Ropivacaine vs Bupivacaine

Ropivacaine is a recently launched local anesthetic in Iran. Because of its more safety profile, it would be an appropriate substitution for routinely used LA, Bupivacaine.

1. ROPIVACAINE VS BUPIVACAINE
Dr. Reza Aminnejad
Assistant Professor Of
Anesthesiology & Critical
Care
Qom University Of
Medical Sciences
22 August 2019 REZA AMINNEJAD, MD.

2. CONTEXT
RopivacainetheS-enantiomeremergedasapossible
replacementofBupivacainewithoutundesirabletoxic
effects.(1)
Ropivacaineisalong-actingamidelocalanaesthetic
agentandfirstproducedasapureenantiomer.(2)
1. KaurA,SinghRB,TripathiRK,ChoubeyS.Comparisionbetween
bupivacaineandropivacaineinpatientsundergoingforearmsurgeriesunder
axillarybrachialplexusblock:aprospectiverandomizedstudy.JClinDiagnRes.
2015;9(1):UC01-UC6.
2. KuthialaG,ChaudharyG.Ropivacaine:Areviewofitspharmacologyand
clinicaluse.IndianJAnaesth.2011;55(2):104-10.
REZA AMINNEJAD, MD.

3. REZA AMINNEJAD, MD.

4. MECHANISM OF ACTION
Ropivacaineproduceseffectssimilartootherlocal
anaestheticsviareversibleinhibitionofsodiumioninflux
innervefibers.(2)
Ropivacaineislesslipophilicthanbupivacaineandis
lesslikelytopenetratelargemyelinatedmotorfibers.
therefore,ithasselectiveactiononthepain-transmitting
AδandCnervesratherthanAβfibers,whichareinvolved
inmotorfunction.(2)
2. KuthialaG,ChaudharyG.Ropivacaine:Areviewofitspharmacologyand
clinicaluse.IndianJAnaesth.2011;55(2):104-10.
REZA AMINNEJAD, MD.

5. PHARMACODYNAMICS
REZA AMINNEJAD, MD.

6. LIPOPHILICITY
Ropivacaineislesslipophilicthanbupivacaine.(2)
Thereducedlipophilicityisalsoassociatedwith
decreasedpotentialforcentralnervoussystemtoxicity
andcardiotoxicity.(2)
Significantchangesincardiacfunctioninvolvingthe
contractility,conductiontimeandQRSwidthoccurred
andtheincreaseinaQRSwidthwasfoundtobe
significantlysmallerwithropivacainethanwith
bupivacaine.(3,4)
2. KuthialaG,ChaudharyG.Ropivacaine:Areviewofitspharmacologyand
clinicaluse.IndianJAnaesth.2011;55(2):104-10.
3. GrafBM.Thecardiotoxicityoflocalanesthetics:Theplaceof
ropivacaine.CurrTopMedChem.2001;1:207–14.
4. CederholmI,EversH,LöfströmJB.Skinbloodflowafterintradermal
injectionofropivacaineinvariousconcentrationswithandwithoutepinephrine
evaluatedbylaserDopplerflowmetry.RegAnesth.1992;17:322–8.
REZA AMINNEJAD, MD.

7. OTHER EFFECTS
Ropivacainehasbeenshowntoinhibitplatelet
aggregationinplasmaatconcentrationsof3.75and
1.88mg/mL(0.375%and0.188%),whichcorrespondto
thosethatcouldoccurintheepiduralspaceduring
infusion.(2)
Likeotheranaesthetics,ropivacainehasantibacterial
activityinvitro,inhibitingthegrowthofStaphylococcus
aureus, Escherichia coli,and Pseudomonas
aeruginosa.(2)
2. KuthialaG,ChaudharyG.Ropivacaine:Areviewofitspharmacologyand
clinicaluse.IndianJAnaesth.2011;55(2):104-10.
REZA AMINNEJAD, MD.

8. PHARMACOKINETICS
Ropivacainerapidlycrossestheplacentaduringepidural
administrationforcaesareansection,resultinginnear
completeequilibriumofthefreefractionofropivacaine
inthematernalandfetalcirculation.However,thetotal
plasmaconcentrationofropivacainewaslowerinthe
fetalcirculationthaninthematernalcirculation,
reflectingthebindingofropivacainetoα1-acid
glycoprotein,whichismoreconcentratedinmaternal
thaninfetalplasma.(2)
2. KuthialaG,ChaudharyG.Ropivacaine:Areviewofitspharmacologyand
clinicaluse.IndianJAnaesth.2011;55(2):104-10. REZA AMINNEJAD, MD.

9. METABOLISM AND EXCRETION
Metabolism in the liver
(cytochrome P450 (CYP) 1A2 and
CYP3A4)
Excretion in urine (86%)
REZA AMINNEJAD, MD.

10. RELATIVE POTENCY
Ropivacainehassimilarpotencytobupivacaineat
higherdoses(eg,dosesrequiredforperipheralnerve
blocksforsurgicalanaesthesia),
Ropivacaineislesspotentthanbupivacaineatlower
doses,suchasthoseusedforepiduralorintrathecal
analgesia.(2)
2. KuthialaG,ChaudharyG.Ropivacaine:Areviewofitspharmacologyand
clinicaluse.IndianJAnaesth.2011;55(2):104-10.
REZA AMINNEJAD, MD.

11. TOLERABILITY
Thesame complicationrateasbupivacaine
(hypotension(32%),nausea(17%),vomiting(7%),
bradycardia(6%),andheadache(5%)).(2)
Theincidenceofropivacaine-inducedcardiovascular
symptomsmaybeage-related.(5)
Thecardiovasculareventsarealsorelatedtotoxicity
duetosuddenIVinjectionormassiveabsorptionfrom
peripheralnerveblocks.(2)
2. KuthialaG,ChaudharyG.Ropivacaine:Areviewofitspharmacologyand
clinicaluse.IndianJAnaesth.2011;55(2):104-10.
5. SimonMJ,VeeringBT,StienstraR,vanKleefJW,BurmAG.Theeffectsof
ageonneuralblockadeandhemodynamicchangesafterepiduralanesthesiawith
ropivacaine.AnesthAnalg.2002;94:1325–30.
REZA AMINNEJAD, MD.

12. InchildrenRopivacainewasgenerallywelltoleratedin
paediatricpatientsagedfrom1monthto15yearsregardless
oftherouteofadministration.Theoverallincidenceofadverse
eventsassociatedwithropivacaineappearedtobelow,with
nauseaand/orvomitingoccurringmostfrequently.(6)
InexposedfoetusesandneonatesRopivacainewasgenerally
welltoleratedinthefoetusorneonatefollowingtheuseof
regionalanaesthesiainwomenundergoingCaesareansection
orduringlabour.Themostcommonfoetalorneonataladverse
eventswithropivacainewerefoetalbradycardia(12%),neonatal
jaundice(8%),andunspecifiedneonatalcomplications(7%).
Theseeventsoccurredwithsimilarfrequencywithbupivacaine
(12%,8%,and7%,respectively).(7)
6. BosenbergA,ThomasJ,LopezT,LybeckA,HuizarK,LarssonLE.Theefficacyof
caudalropivacaine1,2and3mg/mlforpostoperativeanalgesiainchildren.PaediatrAnaesth.
2002;12:53–8.
7. SimpsonD,CurranMP,OldfieldV,KeatingGM.Ropivacaine:Areviewofitsusein
regionalanaesthesiaandacutepainmanagement.Drugs.2005;65:2675–717.
REZA AMINNEJAD, MD.

13. Accordingtoameta-analysisofsixdouble-blindtrials,
ropivacainedidnotinfluencetheneonatalneurological
andadaptivecapacity(NAC)scoreat2hoursafter
deliveryand,at24hoursafterdelivery,totalNACscores
weresignificantlyhigherinneonateswhosemothershad
receivedropivacaineratherthanbupivacaine(P<0.05).
(8)
8. WriterWD,StienstraR,EddlestonJM,GattSP,GriffinR,GutscheBB,etal.
Neonataloutcomesandmodeofdeliveryafterepiduralanalgesiawithropivacaine
andbupivacaine:Aprospectivemeta-analysis.BrJAnaesth.1998;81:713–7.
REZA AMINNEJAD, MD.

14. CARDIOTOXICITY AND CNS
TOXICITY IN COMPARISON TO
BUPIVACAINE
Theincidenceofcardiotoxicityandcentralnervoussystem
(CNS)toxicityasaresultofinadvertentintravascularinjection
ofropivacaineappearstobelow.Accordingtoapooled
analysisofdatafrom≈3000patientsin60clinicalstudies,the
incidenceofprobableaccidentalIVinjectionofropivacainewas
≈0.2%(sixpatients)andonlyonepatientexperienced
convulsions;nopatientshowedsymptomsofcardiotoxicity.(9)
Theconvulsivelocalanaestheticdosesofbupivacaineand
ropivacainewerestudiedindifferentanimalmodels;
bupivacainehasa1.5-to2.5-foldlowerconvulsivethreshold
whencomparedtoropivacaine.Onthebasisofanimaland
volunteerstudies,itcanbeconcludedthatropivacaineseems
tobelessneurotoxicandcardiotoxicthanbupivacaine.(9)
9. SelanderD,SjovallJ,WaldenlindL.Accidentali.vinjectionsof
ropivacaine:Clinicalexperienceofsixcases[abstract]RegAnaesth.1997;22:70.REZA AMINNEJAD, MD.

15. REZA AMINNEJAD, MD.

16. CLINICAL APPLICATION
Surgical anaesthesia
REZA AMINNEJAD, MD.

17. Epiduraladministration
Caesareansection(ropivacaine(0.75%or0.5%)providesa
clinicallysimilaronsetofsensoryandmotorblocktothatof
bupivacaine0.5%.Themediandurationofanalgesiawithin
dermatomesrelevantforsurgery(T6–S3)was1.7–4.2hours
forropivacaineand1.8–4.4hoursforbupivacaine,butthe
mediandurationofcompletemotorblockwassignificantly
longerwithbupivacainethanwithropivacaine(2.5vs0.9
hours,P<0.05).(10))
Hiporlowerlimbsurgery(Inpatientsundergoinglumbar
epiduralanaesthesiaforlowerlimbsurgery,ropivacaine
providedasimilaranaestheticprofile(withregardtoonset
ofanalgesiaoranaesthesiaandonsetofmotorblock)to
thoseofbupivacaine.A20-mldoseofropivacaine0.5%or
bupivacaine0.5%alsoresultedinamediandurationofT10
sensoryblockof3.5versus3.4hours,and15%versus18%
ofpatientswithcompletemotorblock.(11))
10.CrosbyE,SandlerA,FinucaneB,WriterD,ReidD,McKennaJ,etal.
Comparisonofepiduralanaesthesiawithropivacaine0.5%andbupivacaine
0.5%forcaesariansection.CanJAnaesth.1998;45:1066–71.
11.McGladeDP,KalpokasMV,MooneyPH,BucklandMR,VallipuramSK,
HendrataMV,etal.Comparisonof0.5%ropivacaineand0.5%bupivacainein
lumbarepiduralanaesthesiaforlowerlimborthopaedicsurgery.Anaesth
REZA AMINNEJAD, MD.

18. INTRATHECAL ADMINISTRATION
Singledosesof2-4mlof0.5%-2%solutionsof
ropivacainehavebeenshowntobelesspotentthan
bupivacaine.(2)
Hyperbaricsolutionsofropivacainehavebeen
comparedtoisobaricsolutionofthedrugforvarious
proceduresandgenerallyresultedinafasteronsetand
recoveryfromtheblocks.(2)
Theco-administrationofopioidsreducesthetotaldose
oflocalanaestheticrequiredforanaesthesiaand
significantlyprolongsthedurationofcompleteand
effectiveanalgesiawithoutprolongingthedurationof
motorblock.(2)
Onamilligramformilligrambasis,thepotencyof
ropivacainerelativetobupivacaineistwo-thirdswith
regardtosensoryblockandhalfwithregardtomotor
block.(12)
REZA AMINNEJAD, MD.

19. PERIPHERAL NERVE BLOCKS
Thelong-actingsensoryandmotorblockprovidedby
ropivacaine0.5%or0.75%foraxillary,interscaleneand
subclavianperivascularbrachialplexusblockforhandor
armsurgeryiscomparedfavorablywithbupivacaine0.5%
withasimilarqualityofregionalanaesthesia.(2)
Inlowerlimbsurgerieswheresciaticorcombined
femoralandsciaticblockwasgivenforknee,ankle,or
footprocedures,ropivacaine0.75%(25ml)hada
significantlyfasteronsetofsensoryandmotorblock
than25mlbupivacaine0.5%.Althoughropivacainehada
significantlyshorterdurationofsensoryblock,the
durationofmotorblockremainedsimilarwithboth
agents.(13)
13. FanelliG,CasatiA,BeccariaP,AldegheriG,BertiM,TarantinoF,etal.A
double-blindcomparisonofropivacaine,bupivacaine,andmepivacaineduring
sciaticandfemoralnerveblockade.AnesthAnalg.1998;87:597–600.
REZA AMINNEJAD, MD.

20. MANAGEMENT OF
POSTOPERATIVE PAIN
Epiduraladministration:Painreliefismoreeffective
withropivacainecomparedtoIVmorphineandis
comparablewithepiduralbupivacaine.Lowerincidence
ofmotorblockinropivacainerecipientscanleadto
greaterpatientsatisfaction.(2)
Nerveblocks:Comparedtobupivacaine,similarpain
relief,morequicklyreturnofmusclestrengthandless
paresthesiaareadvantagesforropivacaine.(2)
2. KuthialaG,ChaudharyG.Ropivacaine:Areviewofitspharmacologyand
clinicaluse.IndianJAnaesth.2011;55(2):104-10.
REZA AMINNEJAD, MD.

21. MANAGEMENT OF LABOUR
PAIN
Epidurallyadministeredropivacaineiseffectiveinprovidingrelieffrom
labourpain.Itisrecommended toadminister10-20mlbolusof
ropivacaine0.2%withintermittent20-30mgtopupinjectionsora
continuousepiduralinfusionofropivacaine0.2%(6-10ml/hr)for
labouranalgesia.Theanalgesicefficacyofropivacaineissimilartoor
slightlylessthanbupivacaine.Thedifferencebetweentheincidencesof
operativedeliverieswhenropivacainewascomparedwithbupivacaine
wasalsonotfoundsignificant.(2)
Theadditionofnarcoticslikefentanyl2μg/mltoropivacaine0.1%
solutionadministeredat10ml/hrsignificantlyreduceslocal
anaestheticconcentration,asthequalityofanalgesiaissimilarto
ropivacaine0.2%-onlysolutionorropivacaine0.2%plusfentanyl2
μg/mlinfusedataslowerrateof8ml/hr.Additionofadjuvantslike
clonidinealsosignificantlyincreasesthedurationofactionof
ropivacaine.(2)
Intrathecallyadministeredropivacaineasapartofcombinedspinal
epiduraltechniqueproducesrapidandeffectivelabourpainreliefwith
lessincidenceofmotorblock.(2)
REZA AMINNEJAD, MD.

22. CHRONIC PAIN MANAGEMENT
Single-shotepiduralinjectionsofropivacaine0.2%10
mLandbupivacaine0.125%inoutpatientssufferingfrom
chroniclowbackpainarecomparable.(14)
Theprophylacticeffectivenessofropivacaineinjections
inmigrainehasbeendocumented.(15)
14. LierzP,GustorffB,MarkowG,FelleiterP.Comparisonbetween
bupivacaine0.125%andropivacaine0.2%forepiduraladministrationto
outpatientswithchroniclowbackpain.EurJAnaesthesiol.2004;21:32,7.
[PubMed][GoogleScholar]
15. García-LeivaJM,HidalgoJ,Rico-VillademorosF,MorenoV,CalandreEP.
Effectivenessofropivacainetriggerpointsinactivationintheprophylactic
managementofpatientswithseveremigraine.PainMed.2007;8:65–70.
REZA AMINNEJAD, MD.

23. CONCLUSION
Ropivacaineisawelltoleratedregionalanaestheticeffective
forsurgicalanaesthesiaaswellasthereliefofpostoperative
andlabourpain.
Theefficacyofropivacaineissimilartothatofbupivacainefor
peripheralnerveblocksand,althoughitmaybeslightlyless
potentthanbupivacainewhenadministeredepidurallyor
intrathecally,equi-effectivedoseshavebeenestablished.
Clinicallyadequatedosesofropivacaineappeartobe
associatedwithalowerincidenceorgradeofmotorblockthan
bupivacaine.
Ropivacainehasagreaterdegreeofmotorsensory
differentiation,whichcouldbeusefulwhenmotorblockadeis
undesirable
Thus,ropivacaine,withitsefficacy,lowerpropensityformotor
block,andreducedpotentialforCNStoxicityand
cardiotoxicity,appearstobeanimportantoptionforregional
anaesthesiaandmanagementofpostoperativeandlabourpain.
REZA AMINNEJAD, MD.

24. REZA AMINNEJAD, MD.

25. REZA AMINNEJAD, MD.