Local anesthetics

Overview
• Local anesthetics produce a transient
and reversible loss of sensation
(analgesia) in a circumscribed region
of the body without loss of
consciousness.

• Normally, the process is completely

reversible.
ANESTHETICS
• Local anesthetics - esters or
amides
–a lipophilic aromatic group
–to a hydrophilic, ionizable amine.

• Most are weak bases

 Classification of LA
Esters

• Benzocaine

• Procaine/

• Proparacaine
 Classification of LA
Amide
• Bupivacaine

• Levobupivacaine

• Lidocaine/Lignocaine

• Mepivacaine
Ionized
• Block inititation and
propagation of action
potential
 Sequence of clinical anesthesia

•Sympathetic block (vasodilatation)

•Loss of pain and temperature sensation
•Loss of proprioception
•Loss of touch and pressure sensation
•Loss of motor function
 Anesthetic Potency

• Potency = lipid solubility

• Higher solubility = can use a

lower concentration and reduce
potential for toxicity
 DURATION OF ACTION

• Duration = protein binding

• Bupivacaine 95%
Lidocaine 65%
 Pharmacokinetics
• Effective within 5 min
• Duration of action – 1-1.5 h
• Activity is Ph dependent
• Increased action in acidic ph
 CLEARANCE

• ESTERS
hydrolysis via cholinesterase

• AMIDES
metabolism via hepatic enzymes
 Extradural/epidural
• Thoracic, lumbar,
sacral
• Act on nerve roots
• No hypotention
 Spinal anesthesia
• Sympathetic nerve
block
• hypotension
 Prolongation of action
• Add vasoconstrictor – adrenaline

• Can use a larger dose

• Not to – fingers, toes, nose, penis

 Adverse effects

• LA’s cause some vasodilatation at

site

• LA toxicity related to rate of

absorption via blood flow
 Systemic Toxicity
• Blockage of voltaged-gated Na
channel affects action potential
propagation throughout the body

• Potential is present for systemic

toxicity
 Effects of local anesthetics
• Excitation – anxiety, agitation, restlessness

• Convulsions

• Reduced myocardial contractility

• Vasodilatation