Claramax

New Zealand - English - Medsafe (Medicines Safety Authority)

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Active ingredient:
Desloratadine 5 mg
Available from:
Bayer New Zealand Limited
INN (International Name):
Desloratadine 5 mg
Dosage:
5 mg
Pharmaceutical form:
Film coated tablet
Composition:
Active: Desloratadine 5 mg Excipient: Calcium hydrogen phosphate dihydrate Carnauba wax Maize starch Opadry blue 32B10817 Opadry Clear YS-1-19025-A Powdered cellulose Purified talc White beeswax
Units in package:
Blister pack, Aclar/PVC-Al; 3 tablet sample, 3 tablets
Class:
Pharmacy only
Prescription type:
Pharmacy only
Manufactured by:
Schering-Plough Company
Product summary:
Package - Contents - Shelf Life: Blister pack, Aclar/PVC-Al; 3 tablet sample - 3 tablets - 24 months from date of manufacture stored at or below 25°C - Blister pack, Aclar/PVC-Al; 7 tablet pack - 7 tablets - 24 months from date of manufacture stored at or below 25°C - Blister pack, Aclar/PVC-Al; 28 tablet pack - 28 tablets - 24 months from date of manufacture stored at or below 25°C
Authorization number:
TT50-6483
Authorization date:
1999-11-24

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Claramax

Desloratadinetabletsandsyrup

NAMEOFMEDICINE

CLARAMAX(desloratadine5mg)Tablets

CLARAMAX(desloratadine0.5mg/mL)Syrup

DESCRIPTION

CLARAMAXtabletscontaindesloratadine5mgandthefollowinginactiveingredients:

Core:calciumhydrogenphosphate,microcrystallinecellulose,maizestarchandtalc

Coating:OpadryBlue,OpadryClear,carnaubawaxandwhitebeeswax

CLARAMAXSyrupcontainsdesloratadine0.5mg/mLandthefollowinginactiveingredients:

Propyleneglycol,sorbitol,anhydrouscitricacid,sodiumcitrate,disodiumedetate,sucrose,bubblegum

flavour,colourE110,waterandsodiumbenzoateaspreservative.

USES

Actions

Desloratadineisanon-sedatinglong-actinghistamineantagonistwithpotent,selectiveperipheralH

receptorantagonistactivity.Desloratadinehasdemonstratedantiallergic,antihistaminicandanti-

inflammatoryactivities.

Pharmacodynamics

Afteroraladministration,desloratadineselectivelyblocksperipheralhistamineH

-receptorsbecausethe

drugiseffectivelyexcludedfromentrytothecentralnervoussystem.

Inadditiontoantihistaminicactivity,desloratadinehasdemonstratedantiallergicandanti-inflammatory

Inadditiontoantihistaminicactivity,desloratadinehasdemonstratedantiallergicandanti-inflammatory

activitiesfromnumerousinvitro(mainlyconductedoncellsofhumanorigin)andinvivostudies.These

studieshaveshownthatdesloratadineinhibitsthebroadcascadeofeventsthatinitiateandpropagate

allergicinflammationincluding:

ThereleaseofproinflammatorycytokinesincludingIL-4,IL-6,IL-8,IL-13,

ThereleaseofimportantproinflammatorychemokinessuchasRANTES(Regulatedupon

Activation,NormalT-cellExpressedandSecreted),

Superoxideanionproductionbyactivatedpolymorphonuclearneutrophils,

Eosinophiladhesionandchemotaxis,

TheexpressionoftheadhesionmoleculessuchasP-selectin,

IgE-dependentreleaseofhistamine,prostaglandin(PGD2),andleukotriene(LTC4),

Theacuteallergicbronchoconstrictorresponseandallergiccoughinanimalmodels.

Inamultipledoseclinicaltrial,inwhichupto20mgofdesloratadinewasadministereddailyfor14

days,nostatisticallyorclinicallyrelevantcardiovasculareffectwasobserved.Inaclinical

pharmacologicaltrial,inwhichdesloratadinewasadministeredatadoseof45mgdaily(ninetimesthe

clinicaldose)fortendays,noprolongationoftheQTcintervalwasseen.

Desloratadinedoesnotreadilypenetratethecentralnervoussystem.Attherecommendeddoseof5mg

daily,therewasnoexcessincidenceofsomnolenceascomparedtoplacebo.CLARAMAXatadoseof

7.5mgdailydidnotaffectpsychomotorperformanceinclinicaltrials.

Noclinicallyrelevantchangesindesloratadineplasmaconcentrationswereobservedinmultiple-dose

azithromycin,fluoxetine,cimetidine,ketoconazoleanderythromycininteractiontrials.

Inclinicalpharmacologicaltrials,co-administrationofalcoholdidnotincreasethealcohol-induced

impairmentinperformanceorincreaseinsleepiness.Nosignificantdifferenceswerefoundinthe

psychomotortestresultsbetweendesloratadineandplacebogroups,whetheradministeredaloneorwith

alcohol.

Asingledoseofdesloratadine5mgdidnotaffectstandardmeasuresofflightperformanceincluding

exacerbationofsubjectivesleepinessortasksrelatedtoflying.

Assessmentsofqualityoflifeintheclinicaltrialsindicatedthatseasonalallergicrhinitisproduceda

consistentburdenofdisease,andthatimprovementsintherapeuticresponseswereassociatedwith

improvementsinvariousqualityoflifedomainsincludingvitalityandsocialfunctioning.

Inadditiontotheestablishedclassificationsofseasonalandperennial,allergicrhinitiscanalternatively

beclassifiedasintermittentandpersistentallergicrhinitisaccordingtothedurationofsymptoms.

Intermittentallergicrhinitisisdefinedasthepresenceofsymptomsforlessthan4daysperweekorfor

lessthan4weeks.Persistentallergicrhinitisisdefinedasthepresenceofsymptomsfor4daysormore

perweekandformorethan4weeks.

PreclinicalSafety

Desloratadineistheprimaryactivemetaboliteofloratadine.Preclinicalstudiesconductedwith

desloratadineandloratadinedemonstratedthattherearenoqualitativeorquantitativedifferencesinthe

toxicityprofileofdesloratadineandloratadineatcomparablelevelsofexposuretodesloratadine.

Pharmacokinetics

Pharmacokinetics

Desloratadineplasmaconcentrationscanbedetectedwithin30minutesofdesloratadineadministration.

Desloratadineiswellabsorbedwithmaximumconcentrationachievedafterapproximately3hours;the

terminalphasehalf-lifeisapproximately27hours.Thedegreeofaccumulationofdesloratadinewas

consistentwithitshalf-life(approximately27hours)andaoncedailydosingfrequency.The

bioavailabilityofdesloratadinewasdoseproportionalovertherangeof5mgto20mg.

Theenzymeresponsibleforthemetabolismofdesloratadinehasnotbeenidentifiedyet,andtherefore

someinteractionswithotherdrugscannotbefullyexcluded.In-vivostudieswithspecificinhibitorsof

CYP3A4andCYP2D6haveshownthattheseenzymesarenotimportantinthemetabolismof

desloratadine.DesloratadinedoesnotinhibitCYP3A4orCYP2D6andisneitherasubstratenoran

inhibitorofP-glycoprotein.

Desloratadineismoderatelybound(83%-87%)toplasmaproteins.Thereisnoevidenceofclinically

relevantdrugaccumulationfollowingoncedailydosingofdesloratadine(5mgto20mg)for14days.

Inasingledosetrialusinga7.5-mgdoseofdesloratadine,therewasnoeffectoffood(high-fat,high

caloricbreakfast)onthedispositionofdesloratadine.

Inasingledose,crossovertrialofdesloratadine,thetabletandsyrupformulationswerebioequivalent

andnotaffectedbythepresenceoffood(highfat,highcaloricbreakfast).

Inanotherstudy,grapefruitjuicehadnoeffectonthedispositionofdesloratadine.

Inseparatesingledosestudies,attherecommendeddoses,paediatricpatientshadcomparableAUCand

valuesofdesloratadinetothoseinadultswhoreceiveda5mgdoseofdesloratadinesyrup.

ClinicalStudies

SeasonalAllergicRhinitis

Inadultandadolescentpatientswithseasonalallergicrhinitis,CLARAMAXtabletswereeffectivein

relievingsymptomssuchassneezing,nasaldischargeanditching,congestion/stuffiness,aswellas

ocularitching,tearingandredness,anditchingofpalate.CLARAMAXtabletseffectivelycontrolled

symptomsfor24hours.

CLARAMAXwaseffectiveinalleviatingtheburdenofseasonalallergicrhinitisasshownbythetotal

scoreoftherhino-conjunctivitisqualityoflifequestionnaire.Thegreatestameliorationwasseeninthe

domainsofpracticalproblemsanddailyactivitieslimitedbysymptoms.

Intwo4-weektrialsinadultsandadolescentswithseasonalallergicrhinitisandconcurrentasthma,

desloratadinewasshowntobeeffectiveinreducingthesymptomsofseasonalallergicrhinitis

(rhinorrhea,nasalcongestion,nasalitchingandsneezing,itching/burningeyes,tearing/wateringeyes,

rednessofeyes,anditchingofearsorpalate)andasthma(coughing,wheezing,difficultybreathing),

anddecreasingbeta-agonistuse.FEV

wasnotalteredinthedesloratadineorplacebotreatmentgroups.

ChronicIdiopathicUrticaria

Intrialsconductedinadultsandadolescentswithchronicidiopathicurticaria,CLARAMAXtablets

wereeffectiveinrelievingpruritusanddecreasingthesizeandnumberofhivesasearlyas1dayafter

wereeffectiveinrelievingpruritusanddecreasingthesizeandnumberofhivesasearlyas1dayafter

initiationoftreatment.Ineachtrial,theeffectsweresustainedoverthe24hourdosinginterval.

TreatmentwithCLARAMAXtabletsalsoimprovedsleepanddaytimefunction,asmeasuredby

reducedinterferencewithsleepandroutinedailyactivities.

PaediatricPopulation

SafetyofCLARAMAXSyrupwasdemonstratedinthreepaediatrictrials.Childrenaged6months-11

yearswhowerecandidatesforantihistaminetherapyreceivedadailydoseofCLARAMAX1mg(6to

11monthsofage),CLARAMAX1.25mg(1to5yearsofage)orCLARAMAX2.5mg(6to11years

ofage).Treatmentwaswelltoleratedasdocumentedbyclinicallaboratorytests,vitalsignsandECG

intervaldata,includingQTc.Whengivenattherecommendeddoses,theplasmaconcentrationof

desloratadinewascomparableinthepaediatricandadultpopulations.Althoughtheefficacyof

desloratadinehasnotbeendemonstratedinchildrenundertheageof2years.thecourseofthediseases

(seasonalandperennialallergicrhinitisandchronicidiopathicurticaria)andthepharmacokineticprofile

ofdesloratadinearesimilarinadultsandpaediatricpatients.Therefore,desloratadineefficacydatain

adultscanbeextrapolatedtothepaediatricpopulation.

INDICATIONS

CLARAMAXisindicatedforthereliefofsymptomsassociatedwithseasonalandperennialallergic

rhinitis,suchassneezing,nasaldischargeanditching,congestion/stuffiness,aswellasocularitching,

tearingandredness,itchingofpalateandcoughing.

CLARAMAXisalsoindicatedforthereliefofsymptomsassociatedwithchronicidiopathicurticaria

suchasthereliefofitchingandthesizeandnumberofhives.

DOSAGEANDADMINISTRATION

CLARAMAXcanbetakenregardlessofmealtimeforthereliefofsymptomsassociatedwithallergic

rhinitis(includingintermittentandpersistentallergicrhinitis)andchronicidiopathicurticaria.

Intermittentallergicrhinitis(presenceofsymptomsforlessthan4daysperweekorforlessthan4

weeks)shouldbemanagedinaccordancewiththeevaluationofthepatient'sdiseasehistoryandthe

treatmentshouldbediscontinuedaftersymptomsareresolvedandreinitiatedupontheirreappearance.In

persistentallergicrhinitis(presenceofsymptomsfor4daysormoreperweekandformorethan4

weeks),continuedtreatmentmaybeproposedtothepatientsduringallergenexposureperiods.

Adultsandadolescents12yearsandover:OneCLARAMAX5mgfilm-coatedtabletor10mL(5mg)

CLARAMAXSyruponcedaily.

Children6to11yearsofage:5mL(2.5mg)CLARAMAXSyruponcedaily.

Children2to5yearsofage:2.5mL(1.25mg)CLARAMAXSyruponcedaily.

Children6to11monthsofage:2mL(1mg)ofCLARAMAXSyruponcedaily.

CONTRAINDICATIONS

CLARAMAXtabletsandsyruparecontraindicatedinpatientswhohaveshownhypersensitivityor

idiosyncrasytodesloratadine,toanyoftheexcipientsortoloratadine.

WARNINGSANDPRECAUTIONS

EfficacyandsafetyofCLARAMAXinchildrenunder6monthsofagehavenotbeenestablished.

AlthoughCLARAMAXisunlikelytoaffecttheabilitytodriveoroperatemachinery,afewpeople

maybeaffectedandcareshouldbetaken.

UseinPregnancy(CategoryB1)

Thesafeuseofdesloratadineduringpregnancyhasnotbeenestablished.Therefore,CLARAMAXis

nottobeusedduringpregnancyunlessclearlyindicated.

Nooveralleffectonratfertilitywasobservedwithdesloratadineatanexposurethatwas34timeshigher

thantheexposureinhumansattherecommendedclinicaldose.

Noteratogenicormutageniceffectswereobservedinanimaltrialswithdesloratadine.

UseinLactation

Desloratadinepassesintobreastmilk.Hence,theuseofCLARAMAXbybreastfeedingmothersisnot

recommended.

CarcinogenicityandMutagenicity

Desloratadinehasnocarcinogenicriskinmanbasedontheavailabledatawithloratadine.Desloratadine

showednomutageniceffectsininvitroandinvivomutagenicitystudies.

DrugInteractions

NoclinicallyrelevantinteractionswithCLARAMAXwereobservedinclinicaltrials(see

Pharmacologysection).

CLARAMAXtakenconcomitantlywithalcoholdidnotpotentiatetheperformanceimpairingeffectsof

alcohol.

Therewasnoeffectoffoodorgrapefruitjuiceonthedispositionofdesloratadine.

LaboratoryInteractions

CLARAMAXshouldbediscontinuedapproximately48hourspriortoskintestingproceduressince

antihistaminesmaypreventordiminishotherwisepositivereactionstodermalreactivityindicators.

ADVERSEREACTIONS

Inclinicaltrialsinapaediatricpopulation,CLARAMAXSyrupwasadministeredtoatotalof246

childrenaged6monthsto11years.Theoverallincidenceofadverseeventsinchildren2to11yearsof

childrenaged6monthsto11years.Theoverallincidenceofadverseeventsinchildren2to11yearsof

agewassimilarforCLARAMAXsyrupandplacebogroups.Ininfantsandtoddlersaged6to23

months,themostfrequentadverseeventsreportedinexcessofplacebowerediarrhoea(3.7%),fever

(2.3%)andinsomnia(2.3%).

Inclinicaltrialsinarangeofindicationsincludingseasonalallergicrhinitisandchronicidiopathic

urticaria,attherecommendeddoseof5mgdaily,undesirableeffectswithCLARAMAXTabletswere

reportedin3%ofpatientsinexcessofthosetreatedwithplacebo.Themostfrequentadverseevents

reportedinexcessofplacebowerefatigue(1.2%),drymouth(0.8%),andheadache(0.6%).

Noeffectsontheabilitytodriveandusemachineshavebeenobservedwiththeuseofdesloratadine.

Veryrarecasesofhypersensitivityreactions(includinganaphylaxisandrash),psychomotor

hyperactivityandseizureshavebeenreportedduringthemarketingofdesloratadine.

Inaddition,casesoftachycardia,palpitations,elevationsofliverenzymes,hepatitis,and

increasedbilirubinhavebeenreportedveryrarely.

Inclinicaltrialsinapaediatricpopulation,CLARAMAXsyrupwasadministeredto115childrenages2

through11years.TheoverallincidenceofadverseeventswassimilarfortheCLARAMAXSyrupand

theplacebogroups.

OVERDOSAGE

Intheeventofoverdose,considerstandardmeasurestoremoveunabsorbedactivesubstance.

Symptomaticandsupportivetreatmentisrecommended.

Basedonamultipledoseclinicaltrialinadultsandadolescents,inwhichupto45mgofdesloratadine

wasadministered(9timestheclinicaldose),noclinicallyrelevanteffectswereobserved.

Desloratadineisnoteliminatedbyhaemodialysis;itisnotknownifitiseliminatedbyperitoneal

dialysis.

PHARMACEUTICALPRECAUTIONS

Tablets:Theshelf-lifeis24monthswhenstoredbelow25°C.Protectfrommoisture.

Syrup:Theshelf-lifeis24monthswhenstoredbelow30°C.Storeinoriginalcontainer.

MEDICINECLASSIFICATION

PharmacyMedicine

PRESENTATIONANDPACKAGEQUANTITIES

Tablets:5mg,lightblueroundembossedfilmcoated-10s,30s

Syrup:0.5mg/mL,clearorangecolouredsolution-100mLand200mL

NAMEANDADDRESS

Schering-PloughadivisionofSchering-PloughAnimalHealthLimited

36KitchenerStreet

Auckland

NEWZEALAND

Telephone:093759210

DATEOFPREPARATION

8May2008

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