LOCAL

ANAESTHETICS
 Definition
 Drugs that reversibly blocks the impulse
conduction and produces transient loss of
sensation in a restricted region of the body
without causing loss of consciousness.

 The order of block

Pain – Temp – Touch – Pressure
finally – Skeletal muscle power
Basic structure of LA
 Properties of LA
 Quick onset of action.
 Non irritating to the tissue to which it is applied.
 Low systemic toxicity
 Long duration of action to permit the
completion of procedure
 Free from allergic reactions
 Should not cause any permanent damage to the
tissue
 Classification

 According to Clinical Use

- Injectable anaesthetics
- Surface anaesthetics
 According to Structure
- Esters
- Amides
- Others
 Injectable anaesthetics
 Short- acting with low potency :
Procaine, chloroprocaine
 Intermediate -acting with intermediate
potency :
Lignocaine, mepivacaine, prilocaine,
articaine
 Long-acting with high potency :
Tetracaine, bupivacaine, ropivacaine
 Surface anaesthetics
Soluble Insoluble
Cocaine Benzocaine
Lignocaine Oxethazaine
Tetracaine Butylaminobenzoate
Benoxinate
 According to Structure
 Esters : Cocaine, procaine, chloroprocaine,
benzocaine,tetracaine

 Amides : Lignocaine, bupivacaine, dibucaine,

prilocaine, ropivacaine

 Others :Pramoxine, Dyclonine, Oxethazaine

Ester (Procaine)
Ester type
Short acting, low potency
Poor tissue penetrability and
hence no surface anesthetic
effect
Slow onset of action
Metabolized by esterases
Allergic reaction common
Mainly for infiltration and
nerve block
Amide (Lignocaine)
Amide type
Intermediate acting and
potency
Good tissue penetrability
Rapid onset
Metabolized by hepatic
microsomal enzymes
rare
Spinal, epidural, infiltration,
nerve block
 Mechanism of Action
LAs are weak bases

Available as HCl salts

(e.g. Lignocaine HCl)
At tissue pH (7.4)

Partly Partly
unionized ionized
(lipophilic)
Penetrates the nerve membrane

Enters the axon

Axonal pH
Re-ionization takes place

LAs block the voltage gated Na+

channels from inside
 No depolarization

No generation of action potential

No generation & conduction of

impulses to CNS

Local anaesthesia
 Both sensory as well as motor fibers are
affected
 LAs block - Sensory nerve endings
- Nerve trunks
- NMJ
- Ganglia, etc. ( Structures acting
through Na+ permeability)
 Smaller nerve fibres are more sensitive than
larger fibres
 Myelinated fibers are blocked first than
unmyelinated fibres
are blocked earlier than larger fibers
 Autonomic fibres are more susceptible
than somatic fibres
 Factors affecting local anesthetic action
pH

LAs are Weak Bases Inflamed & Infected Areas

pH

Unionized at Alkaline pH Ionized at Acidic pH

Increased Penetrability Poor Penetration of LAs

Through Membranes through Cell Membranes

Good Local Anaesthesia Therefore LAs are Less

Effective in these Areas
 Degree of plasma protein binding

 Duration of action depends upon the protein

binding
- Procaine : poorly bound to PP and has short
duration of action
-Bupivacaine: Highly bound to PP and has a
longer duration of action
 Rate of diffusion from the site of
administration

Higher the concentration - rapid onset of action

Lipid solubility
Higher the lipid solubility more is the
Potency of the drug

Lignocaine is more potent than

Procaine
 Vasoconstrictors in LA
 are the drugs that constricts the blood vessels
and thereby controls tissue perfusion

 are added to LA to oppose the vasodilatory

action of local anaesthetic agents.
Presence of vasoconstrictor (advantages)
LA + Vasoconstrictor (adrenaline)

LA + Vasoconstriction

Localized Systemic Local

action toxicity hemostatic
( Duration) effect
 Disadvantages & contraindications
due to vasoconstrictor with LA
 Intense vasospasm & ischemia in tissues
with end arteries may cause gangrene
e.g. Fingers, toes, ear lobule, tip of the
nose, etc.
 Absorption of adrenaline can cause
systemic toxicity
 May delay wound healing by reducing
the blood flow to the affected area
 Adverse effects

 CNS :
 low doses- tongue numbness, sleepiness,
lightheadedness, visual/auditory disturbances.
 Higher doses- nystagmus and muscular
twitching, convulsions
 CVS : Cardiac depression, bradycardia,
hypotension

Allergic reactions :
 Skin rashes, itching, erythema,
urticaria, wheezing & rarely anaphylactic
reaction – The incidence is more with
Esters than with Amides
 Mucosal irritation -cocaine
 Methemoglobinaemia - prilocaine
 Tetracaine

 Ester
 Highly lipid soluble, Highly potent
Highly toxic
 Has longer duration of action
 Uses - Spinal anesthesia
- surface anesthesia (eye,ear,
URT, etc.)
 Bupivacaine
 Amide
 Highly potent, Highly lipid soluble
 Highly cardiotoxic, has slower onset and
longer duration
of action
 Produces more sensory than motor
blocked – hence used for obst. analgesia
 Ropivacaine
 Congener of bupivacaine
 Less potent & Less cardiotoxic
 Duration of action is same as bupivacaine
 Epidural ropivacaine is used to control:
- post operative pain
- labour pain
 Dibucaine

 Very potent, Very toxic & Longest acting

 Uses:
- for spinal anaethesia
- for topical (surface anaesthetic)
on mucous membrane & skin
 Lignocaine
 Amide type local anaesthetics
 Rapid action, can be used as antiarrhytmic agent in
the treatment of ventricular arryhtmias.
Pharmacokinetics:
 Absorbed rapidly after parenteral administration from
git
 Metabolised in liver,
 Half life- 90mins
 Excreted unchanged in urine
 Prilocaine

 Amide
 Has intermediate onset & intermediate
duration of action
 Has poor vasodilatory effect
 Uses: Infiltration & Regional anaesthesia
 A/E : Methemoglobinaemia
Eutectic Mixture of Local Anaesthesia
(EMLA)

Lig 2.5% + Prilo 2.5% (cream)

The Melting point of the Mixture is Less
than either drug alone
At room temp.
exists as Oil
Can penetrate intact skin up to 5 mm depth
 Uses
- Venipuncture
- Skin graft procedures
 EMLA must not be applied to the
Mucous membrane
 EMLA is CI Methemoglobinemia
 Benoxinate

 Good surface anaesthetic

 Used to anaesthetize cornea for tonometry

 Oxethazaine

 Topical anaesthetic
- to anaesthetize gastric mucosa
- produces symptomatic relief in gastritis
- available with antacids
 Benzocaine
Butylaminobenzoate

 Poorly water soluble

 Poorly absorbed on topical administration
 Uses:
- as lozenges in sore throat
- as powder/ointment on wounds/ulcers
- as suppository for anorectal lesions
 TECHNIQUES
OF
LOCAL ANAESTHETICS
SURFACE ANAESTHESIA
 Surface anaesthesia

 Sensory nerve endings are blocked

 Only superficial layer is anaesthetized
 applied to mucous membranes & abraded skin
- nose, mouth, eyes, throat, URT, urethra, ulcers,
burns, fissures, etc
 Eg- Lignocaine, Tetracaine, Benzocaine, Cocaine
 Surface anaesthesia

 Available as ointment, gel, cream, spray,

lozenges, suspension, suppository, etc.

 Uses: Tonometry, painful lesions, fissures,

burns, i.v. cannulation during endoscopies, etc.
INFILTRATION ANAESTHESIA
 Infiltration Anaesthesia
 Dilute solution of LA injected under the skin
to block the sensory nerve endings.
 Used for minor surgical procedures:
 Eg: incisions, excisions, suturing etc.
 Lignocaine , Bupivacaine can be used
 Field Block
 Injecting LA subcutaneously
 Anaesthetizes the area distal to the inj.
 Uses: For minor procedures on
- scalp, ant. abdominal wall, upper and
lower limbs, etc.
 Nerve block

 LA is injected very close to or around the

peripheral nerve or nerve plexuses

 Brachial plexus block - upper limb

 Cervical plexus block - neck
 Intercostal nerve block – ant. abdominal
SPINAL ANAESTHESIA
 Spinal Anaethesia
 LA injected in the subarachnoid space between
L2-3 or L3-4 of the spinal cord.
 LA of choice- Lignocaine(3-5%),
Bupivacaine(0.5-0.8%), Tetracaine(0.3%-0.5%)

Indications
 Orthopaedic surgery of lower limbs and pelvis.
 Surgery of lower abdomen
 Gynaecological and obstestrics surgeries
Complications
Hypotension
Headache(PDPH)- due to leakage of CSF through
the hole in duramater. Prevented by using small
bore needle.
PDPH is treated by lying down for 24 hrs, plenty
of fluids, abdominal compression.
Others:
Urinary retention
Paralysis of cranial nerves
Meningitis, etc
EPIDURAL ANAESTHESIA
 Epidural anaesthesia
 Given in epidural space(between duramater
and bone) with tuohy’s needle.
 Indicated mostly for controlling :
 post operative pain, upper abdominal
surgeries, thoracic surgeries, painless labour,
chronic pain due to cancer and other
conditions
Spinal versus Epidural anaesthesia
 Spinal anaesthesia is highly reliable, easy to
place and has very quick onset of action.
---It is indicated only for the surgeries of limited
duration, redosing cannot be done. PDPH is its
complication
 Epidural anaesthesia is less reliable, difficut to
perform. Can be used for surgeries of any
duration. Chances of PDPH is very less
INTRAVENOUS REGIONAL
ANAESTHESIA
 Intravenous regional anaesthesia
(Bier’s block)
 Indicated for any procedure on the arm below
elbow or in the leg below knee that will be
completed within 40-60 minutes.
 LA is injected into the vein of the limb
where blood flow is occluded by a
tourniquet
 Mainly used to anaesthetize upper limb
 Lignocaine and prilocaine