25thFebruary2011

10DATEOFREVISIONOFTHETEXT

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 16/05/2012 CRN 2113391 page number: 9

Similar products

Search alerts related to this product

View documents history

Share this information