CITANEST 4% DENTAL INJECTION

Main information

  • Trade name:
  • CITANEST 4% DENTAL INJECTION
  • Dosage:
  • 40mg/ml Per Cent
  • Pharmaceutical form:
  • Unknown
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • CITANEST 4% DENTAL INJECTION
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA1045/002/001
  • Authorization date:
  • 01-04-2000
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

PartII

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

CitanestPlainDental,PrilocaineHydrochloride4%w/vSolutionforInjection.

2QUALITATIVEANDQUANTITATIVECOMPOSITION

EachmlcontainsPrilocaineHydrochloride40mg,(88mgper2.2mlcartridge).

Forlistofexcipients,seesection6.1.

3PHARMACEUTICALFORM

SolutionforInjection.

2.2mlglasscartridgecontainingasterileclearaqueoussolution.

4CLINICALPARTICULARS

4.1TherapeuticIndications

CitanestPlainDentalisalocalanaestheticforuseindentalinfiltrationanaesthesiaanddentalnerveblocktechniques.

4.2Posologyandmethodofadministration

Injectionsshouldalwaysbemadeslowlywithcarefulaspirationbeforeandintermittentlyduringinjectionto

avoidinadvertentintravascularinjection,whichmayhavetoxiceffects.

Thelowestdosethatresultsineffectiveanaesthesiashouldbeused.Thedosewillalsodependontheareaoforal

cavitytobeanaesthetised,thevascularityoftheoraltissuesandtechniqueofanaesthesia.Thetotaldosemustbe

adjustedtotheage,sizeandphysicalstatusofthepatient.

Foreffectivelocalanaesthesiainmostdentalprocedures,anadequatedoseofCitanestPlainDentalsolution

injectedintothetissueis:

Innormallyhealthyadults:1-2ml(=40-80mgprilocainehydrochloride).

Childrenunder10yearsofage:~1ml(=~40mgprilocainehydrochloride).

Duetothespecificneedforbonepenetration,dentallocalanaestheticscontainhighconcentrationsoftheactive

agent(e.g.40mg/mlforCitanestPlainDental).Acombinationofahighpressureinducedbytheuseofadental

cartridgesystemandarapidrateofinjectionmayleadtocomplications(seesection4.9.Overdose)evenafterthe

injectionofsmallamountsoflocalanaestheticduetohighconcentration,especiallyfollowingaccidental

intravascularinjection,whentheinjecteddrugcouldtravelinaretrogrademanneralongthevesseland,incases

ofintra-arterialinjectionintheheadandneckarea,reachthebrainwithoutthesamedegreeofdilutionthat

occurswithanintravenousinjection.Forroutinedentalprocedures,therecommendeddoseis1-2mlandadose

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 17/07/2008 CRN 2034461 page number: 1

4.3Contraindications

Knownhistoryofhypersensitivitytolocalanaestheticagentsoftheamidetypeortoothercomponentsofthesolution.

Congenitaloridiopathicmethaemoglobinaemia.

4.4Specialwarningsandprecautionsforuse

Thesafetyandeffectivenessofthelocalanaestheticagent,prilocainehydrochloride,dependontheproperdosage,the

correctinjectiontechnique,adequateprecautionsandreadinessforemergencies.

Beforeadministrationalocalanaestheticdrug,makesurethatresuscitativeequipment,suchasequipmentrequiredfor

oxygenationandassistedventilation,anddrugsforthetreatmentoftoxicreactionsareimmediatelyavailable.

Thepatientshouldbeadvisedtoexertcautiontoavoidinadvertenttraumatothelips,tongue,cheekmucosaorsoft

palatewhenthesestructuresareanaesthetised.Theingestionoffoodshouldthereforebepostponeduntilnormal

functionreturns.

Intheheadandneckareatheintravascularinjectionofevensmalldosesoflocalanaestheticsmaycausesystemic

adversereactionssimilartothoseseenaftertheinadvertentintravascularinjectionoflargerdosesinotherareas.

Even,ifthedoseofCitanestPlainindentalpracticeisgenerallysmall,somepatientsmayrequirespecialattentionto

reducetheriskofdangeroussideeffects:

Patientswithpartialorcompleteheartblockduetothefactthatlocalanaestheticsmaydepressmyocardial

conduction.

Patientswithadvancedliverdiseaseorsevererenaldysfunction.

Theelderlyandpatientsinpoorgeneralcondition.

Patientswithepilepsyandimpairedrespiratoryfunction.

Localanaestheticsshouldbeadministeredwithcautiontopatientswithsevereoruntreatedhypertension,severeheart

disease,severeanaemiaorcirculatoryfailurefromwhatevercauseoranyotherpathologicalcondition.Local

anaestheticsshouldbeavoidedwhenthereisinflammationintheregionoftheproposedinjection.

Citanest4%isinasingledosevialforuseononepatientduringonetreatmentonly.Theremainingcontentsshouldbe

discarded.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Prilocaineshouldbeusedwithcautioninpatientsreceivingantiarrhythmicdrugs,sincethetoxiceffectsareadditive.

Drugswhichmaypredisposetomethaemoglobinformation,e.g.sulfonamides,antimalarialsandcertainnitric

compounds,couldpotentiatethisadverseeffectofprilocaine.

4.6Pregnancyandlactation

Althoughsafeuseofprilocaineduringpregnancyhasnotbeenestablishedwithrespecttopossibleadverseeffectsupon

foetaldevelopment,itisreasonabletoassumethatCitanestPlainDentalhasbeenadministeredtoalargenumberof

pregnantwomenandwomenofchildbearingage.Nospecificdisturbancestothereproductiveprocesshavesofarbeen

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 17/07/2008 CRN 2034461 page number: 2

Methaemoglobinaemiaintheneonatehasbeenreportedaftertheadministrationofprilocainetothemotherindoses

exceeding600mg.

Prilocainemayenterthemother’smilk,butinsuchsmallamountsthatthereisgenerallynoriskofthisaffectingthe

neonate.

4.7Effectsonabilitytodriveandusemachines

Dependingondosage,localanaestheticsmayhaveaverymildeffectonmentalfunctionandmaytemporarilyimpair

locomotionandco-ordination.

4.8Undesirableeffects

ReactionstoCitanestPlainareveryrareinthedosesusedindentalprocedures.Ifadversereactionsoccur,theyare

similarincharactertothoseobservedwithotherlocalanaesthetics.Psychogenicreactionsinanticipationoforduring

thedentalprocedureare,however,commonandmaymimicthesymptomsofageneralizedsystemicreactiontolocal

anaesthetics.

Allergicreactions

Allergicreactions(inthemostsevereinstancesanaphylacticshock)tolocalanaestheticsoftheamidetypearerare.

Neurologicalcomplications

Theincidenceofadverseneurologicalreactions(e.g.persistentneurologicaldeficit)associatedwiththeuseoflocal

anaestheticsisverylow.Neurologicalreactionsmaybedependentupontheparticulardrugused,therouteof

administrationandthephysicalstatusofthepatients.Manyoftheseeffectsmaybelinkedtotheinjectiontechniques,

withorwithoutacontributionbythedrug(seesection4.4,Specialwarningsandprecautionsforuse).Neurological

reactionsfollowingregionalnerveblockshaveincludedpersistentparaesthesiaandsensorydisturbances.

Acutesystemictoxicity

Prilocainecancauseacutetoxiceffectsifhighsystemiclevelsoccurduetoaccidentalintravascularinjection,fast

absorptionoroverdosage.(seesection5.1,Pharmacodynamicpropertiesandsection4.9,Overdose).

Methaemoglobaemia

Cyanosisduetotheformationofmethaemoglobinmayoccuraftertheadministrationofprilocaine.Therepeated

administrationofprilocaine,eveninrelativelysmalldoses,canleadtoclinicallyovertmethaemoglobinaemia.

Theconversionofhaemoglobintomethaemoglobiniscausedbytheprilocainemetabolite,orthotoluidine,whichhasa

longhalf-lifeandtendstoaccumulate,andinturn,itsconversionto4-and6-hydroxytoluidine.Methaemoglobinhave

risentoclinicallysignificantlevelsinpatientsreceivinghighdosesofprilocaine.Cyanosisoccurswhenthe

methaemoglobinconcentrationinthebloodreaches1-2g/100ml(6-12%ofthenormalhaemoglobinconcentration).

Methaemoglobinoxidisesonlyslowlybacktohaemoglobin,butthisprocesscanbegreatlyacceleratedbygiving

methylenebluei.v.(seesection4.9,Overdose)

Thereductionintheoxygen-carryingcapacityinnormalpatientsismarginal;hencethecyanosisisusually

symptomless.However,inseverelyanaemicpatientsitmaycausesignificanthypoxaemia.Itisimportanttoruleout

othermoreseriouscausesofcyanosissuchasacutehypoxaemiaandand/orheartfailure.Inthedentaldosageof

prilocaine(1-2mlCitanestPlain,i.e.40-80mgprilocainehydrochloride),theoccurrenceofmethaemoglobinaemiain

dentalpracticeappearsremote.However,grossoverdosageindentalpracticehasbeenreportedtocause

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 17/07/2008 CRN 2034461 page number: 3

Note.Evenlowconcentrationsofmethaemoglobinmayinterferewithpulseoximetryreadings,includingafalselow

oxygensaturation.

4.9Overdose

Sinceprilocaineistheleasttoxicoftheamino-amidelocalanaesthetics,itisparticularlyusefulinsituationswhenhigh

dosagemaybeneeded.Thisadvantage,however,shouldbeweighedagainsttheriskofcausing

methaemoglobinaemia.

Acuteemergenciesare,ingeneral,dose-relatedandmayresultfromhighplasmalevelscausedbyexcessivedosage,

rapidabsorption(i.e.rateofincreaseplasmaconcentration)orunintentionalintravascularinjection,ormayresultfrom

hypersensitivityordiminishedtoleranceonthepartofthepatient.

Acutesystemictoxicity

CNSreactionsareexcitatoryordepressantandmaybecharacterizedbynervousness,tinnitus,twitching,euphoria,

drowsiness,blurredordoublevision,dizziness,convulsions,unconsciousnessandpossiblyrespiratoryarrest.The

excitatoryreactionsmaybeverybrieformaynotoccuratall,inwhichcasethefirstmanifestationoftoxicityis

drowsinessmergingintounconsciousnessandevenrespiratoryarrest.

Cardiovascularreactionsaredepressantandmaybecharacterizedbyhypotension,myocardialdepression,bradycardia

andpossiblycardiacarrest.Signsandsymptomsofdepressioncardiovascularfunctionmaycommonlyresultfroma

vasovagalreaction,particularlyifthepatientisinanuprightposition.Lesscommonly,theymayoccurasadirecteffect

ofthedrug.Failuretorecognizepremonitorysignssuchassweating,afeelingoffaintness,changesinpulseor

sensoriummayresultinprogressivecerebralhypoxiaandseizureorseriouscardiovascularcollapse.

Cardiovasculareffectsareusuallyonlyseeninthemostseverecasesandaregenerallyprecededbysignsoftoxicityin

thecentralnervoussystem.

Acidosisorhypoxiainthepatientmayincreasetheriskandseverityoftoxicreactions.Suchreactionsinvolvethe

centralnervoussystemandthecardiovascularsystem.

Treatmentofacutetoxicity

Theimmediatetreatmentofacutesystemictoxicityisasfollows:

Putthepatientisasupineposition.Raisethelegs30 °

abovethehorizontallevel.

b.Ensureapatentairway.Ifventilationisinadequate,ventilatethepatient,withoxygenifavailable.Thisis

importantsincetoxicityincreaseswithacidosis.

Thetreatmentofconvulsionsconsistsinensuringapatentairwayandarrestingconvulsions.Shouldconvulsions

persistdespiteadequateventilation,5-15mgdiazepamor50-200mgthiopentonesodiumshouldbeadministered

intravenously(toarresttheconvulsions).Sincethistreatmentmayalsodepressrespiration,themeansof

mechanicallysupportingorcontrollingventilationshouldbeavailable.

d.Supportivetreatmentofcirculatorydepressionmayrequiretheadministrationofintravenousfluidsand,when

appropriate,avasopressor(e.g.ephedrine5-10mgi.v.andrepeated,ifnecessary,after2-3min)asgovernedby

theclinicalsituation.

Ifthepatientisunresponsiveandthecarotidpulserateistotallyabsent,indicatingcardiacarrest,effective

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 17/07/2008 CRN 2034461 page number: 4

Treatmentofacutemethaemoglobinaemia

Ifclinicalmethaemoglobinaemiaoccurs,itcanberapidlytreatedbyasingleintravenousinjectionofa1%methylene

bluesolution,1mg/kgbodyweight,overa5minuteperiod.Cyanosiswilldisappearinabout15minutes.Thisdose

shouldnotberepeatedasmethyleneblueinhighconcentrationsactsasahaemoglobinoxidant.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacotherapeuticgroup:Anaesthetics,localamides.

ATCcode:NO1BB04.

Prilocaine,likeotherlocalanaesthetics,causesareversibleblockadeofimpulsepropagationalongnervefibresby

preventingtheinwardmovementofsodiumionsthroughthenervemembrane.Localanaestheticsoftheamidetypeare

thoughttoactwithinthesodiumchannelsofthenervemembrane.

Localanaestheticdrugsmayalsohavesimilareffectsonexcitablemembranesinthebrainandmyocardium.If

excessiveamountsofdrugreachthesystemiccirculationrapidly(seesection4.2,Posologyandmethodof

administration),symptomsandsignsoftoxicitywillappear,emanatingmainlyfromthecentralnervousand

cardiovascularsystems.

Centralnervoussystemtoxicity(seesection4.9,Overdose)usuallyprecedesthecardiovasculareffectsasitoccursat

lowerplasmaconcentrations.Directeffectsoflocalanaestheticsontheheartincludeslowconduction,negative

inotropismandeventuallycardiacarrest.

5.2Pharmacokineticproperties

PrilocainehasapKaof7.9andanN-heptane/pH7.4bufferpartitioncoefficientof0.9.

Prilocaineisbetween40%and55%proteinboundinplasma,mainlytoalpha1-acidglycoprotein.

Prilocaineredistributesrapidlyfromthebloodandithasalargeapparentdistributionvolumeofbetween190Land

260L.

Theterminaleliminationhalf-lifeofprilocaineis1.6h.

Prilocainereadilypassestheplacentaandfreeplasmaconcentrationsaresimilarinbothfoetusandmother.Inthe

presenceoffetalacidosis,theymaybeslightlyhigherinthefoetus,duetoiontrapping.Informationconcerningthe

eliminationhalf-lifeofprilocaineinneonatesisnotavailable.

Intheliver,prilocaineisprimarilymetabolisedbyamidehydrolysistoo-toluidineandN-propylamine.o-Toluidineis

subsequentlyhydroxylatedto2-amino-3-hydroxytolueneand2-amino-5-hydroxytoluenemetaboliteswhichare

believedtoberesponsiblefortheoccurrenceofmethaemoglobinaemia.

Onlyasmallproportionofprilocaine(lessthat5%)isexcretedunchangedintheurine.Invitroandanimalstudieshave

shownmetabolismofprilocainebythelungandkidneytissues.

5.3Preclinicalsafetydata

Thereisnopreclinicaldataofrelevancetotheprescriber,whichisadditionaltothatalreadyincludedinothersections

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 17/07/2008 CRN 2034461 page number: 5

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

SodiumChloride

SodiumHydroxide

HydrochloricAcid

WaterforInjections

6.2Incompatibilities

Noneknown.

6.3ShelfLife

3years.

6.4Specialprecautionsforstorage

Donotstoreabove25ºC.

6.5Natureandcontentsofcontainer

2.2mlcolourlessborosilicateglass(Ph.Eur.Type1).Eachcartoncontains100cartridges.Eachcartridgecontainsa

rubberplungerandhasanaluminiumandrubbercombinationcap.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Useononepatientduringonetreatmentonly.Discardunusedcontents.

7MARKETINGAUTHORISATIONHOLDER

DentsplyLimited

HammMoorLane

Addlestone

Weybridge

SurreyKT152SE

UnitedKingdom

TradingasDentsplyPharmaceuticals

8MARKETINGAUTHORISATIONNUMBER

PA1045/002/001

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation: 01April1980

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 17/07/2008 CRN 2034461 page number: 6

10DATEOFREVISIONOFTHETEXT

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 17/07/2008 CRN 2034461 page number: 7