ALLOPURINOL

Main information

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

Documents

Localization

  • Available in:
  • ALLOPURINOL Tablets 100 mg Milligram
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0006/038/001
  • Authorization date:
  • 25-07-1988
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

PartII

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

AllopurinolTablets100mg

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Each tabletcontains100mg ofAllopurinol

Forexcipients, see6.1.

3PHARMACEUTICALFORM

Tablets

Whitebiconvex tabletsabout9.5mmin diameter.Onefaceismarked with‘AP’,abreaklineand‘100’,thereverse

carriestheRoussellogo.

4CLINICALPARTICULARS

4.1TherapeuticIndications

In themanagementofconditionsofexcessbody urate, including gout, neoplasticdiseaseand associated treatment,

enzymedisorderssuch astheLesch–Nyhan Syndrome, renalcalculi, renalfailure, diuretictherapy and psoriasis.

In theprophylaxisand treatmentofcalciumrenallithiasisin patientswith raised serumorurinary uricacid.

4.2Posologyandmethodofadminstration

DOSAGE:

Adults:

Theusualdaily doseis300mg asasingledosewith increments, asindicated by monitoring ofserumand/orurinary

uricacid, to thelevelnecessary foroptimumcontrol, seldomin excessof900mg.Dosagehigherthan 300mg should be

given in divided dosesnotexceeding 300mg atany onetime.

Children:

Theusualdaily doseis10 to 20 mg/kg b.w.

To avoid an acuteattack ofgouty arthritisin theinitialstagesoftreatment, colchicineorotherappropriateagents

should begiven foratleastamonth. When used in neoplasiaallopurinoltherapy should becommenced before

cytotoxics.

In renalinsufficiency, dosagerequirementsmustbereduced ifcreatinineclearanceislessthan 20ml/minute.

CreatinineClearance Dosage

10-20 ml/min 100 to 200mg daily

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Iffrequentrenaldialysisisrequired allopurinol300 to 400mg aftereach dialysismay beused inplaceoftheabove

regimen.

ADMINISTRATION:

Oral

4.3Contraindications

Usein patientshypersensitiveto allopurinol.

Astreatmentforan acuteattack ofgout.Prophylactictherapy may becommenced on subsidenceoftheacute

attack, provided thatanti-inflammatory agentsareconcurrently used.

4.4Special warningsandspecialprecautionsforuse

1.An acuteattackofgoutmay beprecipitated in patientswith xanthinedeposition in tissues.

2.Thedrug should only beused with greatcaution in patientswith renalorhepaticdysfunction.Dosagemay require

adjustmentwith creatinineclearancebetween 20 and 10ml/minute, adoseof100 to 200mg daily issuggested.If

thecreatinineclearanceislessthan 10ml/min thedoseisusually 100mg daily oratlongerintervals.

3.Theremay bepotentialforinteraction between allopurinoland thecoumarin anti-coagulants.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

1.Useofallopurinolconcurrently with 6-mercaptopurineorazathioprinerequiresreduction in dosageofthesedrugs

sincetheinhibition ofxanthineoxidasewillprolong theiractivity.

2.Allopurinolmaybeused concurrently with uricosuricagents, butiftherapy isbeing changed to allopurinol,

overlapping oftreatmentisnecessary to ensurecontinuity ofthehypouricaemiceffect.

4.6Pregnancyandlactation

Allopurinolshould notbeused during pregnancy unlessconsidered essentialby thephysician.No dataisavailableon

excretion ofallopurinoland itsmetabolitesin breastmilk.

4.7Effectsonabilitytodriveandusemachines

Notapplicable.

4.8Undesirableeffects

Adversereactionsin association with AllopurinolTabletsarerarein theoveralltreated population and mostly ofa

minornature.Theincidenceishigherin thepresenceorrenaland/orhepaticdisorder.

Skin and hypersensitivityreactions

Thesearethemostcommon reactionsand may occuratany timeduring treatment.They may bepruritic,

maculopapular, sometimesscaly, sometimespurpuricand rarelyexfoliative.AllopurinolTabletsshould bewithdrawn

immediately should such reactionsoccur.Afterrecovery frommild reactions, AllopurinolTabletsmay, ifdesired, be

re-introduced atasmalldose(e.g. 50mg/day)andgradually increased.Iftherash recurs, AllopurinolTabletsshould be

permanently withdrawn asamoreseverehypersensitivity reaction may occur.Skin reactionsassociated with

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epidermalnecrolysisoccurrarely.Associated vasculitisand tissueresponsemay bemanifested in variousways

including hepatitis, renalimpairmentand, veryrarely, seizures.Ifsuch reactionsdo occur, itmay beatany timeduring

treatment.AllopurinolTabletsshould bewithdrawn immediately and permanently.Corticosteroidsmay bebeneficial

in overcoming hypersensitivity skin reactions.When generalised hypersensitivity reactionshaveoccurred,renaland/or

hepaticdisorderhasusually been presentparticularly when theoutcomehasbeen fatal.

Very rarely acuteanaphylacticshock hasbeen reported.

Angioimmunoblasticlymphadenopathy

Angioimmunoblasticlymphadenopathy hasbeen described rarelyfollowingbiopsy ofageneralisedlymphadenopathy.

Itappearsto bereversibleon withdrawalofAllopurinolTablets.

Hepaticfunction

Rarecasesofhepaticdysfunction ranging fromasymptomaticrisesin liverfunction teststo hepatitis(including hepatic

necrosisand granulomatoushepatitis)havebeen reported withoutovertevidenceofmoregeneralised hypersensitivity.

Gastrointestinaldisorder

In early clinicalstudies, nauseaand vomiting werereported.Furtherreportssuggestthatthisreaction isnota

significantproblemand can beavoided bytaking AllopurinolTabletsaftermeals.Recurrenthaematemesishasbeen

reported asan extremely rareevent, ashassteatorrhoea.

Blood and lymphaticsystem

Occasionalreportshavebeen received ofthrombocytopenia, agranulocytosisand aplasticanaemia, particularly in

individualswith impaired renaland/orhepaticfunction, reinforcing theneed forparticularcarein thisgroupof

patients.

Miscellaneous

Thefollowing complaints, havebeen reported occasionally;fever, generalmalaise, asthenia, headache, vertigo, ataxia,

somnolence, coma, depression, paralysis, paraesthesiae, neuropathy, visualdisorder, cataract, macularchanges, taste

perversion, stomatitis, changed bowelhabit,infertility, impotence, diabetesmellitus, hyperlipaemia, furunculosis,

alopecia, discoloured hair, angina, hypertension, bradycardia, oedema, uraemia, haematuria, angioedema,

gynaecomastia.

4.9Overdose

Ingestion ofup to 22.5g allopurinolwithoutadverseeffecthasbeen reported.Symptomsand signsincluding nausea,

vomiting, diarrhoeaand dizzinesshavebeen reported in apatientwho ingested 20g allopurinol.Recovery followed

generalsupportivemeasures.

Management

Massiveabsorption ofAllopurinolTabletsmay lead to considerableinhibition ofxanthineoxidaseactivity, which

should haveno untoward effectsunlessaffecting concomitantmedication especially with 6-mercaptopurineand/or

azathioprine.Adequatehydration to maintain optimumdiuresisfacilitiesexcretion ofallopurinoland itsmetabolites.

Ifconsidered haemodialysismay beused.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

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5.2Pharmacokineticproperties

Allopurinolisreadily absorbed fromthegutwith ahalf-lifeof1 hour, itisrapidly converted to activemetabolite

oxpurinol(alloxanthine).Neitherallopurinolnoroxypurinolisbound toplasmaprotein and excretion ismainly

urinary.Oxypurinolisreabsorbed by thekidney tubulesto givean effectivehalf-lifeof18-30 hours.

5.3Preclinical safetydata

Noneapplicable

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Lactose

MaizeStarch

Povidone

StearicAcid

6.2Incompatibilities

Notapplicable

6.3ShelfLife

3 years.

6.4Special precautionsforstorage

Storebelow25 o

6.5Natureandcontentsofcontainer

Securitainers.

Allopurinolisavailablein thefollowing pack sizes:21, 100, 250 and 500 tablets.

Notallpack sizesmay bemarketed.

6.6Instructionsforuseandhandling

Notapplicable.

7MARKETINGAUTHORISATIONHOLDER

RousselLaboratoriesLimited

BroadwaterPark

Denham

Uxbridge

Middlesex UB9 5HP

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8MARKETINGAUTHORISATIONNUMBER

PA6/38/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:25 th

July 1988

Dateoflastrenewal:25 th

July 2003

10DATEOFREVISIONOFTHETEXT

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