ALDOMET

Main information

  • Trade name:
  • ALDOMET Coated Tablets 250 mg Milligram
  • Dosage:
  • 250 mg Milligram
  • Pharmaceutical form:
  • Coated Tablets
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • ALDOMET Coated Tablets 250 mg Milligram
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA1568/004/001
  • Authorization date:
  • 13-05-2011
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

AldometFilm-CoatedTablets250mg

2QUALITATIVEANDQUANTITATIVECOMPOSITION

‘Aldomet’tablets250mg,containmethyldopaequivalentto250mganhydrousmethyldopa.

Forafulllistofexcipients,seesection6.1

3PHARMACEUTICALFORM

Film-coatedtablets

Yellowcoloured,round,film-coatedtabletsmarked‘ALDOMET’ononesideand‘250’ontheotherside.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Inthetreatmentofhypertension(mild,moderateorsevere).

4.2Posologyandmethodofadministration

Useinadults:initialdosage:Usually250mgtwoorthreetimesaday,fortwodays.

Adjustment:Usuallyadjustedatintervalsofnotlessthantwodays,untilanadequateresponseisobtained.The

maximumrecommendeddailydosageis3g.

Manypatientsexperiencesedationfortwoorthreedayswhentherapywith‘Aldomet’isstartedorwhenthedoseis

increased.Whenincreasingthedosage,therefore,itmaybedesirabletoincreasetheeveningdosefirst.

Generalconsiderations:Methyldopaislargelyexcretedbythekidney,andpatientswithimpairedrenalfunctionmay

respondtosmallerdoses.

Withdrawalof‘Aldomet’isfollowedbyreturnofhypertension,usuallywithin48hours.Thisisnotcomplicated

generallybyanovershootofbloodpressure.

Therapywith‘Aldomet’maybeinitiatedinmostpatientsalreadyontreatmentwithotherantihypertensiveagentsby

terminatingtheseantihypertensivemedicationsgraduallyifrequired(seemanufacturer’srecommendationsonstopping

thesedrugs).Followingsuchpreviousantihypertensivetherapy,‘Aldomet’shouldbelimitedtoaninitialdoseofnot

morethan500mgdailyandincreasedasrequiredatintervalsofnotlessthantwodays.

‘Aldomet’mayalsobeusedconcomitantlywiththecombinationofamiloridehydrochlorideandhydrochlorothiazide

(suchasModuret-25)orbeta-blockingagents,suchastimololmaleate.

Whenmethyldopaisgiventopatientsonotherantihypertensivesthedoseoftheseagentsmayneedtobeadjustedto

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Useinchildren:Initialdosageisbasedon10mg/kgofbodyweightdailyin2to4oraldoses.Thedailydosageisthen

increasedordecreaseduntilanadequateresponseisachieved.Themaximumdosageis65mg/kgor3gdaily,

whicheverisless.

Useinelderly:syncopeintheolderpatientmayberelatedtoanincreasedsensitivityandadvancedarteriosclerotic

vasculardisease.Thismaybeavoidedbyusinglowerdoses.

4.3Contraindications

‘Aldomet’iscontraindicatedinpatients:

withactivehepaticdisease,suchasacutehepatitisandactivecirrhosis

withhypersensitivity(includinghepaticdisordersassociatedwithpreviousmethyldopatherapy)toanycomponent

oftheseproducts

withdepression

ontherapywithmonoamineoxidaseinhibitors(MAOIs).

‘Aldomet’isnotrecommendedforthetreatmentofphaeochromocytoma(see4.4‘Specialwarningsandprecautionsfor

use’).

4.4Specialwarningsandprecautionsforuse

Acquiredhaemolyticanaemiahasoccurredrarely,shouldsymptomssuggestanaemia,haemoglobinand/orhaematocrit

determinationsshouldbemade.Ifanaemiaisconfirmedtestsshouldbedoneforhaemolysis.Ifhaemolyticanaemiais

present,‘Aldomet’shouldbediscontinued.Stoppingtherapy,withorwithoutgivingacorticosteroid,hasusually

broughtpromptremission.Rarely,however,deathshaveoccurred.

SomepatientsoncontinuedtherapywithmethyldopadevelopapositiveCoombstest.Fromthereportsofdifferent

investigators,theincidenceaveragesbetween10and20%.ApositiveCoombstestrarelydevelopsinthefirstsix

monthsoftherapy,andifithasnotdevelopedwithin12months,itisunlikelytodosolateroncontinuingtherapy.

Developmentisalsodose-related,thelowestincidenceoccurringinpatientsreceiving1gorlessofmethyldopaper

day.Thetestbecomesnegativeusuallywithinweeksormonthsofstoppingmethyldopa.

PriorknowledgeofapositiveCoombsreactionwillaidinevaluatingacross-matchfortransfusion.Ifapatientwitha

positiveCoombsreactionshowsanincompatibleminorcross-match,anindirectCoombstestshouldbeperformed.If

thisisnegative,transfusionwithbloodcompatibleinthemajorcross-matchmaybecarriedout.Ifpositive,the

advisabilityoftransfusionshouldbedeterminedbyahaematologist.

Reversibleleucopenia,withprimaryeffectongranulocyreshasbeenreportedrarely.Thegranulocytecountreturnedto

normalondiscontinuingtherapy.Reversiblethrombocytopeniahasoccurredrarely.

Occasionally,feverhasoccurredwithinthefirstthreeweeksoftherapy,sometimesassociatedwitheosinophiliaor

abnormalitiesinliver-functiontests.Jaundice,withorwithoutfever,alsomayoccur.Itsonsetisusuallywithinthefirst

twoorthreemonthsoftherapy.Insomepatientsthefindingsareconsistentwiththoseofcholestasis.Rarecasesof

fatalhepaticnecrosishavebeenreported.Liverbiopsy,performedinseveralpatientswithliverdysfunction,showeda

microscopicfocalnecrosiscompatiblewithdrughypersensitivity.Liver-functiontestsandatotalanddifferentialwhite

blood-cellcountareadvisablebeforetherapyandatintervalsduringthefirstsixweekstotwelveweeksoftherapy,or

wheneveranunexplainedfeveroccurs.

Shouldfever,abnormalityinliverfunction,orjaundiceoccur,therapyshouldbewithdrawn.Ifrelatedtomethyldopa,

thetemperatureandabnormalitiesinliverfunctionwillthenreturntonormal.Methyldopa,shouldnotbeusedagainin

thesepatients.Methyldopashouldbeusedwithcautioninpatientswithahistoryofpreviousliverdiseaseor

dysfunction.

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Dialysisremovesmethyldopa:therefore,hypertensionmayrecurafterthisprocedure.

Ifcerebralormyocardialinfarctionoccursduringtherapywith‘Aldomet’,adjustmentofdosageortemporary

cessationof‘Aldomet’mayberequiredduringtheacutephase.Therapywith’Aldomet’shouldnotbeinitiatedduring

theacutephaseofcerebralormyocardialinfarction.

Rarely,involuntarychoreoathetoticmovementshavebeenobservedduringtherapywithmethyldopainpatientswith

severebilateralcerbrovasculardisease.Shouldthesemovementsoccur,therapyshouldbediscontinued.

Interferencewithlaboratorytests:Methyldopamayinterferewiththemeasurementofurinaryuricacidbythe

phosphotungstatemethod,serumcreatininebythealkalinepicratemethod,andAST(SGOT)bycolorimetricmethod.

InterferencewithspectrophotometricmethodsforAST(SGOT)analysishasnotbeenreported.

Asmethyldopafluorescesatthesamewavelengthsascatecholamines,spuriouslyhighamountsofurinary

catecholaminesmaybereportedinterferingwithadiagnosisofphaeochromocytoma.

Itisimportanttorecognisethisphenomenonbeforeapatientwithapossiblephaeochromocytomaissubjectedto

surgery.MethyldopadoesnotinterferewithmeasurementsofVMA(vanillylmandelicacid)bythosemethodswhich

convertVMAtovanillin.Methyldopaisnotrecommendedforthetreatmentofpatientswithphaeochromocytoma.

Rarely,whenurineisexposedtoairaftervoiding,itmaydarkenbecauseofbreakdownofmethyldopaorits

metabolites.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Whenmethyldopaisusedwithotherantihypertensivedrugsoralcohol,theantihypertensiveactionmaybeenhanced.

Similarlytheantihypertensiveeffectmaybemodifiedbyconcurrentadministrationoftricyclicantidepressants,

sympathomimetics,phenothiazinesandmonoamineoxidaseinhibitors(MAOIs).Interactionwithhaloperidolhasbeen

reported.Whenmethyldopaandlithiumaregivenconcomitantlythepatientshouldbemonitoredcarefullyfor

symptomsoflithiumtoxicity.Theprogressofpatientsshouldbecarefullyfollowedtodetectsidereactionsor

manifestationsofdrugidiosyncrasy.

Iron:Severalstudiesdemonstrateadecreaseinbioavailabilityofmethyldopawhenitisingestedwithferroussulphate

orferrousgluconate.Thismayadverselyaffectbloodpressurecontrolinpatientstreatedwithmethyldopa.

Patientsmayrequirereduceddosesofanaestheticswhenonmethyldopa.Ifhypotensiondoesoccurduringanaesthesia,

itcanusuallybecontrolledbyvasopressors.Theadrenergicreceptorsremainsensitiveduringtreatmentwith

methyldopa.

4.6Fertility,pregnancyandlactation

Useinpregnancy

‘Aldomet’hasbeenusedunderclosemedicalsupervisionforthetreatmentofhypertensionduringpregnancy.There

wasnoclinicalevidencethat‘Aldomet’causedfoetalabnormalitiesoraffectedtheneonate.

Methyldopadoescrosstheplacentalbarrierandappearsincordblood.

Althoughnoobviousteratogeniceffectshavebeenreported,thepossibilityoffoetalinjurycannotbeexcluded,andthe

useofthedruginwomenwhoareormaybecomepregnantrequiresthatanticipatedbenefitsbeweighedagainst

possiblerisks.

Breast-feedingmothers

Methyldopaappearsinbreastmilk.Theuseofthedruginbreast-feedingmothersrequiresthatanticipatedbenefitsbe

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4.7Effectsonabilitytodriveandusemachines

Sedation,usuallytransient,mayoccurduringtheinitialperiodoftherapyorwheneverthedoseisincreased.If

affected,patientsshouldnotattempttodrive,oroperatemachinery.

4.8Undesirableeffects

Sedation,usuallytransient,mayoccurduringtheinitialperiodoftherapyorwheneverthedoseisincreased.Headache,

astheniaorweaknessmaybenotedasearlyandtransientsymptoms.

Thefollowingreactionshavebeenreported:

Centralnervoussystem:Sedation(usuallytransient),headache,astheniaorweakness,paraesthesiae,Parkinsonism,

Bell’spalsy,involuntarychoreoathetoticmovements.Psychicdisturbancesincludingnightmares,impairedmental

acuityandreversiblemildpsychosesordepression.Dizziness,light-headedness,andsymptomsofcerebrovascular

insufficiency(maybeduetoloweringofbloodpressure).

Cardiovascular:Bradycardia,prolongedcarotidsinushypersensitivity,aggravationofanginapectoris.Orthostatic

hypotension(decreasedailydosage).Oedema(andweightgain)usuallyrelievedbyuseofadiuretic.

(Discontinuemethyldopaifoedemaprogressesorsignsofheartfailureappear.)

Gastro-intestinal:Nausea,vomiting,distension,constipation,flatus,diarrhoea,colitis,milddrynessofmouth,soreor

‘black’tongue,pancreatitis,sialadenitis.

Hepatic:Liverdisordersincludinghepatitis,jaundice,abnormalliver-functiontests.

Haematological:PositiveCoombstest,haemolyticanaemia,bone-marrowdepression,leucopenia,granulocytopenia,

thrombocytopenia,eosinophilia.Positivetestsforantinuclearantibody,LEcells,andrheumatoidfactor.

Allergic:Drug-relatedfeverandlupus-likesyndrome,myocarditis,pericarditis.

Dermatological:Rashasineczemaorlichenoideruption,toxicepidermalnecrolysis.

Other:Nasalstuffiness,riseinbloodurea,breastenlargement,gynaecomastia,hyperprolactinaemia,amenorrhoea,

lactation,impotence,decreasedlibido,failureofejaculation,mildarthralgiawithorwithoutjointswelling,myalgia.

4.9Overdose

Ifingestionisrecent,emesismaybeinducedorgastriclavageperformed.Thereisnospecificantidote.Treatmentis

symptomatic.Infusionsmaybehelpfultopromoteurinaryexcretion.Specialattentionshouldbedirectedtowards

cardiacrateanoutput,bloodvolume,electrolytebalance,paralyticileus,urinaryfunction,andcerebralactivity.

Administrationofsympathomimeticagents,e.g.noradrenaline(norepinephrine),maybeindicated.Whenchronic

overdosageissuspected,‘Aldomet’shouldbediscontinued.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Methyldopareducesbothsupineandstandingbloodpressure.Itusuallyproduceshighlyeffectiveloweringofthe

supinepressurewithinfrequentsymptomaticposturalhypotension.Exercisehypotensionanddiurnalbloodpressure

variationsrarelyoccur.

Themaximumdecreaseinbloodpressureoccursfourtosixhoursafteroraldosage.Onceaneffectivedosagelevelis

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Afterwithdrawal,bloodpressureusuallyreturnstopre-treatmentlevelswithin24to48hours.

Methyldopahasnodirecteffectoncardiacfunctionandusuallydoesnotreduceglomerularfiltrationrate,renalblood

flow,orfiltrationfraction,cardiacoutputusuallyismaintainedwithoutcardiacacceleration.Insomepatientstheheart

rateisslowed.

Normalorelevatedplasmareninactivitymaydecreaseinthecourseofmethyldopatherapy.

5.2Pharmacokineticproperties

Absorptionoforalmethyldopaisvariableandincomplete.Bioavailabilityafteroraladministrationaverages25%.

Peakconcentrationsinplasmaoccurattwotothreehours,andeliminationofthedrugisbiphasic.Plasmahalf-lifeis

1.8±0.2hours.Approximately70%oftheoralformofthedrugwhichisabsorbedisexcretedintheurineas

methyldopaanditsmono-O-sulphateconjugate.

Methyldopacrossestheplacentalbarrier,appearsincordblood,andappearsinbreastmilk.

5.3Preclinicalsafetydata

Norelevantinformation.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

TabletCore

Cellulosepowder

Anhydrouscitricacid

Colloidalanhydroussilica

Ethylcellulose.

Guargum

Magnesiumstearate

Sodiumcalciumedetate

TabletCoating

Propyleneglycol

Anhydrouscitricacid

Hypromellose

Quinolineyellowaluminiumlake(E104)

Redironoxide(E172)

Talc

Titaniumdioxide

CarnabuaWax

6.2Incompatibilities

Notapplicable

6.3Shelflife

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6.4Specialprecautionsforstorage

Bottle

Donotstoreabove25°C

Keepcontainertightlyclosedinordertoprotectfromlight.

Blister

Donotstoreabove25°C

Storeintheoriginalpackageinordertoprotectfromlight.

6.5Natureandcontentsofcontainer

Whitepolyethylenebottleof100and500tabletswithturquoisepolyethyleneclosure.PVCblisterpackswith

aluminiumlidscontain60and90tablets(instripsof10tablets).

Notallpacksizesmaybemarketed.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements.

7MARKETINGAUTHORISATIONHOLDER

AspenEuropeGmbH

Industriestrasse32-36

D-23843BadOldesloe

Germany

8MARKETINGAUTHORISATIONNUMBER

PA1568/4/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:1April1979

Dateoflastrenewal:1April2009

10DATEOFREVISIONOFTHETEXT

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