LOCAL ANAESTHETICS

By

DR: Fahad Jibran Siyal (Ph.D.)

ASSOCIATE PROFESSOR

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ANESTHESIA

Loss of sensation either local or general;

resulting from pharmacological depression of
nerve function

It can be pathological vis. due to nerve

dysfunction e.g. DM, nerve compression

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LOCAL ANESTHESIA

Loss of sensation without loss of

consciousness or impairment of central

control of vital functions

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LOCAL ANESTHETICS

Drugs when applied locally  result in loss

of sensation in limited region of body

Prevent generation & propagation of nerve

action potentials

Result in loss of nociception

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domain of Local anesthetics

When locally applied in appropriate

concentration  act on  
√ Any part of NS
√ Every type of nerve fiber
When applied to nerve trunk  Paralysis of
both sensory & motor functions
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LOCAL ANESTHETICS

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 CLASSIFICATION

Surface / Topical anesthetics

 Lignocaine
 Tetracaine
 Cocaine
 Dyclonine
 Benzocaine
Have good penetration through skin/mucous memb.
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 CLASSIFICATION
Surface / Topical anesthetics (contd.)
Used for anaesthetizing
√ Nasal mucosa √ Oral
mucosa
√ Tracheobronchial system √ Esophagus
√ Rectum / anus √ Skin
√ Urethra / Vagina √ cornea 9
 Classification

Infiltration anesthetics
√ Lignocaine √ Bupivacaine
√ Prilocaine √ Procaine
√ Ropivacaine
Used for direct injection to tissue to paralyze
sensory nerve endings/cutaneous Nn.

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 CLASSIFICATION

Nerve block anesthetics

√ Lignocaine √ Bupivacaine
√ Procaine √ Pilocaine

√ Ropivecaine

Injected close to nerve trunks e.g. brachial

plexus, sacral plexus, cervical plexus, sciatic
nerve, intercostal Nn.
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 CLASSIFICATION

Spinal / Epidural anesthetics

√ Lignocaine √ Prilocaine

√ Bupivacaine √ Procaine

Injected into subarchnoid space

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 CLASSIFICATION

Spinal / Epidural anesthetics ….contd.

Called epidural anesthesia  B/w duramater &

bony spinal canal
Action is upon nerve roots, to induce regional
anesthesia
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 CLASSIFICATION

Intravenous regional anesthetics (Bier’s block)

√ Used for short surgical procedures

√ Drugs used  Lidocaine & Prilocaine

√ Used commonly in limbs

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 CLASSIFICATION

Intravenous regional anesthetics …contd:

√ Tourniquet applied distal to vein 15-30 min.

after procedure  to escape systemic toxic
drug absorption

√ Prolonged inflation of tourniquet leads to

ischemia
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CLASSIFICATION

I.R.A (Bier’s block) …..contd.

Disadvantages

 Pain returns quickly after procedure

 Only effective for few anatomical regions

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CLASSIFICATION

Esters of Benzoic acid Amides

 Cocaine  Lignocaine

 Procaine  Bupivacaine

 Tetracaine  Ropivacaine

 Benzocaine  Prilocaine
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PHARAMACOLOGICAL Properties

Ester types of LA  rapidly hydrolyzed by

plasma AchE  hence short half life

Amide types of LA  Metabolized in liver

Depress contraction of smooth muscles of

intestine

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 Clinical Properties

Produce highly effective analgesia in well-

defined areas of body

The anesthetic effect of LA  prolonged by

adding a vasoconstrictor agent like

adrenaline/NA that slows down the removal of

drug from injection site

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Clinical Properties

Local vasoconstriction is avoided at distal

parts of body e.g. fingers, glans

Onset of action  accelerated by adding

NaHCO3 this maximizes amount it drug in

more lipid-soluble from unionized

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 Clinical Properties

Repeated injections lead to Tachyphylaxis due to

extracellular acidosis( bcz. most LA are formed in
HCl salt to maximize aqueous solubility (pH 4.0-
6.0)
Pregnancy increases susceptibility to LA toxicity
due to elevated levels of estrogen/ progesterone

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Clinical Properties

LA have membrane-stabilizing effect hence

also used in neuropathic pain

Cocaine has an excellent penetration across

skin / mucosa with a tendency to diffuse
away from local site. Only disadvantage is

‘irritation’
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Clinical Properties

Sensitivity of nerve fibre to LA is related to

size of nerve fibre

Smaller fibers conducting pain , temp. and

autonomic activities are more susceptible to

actions of LA

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Mode Of Action

Site of action  Axolema (plasma memb.)

Reversibly block the initiation and

propagation of nerve impulse by preventing

voltage-dependant increase in Na+

conductance in axolema
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Mode Of Action

Nociceptive and sympathetic actions are

blocked first and motor Nn. are blocked last

LA normally abolish sensations but at higher

concentrations  motor activity also lost

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Mode Of Action

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TIME OF ONSET OF ACTION

Most LA are effective within 5 min. of

administration / injection

Duration of action  b/w 1-1.5 hours

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ADVERSE EFFECTS

They are directly related to 

 Concentration of drug

 Systemic absorption of drug

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ADVERSE EFFECTS

Hypersensitivity reactions
Localized infection / Haematoma
Paresthesiae (tingling sensation)
Nerve damage
Headache & Cauda aquina syndrome (related
to spinal anaesthesia)

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ADVERSE EFFECTS

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Toxicity

Toxicity  related with free drug

concentration

Neonates are more prone to toxicity

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Toxicity

Factors that increase plasma conc. of LA 

√ Cancer √ MI √ surgery √ Smoking

√ Trauma √ Uraemia

Factor that decreases free drug concentration

 √ Oral contraceptives
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Lidocaine (Xylocaine)

A prototype drug, introduced in 1948

Can penetrate upto 10 mm thickness

Rapidly absorbed from √ Parentral route

√ Gastrointestinal tract √ Respiratory tract

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Lidocaine (Xylocaine)
Dealkylated in liver by action of Oxidases
 Monoethylglycine xylitide & glycine
xylitide (75% excreted in urine)

Used in almost any condition where

intermediate anesthesia is required
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Lidocaine (Xylocaine)

Adverse Effects
Dose-related  √ Drowsiness √ Tinnitus
√ Dysgeusia √ Dizziness
√ Twitching
At higher doses  √ Seizures √ Respiratory
depression  Leading to COMA
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