Cosopt

New Zealand - English - Medsafe (Medicines Safety Authority)

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Active ingredient:
Dorzolamide hydrochloride 22.26 mg/mL equivalent to 20 mg/mL Dorzolamide free base; Timolol maleate 6.83 mg/mL equivalent to 5 mg/mL Timolol free base
Available from:
Mundipharma New Zealand Ltd
INN (International Name):
Dorzolamide hydrochloride 22.26 mg/mL (equivalent to 20 mg/mL Dorzolamide free base)
Dosage:
20mg/mL, 5mg/mL
Pharmaceutical form:
Eye drops, solution
Composition:
Active: Dorzolamide hydrochloride 22.26 mg/mL equivalent to 20 mg/mL Dorzolamide free base Timolol maleate 6.83 mg/mL equivalent to 5 mg/mL Timolol free base Excipient: Benzalkonium chloride Hyetellose Mannitol Sodium citrate Sodium hydroxide Water for injection
Units in package:
Bottle, plastic, 'professional sample pack', 5 mL
Class:
Prescription
Prescription type:
Prescription
Manufactured by:
F.I.S. Fabbrica Italiana Sintetici SpA
Therapeutic indications:
COSOPT is indicated for the treatment of elevated intraocular pressure (IOP) in patients with: · ocular hypertension · open-angle glaucoma · pseudoexfoliative glaucoma · or other secondary open-angle glaucoma's and who are: · insufficiently responsive to topical beta blocker monotherapy · currently receiving concomitant antiglaucoma therapies such as dorzolamide HCl and timolol maleate
Product summary:
Package - Contents - Shelf Life: Bottle, plastic, 'professional sample pack' - 5 mL - 24 months from date of manufacture stored at or below 30°C protect from light - Bottle, plastic, Occumeter Plus - 5 mL - 24 months from date of manufacture stored at or below 30°C protect from light
Authorization number:
TT50-6009
Authorization date:
1997-07-04

NameofMedicine

COSOPT ®

dorzolamide hydrochloride and timololmaleate

20mg/5mgophthalmicsolution

Presentation

Aclear,colourlessto nearlycolourless,slightlyviscoussolutionavailable ina translucent

plasticdispensingbottle (Occumeter)with a yellowcap. EachmL contains20mgof

dorzolamide (22.26mgdorzolamideHCl)and5 mgoftimolol(6.83mgoftimololmaleate).

TherapeuticClass

COSOPTOphthalmicSolution (dorzolamidehydrochloride and timololmaleate,MSD)is

the firstcombination ofatopicalcarbonicanhydrase inhibitoranda topicalbeta-adrenergic

receptorblockingagent.

Indications

COSOPTisindicatedforthetreatmentofelevated intraocularpressure (IOP)inpatients

with:

ocularhypertension

open-angle glaucoma

pseudoexfoliative glaucoma

orothersecondaryopen-angle glaucoma’s

and who are:

insufficientlyresponsive totopicalbeta blockermonotherapy

currentlyreceivingconcomitantantiglaucomatherapiessuch asdorzolamide HCIand

timolol maleate

DosageandAdministration

The dose isonedropofCOSOPTin the affected eye(s)two timesdaily.When

substitutingCOSOPTforanotherophthalmicantiglaucoma agent(s),discontinue theother

agent(s)afterproperdosingon oneday,andstartCOSOPTonthenextday.

If anothertopicalophthalmicagentisbeingused,COSOPTandtheotheragentshould be

administeredatleasttenminutesapart.

Safetyand efficacyinpaediatricpatientsbelowthe age of2 yearshave notbeen

established.(Forinformation regardingusein paediatricpatients≥2yearsofagesee

Warningsand Precautions,PaediatricUse).

Contraindications

COSOPTiscontraindicatedin patientswith:

reactive airwaydisease,bronchialasthma orotherobstructivelungdisordersora

historyofbronchospasm

uncontrolled heartfailure(seeWarningsand Precautions)

cardiogenicshock

sick sinus syndrome

grade 2 and3 AVblockandinfranodalAVblock

severe bradycardia

hypersensitivityto anycomponentofthisproduct

sino-atrialblock

The above arebasedon the componentsandare notunique tothecombination.

WarningsandPrecautions

Aswith othertopically-appliedophthalmicagents,thismedicine maybeabsorbed

systemically.Thetimololcomponentisabeta-blocker.Therefore,the sametypesof

adverse reactionsfound with systemicadministrationofbeta-blockersmayoccurwith

topicaladministration.

Cardio-respiratoryReactions

Because ofthe timololmaleate component,cardiacfailureshouldbe adequatelycontrolled

beforebeginningtherapywith COSOPT.Patientswitha historyofcardiovasculardisease,

includingcardiacfailure should be watchedforsignsofdeterioration ofthese diseasesand

pulse ratesshouldbechecked.

Due to itsnegative effecton conduction time,beta-blockersshould be givenwith caution

topatientswith firstdegree heartblock.

Respiratoryreactionsandcardiacreactions,includingdeath due tobronchospasmin

patientswith asthmaand rarelydeath inassociation with cardiacfailure,have been

reported followingadministration oftimololmaleate ophthalmicsolution.

In patientswith mild/moderate chronicobstructive pulmonarydisease (COPD),COSOPT

shouldbeused with caution,and onlyifthe potentialbenefitoutweighsthe potentialrisk.

VascularDisorders

Patientswith severeperipheralcirculatorydisturbance/disorders(e.g.severe formsof

Raynaud’sdiseaseorRaynaud’ssyndrome)shouldbetreated withcaution.

RenalandHepatic Impairment

COSOPThasnotbeen studied inpatientswith severe renalimpairment(CrCl<30

millilitre/min).Because dorzolamide hydrochloride and itsmetabolite areexcreted

predominantlybythe kidney,COSOPTisnotrecommended in suchpatients.

COSOPThasnotbeen studied inpatientswith hepaticimpairmentandtherefore should

be used with caution insuch patients.

Immunologyand Hypersensitivity

Aswith othertopically-appliedophthalmicagents,thismedicine maybeabsorbed

systemically.Thedorzolamide componentisa sulphonamide.Therefore,thesame types

ofadverse reactionsfound with systemicadministration ofsulphonamidesmayoccurwith

topicaladministration,such asStevens-Johnson syndrome andtoxicepidermalnecrolysis.

Ifsignsofseriousreactionsorhypersensitivityoccur,discontinueuse ofthispreparation.

In clinicalstudies,localocularadverse effects,primarilyconjunctivitisandlid reactions,

were reported with chronicadministrationofdorzolamidehydrochloride ophthalmic

solution.Some ofthese reactionshadtheclinicalappearanceandcourse ofan allergic-

type reactionthatresolved upondiscontinuation ofmedicine therapy.Similarreactions

have been reported with COSOPT.Ifsuchreactionsare observed,discontinuation of

treatmentwith COSOPTshouldbeconsidered.

While takingβ-blockers,patientswith ahistoryofatopyorahistoryofsevere anaphylactic

reactiontoa varietyofallergensmaybemorereactive to accidental,diagnostic,or

therapeuticrepeated challenge with suchallergens.Suchpatientsmaybe unresponsive

totheusualdosesofepinephrine used to treatanaphylacticreactions.

ConcomitantTherapy

There isapotentialforan additive effecton the known systemiceffectsofcarbonic

anhydrase inhibitioninpatientsreceivingoralandtopicalcarbonicanhydrase inhibitors

concomitantly.The concomitantadministration ofCOSOPTand oralcarbonicanhydrase

inhibitorshasnotbeenstudied and isnotrecommended.

Patientswho arealreadyreceivinga beta-adrenergicblockingagentsystemicallyand who

are given COSOPTshouldbe observedforapotentialadditive effecteitheron the

intraocularpressureoron the known systemiceffectsofbeta-blockade.The use oftwo

topicalbeta-adrenergicblockingagentsisnotrecommended.

Other

The managementofpatientswithacute angle-closure glaucoma requirestherapeutic

interventionsinaddition toocularhypotensive agents.COSOPThasnotbeenstudied in

patientswith acute angle-closure glaucoma.

Choroidaldetachmenthasbeenreported withadministration ofaqueoussuppressant

therapy(e.g.,timolol,acetazolamide,dorzolamide)afterfiltration procedures.

There isan increasedpotentialfordevelopingcornealoedemain patientswith low

endothelialcellcounts. Precautionsshould be used when prescribingCOSOPTtothis

groupofpatients.

There have been reportsofbacterialkeratitisassociated with theuse ofmultidose

containersoftopicalophthalmicproducts.Thesecontainershave beeninadvertently

contaminated bypatientswho,inmostcases,hada concurrentcornealdiseaseora

disruptionoftheocularepithelialsurface.

Patientsshouldbe instructed to avoidallowingthe tipofthedispensingcontainerto

contactthe eye orsurroundingstructures.

Patientshouldalsobeinstructedthatocularsolutions,ifhandled improperly,can become

contaminated bycommonbacteria known tocauseocularinfection.Seriousdamage to

theeye andsubsequentlossofvision mayresultfromusingcontaminated solutions.

Patientsshouldbeadvised thatiftheydevelop anintercurrentocularcondition (eg.

trauma,ocularsurgeryorinfection),theyshould immediatelyseektheirphysician’sadvice

concerningthe continued use ofthe presentmultidose container.

ContactLens Use

COSOPTcontainsthepreservative benzalkoniumchloride,which maybe deposited in soft

contactlenses;therefore,COSOPTshould notbe administered while wearingthese

lenses.The lensesshouldbe removedbefore applicationofthedropsand notbe

reinsertedearlierthan15minutesafteruse.

Pregnancy

There arenoadequateandwell-controlled studiesinpregnantwomen.COSOPTshould

be usedduringpregnancyonlyifthe potentialbenefitjustifiesthe potentialrisktothe

foetus.

Nursing Mothers

Itisnotknown whetherdorzolamidehydrochloride isexcreted in humanmilk.Timolol

maleate doesappearinhumanmilk.Because ofthepotentialforseriousadverse

reactionsonthenursinginfant,a decision should be made whetherto discontinue nursing

ordiscontinuethe medicine,takinginto accountthe importanceofthe medicinetothe

mother.

PaediatricUse

The safetyandefficacyof2%dorzolamidehydrochloride ophthalmicsolution hasbeen

established ina clinicalstudyofchildrenunderthe ageof6 years. In thisstudypatients

under6 and greaterthan 2yearsofage whose IOPwasnotcontrolled with monotherapy

received COSOPT.InthosepatientsCOSOPTwasgenerallywelltolerated.

Dorzolamide hasnotbeen studied inpatientslessthan36 weeksgestationalage and less

than1 weekofage.Patientswith significantrenaltubularimmaturityshouldonlyreceive

dorzolamideaftercarefulconsideration oftheriskbenefitbalancebecauseofthepossible

riskofmetabolicacidosis

Effects ontheAbilitytoUse andDrive Machines

There areadverse effectsassociatedwith COSOPTthatmayaffectsomepatients’ ability

to drive and/oroperatemachinery. (SeeAdverse Effects.)

Systemic Effects ofBeta-AdrenergicBlockingAgents

CardiacFailure

Sympatheticstimulation maybe essentialforsupportofthecirculation in individualswith

diminished myocardialcontractility,anditsinhibition bybeta-adrenergicreceptorblockade

mayprecipitatemore severe failure.

In patientswithoutahistoryofcardiacfailurecontinueddepressionofthemyocardiumwith

beta-blockingagentsovera period oftime can,in somecases,leadto cardiacfailure. At

thefirstsign orsymptomofcardiacfailure COSOPTshouldbediscontinued.

SurgicalAnesthesia

The necessityordesirabilityofwithdrawalofbeta-adrenergicblockingagentspriorto

majorsurgeryiscontroversial. Ifnecessaryduringsurgery,the effectsofbeta-adrenergic

blockingagentsmaybe reversed bysufficientdosesofsuchagonistsasisoproterenol,

dopamine,dobutamineorlevarterenol.

MaskingofHypoglycemicSymptomsin Patientswith DiabetesMellitus

Beta-adrenergicblockingagentsshouldbeadministered with caution in patientssubjectto

spontaneoushypoglycaemia orto diabeticpatients(especiallythosewith labile diabetes)

who are receivinginsulin ororalhypoglycaemicagents.Beta-adrenergicreceptorblocking

agentsmaymaskthesignsand symptomsofacute hypoglycaemia.

Maskingof Thyrotoxicosis

Beta-adrenergicblockingagentsmaymaskcertain clinicalsignsofhyperthyroidism(e.g.

tachycardia). Patientssuspectedofdevelopingthyrotoxicosisshouldbe managed

carefullyto avoid abruptwithdrawalofbeta-adrenergicblockingagentswhich might

precipitate athyroid storm.

MuscleWeakness

Beta-adrenergicblockadehasbeen reportedto increasemuscleweaknessconsistentwith

certain myasthenicsymptoms(e.g.diplopia,ptosis,andgeneralised weakness).Timolol

hasbeenreported rarelyto increasemuscleweaknessin somepatientswith myasthenic

symptoms.

General

Because ofpotentialeffectsofbeta-adrenergicblockingagentsrelative to blood pressure

andpulse,theseagentsshould beused with caution in patientswith cerebrovascular

insufficiency. Ifsignsorsymptomssuggestingreduced cerebralbloodflowdevelop

followinginitiation oftherapywith COSOPT,alternative therapyshould be considered.

Patientswith bronchialasthma,ahistoryofbronchialasthma,severe chronicobstructive

pulmonarydisease,sinusbradycardia,second orthirddegreeatrioventricularblock,or

cardiacfailureshouldbe advised nottotakethisproduct(see Contraindications).

AnimalToxicology

Preclinicalsafetydata

The ocularand systemicsafetyprofileofthe individualcomponentsiswellestablished.

Furthermore,noadverse oculareffectswere seen in animalstreated topicallywith

dorzolamidehydrochloride and timololmaleate ophthalmicsolutionorwith concomitantly-

administereddorzolamide hydrochlorideand timololmaleate.Therefore,no significantrisk

forhuman safetyisexpected with therapeuticdosesofCOSOPT.

AdverseEffects

Inclinical studies,COSOPTwasgenerallywelltolerated;noadverse experiencespeculiar

to thiscombinationmedicine have been observed.Adverse experienceshave been

limited to thosethatwere reported previouslywith dorzolamide hydrochlorideand/or

timolol maleate.In general,common adverse experienceswere mild and didnotcause

discontinuation.

Duringclinicalstudies,1035 patientswere treatedwith COSOPT.Approximately2.4%of

allpatientsdiscontinued therapywith COSOPTbecauseoflocalocularadverse reactions,

approximately1.2%ofallpatientsdiscontinued becauseoflocaladverse reactions

suggestive ofallergyorhypersensitivity.

The mostfrequentlyreportedmedicine-related adverse effectswere:ocularburningand

stinging,tasteperversion,cornealerosion,conjunctivalinjection,blurred vision,tearing

andocularitching. Urolithiasiswasreportedrarely.

Thefollowingadverse reactionshave beenreportedin post-marketingexperience:

dyspnoea,respiratoryfailure,contactdermatitis,bradycardia,heartblock,choroidal

detachmentfollowingfiltration surgery,nausea,Stevens-Johnson syndrome,andtoxic

epidermalnecrolysis.

Additionaladverse effectsthathave been seen with oneofthe componentsandmaybe

potentialadverse effectsofCOSOPTare:

DorzolamideHydrochloride

Headache;eyelid inflammation;nausea;eyelid irritation;eyelid crusting;asthenia/fatigue;

iridocyclitis;rash;dizziness;paresthesia,transientmyopia (which resolved upon

discontinuation oftherapy);localreaction includingpalpebralreactionsand signsand

symptomsofsystemicallergicreactionsincludingangioedema,bronchospasm,urticaria

and pruritus,epistaxis,contactdermatitis,throatirritation,drymouth.

PaediatricPatients

In a clinicaltrialwith 184 paediatricpatientsthe adverse eventprofile ofdorzolamide

hydrochloride wascomparabletothatseen inadultpatients.Inthistrialapproximately

20%ofpatientshadamedicine-related adverse event,themajorityofwhich were local,

non seriousoculareffectssuchasburningstinging,injection andeye pain.Asmall

percentage ofpatientsin thistrial(<4%)were observed tohave cornealoedemaorhaze.

Localreactionsappeared similarinfrequencyto the comparator.

In postmarketingdata,metabolicacidosisinthe veryyoungchildrenparticularlywith renal

immaturity/impairmenthasbeen rarelyreported.

TimololMaleate(topicalformulation)

Signsand symptomsofocularirritation,includingconjunctivitis,blepharitis,keratitis,and

decreased cornealsensitivity,dryeyes;visualdisturbances,includingrefractive changes

(due to withdrawalofmiotictherapyin somecases),diplopia,andptosis;tinnitus;

arrhythmia;hypotension;syncope; cerebrovascularaccident;cerebralischaemia;

congestive heartfailure;palpitation;cardiacarrest;oedema,claudication,Raynaud’s

phenomenon,coldhandsandfeet;bronchospasm(predominantlyin patientswith pre-

existingbronchospasticdisease);cough;headache;asthenia;fatigue;chestpain;

alopecia,psoriasiformrash orexacerbationofpsoriasis;signsand symptomsofallergic

reactionsincludinganaphylaxis,angioedema,urticaria,localised andgeneralised rash;

dizziness;depression,insomnia,nightmares,memoryloss;increasein signsand

symptomsofmyasthenia gravis,paresthesia;nausea,diarrhoea,dyspepsia,drymouth;

decreased libido,Peyronie’sdisease;systemiclupuserythematosus.

LaboratoryFindings

COSOPTwasnotassociated with clinicallymeaningfulelectrolyte disturbancesinclinical

studies.

Interactions

Specificmedicine interaction studieshave notbeen performed withCOSOPT.

In clinicalstudies,COSOPTwasusedconcomitantlywith thefollowingsystemic

medicationswithoutevidenceofadverse interactions:ACE-inhibitors,calciumchannel

blockers,diuretics,non-steroidalanti-inflammatorymedicinesincludingaspirin,and

hormones(e.g.,oestrogen,insulin,thyroxine).

However,the potentialexistsforadditive effectsand production ofhypotensionand/or

marked bradycardia whentimololmaleate ophthalmicsolution isadministered together

with oralcalciumchannelblockers,catecholamine-depletingmedicines,antiarrhythmics,

parasympathomimeticsorbeta-adrenergicblockingagents.

Potentiatedsystemicbeta-blockade(e.g.,decreasedheartrate,depression) hasbeen

reported duringcombinedtreatmentwithCYP2D6 inhibitors(e.g.quinidine,SSRIs)and

timolol.

The dorzolamide componentofCOSOPTisacarbonicanhydrase inhibitorandalthough

administeredtopically,isabsorbed systemically.Inclinical studies,dorzolamide

hydrochloride ophthalmicsolution wasnotassociated with acid-base disturbances.

However,thesedisturbanceshave been reported with oralcarbonicanhydrase inhibitors

andhave in some instances,resulted inmedicine interactions(e.g.,toxicityassociated

withhigh-dose salicylate therapy).Therefore,the potentialforsuch medicineinteractions

shouldbe considered in patientsreceivingCOSOPT.

Oralβ-adrenergicblockingagentsmayexacerbate the reboundhypertension which can

followthe withdrawalofclonidine.Ifthe twomedicinesareco-administered,theβ-

adrenergicblockingagentshouldbewithdrawn severaldaysbefore the gradualwithdrawal

ofclonidine.Ifreplacingclonidine byβ-blockertherapy,the introduction ofβ-adrenergic

blockingagentsshouldbedelayedforseveraldaysafterclonidine hasstopped.

Overdosage

No data areavailablewith regard to human overdosage byaccidentalordeliberate

ingestionof COSOPT.

There have been reportsofinadvertentoverdosage with timololmaleateophthalmic

solutionresultingin systemiceffectssimilarto those seenwith systemicbeta-adrenergic

blockingagentssuchasdizziness,headache,shortnessofbreath,bradycardia,

bronchospasm,and cardiacarrest.Themostcommon signsand symptomsto be

expected with overdosage ofdorzolamideareelectrolyte imbalance,developmentofan

acidoticstate,and possiblycentralnervoussystemeffects.

Treatmentshould be symptomaticand supportive.Serumelectrolyte levels(particularly

potassium)andbloodpHlevelsshouldbemonitored.Studieshaveshown thattimolol

doesnotdialyse readily.

Actions

COSOPTiscomprisedoftwo components:dorzolamide hydrochloride andtimolol

maleate. Eachofthese two componentsdecreaseselevated intraocularpressureby

reducingaqueoushumorsecretion,butdoesso bya differentmechanismofaction.

Dorzolamide hydrochloride isa potentinhibitorofhuman carbonicanhydrase II.Inhibition

ofcarbonicanhydrasein theciliaryprocessesoftheeye decreasesaqueoushumor

secretion,presumablybyslowingtheformation ofbicarbonate ionswith subsequent

reduction in sodiumandfluidtransport.Timololmaleate isanon-selective beta-adrenergic

receptorblockingagentthatdoesnothave significantintrinsicsympathomimetic,direct

myocardialdepressant,orlocalanaesthetic(membrane-stabilising)activity. The

combinedeffectofthese two agentsresultsin additionalintraocularpressure reduction

comparedtoeithercomponentadministeredalone.

Followingtopicaladministration,COSOPTreduceselevated intraocularpressure,whether

ornotassociatedwith glaucoma. Elevated intraocularpressure isamajorriskfactorinthe

pathogenesisofopticnerve damage and glaucomatousvisualfieldloss.Thehigherthe

levelofintraocularpressure,the greaterthelikelihoodofglaucomatousvisualfield loss

andopticnerve damage. COSOPTreducesintraocularpressurewithoutthe common

adverse effectsofmioticssuch asnightblindness,accommodative spasmand pupillary

constriction.

Pharmacokinetics

DorzolamideHydrochloride

Unlike oralcarbonicanhydrase inhibitors,topicaladministration ofdorzolamide

hydrochloride allowsforthemedicine to exertitseffectsdirectlyin the eye atsubstantially

lowerdosesandtherefore with lesssystemicexposure. In clinicaltrials,thisresultedin a

reduction in IOPwithoutthe acid-basedisturbancesoralterationsin electrolytes

characteristicoforalcarbonicanhydrase inhibitors.

Whentopicallyapplied,dorzolamide reachesthesystemic circulation.Toassessthe

potentialforsystemiccarbonicanhydrase inhibitionfollowingtopicaladministration,

medicine andmetabolite concentrationsin RBCsandplasmaand carbonicanhydrase

inhibition in RBCswere measured.DorzolamideaccumulatesinRBCsduringchronic

dosingasaresultofselective bindingto CA-IIwhile extremelylowconcentrationsoffree

medicinein plasma aremaintained.Theparentmedicine formsasingleN-desethyl

metabolite thatinhibitsCA-II lesspotentlythan the parentmedicinebutalso inhibitsa less

active isoenzyme (CA-I). Themetabolitealsoaccumulatesin RBCswhere itbinds

primarilytoCA-I. Dorzolamide bindsmoderatelyto plasma proteins(approximately33%).

Dorzolamide isprimarilyexcreted unchangedin theurine;the metabolite isalsoexcreted

in urine.Afterdosingends,dorzolamide washesoutofRBCsnonlinearly,resultingin a

rapid declineofmedicine concentration initially,followed bya slowereliminationphase

with a half-lifeofaboutfourmonths.

Whendorzolamide wasgiven orallyto simulate themaximumsystemicexposureafterlong

termtopicalocularadministration,steadystate wasreached within13 weeks. Atsteady

state,there wasvirtuallyno freemedicine ormetabolite inplasma;CAinhibitioninRBCs

waslessthanthatanticipated tobenecessaryforapharmacologicaleffectonrenal

function orrespiration.Similarpharmacokineticresultswere observed afterchronic,

topicaladministrationofdorzolamidehydrochloride.However,someelderlypatientswith

renalimpairment(estimated CrCl30-60millilitre/min)hadhighermetabolite concentrations

in RBCs,butnomeaningfuldifferencesin carbonicanhydrase inhibition and no clinically

significantsystemicadverse effectswere directlyattributabletothisfinding.

Timolol Maleate

In a studyofplasmamedicine concentration in sixsubjects,the systemicexposure to

timololwasdeterminedfollowingtwice dailytopicaladministrationoftimololmaleate

ophthalmicsolution 0.5%.Themeanpeakplasmaconcentrationfollowingmorningdosing

was0.46ng/mLandfollowingafternoon dosingwas0.35ng/mL.

PharmaceuticalPrecautions

Storage

StoreCOSOPTat 15-30°C(59-86°F).Protectfromlight.

MedicineClassification

PrescriptionMedicine

Package Quantities

COSOPTisavailable in bottlescontaining5mLofsolution.

FurtherInformation

Chemistry

COSOPTcontainsdorzolamide hydrochloride and timololmaleate.

Dorzolamide Hydrochloride

Dorzolamide hydrochloride isdescribed chemicallyas:(4S-trans)-4-(ethylamino)-5,6-

dihydro-6-methyl-4 H-thieno[2,3-b]thiopyran-2-sulphonamide 7,7-dioxide

monohydrochloride.

Itsempirical formulaisC

HCland itsstructuralformulais:

Dorzolamide hydrochloride hasamolecularweightof360.91.Itisawhitetooff-white, free

flowingcrystalline powder,which issolubleinwaterand slightlysoluble inmethanoland

ethanol.

Timolol Maleate

Timololmaleate isdescribed chemicallyas:(S)-1-[(1,1-dimethylethyl)amino]-3-[[4-(4-

morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol,(Z)-2-butenedioate (1:1)(salt).Timolol

maleatepossessesanasymmetriccarbonatomin the structureand isprovided asthe

levoisomer.The empiricalformula isC

SC

and the structuralformula is:

Timololmaleatehasamolecularweightof432.50.Itisa white,odourless,crystalline

powderwhich issoluble in water,methanol,and alcohol.

Composition

Active Ingredients

COSOPTissuppliedasa sterile,isotonic,buffered,slightlyviscous,aqueoussolution.

EachmillilitreofCOSOPTcontains20.00mgdorzolamide (22.26mgofdorzolamide

hydrochloride)and 5.00 mgtimolol(6.83mgoftimololmaleate)asthe active ingredients.

Inactive Ingredients

COSOPTcontainsthefollowinginactive ingredients:sodiumcitrate,hydroxyethylcellulose,

sodiumhydroxide,mannitol,andwaterforinjection. Benzalkoniumchloride (0.0075%)is

added aspreservative.

NameandAddress

MerckSharp&Dohme(NewZealand)Limited

POBox99851

Newmarket

Auckland

NEWZEALAND

Tel.0800500673

Date ofPreparation

5 November2012

DP-CST-1209(211209)

Registered TrademarkofMerckSharp&DohmeCorp.,asubsidiaryofMerck&Co.,Inc.,Whitehouse

Station, NJ, USA

Copyright©2009MerckSharp &Dohme Corp.,asubsidiaryofMerck&Co.,Inc.,Whitehouse Station,NJ,

USA.Allrightsreserved.

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