AMOLIN

Main information

  • Trade name:
  • AMOLIN Tablets 50 mg Milligram
  • Dosage:
  • 50 mg Milligram
  • Pharmaceutical form:
  • Tablets
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • AMOLIN Tablets 50 mg Milligram
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0593/004/002
  • Authorization date:
  • 16-05-1994
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Amolin50mgTablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Eachtabletcontains50mgatenolol.

Eachtabletalsocontains30.90mglactosemonohydrate

Forafulllistofexcipients,seesection6.1

3PHARMACEUTICALFORM

Tablets

White,round,biconvexscoredtabletwithinscriptionontheupperside:“C24”.

Thescorelineallowsthetablettobedividedintoequalhalves.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Managementofhypertension

Managementofanginapectoris

Managementofcardiacdysrhythmias

Myocardialinfarction:earlyinterventionintheacutephase.

4.2Posologyandmethodofadministration

Thedosageshouldbeindividuallydetermined,basedmainlyonthepulserateorthetherapeuticaleffectiveness.Itis

advisabletostartthetherapywiththelowestpossibledosageinordertobeabletoidentifycardiacdecompensationor

bronchialphenomenaatanearlystage;thisisespeciallyimportantintheelderly.WithAmolinastepwiseincreaseup

tothefullyeffectivedoseispossible.Subsequentincreasesindoseshouldtakeplaceslowly(e.g.onceaweek)under

controloronthebasisofclinicaleffect.

Adults

Hypertension:

Whilesomepatientswillrespondtoasingledailydoseof50mg,theusualdailydosageis100mgasasingledose.

Theeffectwillbefullyestablishedafteronetotwoweeks.Afurtherreductioninbloodpressuremaybeachievedby

combiningAmolinwithotherantihypertensiveagents,e.g.adiuretic.

Anginapectoris:

Theusualdailydoseis100mggivenoncedailyor50mgtwicedaily.Itisunlikelythatadditionalbenefitwillbe

gainedbyincreasingthedose.

Dysrhythmias:

Followingcontrolofthedysrhythmiawithintravenousatenolol,asuitableoralmaintenancedosageis50–100mg

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Acutemyocardialinfarction:

Forsuitablepatientspresentingwithin12hoursoftheonsetofthechestpain,atenolol5-10mgshouldbegivenby

slowintravenousinjection(1mg/ml)followedbyatenolol50mgorallyabout15minutesaftertheintravenousinjection

providednountowardeffectsoccurfromtheintravenousdose.Thisshouldbefollowedby50mgorally12hoursafter

theintravenousdoseandthen12hourslaterby100mgorallytobegivenoncedaily.

Amolin50mgTabletsmustbediscontinuedimmediatelyintheeventofheartrateand/orbloodpressurefallsorany

othercomplicationsrequiringtherapeuticintervention.

Children:

Thereisnopaediatricexperiencewithatenololandforthisreasonitisnotrecommendedforuseinchildren.

Elderly:

Dosagemayneedtobereducedespeciallyinpatientswithimpairedrenalfunction.

Renalfailure:

Patientswithrenaldysfunctionneedtohavetheiratenololdoseadjustedtorenalclearanceofthedrug.Nosignificant

accumulationofatenololoccursinpatientswhohaveacreatinineclearancegreaterthan35ml/min.Ifthecreatinine

clearanceisdecreasedto15-35ml/min(equivalenttoserumcreatinine<3-6mg/dl)theoraldoseshouldbe50mg

daily.Forpatientswithacreatinineclearance<15ml/min(equivalenttoserumcreatinine>6mg/dl)theoraldose

shouldbe25mgdailyor50mgonalternatedays.Patientsonhaemodialysisshouldbegiven50mgorallyaftereach

dialysis,thisshouldbedoneunderhospitalsupervisionasmarkedfallsinbloodpressurecanoccur.

Typeanddurationofadministration

Thetabletsshouldbeingestedwholewithsomeliquidbeforemeals.

4.3Contraindications

Amolin50mgiscontraindicatedinpatientswith:

Overtheartfailure

Shock

SecondandthirddegreeAVblock

Sicksinussyndrome

SAblock

Bradycardia(heartrateatrest<50beats/minutebeforetherapy)

Hypotension(systolicbloodpressure<90mmHg)

MetabolicAcidosis

Bronchialhyperreactivity(e.g.inbronchialasthma)

Advancedstagesofperipheralarterialocclusivedisease

ConcurrentMAOinhibitortherapy(exceptMAO-Binhibitor)

Hypersensitivitytoatenololorotherbeta-adrenergicreceptorblockingagents

Intravenousverapamil-typeordiltiazem-typecalciumantagonistsandotherintravenousanti-arrhythmics(suchas

disopyramide)arecontra-indictedinpatientsonatenololtherapy(exceptinanintensivecaresetting).

4.4Specialwarningsandprecautionsforuse

IfAmolin50mgtherapyistobeinterruptedordiscontinuedafterprolongeduse,thisshouldalwaysbedoneby

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anginapectorisortomyocardialinfarction,ormaycauseexacerbationofhypertension.

Particularlyclosemedicalmonitoringisrequiredinpatientswith:

Patientswithfirst-degreeAVblock

Diabeticswithhighlyunstablebloodglucoseconcentrations

(becauseoftheriskofseverehypoglycemicepisodes).

Patientsfollowinganabsolutedietforprolongedperiodsoftimeandthosesubjecttogreatphysicalexertion

(becauseoftheriskofseverehypoglycaemicepisodes)

Patientswithpheochromocytoma(tumouroftheadrenalmedulla:prioralpha-blockertherapyisindicated)

Patientswithimpairedkidneyfunction

Beta-receptorblockingdrugsshouldbeusedonlyaftercarefullyweighingexpectedbenefitsagainstpotentialrisksin

patientswithahistoryorfamilyhistoryofpsoriasis.

Betareceptorblockingdrugsmayincreasesusceptibilitytoallergensandtheseverityofanaphylacticreactions.Beta-

receptorblockingdrugsshouldthereforebeusedonlyifclearlyneededinpatientswithahistoryofsevere

hypersensitivityreactionsandthosereceivingspecifichyposensitisationtherapy(becauseoftheriskofexaggerated

anaphylacticreactions).

Patientswithrarehereditaryproblemsofgalactoseintolerance,theLapplactasedeficiencyorglucose-galactose

malabsorptionshouldnottakethismedicine.

SpecialLabellingRequirement:

Donottakethismedicinewithoutconsultingyourdoctorifyouhaveahistoryofwheezingorasthma.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

IncaseofaconcomitantuseofAmolinandotherdrugsthefollowinginteractionsshouldbetakenintoconsideration.

Notrecommendedassociation

Calciumantagonistsoftheverapamilordiltiazemtype:

negativeinfluenceoncontractilityandauriculo-ventricularconduction.Neitherdrugshouldbeadministeredintravenously

within48hoursofdiscontinuingtheother.

Clonidine:

increasestheriskof"reboundhypertension".

UponabruptwithdrawalofclonidinewhileAmolinisgivenconcurrently,theremaybeanexaggeratedincreaseinblood

pressure.ClonidinemustthereforenotbediscontinuedunlessAmolintherapyhasbeenstoppedseveraldayspreviously.

Onlythencanclonidinebewithdrawngradually.

Precautionsforuse

ClassIantiarrhythmicdrugs(e.g.disopyramide,quinidine)andamiodarone:

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Insulinororalantidiabetic:

mayintensifythebloodsugarloweringeffect.Beta-adrenergicblockademaypreventtheappearanceofsignsof

hypoglycaemia(tachycardia).Regularbloodsugardeterminationsarethereforenecessary.

Anaesthetics,peripheralmusclerelaxants:

Anaestheticsmayattenuatethereflextachycardiaandincreasetheriskofhypotension.Continuationofbeta-blockades

reducetheriskofarrhythmiaduringinductionandintubation.Anaestheticdrugscausingmyocardialdepression,suchas

cyclopropaneandtrichlorethylene,arebestavoided.

Neuromuscularblockadeinducedbyperipheralmusclerelaxants(e.g.succinylcholine,tubocurarine)maybeenhancedby

beta-adrenergicreceptorblockadeofatenolol.

Ifatenololcannotbediscontinuedbeforeasurgicalprocedureundergeneralanaesthesiaorpriortotheuseofperipheral

musclerelaxant,theanaesthetist/anaesthesiologistmustbeinformedaboutatenololtherapybeforehand.

Takeintoaccount

Calciumantagonist:dihydropyridinederivativessuchasnifedipine:

theriskofhypotensionmaybeincreased.Inpatientswithlatentcardiacinsufficiency,treatmentwithbeta-blockingagents

mayleadtocardiacfailure.

Indomethacin:

maydecreasethehypotensiveeffectofatenolol.

Norepinephrineorepinephrine:

maycounteracttheeffectofbeta-adrenergicblockingagents.

Tricyclicantidepressants,barbituratesorphenothiazines,ordiuretics,vasodilatorsorotherantihypertensivedrugs:

mayincreasethebloodpressureloweringeffect.

4.6Fertility,pregnancyandlactation

Atenololcrossestheplacentalbarrierandappearsinthecordblood.Nostudieshavebeenperformedontheuseof

Atenololinthefirsttrimesterandthepossibilityoffoetalinjurycannotbeexcluded.Atenololhasbeenusedunder

closesupervisionforthetreatmentofhypertensioninthethirdtrimester.AdministrationofAtenololtopregnant

womeninthemanagementofmildtomoderatehypertensionhasbeenassociatedwiththeintra-uterinegrowth

retardation.TheuseofAtenololinwomenwhoare,ormaybecome,pregnantrequiresthattheanticipatedbenefitbe

weighedagainstthepossiblerisks,particularlyinthefirstandsecondtrimesters.

ThereissignificantaccumulationofAtenololinbreastmilk.

NeonatesborntomotherswhoarereceivingAtenololatparturitionorbreast-feedingmaybeatriskforhypoglycemia.

CautionshouldbeexercisedwhenAtenololisadministeredduringpregnancyortoawomanwhoisbreast-feeding.

4.7Effectsonabilitytodriveandusemachines

Sincethereareonlyrarereportsofbeta-blockerscausingsymptomatichypotensionandbradycardia,theuseofAmolin

isunlikelytoresultinanyimpairmentoftheabilityofpatientstodriveoroperatemachinery.

4.8Undesirableeffects

Inthissectionundesirableeffectsaredefinedasfollows:

Verycommon(>1/10),common(>1/100-<1/10),uncommon(>=1/1,000-<1/100),rare(>=1/10,000-<1/1,000),very

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Immunesystemdisorders

Common:Allergicskinreactions(erythema,pruritus,exanthema).

Endocrinedisorders

Inpatientswithhyperthyroidism,theclinicalsignsofthyrotoxicosis(e.g.tachycardia,tremor)maybemaskedduring

atenololtherapy.

Metabolismandnutritiondisorders

Uncommon:Latentdiabetesmellitusbecomingmanifestormanifestdiabetesmellitusbecomingworse.

Patientsfollowinganabsolutedietforprolongedperiodsoftimeandthosesubjecttogreatphysicalexertionmay

experiencehypoglycaemicepisodeswhenusingatenololatthesametime.Thewarningsignsofhypoglycaemia

(tachycardiaandtremorinparticular)maybemasked.

Atenololtherapymaybeassociatedwithlipidmetabolismdisruptions.Whiletotalcholesterolwasusuallynormal,HDL

cholesterolwasreducedandplasmatriglycerideswereelevated.

Nervoussystemdisorders

Common:disturbancesofthecentralnervoussystemsuchasfatigue,dizziness,headache,visualdisturbances,sweating,

drowsiness,confusion,hallucinations,psychosis,nightmaresorincreaseddreamactivity,sleepdisturbancesanddepressive

disorders(especiallyatthestartoftherapy);paresthesias;coldsensationsintheextremities.

Eyedisorders

Common:Conjunctivitis;reducedlacrimation(thisshouldbeborneinmindbypatientswearingcontactlenses).

Cardiacandvasculardisorders

Common:Excessivehypotension,bradycardia,syncope,atrioventricularconductiondisturbancesorexacerbationof

cardiacinsufficiency.

Inpatientswithanginapectoris,worseningofanginalattackscannotberuledouttooccurinisolatedinstances.

Therehavebeenreportsofworseningcomplaintsinpatientswithperipheralarterialocclusivedisease(includingthose

withRaynaud’ssyndrome).

Respiratory,thoracicandmediastinaldisorders

Patientswithbronchospasticdisease(especiallythosewithobstructiveairwaydisease)mayexperiencebreathlessness

becausethisdrugmayincreaseairwayresistance.

Gastrointestinaldisorders

Common:Transientgastro-intestinalsymptoms(nausea,vomiting,constipation,diarrhoea).

Uncommon:Drymouth.

Skinandsubcutaneoustissuedisorders

Veryrare(incl.Isolatedreports):Beta-receptorblockingdrugsmayprecipitateorworsenpsoriasisorproduce

psoriasiformskineruptions.

Musculoskeletalandconnectivetissuedisorders

Uncommon:Muscleweakness,musclecramps.

Reproductivesystemandbreastdisorders

Veryrare(incl.isolatedreports):Reducedlibido,impotence.

Precautionarynotes

Aspatientswithpre-existingsevererenalinsufficiencyhave,inisolatedinstances,experienceddeteriorationofkidney

functionduringtreatmentwithotherbeta-receptorblockingdrugs,atenololtherapyshouldbeaccompaniedby

appropriatekidneyfunctionmonitoring.

Reportsofelevatedliverenzymeshavebeennotedwiththeuseofatenololbuttheyarerare.Otherbeta-blockingdrugs

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Asotherbetareceptorblockingdrugshavebeenassociatedwiththrombocytopenicornon-thrombocytopenicpurpura,

patientsonatenololtherapyshouldbewatchedforsignsofpurpura.

4.9Overdose

Symptomsofanoverdose

Dependingontheextentofintoxication,theclinicalpicturetypicallyincludescardiovascularandCNSsymptoms.

Overdosagemaycausehypotension,bradycardia,acutecardiacinsufficiency,andcardiogenicshock.Additionalsignsand

symptomsmayincludedifficultybreathing,bronchospasm,vomiting,disturbedconsciousness,aswellasgeneralized

convulsionsintheoccasionalpatient.

Managementofanoverdose

Intheeventofanoverdoseoralife-threateningfallintheheartrateand/orbloodpressure,Amolin50mgtherapymustbe

discontinued.

Apartfromgeneralmeasures(primarydetoxificationbygastriclavage,administrationofactivatedcharcoalandalaxative),

thevitalsignsmustbemonitoredand,ifnecessary,treatedinanintensivecareward.

Thefollowingagentsmaybeusefulantidotes:

Atropine:0.5-2mgintravenouslyasbolus,

Glucagon:initially8-10mgintravenously,afterwards1-3mgperhourasprolongedinfusion

-sympathomimetics,dependingonbodyweightandeffect:Dobutamine,isoprenaline,orciprenalineoradrenaline.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Atenololisahydrophilicrelativelybeta1-selective(i.e.,"cardioselective")beta-adrenergicreceptorblockingagentwithout

intrinsicsympathomimeticactivity(ISA)andwithoutamembrane-stabilizingeffect.

Atenolollowerstheheartrate,myocardialcontractility,AVconductionvelocity,andplasmareninactivityasafunctionof

sympathetictone.Atenololmayincreasesmoothmuscletonebyinhibitingbeta2-receptors.

5.2Pharmacokineticproperties

Orallyadministeredatenololisapprox.50%absorbedoutofthegastro-intestinaltract.Becausethereisno"first-pass

effect",thesystemicavailabilityisapprox.50%aswell.Amaximalplasmacountisreachedin2-4hours.Theplasma

proteinboundfractionisapproximately3%;relativevolumeofdistribution:0.7l/kg.Atenololismetabolizedinminimal

amounts.Noactivemetaboliteswithclinicalrelevancearise.Within48hours,approximately90%ofthesystemic

availableatenololiseliminatedbythekidneysunchanged.Thehalflifeoftheeliminationis6-10hours.Inend-stagerenal

failurepatients,theeliminationhalf-lifemaybeaslongas140hours.

Bioavailability

Amolin50mg:

Thebioavailability(AUC

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5.3Preclinicalsafetydata

Acutetoxicity

Seepoint4.9overdosage(symptoms,emergencymeasures,antidote).

Chronictoxicity

RatsanddogswhichweregivenAtenololinvariousdosagesoverlongerperiodsoftime(3-12months)showedno

significantbiochemical,morphologicalorhaematologicalchanges.Whenthedosagewasveryhigh,weightgainsinthe

heartandspleenwereobserved.

Tumorigenicandmutagenicpotential

Tumorigenicity:

Long-termstudiesinratsandmiceyieldednoevidenceofatumorigenicpotentialofatenolol.

Mutagenicity:

Atenololhasnotbeenstudiedextensivelyinmutagenicitytests.However,bothinvitroandinvivotestsconductedtodate

havegivenclearlynegativeresults.

Reproductiontoxicology

TheembryotoxicpotentialofAtenololhasbeenexaminedontwotypesofanimals(ratsandrabbits).Embryoabsorption

wasobservedwhenthedoseswerebelowthematernaltoxicrange.Malformationswerenotobserved.Adetrimentaleffect

onfertilityhasnotbeendetermined.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Maizestarch

Pregelatinisedmaizestarch

Lactosemonohydrate

Povidone

Sodiumlaurilsulfate

Colloidalanhydroussilica

Magnesiumstearate

6.2Incompatibilities

Notapplicable.

6.3Shelflife

5years.

Themedicationshouldnotbeusedaftertheprintedexpirationdate.

6.4Specialprecautionsforstorage

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6.5Natureandcontentsofcontainer

BlisterpacksconsistingofaluminiumfoilandPVC/PVDCfilm.Blistersarepacked,alongwithapackageleaflet,ina

foldedcardboardbox.

Packsizes:20,30,50and100tablets

Notallpacksizesmaybemarketed.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements.

7MARKETINGAUTHORISATIONHOLDER

StadaArzneimittelAG

Stadastrae2-18

D-61118BadVilbel

Germany

8MARKETINGAUTHORISATIONNUMBER

PA593/4/2

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorization:16 th

May1994

Dateoflastrenewal:16 th

May2009

10DATEOFREVISIONOFTHETEXT

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