Canesten Fluconazole

New Zealand - English - Medsafe (Medicines Safety Authority)

Buy It Now

Active ingredient:
Fluconazole 150 mg; Fluconazole 150 mg
Available from:
Bayer New Zealand Limited
INN (International Name):
Fluconazole 150 mg
Dosage:
150 mg
Pharmaceutical form:
Capsule
Composition:
Active: Fluconazole 150 mg Fluconazole 150 mg
Units in package:
Blister pack, PVC/PVdC/Al, 1 capsule
Class:
Restricted
Prescription type:
Restricted
Manufactured by:
Mylan Laboratories Limited
Therapeutic indications:
Canesten Fluconazole Capsule, given orally, is indicated for vaginal candidiasis.
Product summary:
Package - Contents - Shelf Life: Blister pack, PVC/Al or PVC/PVdC/Al - 1 capsules - 36 months from date of manufacture stored at or below 25°C
Authorization number:
TT50-7597
Authorization date:
2006-03-03

CanestenFluconazoleCMI

19May2009

Consumer Medicine Information

Canesten

Fluconazole Capsule

Fluconazoleoralcapsule150mg

Whatisinthisleaflet

Thisleafletanswerssome commonquestionsaboutCanestenFluconazole Capsule.

Itdoes notcontain alltheavailable information.Itdoes nottaketheplaceoftalking toyour

doctororpharmacist.

Allmedicineshave risksand benefits.Yourpharmacisthasweighedtherisksofyouusing

CanestenFluconazole Capsuleagainstthebenefitstheyexpectitwillhaveforyou.

Ifyouhave anyconcernsaboutusingthismedicine,askyourdoctororpharmacist.

Keep thisleafletwiththemedicine.

Youmayneedtoread itagain.

WhatCanestenFluconazoleCapsuleisusedfor

CanestenFluconazole Capsuleisusedtotreatafungalinfection inthevagina(vaginal

thrush).

Thismedicinebelongstoagroup ofmedicinescalledazole antifungals.

CanestenFluconazole Capsule is takenbymouthand worksfromtheinsidetopreventthe

growth ofthefungicausingyourinfection.

What isvaginalthrush?

Vaginalthrushisthecommonnameforvaginalcandidiasis,aninfectioncausedbya yeast-

likefungus calledCandida.Candidacanmultiplyrapidlyand cause damagetothevagina

when othermicro- organismsaren’tpresentina normalbalance.

Somesituationswhich canincreasesusceptibilitytothrushare:

diabetes

obesity

illness

fatigue

hormonalfluctuations(pregnancy,menstrualcycle,oralcontraceptive pill,HRT)

prolongeduseofantibioticsorsteroids

Thrushmaycausethefollowingsymptoms:

vaginalitching

CanestenFluconazoleCMI

19May2009

Consumer Medicine Information

vaginalburningorsoreness

awhite odourless dischargefromthevagina(likecottagecheese)

pain duringintercourse

Thesymptomsbelowarenotusuallysigns ofthrush:

abnormalorirregularvaginalbleeding

blood stained discharge

vulva orvaginalsores,ulcersorblisters

lowerabdominalpain

pain when passingurine

feverorchills

foulsmellingand/orunusualcoloureddischarge

Seeyourdoctorifyouexperience anyoftheabove symptoms.

Askyourdoctororpharmacistifyouhave any questions aboutwhetherthismedicine

is suitableforyou.

CanestenFluconazole Capsule is a“PharmacistOnlyMedicine”.Itisavailablewithouta

doctor’sprescription,butyourpharmacist’sadvice is required.

BeforeyoutakeCanestenFluconazoleCapsule

Whenyou must nottakeit

Do nottake CanestenFluconazoleCapsuleifyouhave anallergyto:

anymedicinecontainingfluconazole

anyothersimilarantifungalssuchasmiconazole,ketoconazoleorclotrimazole

anyoftheingredientslistedattheend ofthisleaflet.

Someofthesymptomsofanallergicreactionmayincludeshortnessofbreath,wheezingor

difficultybreathing,swellingoftheface,lips,tongue orotherpartsofthebody;rash,itching

orhives ontheskin.

Do nottake CanestenFluconazoleCapsuleifyouaretakingcisapride(Prepulsid ® ) –a

medicineusedtotreatstomachproblems.

CombiningCanestenFluconazole Capsulewith cisapride maycause serioussideeffects

suchasanabnormalheartrhythm.

CanestenFluconazoleCapsuleisnotrecommended forchildrenunder18yearsofage

unless recommendedbya doctor.

Safetyand effectiveness inchildrenunder18yearsofagehave notbeenestablished.

Do nottakethismedicineaftertheexpirydate printedonthepackorifthepackaging

istorn orshowssignsoftampering.

Ifithasexpiredorisdamaged,returnittoyourpharmacistfordisposal.

Ifyouarenotsurewhetheryoushould starttakingthismedicine,talktoyourdoctor

orpharmacist.

CanestenFluconazoleCMI

19May2009

Consumer Medicine Information

Beforeyou start touseit

Tellyourdoctororpharmacistifyouarepregnantorsuspectyoumaybepregnant.

CanestenFluconazole Capsuleisnotrecommendedforusebypregnantwomenas itmay

affectthedevelopingbaby.

CanestenFluconazole Capsuleisnotrecommendedforwomenwhomaybeatriskoffalling

pregnantunless contraceptionisbeingused.

Tellyourdoctorifyouarebreast-feeding.

CanestenFluconazole Capsuleisnotrecommendedforusebywomenwhoarebreast-

feedingas itpasses intobreastmilkandmayaffectthebaby.

Seeyourdoctorif:

thisisyourfirstinfection

youareunder18yearsofage

youhave had 3ormore infectionsin thelast6months

Tellyourdoctororpharmacistifyouhave any otherhealth problems,including:

anyliverproblems

anyheartproblems

severekidneyproblems

ifyouhaveHIVorAIDS

Tellyourdoctororpharmacistifyouhave previouslydeveloped arashwhiletaking

fluconazole.

Tellyourdoctororpharmacistifyouaretakingwarfarin(Marevan ® ,Coumadin ® ),as

bleedingorbruisingmayoccur.

Tellyourdoctororpharmacistifyouareallergicto anyothermedicines,foods,

preservativesordyes.

Tellyourdoctorifyouarediabetic.

Thrushin diabeticscanmeanthatyourblood sugarlevelsarenotwellcontrolled.Your

doctorwillbeable tocheckthisforyouandadvise treatment.

Ifyouhave nottold yourdoctoraboutanyoftheabove,dosobefore youstarttaking

CanestenFluconazoleCapsule.

Taking other medicines

Tellyourdoctororpharmacistifyouaretakinganyothermedicines,includinganyyouhave

boughtwithoutaprescriptionfroma pharmacy,supermarketorhealthfood shop.

Somemedicinesand CanestenFluconazole Capsulemayinterferewith each other.These

include:

cisapride(Prepulsid ® ) –a medicineusedtotreatstomach problems.Donottake

CanestenFluconazoleCapsuleifyouaretakingcisapride.

CanestenFluconazoleCMI

19May2009

Consumer Medicine Information

somemedicinesusedtotreatdiabetessuchastolbutamide,glimepiride,

gliclazide,pioglitazone,rosiglitazone orglibenclamide

phenytoin(Dilantin ® ) –amedicineusedtotreatepilepsy

hydrochlorothiazide –amedicineforhigh bloodpressureand otherheart

conditions

rifampicin(Rifadin ® ,Rifinah ® )orrifabutin(Mycobutin ® ) –antibioticmedicines

tacrolimus(Prograf ® ) –amedicineusedtopreventorgantransplantrejectionor

treatproblemswith theimmunesystem

zidovudine(Retrovir ® ) –a medicineforHIV/AIDS

warfarin(Coumadin ®

,Marevan ®

) –amedicinetotreatorpreventbloodclots

ThesemedicinesmaybeaffectedbyCanestenFluconazole Capsule ormayaffecthowwell

itworks.

Yourdoctororpharmacistwillhave moreinformationonmedicinesto becarefulwith or

avoidwhile takingCanestenFluconazole Capsule.

HowtotakeCanestenFluconazoleCapsule

Followalldirections givento youbyyourdoctororpharmacistcarefully.

Theymaydifferfromtheinformationcontained inthisleaflet.

Ifyoudonotunderstand theinstructionsbelow,oronthebox,askyourdoctoror

pharmacistforhelp.

How totakeit

Thecompletetreatmentforvaginalthrushisone150 mg capsule –onlyasingle doseis

needed.Take onlyonecapsule.Swallowthe capsule wholewith aglassofwater.

Thecapsule canbetaken with orwithoutfood.

Aftertaking CanestenFluconazoleCapsule,symptomsofthrushusuallystarttogetbetterin

aboutoneday.

Whentotakeit

CanestenFluconazole Capsule canbetakenatanytime oftheday.

Ifyouarenotsurewhattodo,askyourdoctororpharmacist.

If you taketoo much(overdose)

ImmediatelytelephoneyourdoctorortheNationalPoisonsInformationCentre(0800

POISONor0800764766)foradviceorgotoyournearestAccidentandEmergency

Centreifyouthink youoranyone elsemayhave takentoomuchCanesten

FluconazoleCapsule.Do thisevenifthereare no signs ofdiscomfortorpoisoning.

Youmayneedmedicalattention.

WhileyouaretakingCanestenFluconazoleCapsule

Thingsyou must do

CanestenFluconazoleCMI

19May2009

Consumer Medicine Information

Discontinuetreatmentand tellyourdoctororpharmacistifyoudevelop areactionto

thisproduct.

Seeyourdoctorifthesymptomsdonotimprove afterthreedays,oriftheybecome

worse.

Tellalldoctors,dentists andpharmacistswhoaretreatingyouthatyouaretakingor

have takenCanestenFluconazole Capsule.

Useeffective contraceptiontopreventpregnancywhiletakingCanesten Fluconazole

Capsule.

Thingsyou must notdo

Do notuseCanestenFluconazole Capsuletotreatanyothercomplaintsunless your

doctortells youto.

Do notgiveyourtreatmenttoanyone else,evenifyoususpecttheyhave thesame

conditionasyou.

Thingstobecarefulof

CanestenFluconazole Capsuleisnotexpectedtoaffectyourabilityto drive acaroroperate

machinery.

Thingsthat mayhelpto resolveThrush

Someselfhelpmeasuressuggestedbelowmayhelp yourcondition.Yourdoctoror

pharmacistcangive youmoreinformationaboutthese measures.

blotwith toiletpaperafterurinating(instead ofwipingbacktofront).

changeunderwear,nightattire,towelsand linen daily.

Avoidwhere possible:

perfumedtoiletpaper

fragrantsoapsand bathoils

wearingtightorsyntheticunderwear

douches orvaginaldeodorants

Sideeffects

Tellyourdoctororpharmacistassoonaspossibleifyoudonotfeelwellor

experiencediscomfortwhile youaretakingCanesten FluconazoleCapsule.

Thismedicinehelpsmostpeople withvaginalthrush butitmayhave unwantedsideeffectsin

afewpeople.Allmedicinescanhave sideeffects.Sometimestheyareserious,mostofthe

timetheyarenot.Youmayneedmedicalattentionifyougetsome ofthesideeffects.

Do notbealarmedbythefollowinglistofsideeffects.Youmaynotexperienceanyof

them.

CanestenFluconazoleCMI

19May2009

Consumer Medicine Information

Askyourdoctororpharmacistto answeranyquestionsyoumayhave.

Tellyourdoctororpharmacistifyounoticeanyofthefollowingandtheyworryyou:

nausea orfeelingsick,vomiting

headache

stomach pain

indigestion

diarrhoea

Thelistabove includesthemore commonsideeffectsoffluconazole.Theyareusuallymild

and short-lived.

Tellyourdoctorassoon aspossibleifyounoticeanyofthefollowing:-

swellingoftheface,lipsortonguewhich maycause difficultyswallowingor

breathing

asthma,wheezing,shortnessofbreath

sudden orsevereitching,skinrash,hives

fainting,seizuresorfits

flaking oftheskin

yellowingoftheskin oreyes,also calledjaundice

bleedingorbruisingmore easilythan normal,orreddish orpurplish blotches

undertheskin

signsoffrequentorworryinginfectionssuchasfever,severechills,sorethroator

mouthulcers

fastorirregularheartbeat

Thesesideeffectsareusuallyrare butcanbe seriousandmayneedurgentmedical

attention.

Thisisnota completelistofallpossible sideeffects.Othersmayalso occurinsomepeople

and theremaybesomesideeffectsnotyetknown.

Tellyourdoctororpharmacistifyounoticeanything thatismakingyoufeelunwell,

evenifitisnotonthislist.

Askyourdoctororpharmacistifyou don’tunderstand anything onthislist.

AfterusingCanestenFluconazoleCapsule

Storage

Keepyourmedicineintheoriginalpack untilitistimeto useit.

Ifyoutakethecapsuleoutofitspackagingitmaynotkeep well.

Keepyourcapsulein acooldryplacewherethetemperaturestays below25

C.

Do notstoreyourmedicineinthebathroomornearasink.Do notleave itona

windowsillorinthecar.

Heatand dampnesscandestroysomemedicines.

CanestenFluconazoleCMI

19May2009

Consumer Medicine Information

Keep thetreatmentwherechildrencannotreachit.

Alockedcupboard atleastone-and-a-halfmetresabove thegroundisagoodplacetostore

medicines.

Expiry

Theexpirydate ismarked onthefoil/blisterand on thecarton.

Disposal

Ifyourdoctortellsyouto stopusingthismedicineortheexpirydate has passed,ask

yourpharmacistwhatto dowith anymedicinethatisleftover.

Discardthemedicineoutofthereachofchildren.

Productdescription

What it lookslike

CanestenFluconazole Capsuleisawhite opaquecapsule with “FC150”printedin blackon

one end and“G”ontheother.

Ingredients

CanestenFluconazoleCapsule

Thecapsulecontains150mgfluconazole astheactiveingredient.Italsocontains:

lactose

maize (corn)starch

sodiumlaurylsulphate

colloidalhydratedsilica

magnesiumstearate

titaniumdioxide

gelatin

Theingredientsin theblack printinginkusedforcodingthecapsules include:-

shellac

dehydratedalcohol

isopropylalcohol

butylalcohol

propylene glycol

ammoniasolution

potassiumhydroxide

black ironoxide

Thismedicinedoesnotcontain sucrose,gluten,tartrazineoranyotherazo dyes.

Manufacturer

CanestenFluconazole Capsules aremadeinCanada.

CanestenFluconazoleCapsuleisdistributedin NewZealand by:

CanestenFluconazoleCMI

19May2009

Consumer Medicine Information

BayerNewZealand Limited

ConsumerCareBusinessGroup

3ArgusPlace

Hillcrest

North Shore 0627

AUCKLAND

TollFree:0800847874

Thisleafletwaspreparedon19May2009.

Reference:CanestenFluconazoleCapsuleDataSheetdated2April2009.

=RegisteredTrademark

CanestenFluconazoleDataSheet

2April2009

Data Sheet

CANESTENFLUCONAZOLE CAPSULE

FluconazoleOralCapsule150mg

NameofMedicine

Fluconazole

Fluconazoleisabis-triazole:2-(2,4-difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)-2-propanol.Itisawhite tooff-

white crystallinepowderwhich issparinglysoluble inwaterand saline.Ithasamolecularweight of306.3.

Structuralformula:

Description

Each CanestenFluconazoleCapsule containsfluconazole 150mg astheactiveingredient.

Size1 hard gelatin capsulewithwhiteopaquebodyandwhiteopaque cap.Thebodyhas"FC 150"and the cap

has"G"printedin black. Thecapsule containswhiteto off-whitepowder. Otheringredientspresentinclude

lactose,maize (corn)starch,sodiumlaurylsulphate,colloidalhydratedsilica,magnesiumstearate, gelatinand

titaniumdioxide(E171). Theingredientspresentintheblackprintinginkusedfor coding the capsulesinclude

shellac, dehydrated alcohol, isopropylalcohol,butylalcohol, propyleneglycol,ammonia solution, potassium

hydroxideand blackironoxide(E172).

Pharmacology

Actions

Fluconazoleisamemberofthe bis-triazoleantifungalagents. Fluconazoleisahighlyselectiveinhibitor offungal

cytochrome P-450 sterolC-14alpha demethylation.Mammaliancelldemethylation ismuch lesssensitiveto

fluconazole inhibition.Thesubsequentlossofnormalsterolscorrelateswiththeaccumulation of14alpha-methyl

sterolsinfungiand mayberesponsible for the fungistaticactivityoffluconazole.Interactionstudieswith antipyrine

indicatethatsingleor multipledosesoffluconazole50mg do notaffect itsmetabolism.

Pharmacokinetics

Fluconazoleiswellabsorbedandoralabsorptionisnotaffectedbyconcomitant foodintake.Infastednormal

volunteers, peakplasma concentrationsoccurbetween1and 2hourspost dosewitha terminalplasma elimination

half-life ofapproximately30hours(range 20-50hours). Theapparentvolume ofdistributionapproximatestototal

bodywater.Plasma proteinbindingislow (11-12%).

N N N

N

N N

F

F OH

CanestenFluconazoleDataSheet

2April2009

Fluconazolehasbeenfound toachievegoodpenetrationintoalltissuesandbodyfluidsstudied.Thelevelsof

fluconazole in saliva andsputumare similar to plasma levels.

Themajor routeofexcretion isrenal,with approximately80%ofthe administereddose appearingin the urineas

unchangedmedicine.About11%ofthedoseisexcretedin theurineasmetabolites.Thepharmacokineticsof

fluconazole are markedlyaffectedbyreductionin renalfunction,howevernoadjustmentsin single-dosetherapy

are necessary.There isaninverse relationshipbetweenthe eliminationhalf-life andcreatinineclearance.

Thelongplasma elimination half-life providesthebasisfor single dose therapyforvaginalcandidiasis.

There are differencesin thepharmacokineticsbetweenadultsand children,withchildrenafter theneonatalperiod

generallyhavingfaster elimination rateand largervolume ofdistribution thanadults.

Microbiology

Fluconazoleadministered orallywasactiveina varietyofanimalmodelsoffungalinfectionsusingstandard

laboratorystrainsoffungi.

Fluconazoleexhibitsin vitroactivityagainstCryptococcusneoformansandCandidaspp.Activityhasbeen

demonstratedin vivoinnormaland immunocompromisedanimalsagainst infectionswithCandidaspp,including

systemiccandidiasisand innormalanimalswithC.neoformans, including intracranialinfections.Onecaseof

cross-resistance ofCandidatofluconazole in apatient(non-HIV)previouslytreatedwith ketoconazole hasbeen

reported.Theefficacyoffluconazolein vivoisgreaterthanwouldbeapparent fromin vitrotesting against the

above-mentionedfungi.

ConcurrentadministrationoffluconazoleandamphotericinBininfectednormalandimmunocompromisedmice

showedantagonismofthe two medicinesin systemicinfectionwithAspergillusfumigatus.Theclinicalsignificance

ofresultsobtainedin thesestudiesisunknown.

Indications

Canesten FluconazoleCapsule,givenorally,isindicatedfor vaginalcandidiasis.

Contraindications

Canesten FluconazoleCapsule should not beusedinpatientswithknown sensitivitytofluconazole;relatedazole

compounds;or to anyoftheexcipients.

Concomitant administrationwithcisaprideiscontraindicated.(SeeWarningsandPrecautions).

Warnings andPrecautions

Inrare cases, aswithotherazoles,anaphylaxishasbeen reported.

Fluconazolehasbeenassociatedwith rare casesofserioushepatictoxicityincludingfatalities, primarilyin patients

withseriousunderlying medicalconditions. In casesoffluconazole-associatedhepatotoxicity,noobvious

relationshiptototaldailydose,durationoftherapy,sexor ageofpatienthasbeenobserved.Canesten

FluconazoleCapsuleshould notbeusedagainifclinicalsignsand symptomsconsistentwithliverdisease develop

that maybeattributable to fluconazole(seeAdverse Effects).

Patientshave rarelydevelopedexfoliative cutaneousreactions, such asStevens-JohnsonSyndrome andtoxic

epidermalnecrolysis, during treatmentwithfluconazole.AIDSpatientsare moreproneto the development of

seriouscutaneousreactionstomanymedicines. Fluconazole should notbe usedagainifarash developswhichis

attributabletofluconazole.

CanestenFluconazoleDataSheet

2April2009

Some azoles,includingfluconazole,have been associatedwith prolongationofthe QTintervalonthe

electrocardiogram. Duringpost-marketingsurveillance, therehavebeenveryrarecasesofQTprolongationand

torsade de pointesin patientstakingfluconazole. These reportsincludedseriouslyillpatientswith multiple

confoundingriskfactors, such asstructuralheartdisease,electrolyteabnormalitiesand concomitantmedications

that mayhavebeencontributory(see Adverse Effects). Fluconazole should beadministeredwith caution to

patientswiththesepotentiallyproarrhythmicconditions(seeAdverseEffects).

UseinPregnancy(PregnancyCategoryD)

CategoryD. There arenoadequateandwell-controlledstudiesoffluconazole in pregnantwomen. There have

beenreportsofmultiple congenitalabnormalitiesin infantswhose motherswerebeing treatedfor 3or more months

withhighdose (400-800mg/day)fluconazole therapyfor coccidiomycosis. Therelationshipbetweenfluconazole

use and these eventsisunclear.

Adverse foetaleffectshavebeen seeninanimalsonlyathighdoselevelsassociatedwithmaternaltoxicity.

Fluconazoleshouldnotbeusedinwomenwho arepregnant,or inwomenofchildbearingpotentialunless

adequate contraceptionisemployed.

UseinLactation

Fluconazolehasbeenfound inhumanbreast milkatconcentrationssimilar tothose inplasma,henceitsusein

nursingmothersisnotrecommended.

Carcinogenesis,MutagenesisandImpairmentofFertility

Fluconazoleshowed no evidenceofcarcinogenicpotentialin mice andratstreated orallyfor 24 monthsatdosesof

2.5,5 or10 mg/kg/day(approximately2-7 timesthe recommended humandose). Male ratstreatedwith5 and10

mg/kg/dayhad an increased incidence ofhepatocellular adenomas.

Fluconazole,withorwithout metabolicactivation,wasnegativein testsformutagenicityin4 strainsofSalmonella

typhimuriumandin themouse lymphoma system. Cytogeneticstudiesin vivoandinvitroshowednoevidence of

chromosomalmutations.

Fluconazoledid notaffect the fertilityofmale orfemale ratstreatedorallywithdailydosesof5,10or20mg/kg or

withparenteraldosesof5,25or 75 mg/kg,althoughthe onsetofparturitionwasslightlydelayed at20mg/kgp.o.

Inanintravenousperinatalstudyin ratsat5, 20and 40 mg/kg,dystociaand prolongationofparturitionwere

observedin afewdamsat20mg/kg and40mg/kg,but notat5 mg/kg.Thedisturbancesin parturitionwere

reflectedbyaslightincrease inthenumberofstillbornpupsanddecrease ofneonatalsurvivalatthese dose levels.

Theeffectsonparturitioninratsare consistentwiththespeciesspecificoestrogen-loweringpropertyproduced by

high dosesoffluconazole.Such ahormone changehasnotbeen observed inwomentreatedwithfluconazole.

DrivingorUsingMachinery

Experiencewithfluconazolei ndicatesthat the therapyisunlikelytoimpairapatient’sabilityto driveor use

machinery.

Interactions

Therelevanceofthe followingmedicineinteractionstosingle-dose fluconazoleisunknown. Patientsonother

medicationsshouldbeadvisedtoconsulttheirdoctor orpharmacist before startingCanestenFluconazole Capsule.

Fluconazoleisan inhibitorofthe cytochrome P450 system, particularlytheCYP2C and toalesser extent the CYP

3Aisoforms.There are possibilitiesthatothermedicinesmayaffect the metabolismoffluconazole andthat

fluconazole mayaffect the metabolismofothermedicines. Invitro studiesconductedin humanhepatic

microsomes, demonstratethattheextentofinhibition ofCYP3Aisoformsislowest with fluconazole,when

comparedwithketoconazole and itraconazole.

CanestenFluconazoleDataSheet

2April2009

Azithromycin:Anopen-label, randomised, three-waycrossover studyin18healthysubjectsassessedtheeffect of

a single1200 mg oraldoseofazithromycin onthepharmacokineticsofasingle 800mg oraldose offluconazole as

wellasthe effectsoffluconazoleonthepharmacokineticsofazithromycin.Therewasnosignificant interaction

betweenfluconazole andazithromycin.

Hydrochlorothiazide. Concomitant oraladministrationof100 mg fluconazoleand50mg hydrochlorothiazidefor 10

daysinnormalvolunteersresulted in an increase of41% in C

andanincreaseof43% inAUC offluconazole,

comparedtofluconazolegivenalone. An effect ofthismagnitude shouldnotnecessitatea changeinthe

fluconazole doseregimenin subjectsreceivingdiuretics, althoughtheprescribershould bear itinmind.

Rifampicin.Administrationofasingle oral200 mg dose offluconazole after chronicrifampicin administration

resultedin a25% decreaseinAUCanda 20% shorter half-life offluconazoleinnormalvolunteers. Dependingon

clinicalcircumstances, anincrease ofthedoseoffluconazole should be consideredwhenitisadministeredwith

rifampicin.

Cisapride.Cardiaceventsincludingtorsadesdepointeshave beenreported in patientsreceiving fluconazoleand

cisapride concomitantly.Inmost ofthese cases, thepatientsappearto havebeenpredisposedto arrhythmiasor

had seriousunderlying illness. Acontrolledstudyfound that concomitant fluconazole200mg once dailyand

cisapride 20mg fourtimesa dayyieldeda significantincrease in cisaprideplasma levelsand prolongation ofQTc

interval. Co-administrationofcisaprideiscontraindicatedin patientsreceivingfluconazole (seeContraindications).

Cyclosporin.Akineticstudyin renaltransplantpatientsfoundfluconazole200mgdailytoslowlyincrease

cyclosporin concentrations.However,inanothermultiple dose studywith100 mg daily,fluconazoledid notaffect

cyclosporinlevelsinpatientswithbone marrowtransplants. Cyclosporinplasma concentration monitoringin

patients,withorwithoutimpaired renalfunction, receivingfluconazole isrecommended.

OralContraceptives.Three kineticstudieswitha combinedoralcontraceptive havebeen performedusingmultiple

dosesoffluconazole.Therewerenorelevant effectsoneither hormone levelin the50 mg fluconazole study, while

at200 mg dailytheAUC’sofethynylestradiolandlevonorgestrelwere increased40% and24% respectively. In a

300 mg onceweekly fluconazole study, the AUC’sofethynylestradiolandnorethindronewereincreased by24%

and13% respectively.Thus,multipledoseuse offluconazole at these dosesisunlikelytohaveaneffect onthe

efficacyofthe combined oralcontraceptive.

OralHypoglycaemicAgents.Theeffectsoffluconazole onthepharmacokineticsofthe sulphonylurea oral

hypoglycaemicagentstolbutamide, glipizideandglibenclamidewereexamined inthreeplacebo-controlled

crossover studiesinnormalvolunteers.Allsubjectsreceivedthesulphonylurea aloneand following treatment with

100 mg offluconazoleasasingle dailyoraldose for 7days.Fluconazole administration resultedin significant

increasesin C

and AUCofthe sulphonylurea.Severalsubjectsin these three studiesexperienced symptoms

consistentwith hypoglycaemia.Intheglibenclamidestudy, severalvolunteersrequired oralglucosetreatment.As

fluconazole isapotentinhibitorofCYP2C8andCYP2C9, it mayalsointeractwithothersulphonylureas(eg.

glimepirideandgliclazide)and thethiazolidinediones(eg. pioglitazone androsiglitazone),whichare metabolisedby

these enzymes.When fluconazole andsulphonylureasor thiazolidinedionesareco-administered,bloodglucose

concentrationsshould be monitored carefully. Thepossibilityofahypoglycaemicepisodeshould be borneinmind.

Phenytoin.Concomitant administrationoforalfluconazole (200 mg) withphenytoin at steadystate resultedinan

averageincreaseof75% ofphenytoin AUCvaluesin normalvolunteers. Carefulmonitoringofphenytoin

concentrationsinpatientsreceiving fluconazole and phenytoinisrecommended.

Short-actingBenzodiazepines.Studiesinhumansubjectshave reported changesin midazolampharmacokinetics

and clinicaleffectsthataredependenton dosageand routeofadministration.Singledosesoffluconazole150 mg

resultedin modest increasesin midazolamconcentrationsand psychomotoreffectsfollowingoraladministrationof

10mg that maynotbeclinicallysignificant.At dosesusedtotreatsystemicmycoses, fluconazole resultedin

substantialincreasesin midazolamconcentrationsand psychomotoreffectsfollowingoraladministrationof

midazolam7.5 mg,but onlymodest increasesthatarenotlikelytobe clinicallysignificant followingintravenous

infusionofmidazolam0.05mg/kg.Ifconcomitant benzodiazepinetherapyisnecessaryinpatientsbeingtreated

withfluconazole,considerationshouldbegiventodecreasing the benzodiazepinedosage, and the patientsshould

beappropriatelymonitored.

Rifabutin.Therehave been reportsthataninteractionexistswhen fluconazoleisadministered concomitantlywith

rifabutin, leading toincreasedserumlevelsofrifabutin.There have beenreportsofuveitisin patientstowhom

fluconazole and rifabutinwere co-administered.Patientsreceivingrifabutinand fluconazole concomitantlyshould

becarefullymonitored.

CanestenFluconazoleDataSheet

2April2009

Tacrolimus.There have beenreportsthataninteraction existswhenfluconazole isadministered concomitantly

withtacrolimus, leadingtoincreasedserumlevelsoftacrolimus.There havebeenreportsofnephrotoxicityin

patientstowhomfluconazole andtacrolimuswere co-administered.Patientsreceivingtacrolimusand fluconazole

concomitantlyshouldbecarefullymonitored.

Theophylline.In aplacebocontrolledinteractionstudy,theadministrationoffluconazole200mg for 14 days

resultedin an18%decrease inthemean plasma clearance oftheophylline.Patientswhoare receivinghighdose

theophylline orwhoare otherwise atincreasedriskoftheophylline toxicityshouldbeobserved for signsof

theophylline toxicitywhile receiving fluconazole,andtherapymodifiedappropriatelyifsignsoftoxicitydevelop.

Warfarin.Asingle dose ofwarfarin(15mg) givento normalvolunteers, following14daysoforallyadministered

fluconazole (200 mg) resultedin a12%increaseintheprothrombin time response (areaunder theprothrombin

time-time curve).Oneof13subjectsexperienceda2-fold increase in hisprothrombin time response.Inpost-

marketingexperience,aswithotherazole antifungals,bleedingevents(bruising,epistaxis,gastrointestinal

bleeding,haematuriaandmelaena) havebeenreportedin associationwithincreasesinprothrombin time in

patientsreceiving fluconazole concurrentlywithwarfarin.Carefulmonitoringofprothrombin time inpatients

receiving fluconazoleand coumarin-typeanticoagulantsisrecommended.

Zidovudine.TheAUC ofzidovudinesignificantlyincreased(74%)duringco-administrationwith fluconazole.

Patientsreceiving thiscombinationshould be monitoredfor thedevelopment ofzidovudine-relatedadverse

reactions.

GastrointestinalMedicines.Infastednormalvolunteers, absorptionoforallyadministeredfluconazoledoesnot

appear tobeaffectedbyagentsthatincrease gastricpH.Singledoseadministrationoffluconazole (100mg) with

cimetidine(400mg) resulted ina13% reduction inAUC and21% reductioninC

offluconazole.Administration

ofanantacid containingaluminiumandmagnesiumhydroxidesimmediatelyprior to asingle dose offluconazole

(100 mg) hadno effect on theabsorptionor elimination offluconazole.

Physiciansshouldbealertto thepotentialfor interactionswithother medicinesfor whichpharmacokinetic

interaction studieshave notbeen conducted.

AdverseReactions

Fluconazoleisgenerallywelltolerated.

Themost commonundesirable effectsobservedduring vaginalcandidiasisclinicaltrialsandassociatedwith

fluconazolewithanincidence >1%are:

Nervous System Disorders:Headache.

GastrointestinalDisorders:Nausea,abdominalpain,diarrhoea,dyspepsia.

Inaddition,the uncommonundesirable effectsobserved duringvaginalcandidiasisclinicaltrialsassociatedwith

fluconazole are:

Dermatological:Pruritus,genitalpruritus, rash,erythematousrash,dryskin,abnormalskin odour, urticaria.

Nervous System Disorders:Dizziness, flushing, drymouth,vertigo,hyperkinesia,hypertonia,tasteperversion.

GastrointestinalDisorders:Vomiting,anorexia, flatulence,constipation,loosestools.

Metabolic:Thirst.

Psychiatric:Insomnia,nervousness, female sexualdysfunction.

Reproductive:Intermenstrualbleeding, dysmenorrhoea,leucorrhoea, menorrhagia,uterinespasm, vaginal

disorder.

Respiratory:Pharyngitis.

Specialsenses:Tasteperversion,abnormalvision,visualfield defect.

Urinary:Polyuria,renalpain.

General:Fatigue,hotflushes, malaise,backpain,herpessimplex, pain,rigors.

Thefollowingadverse eventshave occurredduringexperiencewithoverallfluconazoleuse:

CanestenFluconazoleDataSheet

2April2009

BloodandLymphaticSystem Disorders:Leukopenia includingneutropenia and agranulocytosis,

thrombocytopenia.

CardiovascularDisorders:QTprolongation,torsadedepointes(seeWarningsandPrecautions).

Nervous System Disorders:Seizures.

Immune SystemDisorders:Anaphylaxis(including face oedema,angioedema,urticariaandpruritus).

MetabolicandNutritionalDisorders:Hypercholesterolemia,hypertriglyceridemia and hypokalemia.

HepatobiliaryDisorders:Hepaticfailure, hepatitis, hepatocellular necrosis, jaundice.

SkinandSubcutaneous Tissue Disorders:Alopecia,exfoliative skin disordersincludingStevens-Johnson

Syndrome andtoxicepidermalnecrolysis.

DosageAndAdministration

Canesten FluconazoleCapsuleisadministered orally.

UseinAdults

For vaginalcandidiasis,CanestenFluconazole Capsuleshouldbeadministeredasasingleoraldose.

Themediantime to onsetofsymptomrelieffollowing a150mg oraldose for the treatment ofvaginalcandidiasisis

oneday. Therange oftime to onset ofsymptomsreliefisonehour tonine days.

Usein Children

Single dose fluconazoleisnot recommended for use in childrenunder18yearsofage exceptunder doctor

supervision.

Usein RenalImpairment

Fluconazoleispredominantlyexcretedin theurineasunchangedmedicine.No adjustmentsin single-dose therapy

are necessaryinpatientswithminortomoderaterenalimpairment.

Overdosage

There have beenreportsofoverdosagewithfluconazole andinone case, a42-year-oldpatientinfectedwith

humanimmunodeficiencyvirusdevelopedhallucinationsandexhibitedparanoidbehaviourafter reportedly

ingesting 8,200 mg offluconazole.Thepatientwasadmitted to hospital,andhisconditionresolvedwithin48

hours.

Inthe event ofoverdosage,symptomatictreatment (with supportive measuresandgastriclavageifnecessary)

should beundertaken.

Fluconazoleislargelyexcretedintheurine;forcedvolume diuresiswouldprobablyincrease the eliminationrate. A

three hourhaemodialysissessiondecreasesplasma levelsbyapproximately50%.

PharmaceuticalPrecautions

Storebelow25ºC.

PresentationsandPack Sizes

Canesten FluconazoleCapsuleblister pack: Packsofone fluconazole 150mg capsule.

CanestenFluconazoleDataSheet

2April2009

Medicine Classification

Pharmacist OnlyMedicine

Name andAddress

Bayer New ZealandLimited

Consumer Care Division

C. P. O.Box2825

Auckland

Ph:(09)4433093

Fax: (09) 443 3094

DateofPreparation

2 April2009

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