AVLOCLOR TABLETS 250 MG

Main information

  • Trade name:
  • AVLOCLOR TABLETS 250 MG
  • Dosage:
  • 250 Milligram
  • Pharmaceutical form:
  • Tablets
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • AVLOCLOR TABLETS 250 MG
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0970/029/001
  • Authorization date:
  • 01-04-1997
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

IRISHMEDICINESBOARDACTS1995AND2006

MEDICINALPRODUCTS(CONTROLOFPLACINGONTHEMARKET)REGULATIONS,2007

(S.I.No.540of2007)

PA0970/029/001

CaseNo:2060697

TheIrishMedicinesBoardinexerciseofthepowersconferredonitbytheabovementionedRegulationsherebygrantsto

AstraZenecaUKLimited

600CapabilityGreen,Luton,LU13LU,UnitedKingdom

anauthorisation,subjecttotheprovisionsofthesaidRegulations,inrespectoftheproduct

AvloclorTablets250mg

TheparticularsofwhicharesetoutinPartIandPartIIoftheattachedSchedule.Theauthorisationisalsosubjecttothegeneralconditionsas

maybespecifiedinthesaidRegulationsaslistedonthereverseofthisdocument.

Thisauthorisation,unlesspreviouslyrevoked,shallcontinueinforcefrom30/01/2009.

SignedonbehalfoftheIrishMedicinesBoardthis

________________

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PartII

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

AvloclorTablets250mg

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Eachtabletcontains250mgchloroquinephosphatewhichisequivalentto155mgchloroquinebase.

Forafulllistofexcipientsseesection6.1.

3PHARMACEUTICALFORM

Tablets.

AvloclorTabletsarewhiteincolour,round,biconvexwithabreaklineandoneithersideofthelinean‘A’intagliation

ispresent.Thereversefaceofthetabletisplain.

Thebreaklineisonlytofacilitatebreakingforeaseofswallowingandnottodivideintoequaldoses.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Treatmentofmalaria.

Prophylaxisandsuppressionofmalaria.

Treatmentofamoebichepatitisandabscess.

Treatmentofdiscoidlupuserythematosus.

Treatmentofsystemiclupuserythematosus.

Treatmentofrheumatoidarthritis.

4.2Posologyandmethodofadministration

Thedoseshouldbetakenafterfood.

a) Treatmentofmalaria

i) P.falciparumandP.malariaeinfections

Adults:Theinitialdoseisfourtabletswhichisfollowedbytwotabletssixhoursafterandthentwotabletsadayfor

twodays.

Children:Asingledoseof10mgbase/kg,followedsixhourslaterby5mgbase/kgand5mgbase/kgadayfortwo

days.

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Adults:Theinitialdoseisfourtabletswhichisfollowedbytwotabletssixhourslaterandthentwotabletsadayfor

twodays.Followwithacourseoftreatmentwithprimaquineifaradicalcureisrequired.

Children:Asingledoseof10mgbase/kgfollowedsixhourslaterby5mgbase/kgand5mgbase/kgfortwodays.

Followwithacourseoftreatmentwithprimaquineifaradicalcureisrequired.

b) Prophylaxisandsuppressionofmalaria

Adults:Twotabletstakenonceaweek,onthesamedayeachweek,startingoneweekbeforeexposuretorisk,

continuedduringexposureandforfourweeksafterleavingthemalariousarea.

Children:Asingledoseof5mgchloroquinebase/kgperweek,onthesamedayeachweekstartingoneweekbefore

exposuretorisk,continuedduringexposureandforfourweeksafterleavingthemalariousarea.

Forpracticalpurposes,childrenagedover14yearsmaybetreatedasadults.Thedosegiventoinfantsandchildren

shouldbecalculatedontheirbodyweightandmustnotexceedtheadultdoseregardlessofweight.

Adoseof5mgchloroquinebase/kginchildrencanbeapproximatedfromthetable.

Under1year 1/8adultdose[0.25tablet]

1-4years 1/4adultdose[0.5tablet]

5-8years 1/2adultdose[1tablet]

9-14years 3/4adultdose[1.5tablets]

c) Amoebichepatitis

Adults:Fourtabletsdailyfortwodaysfollowedbyonetablettwicedailyfortwoorthreeweeks.

d) Lupuserythematosus

Adults:Onetablettwicedailyforonetotwoweeksfollowedbyamaintenancedosageofonetabletdaily.

e) Rheumatoidarthritis

Adults:Theusualdosageisonetabletdaily.

Elderlypatients:Therearenospecialdosagerecommendationsfortheelderly,butitmaybeadvisabletomonitor

elderlypatientssothatoptimumdosagecanbeindividuallydetermined.

4.3Contraindications

TherearenoknownabsolutecontraindicationstotheuseofAvloclor.

4.4Specialwarningsandprecautionsforuse

Inanylocalitywheredrugresistantmalariaisknownorsuspected,itisessentialtotakeprofessionaladviceonwhat

prophylacticregimenortreatmentregimenisappropriate.

CautionisnecessarywhengivingAvloclortopatientswithimpairedhepaticfunction,particularlywhenassociated

withcirrhosis.Cautionisalsonecessaryinpatientswithporphyria.Avloclormayprecipitatesevereconstitutional

symptomsincludingabdominalandneuropsychiatricdisturbances,hepaticimpairmentandphotosensitivity.Avloclor

mayalsocauseanincreaseintheamountofporphyrinsexcretedintheurineespeciallyinpatientswithhighalcohol

intake.

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Avloclorshouldbeusedwithcareinpatientswithahistoryofepilepsy.Potentialrisksandbenefitsshouldbecarefully

evaluatedbeforeuseinsubjectstakinganti-convulsanttherapyorwithahistoryofepilepsyas,rarely,casesof

convulsionshavebeenreportedinassociationwithchloroquine.

ConsiderablecautionisneededintheuseofAvloclorforlong-termhighdosagetherapyandsuchuseshouldonlybe

consideredwhennootherdrugisavailable.

Prolongedtherapywithhighdosesmayleadtooccasionaldevelopmentofirreversibleretinaldamage.

PatientsreceivingAvloclorcontinuouslyathigherdoselevelsforperiodslongerthan12monthsshouldundergo

ophthalmicexaminationbeforetreatmentandatthreemonthlyintervals.Thisalsoappliestopatientsreceiving

Avlocloratweeklyintervalsforaperiodofmorethan3yearsorifthetotalconsumptionisexpectedtoexceed1.6g/kg.

Fullbloodcountsshouldbecarriedoutregularlyduringextendedtreatmentasbonemarrowsuppressionmayoccur

rarely.

TheuseofAvloclorinpatientswithpsoriasismayprecipitateasevereattackofpsoriasis.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Chloroquinemaypotentiatetheneuromuscularblockingeffectsofaminoglycosidesorotherneuromuscularblocking

drugs.

Ifthepatientistakingciclosporinthenchloroquinemaycauseanincreaseinciclosporinlevels.

Whenrabiesvaccineisinjectedintotheskinchloroquinemayreduceitseffectiveness.

Chloroquinesignificantlyreduceslevelsofpraziquantel.Cautionisthereforeadvisedduringco-administration.

Prescribersmayconsiderincreasingthedoseofpraziquantelifthepatientdoesnotrespondtotheinitialdose.

CautionisnecessarywhenAvloclorisadministeredwithknownhepatotoxicdrugs.

Antacids(aluminium,calciumandmagnesiumsalts)andadsorbents(egkaolin)mayreducetheabsorptionof

chloroquine,soshouldbetakenwellseparatedfromAvloclor(atleastfourhoursapart).

4.6Pregnancyandlactation

Pregnancy:Malariainpregnantwomenincreasestheriskofmaternaldeath,miscarriage,still-birthandlowbirth

weightwiththeassociatedriskofneonataldeath.Malarialprophylaxisisthereforestronglyadvisedinpregnantwomen

atriskofcatchingmalaria.ItisthereforeacceptabletotaketherecommendeddosageofAvloclorduringallstagesof

pregnancy.Medicaladviceshouldbesoughtbysubjectsduringthefirsttrimester.

ThereisevidencetosuggestthatAvloclorgiventowomeninhighdosesthroughoutpregnancycangiverisetofoetal

abnormalitiesincludingocularorcochleardamage.

Lactation:AlthoughAvloclorisexcretedinbreastmilk,theamountisinsufficienttoconferanybenefitontheinfant.

Separatechemoprophylaxisfortheinfantisrequired.

4.7Effectsonabilitytodriveandusemachines

DefectsinvisualaccommodationmayoccuronfirsttakingAvloclorandpatientsshouldbewarnedregardingdriving

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4.8Undesirableeffects

Theadversereactionswhichmayoccuratdosesusedintheprophylaxisortreatmentofmalariaaregenerallynotofa

seriousnature.Whereprolongedhighdosageisrequired,i.e.inthetreatmentofrheumatoidarthritis,adversereactions

canbeofamoreseriousnature.

Adversereactionsreportedafter‘Avloclor’useare:

Headache

Gastro-intestinaldisturbances

Skineruptions

Pruritus

Exfoliativedermatitis,

Photosensitivity

Ototoxicity

Slate-greypigmentationofthenailsandmucosae

Occasionaldepigmentationorlossofhair

Difficultyinaccommodation

Blurringofvision

Cornealopacities

Retinaldegeneration

Electrocardiographicchanges

Neurologicalandpsychiatricchanges,includingconvulsionsandpsychosis

Thrombocytopenia

Agranulocytosis

Aplasticanaemia

Allergicreactions-manifestedasanaphylacticreactions,urticaria,angioedemaandvasculitis

Toxicepidermalnecrolysis

Erythemamultiforme

Stevens-Johnsonsyndrome

Cardiomyopathy

Neuromyopathy

Myopathy

Proteinuria

4.9Overdose

Chloroquineishighlytoxicinoverdoseandchildrenareparticularlysusceptible.Thechiefsymptomsofoverdosage

includecirculatorycollapseduetoapotentcardiotoxiceffect,respiratoryarrestandcoma.Overdosemayleadto

multiorganfailureincludingliverfailure,pancreatitisandrhabdomyolysis.Symptomsmayprogressrapidlyafter

initialnauseaandvomiting.Cardiaccomplicationsmayoccurwithoutprogressivelydeepeningcoma.

Deathmayresultfromcirculatoryorrespiratoryfailureorcardiacdysrhythmia.Ifthereisnodemonstrablecardiac

outputduetodysrhythmias,asystoleorelectromechanicaldissociation,externalchestcompressionshouldbepersisted

withforaslongasnecessary,oruntiladrenaline(epinephrine)anddiazepamcanbegiven(seebelow).

Gastriclavageshouldbecarriedouturgently,firstprotectingtheairwayandconstitutingartificialventilationwhere

necessary.Thereisariskofcardiacarrestfollowingaspirationofgastriccontentsinmoreseriouscases.Activated

charcoalleftinthestomachmayreduceabsorptionofanyremainingchloroquinefromthegut.

Circulatorystatus(withcentralvenouspressuremeasurement),respiration,plasmaelectrolytesandbloodgasesshould

bemonitored,withcorrectionofhypokalaemiaandacidosisifindicated.Cardiacdysrhythmiasshouldnotbetreated

unlesslifethreatening;drugswithquinidine-likeeffectsshouldbeavoided.Intravenoussodiumbicarbonate1-

2mmol/kgover15minutesmaybeeffectiveinconductiondisturbances,andDCshockisindicatedforventricular

tachycardiaandventricularfibrillation.

Earlyadministrationofthefollowinghasbeenshowntoimprovesurvivalincasesofseriouspoisoning:

Adrenaline(epinephrine)infusion0.25micrograms/kg/mininitially,withincrementsof0.25

micrograms/kg/minuntiladequatesystolicbloodpressure(morethan100mmHg)isrestored;adrenaline

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Diazepaminfusion(2mg/kgover30minutesasaloadingdose,followedby1-2mg/kg/dayforupto

2-4days).Diazepammayminimisecardiotoxicity.Acidificationoftheurine,haemodialysis,peritoneal

dialysisorexchangetransfusionhavenotbeenshowntobeofvalueintreatingchloroquinepoisoning.

Chloroquineisexcretedveryslowly,thereforesymptomaticcasesmeritobservationforseveraldays.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Avloclorisananti-malarialdrugofthe4-aminoquinolinegroup.

Themodeofactionofchloroquineonplasmodiahasnotbeenfullyelucidated.Chloroquinebindstoandaltersthe

propertiesofDNA.ChloroquinealsobindstoferriprotoporphyrinIXandthismayleadtolysisoftheplasmodial

membrane.

Insuppressivetreatment,chloroquineinhibitstheerythrocyticstageofdevelopmentofplasmodia.Inacuteattacksof

malaria,itinterruptserythrocyticschizogonyoftheparasite.Itsabilitytoconcentrateinparasitisederythrocytesmay

accountfortheselectivetoxicityagainsttheerythrocyticstagesofplasmodialinfection.

5.2Pharmacokineticproperties

Studiesinvolunteersusingsingledosesofchloroquinephosphateequivalentto300mgbasehavefoundpeakplasma

levelstobeachievedwithinonetosixhours.Theselevelsareintheregionof54-102microgram/litre,the

concentrationinwholebloodbeingsome4to10timeshigher.Theeliminationhalf-lifeofchloroquineisdose

dependentandisapproximatelyonehundredhours.Followingasingledose,chloroquinemaybedetectedinplasma

formorethanfourweeks.Meanbioavailabilityfromtabletsofchloroquinephosphateis89%.Chloroquineiswidely

distributedinbodytissuessuchastheeyes,kidneys,liverandlungswhereretentionisprolonged.Theeliminationof

chloroquineisslow,withamultiexponentialdeclineinplasmaconcentration.Theinitialdistributionphasehasahalf-

lifeof2–6dayswhiletheterminaleliminationphaseis10-60days.Approximately50-70%ofchloroquineinplasma

isboundtotheplasmaproteins.

Theprincipalmetaboliteismonodesethylchloroquine,whichreachesapeakconcentrationof10-20microgram/litre

withinafewhours.Meanurinaryrecovery,within3-13weeks,isapproximately50%oftheadministereddose,most

beingunchangeddrugandtheremainderasmetabolite.Chloroquinemaybedetectedinurineforseveralmonths.

5.3Preclinicalsafetydata

Avloclorhasbeenwidelyusedformanyyearsinclinicalpractice.Thereisnoanimaldatawhichaddssignificant

informationrelevanttotheprescriber,tothatcoveredelsewhereinthisdocument.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

MagnesiumStearate

MaizeStarch

6.2Incompatibilities

Notapplicable.

6.3ShelfLife

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6.4Specialprecautionsforstorage

Donotstoreabove30°C.Storeintheoriginalpackageinordertoprotectfromlightandmoisture.

6.5Natureandcontentsofcontainer

PVC/AluminiumFoilBlisterPackof20Tablets.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements.

7MARKETINGAUTHORISATIONHOLDER

AstraZenecaUKLimited

600CapabilityGreen

LutonLU13LU

UnitedKingdom

8MARKETINGAUTHORISATIONNUMBER

PA970/29/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:1 st

April1977

Dateoflastrenewal: 1 st

April2007

10DATEOFREVISIONOFTHETEXT

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