ASACOLON 400 Milligram Tablets Gastro-Resistant

Ireland - English - HPRA (Health Products Regulatory Authority)

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Active ingredient:
MESALAZINE
Available from:
Tillotts Pharma Limited
INN (International Name):
MESALAZINE
Dosage:
400 Milligram
Pharmaceutical form:
Tablets Gastro-Resistant
Prescription type:
Product subject to prescription which may be renewed (B)
Authorization status:
Authorised
Authorization number:
PA1204/001/002
Authorization date:
0000-00-00

PACKAGE LEAFLET: INFORMATION FOR THE USER

Asacolon 400 mg and800 mgGastro-resistant Tablets

Active substance: mesalazine

Read all of this leaflet carefully before you start taking this medicine.

Keep this leaflet. You may need to read it again.

Ifyou have any further questions, please ask your doctor or pharmacist.

This medicine has been prescribed for you. Do not pass it on to others. It mayharm

them, even if their symptoms are the same as yours.

If any ofthe side effects gets serious, or if younotice anyside effects not listed in this

leaflet, please tell your doctor or pharmacist.

In this leaflet:

1.WhatAsacolonis and what it is used for

2.Before you takeAsacolon

3.How to takeAsacolon

4.Possible side-effects

5.How to storeAsacolon

6.Further Information

1.WhatAsacolonisandwhatitisusedfor

ThenameofyourmedicineisAsacolon400mgGastro-resistantTablets/Asacolon800mg

Gastro-resistantTablets.Thetabletsarecalledgastro-resistanttabletsbecausetheyare

coveredwithacoatingwhichallowsthetabletstopassthroughthestomachwithout

dissolving.Thetabletcoatingwillbreakdowninthebowelwheretheactivemesalazineis

released.

AsacolonGastro-resistantTabletscontaintheactivesubstancemesalazine.Thisisananti-

inflammatorymedicineusedtotreatulcerativecolitisandtopreventfurtherepisodesof

Crohn’s disease.

Ulcerativecolitisisadiseaseinwhichtheliningofthelargebowel(colon)orbackpassage

(rectum)becomesinflamed(redandswollen).Asacolonactslocallyattheinflamedsitesto

reduce the inflammation. It can also be used to prevent further attacks of ulcerative colitis.

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becomesinflamed.IfyouhavebeentreatedbysurgeryforCrohn’sdiseaseanditisunder

control, Asacolon act to prevent further episodes of Crohn’s disease.

2.BeforeyoutakeAsacolon

DO NOTtakeAsacolon

Ifyouareallergic(hypersensitive)tomesalazineoranyoftheotheringredientsof

Asacolontablets.

Ifyou have a historyofallergy to salicylates.

Ifyou have kidney problems.

Ifyou have severe liver problems.

Ifyou have ulcers of the stomach and the part of the gut following the stomach.

This medicine should not be provided to children under the age of 2 years.

Take special care withAsacolon

Please tell your doctor if you have any medical conditions or illnesses, particularly:

Ifyou have ever had anyproblems withyourliver orkidneys.

Thisisespeciallyimportantifyouareelderly.WhenyoustarttakingAsacolon,your

doctor may test your blood regularlyto check that yourliver andkidneys work properly.

Ifyouhaveanylungproblems,e.g.asthma,yourdoctormaywanttocheckyourbreathingfrom

time to time.

-If you have ever had problems of sensitivity to sulphasalazine, another medicine used to treat

ulcerative colitis and Crohn’s ileo-colitis.

Veryrarely,seriousbloodproblemshavebeenreportedwiththeuseofthismedicine.

YourdoctormayperformregularbloodtestswhenyouaretakingAsacolontocheck

that your blood counts(thenumber ofcellsin theblood)are normal.Furtherblood tests

will be necessaryif signs of changes in the blood develop.These signsinclude:

unexplained bleeding

easybruising (haematomas)

purplespots or patches (purpura)

persistent fever

sore throat.

Ifany of thesesigns develop, you should stop taking Asacolon immediately and tell your

doctor.

Taking other medicines

Pleasetellyourdoctororpharmacistifyouaretakingorhaverecentlytakenanyother

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Examples of drugs that may affect, or be affected by, Asacolon are:

Drugs that reduce inflammation or pain (pain killers)

Drugsthatreducetheactivityoftheimmunesystem(e.g.azathioprine,or6-

mercaptopurine, or thioguanine)

Anti-cancer drugs(e.g. methotrexate)

Drugs that prevent the formation of blood clots (anticoagulants,e.g. warfarin).

TakingAsacolonwith food and drink

Asacolonshouldbetakenwithaglassofwateronehourbeforeameal.BecauseAsacolon

worksinsidethebowel, thetimeatwhichyoutakeyourmedicinewithrespect toyourmeals

isimportant.

Childrenand adolescents

Asacolonis only recommended for use in children6 years and older.

Pregnancy and breast-feeding

You should tell your doctor,ifyou

arepregnant

think you could be pregnant

plan to become pregnant

arebreast-feeding.

Your doctor will decide if you should use Asacolon.

Ask your doctor or pharmacist for advice before taking anymedicine.

Driving and using machines

Asacolondoes not affect your abilityto drive or use machinery.

ImportantinformationaboutsomeoftheingredientsofAsacolonGastro-resistant

Tablets

AsacolonGastro-resistantTabletscontainmilksugar(lactose).Ifyouhaveintoleranceto

certain sugars, tell your doctor before taking this medicine.

3. HowtotakeAsacolon

Instruction for proper use

Yourdoctormaytellyoutotakethetabletsatdifferenttimes,e.g.morning,middayor

evening.

Asacolonshould be taken one hour before a meal.Because it works inside the bowel, the time

at which you take your medicine withrespect to your meals is important.

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Therehavebeenafewreports ofintact tabletsinstool.Whatappearto beintacttabletsmay

sometimesbetheremainsofthetabletcoating.Ifyou oftenobservetabletsor tabletshellsin

the stool, you should consult your doctor .

Dosage

AlwaystakeAsacolonexactlyasyourdoctorhastoldyou.Youshouldcheckwithyour

doctor or pharmacist if you are not sure.

Yourdoctorwillestablishanappropriatedoseforyouindividuallyaccordingtoyour

condition.Themaximumdailydoseis4800mgindivideddoses.Yourdoctorwilltellyou

how manytablets you should take and how often. Do not take more than6x 800 mg tabletsor

12x 400 mg tabletsper day.

The usual dose for adultsis:

To treat ulcerative colitis:

2400mgmesalazineperdayindivideddoses.Ifrequiredthiscanbeincreasedto4800mg

per day.

To prevent an episode of ulcerative colitis:

1200–2400 mg mesalazine per day,once dailyorin divided doses.

To prevent an episode of Crohn’s disease:

2400 mg per day,once daily orin divided doses.

These can be taken as various combinations of tablets, for example:

1200 mg = 3 x 400 mg tablets

1600 mg = 4 x 400 mg tablets or 2 x 800 mg tablets

2400 mg = 6 x 400 mg tablets or 3 x 800 mg tablets

4000 mg = 10 x 400 mg tablets or5 x 800 mg tablets

4800 mg = 12 x 400 mg tablets or 6 x 800 mg tablets

Elderly people:

No dose adjustmentis required.

Childrenand adolescents:

Asacolonis only recommended for use in children 6 years of age and older.

Theactualdosewillvaryasitisdeterminedindividuallybasedonthediseasephaseandthe

child’s weight in kilograms. For further information please talk to your doctor.

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Youshouldnottakeahigherdosethanyourdoctorhasprescribedforyou.Contactyour

doctor,hospitalor pharmacyifyouhavetakenmoreAsacolontabletsthanprescribedinthis

information or byyour doctor (and you do not feel well).

Common symptoms of over dosage are:

excessive sweating

vomiting

rapidbreathing

feeling faint or dizzy.

If you forget to takeAsacolon

Ifyou forget to take a dose at the right time, just take the next dose as normal.

Do not take a double dose to make up fora forgottendose.

If you stop takingAsacolon

Take your tablets for as long as your doctor tells you to.You should talk to your doctorbefore

changingor stoppingthe treatment.

Ifyou have any further questions on the use of this product, ask your doctor or pharmacist.

4. Possibleside-effects

Likeallmedicines,Asacoloncancausesideeffects,althoughnoteverybodygetsthem.

Evaluation of the side effects is based on the following frequencies:

StoptakingAsacolonimmediatelyandtellyourdoctorifyoubruiseeasily,orifyousuffer

from:

any unexplained bleeding(e.g. nosebleeds)

bleeding under your skin

purple spots under your skin

sore throat

persistentfever.

Your doctor mayneed to take a blood test(see section2, “Before you take Asacolon”).

Commonside effects:

Very common: In more than 1 in 10 patients treated

Common: In less than 1 in 10, but more than 1 in 100 patients treated

Uncommon: Inless than 1 in 100, but more than 1 in 1,000 patients treated

Rare: In less than 1 in 1,000, but more than 1 in 10,000 patients treated

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Uncommonside effects:

low number of red blood cells (anaemia)

buzzing, ringing or whistlingin the ears (tinnitus)

feeling of pins and needles (paresthesia)

itching skin (pruritus)

hives (urticaria)

no drug effect.

Rareside effects:

headache

feeling dizzy(dizziness)

inflammation of the heart muscle (myocarditis) or heart sac (pericarditis)

abdominalpain

diarrhoea

bloating of the abdomen (flatulence)

feeling sick(nausea)

vomiting

indigestion(dyspepsia).

Very rareside effects:

blood disorders, including:

-low number of whiteblood cells (leucopenia, neutropenia), which sometimes

-can be severe (agranulocytosis)

-low numbers of all blood cells (pancytopenia)

-low number of platelets(thrombocytopenia)

-bone marrow depression (aplastic anaemia)

-high numbers of certain white blood cells calledeosinophil granulocytes

-(eosinophilia)

-bone marrow depression

hypersensitivity reactions such as:

-allergic exanthem (rash or skin eruption)

-drug fever (fever that occurs while taking the medicine and which disappears

-when the medicine is stopped)

-lupus erythematosus syndrome (autoimmune disease that can involve the

-organs and joints)

-pancolitis (ulcerative colitisinvolving the entire colon)

tingling, numbness, unusual sensations,weakness, burning pain(peripheral neuropathy)

allergic (hypersensitivity) and fibrotic lung reactions (the alveoli, tiny air sacs in the lungs

that transfer oxygen to the blood, become damaged and inflamed) including:

-dyspnoea (difficultybreathing)

-cough

-bronchospasm (difficultybreathing)

-alveolitis (inflammation of the alveoli-tiny air sacs of the lungs)

-pulmonaryeosinophilia (lung inflammation withan increase in eosinophils,

-atype of white blood cells)

-lung infiltration (fluid collects and gets filled in the lungs)

-pneumonitis (inflammation of lung tissue)

-eosinophilic pneumonia (inflammation ofthe lung)

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-eosinophilic pneumonia

inflammation of the pancreas (pancreatitis)

liver problems, such as:

-abnormalliver function tests (blood tests to investigate how well the liver is

-working)

-jaundice (yellowdiscolorationofthe skin andofthe whites oftheeyes)

-inflammation of the liver (hepatitis)

hairloss (alopecia)

musclepain (myalgia)

jointpain(arthralgia)

impairment of kidney functionincluding:

-interstitialnephritis (inflammation of the kidneys)

-kidney insufficiency

-kidney failure, which maybe reversible if treatment is stopped

-nephrotic syndrome

reversible oligospermia (reduced sperm count that occurs while taking the medicine and

which disappears when the medicine is stopped)

chest pain

lupus-like syndrome. This is a disorder of the immune system which can cause:

-pericarditis(an inflammation of the membrane around the heart)

-pleuropericarditis (aninflammation of the membranes around the lungs and heart)

-rash

-jointpain (arthralgia)

worsening ofthe symptoms of colitis.

AllergicreactionstoAsacoloncanoccur.Tellyour doctorifyougetarash,anyshortnessof

breath(bronchospasm),palpitations(fastheartbeat),slowheartbeat,chestpain,orifyour

colitis starts to feelworse. These effects will usuallydisappear whenAsacolonis stopped.

Tellyourdoctorimmediatelyifyoushowsignsofnottoleratingthismedicine(e.g.cramps,

stomach pain, fever, severe headache or rash).

You mayfind tablets in your stools(seesection3“How to take Asacolon”).

Ifanyofthesideeffectsgetsserious,orifyounoticeanysideeffectsnotlistedinthis

leaflet, please tellyour doctor or pharmacist. Some side effects may need treatment.

5. HowtostoreAsacolon

Your tablets willhave anexpiry (EXP) date on the pack showing themonthandyear. Do not

useAsacolonGastro-resistantTabletsaftertheexpirydatewhichisstatedonthecartonand

blister.Theexpirydatereferstothelastdayofthatmonth.Callyourdoctortogetanew

pack.

Do not store your Asacolon Gastro-resistant Tablets above25°C. Store your Asacolon Gastro-

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Keepallmedicinesoutofreachandsightofchildren–preferablyinalockedcupboard

or medicine cabinet.

Rememberthis medicine has been prescribed just for you. Never offer your medicine to other

people. It may notbe suitable for them even if their symptoms seem the same as yours.

Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist

howtodisposeofmedicinesnolongerrequired.Thesemeasureswillhelptoprotectthe

environment.

6. FurtherInformation

WhatAsacoloncontains

The active substance ismesalazine.

Each tablet contains400 mg or800 mg mesalazine.

The other ingredients are:

Tablet core

lactose monohydrate

sodium starch glycolate(Type A)

magnesium stearate

talc E553b

povidone E1201

Tablet coat

methacrylic acid–methylmethacrylate copolymer (1:2)

talc E553b

triethyl citrate

yellow and red iron oxides E172

macrogol6000.

WhatAsacolonlooks like and contents of the pack

Asacolon400mgGastro-resistantTablets/Asacolon800mgGastro-resistantTabletsare

reddish to brownish oblong tabletswitha glossyto matt finish.

Asacolon400mgGastro-resistantTabletscomeinblisterstripsoftentablets,whichare

packed as100 tablets per carton.

Asacolon800mgGastro-resistantTabletscomeinblisterstripsoftentablets,whichare

packed as90 tablets per carton.

Marketing Authorisation Holder and Manufacturer

The marketing authorisation holder is:

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United Drug House

Magna Drive

Magna Business Park

Citywest Road

Dublin 24, Ireland

The manufacturers are:

Pharmaceutical Packaging Service

United Drug House, Magna Drive, Magna Business Park

Citywest Road, Dublin 24, Ireland

RottendorfPharma GmbH

AmFleigendahl 3

59320 Ennigerloh

Germany

In additionyoumaywish to contact the NationalAssociationfor Colitis and Crohn’s Disease

which offers information, advice and local support groups.

Irish Societyfor Colitis and Crohn’s Disease

Carmichael House, North Brunswick Street, DUBLIN 7

‘Asacolon’ is a registered trade mark.

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SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Asacolon400mgGastro-ResistantTablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Eachgastro-resistanttabletcontains:Mesalazine400mg.

Excipients:alsocontains76.4mgoflactosemonohydrate,seesection4.4.forfurtherdetails.

Forafulllistofexcipients,seesection6.1.

3PHARMACEUTICALFORM

Gastro-resistantTablet.

Thetabletsarereddishtobrownishandoblong-shaped.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Forthetreatmentofmildacuteulcerativecolitis.Forthemaintenanceofremissionofulcerativecolitis.

Forthemaintenanceofsurgically-inducedremissionofCrohn’sDisease.

4.2Posologyandmethodofadministration

Posology

Adults:

Ulcerativecolitis:

Inductionofremission:

2.4g(6tablets)perdayindivideddoses.Ifrequiredthedosemaybeincreasedto4.8g(12tablets)daily.

Thedosagecanbeadjustedinaccordancewiththeresponsetothetreatment.

Maintenanceofremission:

1.2to2.4g(3to6tablets)perdayoncedailyorindivideddoses.

Crohn’sdisease:

Maintenanceofremission:

2.4g(6tablets)perdayoncedailyorindivideddoses.

Elderlypopulation

Asforadultsaboveunlessliverorrenalfunctionisseverelyimpaired(seesection4.3and

4.4).Nostudieshavebeencarriedoutintheelderlypopulation.

Paediatricpopulation

Thereisonlylimiteddocumentationforaneffectinchildren(age6-18years).

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Activedisease:Tobedeterminedindividually,startingwith30-50mg/kg/dayindivideddoses.Maximumdose:

75mg/kg/dayindivideddoses.Thetotaldoseshouldnotexceed4.0g/day.

Maintenancetreatment:Tobedeterminedindividually,startingwith15-30mg/kg/dayindivideddoses.Thetotal

doseshouldnotexceed2.0g/day.

Methodofadministration:oral.

Thetabletsmustbeswallowedwholepreferablywithsomeliquidbeforefoodintake.

Theymustnotbechewed,crushedorbrokenbeforeswallowing.

Ifoneormoredoseshavebeenmissed,thenextdoseistobetakenasusual.

4.3Contraindications

Asacoloniscontraindicatedincasesof:

-Historyofhypersensitivitytosalicylates.

-Hypersensitivitytomesalazineoranyoftheexcipients(seesection6.1).

-Severerenalimpairment(GFRlessthan30mLperminute).

-Severeliverimpairment.

-Gastricandduodenalulcers

-Childrenunder2yearsofage.

4.4Specialwarningsandprecautionsforuse

Renalimpairment

Urinarystatus(dipsticks)shouldbedeterminedpriortoandduringtreatment,atthediscretionofthetreating

physician.Notrecommendedforuseinpatientswithrenalimpairment.Cautionshouldbeexercisedinpatientswith

raisedbloodureaorproteinuria.

Thepossibilityofmesalazine-inducednephrotoxicityshouldbesuspectedinpatientsdevelopingimpairmentofrenal

functionduringtreatment.

ItisrecommendedthatallpatientshaveanevaluationoftheirrenalfunctionpriortoinitiationofAsacolontherapyand

periodicallywhileonAsacolontherapy.Asaguideline,follow-uptestsarerecommended14daysofinitiationof

therapyandthenevery4weeksforthefollowing12weeks.ShortmonitoringintervalsearlyafterthestartofAsacolon

therapywilldiscoverrareacuteallergicimpairmentofrenalfunction.Intheabsenceofanacuteallergicrenalresponse

monitoringintervalscanbeextendedtoevery3monthsandthenannuallyafter5years.Ifadditionalsignsofillness

appear,thesetestsshouldbeperformedimmediately.TreatmentwithAsacolonshouldbestoppedimmediatelyifthere

isevidenceofrenalimpairmentandpatientsshouldseekimmediatemedicaladvice.

Liverimpairment

Therehavebeenreportsofincreasedliverenzymelevelsinpatientstakingpreparationscontainingmesalazine.Caution

isrecommendedifAsacolonisadministeredtopatientswithliverimpairment.Bloodtests(liverfunctionparameters

suchasALTorAST)shouldbedeterminedpriortoandduringtreatment,atthediscretionofthetreatingphysician.As

aguideline,follow-uptestsarerecommended14daysaftercommencementoftreatment,thenafurthertwotothree

testsatintervalsof4weeks.Ifthefindingsarenormal,follow-uptestsshouldbecarriedoutevery3months.If

additionalsymptomsoccur,thesetestsshouldbeperformedimmediately.

Cardiachypersensitivityreactions

Mesalazine-inducedcardiachypersensitivityreactions(myo-andpericarditis)havebeenreportedrarelywithAsacolon.

Incaseofpreviousmesalazine-inducedcardiacAT400-IEhypersensitivityAsacolonmustnotbereintroduced.Caution

shouldbeusedinpatientswithpreviousmyo-andpericarditisofallergicbackgroundregardlessofitsorigin.

Pulmonarydisease

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withAsacolon.

HypersensitivitytoSulphasalazine

Inpatientswithahistoryofhypersensitivitytosulphasalazine,therapyshouldbeinitiatedonlyunderclosemedical

supervision.Treatmentmustbestoppedimmediatelyifacutesymptomsofintoleranceoccursuchasabdominal

cramps,acuteabdominalpain,fever,severeheadacheandrash.

Blooddyscrasia

Veryrarelyseriousblooddyscrasiahasbeenreportedwiththismedicinalproduct.TreatmentwithAsacolonshouldbe

stoppedimmediatelyifthereisasuspicionorevidenceofblooddyscrasia,suchasunexplainedbleeding,haematoma,

purpura,anaemia,persistentfeverorsorethroat,andpatientsshouldseekimmediatemedicaladvice.Haematological

investigationsincludingacompletebloodcountshouldbeperformedpriortoinitiationandwhileontherapyatthe

discretionofthetreatingphysician.Asaguideline,follow-uptestsaregenerallyrecommended14daysafterinitiation

oftherapyandthenevery4weeksforthefollowing12weeks.Iftheresultsarenormal,follow-uptestsshouldbe

carriedoutevery3months.Ifadditionalsymptomsoccur,thesetestsshouldbeperformedimmediately.

Tabletsinstool

Alimitednumberofreportsofintacttabletsinstoolhavebeenreceived.Whatappeartobeintacttabletsmayinsome

casesrepresentlargelyemptyshellsofthetabletcoating.Asacolon400mgGastro-resistantTabletsreleasetheir

contentinthelowergutevenifthecoatingdoesnotdissolveentirely.OncepH7.0isreached,cracksinthecoatingare

sufficientforthereleaseofmesalazinefromthetablets.Thisprocessisirreversiblefromhereonandmesalazinewill

thereforebereleasedcontinuously,independentofintestinalpH.Iftabletsareobservedinthestoolrepeatedly,the

patientshouldconsulthis/herphysician.

Intolerancetocarbohydrates

Patientswithrarehereditaryproblemsofgalactoseintolerance,theLapplactasedeficiencyorglucose-galactose

malabsorptionshouldnottakethismedicine.

Theelderly

Useintheelderlyshouldbehandledwithcautionandtheproductshouldonlybeprescribedtopatientshavinganormal

renalfunction.

Paedriaticpopulation

Thereisonlylimiteddocumentationforaneffectinchildren(age6-18years),seesection4.2.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Specificinteractionstudieshavenotbeenperformed.

Sulphasalazinedecreasestheabsorptionofdigoxin.Therearenodataoninteractionofdigoxinwithmesalazine.

Mesalazinecanincreasethemyelosuppressiveeffectsofazathioprine,or6-mercaptopurine,orthioguanine.Life-

threateninginfectioncanoccur.Patientsshouldbecloselyobservedforsignsofinfectionandmyelosuppression.

Haematologicalparameters,suchasleukocyteandlymphocytecellcountsshouldbemonitoredregularly(weekly),

especiallyatinitiationofsuchcombinationtherapy(seesection4.4).Ifwhitebloodcellsarestableafter1month,

testingevery4weeksforthefollowing12weeksfollowedby3monthlymonitoringintervalsappearstobejustified.

Theconcurrentuseofknownnephrotoxicagents,suchasNSAIDs,azathioprine,ormethotrexate,mayincreasetherisk

ofrenalreactions.However,noadverseeventsprovingsuchinteractionshavebeenreported(seesection4.4).

Thereisweakevidencethatmesalazinemightdecreasetheanticoagulanteffectofwarfarin.

Apartfrompurineantimetabolitesinteractionstudiesinadultsandchildren,nootherinteractionstudiesinadultsor

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4.6Fertility,pregnancyandlactation

TherearenoadequatedataontheuseofAsacoloninpregnantwomen.However,datafromalimitednumber(627)of

exposedpregnanciesindicatenoadverseeffectofmesalazineonthepregnancyoronthehealthofthefetus/newborn

child,butmorefrequentpre-termbirthscannotbeexcluded.Todatenootherrelevantepidemiologicdataareavailable.

Inonesinglecaseafterlong-termuseofahighdoseofmesalazine(2-4g,orally)duringpregnancy,renalfailureina

neonatewasreported.

Animalstudiesonoralmesalazinedonotindicatedirectorindirectharmfuleffectswithrespecttopregnancy,

embryonic/fetaldevelopment,parturitionorpostnataldevelopment.

Mesalazinecrossestheplacentalbarrier.Asacolonshouldonlybeusedduringpregnancyif

thepotentialbenefitoutweighsthepossiblerisk.Cautionshouldbeexercisedwhenusinghighdosesofmesalazine.

N-acetyl-5-aminosalicylicacidandtoalesserdegreemesalazineareexcretedinbreastmilk.Theclinicalsignificance

ofthishasnotbeendetermined.Onlylimitedexperienceduringlactationinwomenisavailabletodate.

Hypersensitivityreactionssuchasdiarrhoeaintheinfantcannotbeexcluded.Therefore,Asacolonshouldonlybeused

duringbreast-feeding,ifthepotentialbenefitoutweighsthepossiblerisk.Iftheinfantdevelopsdiarrhoea,breastfeeding

shouldbediscontinued.

4.7Effectsonabilitytodriveandusemachines

Noeffectsontheabilitytodriveandusemachineshavebeenobserved.

4.8Undesirableeffects

TheAsacolonclinicaltrialdatabaseincludes651patientstreatedwithAsacolon400mgGRTablets.Themesalazine

doseswereintherangeof0.8to4.8g/day,theaveragetreatmentdurationvariedbetweenfourweeksandfouryears.

Undesirableeffectsrelevantforthelabellingreportedfromninedouble-blindandsixopenclinicalstudiesand

informationfromspontaneousreportingortheliteratureislistedbelow.

Thelatterwasreportedfromapopulationofunknownsize.Theirfrequencyisnotknown.

Bloodandlymphaticsystemdisorders

Uncommon:anaemia.

Veryrare:alteredbloodcounts(aplasticanaemia,agranulocytosis,pancytopenia,neutropenia,leucopenia,

thrombocytopenia),bonemarrowdepression,eosinophilia,blooddisorder.

Immunesystemdisorders

Veryrare:hypersensitivityreactionssuchasallergicexanthema,drugfever,lupus

erythematosussyndrome,pancolitis.

Nervoussystemdisorders

Uncommon:tinnitus,paresthesia.

Rare:headache,dizziness.

Veryrare:peripheralneuropathy.

Cardiacdisorders

Rare:myocarditis,pericarditis.

Respiratory,thoracicandmediastinaldisorders

Veryrare:allergicandfibroticlungreactions(includingdyspnoea,cough,

bronchospasm,alveolitis,pulmonaryeosinophilia,lunginfiltration,

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Gastrointestinaldisorders

Rare:abdominalpain,diarrhoea,flatulence,nausea,vomiting,dyspepsia.

Veryrare:acutepancreatitis.

Notknown:exacerbationofthesymptomsofcolitis.

Hepato-biliarydisorders

Veryrare:changesinliverfunctionparameters(increaseintransaminasesand

cholestasisparameters),hepatitis,cholestatichepatitis.

Skinandsubcutaneoustissuedisorders

Common:rash.

Uncommon:pruritus,urticaria.

Veryrare:alopecia.

Musculoskeletalandconnectivetissuedisorders

Veryrare:myalgia,arthralgia.

Notknown:lupus-likesyndromewithpericarditisandpleuropericarditisasprominentsymptomsaswellasrashand

arthralgia.

Renalandurinarydisorders

VeryRare:impairmentofrenalfunctionincludingacuteandchronicinterstitialnephritisandrenalinsufficiency,

nephroticsyndrome,renalfailurewhichmaybereversibleonwithdrawal.

Reproductivesystemandbreastdisorders

Veryrare:oligospermia(reversible).

Generaldisordersandadministrationsiteconditions

Common:drugfever.

Uncommon:drugineffective.

Veryrare:chestpain.

Verycommon: 1/10,common: 1/100and<1/10,uncommon: 1/1,000and

<1/100,rare: 1/10,000and<1/1,000,veryrare:<1/10,000,notknown(cannotbeestimatedfromtheavailabledata)

AnunknownnumberoftheaboveundesirableeffectsareprobablyassociatedtotheunderlyingIBDratherthan

Asacolon/mesalazinemedication.Thisholdstrueespeciallyforgastrointestinalundesirableeffectsandarthralgia.

Mesalazine-inducednephrotoxicity,whichmaybereversibleonwithdrawal,shouldbesuspectedinpatients

developingrenaldysfunctionduringtreatment(seesection4.4).

Toavoidblooddyscrasiaresultingfromdevelopingbonemarrowdepressionpatientsshouldbemonitoredwithcare

(seesection4.4).

Co-administrationofmyelosuppressivedrugssuchasazathioprine,or6-MP,orthioguaninecanprecipitateleucopenia

(seesection4.5).

ConcurrentuseofNSAIDs,azathioprine,ormethotrexatemayincreasetheriskofrenalreactions(seesection4.5).

4.9Overdose

Thereareraredataonoverdose(e.g.intendedsuicidewithhighoraldosesofmesalazine),whichdonotindicaterenal

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5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Asacolon400mgGastro-resistantTabletscontainmesalazine[ATCA07EC02],or5-aminosalicylicacid,whichhasan

anti-inflammatoryeffectthroughamechanismthathasnotyetbeenfullyclarified.Mesalazineinhibitsmigrationof

polymorphnuclearleukocytesandlipooxygenaseofcellsatconcentrationsreachedinthelargeintestineduring

treatment.Theproductionofpro-inflammatoryleukotrienes(LTB4and5-HETE)inmacrophagesoftheintestinalwall

istheninhibited.Intrialconditionsmesalazinehasalsoinhibitedcyclooxygenaseandthus,thereleaseofthromboxane

B2andprostaglandinE2,buttheclinicalmeaningofthiseffectisstillunclear.Mesalazineinhibitsformationofplatelet

activatingfactor(PAF).Mesalazineisalsoanantioxidant;ithasbeenshowntodecreaseformationofreactiveoxygen

productsandtocapturefreeradicals.Furthermore,mesalazineinhibitssecretionofwaterandchlorideandincreasesthe

re-absorptionofsodiumintheintestineinexperimentalcolitisintestanimals.

5.2Pharmacokineticproperties

Asacolon400mgGastro-resistantTabletsarecoatedwithapolymer[EudragitTMS]whichallowstheactiveprinciple

tobereleasedwhentheintraluminalpHisabove7,thatiswithintheterminalileumandcolon,whicharethemainsites

ofinflammation.Asacolontabletshavebeendesignedtominimiseabsorptionofmesalazineinthedigestivetract.

Absorptionbytheoralrouteisapproximately26%.Consequently,74%oftheadministereddoseremainwithinthe

terminalileum,colon,andrectum,beingavailabletoexertatopicalanti-inflammatoryeffect.Mesalazineis

metabolisedbothbytheliverandtheintestinalmucosatoaninactivederivative,N-acetyl-5-aminosalicylicacid.

Mesalazinehasaneliminationhalf-lifebetween9hours(singledose)and11hours(steadystate).Theeliminationof

mesalazineisessentiallyfaecalandurinary,intheformofmesalazineanditsN-acetylmetabolite.

5.3Preclinicalsafetydata

Toxicityofmesalazineafteroraladministrationhasbeeninvestigatedinseveralstudieswithbothsingleandrepeated

doses.Whenadoseof1g/kgbodyweight/daywasadministeredrepeatedlytorats,itcauseddamageinkidneysandthe

gastro-intestinaltract.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Lactosemonohydrate

Sodiumstarchglycolate(TypeA)

Magnesiumstearate

Talc(E553b)

Povidone(E1201)

FilmCoating

Methacrylicacid-methylmethacrylatecopolymer(1:2)

Talc(E553b)

TriethylCitrate

Yellowpigment(ferricoxide)(E172)

Macrogol6000

Redpigment(ferricoxide)(E172)

6.2Incompatibilities

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6.3Shelflife

3years

6.4Specialprecautionsforstorage

Donotstoreabove25ºC.Storeintheoriginalpackageinordertoprotectfrommoisture.

6.5Natureandcontentsofcontainer

BlisterstripsofaluminiumfoilandPVCcontainedwithinanoutercardboardcarton,containing100tablets.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements.

7MARKETINGAUTHORISATIONHOLDER

TillottsPharmaLimited

UnitedDrugHouse

MagnaDrive

MagnaBusinessPark

CitywestRoad

Dublin24

Tradingas:

TillottsPharmaLimited

8MARKETINGAUTHORISATIONNUMBER

PA1204/001/002

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation: 11December1990

Dateoflastrenewal: 11December2010

10DATEOFREVISIONOFTHETEXT

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