Local Anesthetics

Introduction

local anesthetics are agents that produce a reversible blockade of

neural transmission in autonomic, sensory and motor fibers,

Preventing depolarization and action potential propagation

 Local anesthetics - Classes (Rule of “i’s”)

Esters Am”i”des
• Cocaine • lidocaine
• Procaine
• Bupivacaine
• Chloroprocaine
• Ropivacaine
• Tetracaine
• Etidocaine
• Mepivacaine
 Differences
ESTERS AMIDES
• Short duration of action & Less intense • Produce more intense and longer lasting
analgesia analgesia
• Higher risk of hypersensitivity • Rarely cause hypersensitivity reactions-

• Hydrolyzed by Plasma Cholinesterase in • Not hydrolyzed by Plasma Cholinesterase,

blood. but in liver
• Rarely used for Infiltration anesthesia • Most commonly used
But useful topically.
 Mechanism of Action of L A
• Ionized form of weak base blocks Na+ channels by binding to an internal
sequence involved in channel inactivation.

• to gain access to intracellular face of the Na+ channel, local anesthetics must
penetrate the nerve in the un-ionized, or neutral, form; hence, action is strongly
dependent upon local pH ( alkaline – good; acidic – bad)
 Factors related to LA

• Lipid solubility

• pH influence

• Protein binding
 Lipid solubility
• Lipid solubility is an important
characteristic.

• Potency is related to lipid

solubility, because 90% of the
nerve cell membrane is composed
of lipid.

• This improve transit into the cell

membrane
 pH influence
• Usually at range 7.6 – 8.9

• Decrease in pH shifts equilibrium toward the ionized form, delaying the

onset action.

• Lower pH, solution more acidic, gives slower onset of action

• Presence of Pus and inflammation will retard the action of LA. ( probably
low acidic pH)
 Protein binding
• Amide anesthetics are primarily protein bound

• Bupivicaine, levo bupivicaine and ropivicaine are more than

90% bound to alpha acid glycoproteins ( high affinity).
1
• Free or unbound fraction of the local anesthetic is active
 Esters
• Unstable in solution

• Rapidly hydrolysed by plasm cholinesterase

• More commonly associated with allergies

• Cocaine, Procaine, Chloroprocaine, Tetracaine
Of the following local anesthetics , which is not an ester ?

• procaine

• lidocaine

• tetracaine

• cocaine

• all of the above

 Commonly used amides

• Lidocaine

• Bupivacaine

• Levobupivacaine

• Mepivacaine

• Ropivacaine

• Etidocaine
 Lidocaine
• Rapid onset and medium duration of onset

• Amide anesthetic and a class 1b anti- arrhythmic drug

• Maximum dose 3 mg without epinephrine - 7 mg with epinephrine

• Local infiltration, topical anesthesia, epidurals,

 Bupivicaine

• Amide anesthetic

• Slow onset with a prolonged duration of action

• Maximum safe dose 2.5 mg

• Particularly cardiotoxic (it enters the Na channel fast but diffuses out
slowly

• Spinal and epidural anesthesia, nerve blocks, local infiltration

 Vasoactive additives epinephrine

• prolongation of local block

• increased intensity

• decreased systemic absorption of local anesthetic

 local anesthetic toxicities

• Allergic reactions: restricted to esters – metabolized to allergenic p-

amino benzoic acid (PABA)

• Cardiovascular: may be due to anesthetic (cardio depression,

hypotension) or vasoconstrictor (hypertension, tachycardia), monitor
pulse/blood pressure

• CNS: excitability (agitation, increased talkativeness – may →

convulsions) followed by CNS depression
 Therapeutic Uses

1. Surface anesthesia

2. Infiltration anesthesia

3. Conduction block

a. Field block b. Nerve Block

4. Spinal anesthesia

5. Epidural anesthesia

6. I V R A (Bier’s Block)
 1. Surface anesthesia

• Used in eye, throat, urethra, rectum and skin.

• Lidocaine
 Infiltration anaesthesia

• Around Nerve endings result in

anesthesia

• Procaine, Lidocaine 2 % are used either

with or without Adrenaline 1 : 2,00,000

 Nerve block or Conduction block

• Drug is injected close to the nerve or big

nerve trunks

• Nerve blocks are used for pain

treatment and management. Often a

group of nerves, called a plexus or

ganglion, that causes pain to a specific

organ or body region can be blocked

• eg. Brachial Block, Sciatic, Femoral

Nerve, Radial, Ulnar Nerves.

Axillary nerve glassopharyngeal nerve

Superior Laryngeal Nerve Median Nerve

 Spinal Anesthesia

• LA is injected into the subarachnoid space.

• When the anesthetic in injected outside the dura, the

technique is known as Epidural anesthesia.

• Lidocaine, Bupivacaine the two agents most commonly used

regularly in anesthesia practice.
 Complications of Spinal Anesthesia

Bradycardia

Hypotension

Headache

Septic meningitis
 I V R A (Bier’s Block)

• Intravenous regional anesthesia

• Agent of choice------ Lidocaine

• Used for only for Upper Limb orthopedic surgeries.

 What is the difference among these three?

• Lignocaine

• Xylocaine

• lidocaine

Thanks