LOCAL ANESTHETICS

Drugs producing REVERSIBLE loss of

sensation in a LOCALIZED area WITHOUT
LOSS OF CONSCIOUSNESS.
 *Classification
Esters Long acting Tetracaine

Short acting Procaine

Surface active Benzocaine

Cocaine
Tetracaine
Amides Long acting Bupivacaine
Ropivacaine

Medium acting Lidocaine

 *PHARMACOKINETICS
*Most are not absorbed from unbroken skin
*Absorption varies with agent, site, blood flow,
vasoconstrictors etc.
* For topical effect on intact skin used,
(PRILOCAINE & LIGNOCAINE)

*Effect terminated by removal from site

*Esters metabolized by plasma cholinesterases
*Amides are metabolized by cytochrome P450
iso-enzymes

*Liver dysfunction
*Acidification of urine promotes ionization
*Rapidly excreted via kidneys
 *MECHANISM OF ACTION
*Prevent generation & conduction of nerve
impulse

*Main site of action is cell membrane

*Inside cell dissociated to their ionized forms
*Bind with intracellular end of sodium
channels
 *CNS TOXICITY
* Sleepiness, vertigo, visual & auditory
disturbances

* Circumoral & tongue numbness, nystagmus,

muscle twitching, convulsions

* Excitatory effects, generalized CNS

depression

* Cocaine produces hallucinations, tremors,

insanity & addiction
*CARDIOVASCULAR SYSTEM
* Myocardial depression

* Cardiac arrhythmias

* PRILOCAINE large doses

methemoglobinemia (toluidine)

* Arteriolar dilatation, hypotension

except cocaine
 * INTOLERANCE/ALLERGY

* Allergic skin reactions or

asthmatic attacks or severe
anaphylactic reactions

* More common with ester type

*TYPES OF LOCAL ANESTHESIA
Surface (Topical)
anesthesia

Infiltrative anesthesia

Regional anesthesia Nerve Block

Intravenous (Bier’s block)

Epidural/Extradural

Spinal/Subdural/Sub-
arachinoid
 * SURFACE (TOPICAL) ANESTHESIA
* Can be produced by direct application of aqueous
solutions of salts of many LA or by suspension of
the poorly soluble LA

* Mucous membrane (nose, nasopharynx, mouth,

genitourinary tract) for mouth ulcers, fissures,
burns, male catheterization

* LIGNOCAINE, TETRACAINE, BENZOCAINE,

PRILOCAINE
 *INFILTRATIVE ANESTHESIA
* Injected in vicinity of nerve endings

* PROCAINE, LIGNOCAINE, BUPIVACAINE

* Can be mixed with epinephrine to prolong

effects

* Used for short procedures like abscess

drainage, wound stitching, dental
extraction, pain management etc.
 * REGIONAL ANESTHESIA/ FIELD BLOCK

*A specific part of body is anesthetized

* FOUR TYPES
* Nerve Block
* Intravenous (Bier’s block)
* Epidural/Extradural
* Spinal/Subdural/Sub-arachinoid
 * NERVE BLOCK ANESTHESIA

* Drug is injected near nerve

plexus or large peripheral nerves

* Used in orthopedic practice for

surgery of limbs
 *INTRAVENOUS ANESTHESIA
* Injected into a vein of a limb after applying cuff
proximal to area of injection

* Anesthesia occurs in 6–8 minutes and will last

for about 30–40 minutes

* Cuff deflated 20 min after the procedure

* LIGNOCAINE drug of choice, PRILOCAINE

 *EPIDURAL ANESTHESIA
* Injected in the thoracic, lumbar or sacral area in extradural
space

* Act on spinal nerve roots & paralyze them

* Usually employed in obstetric procedures
* LIGNOCAINE, CHLORPROCAINE, BUPIVACAINE
* Requires greater degree of skill as can be injected in to a vein
 *SPINAL ANESTHESIA
* Injected into subarachnoid space at L2.
* LIGNOCAINE, TETRACAINE & BUPIVACAINE
* Obstetric procedures, short surgical procedures like hernia,
perineal & lower limb surgery

* Hypotension due to sympathetic blockade, bed tilting, I/V saline

& adrenergic agonists

* Traumatic damage to nerve roots can occur

 Subarachnoid
Epidural Anaesthesia
Anaesthesia
Volume of drug Large (in extradural
Small (in fluid)
administered space)
Onset Fast Slow

Potential for patchy

Density of blockade Usually dense
sensory blockade

Opportunity for re- No, unless a catheter Yes, as catheter was

dosing was inserted (rare) inserted

Systemic blood levels

Negligible May be significant
of injected medications

Anatomic region Lumbar Any vertebral level

Ability to augment Excellent and for a

Minimal (< 24 hours)
postoperative analgesia number of days
* THANK YOU