BETALOC

Main information

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

Documents

Localization

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

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PPA1328/020/002
  • Authorization date:
  • 21-12-2006
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

IRISHMEDICINESBOARDACT1995

MEDICINALPRODUCTS(LICENSINGANDSALE)REGULATIONS,1998

(S.I.No.142of1998)

PPA1328/020/002

CaseNo:2034068

TheIrishMedicinesBoardinexerciseofthepowersconferredonitbytheabovementionedRegulationsherebygrants

B&SHealthcare

Unit4,BradfieldRoad,Ruislip,Middlesex,HA40NU,UnitedKingdom

anauthorisation,subjecttotheprovisionsofthesaidRegulations,inrespectoftheproduct

Betaloc100MilligramTablets

TheparticularsofwhicharesetoutinPartIandPartIIoftheattachedSchedule.Theauthorisationisalsosubjectto

thegeneralconditionsasmaybespecifiedinthesaidRegulationsaslistedonthereverseofthisdocument.

Thisauthorisation,unlesspreviouslyrevoked,shallcontinueinforcefrom26/03/2007until20/12/2011.

SignedonbehalfoftheIrishMedicinesBoardthis

________________

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PartII

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

BetalocTablets100mg

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Eachtabletcontains100mgMetoprololtartrate

Excipients:Lactose

Forafulllistofexcipients,seesection6.1.

3PHARMACEUTICALFORM

Tablet.

ProductimportedfromtheUK:

Whitetooff-white,circular,biconvextablet,scoredandengraved‘A/ME’ononeside.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Inthemanagementofhypertensionandanginapectoris.Cardiacarrhythmias,especially

supraventriculartachyarrhythmias.

Adjuncttothetreatmentofhyperthyroidism.

EarlyinterventionwithBetalocinacutemyocardialinfarctionreducesinfarctsizeandtheincidence

ofventricularfibrillation.Painreliefmayalsodecreasetheneedforopiateanalgesics.

Betalochasbeenshowntoreducemortalitywhenadministeredtopatientswithacutemyocardial

infarction.

Prophylaxisofmigraine.

4.2Posologyandmethodofadministration

Thetabletsshouldbetakenonanemptystomach.

Thedosemustalwaysbeadjustedtotheindividualrequirementsofthepatient.Thefollowingare

guidelines:

Hypertension

Therecommendedmaintenancedosageinpatientswithhypertensionis100mg-200mgdaily,givenas

asingledoseinthemorningorindivideddoses(morningandevening).Beginwith50mgtwicedaily

or100mgoncedaily.Doseincrementsshouldbeatintervalsthereafteraccordingtoindividualpatient

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otherantihypertensiveagentsmaybeadded.

Long-termantihypertensivetreatmentwithmetoprololindailydosesof100-200mghasbeenshownto

reducetotalmortality,includingsuddencardiovasculardeath,stroke,andcoronaryeventsin

hypertensivepatients.

AnginaPectoris

Therecommendeddosageis100-200mgdaily,givenindivideddoses(morningandevening).Begin

with50mgtwicedaily.Doseincrementsshouldbeatintervalsthereafteraccordingtoindividual

patientresponses.

Maximumdose,usually200mgdaily(individeddoses).Dosesupto300mgdaily(individeddoses)

havebeenused.Ifneeded,otherantianginalagentsmaybeadded.

CardiacArrhythmias

Therecommendeddosageis100-200mgdailygivenindivideddoses(morningandevening).If

needed,otherantiarrhythmicagentsmaybeadded.

Hyperthyroidism

Therecommendeddosageis50mgfourtimesaday.

MyocardialInfarction

Earlyintervention

ToachieveoptimalbenefitsfromintravenousBetalocsuitablepatientsshouldpresentwithin12hours

oftheonsetofchestpain.Therapyshouldcommencewith5mgi.v.every2minutestoamaximumof

15mgtotalasdeterminedbybloodpressureandheartrate.Thesecondorthirddoseshouldnotbe

givenifthesystolicbloodpressureis<90mmHg,theheartrateis<40beats/minandtheP-Qtimeis

>0.26seconds,orifthereisanyaggravationofdyspnoeaorcoldsweating.Oraltherapyshould

commence15minutesafterthelastinjectionwith50mgevery6hoursfor48hours.Patientswhofail

totoleratethefullintravenousdoseshouldbegivenhalfthesuggestedoraldose.

Maintenance

Theusualmaintenancedoseis200mgdaily,givenindivideddoses.

MigraineProphylaxis

Therecommendeddosageis100-200mgdaily,givenindivideddoses(morningandevening).

ImpairedRenalFunction

Doseadjustmentisgenerallynotneededinpatientswithimpairedrenalfunction.

ImpairedHepaticFunction

Doseadjustmentisnormallynotneededinpatientssufferingfromlivercirrhosisbecausemetoprolol

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theseverityofhepaticimpairment.

Elderly

Severalstudiesindicatethatage-relatedphysiologicalchangeshavenegligibleeffectsonthe

pharmacokineticsofmetoprolol.

Children

Thereislimitedexperiencewithmetoprololtreatmentinchildren.

4.3Contraindications

Betaloc,aswithotherbeta-blockers,shouldnotbeusedinpatientswithanyofthefollowing:

-AVblockofsecond-orthird-degree,

-Unstabledecompensatedcardiacfailure(pulmonaryoedema,hypoperfusionorhypotension),

-Continuousorintermittentinotropictherapyactingthroughbeta-receptoragonism,

-Bradycardia,(<45bpm),

-Sicksinussyndrome,

-Cardiogenicshock,

-Severeperipheralarterialcirculatorydisorder,

-Untreatedphaeochromocytoma,

-Metabolicacidosis.

KnownhypersensitivitytoanycomponentofBetalocorotherbeta-blockers.

Betalocisalsocontra-indicatedwhensuspectedacutemyocardialinfarctioniscomplicatedbybradycardia(<45bpm),

firstdegreeheartblock(theP-Qintervalis>0.24sec)orsystolicbloodpressure<100mmHg.

4.4Specialwarningsandprecautionsforuse

Betalocaswithotherbeta-blockers:

shouldnotbewithdrawnabruptly.Whenpossible,Betalocshouldbewithdrawngraduallyovera

periodof10-14days,indiminishingdosesto25mgdailyforthelast6days.Duringitswithdrawal

patientsshouldbekeptunderclosesurveillance,especiallythosewithknownischaemicheartdisease.

Theriskforcoronaryevents,includingsuddendeath,mayincreaseduringthewithdrawalofbeta-

blockade.

mustbereportedtotheanaesthetistpriortogeneralanaesthesia.Itisnotgenerallyrecommendedto

stopBetaloctreatmentinpatientsundergoingsurgery.

althoughcontra-indicatedinsevereperipheralarterialcirculatorydisturbances(seeSection4.3),may

alsoaggravatelesssevereperipheralarterialcirculatorydisorders.

maybeadministeredwhenheartfailurehasbeencontrolled.Digitalisationand/ordiuretictherapy

shouldalsobeconsideredforpatientswithahistoryofheartfailure,orpatientsknowntohaveapoor

cardiacreserve.

maycausepatientstodevelopincreasingbradycardia,insuchcasestheBetalocdosageshouldbe

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duetothenegativeeffectonconductiontime,mayaggravatepre-existingconductiontimedisorders

ofmoderatedegree,whichmayleadtoAVblock,andshouldonlybegivenwithcautiontopatients

withfirstdegreeheartblock.

mayincreasethenumberanddurationofanginaattacksinpatientswithPrinzmetal'sangina,dueto

unopposedalpha-receptormediatedcoronaryarteryvasoconstriction.Betalocisabeta

-selectivebeta-

blocker;consequently,itsusemaybeconsideredalthoughutmostcautionmustbeexercised.

maymasktheearlysignsofacutehypoglycaemia,inparticulartachycardia.Duringtreatmentwith

Betaloc,theriskofinterferingwithcarbohydratemetabolismormaskinghypoglycaemiaislessthan

withnon-selectivebeta-blockers.

maymaskthesymptomsofthyrotoxicosis.

mayincreaseboththesensitivitytowardsallergensandtheseriousnessofanaphylacticreactions.

Althoughcardioselectivebeta-blockersmayhavelesseffectonlungfunctionthannon-selectivebeta-

blockers,aswithallbeta-blockers,theseshouldbeavoidedinpatientswithreversibleobstructive

airwaysdiseaseunlesstherearecompellingclinicalreasonsfortheiruse.Whenadministrationis

necessary,thesepatientsshouldbekeptunderclosesurveillance.Theuseofabeta

-bronchodilator

(e.g.terbutaline)maybeadvisableinsomepatients.Thedosageofthebeta

-agonistmayrequirean

increasewhentreatmentwithBetalociscommenced.

Aswithallbeta-blockers,carefulconsiderationshouldbegiventopatientswithpsoriasisbefore

Betalocisadministered.

InthepresenceoflivercirrhosisthebioavailabilityofBetalocmaybeincreased.

Inpatientswithaphaeochromocytoma,analpha-blockershouldbegivenconcomitantly.

Inlabileandinsulin-dependentdiabetesitmaybenecessarytoadjustthehypoglycaemictherapy.

Intravenousadministrationofcalciumantagonistsoftheverapamil-typeshouldnotbegivento

patientstreatedwithbeta-blockers.

Theinitialtreatmentofseveremalignanthypertensionshouldbesodesignedastoavoidsuddenreductionindiastolic

bloodpressurewithimpairmentofautoregulatorymechanisms.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Betaloccanreducemyocardialcontractilityandimpairintracardiacconduction.Careshouldbe

exercisedwhendrugswithsimilaractivity,e.g.antiarrhythmicagents(ofthequinidinetypeand

amiodarone),orgeneralanaesthetics,aregivenconcurrently.

IncreasednegativeinotropicandchronotropiceffectsmayoccurwhenBetalocisgiventogetherwith

calciumantagonistsoftheverapamilanddiltiazemtype,causingbradycardia,hypotensionand

asystole.Inpatientstreatedwithbeta-blockersintravenousadministrationofcalciumantagonistsof

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Patientsreceivingconcomitanttreatmentwithsympatheticganglionblockingagents,otherbeta-

blockers(i.e.eyedrops),orMonoAmineOxidase(MAO)inhibitorsshouldbekeptunderclose

surveillance.

Ifconcomitanttreatmentwithclonidineistobediscontinued,Betalocshouldbewithdrawnseveral

daysbeforeclonidine.

Betalocwillantagonisethebeta

-effectsofsympathomimeticagentsbutshouldhavelittleinfluence

onthebronchodilatoreffectsofbeta

-agonistsatnormaltherapeuticdoses.

Theadministrationofadrenaline(epinephrine)topatientsundergoingbeta-blockadecanresultinan

increaseinbloodpressureandbradycardiaalthoughthisislesslikelytooccurwithbeta

-selective

drugs.

Betalocmayimpairtheeliminationoflidocaine.

MetoprololisametabolicsubstratefortheCytochromeP450isoenzymeCYP2D6.Drugsthatactas

enzyme-inducingandenzyme-inhibitingsubstancesmayexertaninfluenceontheplasmalevelof

metoprolol.Plasmalevelsofmetoprololmayberaisedbyco-administrationofcompounds

metabolisedbyCYP2D6,e.g.antiarrhythmics,antihistamines,histamine-2-receptorantagonists,

antidepressants,antipsychotics,andCOX-2-inhibitors.Theplasmaconcentrationofmetoprololis

loweredbyrifampicinandmayberaisedbyalcoholandhydralazine.

Aswithotherbeta-blockers,concomitanttherapywithdihydropyridinese.g.nifedipine,mayincrease

theriskofhypotension,andcardiacfailuremayoccurinpatientswithlatentcardiacinsufficiency.

Concomitanttreatmentwithindometacinorotherprostaglandinsynthetaseinhibitingdrugsmay

decreasetheantihypertensiveeffectofbeta-blockers.

Thebeta-blockermaymasksomeofthesymptomsofthyrotoxicosisandofhypoglycaemiaby

inhibitionofsympatheticnervefunctions.Theeffectsofhypoglycaemicagentsmaybeincreased,

particularlybythenon-cardioselectivebeta-blockers.Thedosagesoforalantidiabeticsandalsoof

insulinmayhavetobereadjustedinpatientsreceivingbeta-blockers.Thetachycardiaof

hypoglycaemiamaybemodified.

Asbeta-blockersmayaffecttheperipheralcirculation,careshouldbeexercisedwhendrugswith

similaractivitye.g.ergotaminearegivenconcurrently.

TheeffectsofBetalocandotherantihypertensivedrugsonbloodpressureareusuallyadditive.

Careshouldbetakenwhencombiningwithotherantihypertensivedrugsordrugsthatmightreducebloodpressure,

suchastricyclicantidepressants,barbituratesandphenothiazines.However,combinationsofantihypertensivedrugs

mayoftenbeusedwithbenefitstoimprovecontrolofhypertension.

4.6Pregnancyandlactation

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Betalocshouldnotbeusedinpregnancyornursingmothersunlessthephysicianconsidersthatthe

benefitoutweighsthepossiblehazardtothefoetus/infant.Beta-blockersreduceplacentalperfusion,

whichmayresultinintrauterinefoetaldeath,immatureandprematuredeliveries.

Aswithallbeta-blockers,Betalocmaycauseside-effectsespeciallybradycardiaandhypoglycaemia

inthefoetus,andinthenewbornandbreastfedinfant.

Betalochas,however,beenusedinpregnancyassociatedhypertensionunderclosesupervision,after

20weeksgestation.AlthoughBetaloccrossestheplacentalbarrierandispresentinthecordblood,as

yetnoevidenceoffoetalabnormalitieshasbeenreported.

Lactation

Theamountofmetoprololingestedviabreastmilkshouldnotproducesignificantbeta-blockingeffectsintheneonate

ifthemotheristreatedwiththenormaltherapeuticdoses.

4.7Effectsonabilitytodriveandusemachines

PatientsshouldknowhowtheyreacttoBetalocbeforetheydriveorusemachinesbecauseoccasionallydizzinessor

fatiguemayoccur.

4.8Undesirableeffects

Betalociswelltoleratedandadversereactionshavegenerallybeenmildandreversible.Thefollowing

eventshavebeenreportedasadverseeventsinclinicaltrialsorreportedfromroutineuse.A

relationshiptotreatmentwithmetoprololhasnotalwaysbeenestablished.

Thefollowingdefinitionsoffrequenciesareused:

Verycommon( ≥

10%),common(1-9.9%),uncommon(0.1-0.9%),rare(0.01-0.09%)andveryrare

(<0.01%).

Cardiovascularsystem

Common: Bradycardia,posturaldisorders(veryrarelywith

syncope),coldhandsandfeet,palpitations.

Uncommon: Deteriorationofheartfailuresymptoms,first-degreeheart

block,oedema,pericordialpain.

Rare: Disturbancesofcardiacconduction,cardiacarrhythmias.

Veryrare: Gangreneinpatientswithpre-existingsevereperipheral

circulatorydisorders.

Centralnervoussystem

Verycommon: Fatigue.

Common: Dizziness,headache.

Uncommon: Paraesthesiae,musclecramps.

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Common: Nausea,abdominalpain,diarrhoea,constipation.

Uncommon: Vomiting.

Rare: Drymouth.

Haematologic

Veryrare: Thrombocytopenia.

Hepatic

Rare: Liverfunctiontestabnormalities.

Veryrare: Hepatitis.

Metabolism

Uncommon: Weightgain.

Musculoskeletal

Veryrare: Arthralgia.

Psychiatric

Uncommon: Depression,concentrationimpairment,somnolenceor

insomnia,nightmares.

Rare: Nervousness,anxiety,impotence/sexualdysfunction.

Veryrare: Amnesia/memoryimpairment,confusion,hallucinations.

Respiratory

Common: Dyspnoeaonexertion.

Uncommon: Bronchospasm.

Rare: Rhinitis.

Senseorgans

Rare: Disturbancesofvision,dryand/orirritatedeyes,

conjunctivitis.

Veryrare: Tinnitus,tastedisturbances.

Skin

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skinlesions),increasedsweating.

Rare: Lossofhair.

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4.9Overdose

Symptoms

PoisoningduetoanoverdoseofBetalocmayleadtoseverehypotension,sinusbradycardia,

atrioventricularblock,heartfailure,cardiogenicshock,cardiacarrest,bronchospasm,impairmentof

consciousness,coma,nausea,vomiting,cyanosis,hypoglycaemiaand,occasionally,hyperkalaemia.

Concomitantingestionofalcohol,antihypertensives,quinidineorbarbituratesmayaggravatethe

patient'scondition.

Thefirstmanifestationsusuallyappear20minutesto2hoursafterdrugingestion.

Management

Treatmentshouldincludeclosemonitoringofcardiovascular,respiratoryandrenalfunction,and

bloodglucoseandelectrolytes.Furtherabsorptionmaybepreventedbyinductionofvomiting,gastric

lavageoradministrationofactivatedcharcoalifingestionisrecent.Cardiovascularcomplications

shouldbetreatedsymptomatically.Inthepresenceofseverehypotension,bradycardia,andimpending

heartfailure,administerabeta

-agonistuntilthedesiredeffectisachieved.Whereaselectivebeta

agonistisnotavailable,dopaminemaybeused;oratropinesulphateivmaybeusedinordertoblock

thevagusnerve.Ifasatisfactoryeffectisnotachieved,othersympathomimeticagents(e.g.

noradrenaline[norepinephrine],metaraminol),orinotropicagents(e.g.dobutamine)maybeused.

TemporarypacingmayberequiredforAVblock.Glucagoncanreversetheeffectsofexcessivebeta-

blockade,giveninadoseof1-10mgintravenously.

Intravenousbeta

-stimulantse.g.terbutalinemayberequiredtorelievebronchospasm.

Itshouldbenotedthatthedosagesofdrugs(antidotes)neededtotreatoverdoseofbeta-blockadeare

muchhigherthannormallyrecommendedtherapeuticdosages.Thisisbecausethebeta-receptorsare

occupiedbythebeta-blocker.

Theuseofhaemodialysisorhaemoperfusionmaybeconsidered.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Metoprololisacompetitive-adrenoceptorantagonist.Itactspreferentiallytoinhibit

adrenoceptors(conferringsomecardioselectivity),isdevoidofintrinsicsympathomimeticactivity

(partialagonistactivity)andpossesses-adrenoceptorblockingactivitycomparableinpotencywith

propranolol.

Anegativechronotropiceffectontheheartisaconsistentfeatureofmetoprololadministration.Thus,cardiacoutput

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5.2Pharmacokineticproperties

Metoprololtabletsdissolverapidlywhichresultsinarapidandcompleteabsorptionwitht

within

2hoursandconsistentbioavailabilitydatabetweendifferentstudypopulations.

MetoprololundergoesoxidativemetabolismintheliverprimarilybytheCYP2D6isoenzyme.

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5.3Preclinicalsafetydata

Theacutetoxicityofmetoprololislowtomoderate.Signsoftoxicityarenon-specificanddonot

indicateanytargetorgan.Signsinratsanddogsindicatethatmetoprololcanexertacardiopressive

actionathighplasmaconcentrations.Acutetoxicityafteroraladministrationislowerinrodentsthan

indogs.

Thereisnospecificgeneraltoxicityafterrepeatedadministrationtoratsordogs.Reproductionandmutagenicity

studieshaverevealednoevidenceofadverseeffects.Carcinogenicitystudiesinratsandmicehaveshownnoincreased

incidenceofneoplasmsrelatedtometoprolol.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Microcrystallinecellulose

Lactosemonohydrate

Sodiumstarchglycollate

Colloidalanhydroussilica

Povidone

Magnesiumstearate

6.2Incompatibilities

Notapplicable.

6.3ShelfLife

Theshelf-lifeexpirydateofthisproductshallbethedateshownonthecontainerandouterpackageof

theproductonthemarketinthecountryoforigin.

6.4Specialprecautionsforstorage

Donotstoreabove25°C.

6.5Natureandcontentsofcontainer

PVC/Aluminiumblisterpacks:

100(10x10Blisters)

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerials

derivedfromsuchmedicinalproductandotherhandlingoftheproduct

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7ParallelProductAuthorisationHolder

B&SHealthcare

Unit4

BradfieldRoad

Ruislip

Middlesex

HA40NU

UnitedKingdom

8ParallelProductAuthorisationNumber

PPA1328/20/2

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

DateofFirstAuthorisation:21stDecember2006

10DATEOFREVISIONOFTHETEXT

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