ACARBOSE 100 Milligram Tablets

Ireland - English - HPRA (Health Products Regulatory Authority)

Buy It Now

Active ingredient:
ACARBOSE
Available from:
McDermott Laboratories Ltd t/a Gerard Laboratories
INN (International Name):
ACARBOSE
Dosage:
100 Milligram
Pharmaceutical form:
Tablets
Prescription type:
Product subject to prescription which may be renewed (B)
Authorization status:
Authorised
Authorization number:
PA0577/171/002
Authorization date:
0000-00-00

PACKAGELEAFLET:INFORMATION FOR THEUSER

Acarbose 50mgTablets

Acarbose100 mg Tablets

acarbose

Read all ofthisleafletcarefullybeforeyou starttakingthismedicinebecauseitcontains

importantinformation foryou.

Keepthis leaflet.Youmayneedtoreaditagain.

Ifyouhaveanyfurtherquestions,ask yourdoctororpharmacist.

Thismedicinehasbeen prescribed foryou only.Donotpassiton to others.Itmayharmthem,

evenifthe signs ofillnessare the sameas yours.

Ifyougetany sideeffects,talktoyourdoctororpharmacist.This includes anypossible side

effectsnot listedinthisleaflet.

Whatisin thisleaflet:

1. WhatAcarbose is andwhatitis usedfor.

2. Whatyouneed to do beforeyou takeAcarbose.

3. How totake Acarbose.

4. Possible side effects.

5. How tostore Acarbose.

6. Contentsofthepack and otherinformation.

1. WHATACARBOSEISANDWHATITISUSEDFOR

The active ingredientinthismedicine isacarbose.This belongs toa groupofmedicines called

glucosidaseinhibitors.

Acarbose is usedinthe treatmentofnon-insulindependentdiabetes mellitus inpatients inadequately

controlled ondietalone,oron dietandoralhypoglycaemicagents.Acarboseisindicated in adults

agedover18years.This medicine has been prescribed foryou byyourdoctorto treatyourdiabetes.

Acarbose willhelptocontrolyourbloodsugarlevels.This is because Acarboseworks byslowing

down thedigestion ofcarbohydrates(complex sugars)fromyourdiet,and thisreducestheabnormally

highbloodsugarlevels thatoccuraftereachmeal.

2. WHATYOU NEEDTOKNOW BEFORE YOUTAKE ACARBOSE

DonottakeAcarbose

ifyou areallergicto acarboseoranyoftheotheringredientsofthismedicine(listed in section6)

ifyou arepregnantorbreastfeeding

ifyou sufferfrominflammation orulceration ofthebowel,forexampleulcerativecolitisor

Crohn’s disease

ifyouhavean obstructioninyourintestines,orarelikelyto getthis

ifyouhavealargehernia,oranyothercondition whereincreasedgas inyourintestinemaymake

itworse

ifyouhavean intestinaldiseasewhereyou do notdigestorabsorb food properly

ifyouhaveseverekidneyproblems

ifyouhavealiverdisorder.

Ifyouhaveakidneydisorder,do nottakeAcarbosewithoutconsultingyourdoctorfirst.Ifyou are

unsurewhetheryou mighthaveany oftheseconditions,pleaseaskyourdoctor.

Warningsand Precautions

Treatinghypoglycaemicepisodes(‘hypos’)

As a diabeticyoumayalsobe receivingothertreatments foryourdiabetes.

Ifyou aretaking insulin orsulphonylureasdrugsto controlyourblood sugar,youwillprobably be

used to avoiding hypoglycaemicepisodesbytaking sugarwhenyou feelthatyourblood sugar

level istoolow.

Whentaking acarboseDONOTtreata hypoglycaemic episode withordinarysugar(sucrose)

insteadtake some glucose (alsoknownas dextrose)tablets,syrup,orsweetswhichshouldbe

available fromyourpharmacist.

This medicinemayaffectthe levelofcertainproteinscalledenzymesin yourblood.Yourdoctormay

wish to seeyou morefrequentlyinorderto monitorthelevelsoftheseenzymes.Yourdoctormay

decide toreduce the dose orstoptreatmentwithAcarbose.

Othermedicines andAcarbose

Tellyourdoctororpharmacistifyou aretaking,haverecentlytaken ormighttakeany other

medicines.Acarbosemayalterthe effectofotherdrugs,oralternatively,some drugs mayalterthe

effectofAcarbose:

medicines calledintestinalabsorbants,suchas charcoal

medicines containingdigestive enzymes thathelpdigestion,suchas amylase andlipase

neomycin, anantibiotic

colestyramine,totreathighcholesterol

digoxin,to treatheartproblems

otherblood glucoselowering drugs(e.gsulphonylureas,metformin,orinsulin).

Acarbosewith food anddrink

Keep to thedietprescribedbyyourdoctor.Ifdistressing complaintsdevelop in spiteofstrict

adherence toyourdiet(see“Possible side effects”),contactyourdoctoras yourdose ofAcarbosemay

need to bereduced.

Household sugar(canesugar)and foodscontaining itcan causeabdominaldiscomfortoreven

diarrhoeadueto carbohydrate-fermentation inthecolon during treatmentwith Acarbose.

Youmaynotice side effects suchas severe flatulenceanddiarrhoea ifyouhave takenAcarbose

togetherwithcarbohydratecontainingdrinksorfood.In thiscase,do noteatordrink carbohydrate

containingdrinksorfood for4 to6 hours.

Pregnancyandbreast-feeding

DonottakeAcarboseifyou arepregnantorbreastfeeding.Ifyouthinkyou mightbepregnantorare

planningafamily,tellyourdoctorbeforetaking thismedicine.

Drivingandusingmachines

Acarbose is unlikelytoaffectyourabilitytodrive orusemachines.

3. HOWTO TAKEACARBOSE

Alwaystakethismedicineexactlyasyourdoctorhastoldyou.Check withyourdoctororpharmacist

ifyou arenotsure.

Adultsincludingover65s:

The recommendeddose is1or2tablets,three times aday.Tostarttreatmentyourdoctormay

recommendtakingthe tablets onlyonceortwice a day.He orshe willthenincrease yourdose tothree

times a day.The maximumdose is 200mgthree times a day.

Use inchildrenandadolescents under18years ofage:

Acarbose is notrecommendedinpatientsunder18yearsofage.

Method ofadministration

Tablets are swallowedwhole witha glass ofwaterimmediatelybeforethemealorchew withthe first

mouthfuloffood.

Thescorelineon the100mg tabletisnotintended forbreaking thetablet.

Thetreatmentis forlong-termuse.Takethetabletsforaslong asyourdoctorhastoldyou to.

IfyoutakemoreAcarbosethanyoushould

Gotoyourdoctorornearesthospitalimmediately.Take the containerandanyremainingtablets with

you.Donottakefood ordrinkscontaining carbohydrates.

Ifyouforgettotake Acarbose

Do nottakeadoubledoseto makeup foraforgotten dose.Takethenextdosewithyournextmeal.

Donottake the tablets betweenmeals.

Ifyoustoptaking Acarbose

Ifyou suddenly stop takingAcarboseyourblood glucoselevelmayrise.Speak toyourdoctorbefore

stoppingthismedicine.

Ifyouhaveanyfurtherquestionson theuseofthismedicine,ask yourdoctororpharmacist.

4. POSSIBLESIDEEFFECTS

Likeallmedicines,Acarbose cancause side effects,althoughnoteverybodygets them.

Effects occurringinthe firsttwoor three days:

increasedwind(flatulence)

rumbling inyourstomach

feeling offullnessorabdominalcramps.

Contactyourdoctoriftheseeffects continue formorethan2or3days,iftheyare severe,or

particularlyifyouhave diarrhoea.Donottake indigestionpreparations (antacids)as theyare unlikely

to help.

Ifyou thinkyou mayhaveanyofthefollowingsideeffects, stoptakingthismedicineand contact

yourdoctororgo toyournearesthospitalemergency roomimmediately:

yellowingofthe whites ofthe eyes orskin(jaundice)(rare,mayaffectup to 1 in1,000

people)

inflammation oftheliver(hepatitis)(frequencynotknown).

Other possible side effects:

Very common:may affectmorethan1 in10people

wind(flatulence).

Common:may affectupto 1 in10 people

diarrhoea

stomach orabdominalpain.

These side effects are likelytooccurafteramealcontainingsugar(sucrose).Symptomsmaybe

reduced byavoiding foodsand drinksthatcontain sugar(sucrose,canesugar).Ifyourdiarrhoeadoes

notgo awayyourdoctorwillreduceyourdoseorinsomecasesstop treatment.Do nottake

indigestion remediesto treattheabovesideeffects asthis canmakethe symptoms worse.

Uncommon:may affectupto 1 in100people

feelingsick(nausea)

being sick (vomiting)

indigestion

increase inliverenzymes(transaminases)inthe blood.

Rare:may affectupto 1 in1,000 people

swollenskin(oedema).

Notknown:frequencycannotbeestimated fromtheavailabledata:

a decrease inthe numberofbloodcells necessaryforclotting

allergic reaction,suchas rash,redness ofthe skin,skineruptions,itching

a decrease inbowelactivity

gas pockets inthe bowel(Pneumatosiscystoides intestinalis).

rashwithpus filledpimples/blisters (acute generalisedexanthematous pustulosis)

In addition,eventsreported asliverdisorder,abnormalliverfunction and liverinjuryhavebeen

received,particularlyfromJapan.

Individualcases ofsuddenhepatitis witha fataloutcome have beenreportedinJapan.Itis notclear

whetherthose are as a resultoftakingacarbose.

Reportingofside effects

Ifyougetanyside effects,talktoyourdoctor,pharmacistornurse.This includes anypossibleside

effects notlistedinthis leaflet.Youcanalsoreportside effects directly(see details below).By

reporting sideeffectsyou can help providemoreinformation on thesafetyofthismedicine.

IRELAND:

FREEPOST

Pharmacovigilance Section,

IrishMedicines Board,

KevinO’MalleyHouse,

EarlsfortCentre,

EarlsfortTerrace,

Dublin 2,Ireland.

Tel:+353 16764971

Fax:+353 16762517

Website: www.imb.ie

E-mail:imbpharmacovigilance@imb.ie

5. HOW TOSTORE ACARBOSE

Keep thismedicineoutofthesightand reach ofchildren.

Donotuse thismedicine afterthe expirydate,whichis statedonthe cartonandblisterafter

‘EXP’. Theexpirydatereferstothelast dayofthat month.

Thismedicinalproductdoesnotrequireany specialtemperaturestorageconditions.Storeinthe

originalpackagein orderto protectfrommoisture.

Do notusethismedicineifyounoticeanydiscolouration.

Donotthrow awayanymedicines via wastewaterorhouseholdwaste.Askyourpharmacisthow

to throwaway medicinesyou no longeruse.Thesemeasureswillhelp to protecttheenvironment.

6. CONTENTSOFTHE PACKANDOTHER INFORMATION

WhatAcarbose tablets contain

The active substance is acarbose.Each tabletcontainseither50 mg or100mg ofacarbose.

The otheringredients are silica,colloidalanhydrous;maize starch;magnesiumstearate;cellulose,

microcrystalline.

WhatAcarbosetabletslook likeand contentsofthepack

Yourmedicine comes asawhiteround tablet.

Acarbose 50mgtablets aremarked“A”over“50” onone side ofthe tabletand“M” onthe otherside.

Acarbose 100mgtabletsaremarked“AB”(breakline)“100”ononesideofthetabletand“M”on the

otherside.

Acarboseisavailablein blisterpacksof90 and100tablets.

Notallpacksizesmaybemarketed.

MarketingAuthorisation Holder:

McDermottLaboratories Limited

Tradingas GerardLaboratories

35/36BaldoyleIndustrial Estate,

GrangeRoad,Dublin 113,Ireland

Manufacturer(s):

McDermottLaboratories Limited

Tradingas GerardLaboratories

35/36BaldoyleIndustrial Estate,

GrangeRoad,Dublin 113,Ireland

or

Generics[UK]Limited,StationClose,

PottersBar, Hertfordshire, EN61TL,

United Kingdom

or

MylanHungarykft

H-2900,KomáromMylanutca 1,

Hungary

Thismedicinal productisauthorised in theMemberStatesoftheEEA

underthefollowingnames:

Ireland Acarbose50 mg Tablets

Acarbose100 mg Tablets

United Kingdom Acarbose 50mgTablets

Acarbose100 mg Tablets

This leafletwas lastrevisedin11/2013.

Document Outline

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Acarbose100mgTablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Eachtabletcontains100mgacarbose.

Forthefulllistofexcipients,seesection6.1.

3PHARMACEUTICALFORM

Tablet

Awhitetooff-white,11/32”round,biconvextabletdebossedwithABbreakline100ononesideofthetabletandMon

theotherside.Thescorelineisnotintendedforbreakingthetablet.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Acarboseisindicatedinadultsandadolescentsagedover18years.

AcarboseisrecommendedforthetreatmentoftypeIIdiabetesmellitusinpatientsinadequatelycontrolledondiet

alone,orondietandoralhypoglycaemicagents.

4.2Posologyandmethodofadministration

Owingtothegreatindividualvariationofglucosidaseactivityintheintestinalmucosa,thereisnofixeddosage

regimen,andpatientsshouldbetreatedaccordingtoclinicalresponseandtoleranceofintestinalside-effects.

Therecommendedinitialdoseis50mgthreetimesaday.However,somepatientsmaybenefitfrommoregradual

initialdosetitrationtominimisegastrointestinalside-effects.Thismaybeachievedbyinitiatingtreatmentat50mg

onceortwiceaday,withsubsequenttitrationtoathreetimesadayregimen.

Ifaftersixtoeightweeks'treatmentpatientsshowaninadequateclinicalresponse,thedosagemaybeincreasedto100

mgthreetimesaday.Afurtherincreaseindosagetoamaximumof200mgthreetimesadaymayoccasionallybe

necessary.Patientsreceivingthemaximumdoserequirecarefulmonitoring(seeSpecialwarningsandprecautionsfor

use,section4.4).

Ifdistressingcomplaintsdevelopinspiteofstrictadherencetothediet,thedoseshouldnotbeincreasedfurther,andif

necessaryshouldbesomewhatreduced.

Theaveragedoseis300mgAcarbose/day(correspondingto3x2tabletsof50mgAcarbose/day,or3x1tabletof100

mgAcarbose/day).

Acarboseisintendedforcontinuouslong-termtreatment .

Elderlypatients

Nomodificationofthenormaladultdosageregimenisnecessary.

Patientswithhepaticimpairment

Nodoseadjustmentisrequiredinpatientswithpre-existingimpairedhepaticfunction,however,liverenzymesshould

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Paediatricpopulation

Thesafetyandefficacyofacarboseinchildrenandadolescentsunder18yearsofagehavenotyetbeenestablished.

Acarboseisnotrecommendedforpatientsundertheageof18years.

Methodofadministration

Acarbosetabletsaretakenorallyandshouldbechewedwiththefirstmouthfuloffood,orswallowedwholewitha

littleliquiddirectlybeforethemeal.

4.3Contraindications

Hypersensitivitytoacarboseoranyoftheexcipientslistedinsection6.1.

Inflammatoryboweldisease,coloniculceration,partialintestinalobstructionorpredispositiontointestinal

obstruction.Inaddition,acarboseshouldnotbeusedinpatientswhohavechronicintestinaldiseasesassociatedwith

markeddisordersofdigestionorabsorptionandinpatientswhosufferfromstateswhichmaydeteriorateasaresultof

increasedgasformationintheintestine,e.g.largerhernias.

Severekidneyfailure(creatinineclearance<25ml/min/1.73m 2

Severehepaticimpairment(e.g.livercirrhosis)

4.4Specialwarningsandprecautionsforuse

Hypoglycaemia

Acarbosehasanantihyperglycaemiceffect,butdoesnotitselfinducehypoglycaemia.Ifacarboseisprescribedin

additiontootherbloodglucoseloweringdrugs(e.gsulphonylureas,metformin,orinsulin)afallofthebloodglucose

valuesintothehypoglycaemicrangemayrequireadoseadaptionoftherespectiveco-medication.Ifacute

hypoglycaemiadevelopsglucoseshouldbeusedforrapidcorrectionofhypoglycaemia(seesection4.5).

Episodesofhypoglycaemiaoccurringduringtherapymust,whereappropriate,betreatedbytheadministrationof

glucose,notsucrose.Thisisbecauseacarbosewilldelaythedigestionandabsorptionofdisaccharides,butnot

monosaccharides.

Transaminases

Casesoffulminanthepatitishavebeenreportedduringacarbosetherapy.Themechanismisunknown,butacarbose

maycontributetoamultifactorialpathophysiologyofliverinjury.Patientstreatedwithacarbosemay,onrare

occasions,experienceanidiosyncraticresponsewitheithersymptomaticorasymptomatichepaticdysfunction.Inthe

majorityofcasesthisdysfunctionisreversibleondiscontinuationofacarbosetherapy.Itisrecommendedthatliver

enzymemonitoringisconsideredduringthefirstsixtotwelvemonthsoftreatment(seesection4.8).Ifelevationof

liverenzymesareobserved,areductionindosageorwithdrawaloftherapymaybeindicated,particularlyifthe

elevationspersist.Insuchcircumstances,patientsshouldbemonitoredatweeklyintervalsuntilnormalvaluesare

established.

Paediatricpopulation

Thesafetyandefficacyofacarbosehasnotbeenestablishedinpatientsunder18yearsofage.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Acarbosehasananti-hyperglycaemiceffectbut,byitself,doesnotcausehypoglycaemia.Inpatientstreated

simultaneouslywithacarboseandsulphonylurea,metforminorinsulin,theglycaemiavaluesmaydropto

hypoglycaemiclevelsandsodoseadjustmentofthesemedicinalproductsmaybenecessary.Inindividualcases

hypoglycaemicshockmayoccur(i.e.clinicalsequelaeofglucoselevels<1mmol/Lsuchasalteredconsciouslevels,

confusionorconvulsions).

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glucoseisslowerduringtreatment;forthisreason,sucroseisnotsuitableforfastrelieffromhypoglycaemiaand

glucoseshouldbeusedinstead.

Episodesofhypoglycaemiaoccurringduringtherapymust,whereappropriate,betreatedbytheadministrationof

glucose,notsucrose.Thisisbecauseacarbosewilldelaythedigestionandabsorptionofdisaccharides,butnot

monosaccharides.

Sucrose(canesugar)andfoodscontainingsucroseoftencauseabdominaldiscomfortorevendiarrhoeaduring

treatmentwithacarboseasaresultofincreasedcarbohydratefermentationinthecolon.

Intestinaladsorbents(e.g.charcoal)anddigestiveenzymepreparationscontainingcarbohydratesplittingenzymes(e.g.

amylase,pancreatin)mayreducetheeffectofacarboseandshouldnotthereforebetakenconcomitantly.

Theconcomitantadministrationofacarboseandoralneomycinmayleadtoenhancedreductionsofpostprandialblood

glucoseandtoanincreaseinthefrequencyandseverityofgastro-intestinalside-effects.Ifthesymptomsaresevere,a

temporarydosereductionofacarbosemaybeconsidered.

Thesimultaneousadministrationofcolestyramine,intestinaladsorbentsandmedicinalproductswithdigestive

enzymesshouldbeavoidedastheymaypossiblyinfluencetheactionofacarbose,,particularlywithrespectto

reducingpostprandialinsulinlevels.Intherarecircumstancethatbothacarboseandcolestyraminetherapyare

withdrawnsimultaneously,careisneededasareboundphenomenonhasbeenobservedwithrespecttoinsulinlevelsin

non-diabeticsubjects.

Inisolatedcasesacarbosemayaffectthebioavailabilityofdigoxin,makingdoseadjustmentnecessary.Monitoringof

serumdigoxinlevelsshouldbeconsidered.

Theadministrationofantacidpreparationscontainingmagnesiumandaluminiumsalts,e.g.hydrotalcite,hasbeen

shownnottoamelioratetheacutegastrointestinalsymptomsofacarboseandshould,therefore,notberecommendedto

patientsforthispurpose.

Inapilotstudytoinvestigateapossibleinteractionbetweenacarboseandnifedipine,nosignificantorreproducible

changeswereobservedintheplasmanifedipineprofiles.

4.6Fertility,pregnancyandlactation

Pregnancy

Acarboseshouldnotbeadministeredduringpregnancyasnoinformationisavailablefromclinicalstudiesonitsusein

pregnantwomen.

Breastfeeding

Aftertheadministrationofradioactivelymarkedacarbosetonursingrats,asmallamountofradioactivitywas

recoveredinthemilk.Todatetherehavebeennosimilarfindingsinhumans.

Nevertheless,asthepossibilityofdruginducedeffectsonnursinginfantscannotbeexcluded,theprescriptionof

acarboseisnotrecommendedduringbreastfeeding.

Fertility

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4.7Effectsonabilitytodriveandusemachines

Nodataareavailableonalterationoftheabilitytodrivevehiclesorusemachineswhileontreatmentwithacarbose.

4.8Undesirableeffects

TheundesirableeffectsofacarbosefoundintheplacebocontrolledclinicaltrialsandclassifiedaccordingtoCIOMSIII

frequencycategories(placebocontrolledstudiesintheclinicaltrialdatabase:acarboseN=8595;placeboN=7278;

status:10February2006)aredescribedbelow.

Withineachfrequencygrouping,undesirableeffectsarepresentedinorderofdecreasingseriousness.Frequenciesare

definedasverycommon(1/10),common(1/100to<1/10),uncommon(1/1,000to<1/100)andrare(1/10,000

to<1/1,000).

TheADRsidentifiedonlyduringpostmarketingsurveillance(status:31Dec2005)andforwhichafrequencycouldnot

beestimated,arelistedunder“notknown”.

Inpostmarketingcasesofliverdisorder,abnormalhepaticfunctionandliverinjuryhavebeenreceived,particularly

SystemOrgan

Class

(MedDRA) Verycommon Common Uncommon Rare Notknown

Bloodand

lymphatic

system

disorders Thrombocytopenia

Immunesystem

disorders Drug

hypersensitivity

hypersensitivity

(rash,

erythema,

exanthema,

urticaria)

Vascular

disorders Oedema

Gastrointestinal

disorders Flatulence Diarrhoea

Gastrointestinal

andabdominal

pains Nausea

Vomiting

Dyspepsia Subileus/Ileus

Pneumatosis

cystoides

intestinalis

Hepatobiliary

disorders Increasein

transaminases Jaundice Hepatitis

Skinand

subcutaneous

tissuedisorders Acute

generalised

exanthematous

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IndividualcasesofsuddenhepatitiswithafataloutcomehavebeenreportedparticularlyinJapan.Itisnotclear

whetherthoseareasaresultoftakingacarbose.

Thelackofcompliancewiththeprescribeddietmaygiverisetointensificationofintestinalsideeffects.Intheevent

thattheyshouldappearinspiteofcomplyingwiththeprescribeddiabeticdiet,thedoctorshouldbeconsultedandthe

dosereducedeithertemporarilyorpermanently.

Inpatientstreatedwiththerecommendeddailydoseof150mgto300mgacarboseaday,clinicallyrelevantabnormal

liverfunctiontests(threetimesabovenormallimits)wererarelyobserved.Abnormalvaluesmaybetransientduring

treatmentwithacarbose(seesection4.4).

Iftheprescribeddiabeticdietisnotobservedtheintestinalsideeffectsmaybeintensified.

Ifstronglydistressingsymptomsdevelopinspiteofadherencetothediabeticdietprescribed,thedoctormustbe

consultedandthedosetemporarilyorpermanentlyreduced.

Reportingofsuspectedadversereactions

Reportingsuspectedadversereactionsafterauthorisationofthemedicinalproductisimportant.Itallowscontinued

monitoringofthebenefit/riskbalanceofthemedicinalproduct.Healthcareprofessionalsareaskedtoreportany

suspectedadversereactionsviatheonlinereportingoption(preferredmethod)accessiblefromtheIMBhomepage

www.imb.ie ).AdownloadablereportformisalsoaccessiblefromtheIMBwebsite,whichmaybecompleted

manuallyandsubmittedtotheIMBvia‘freepost’(seedetailsbelow).Alternatively,thetraditionalpost-paid‘yellow

card’optionmayalsobeused.

FREEPOST

PharmacovigilanceSection

IrishMedicinesBoard

KevinO’MalleyHouse

EarlsfortCentre

EarlsfortTerrace

Dublin2

Tel:+35316764971

Fax:+35316762517

Website: www.imb.ie

e-mail: imbpharmacovigilance@imb.ie

4.9Overdose

Whenacarboseistakenwithbeveragesand/ormealscontainingcarbohydrates(polysaccharides,oligosaccharidesor

disaccharides),overdosemayleadtometeorism,flatulenceanddiarrhoea.However,intheeventthatacarbosehasbeen

ingestedinoverdoseoutsidemealtimes,noexcessiveintestinalsymptomsshouldbeexpected.

Intheeventofoverdosetheintakeofbeveragesormealscontainingcarbohydratesshouldbeavoidedoverthenext4-6

hours.

Nospecificantidotestoacarboseareknown.

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5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacotherapeuticgroup:Alphaglucosidaseinhibitors,ATCcode:A10BF01.

Inallspeciestested,acarboseexertsitsactivityintheintestinaltract.Theactionofacarboseisbasedonthe

competitiveinhibitionofintestinalenzymes(-glucosidases)involvedinthedegradationofdisaccharides,

oligosaccharides,andpolysaccharides.Thisleadstoadose-dependentdelayinthedigestionofthesecarbohydrates.

Glucosederivedfromthesecarbohydratesisreleasedandtakenupintothebloodmoreslowly.Inthisway,acarbose

reducesthepostprandialriseinbloodglucose,thusreducingbloodglucosefluctuations.

Undertheinfluenceofacarbose,thedigestionofstarchandsucroseintoabsorbablemonosaccharidesinthesmall

intestineisdose-dependentlydelayed.Indiabeticsubjects,thisresultsinaloweringofpostprandialhyperglycaemia

andasmoothingeffectonfluctuationsinthedailybloodglucoseprofile.Treatmentwithacarbosealsoresultsina

reductionoffastingbloodglucoseandtomodestchangesinlevelsofglycatedhaemoglobin(HbA1,HbA1C).

5.2Pharmacokineticproperties

Followingadministration,only1-2%oftheactiveinhibitorisabsorbed.

Thepharmacokineticsofacarbosewereinvestigatedafteroraladministrationofthe14

-labelledsubstance(200mg)to

healthyvolunteers.Onaverage,35%ofthetotalradioactivity(sumoftheinhibitorysubstanceandanydegradation

products)wasexcretedbythekidneyswithin96h.Theproportionofinhibitorysubstanceexcretedintheurinewas

1.7%oftheadministereddose.50%oftheactivitywaseliminatedwithin96hoursinthefaeces.Thecourseofthetotal

radioactivityconcentrationinplasmawascomprisedoftwopeaks.Thefirstpeak,withanaverageacarboseequivalent

concentrationof52.2±15.7µg/lafter1.1±0.3h,isinagreementwithcorrespondingdatafortheconcentrationcourse

oftheinhibitorsubstance(49.5±26.9µg/lafter2.1±1.6h).Thesecondpeakisonaverage586.3±282.7µg/landis

reachedafter20.7±5.2h.Thesecond,higherpeakisduetotheabsorptionofbacterialdegradationproductsfrom

distalpartsoftheintestine.Incontrasttothetotalradioactivity,themaximumplasmaconcentrationsoftheinhibitory

substancearelowerbyafactorof10-20.Theplasmaeliminationhalf-livesoftheinhibitorysubstanceare3.7±2.7h

forthedistributionphaseand9.6±4.4hfortheeliminationphase.

Arelativevolumeofdistributionof0.32l/kgbody-weighthasbeencalculatedinhealthyvolunteersfromthe

concentrationcourseintheplasma.

5.3Preclinicalsafetydata

Non-clinicaldatarevealnospecialhazardforhumansbasedonconventionalstudiesofsafetypharmacology,repeated

dosetoxicity,genotoxicity,carcinogenicpotential,toxicitytoreproduction,besidethesedescribedinothersectionsof

thisSPC.

Animalstudies

Amarkedlyreducedbodyweightgaininratsanddogsafterrepeatedadministrationofacarbosewasconsideredas

pharmacodynamiceffect(lossofcarbohydrates)andcouldbecounteractedbyincreaseoffoodorglucose

supplementation.

CarcinogenicitywasstudiedinSprague-Dawleyrats,Wistarratsandhamsters.Anincreasedtumourincidencein

certaintissues(kidney,testis)wasobservedifmalnutritionduetoacarbosewasnotcorrected.Noincreaseintumour

ratewasobservedifthebodyweightgainwaskeptnormalbyfoodorglucosesupplementation.

Inratsnoimpairmentoffertilitywasobservedinmalesorfemalesatdosesofupto540mg/kg/day.Theoral

administrationofupto540mg/kg/daytoratsduringfoetaldevelopmentandlactationhadnoeffectonparturitionoron

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6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Silica,colloidalanhydous

Maizestarch

Magnesiumstearate

Cellulose,microcrystalline

6.2Incompatibilities

NotApplicable

6.3Shelflife

2years.

6.4Specialprecautionsforstorage

Thismedicinalproductdoesnotrequireanyspecialtemperaturestorageconditions.Storeintheoriginalpackagein

ordertoprotectfrommoisture.

6.5Natureandcontentsofcontainer

ClearAclar–PVC/Aluminiumblistersincardboardcartoncontaining90and100tablets.

Notallpacksizesmaybemarketed.

6.6Specialprecautionsfordisposal

Nospecialrequirements.

Anyunusedproductorwastematerialshouldbedisposedofinaccordancewithlocalrequirements.

7MARKETINGAUTHORISATIONHOLDER

McDermottLaboratoriesLtdt/aGerardLaboratories

35/36BaldoyleIndustrialEstate

GrangeRoad

Dublin13

Ireland

8MARKETINGAUTHORISATIONNUMBER

PA0577/171/002

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

DateofFirstAuthorisation:18 th

January2013

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 05/12/2013 CRN 2137648 page number: 7

December2013 Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 05/12/2013 CRN 2137648 page number: 8

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