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Laclassii 100612000838 Phpapp02

Local anesthetics work by reversibly blocking nerve impulses at localized sites without damaging neurons. They are commonly used in dermatology, dentistry, and for spinal or regional anesthesia. Local anesthetics block pain sensation and sympathetic functions by preventing the generation and conduction of nerve impulses. The mechanism of action involves preventing the entry of sodium ions needed for action potentials. Factors like lipid solubility and pH influence the onset and duration of local anesthetic effects.

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55 views18 pages

Laclassii 100612000838 Phpapp02

Local anesthetics work by reversibly blocking nerve impulses at localized sites without damaging neurons. They are commonly used in dermatology, dentistry, and for spinal or regional anesthesia. Local anesthetics block pain sensation and sympathetic functions by preventing the generation and conduction of nerve impulses. The mechanism of action involves preventing the entry of sodium ions needed for action potentials. Factors like lipid solubility and pH influence the onset and duration of local anesthetic effects.

Uploaded by

khuzaima9
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Local Anaesthetics

Common Uses of Local


Anaesthetics:

Dermatology
Excision
Dentistry

Spinal Anaesthesia
Definition:

Local anaesthetics are drugs which upon topical


application or local injection cause reversible loss of
sensory perception, especially of pain in a localized area
of the body.
Block generation and conduction of nerve impulses at a
localized site of contact without structural damage to neurons.

Clinically - to block pain sensation fromor sympathetic


vasoconstrictor impulses tospecific areas of the body
Loss of sensory as well as motor impulses
Some Clinical Examples of their
Use
Topically: Nasal mucosa and wound
margins
Infiltration: Vicinity of peripheral nerve
endings and major nerve trunks
Epidural or Subarachnoid spaces:
surrounding spinal nerves
Regional anesthesia: Intravenous
injection in arm or leg (Bier block)
Local Vs General Anaesthesia
General Local

Site of action CNS Peripheral nerves

Area Whole body Restricted areas

Consciousness Lost Unaltered

Preferential use Major surgery Minor surgery

Use in non-coperative Possible Not possible


patients
Poor health patient Risky Safer

Care for vital functions Essential Not needed


Chemistry of LA contd. (LAs are
Weak Bases)
Intermediate chain
Aromatic portion Amine portion
O
R

C O R N
R
ESTER

O R

NH C R N
R
AMIDE
LIPOPHILIC HYDROPHILIC
Chemistry of LAs contd.
ESTER LINKAGE AMIDE LINKAGE (2 EYES!!)

PROCAINE LIDOCAINE
procaine (Novocaine) lidocaine (Xylocaine)
tetracaine (Pontocaine) mepivacaine (Carbocaine)
benzocaine bupivacaine (Marcaine)
cocaine etidocaine (Duranest)
ropivacaine (Naropin)
Mechanism - LAs
As you know, entry of
Na+ is essential for Action
potential
Two things happen:
Rate and rise of AP and
maximum depolarization
decreases slowing of
conduction.
Finally, local depolarization
fails to reach threshold
potential conduction block.
Voltage gated Sodium Channel
Most LA are
in this form
at pH 7.4

B+H+ BH+ pH = 7.4


Nerve sheath

B+H+ BH+ pH = 7.4

Specific
B
action

pH = 6.9
axoplasm
B+H +
BH+ (active form)
Non-specific action
Influencing factor of LA action
Lipid solubility
All local anesthetics have weak bases. Increasing the lipid solubility leads
to faster nerve penetration, block sodium channels, and speed up the onset
of action.
Influence of pH
Lower pKa (7.6 7.8) faster acting (lidocaine, mepivacaine)
Higher pKa (8.1 8.9) slower acting (procaine, tetracaine, bupivacaine)
Vasoconstrictors
Cocaine itself is vasoconstrictor
Adrenaline
Potential adverse effects of vasoconstrictors
DONT use in areas of toes, fingers, ear lobes, penis (ischemia) and necrosis
Inflammation tends to produce lower pH in tissues therefore
LA are more ionized - dont penetrate very well
Blood flow
Decreased ability of LA to produce effects
Functions lost with LA
Answer The order of blockade:
Pain perception Initially gr.`C` fibres are
Temperature blocked pain and
sympathetic
Touch sensation
vasoconstrictors
Proprioception
Then gr.`A` fibres
Skeletal muscle tone
Pain temperature
touch - pressure and
vibration motor fibres
(Muscle)
Tongue: bitter sweet
sour - salt
Undesired effects of LA contd.
CNS Stimulation:
(More sensitive than cardiac)
Dose-related spectrum of effects
and All effects are due to
depression of neurons
First an apparent CNS
stimulation (convulsions
most serious)
Followed by CNS depression
(death due to respiratory
depression)
Premonitory signs include:
ringing in ears, metallic taste,
numbness around lips

Cocaine - euphoria (unique in its


ability to stimulate CNS)
Lidocaine - sedation even at non-
toxic doses
Cardiovascular System
ARRHYTHMIAS: direct HYPOTENSION: Arteriolar
effect (More resistant dilation is a result of:
than CNS) Direct effect (procaine and
Decrease cardiac lidocaine have most effect)
excitability and contractility Block of postganglionic
Decreased conduction sympathetic fiber function
rate CNS depression
Increased refractory rate Avoid by adding
(bupivicaine)
vasoconstrictor to the
ALL can cause
preparation
arrhythmias if conc. is high
enough Cocaine is exception:
Note: cocaine is produces vasoconstriction,
exception......it blocks catecholamine
stimulates heart reuptake
EMLA application
Newer Techniques of LA
Iontophoresis: Lidocaine-soaked sponges
ou
Y Most LA are
in this form

nk at pH 7.4

h a B+H+ BH+ pH = 7.4

T Nerve sheath

B+H+ BH+ pH = 7.4

Specific
B
action

pH = 6.9
axoplasm
B+H +
BH+ (active form)
Non-specific action

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