Local Anesthetics
Local Anesthetics
Local Anesthetics
Esters
• Benzocaine
• Procaine/
• Proparacaine
Classification of LA
Amide
• Bupivacaine
• Levobupivacaine
• Lidocaine/Lignocaine
• Mepivacaine
Ionized
• Local anesthetics gain access to the
inner axonal membrane by
• 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
LA
• Infiltration anesthesia
• Regional anesthesia
• Surface anesthesia
LA
• Infiltration anesthesia
• Regional anesthesia
• Surface anesthesia
Regional anaesthesia
• Nerve block
• Intravenous
• Extradural
• Anaesthetise a region
Intravenous
• 0.5-1% lidocaine
without adrenaline
Extradural/epidural
• Thoracic, lumbar,
sacral
• Act on nerve roots
• No hypotention
Spinal anesthesia
• Sympathetic nerve
block
• hypotension
LA
• Infiltration anesthesia
• Regional anesthesia
• Surface anesthesia
• On intact skin – eutectic
mixture of bases of
prilocaine (EMLA)
• Slow absorption
Prolongation of action
• Add vasoconstrictor –
adrenaline
• Blockage of voltaged-gated Na
channel affects action potential
propagation throughout the body
• Convulsions
• Vasodilatation