DITROPAN

Main information

  • Trade name:
  • DITROPAN Oral Solution 2.5 MG/5ml
  • Dosage:
  • 2.5 MG/5ml
  • Pharmaceutical form:
  • Oral Solution
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • DITROPAN Oral Solution 2.5 MG/5ml
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0540/146/001
  • Authorization date:
  • 12-12-2008
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Ditropan2.5mg/5mlOralSolution

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Each5mlcontains2.5mgoxybutyninhydrochloride.

Excipients:Each5mlcontains1.265gsucrose,1.925gsorbitol(E420)and2.85mgsodiummethyl-p-hydroxybenzoate

(E219)

Forafulllistofexcipients,seesection6.1

3PHARMACEUTICALFORM

OralSolution

Aclearcolourlessviscousoralsolution.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Asananticholinergicagent,alsowithadirectrelaxanteffectonsmoothmuscle,oxybutynininhibitsbladdermuscle

contractionsandspasm.Foruseinurinaryincontinence,urgencyandfrequencyintheunstablebladder;whetherdue

toneurogenicbladderdisorders(detrusorhyperreflexia)inconditionssuchasmultiplesclerosisandspinabifidaorto

idiopathicdetrusorinstability(motorurgeincontinence).

Itisalsousefulinthecontrolofvesicalhyperactivityseenaftersurgeryofthebladderorprostate,oraccompanying

cystitis.

Peadiatricpopulation

Oxybutninhydrochlorideisindicatedinchildrenover5yearsofagefor:

-Urinaryincontinence,urgencyandfrequencyinunstablebladderconditionsduetoidiopathicoveractivebladderor

neurogenicbladderdisorders(detrusoroveractivity).

-Nocturnalenuresisassociatedwithdetrusoroveractivity,inconjunctionwithnon-drugtherapy,whenothertreatment

hasfailed.

4.2Posologyandmethodofadministration

Adults:Theusualdoseis5mg(10ml)twoorthreetimesaday.Thismaybeincreasedtoamaximumof5mgfour

timesadaytoobtainaclinicalresponseprovidedthatthesideeffectsaretolerated.

Elderly:Theeliminationhalf-lifeisincreasedintheelderly,therefore,adoseof2.5mg(5ml)twiceaday,particularly

ifthepatientisfrail,islikelytobeadequate.Thisdosemaybetitratedupwardsto5mgtwotimesadaytoobtaina

clinicalresponseprovidedthesideeffectsarewelltolerated.

Children(under5yearsofage):Notrecommended.

Children(over5yearsofage):Neurogenicbladder:theusualdoseis2.5mg(5ml)twiceaday.Thisdosemaybe

titratedupwardsto5mgtwoorthreetimesadaytoobtainaclinicalresponseprovidedthatthesideeffectsarewell

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Thisdosemaybetitratedupwardsto5mgtwoorthreetimesadaytoobtainaclinicalresponseprovidedtheside

effectsaretolerated.Thelastdoseshouldbegivenbeforebedtime.

Followinginitialcontrol,itmaybepossibletointroduceareducedmaintenancedose.

4.3Contraindications

Hypersensitivitytooxybutyninoranycomponent.

Myastheniagravis.

Narrow-angleglaucomaorshallowanteriorchamber.

Duetotheriskofprovokinghyperpyrexia,thisproductshouldnotbegiventopatientswithpyrexiaorwherethe

ambienttemperatureishigh.

Useinchildrenundertheageoffiveyears.

Useinoesophagealdysfunctionincludinghiatushernia.

Functionalororganicgastrointestinalobstructionincludingpyloricstenosis,paralyticstenosis,paralyticileus,intestinal

atony.

Patientswithileostomy,colostomy,toxicmegacolon,severeulcerativecolitis.

Patientswithbladderoutflowobstructionwhereurinaryretentionmaybeprecipitatedsuchasprostasticenlargement.

4.4Specialwarningsandprecautionsforuse

Duetothepresenceofsorbitolandsucroseinthisproduct,patientswithrarehereditaryproblemsoffructose

intoleranceshouldnottakethismedicine.

Duetothepresenceofsucroseinthisproduct,patientswithglucose-galactosemalabsorptionorsucrose-isomaltase

insufficiencyshouldnottakethismedicine.

Sodiummethyl-p-hydroxybenzoatemaycauseallergicreactions(possiblydelayed),andexceptionally,bronchospasm.

Oxybutyninshouldbeusedwithcautioninthefrailelderlywhomaybemoresensitivetotheeffectsoftheproductand

inpatientswithautonomicneuropathy,hepaticorrenalimpairment,gastrointestinalpathologyincludingsevere

gastrointestinalmotilitydisorders.

Oxybutyninmayaggravatethesymptomsofhyperthyroidism,congestiveheartfailure,cardiacarrhythmia,tachycardia,

hypertensionandprostatichypertrophy.

Oxybutyninhydrochlorideisconsideredtobeunsafeinpatientswithporphyriabecauseithasbeenshowntobe

porphyrinogenicinanimalsandinvitrosystems.

Chronicusemayresultinanincreaseindentalcaries,asaconsequenceofreducedorinhibitedsalivation.Regular

dentalcheck-upsarethereforeadvisableduringlong-termtreatment.

Paediatricpopulation

Oxybutyninhydrochlorideisnotrecommendedforuseinchildrenbelowage5yearsduetoinsufficientdataonsafety

andefficacy.

ThereislimitedevidencesupportingtheuseofOxybutynininchildrenwithmonosymptomaticnocturnalenuresis(not

relatedtodetrusoroveractivity).

Inchildrenover5yearsofage,Oxybutninhydrochlorideshouldbeusedwithcautionastheymaybemoresensitiveto

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4.5Interactionwithothermedicinalproductsandotherformsofinteraction

CareshouldbetakenifotheranticholinergicagentsareadministeredtogetherwithDitropanaspotentiationof

anticholinergiceffectscouldoccur.

Occasionalcasesofinteractionbetweenanticholinergicsandphenothiazines,amantadine,butyrophenones,L-dopa,

digitalisandtricyclicantidepressantshavebeenreportedandcareshouldbetakenifDitropanisadministered

concurrentlywithsuchdrugs.

Byreducinggastricmotility,oxybutyninmayaffecttheabsorptionofotherdrugs.

4.6Fertility,pregnancyandlactation

Pregnancy

ThereisnoevidenceastothesafetyofDitropaninhumanpregnancynoristhereevidencefromanimalworkthatis

totallyfreefromhazard.Avoidinpregnancyunlessthereisnosaferalternative.

Lactation

Smallamountsofoxybutyninhavebeenfoundinmother’smilkoflactatinganimals.Breastfeedingwhileusing

oxybutyninisthereforenotrecommended.

4.7Effectsonabilitytodriveandusemachines

Theproductmaycausedrowsinessorblurredvision.Patientsshouldnotdriveoroperatemachineryunlessithasbeen

shownnottoaffectphysicalormentalability.

4.8Undesirableeffects

Gastro-intestinaldisorders

Nausea,diarrhoea,constipation,drymouth,abdominaldiscomfort,anorexia,vomiting,gastroesophagealreflux.

CNSandpsychiatricdisorders

Agitation,headache,dizziness,drowsiness,cognitivedisorders(disorientation,anxiety,paranoia),hallucinations,

nightmares,convulsions.

Cardiovasculardisorders

Tachycardia,cardiacarrhythmia.

Visiondisorders

Blurredvision,mydriasis,intraocularhypertension,onsetofnarrow-angleglaucoma,dryeyes.

Renalandurinarydisorders

Urinaryretention,difficultyinmicturition.

Skinandappendages

Facialflushingwhichmaybemoremarkedinchildren,dryskin,allergicreactionssuchasrash,urticaria,angioedema,

photosensitivity.

4.9Overdose

ThesymptomsofoverdosagewithDitropanprogressfromanintensificationoftheusualsideeffectsofCNS

disturbances(fromrestlessnessandexcitementtopsychoticbehaviour),circulatorychanges(flushing,fallinblood

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Measurestobetakenare:

1)Immediategastriclavage

2)Physostigminebyslowintravenousinjection

Adults:0.5-2.0mgphysostigminei.v.slowly,repeatedafter5minutesifnecessary,uptoamaximumtotaldoseof5mg.

Children:30µg/kgphysostigminei.v.slowly,repeatedafter5minutesifnecessary,uptoamaximumtotaldoseof

2mg.

Fevershouldbetreatedsymptomaticallywithtepidspongingoricepacks.

Inpronouncedrestlessnessorexcitation,diazepam10mgmaybegivenbyintravenousinjection,tachycardiamaybe

treatedbyintravenousinjectionofpropranololandurinaryretentioncanbemanagedbycatheterisation.Intheeventof

progressionofthecurarelikeeffecttotheparalysisoftherespiratorymuscles,mechanicalventilationwillberequired.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Oxybutyninhydrochloridehasbothdirectantispasmodicactiononthesmoothmuscleofthebladderdetrusoraswellas

ananticholinergicactioninblockingthemuscariniceffectsofacetylcholineonsmoothmuscle.Thesepropertiescause

relaxationofthedetrusormuscleofthebladderinpatientswithanunstablebladder.Ditropanincreasesbladder

capacityandreducestheincidenceofspontaneouscontractionsofthedetrusormuscle.

5.2Pharmacokineticproperties

Pharmacokineticreportsshowoxybutynintoberapidlyabsorbedfromthegastrointestinaltractfollowingoral

administrationwithmaximumplasmaconcentrationsreachedinlessthan1hoursubsequentlyfallingbiexponentially

withahalf-lifeofbetween2and3hours.Maximumeffectcanbeseenwithin3-4hourswithsomeeffectstillevident

after10hours.

Repeatedoraladministrationachievedsteadystateaftereightdays.Oxybutynindoesnotappeartoaccumulatein

activeelderlypatientsandthepharmacokineticsaresimilartothoseinotheradults.However,infrailelderlypatients,

andAUCvaluesaresignificantlyincreased.Oxybutyninisextensivelymetabolisedbytheliver,primarilybythe

cytochromeP450enzymesystem,particularlyCYP3A4foundmostlyintheliverandgutwall,themetabolitesalso

appearingtohaveantimuscarinicproperties.Themaineliminationrouteisviathekidneyswithonly0.3-0.4%of

unchangeddrugappearingintheurineoftheratafter24hoursand1%appearingintheurineofthedogafter48hours.

Inratsanddogstherefore,oxybutyninappearstobealmostcompletelymetabolised.

5.3Preclinicalsafetydata

Nodataoftherapeuticrelevance.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

CitricAcidmonohydrate

SodiumCitratedihydrate

Sucrose

Sorbitolliquid(non-crystallising)(E420)

Glycerol(E422)

SodiumMethyl-p-Hydroxybenzoate(E219)

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6.2Incompatibilities

Notapplicable

6.3Shelflife

Unopened: 2.5years.

Onceopened:Discardanyremainingsolution28daysafterfirstopeningthebottle.

6.4Specialprecautionsforstorage

Storebelow25°C.Storeintheoriginalcontainerinordertoprotectfromlight.

6.5Natureandcontentsofcontainer

30ml(samplesize)and150mltypeIIIamberglassbottlewithapolypropylenechild-proofcapcontainingPVDC/PE

liner.

Notallpacksizesmaybemarketed.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Nospecialrequirements.

7MARKETINGAUTHORISATIONHOLDER

Sanofi-AventisIrelandLtd.T/ASANOFI

CitywestBusinessCampus

Dublin24

Ireland

8MARKETINGAUTHORISATIONNUMBER

PA540/146/001

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:4 th

January1994

Dateoflastrenewal:1 st

March2008

10DATEOFREVISIONOFTHETEXT

Irish Medicines Board

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