DIASTABOL

Main information

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

Documents

Localization

  • Available in:
  • DIASTABOL Tablets 100 Milligram
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0540/144/002
  • Authorization date:
  • 09-03-2007
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Diastabol100mgtablet.

2QUALITATIVEANDQUANTITATIVECOMPOSITION

EachDiastabol100mgtabletcontainsmiglitol100mg.

Forexcipientsseesection6.1.

3PHARMACEUTICALFORM

Tablet.

Whitetoslightlypaleyellow,round,biconvextablet.

Diastabol100mgtabletsareblankononesideandimprintedwith‘MIG100’ontheotherside.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Diastabolisrecommendedasanadjuncttodietordietandsulfonylureasforthetreatmentofnon-insulin-dependent

diabetesmellitus(NIDDM)inpatientsinadequatelycontrolledondietalone,orondietandsulfonylureas.

4.2Posologyandmethodofadministration

Diastaboltabletsaretakenorallyandshouldbechewedwiththefirstmouthfuloffood,orswallowedwholewitha

littleliquiddirectlybeforethemeal.

Adults

Therecommendedinitialdoseis50mgthreetimesaday.Dependingupontolerability,thedoseshouldnormallybe

increasedtotherecommendedmaintenancedoseof100mgthreetimesadayafterfourortwelveweeks’treatment.

Elderlypatients

Nomodificationofthenormaladultdosageregimenisnecessary.

Hepaticimpairment

Nodosageadjustmentisnecessary.

Renalimpairment

Nodosageadjustmentisnecessaryforpatientswithmildtomoderaterenalinsufficiency(creatinineclearance>25

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4.3Contraindications

Hypersensitivitytomiglitolortoanyoftheexcipients.

Miglitolshouldnotbeusedinchildrenandindividualslessthan18yearsofage.

Breast-feedingwoman.

Patientswithinflammatoryboweldisease,coloniculceration,partialintestinalobstructionorpatients

predisposedtointestinalobstruction.Inaddition,miglitolshouldnotbeusedinpatientswhohavechronic

intestinaldiseasesassociatedwithmarkeddisordersofdigestionorabsorptionandpatientswhosufferfromstates

whichmaydeteriorateasaresultofincreasedgasformationintheintestine(e.g.largerhernias).

Asmiglitolclearancehasshowntobereducedwithimpairedrenalfunctionanditseffectshavenotbeenfully

evaluatedinpatientswithmarkedrenalimpairment,itsuseiscontra-indicatedinpatientswithacreatinine

clearanceoflessthan25ml/min.

4.4Specialwarningsandprecautionsforuse

Hypoglycaemia

Miglitolmayacttopotentatethehypoglycaemiceffectsofsulfonylureas,andthedosagesoftheseagentsmayneedto

beadjustedaccordingly.However,thiseffecthasnotbeenseeninclinicaltrialswithmiglitol.Hypoglycaemicepisodes

occurredinclinicaltrialsincombinationwithinsulin.Episodesofhypoglycaemiaoccurringduringtherapymust,

whereappropriate,betreatedbytheadministrationofglucose,notsucrose.Thisisbecausemiglitoldelaysthe

absorptionofdisaccharides,butnotmonosaccharides.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Thebioavailabilityofglibenclamideandmetforminisslightlyreducedwhenadministeredconcomitantlywithmiglitol,

buttheresultsofclinicaltrialswiththesecombinationsindicatethatanypharmacokineticinteractionbetweenthese

agentsisunlikelytobeofclinicalrelevance.

Intestinaladsorbents(e.g.charcoal)anddigestiveenzymepreparationscontainingcarbohydrate-splittingenzymes(e.g.

amylase,pancreatin)mayreducetheeffectofmiglitolandthereforeshouldnotbetakenconcomitantly.

Sincemiglitolmayleadtogastro-intestinalsymptomsincludingsoftstoolsanddiarrhoea,theeffectsoflaxativesmay

beenhanced.Aswithothercausesofdiarrhoea,thepotentialeffectsonconcomitantmedicinalproducts,particularly

sustainedreleasepreparations,shouldalsobeconsideredowingtothepossibilityofalteredgastro-intestinaltransit

times.

Asmiglitoladministrationmayleadtoreducedabsorptionofpropranolol,doseadjustmentofthesecompoundsmaybe

necessarywhentheyaregivenincombinationwithmiglitol.However,regardingpropranolol,nomodificationof

hemodynamicparameterswasseeninpharmacologicalstudies.Concomitantadministrationofmiglitolanddigoxinto

non-patientsvolunteershasresultedinareductionindigoxinplasmaconcentrations.However,thiseffectwasnot

observedinNIDDMpatientspre-treatedforatleastfourweekswithdigoxin.Thispharmacokineticinteractionmay

thereforebeofnoclinicalrelevance.

Nointeractionwasobservedbetweenmiglitolandnifedipine,orbetweenmiglitolandantacidsconsistingof

magnesiumhydroxideandaluminiumhydroxide.

4.6Fertility,pregnancyandlactation

Pregnancy

Nodataconcerningtheuseofmiglitolduringpregnancyinhumansisavailable.Animalstudiesdonotindicateharmful

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Whenthepatientplanstobecomepregnantandduringpregnancy,diabetesshouldnotbetreatedwithmiglitolbut

insulinshouldbeusedtomaintainbloodglucoselevelsasclosetonormalaspossibleinordertolowerriskoffœtal

malformationsassociatedwithabnormalbloodglucoselevels.

Lactation

Miglitolmustnotbeusedduringlactation(See4.3).Miglitolisexcretedinmilkinverylowconcentrations.

4.7Effectsonabilitytodriveandusemachines

Nostudiesontheeffectsontheabilitytodriveandusemachineshavebeenperformed.

Patientsshouldbealertedtothepossibleriskofhypoglycaemiawhenmiglitolisusedincombinationwitha

sulfonylurea.

4.8Undesirableeffects

Thefrequencieslistedbelowaredefinedas:verycommon( ≥1/10),common(≥1/100to<1/10)

anduncommon( ≥1/1,000to<1/100).

Metabolismandnutritiondisorders

Whenusedincombinationwithotheranti-diabetictreatments(sulfonylureasandinsulin),hypoglycaemiahasbeen

commonlyreported(See4.4).

Gastrointestinaldisorders

Owingtoitsmodeofaction,miglitolmayresultinagreaterproportionofundigestedcarbohydratebeingdigestedin

thelargebowel.Thesecarbohydratesmayalsobeutilisedbytheintestinalflora,resultingintheincreasedformationof

intestinalgas.Themajorityofpatientsarethereforelikelytoexperienceoneormoregastro-intestinalsymptoms:

Verycommon:flatulence,diarrhoeaandabdominalpain.

Common:nausea,constipationanddyspepsia.

Thesymptomsarerelatedtobothdoseanddietarysubstrateandmaysubsidewithcontinuedtreatment.Symptomscan

bereducedbyadherencetotheprescribeddiabeticdietandtheavoidanceofsucrose,orfoodstuffscontainingsugar.If

symptomsarepoorlytolerated,areductionindosageisrecommended.

Shoulddiarrhoeapersist,patientsshouldbecloselymonitoredandthedosagereducedortherapywithdrawn,if

necessary.

Common:transaminasesincreased.

Uncommon:hepaticfunctionabnormal

4.9Overdose

Nocaseofoverdosehasbeenreported.Nospecificantidotestomiglitolareknown.Intheeventofoverdosing,patients

arelikelytosufferfromgastro-intestinalsymptoms,forexample,flatulence,diarrhoeaandabdominalpain.Abdominal

distension,softerstools,borborygmi(meteorism)andafeelingoffullnessmayalsooccur.

Intakeofcarbohydrate-containingmealsorbeveragesshouldbeavoidedfor4-6hours.

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5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacotherapeuticgroup:Alpha-GlucosidaseInhibitor

ATCcode:A10BF02

Miglitolisareversibleinhibitorofintestinalalpha-glucosidases.Undertheinfluenceofmiglitol,thedigestionof

complexcarbohydratesintoabsorbablemonosaccharidesinthesmallintestineisdose-dependentlydelayed.

Administrationofmiglitolthusleadstoreducedpostprandialhyperglycaemiaandasmoothingeffectonfluctuationsin

thedailybloodglucoseprofile.Theabsorptionoforallyadministeredglucoseisnotinhibitedbymiglitol.

Incontrasttosulfonylureasmiglitoldoesnotstimulatepancreaticinsulinsecretion.

Treatmentwithmiglitolalsoresultsinareductionoffastingbloodglucoseandtochangesinlevelsofglycosylated

haemoglobin(HbA1,HbA1c).ThechangesmaybeareductionorreduceddeteriorationinHbA1orHbA1clevels,

dependinguponthepatient’sclinicalstatusanddiseaseprogression.Theseparametersareaffectedinadose-dependent

mannerbymiglitol.

5.2Pharmacokineticproperties

Thepharmacodynamicactionofmiglitolislocalinthegastro-intestinaltract.

Followingoraladministrationoflowdosesofmiglitol(12.5to25mg),thecompoundisalmostquantitativelyabsorbed.

Increasingtheoraldoseofmiglitolfrom25to200mgresultedinnon-linearchangesinitsabsorption.Withinthe

recommendeddosagerange,approximately90%ofa50mgdoseisabsorbedincomparisonto60%ofa100mgdose.

TheabsorptioncharacteristicsofmiglitolfollowMichaelis-Mentenkineticswithanabsorptionwindowof6-10hours

followingadministration.Itssteady-statevolumeofdistribution(Vss)of0.18l/kgindicatesthatmiglitolisdistributed

principallyintheextracellularspace.Miglitolisboundtoplasmaproteinsonlyinnegligiblequantities(<4%).

Thedrugisnotmetabolisedinthegutorafterabsorption,butiseliminatedunchangedalmostexclusivelyviathe

kidneys.Miglitolclearancemaybereducedinpatientswithimpairedrenalfunction.Thebiliaryexcretionofmiglitolis

negligible(<1%).Thetotalbodyclearanceisthereforeequaltotherenalclearance(99to114ml/mininyoungnon-

patientvolunteers),andcorrespondstotheglomerularfiltrationrate.Theapparentterminalhalf-life,t1/2,inthe

majorityofyoungnon-patientvolunteersisintherangeof2-3hours.

5.3Preclinicalsafetydata

Inchronictoxicitystudiesweightlosswasthedose-limitingtoxicity.Specifictargetorgansfortoxicitycouldnotbe

determined.

Miglitolhadnogenotoxicpotentialinabatteryofgenotoxicitytests,andtherewasnosignofmiglitol-induced

carcinogenicityinmiceandrats.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Microcrystallinecellulose

Magnesiumstearate

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6.2Incompatibilities

Notapplicable.

6.3ShelfLife

3years.

6.4Specialprecautionsforstorage

Nospecialprecautionforstorage.

6.5Natureandcontentsofcontainer

Blisterstripsinhardcardboardouterscomprising:

Polypropylenefoil(colourless)sealedwithaluminiumfoil

PVC/PVDCfoil(colourless)andaluminiumfoil

Polyamide/aluminium/PVCfoilandaluminiumfoil

Packsizes:15,20,30,50,60,90,120,240tablets.

Notallpacksizesmaybemarketed.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements.

7MARKETINGAUTHORISATIONHOLDER

sanofi-aventisIrelandLimited

CitywestBusinessCampus

Dublin24

8MARKETINGAUTHORISATIONNUMBER

PA0540/144/002

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:4thApril1997

Dateoflastrenewal:23rdJuly2006

10DATEOFREVISIONOFTHETEXT

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