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
