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LOCAL ANAESTHETICS
OPTOM FASLU MUHAMMED
• LA are agents which produce reversible block
of nerve conduction without any structural
damage to the neuron concerned and without
any loss of consciousness.
• local anesthetics are used to block all
sensation in the part supplied by the nerve.
• Most local anesthetic agents consist of a
lipophilic group (eg, an aromatic ring)
connected by an intermediate chain via an
ester or amide to an ionizable group (eg, a
tertiary amine)
CLASSIFICATION
• ESTER TYPE
-COCAINE, TETRACAINE, PROCAINE,
BENZOCAINE etc .
 AMIDE TYPE
-LIDOCAINE, BUPIVACAINE, PRILOCAINE,
DIBUCAINE etc.
MECHANISM OF ACTION
 Sensory information passes along nerve fibers via
electrical impulse, or action potential.
 When nerve is at rest , the interior has a negative
charge.
 An action potential is generated by the influx of Na
ions in to the interior of the nerve, giving it a positive
charge-Depolarization
 The nerve fiber is returned to its resting potential by
efflux of k ions- repolarization.
 The action potential is then generated along the axon
by successive depolarization & repolarization of
adjacent regions.
• The primary mechanism of action of local
anesthetics is blockade of voltage-gated
sodium channels .
• Bind to receptors near the intracellular
end of the voltage gated Na channels.
• This reduce the permeability of cell
membrane to Na ions , so action
potential is not generated.
USES
• FOREIGN BODY REMOVAL
• A drop of LA will make location & removal of
the offending object very much easier.
• TONOMETRY
• Topical anesthesia is essential for the
assessment of IOP
• CONTACT LENS FITTING- eye impressions for
the constriction of scleral lenses
• Certain diagnostic procedures: LA are used
before a schirmer test of lacrimal function.
Commonly used local anesthetics in
ophthalmic practice.
• Lidocaine- -1-4%
• Bupivacaine-0.25-0.75%
• Etidocaine-1-1.5%
• Prilocaine-1-2%
• Mepivacaine-1-2%
• Hexylcaine-1-2%
• Proparacaine-0.75%
• Tetracaine-0.5%
Common topical anesthetics.
Lignocaine-2-4%
Tetracaine-0.5%
Proparacaine-0.75%
Common regional anesthetics
Lignocaine-1-2%
Bupivacaine-0.5%
Hexylcaine-1-2%
Pharmacokinetics
ABSORPTION
Systemic absorption of injected local anesthetic
from the site of administration is determined
by several factors, including dosage, site of
injection, drug-tissue binding, local blood flow
• Application of a local anesthetic to a highly
vascular area such as the tracheal mucosa or
the tissue surrounding intercostal nerves
results in more rapid absorption
DISTRIBUTION
• The amide local anesthetics are widely
distributed after intravenous bolus
administration.
• After an initial rapid distribution phase, which
consists of uptake into highly perfused organs
such as the brain, liver, kidney, and heart, a
slower distribution phase occurs with uptake
into moderately well-perfused tissues, such as
muscle and the gastrointestinal tract.
METABOLISM AND EXCRETION
• The local anesthetics are converted in the liver
(amide type) or in plasma (ester type) to more
water-soluble metabolites and then excreted
in the urine.
• Ester type LA is metabolized by
pseudocholinesterase and amide type by
hepatic microsomal enzymes and enzyme
amidase.
SIDE EFFECTS
• Cardiovascular
-depression of heart, bradycardia, hypotension,
cardiac arrhythmias etc.
 CNS
-rapid absorption produce restlessness, tremor,
convulsions.
 Anaphylactic reaction
-common with ester type.
-causes asthma, dermatitis, skin rash etc.
• Corneal change
-very rarely reversible corneal change may occur.
ROUTES OF APPLICATION
• SURFACE ANAESTHESIA
-Most popular method in ophthalmology.
-lignocaine 4% is used .
INFILTRATION ANESTHESIA
 Nerve endings are anaesthetized by direct
exposure to drug.
 Drug is infiltrated subcutaneously
Procaine [2%] and lignocaine [2%] used.
NERVE BLOCK ANAESTHESIA
Drug is injected very close to nerve eg; brachial
plexus.
SPINAL ANAESTHESIA
Drug is injected to the subarachnoid spaces.
Eg; procaine and lignocaine.
EPIDURAL ANAESTHESIA
Drug is injected outside the dura.
Commonly used drug with LA
 Adrenaline –to prolong the effect of LA and to
reduce the toxicity by reducing absorption
from local area.
 Hyaluronidase-enzyme which cause
depolymerization of hyaluronic acid and
increase the permeability of injected fluid.
TETRACAINE [Amethocaine]
 Topical anaesthetic [0.5%] in ophthalmic
practice.
 Onset of action is 30 minutes.
 Side effects-stinging sensation, punctate ,drug
allergy.
PROPARACAINE
Topical anaesthetic. [0.75%]
Onset of action-30 sec
COCAINE
First local anaesthetic obtained from leaves of
plant Erythroxylon Coca.
It is no more in use nowadays because of its
corneal toxicity, addicting nature etc.
PROCAINE
• First synthetic local anaesthetic
• Used as a small area infiltration and spinal
anaesthetic.
• It is poorly absorbed from mucous membrane-
so no topical use.
• 2% injection is the usual preparation.
LIGNOCAINE
 Most commonly used LA
 In ophthalmology 4% [topical] and 2%
[infiltration] solutions are commonly used.
 It has quick onset of action and high degree of
penetration.
 The drug is recommended for topical, nerve
block, infiltration and epidural injection and
for dental analgesia.
 It may cause drowsiness.
BUPIVACAINE
• Onset of action is slow
• A 0.75% solution produce anaesthesia and
akinesia for 8-12 hours.
• In ophthalmic practice, usually a combination
of 2% lignocaine,0.75% bupivacaine and 7.5
TRU of hyaluronidase is used for periocular
injection, and surgery of any kind may be
performed on such type of anaesthetized eye.

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Local anasthetic

  • 2. • LA are agents which produce reversible block of nerve conduction without any structural damage to the neuron concerned and without any loss of consciousness. • local anesthetics are used to block all sensation in the part supplied by the nerve.
  • 3. • Most local anesthetic agents consist of a lipophilic group (eg, an aromatic ring) connected by an intermediate chain via an ester or amide to an ionizable group (eg, a tertiary amine)
  • 4. CLASSIFICATION • ESTER TYPE -COCAINE, TETRACAINE, PROCAINE, BENZOCAINE etc .  AMIDE TYPE -LIDOCAINE, BUPIVACAINE, PRILOCAINE, DIBUCAINE etc.
  • 5. MECHANISM OF ACTION  Sensory information passes along nerve fibers via electrical impulse, or action potential.  When nerve is at rest , the interior has a negative charge.  An action potential is generated by the influx of Na ions in to the interior of the nerve, giving it a positive charge-Depolarization  The nerve fiber is returned to its resting potential by efflux of k ions- repolarization.  The action potential is then generated along the axon by successive depolarization & repolarization of adjacent regions.
  • 6. • The primary mechanism of action of local anesthetics is blockade of voltage-gated sodium channels . • Bind to receptors near the intracellular end of the voltage gated Na channels. • This reduce the permeability of cell membrane to Na ions , so action potential is not generated.
  • 7. USES • FOREIGN BODY REMOVAL • A drop of LA will make location & removal of the offending object very much easier. • TONOMETRY • Topical anesthesia is essential for the assessment of IOP • CONTACT LENS FITTING- eye impressions for the constriction of scleral lenses • Certain diagnostic procedures: LA are used before a schirmer test of lacrimal function.
  • 8. Commonly used local anesthetics in ophthalmic practice. • Lidocaine- -1-4% • Bupivacaine-0.25-0.75% • Etidocaine-1-1.5% • Prilocaine-1-2% • Mepivacaine-1-2% • Hexylcaine-1-2% • Proparacaine-0.75% • Tetracaine-0.5%
  • 9. Common topical anesthetics. Lignocaine-2-4% Tetracaine-0.5% Proparacaine-0.75% Common regional anesthetics Lignocaine-1-2% Bupivacaine-0.5% Hexylcaine-1-2%
  • 10. Pharmacokinetics ABSORPTION Systemic absorption of injected local anesthetic from the site of administration is determined by several factors, including dosage, site of injection, drug-tissue binding, local blood flow • Application of a local anesthetic to a highly vascular area such as the tracheal mucosa or the tissue surrounding intercostal nerves results in more rapid absorption
  • 11. DISTRIBUTION • The amide local anesthetics are widely distributed after intravenous bolus administration. • After an initial rapid distribution phase, which consists of uptake into highly perfused organs such as the brain, liver, kidney, and heart, a slower distribution phase occurs with uptake into moderately well-perfused tissues, such as muscle and the gastrointestinal tract.
  • 12. METABOLISM AND EXCRETION • The local anesthetics are converted in the liver (amide type) or in plasma (ester type) to more water-soluble metabolites and then excreted in the urine. • Ester type LA is metabolized by pseudocholinesterase and amide type by hepatic microsomal enzymes and enzyme amidase.
  • 13. SIDE EFFECTS • Cardiovascular -depression of heart, bradycardia, hypotension, cardiac arrhythmias etc.  CNS -rapid absorption produce restlessness, tremor, convulsions.  Anaphylactic reaction -common with ester type. -causes asthma, dermatitis, skin rash etc.
  • 14. • Corneal change -very rarely reversible corneal change may occur.
  • 15. ROUTES OF APPLICATION • SURFACE ANAESTHESIA -Most popular method in ophthalmology. -lignocaine 4% is used . INFILTRATION ANESTHESIA  Nerve endings are anaesthetized by direct exposure to drug.  Drug is infiltrated subcutaneously Procaine [2%] and lignocaine [2%] used.
  • 16. NERVE BLOCK ANAESTHESIA Drug is injected very close to nerve eg; brachial plexus. SPINAL ANAESTHESIA Drug is injected to the subarachnoid spaces. Eg; procaine and lignocaine. EPIDURAL ANAESTHESIA Drug is injected outside the dura.
  • 17. Commonly used drug with LA  Adrenaline –to prolong the effect of LA and to reduce the toxicity by reducing absorption from local area.  Hyaluronidase-enzyme which cause depolymerization of hyaluronic acid and increase the permeability of injected fluid.
  • 18. TETRACAINE [Amethocaine]  Topical anaesthetic [0.5%] in ophthalmic practice.  Onset of action is 30 minutes.  Side effects-stinging sensation, punctate ,drug allergy.
  • 19. PROPARACAINE Topical anaesthetic. [0.75%] Onset of action-30 sec COCAINE First local anaesthetic obtained from leaves of plant Erythroxylon Coca. It is no more in use nowadays because of its corneal toxicity, addicting nature etc.
  • 20. PROCAINE • First synthetic local anaesthetic • Used as a small area infiltration and spinal anaesthetic. • It is poorly absorbed from mucous membrane- so no topical use. • 2% injection is the usual preparation.
  • 21. LIGNOCAINE  Most commonly used LA  In ophthalmology 4% [topical] and 2% [infiltration] solutions are commonly used.  It has quick onset of action and high degree of penetration.  The drug is recommended for topical, nerve block, infiltration and epidural injection and for dental analgesia.  It may cause drowsiness.
  • 22. BUPIVACAINE • Onset of action is slow • A 0.75% solution produce anaesthesia and akinesia for 8-12 hours. • In ophthalmic practice, usually a combination of 2% lignocaine,0.75% bupivacaine and 7.5 TRU of hyaluronidase is used for periocular injection, and surgery of any kind may be performed on such type of anaesthetized eye.