ACARBOSE TECNIMEDE

Main information

  • Trade name:
  • ACARBOSE TECNIMEDE
  • Dosage:
  • 100 Milligram
  • Pharmaceutical form:
  • Tablets
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • ACARBOSE TECNIMEDE
    Ireland
  • Language:
  • English

Other information

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA1773/001/002
  • Authorization date:
  • 13-01-2012
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage,interactions,side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

AcarboseTecnimede100mgTablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Eachtabletcontains100mgofAcarbose.

Forafulllistofexcipients,seesection6.1.

3PHARMACEUTICALFORM

Tablet.

White,plain,roundtablets,scoredononeside.

Thescorelineisonlytofacilitatebreakingforeaseofswallowingandnottodivideintoequaldoses.

4CLINICALPARTICULARS

4.1TherapeuticIndications

AcarboseisrecommendedforthetreatmentoftypeIIdiabetesmellitusinpatientsinadequatelycontrolledondiet

alone,orondietandoralhypoglycaemicagents.

4.2Posologyandmethodofadministration

Acarbosetabletsaretakenorallyandshouldbechewedwiththefirstmouthfuloffood,orswallowedwholewitha

littleliquiddirectlybeforethemeal.Owingtothegreatindividualvariationofglucosidaseactivityintheintestinal

mucosa,thereisnofixeddosageregimen,andpatientsshouldbetreatedaccordingtoclinicalresponseandtoleranceof

intestinalsideeffects.

Adults

Therecommendedinitialdoseis100mgthreetimesaday.However,somepatientsmaybenefitfrommoregradual

initialdosetitrationtominimisegastrointestinalsideeffects.Thismaybeachievedbyinitiatingtreatmentat100mg

onceortwiceaday,withsubsequenttitrationtoathreetimesadayregimen.

Ifaftersixtoeightweeks'treatmentpatientsshowaninadequateclinicalresponse,thedosagemaybeincreasedto100

mgthreetimesaday.Afurtherincreaseindosagetoamaximumof200mgthreetimesadaymayoccasionallybe

necessary.

Patientsreceivingthemaximumdose

requirecarefulmonitoring(seeSpecialwarningsandprecautionsforuse,Section4.4).

Acarboseisintendedforcontinuouslong-termtreatment.

Elderlypatients

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Childrenandadolescentsunder18years

Theefficacyandsafetyofacarboseinchildrenandadolescentshavenotbeenestablished.Acarboseisnot

recommendedforpatientsundertheageof18years.

Renalorhepaticimpairment

Seesection4.3.

4.3Contraindications

Hypersensitivitytoacarboseoranyoftheexcipients.Acarboseisalsocontra-indicatedinpatientswithinflammatory

boweldisease,coloniculceration,partialintestinalobstructionorinpatientspredisposedtointestinalobstruction.In

addition,shouldnotbeusedinpatientswhohavechronicintestinaldiseasesassociatedwithmarkeddisordersof

digestionorabsorptionandinpatientswhosufferfromstateswhichmaydeteriorateasaresultofincreasedgas

formationintheintestine,e.g.largerhernias.

Acarboseiscontra-indicatedinpatientswithhepaticimpairment

AsAcarbosehasnotbeenstudiedinpatientswithsevererenalimpairment,itshouldnotbeusedinpatientswitha

creatinineclearance<25ml/min/1.73m².

4.4Specialwarningsandprecautionsforuse

Hypoglycaemia:Whenadministeredalone,Acarbosedoesnotcausehypoglycaemia.Itmay,however,acttopotentiate

thehypoglycaemiceffectsofinsulinandsulphonylureadrugs,andthedosagesoftheseagentsmayneedtobemodified

accordingly.Inindividualcaseshypoglycaemicshockmayoccur(i.e.clinicalsequelaeofglucoselevels<1mmol/L

suchasalteredconsciouslevels,confusionorconvulsions).

Episodesofhypoglycaemiaoccurringduringtherapymust,whereappropriate,betreatedbytheadministrationof

glucose,notsucrose.Thisisbecauseacarbosewilldelaythedigestionandabsorptionofdisaccharides,butnot

monosaccharides.

Transaminases:Patientstreatedwithacarbosemay,onrareoccasions,experienceanidiosyncraticresponsewitheither

symptomaticorasymptomatichepaticdysfunction.Inthemajorityofcasesthisdysfunctionisreversibleon

discontinuationofacarbosetherapy.Itisrecommendedthatliverenzymemonitoringisconsideredduringthefirstsix

totwelvemonthsoftreatment.Ifelevatedtransaminasesareobserved,withdrawaloftherapymaybewarranted,

particularlyiftheelevationspersist.Insuchcircumstances,patientsshouldbemonitoredatweeklyintervalsuntil

normalvaluesareestablished.

Theadministrationofantacidpreparationscontainingmagnesiumandaluminiumsalts,e.g.hydrotalcite,hasbeen

shownnottoamelioratetheacutegastrointestinalsymptomsofAcarboseinhigherdosageandshould,therefore,notbe

recommendedtopatientsforthispurpose.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

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

amylase,pancreatin)mayreducetheeffectofAcarboseandshouldnotthereforebetakenconcomitantly.

Theconcomitantadministrationofneomycinmayleadtoenhancedreductionsofpostprandialbloodglucoseandtoan

increaseinthefrequencyandseverityofgastro-intestinalsideeffects.Ifthesymptomsaresevere,atemporarydose

reductionofAcarbosemaybewarranted.

TheconcomitantadministrationofcolestyraminemayenhancetheeffectsofAcarbose,particularlywithrespectto

reducingpostprandialinsulinlevels.SimultaneousadministrationofAcarboseandcolestyramineshould,therefore,be

avoided.IntherarecircumstancethatbothAcarboseandcolestyraminetherapyarewithdrawnsimultaneously,careis

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InindividualcasesAcarbosemayaffectdigoxinbioavailability,whichmayrequiredoseadjustmentofdigoxin.

Monitoringofserumdigoxinlevelsshouldbeconsidered.

InapilotstudytoinvestigateapossibleinteractionbetweenAcarboseandnifedipine,nosignificantorreproducible

changeswereobservedintheplasmanifedipineprofiles.

4.6Fertility,pregnancyandlactation

Pregnancy

Foracarbose,noclinicaldataonexposedpregnanciesareavailable.Animalstudiesdonotindicatedirectorindirect

harmfuleffectswithrespecttopregnancy,embryonic/foetaldevelopment,parturitionorpostnataldevelopment(see

section5.3).

Acarboseisnotrecommendedduringpregnancy.

Whenthepatientplanstobecomepregnantandduringpregnancy,diabetesshouldbetreatedwithinsulintomaintain

bloodglucoselevelsasclosetonormalaspossibleinordertolowertheriskoffoetalmalformationsassociatedwith

abnormalbloodglucoselevels.

Lactation

Itisunknownwhetheracarboseisexcretedinhumanbreastmilk.Animalstudieshaveshownexcretionofacarbosein

breastmilk.Acarboseshouldnotbeusedduringbreast-feeding.

4.7Effectsonabilitytodriveandusemachines

Acarbosemonotherapydoesnotcausehypoglycaemiaandisthereforeunlikelytohaveeffectsontheabilitytodriveor

tousemachines.However,patientsshouldbealertedtotheriskofhypoglycaemiawhenacarboseisusedin

combinationwithotherantidiabeticagents

4.8Undesirableeffects

Adversedrugreactions(ADRs)basedonplacebo-controlledstudieswithacarbosesortedbyCIOMSIIIcategoriesof

frequency(placebo-controlledstudiesinclinicaltrialdatabase:acarboseN=8,595;placeboN=7,278;status:10Feb

2006)arelistedbelow.

ADRsderivedfrompostmarketingreports(status:31Dec2005)areprintedinitalic.

SystemOrgan

Class VeryCommon

(1/10) Common

(1/100,<

1/10) Uncommon

(1/1000,<

1/100) Rare

(

1/10,000,<

1/1000) VeryRare

(<1/10,000)

Bloodandthe

lymphatic

system

disorders Thrombocytopenia

Gastrointestinal

disorders(1) Flatulence

Borborygmi

Abdominal

distension Diarrhoea

Abdominal

pain Nausea

Vomiting Ileus

Subileus

Constipation

Hepatobiliary

disorders(2) Liver

enzyme

increase Hepatitis

Jaundice

Skinand

subcutaneous

tissuedisorders Hypersensitivityskin

reactions(Rash,

Erythema,

Exanthema,Urticaria)

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(1)Diarrhoeaandabdominalpainmayoccuraftersucrose-containingfoodsareingested.Iftheprescribeddiabeticdiet

isnotobservedthegastrointestinaladverseeventsmaybeintensified.Thesymptomsarerelatedbothtothedoseandto

thedietarysubstrateandmaydiminishwithcontinuedtreatment.Ifseveresymptomsdevelopinspiteofadherenceto

theprescribeddiabeticdietthedosemustbetemporarilyorpermanentlyreduced.Oftenthedosereductionissufficient

foroneofthemainmeals(lunchordinner).Shoulddiarrhoeapersist,thenpatientsshouldbecloselymonitoredandthe

dosagereducedortherapywithdrawn,ifnecessary.

(2)Rarely,clinicallysignificantabnormalhepaticfunctiontests(threetimesabovetheupperlimitfornormalvalues)

havebeenobservedinpatientstreatedwiththerecommendeddailydoseof150mgto300mgofacarbosedaily.

Abnormalvaluesmaybetemporaryduringtreatment(seesection4.4).

Ifileusorsubileusissuspected,treatmentmustbestoppedimmediately.InJapan,individualcasesoffulminantliver

failurehavebeenobserved,althoughtheroleofacarboseisunclear.

IndividualcasesoffulminanthepatitiswithfataloutcomehavebeenreportedinJapan.Therelationshiptoacarboseis

unclear.

Iftheprescribeddiabeticdietisnotobservedtheintestinalsideeffectsmaybeintensified.

Ifstronglydistressingsymptomsdevelopinspiteofadherencetothediabeticdietprescribed,thedoctormustbe

consultedandthedosetemporarilyorpermanentlyreduced.

Inpatientsreceivingtherecommendeddailydoseof150to300mgAcarbose,clinicallyrelevantabnormalliver

functiontests(threetimesaboveupperlimitofnormalrange)wererarelyobserved.Abnormalvaluesmaybetransient

underongoingAcarbosetherapy.(SeeSection4.4).

4.9Overdose

WhenAcarbosetabletsaretakenwithdrinksand/ormealscontainingcarbohydratesoverdosemayleadtometeorism,

flatulenceanddiarrhoea.IfAcarbosetabletsaretakenindependentlyoffood,excessiveintestinalsymptomsneednot

beanticipated.

NospecificantidotestoAcarboseareknown.

Intakeofcarbohydrate-containingmealsorbeveragesshouldbeavoidedfor4-6hours.

Diarrhoeashouldbetreatedbystandardconservativemeasures.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacotherapeuticgroup:Alphaglucosidaseinhibitors,ATCcode:A10BF01.

Inallspeciestested,acarboseexertsitsactivityintheintestinaltract.Theactionofacarboseisbasedonthe

competitiveinhibitionofintestinalenzymes(-glucosidases)involvedinthedegradationofdisaccharides,

oligosaccharides,andpolysaccharides.Thisleadstoadose-dependentdelayinthedigestionofthesecarbohydrates.

Glucosederivedfromthesecarbohydratesisreleasedandtakenupintothebloodmoreslowly.Inthisway,acarbose

reducesthepostprandialriseinbloodglucose,thusreducingbloodglucosefluctuations.

5.2Pharmacokineticproperties

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ThepharmacokineticsofAcarbosewereinvestigatedafteroraladministrationofthe 14

C-labelledsubstance(200mg)

tohealthyvolunteers.Onaverage,35%ofthetotalradioactivity(sumoftheinhibitorysubstanceandanydegradation

products)wasexcretedbythekidneyswithin96h.Theproportionofinhibitorysubstanceexcretedintheurinewas1.7

%oftheadministereddose.50%oftheactivitywaseliminatedwithin96hoursinthefaeces.Thecourseofthetotal

radioactivityconcentrationinplasmawascomprisedoftwopeaks.Thefirstpeak,withanaverageacarbose-equivalent

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.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Microcrystallinecellulose

Colloidalanhydroussilica

Magnesiumstearate

Pregelatinisedstarch

6.2Incompatibilities

Notapplicable

6.3Shelflife

2years

6.4Specialprecautionsforstorage

Donotstoreabove30°C.Storeintheoriginalpackagingtoprotectfromlightandmoisture.

6.5Natureandcontentsofcontainer

TransparentandcolourlessPVC/PCTFE/PVCfilm/Alfoilblisters,packedinoutercartonsisusedascontainerclosure

systemforAcarbosetablets.

Packsizes:10,20,30,50,60,90,120and270tablets.

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6.6Specialprecautionsfordisposal

Nospecialrequirements.

Anyunusedproductorwastematerialshouldbedisposedofinaccordancewithlocalrequirements.

7MARKETINGAUTHORISATIONHOLDER

MultigenerisGmbH

Marlowring21

22525Hamburg

Germany

8MARKETINGAUTHORISATIONNUMBER

PA1773/001/002

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:29January2010

10DATEOFREVISIONOFTHETEXT

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