classification of local anesthetics

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CLASSIFICATION OF LOCAL CLASSIFICATION OF LOCAL ANESTHETICS ANESTHETICS By By Helen R. Hallare, DDM Helen R. Hallare, DDM

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Page 1: CLASSIFICATION OF LOCAL ANESTHETICS

CLASSIFICATION OF LOCAL CLASSIFICATION OF LOCAL ANESTHETICSANESTHETICS

ByBy

Helen R. Hallare, DDMHelen R. Hallare, DDM

Page 2: CLASSIFICATION OF LOCAL ANESTHETICS

Chemical Groups of LOCAL Chemical Groups of LOCAL ANESTHETICS commonly used ANESTHETICS commonly used

in dentistry:in dentistry:

I.I. Ester groupEster group

A.A. Benzoic acid estersBenzoic acid esters

1.1. Cocaine (topical only) naturally Cocaine (topical only) naturally occurringoccurring

2.2. Benzocaine (topical only)Benzocaine (topical only)

Page 3: CLASSIFICATION OF LOCAL ANESTHETICS

Chemical Groups of LOCAL Chemical Groups of LOCAL ANESTHETICS commonly used in ANESTHETICS commonly used in

dentistry:dentistry:

B.B. Para-aminobenzoic acid estersPara-aminobenzoic acid esters

1.1. Procaine (Novocaine)Procaine (Novocaine)

2.2. Tetracaine (Pontocaine)Tetracaine (Pontocaine) extremely extremely strong local anesthetic for surface strong local anesthetic for surface anesthesia; no real injection useanesthesia; no real injection use

3.3. Propoxycaine (Ravocaine)Propoxycaine (Ravocaine)

4.4. 2-Chloroprocaine (Nesacaine) (not 2-Chloroprocaine (Nesacaine) (not marketed in an dental cartridge)marketed in an dental cartridge)

Page 4: CLASSIFICATION OF LOCAL ANESTHETICS

ChemicalChemical Groups of LOCAL Groups of LOCAL ANESTHETICS commonly used in ANESTHETICS commonly used in

dentistry:dentistry:

II.II. Nonester groupNonester groupA.A. Anilide (Nonester type)Anilide (Nonester type)

1.1. Bupivacaine (Marcaine, Bupivacaine (Marcaine, Sensorcaine)Sensorcaine)

2.2. Etidocaine (Duranest)Etidocaine (Duranest)3.3. Lidocaine (Xylocaine)Lidocaine (Xylocaine)4.4. Mepivacaine (Carbocaine)Mepivacaine (Carbocaine)5.5. Prilocaine (Citanest)Prilocaine (Citanest)

Page 5: CLASSIFICATION OF LOCAL ANESTHETICS

Excretion and Absorption of Excretion and Absorption of Local AnestheticsLocal Anesthetics

1.1. EstersEsters: Hydrolyzed by plasma : Hydrolyzed by plasma esterase and by products esterase and by products excreted in urine. Note that one excreted in urine. Note that one by product is PABA (para-amino by product is PABA (para-amino benzoic acid)benzoic acid)

2.2. AmidesAmides: Metabolized in liver by : Metabolized in liver by microsomal enzymes and only microsomal enzymes and only 10—20% is excreted unchanged10—20% is excreted unchanged

Page 6: CLASSIFICATION OF LOCAL ANESTHETICS

CocaineCocaineFrom the leaves of a plant called From the leaves of a plant called Erthroxylon coca; 1855 French Erthroxylon coca; 1855 French chemist F. Gaedckechemist F. Gaedcke

Albert Niemann isolated the alkaloid Albert Niemann isolated the alkaloid in its pure form—named it ‘cocaine’in its pure form—named it ‘cocaine’

1884, Carl Koller, encouraged by 1884, Carl Koller, encouraged by Sigmund Freud, discovered that it is Sigmund Freud, discovered that it is effective surface anesthesia of the effective surface anesthesia of the corneacornea

Page 7: CLASSIFICATION OF LOCAL ANESTHETICS

CocaineCocaineWilliam Steward Halsted in America William Steward Halsted in America used the solution to produce used the solution to produce anesthesia in the inferior dental anesthesia in the inferior dental nerve; victim of the drug’s nerve; victim of the drug’s addictiveaddictive propertiesproperties First record of use in Britain, JADA First record of use in Britain, JADA 1886, William Alfred Hunt described 1886, William Alfred Hunt described use in infiltrationuse in infiltration1901, E. Mayer suggested addition of 1901, E. Mayer suggested addition of adrenaline—promote adrenaline—promote vasoconstriction, prolong duration, vasoconstriction, prolong duration, and intensify depth of anesthesiaand intensify depth of anesthesia

Page 8: CLASSIFICATION OF LOCAL ANESTHETICS

CocaineCocaine

Rarely used these days due to Rarely used these days due to problems of misuseproblems of misuse

Methyl 3Methyl 3ββ-hydroxy-1-hydroxy-1ααH-tropan-2H-tropan-2ββ--carboxylate ester benzoate (chemical carboxylate ester benzoate (chemical name)name)

Unique among local anesthetic Unique among local anesthetic agents in that it produces agents in that it produces vasoconstrictionvasoconstriction

Page 9: CLASSIFICATION OF LOCAL ANESTHETICS

CocaineCocainePreparation:Preparation:

Topical preparation as a 4 - 10% solutionTopical preparation as a 4 - 10% solution

Recommended uses in Dentistry:Recommended uses in Dentistry:

Should not be considered as a normal Should not be considered as a normal part of dental local anesthetic part of dental local anesthetic armamentarium due to its obvious armamentarium due to its obvious disadvantage—potential for abusedisadvantage—potential for abuse

Occasionally used topically intranasally Occasionally used topically intranasally during apical surgery on maxillary during apical surgery on maxillary incisor teeth when the nasal floor is in incisor teeth when the nasal floor is in close proximityclose proximity

Page 10: CLASSIFICATION OF LOCAL ANESTHETICS

BenzocaineBenzocaineMost commonly used ester local Most commonly used ester local anestheticanesthetic

Ethyl-Ethyl-pp-aminobenzoate (chemical -aminobenzoate (chemical name)name)

DosageDosage

Due to its extremely poor solubility in Due to its extremely poor solubility in water and poor absorption, toxic water and poor absorption, toxic reactions to benzocaine are almost reactions to benzocaine are almost unknownunknown

Page 11: CLASSIFICATION OF LOCAL ANESTHETICS

BenzocaineBenzocainePreparation:Preparation: Extremely poor water solubility – not Extremely poor water solubility – not

suitable for injection; available only suitable for injection; available only in topical preparationsin topical preparations

Available in number of Available in number of concentrations up to 20% and in concentrations up to 20% and in combination with other agents combination with other agents

Different flavors have been added to Different flavors have been added to benzocaine gel to make them benzocaine gel to make them particularly popular with childrenparticularly popular with children

Page 12: CLASSIFICATION OF LOCAL ANESTHETICS

BenzocaineBenzocaine

Recommended uses in Dentistry:Recommended uses in Dentistry:

Topical application prior to an Topical application prior to an infiltration – means of reducing paininfiltration – means of reducing pain

Incorporated into proprietary Incorporated into proprietary medications for application to painful medications for application to painful intraoral lesions – ulcersintraoral lesions – ulcers

Sole source of anesthesia for Sole source of anesthesia for superficial soft tissue manipulationsuperficial soft tissue manipulation

Page 13: CLASSIFICATION OF LOCAL ANESTHETICS

Procaine Procaine

Produced synthetically procaine Produced synthetically procaine hydrochloride by two Swedish hydrochloride by two Swedish chemists, Alfred Einhorn & E. Uhlfelderchemists, Alfred Einhorn & E. Uhlfelder

Tested clinically by Henrich Braun and Tested clinically by Henrich Braun and marketed as Novocaine (proprietary marketed as Novocaine (proprietary name)name)

Archetypal dental local anesthetic Archetypal dental local anesthetic prior to the introduction of lignocaineprior to the introduction of lignocaine

Page 14: CLASSIFICATION OF LOCAL ANESTHETICS

ProcaineProcaine

Use has declined for a number of Use has declined for a number of reasons: susceptible persons may reasons: susceptible persons may become sensitized to this substance; become sensitized to this substance; can cause dermatitis, urticaria and can cause dermatitis, urticaria and even eodema of the glottiseven eodema of the glottis

Not as potent as cocaine, but it is Not as potent as cocaine, but it is very much less toxicvery much less toxic

Page 15: CLASSIFICATION OF LOCAL ANESTHETICS

ProcaineProcainePreparation:Preparation:

Rarely used as sole anesthetic in Rarely used as sole anesthetic in Dentistry todayDentistry todayNo longer available in cartridges in No longer available in cartridges in some parts of the world and must be some parts of the world and must be drawn up in ampuledrawn up in ampuleNormal presentation is 2% solution, Normal presentation is 2% solution, however 1:80,000 adrenaline may be however 1:80,000 adrenaline may be addedaddedNot available as a topical agentNot available as a topical agent

Page 16: CLASSIFICATION OF LOCAL ANESTHETICS

ProcaineProcaine

Recommended uses in DentistryRecommended uses in DentistryOnly indication for use as a local Only indication for use as a local anesthetic is in patients with proven anesthetic is in patients with proven allergy to the amide groupallergy to the amide groupUseful in intravenous sedation Useful in intravenous sedation relevant to dental practicerelevant to dental practiceRecognized regimen to treat Recognized regimen to treat arteriospasm when it is administered arteriospasm when it is administered intra-arterially – excellent intra-arterially – excellent vasodilatory propertiesvasodilatory properties

Page 17: CLASSIFICATION OF LOCAL ANESTHETICS

ProcaineProcaineOnset and duration of actionOnset and duration of action

Onset of action: 10 minutes (pulpal)Onset of action: 10 minutes (pulpal)

Duration of action: plain solution, Duration of action: plain solution, extremely short-lived pulpal extremely short-lived pulpal anesthesia of approximately 5 minutesanesthesia of approximately 5 minutes

solution with adrenaline, pulpal solution with adrenaline, pulpal anesthesia of 30 minutesanesthesia of 30 minutes

DosageDosage

Maximum dose is 6 mg/kg with ceiling Maximum dose is 6 mg/kg with ceiling of 400 mgof 400 mg

Page 18: CLASSIFICATION OF LOCAL ANESTHETICS

TetracaineTetracainePara-butylaminobenzoyl-2-Para-butylaminobenzoyl-2-dimethylaminoethanol hydrochloride dimethylaminoethanol hydrochloride (chemical name)(chemical name)Proprietary name: PontocaineProprietary name: Pontocaine10x as potent and 10x as toxic as 10x as potent and 10x as toxic as procaineprocaineChemically it is closely related to Chemically it is closely related to procaine but pharmacologically it is procaine but pharmacologically it is closer to cocainecloser to cocainePotent topical agent, does not Potent topical agent, does not possess vasoconstricting propertiespossess vasoconstricting properties

Page 19: CLASSIFICATION OF LOCAL ANESTHETICS

TetracaineTetracaine

Popular for the production of spinal Popular for the production of spinal anesthesiaanesthesia

No longer available in cartridges for No longer available in cartridges for use in dentistryuse in dentistry

Limited almost exclusively to topical Limited almost exclusively to topical applicationapplication

Rapidly absorbed into systemic Rapidly absorbed into systemic circulation—toxic effects, not circulation—toxic effects, not sprayed on mucous membranesprayed on mucous membrane

Page 20: CLASSIFICATION OF LOCAL ANESTHETICS

TetracaineTetracaine

PreparationPreparation 0.15%, 1% and 2% topical solutions0.15%, 1% and 2% topical solutions Plain tetracaine hydrochloridePlain tetracaine hydrochloride Tetracaine hydrochloride with Tetracaine hydrochloride with

1:100,000 vasodilator 1:100,000 vasodilator

DosageDosage Maximum of 20 mg (1 ml of 2% Maximum of 20 mg (1 ml of 2%

solution) be applied at one timesolution) be applied at one time

Page 21: CLASSIFICATION OF LOCAL ANESTHETICS

TetracaineTetracaine

Duration of actionDuration of action

When injected, plain 0.15% solution When injected, plain 0.15% solution will produce 30 – 45 minutes of will produce 30 – 45 minutes of analgesiaanalgesia

Same concentration with 1:100,000 Same concentration with 1:100,000 epinephrine will produce 75 – 120 epinephrine will produce 75 – 120 minutes of analgesiaminutes of analgesia

Page 22: CLASSIFICATION OF LOCAL ANESTHETICS

TetracaineTetracaine

Recommended use in DentistryRecommended use in Dentistry Although efective when given by Although efective when given by

injection, it is not used in this manner injection, it is not used in this manner due to its toxicity.due to its toxicity.

It is available in topical preparations It is available in topical preparations both on its own and in combination both on its own and in combination with other anesthetic agents such as with other anesthetic agents such as lignocainelignocaine

Page 23: CLASSIFICATION OF LOCAL ANESTHETICS

Propoxycaine (Ravocaine)Propoxycaine (Ravocaine)2-diethylaminoethyl 4-amino-2-2-diethylaminoethyl 4-amino-2-propoxybenzoate is its chemical namepropoxybenzoate is its chemical name

Equal in potency and toxicity to Equal in potency and toxicity to tetracainetetracaine

PreparationPreparation

Not used alone in dentistry, combined Not used alone in dentistry, combined with procaine, in a procaine 2%, with procaine, in a procaine 2%, propoxycaine 0.4% solution with propoxycaine 0.4% solution with either 1:20,000 levondefrin or 1: either 1:20,000 levondefrin or 1: 30,000 levarterenol as vasoconstrictor30,000 levarterenol as vasoconstrictor

Page 24: CLASSIFICATION OF LOCAL ANESTHETICS

PropoxycainePropoxycaineDuration of actionDuration of action Combination of procaine and Combination of procaine and

propoxycaine gives rapid and profound propoxycaine gives rapid and profound anesthesia with a pulpal analgesia of anesthesia with a pulpal analgesia of about 1 – 1.5 hours and soft tissue about 1 – 1.5 hours and soft tissue duration of 2 – 3 hoursduration of 2 – 3 hours

DosageDosage Suggested maximum dose is 6.6 mg’kg (3 Suggested maximum dose is 6.6 mg’kg (3

mg/lb)mg/lb) Maximum total anesthetic (procaine plus Maximum total anesthetic (procaine plus

propoxycaine) dosage should not exceed propoxycaine) dosage should not exceed 400 mg400 mg

Page 25: CLASSIFICATION OF LOCAL ANESTHETICS

2-Chloroprocaine2-Chloroprocaine

Proprietary name: NesacaineProprietary name: Nesacaine

Beta-diethylaminoethyl-2-chloro-4-Beta-diethylaminoethyl-2-chloro-4-aminobenzoate (chemical name)aminobenzoate (chemical name)

Differs from other local anesthetic of Differs from other local anesthetic of the ester group in having a chloride the ester group in having a chloride atom substituted in the benzene ringatom substituted in the benzene ring

2x as potent but less toxic than 2x as potent but less toxic than procaine – hydrolyzed 4x-5x faster procaine – hydrolyzed 4x-5x faster than procaine than procaine

Page 26: CLASSIFICATION OF LOCAL ANESTHETICS

2-Chloroprocaine2-Chloroprocaine

PreparationPreparation Not available in dental cartridge, Not available in dental cartridge,

multiple dose vial via disposable 3 to multiple dose vial via disposable 3 to 5 cc syringe with a 25-gauge Leur-5 cc syringe with a 25-gauge Leur-Lok needleLok needle

Available in 1.2% or 3% Available in 1.2% or 3% concentrations, must be used with a concentrations, must be used with a vasoconstrictor due to its shortness vasoconstrictor due to its shortness of duration of duration

Page 27: CLASSIFICATION OF LOCAL ANESTHETICS

2-Chloroprocaine2-Chloroprocaine

Onset and duration of actionOnset and duration of action Extremely rapid onset with a Extremely rapid onset with a

satisfactory short-acting anesthetic satisfactory short-acting anesthetic (low toxicity) thus advantageous in (low toxicity) thus advantageous in use for children who may use for children who may inadvertently traumatize the lip, inadvertently traumatize the lip, tongue or cheek with longer-acting tongue or cheek with longer-acting agentsagents

Page 28: CLASSIFICATION OF LOCAL ANESTHETICS

LignocaineLignocaineMost commonly used dental anestheticMost commonly used dental anestheticSynthetized in 1943, has been in clinical Synthetized in 1943, has been in clinical use since 1948use since 1948Proprietary names: Xylocaine, Proprietary names: Xylocaine, Lignospan, Lignostab, & Lidocaine Lignospan, Lignostab, & Lidocaine (North America)(North America)Chemical name: 2-diethylamino-2,6-Chemical name: 2-diethylamino-2,6-acetoxylidide.acetoxylidide.2x potency than procaine 2x potency than procaine More profound anesthesia and long More profound anesthesia and long duration (spreads more widely through duration (spreads more widely through tissues)tissues)

Page 29: CLASSIFICATION OF LOCAL ANESTHETICS

LignocaineLignocaine

Preparations:Preparations:

Dental cartridges – plain 2% Dental cartridges – plain 2% solution and a 2% solution with solution and a 2% solution with 1:80,000 or 1:100,000 1:80,000 or 1:100,000 adrenalineadrenaline

Topical – 4% and 10% spray, Topical – 4% and 10% spray, 2% gels, and 5% ointment2% gels, and 5% ointment

Page 30: CLASSIFICATION OF LOCAL ANESTHETICS

LignocaineLignocaine

Recommended uses in Dentistry:Recommended uses in Dentistry:2% with 1:80,000 adrenaline--ideal 2% with 1:80,000 adrenaline--ideal for infiltration, intraosseous, for infiltration, intraosseous, intraligamentary, and regional block intraligamentary, and regional block anesthesia for majority of patientsanesthesia for majority of patientsContraindicated in those allergic to Contraindicated in those allergic to amides and in individuals where amides and in individuals where increased adrenaline levels may be increased adrenaline levels may be hazardoushazardous

Page 31: CLASSIFICATION OF LOCAL ANESTHETICS

LignocaineLignocaine

Recommended uses in Dentistry:Recommended uses in Dentistry:Plain solution is not very effective in Plain solution is not very effective in obtaining pulpal anesthesiaobtaining pulpal anesthesiaUse for soft tissue procedures is very Use for soft tissue procedures is very limited—poor hemorrhage controllimited—poor hemorrhage controlNevertheless, effective topical Nevertheless, effective topical anesthetic for non-keratinized tissue: anesthetic for non-keratinized tissue: reflected mucosa & as a reflected mucosa & as a symptomatic treatment for painful symptomatic treatment for painful mucosal lesions such as ulcersmucosal lesions such as ulcers

Page 32: CLASSIFICATION OF LOCAL ANESTHETICS

LignocaineLignocaineOnset and duration of actionOnset and duration of action

Short onset of action, pulpal anesthesia Short onset of action, pulpal anesthesia obtained in 2-3 minutes ff. infiltrationobtained in 2-3 minutes ff. infiltration

Plain solution is classified as short-acting Plain solution is classified as short-acting agent, will provide pulpal anesthesia for 10 agent, will provide pulpal anesthesia for 10 minutes; 1-1 ½ hours soft tissue anesthesiaminutes; 1-1 ½ hours soft tissue anesthesia

Adrenaline containing solution is Adrenaline containing solution is intermediate in duration providing 45-60 intermediate in duration providing 45-60 minutes (1-1 ½ hours) of pulpal anesthesia; minutes (1-1 ½ hours) of pulpal anesthesia; 3-4 hours soft tissues anesthesia3-4 hours soft tissues anesthesia

Page 33: CLASSIFICATION OF LOCAL ANESTHETICS

PrilocainePrilocaineToluidine derivative; related both Toluidine derivative; related both chemically and pharmacologically to chemically and pharmacologically to both lignocaine and mepivacaineboth lignocaine and mepivacaine

Proprietary name: CitanestProprietary name: Citanest

2-propylamino-2-propylamino-oo-propionotoluidine -propionotoluidine (chemical name)(chemical name)

As potent as lignocaine but is less As potent as lignocaine but is less toxictoxic

Metabolized more rapidly than Metabolized more rapidly than lignocainelignocaine

Does not produce topical anesthesiaDoes not produce topical anesthesia

Page 34: CLASSIFICATION OF LOCAL ANESTHETICS

PrilocainePrilocainePreparationsPreparations

Plain solution is 4%Plain solution is 4%Vasoconstrictor-containing version is Vasoconstrictor-containing version is 3% with 0.03 IU/ml felypressin (UK)3% with 0.03 IU/ml felypressin (UK)In other parts of the world prilocaine In other parts of the world prilocaine is available with adrenalineis available with adrenalineTopical anesthetic agent available – Topical anesthetic agent available – combination prilocaine & lignocaine combination prilocaine & lignocaine EMLA (Eutectic Mixture of Local EMLA (Eutectic Mixture of Local Anesthetics) Anesthetics)

Page 35: CLASSIFICATION OF LOCAL ANESTHETICS

PrilocainePrilocaine

Recommended use in DentistryRecommended use in Dentistry3% with 0.03 IU felypressin is the alternative 3% with 0.03 IU felypressin is the alternative to lignocaine with adrenaline when a to lignocaine with adrenaline when a vasoconstrictor-containing solution is requiredvasoconstrictor-containing solution is requiredEffective when administered as an infiltration Effective when administered as an infiltration or regional block anestheticor regional block anestheticNot as effective as lignocaine during Not as effective as lignocaine during intraligamentary techniquesintraligamentary techniques4% plain prilocaine more effective than 2% 4% plain prilocaine more effective than 2% lignocaine when a vasoconstrictor-free lignocaine when a vasoconstrictor-free solution must be employedsolution must be employedEMLA useful prior to venepuncture in children EMLA useful prior to venepuncture in children and during dental sedation; oral application and during dental sedation; oral application not recommended by manufacturersnot recommended by manufacturers

Page 36: CLASSIFICATION OF LOCAL ANESTHETICS

PrilocainePrilocaine

ContraindicationsContraindications

Should not be administered to infants, Should not be administered to infants, patients with methaemoglobineamia, kidney patients with methaemoglobineamia, kidney disease, hypoxia, anemia, liver disease or disease, hypoxia, anemia, liver disease or heart failure, or any other condition in which heart failure, or any other condition in which problems with oxygenation could be critical, problems with oxygenation could be critical, such as pregnancysuch as pregnancy

Should not be used in patients who have a Should not be used in patients who have a history of either sensitivity to an amide-type history of either sensitivity to an amide-type local anesthetic agent or paraben allergylocal anesthetic agent or paraben allergy

Page 37: CLASSIFICATION OF LOCAL ANESTHETICS

PrilocainePrilocaine

Onset and duration of actionOnset and duration of actionSlower onset of action than lignocaine: Slower onset of action than lignocaine: pulpal anesthesia 4 minutespulpal anesthesia 4 minutes4% prilocaine short-acting agent with 4% prilocaine short-acting agent with pulpal anesthesia lasting around 10 pulpal anesthesia lasting around 10 minutesminutes3% with 0.03 IU felypressin provides 3% with 0.03 IU felypressin provides duration of anesthesia similar to that duration of anesthesia similar to that afforded by lignocaineafforded by lignocaine

Page 38: CLASSIFICATION OF LOCAL ANESTHETICS

MepivacaineMepivacaine

The least vasodilatory of the amide The least vasodilatory of the amide local anestheticlocal anesthetic

Proprietary name: Scandonest (UK), Proprietary name: Scandonest (UK), Carbocaine Pharmaceutical Carbocaine Pharmaceutical Manufacturing Co.Manufacturing Co.

1-methyl-2,6-pipecoloxylidide 1-methyl-2,6-pipecoloxylidide (chemical name)(chemical name)

Mepivacaine without adrenaline has Mepivacaine without adrenaline has a 5-year shelf-life, irrespective of the a 5-year shelf-life, irrespective of the conditions of storageconditions of storage

Page 39: CLASSIFICATION OF LOCAL ANESTHETICS

MepivacaineMepivacaine

PreparationsPreparations

3% plain solution3% plain solution

2% solution with 1:80,000 2% solution with 1:80,000 adrenalineadrenaline

Not available in a topical Not available in a topical preparationpreparation

Page 40: CLASSIFICATION OF LOCAL ANESTHETICS

MepivacaineMepivacaine

Recommended use in Dentistry:Recommended use in Dentistry:Prime indication is for the use is Prime indication is for the use is when vasoconstrictor-free solution when vasoconstrictor-free solution must be employed as 3% must be employed as 3% mepivacaine is more effective than mepivacaine is more effective than plain lignocaine or prilocaine plain lignocaine or prilocaine solutionssolutionsSolution with adrenaline has identical Solution with adrenaline has identical indications for use as lignocaine with indications for use as lignocaine with adrenaline although it has a shorter adrenaline although it has a shorter duration of actionduration of action

Page 41: CLASSIFICATION OF LOCAL ANESTHETICS

MepivacaineMepivacaine

Onset and duration of actionOnset and duration of actionRapid onset of action: (pulpal) 2 minutesRapid onset of action: (pulpal) 2 minutesDuration of action: Duration of action:

(pulpal) plain solution—30 minutes(pulpal) plain solution—30 minuteswith adrenaline provides anesthesia with adrenaline provides anesthesia

of similar depth as lignocaine but of of similar depth as lignocaine but of slightly shorter durationslightly shorter duration

Page 42: CLASSIFICATION OF LOCAL ANESTHETICS

DosagesDosages

Anesthetic solution

Max. dose

(mg/kg) [absolute ceiling

(mg)]

Max. dose of 1.8 ml cartridges

in an adult of 70 kg

Max. dose of 1.8 ml cartridges

in a 5-year-old child of

20kg

Max. dose of 2.2 ml cartridges

in an adult of 70 kg

Max. dose of 2.2 ml cartridges

in a 5-year-old child of

20kg

2% lignocaine 4.4 [300]

8.3 2.4 6.8 2

2% mepivacaine

4.4 [300]

8.3 2.4 6.8 2

3% mepivacaine

4.4 [300]

5.6 1.6 4.5 1.3

3% prilocaine 6.0 [400]

7.4 2.2 6 1.8

4% prilocaine 6.0 [600]

5.5 1.7 4.5 1.4

Page 43: CLASSIFICATION OF LOCAL ANESTHETICS

BupivacaineBupivacaineDeveloped from mepivacaine and is Developed from mepivacaine and is thus chemically related to lignocainethus chemically related to lignocaineDiffers from mepivacaine in that a Differs from mepivacaine in that a methyl group in the piperidine ring methyl group in the piperidine ring has been replaced by a butyl grouphas been replaced by a butyl groupProprietary name: Marcaine, Proprietary name: Marcaine, SensorcaineSensorcaine1-butyl-2,6-pipecoloxylidide 1-butyl-2,6-pipecoloxylidide (chemical name)(chemical name)4x as potent as lignocaine4x as potent as lignocaine

Page 44: CLASSIFICATION OF LOCAL ANESTHETICS

BupivacaineBupivacaine

Preparations:Preparations:

Has recently been available to the Has recently been available to the dental profession in conventional 1.8 dental profession in conventional 1.8 ml cartridgesml cartridges

Supplied in 10,30, & 50 ml vials Supplied in 10,30, & 50 ml vials containing 0.25%, 0.375%, 0.5%, containing 0.25%, 0.375%, 0.5%, 0.75% solutions available with or 0.75% solutions available with or without 1:200,000 adrenalinewithout 1:200,000 adrenaline

Page 45: CLASSIFICATION OF LOCAL ANESTHETICS

BupivacaineBupivacaineRecommended uses in DentistryRecommended uses in Dentistry

Few indications in routine restorative Few indications in routine restorative dentistrydentistryMain uses are in oral surgery—Main uses are in oral surgery—regional block, long lasting anesthesiaregional block, long lasting anesthesiaUseful for post-operative pain control Useful for post-operative pain control following procedures such as the following procedures such as the surgical removal of impacted third surgical removal of impacted third molarsmolarsShort-term temporary relief of acutely Short-term temporary relief of acutely painful conditions—trigeminal painful conditions—trigeminal neuralgianeuralgia

Page 46: CLASSIFICATION OF LOCAL ANESTHETICS

BupivacaineBupivacaine

Onset and duration of action:Onset and duration of action:Onset of action: longer than Onset of action: longer than lignocaine, may take more than 5 lignocaine, may take more than 5 minutes pulpal anesthesiaminutes pulpal anesthesiaDuration of action: longer 1.5 – 2 Duration of action: longer 1.5 – 2 hours pulpal anesthesiahours pulpal anesthesiaWhen used as a regional block, soft When used as a regional block, soft tissue anesthesia of 6 – 8 hours is tissue anesthesia of 6 – 8 hours is possiblepossible

Page 47: CLASSIFICATION OF LOCAL ANESTHETICS

BupivacaineBupivacaine

DosageDosage Total doses in the healthy adult Total doses in the healthy adult

should not exceed 2.0 mg/kg (0.9 should not exceed 2.0 mg/kg (0.9 mg/lb), not to exceed 225 mg with mg/lb), not to exceed 225 mg with epinephrine 1:200,000 and 175 mg epinephrine 1:200,000 and 175 mg without vasoconstrictor.without vasoconstrictor.

These total doses may be repeated These total doses may be repeated up to once every 3 hours not to up to once every 3 hours not to exceed 400 mg in 24 hoursexceed 400 mg in 24 hours

Page 48: CLASSIFICATION OF LOCAL ANESTHETICS

EtidocaineEtidocaine

Amide derivative that is structurally Amide derivative that is structurally similar to lidocainesimilar to lidocaine

4x as potent as lidocaine, with a 4x as potent as lidocaine, with a twofold increase in the duration of twofold increase in the duration of action, twice as toxicaction, twice as toxic

Proprietary name: DuranestProprietary name: Duranest

2-ethylpropylethylbutyroxylidide 2-ethylpropylethylbutyroxylidide (chemical name)(chemical name)

Page 49: CLASSIFICATION OF LOCAL ANESTHETICS

EtidocaineEtidocaine

Preparations:Preparations:

Dental local anesthetic cartridges as Dental local anesthetic cartridges as 1.5% solution with 1:200,000 1.5% solution with 1:200,000 adrenalineadrenaline

Onset and duration of actionOnset and duration of action

Onset of action: 2 – 3 minutes pulpalOnset of action: 2 – 3 minutes pulpal

Duration of action: long-acting Duration of action: long-acting anesthetic similar to bupivacaineanesthetic similar to bupivacaine

Page 50: CLASSIFICATION OF LOCAL ANESTHETICS

EtidocaineEtidocaine

Recommended use in Dentistry:Recommended use in Dentistry:Main indications for use are similar to Main indications for use are similar to those mentioned for bupivacaine as those mentioned for bupivacaine as a regional block anesthetica regional block anestheticWhen used in infiltration techniques When used in infiltration techniques for surgical procedures 1.5% for surgical procedures 1.5% etidocaine with 1:200,000 adrenaline etidocaine with 1:200,000 adrenaline is not as effective as 2% lignocaine is not as effective as 2% lignocaine with 1:80,000 adrenalinewith 1:80,000 adrenaline