1. A Review of The Use ofA Review of The Use of
Local Anesthetics andLocal Anesthetics and
Anxiolytics in The DentalAnxiolytics in The Dental
Practice SettingPractice Setting
Charles Sharkey M.S. M.B.A.Charles Sharkey M.S. M.B.A.
Pharm D.Pharm D.
Pharmacy Site ManagerPharmacy Site Manager
Brooklyn/SAECC campusBrooklyn/SAECC campus
January 2008January 2008
2. Learning ObjectivesLearning Objectives
At the conclusion of this presentationAt the conclusion of this presentation
the practicing dentist will have anthe practicing dentist will have an
increased understanding of theincreased understanding of the
following for local anesthetics, andfollowing for local anesthetics, and
anxiolytic drugs.anxiolytic drugs.
PharmacologyPharmacology
Monitoring parametersMonitoring parameters
Adverse effect profileAdverse effect profile
3. Historical Perspective on LocalHistorical Perspective on Local
AnestheticsAnesthetics
Local Anesthetics have been used inLocal Anesthetics have been used in
Dentistry for over 100 years.Dentistry for over 100 years.
Prior to this in the 1800’s a “swig ofPrior to this in the 1800’s a “swig of
whiskey” was used before a dentalwhiskey” was used before a dental
procedure.procedure.
1840 Dr. Horace Wells used Nitrous1840 Dr. Horace Wells used Nitrous
OxideOxide
1840 Dr. William Morton used Ether1840 Dr. William Morton used Ether
4. Historical Perspective on LocalHistorical Perspective on Local
AnestheticsAnesthetics
On September 30, 1846 Dr. MortonOn September 30, 1846 Dr. Morton
extracted a tooth while using Ether.extracted a tooth while using Ether.
The patients name was Mr. EbenThe patients name was Mr. Eben
Frost.Frost.
1859 Albert Niemann extracted an1859 Albert Niemann extracted an
alkaloid called Cocaine.alkaloid called Cocaine.
1901 Heinrich Braun demonstrated1901 Heinrich Braun demonstrated
use of Epinephrine to retarduse of Epinephrine to retard
absorption of local anesthetics.absorption of local anesthetics.
5. Historical Perspective of LocalHistorical Perspective of Local
AnestheticsAnesthetics
1904 Alfred Einhorn introduced1904 Alfred Einhorn introduced
Procaine (Novocaine)Procaine (Novocaine)
The race began for more effectiveThe race began for more effective
local anesthetics in dentistry.local anesthetics in dentistry.
1943 Nils Lofgren introduced1943 Nils Lofgren introduced
Lidocaine (Xylocaine)Lidocaine (Xylocaine)
Movement here is from generalMovement here is from general
anesthetics to local agents.anesthetics to local agents.
6. Classification of Local AnestheticsClassification of Local Anesthetics
Three components: aromatic group,Three components: aromatic group,
intermediate chain, and aminointermediate chain, and amino
terminus.terminus.
Ester or AmideEster or Amide
Lipophilic and hydrophilic groupsLipophilic and hydrophilic groups
Weak basesWeak bases
Balance between hydrophilicity (i.e.Balance between hydrophilicity (i.e.
ability to be solubilized in dentalability to be solubilized in dental
syringe) and lipophilicity (onset andsyringe) and lipophilicity (onset and
duration of clinical action)duration of clinical action)
7. Classification of Local AnestheticsClassification of Local Anesthetics
Ester or Amide classificationEster or Amide classification
Amides are preferred.Amides are preferred.
Preference is due to the way thePreference is due to the way the
drugs are broken down in the body.drugs are broken down in the body.
Amides are reduced in the liver andAmides are reduced in the liver and
excreted in the kidney.excreted in the kidney.
Amides less likely to cause allergicAmides less likely to cause allergic
reactions.reactions.
8. Pharmacology of the LocalPharmacology of the Local
AnestheticsAnesthetics
Local anesthesia is produced whenLocal anesthesia is produced when
propagation of action potential ispropagation of action potential is
prevented.prevented.
Block the entry of sodium ions.Block the entry of sodium ions.
Sensations cannot be transmittedSensations cannot be transmitted
from the tooth to the brain.from the tooth to the brain.
Reversible reaction. No loss ofReversible reaction. No loss of
consciousnessconsciousness
9. Pharmacology of Local AnestheticsPharmacology of Local Anesthetics
Local anesthetics effect axonalLocal anesthetics effect axonal
membranes of peripheral nerves.membranes of peripheral nerves.
General Anesthetics work on theGeneral Anesthetics work on the
synapses of the Central Nervoussynapses of the Central Nervous
SystemSystem
Local Anesthetics work best on TypeLocal Anesthetics work best on Type
C small nerve fibers in comparison toC small nerve fibers in comparison to
Type A or Type B.Type A or Type B.
This translates into no feeling of painThis translates into no feeling of pain
but may experience feeling ofbut may experience feeling of
pressurepressure
10. Requirements for a LocalRequirements for a Local
AnestheticAnesthetic
High intrinsic activityHigh intrinsic activity
Rapid onsetRapid onset
Duration of action of 30 to 60Duration of action of 30 to 60
minutesminutes
Low systemic toxicityLow systemic toxicity
Low incidence of serious adverseLow incidence of serious adverse
reactions.reactions.
11. Factors to considerFactors to consider
pH of the surrounding tissuepH of the surrounding tissue
pKa of the drugpKa of the drug
Balance of lipophilicity andBalance of lipophilicity and
hydrophilicityhydrophilicity
Proximity of injection to the nerve.Proximity of injection to the nerve.
Chemical classChemical class
VasoconstrictorVasoconstrictor
12. Local Anesthetics In PerspectiveLocal Anesthetics In Perspective
Dentists in the U.S. useDentists in the U.S. use
approximately 1,500 to 2000approximately 1,500 to 2000
cartridges per year.cartridges per year.
300 million cartridges are300 million cartridges are
administered per year.administered per year.
Local anesthetics are Relatively safeLocal anesthetics are Relatively safe
medications based on statistics,medications based on statistics,
doses used, and application.doses used, and application.
13. Response to Local AnestheticsResponse to Local Anesthetics
Patients Psychological StatePatients Psychological State
Health of tissueHealth of tissue
Injection techniqueInjection technique
Agent selectedAgent selected
Vasoconstrictor or NotVasoconstrictor or Not
14. Development of Local AnestheticsDevelopment of Local Anesthetics
1884 Cocaine1884 Cocaine
1904 Procaine1904 Procaine
1932 Tetracaine1932 Tetracaine
1948 Lidocaine1948 Lidocaine
1963 Bupivacaine1963 Bupivacaine
1969 Articaine1969 Articaine
15. Duration of actionDuration of action
Bupivacine with EpiBupivacine with Epi >90>90
minutesminutes
Etidocaine with EpiEtidocaine with Epi >90>90
minutesminutes
Lidocaine (No epi)Lidocaine (No epi) 3030
minutesminutes
Lidocaine with EpiLidocaine with Epi 6060
minutesminutes
MepivacaineMepivacaine (No epi)(No epi) 30 to30 to
60 min
16. Local Anesthetics-Clinical PearlsLocal Anesthetics-Clinical Pearls
Lidocaine with Epi 1:100,000Lidocaine with Epi 1:100,000
common.common.
Mepivacaine with NO EPI used forMepivacaine with NO EPI used for
patients who cannot tolerate apatients who cannot tolerate a
vasoconstrictor.vasoconstrictor.
Bupivacaine is used for longerBupivacaine is used for longer
procedures.procedures.
Bupivacaine is not recommended forBupivacaine is not recommended for
children or handicapped due tochildren or handicapped due to
increased risk of postop injury.increased risk of postop injury.
17. Local Anesthetics-Adverse EffectsLocal Anesthetics-Adverse Effects
Psychogenic including syncope,Psychogenic including syncope,
hyperventilation, nausea, vomiting.hyperventilation, nausea, vomiting.
Allergic reactions to esters,Allergic reactions to esters,
preservatives.preservatives.
Sedation, slurred speech.Sedation, slurred speech.
MethemoglobinemiaMethemoglobinemia
ParenthesisParenthesis
18. A Word About VasoconstrictorsA Word About Vasoconstrictors
Local anesthetics have vasodilatorLocal anesthetics have vasodilator
properties.properties.
Prolong the duration of action of theProlong the duration of action of the
local anestheticlocal anesthetic
Decrease absorption of anestheticDecrease absorption of anesthetic
Range of 1:50,000 t0 1:200,000 ofRange of 1:50,000 t0 1:200,000 of
Epinephrine.Epinephrine.
19. Local Anesthetic Drug InteractionsLocal Anesthetic Drug Interactions
Beta blockers + EpiBeta blockers + Epi
Tricyclic antidepressants + EpiTricyclic antidepressants + Epi
Cocaine + EpiCocaine + Epi
20. Special Patient PopulationsSpecial Patient Populations
Fairly safe in pregnant and lactatingFairly safe in pregnant and lactating
patients. Lidocaine has a Categorypatients. Lidocaine has a Category
rating of FDA B.rating of FDA B.
Pediatrics should avoid BupivacainePediatrics should avoid Bupivacaine
Geriatric patients should have noGeriatric patients should have no
significant difference in responsesignificant difference in response
22. Articaine vs. LidocaineArticaine vs. Lidocaine
Articaine was approved in the US forArticaine was approved in the US for
dental use in 2000dental use in 2000
Some dentists claim it has betterSome dentists claim it has better
bone perfusion, and actually worksbone perfusion, and actually works
betterbetter
Thiophene ring, and ester linkageThiophene ring, and ester linkage
23. Articaine vs. LidocaineArticaine vs. Lidocaine
Anecdotal reports claiming superiorAnecdotal reports claiming superior
efficacy of Articaineefficacy of Articaine
Literate points to comparableLiterate points to comparable
efficacy with Lidocaine 2% plusefficacy with Lidocaine 2% plus
epinephrineepinephrine
24. Antianxiety MedicationsAntianxiety Medications
Fear and anxiety are common inFear and anxiety are common in
dental patientsdental patients
Mild fears can impact oral healthMild fears can impact oral health
Antianxiety medications are used inAntianxiety medications are used in
clinical dentistry for premedication ofclinical dentistry for premedication of
the nervous and apprehensivethe nervous and apprehensive
patientpatient
25. Antianxiety medicationsAntianxiety medications
Benzodiazepines are the most widelyBenzodiazepines are the most widely
prescribed classprescribed class
Selective, effective, and safeSelective, effective, and safe
Pharmacologically act in the CNSPharmacologically act in the CNS
Several dozen agents marketedSeveral dozen agents marketed
worldwideworldwide
26. Pharmacology of BenzodiazepinesPharmacology of Benzodiazepines
Stimulate gamma amino-butyric acidStimulate gamma amino-butyric acid
(GABA)(GABA)
GABA is a major inhibitoryGABA is a major inhibitory
neurotransmitter in the CNSneurotransmitter in the CNS
Effect the flow of chloride ions inEffect the flow of chloride ions in
neuronal tissue which effects nerveneuronal tissue which effects nerve
transmissiontransmission
28. BenzodiazepinesBenzodiazepines
The dentist is faced with the questionThe dentist is faced with the question
of which agent to use?of which agent to use?
But the real issue is not so muchBut the real issue is not so much
which agent to use but when towhich agent to use but when to
administeradminister
Avoid excessive CNS adverse effectsAvoid excessive CNS adverse effects
29. Properties of benzodiazpinesProperties of benzodiazpines
Triazolam 0.125mg-0.5mg orally hasTriazolam 0.125mg-0.5mg orally has
a 2-4 hour durationa 2-4 hour duration
Midazolam 0.5mgs/kg IV has aMidazolam 0.5mgs/kg IV has a
duration of 1-2 hoursduration of 1-2 hours
Lorazepam 1-3mgs orally has a 6-8Lorazepam 1-3mgs orally has a 6-8
hour durationhour duration
30. Properties of benzodiazepinesProperties of benzodiazepines
Alprazolam 1mg orally has a durationAlprazolam 1mg orally has a duration
of 6-8 hoursof 6-8 hours
Diazepam 5mgs-10mgs orally has aDiazepam 5mgs-10mgs orally has a
duration of 6-8 hoursduration of 6-8 hours
31. Benzodiazepines—Adverse EffectsBenzodiazepines—Adverse Effects
CNS related including drowsiness,CNS related including drowsiness,
excessive sedation, lethargy.excessive sedation, lethargy.
Normal doses do not effectNormal doses do not effect
respiration. However, it does haverespiration. However, it does have
some respiratory depressantsome respiratory depressant
potentialpotential
32. BenzodiazepinesBenzodiazepines
Recommend you select a short actingRecommend you select a short acting
agent i.e. Alprazolam and administeragent i.e. Alprazolam and administer
it before the procedureit before the procedure
Avoid a longer acting agent such asAvoid a longer acting agent such as
diazepamdiazepam
