EBASTION

Main information

  • Trade name:
  • EBASTION Film Coated Tablet 10 Milligram
  • Dosage:
  • 10 Milligram
  • Pharmaceutical form:
  • Film Coated Tablet
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • EBASTION Film Coated Tablet 10 Milligram
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA1599/001/001
  • Authorization date:
  • 26-02-2010
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Ebastion10mgfilm-coatedtablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Ebastion10mgfilm-coatedtablets:

1film-coatedtabletofEbastion10mgcontains:10mgebastine

Forafulllistofexcipients,seesection6.1.

3PHARMACEUTICALFORM

Film-coatedtablet

Ebastion10mgfilm-coatedtabletsarewhitetooff-white,round,bevelledfilm-coatedtabletswithascorelineonone

sideandadiameterof7.1mm.

Thetabletcanbedividedintoequalhalves.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Forthesymptomatictreatmentofseasonalandperennialallergicrhinitiswithorwithoutallergicconjunctivitis.

Toimproveitchingandtoreducenewwealformationinurticariaofunclearorigin.

4.2Posologyandmethodofadministration

Theexperienceinchildrenundertheageof12yearsislimited.

Allergicrhinitis:

Forchildren12yearsandaboveandadultsthefollowingdosagerecommendationsapply:1film-coatedtablet(10mg

ebastine)oncedaily.Incasesofseveresymptomsandforperennialallergicrhinitisthedosemaybeincreasedto2

film-coatedtablets(20mgebastine)oncedaily.

Urticaria:

Foradultsabove18yearsthefollowingdosagerecommendationsapply:1film-coatedtablet(10mgebastine)once

daily.

Specialsubjectgroups:

Inpatientswithrenalinsufficiency,nodoseadjustmentisnecessaryfortreatmentupto5days.

Inpatientswithmildtomoderatehepaticinsufficiency,nodoseadjustmentisnecessaryfortreatmentupto7days.

Adosageof10mgdailyshouldnotbeexceededinpatientswithseverehepaticinsufficiency.

Methodofadministration:

Thefilm-coatedtabletsshouldbetakenunchewedwithliquid.

Ebastinecanbetakenatmealtimesorindependentlyofmeals.

Durationofuse:

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Forallergicrhinitisthereisclinicalexperienceofuseforadurationofupto1yearand,forurticariaofunclearorigin,

forupto3months.

4.3Contraindications

Hypersensivitytotheactivesubstanceortoanyoftheexcipients.

Ebastinemustnotbeusedforthetreatmentofurticariainadolescentsbelowtheageof18years,asatpresentthereis

onlylittleexperienceinthisagegroupandnoexperienceinchildrenbelow12yearsofage.

Lactation.

4.4Specialwarningsandprecautionsforuse

Aswithotherantihistamines,cautionshouldbeexercisedwhenebastineisadministeredtopatientswithknown

prolongationoftheQTcintervalontheECG,hypokalaemiaandincasesofconcomitantuseofmedicinalproducts

knowntoprolongtheQTcintervalorinhibitthehepaticCYP450-2J2,-4F12or-3A4enzymesystem,suchasazole

antifungalagentsandmacrolideantibiotics(seesection4.5).Cautionshouldbeexercisedinpatientswithsevere

hepaticinsufficiency(seesection4.2).

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Interactionstudiesofebastinewithketoconazoleorerythromycin(activesubstancesknowntoprolongtheQTc

interval)showedinteractionsintheformofhigherplasmaebastinelevelsandaprolongationoftheQTcintervalof

onlyapprox.10mseccomparedwiththeadministrationofketoconazoleorerythromycinalone.Incorresponding

clinicalstudies,nointeractionsofebastinewiththeophylline,warfarin,cimetidine,diazepamoralcoholwereobserved.

Incasesofconcomitantfoodintakethereisa1.5-to2.0-foldriseintheplasmalevelofcarebastine,theactiveprincipal

metaboliteofebastine,andanincreaseintheAUC,whileT

remainsunchanged.However,clinicalefficacyisnot

affected.

4.6Fertility,pregnancyandlactation

Therearenodatafromtheuseofebastineinpregnantwomen.Animalstudiesdonotindicatedirectorindirectharmful

effectswithrespecttopregnancy,embryonal/foetaldevelopment,parturitionorpostnataldevelopment(see5.3).

Therefore,ebastineshouldbeusedinpregnancyonlyifclearlyneeded.

Itisnotknownwhethertheactivesubstanceisexcretedinhumanbreastmilk.Inratexcretionofebastininmilkhas

beenshown.Ebastineshouldnotbeusedduringthelactationperiod.

4.7Effectsonabilitytodriveandusemachines

Ebastinehasnegligibleinfluenceontheabilitytodriveandusemachines.

Mostpatientstreatedwithebastinemaydriveorcarryoutotheractivitiesthatrequireagoodreactioncapacity.

However,inordertoidentifysensitivesubjectswhoreactunusuallytoebastine,itisadvisabletoknowtheindividual

reactionsbeforeapatientdrivesorcarriesoutcomplicatedactivities.

4.8Undesirableeffects

Intheevaluationofundesirableeffectsthefollowingfrequencyconventionsaretakenasthebasis:

Verycommon(1/10)

Common(1/100to<1/10)

Uncommon(1/1,000to<1/100)

Rare(1/10,000to1/1,000)

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Cardiacdisorders:

Veryrare:Tachycardia,Palpitations

Nervoussystemdisorders:

Common:Somnolence,Headache

Veryrare:Dysaesthesia

Respiratory,thoracicandmediastinaldisorders:

Uncommon:Epistaxis,Pharyngitis,Rhinitis

Veryrare:Sinusitis

Gastrointestinaldisorders:

Common:Drymouth

Uncommon:Nausea,Abdominalpain,Dyspepsia

Veryrare:Vomiting

Skinandsubcutaneoustissuedisorders:

Veryrare:Exanthema,Urticaria,Eczema,Rash,Dermatitis

Generaldisorders:

Uncommon:Dizziness,Asthenia,Insomnia

Veryrare:Oedema

Hepatobiliarydisorders:

Veryrare:Abnormalliverfunctiontest

Reproductivesystemandbreastdisorders:

Veryrare:Dysmenorrhoea,Menstrualdisorders

Psychiatricdisorders:

Veryrare:Generalnervousness

4.9Overdose

Instudieswithahighdosageupto100mgoncedaily,noclinicallysignificantsymptomsorsignsofoverdosewere

seen.Aspecificantidoteforebastineisnotknown.Intheeventofoverdose,monitoringofvitalfunctions,including

ECGmonitoringwithevaluationoftheQTintervalforatleast24hours,symptomatictreatmentandgastriclavageare

indicated.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacotherapeuticgroup:otheranti-histaminesforsystemicuse

ATCcode:R06AX22

Pre-clinical

IninvitroandinvivostudiesebastinedemonstratesgreataffinityforH1receptors,whicharerapidlyandselectively

inhibitedoveralongperiodoftime.

Impairmentofcentralfunctionsisonlyslight;theriskofoccurrenceofanticholinergiceffectsislow,but,onthebasis

ofthestudiesavailable,cannotbecompletelyruledout.

Afteroraladministration,neitherebastinenoritsactivemetabolitecrosstheblood-brainbarrier.Thischaracteristicis

consistentwiththelowlevelofsedationdeterminedinexperimentalstudiesontheeffectsofebastineonthecentral

nervoussystem.

Invitroandinvivodatashowthatebastineisapotent,highlyselectiveantagonistofthehistamineH1receptorswith

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Clinicalproperties

Whealtestsrevealedastatisticallyandclinicallysignificantanti-histamineeffectcommencing1hourafter

administrationandlastingmorethan48hours.Whentreatmentwithebastinewashaltedafter5days,itsanti-histamine

effectremaineddetectableformorethan72hours.Thiseffectisreflectedintheplasmalevelsoftheprincipalactive

metabolite,carebastine.

Afterrepeatedadministration,inhibitionoftheperipheralreceptorsremainedataconstantlevel,withouttachyphylaxis.

Theseresultssuggestthat,atadoseofatleast10mg,ebastineproducesrapid,intenseandprolongedinhibitionofthe

peripheralH1histaminereceptors,whichpermitsonce-dailyadministration.

ThesedativeeffectwasstudiedbymeansofpharmacologicalEEG,cognitivetests,oculomotorcoordinationtestsand

onthebasisofsubjectiveevaluation.Nosignificantincreaseinsedationwasobservedattherecommendedtherapeutic

dose.Thesefindingsareconsistentwiththoseobtainedindouble-blindclinicalstudies:theincidenceofsedative

effectsofebastineiscomparabletothatofplacebo.

Followingadministrationattherecommendeddoses,noprolongationoftheQTintervalorotherundesirablecardiac

effectswereobservedinspecificstudiesonthecardiaceffectsofebastine.

WhilenoeffectofebastineoverdoseontheQTcintervalwasobservedwithoverdosesofupto60mgdaily,overdoses

of100mgdailyproducedastatisticallysignificant,butclinicallyirrelevantincreaseof10ms(2.7%).

5.2Pharmacokineticproperties

Ebastineisrapidlyabsorbedandundergoesextensivefirst-passmetabolismafteroraladministration.Ebastineisalmost

totallyconvertedtoitsactivemetabolite,carebastine.Afteranoraldoseof10mgebastine,maximumplasmalevelsof

80to100ng/mlcarebastinewereobservedafter2.6to4hours.Thehalf-lifeofthemetaboliteis15-19hours,66%of

whichisexcretedinurineintheformofconjugatedmetabolites.Afterrepeatedadministrationofadailydoseof10

mg,steadystatewithplasmalevelsof130-160ng/mlisreachedafter3to5days.

Afterasingle20mgoraldose,peakplasmalevelsofebastineoccurat1to3hoursandachieveameanlevelof2.8

ng/ml.Peakplasmalevelsofthemetabolite,carebastine,achieveameanvalueof157ng/ml.

Morethan95%ofbothebastineandcarebastineisboundtoplasmaproteins.

Invitrostudiesonhumanhepaticmicrosomesshowthatebastineismetabolisedtocarebastinepredominantlyviathe

CYP450(-2J2,-4F12and-3A4)enzymesystems.Afterconcomitantadministrationofketoconazoleorerythromycin

(bothinhibitorsofCYP450-3A4)significantincreasesinplasmaebastineandcarebastineconcentrationswereobserved

(see4.5).

Inelderlypatients,nochangesinpharmacokineticswereobservedcomparedwithyoungadults.

Inpatientswithmild,moderateorsevererenalinsufficiencyandinpatientswithmildtomoderatehepaticinsufficiency

treatedwithdailydosesof20mgebastine,theplasmaconcentrationsofebastineandcarebastineonthefirstandfifth

dayoftreatmentweresimilartothoseobtainedinhealthyvolunteers.

Inpatientswithrenalinsufficiency,theeliminationhalf-lifeofthemetabolite,carebastineisprolongedto23-26

hours.Inpatientswithhepaticinsufficiency,thehalf-lifeis27hours.

5.3Preclinicalsafetydata

Non-clinicaldatainratsandmicerevealnospecialhazardforhumansbasedonconventionalstudiesofsafety

pharmacology,repeateddosetoxicity,genotoxicity,carcinogenicpotential,toxicitytoreproduction.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Tabletcore:

Cellulose,microcrystalline

Sodiumstarchglycolate(typeA)

Silica,colloidal,anhydrous

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Tabletcoat:

Hypromellose

Titaniumdioxide(E171)

Macrogol400

6.2Incompatibilities

Notapplicable

6.3Shelflife

27months

6.4Specialprecautionsforstorage

Donotstoreabove25°C.

Storeintheoriginalpackageinordertoprotectfromlight.

6.5Natureandcontentsofcontainer

Alu-PVC/PVDCblister

Packsizes:10,15,20,30,50,100film-coatedtablets

Notallpacksizesmaybemarketed.

6.6Specialprecautionsfordisposal

Nospecialrequirements.

Anyunusedproductorwastematerialshouldbedisposedofinaccordancewithlocalrequirements.

7MARKETINGAUTHORISATIONHOLDER

LindopharmGmbH

Neustraße82

40721Hilden

Germany

8MARKETINGAUTHORISATIONNUMBER

PA1599/1/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:26February2010

10DATEOFREVISIONOFTHETEXT

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