Clinical actions of specific

agents
BY -
M I T A L K A T A RI Y A
3 R D Y E A R B. D . S .
 Acknowledgements
Firstly, I would like to thank Dr. Namish Batra , Dr.
Dharti Bhatt and Dr.Nazneen for giving me this
opportunity.
I would like also like to thank my senior interns for
guiding me all though.
Lastly, I would like to thank my friends for helping me
when required.
Thank you to all.
 Contents

Duration
Maximum doses of LA
Ester-type LA
Amide-type LA
Anesthetics for topical application
Selection of LA
 Duration

Factors affecting the depth and duration of a drug’s

anesthetic action are:
1. Individual response to drug
2. Accuracy in deposition of LA
3. Status of tissue at the site of drug deposition
4. Anatomic variations
5. Type of injection administered
 Normal distribution curve (bell-shaped curve)

Variations in individual response to drug is depicted

in normal distribution curve.
According to curve individuals can be divided into 3
categories:
1. Normo-responders
2. Hyperresponders
3. Hyporesponders
 Normo-responders :
• Duration of anesthesia 60 minutes.
• In 70% people.
 Hyperresponders:
• Duration of anesthesia 70-80 minutes.
• Approximately 15% people.
 Hyporesponders:
• Duration of anesthesia 15-40 minutes or even less.
• Approximately 15% people.
 Accuracy in administration of LA

Deposition of LA close to nerve provides greater

depth and duration of anesthesia compared with an
anesthesia deposited at a greater distance from the
nerve to be blocked.
Not significant in supraperiosteal technique
Not significant with articane
 Status of tissue into which LA is deposited

Inflammation, infection, or pain (acute or chronic)

usually decreases depth and anticipated duration of
anesthesia.
Increased vascularity at the site of drug deposition
results in more rapid absorption of LA and a
decreased duration of anesthesia.
 Anatomic variation

Supraperiosteal infiltration, usually effective in

providing pulpal anesthesia for all maxillary teeth,
provides a shorter duration than expected when
alveolar bone is more dense than usual.
When zygomatic arch is lower, infiltration anesthesia
of maxillary first and second molar may provide
shorter duration or may even fail to provide
adequate depth of pulpal anesthesia.
The palatal root of maxillary molars may not be
adequately anesthetized when the root flares greatly
towards the midline of the palate.
In the mandible, it is stated that supraperiosteal
infiltration is not effective in adults because their
cortical plate of bone is too thick.
 Type of injection administered

Administration of a nerve block provides a longer

duration of pulpal and soft tissue anesthesia than is
provided by supraperiosteal injection.
LA Infiltration (min) Nerve Block (min)

Mepivacaine HCl 5-10 20-40

3% no vasoconstrictor

Prilocaine HCl 10-15 40-60

4% no vasoconstrictor

Bupivacaine HCl 60 Up to 12 hours

0.5%+epinephrine
1:200000
 Maximum doses of LA

Doses of local anesthetic drug are presented in terms

of milligram of drug per unit of body weight (eg. As
mg/kg or as mg/lb).
Two groups of patients represent potentially
increased risk from overly high LA blood levels:
1. The smaller, lighter-weight child
2. The debilitated elderly individuals
The maximum recommended dose calculated
should always be decreased in medically
compromised, debilitated, or elderly persons.
Changes in liver function, plasma protein binding,
blood volume, and other important physiologic
functions influence the manner in which LA are
distributed and biotransformed.
The net result of these changes is increased plasma
blood levels of drug, associated with increased
relative risk of overdose reaction.
Ester-type local anesthetics
 Ester Group

 Benzoic acid esters:

 Cocaine (topical only)
 Benzocaine (topical only)
 Para aminobenzoic acid esters:
 Procaine (novocain)
 Tetracaine (pontocaine)
 Propoxycaine(ravocaine)
 Procaine HCl

• Potency: 1 (procaine=1)
Toxicity: 1 (procaine=1)
Metabolism: hydrolyzed rapidly in plasma by plasma
pseudocholinesterase
Excretion: more than 2% unchanged in urine (90%
as para-aminobenzoic acid [PABA], 8% as
diethylaminoethanol)
 Anesthetic Half-Life: 6 minutes
 Nervous system:
o Procaine crosses the blood brain barrier and
producing the clinical appearance of both stimulation
and depression of the CNS.
 Cardiovascular system:
o Effects of procaine on CVS depend on the amount of
drug used.
o In small amounts, as used in dentistry, procaine has
no effect on CVS other than vasodilation of the area of
injection.
o In large doses procaine may produce hypotension by
a relaxation of the smooth muscles of the arterioles.
 Respiratory system:
o Procaine have little direct effect on the respiratory
system.
o Large toxic doses may severely depress respiration as
a result of the CNS.
o Toxic overdose of LA , respiratory arrest occurs
before cardiac arrest.
Vasodilating properties: produce the greatest
vasodilation of all currently used LA
pH of plain solution: 5.0 to 6.5
pH of vasoconstrictor containing LA: 3.5 to 5.5
Onset of action: 6 to 10 minutes
Effective dental concentration: 2% to 4%
Anesthetic half-life: 0.1 hour (6 minutes)
Topical anesthetic action: not in clinically acceptable
concentrations
 Propoxycaine HCl

Chemical formula: 2-Diethylaminoethyl-4-amino-2-

propoxybenzoate hydrochloride
Potency: 7 to 8 (procaine=1)
Toxicity: 7 to 8 (procaine=1)
Metabolism: hydrolyzed in both plasma and liver
Excretion: via kidney; almost entirely hydrolyzed
Vasodilating properties: yes, but not as profound as
those of procaine
Onset of action: rapid (2 to 3 minutes)
Effective dental concentration: 0.4%
Topical anesthetic action: not in clinically acceptable
concentrations

It was combined with procaine in solution to provide

more rapid onset and more profound and longer-
lasting anesthesia than could be obtained with
procaine alone.
Amide-type local anesthesia
 Amide Group

 Bupivacaine (marcaine, sensorcaine)

 Etidocaine ( duranest)
 Lidocaine (xylocaine, lignocaine)
 Mepivacaine (carbocaine)
 Prilocaine (citanest)
 Articaine
 Lidocaine HCl

Potency: 2 (compared to procaine=1) [lidocaine=1

for all LA]
Toxicity: 2 (compared to procaine)
Metabolism: in liver, by microsomal fixed-function
oxidase
Excretion: via kidney; less than 10% unchanged,
more than 80% various metabolites
Vasodilating properties: less than procaine, greater
than prilocaine and mepivacaine
pH of plain solution: 6.5
pH of vasoconstrictor-containing solution: 3.5
Onset of action: rapid (3 to 5 minutes)
Effective dental concentration: 2%
Anesthetic half-life: 1.6 hours (90 minutes)
Topical anesthetic action: yes (in clinically
acceptable concentration [5%])
Lidocaine without vasoconstrictor= 4.4mg/kg
With vasoconstricter= 7mg/kg
Nervous system:
o In toxic doses of lidocaine first produces stimulation then
depression of the CNS.
o Convulsions may be induced.
 Cardiovascular system:
o The effect of lidocaine on the CVS depend on the dose used.
o Large doses produce-
Decrease in the electrical excitability of myocardium.
Decrease in the force of contraction.
 Respiratory system:
o Small doses of lidocaine have a mild bronchodilating
effect on the respiratory system.
o Overdose of LA cause respiratory arrest (apnea).
%LA Vasoconstri Pulpal Soft tissue MRD
ctor duration duration
2 Epinephrine 60 180-300 7 mg/kg
1:50000
2 Epinephrine 60 180-300 7 mg/kg
1:100000
 Mepivacaine HCl

Chemical formula: 1-methyl 2’,6’-pipecoloxylidide

hydrochloride
Potency: 2 (procaine=1; lidocaine=2)
Toxicity: 1.5 to 2 (procaine=1; lidocaine=2)
Metabolism: in liver, by microsomal fixed-functional
oxidase
Excretion: via kidney; approx. 1% to 16% unchanged
Vasodilating properties: slight vasodilation
pH of plain solution: 5.5 to 6.0
pH of vasoconstrictor containing solution: 4
Onset of action: rapid (3 to 5 minutes)
Effective dental concentration: 3% w/o
vasoconstrictor; 2% with vasoconstrictor
Anesthetic half-life: 1.9 hours
Topical anesthetic action: not in clinically acceptable
concentrations
% LA Vasoconstri Pulpal Soft tissue MRD
ctor duration duration
3 None 20-infiltration 120-180 6.6mg/kg
2 Levonordefrin 60 180-300 6.6mg/kg
 Prilocaine HCl

Chemical formula: 2-Propylamino-o-

propionotoluidine hydrochloride
Potency: 2
Toxicity: 1
Metabolism: hydrolyzed by hepatic amidase
Excretion: via kidney
Vasodilating properties: produces greater
vasodilation than mepivacaine but less than lidocaine
pH of plain solution: 6 to 6.5
pH of vasoconstrictor containing solution: 4
Onset of action: slightly slower than lidocaine (3 to 5
minutes)
Effective dental dose: 4%
Anesthetic half-life: 1.6 hours
Topical anesthetic action: not in clinically acceptable
concentrations
% LA Vasoconstri Pulpal Soft tissue MRD
ctor duration duration
4 None 10-15 90-120 7.9 mg/kg
infiltration infiltration
40-60 nerve 120-240 nerve
block block
4 Epinephrine 60-90 180-480 7.9 mg/kg
1:200000
 Articaine HCl

Chemical formula: 3-N-Propylamino-proprionylamino-

2-carbomethoxy-4-methylthiophene hydrochloride
Potency: 1.5 times that of lodocaine; 1.9 times that of
procaine
Toxicity: similar to lidocaine and procaine
Metabolism: occurs in both plasma (by plasma
esterase) and liver (by hepatic microsomal enzymes)
Excretion: via kidney; approx. 5% to 10% unchanged,
90% metabolites
Vasodilating properties: equal to lidocaine
pH of vasoconstrictor containing solution: 3.5 to 4
Onset of action: articaine 1:200000, infiltration 1 to
2 minutes, mandibular block 2 to 3 minutes
Effective dental dose: 4% with 1:100000 or
1:200000 epinephrine
Anesthetic half-life: 0.5 hours (27 minutes)
Topical anesthetic action: not in clinically acceptable
concentrations
% LA Vasoconstri Pulpal Soft tissue MRD
ctor duration duration
4 Epinephrine 60-75 180-360 7 mg/kg
1:100000
4 Epinephrine 45-60 120-300 7 mg/kg
1:200000
 Bupivacaine HCl

Chemical formula: 1-Butyl-2’,6’-pipecoloxylidide

hydrochloride
Potency: four times that of lidocaine, mepivacaine
and prilocaine
Metabolism: metabolized in liver by amidase
Excretion: via kidney; 16% unchanged bupivacaine
has been recovered from human urine
Vasodilating properties: relatively significant,
greater than lidocaine and mepivacaine
pH of plain solution: 4.5 to 6
pH of vasoconstrictor containing solution: 3 to 4.5
Onset of action: slower onset time than other
commonly used LA (6 to 10 minutes)
Effective dental dose: 0.5%
Anesthetic half-life: 2.7 hours
Topical anesthetic action: not in clinically acceptable
concentrations
% LA Vasoconstri Pulpal Soft tissue MRD
ctor duration duration
0.5 Epinephrine 90-180 240-540 United states:
1:200000 no mg/kg
listed
Canada:
2mg/kg
Anesthetics for topical
application
Use of topical LA is an important component of
atraumatic administration of intraoral LA.
Concentration of LA applied topically is greater than
that of LA administered by injection.
Higher concentration facilitates diffusion of drug
through mucous membrane.
Higher concentration also increases risk of toxicity,
both locally to tissue and systemically if drug is
efficiently absorbed.
Topical anesthesia are effective only on surface
tissues (2 to 3 m). Tissues deep to area of application
are poorly anesthetized, if at all.
The topical application of benzocaine and lidocaine
are water insoluble. However they are soluble in
alcohol, propylene glycol, polyethylene glycol, and
other vehicles suitable for surface application
 Benzocaine

1. Poor solubility in water

2. Poor absorption into CVS
3. Systemic toxic reactions virtually unknown
4. Not suitable for injection
5. Localized allergic reaction may occur after
prolonged or repeated use
6. Available as aerosol, gel, gel patch, ointment, and
solution
7. It is an ester LA (ethyl p-aminobenzoate)
 Cocaine hydrochloride

1. Rapid onset, usually within one minute

2. Long duration of action, as long as 2 hours
3. Rapidly absorbed but slowly eliminated
4. Undergoes metabolism in liver and plasma
5. It is the only LA that consistently produce vasoconstriction
6. Clinical manifestation of mild overdose are euphoria,
excitement, restlessness, tremors, hypertension,
tachycardia, and tachypnea
7. Available concentration: 2% to 10%
8. Occurs naturally as white crystalline solid soluble in water
(benzomethylecgonine hydrochloride)
 Dyclonine hydrochloride

1. Slightly soluble in water

2. Potency equal to cocaine
3. Slow onset, require up to 10 minutes
4. Long duration, about 1 hour
5. Systemic toxicity extremely low
6. Not indicated for use as injection, irritating to tissue at site of
application
7. 0.5% solution is used in dentistry
8. It is a ketone derivative (4’-butoxy-3-piperidinopropiophenone
hydrochloride) w/o an ester or amide linkage that may be used
in patients allergic to common anesthetics.
 EMLA (Eutectic Mixture of LA)

EMLA cream is composed of lidocaine 2.5% and

prilocaine 2.5%
It is designed as a topical anesthesia able to provide
surface anesthesia for intact skin (other topical
anesthesia do not produce anesthesia on intact skin,
only abraded skin)
It is used during leg ulcer debridement and in
gynecologic procedures.
It is contraindicated for patients with congenital or
idiopathic methemoglobinemia, patients sensitive to
amine-type of LA and in infants below 12months.
 Lidocaine

1. Amide LA with an exceptionally low incidence of allergic

reaction
2. Maximum recommended dose following topical application is
200mg
3. Available as aerosol, spray, ointment, patch, and solution in
various dosage forms
4. Available as oral topical solution in 20mg/mL (viscous) and
40 mg/mL (solution)
5. It is available in 2 forms: poorly soluble in water (5%
concentration) and water soluble (2% concentration)
6. Water soluble form penetrates tissues more efficiently than
base form
 Tetracaine hydrochloride

1. Highly soluble in water

2. Applied topically, 5 to 8 times more potent than cocaine
3. Onset of action after topical application is slow
4. Duration of action approx. 45 minutes
5. Metabolized in plasma and liver
6. 2% concentration is used for topical application
7. Rapidly absorbed through mucous membrane
8. Great potential of systemic toxicity
9. It is a long-duration ester LA (2-dimethylaminoethyl-4-
butylaminobenzoate hydrochloride)
10. When used by injection, available as a 0.15% concentration.
 Selection of LA

A rational approach to selection of LA for a patient

includes following:
1. The length of time for which pain control is
necessary
2. The need for posttreatment pain control
3. Need for hemostasis
4. Whether any contraindication exist to
administration of selected LA
 Bibliography

Handbook of LOCAL ANESTHESIA by Stanley F.

Malamed
Google images
Monheim’s local anesthesia and pain control in
dental practice.
Thank You