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Local Anaesthetics
Dr. Pravin Prasad
M.B.B.S., MD Clinical Pharmacology
Lecturer, Lumbini Medical College
31 July 2018 (15 Shrawan 2075),
Tuesday
At the end of the class, MBBS
Sem IV students will be able
to:
Review relevant physiology of pain (definition,
conducting pathways, fibres, channels and ions
involved)
Classify local anaesthetics (LA)
Explain the mechanism of action of LA
List the actions of LAs
Discuss the salient features of different LAs
Individual compounds:
Cocaine
Good surface anaesthetic
Causes psychological dependence
Reverse tolerance might be seen
Stimulates most of the centres
Blocks uptake of NA in peripheral adrenergic
nerves
Not used due to higher side effects
Individual compounds:
Lignocaine
Used as surface and injectable anaesthesia
Onset of action after injection- 3 minutes
Action more intense and longer lasting
Cross sensitivity with ester LA not seen
Early CNS effects- depressant
Overdose: muscle twitching, convulsions,
arrhythmia, coma, respiratory arrest
Individual compounds:
Bupivacaine
Used as injectable LA:
Infiltration, nerve block
Epidural and spinal anaesthesia of long
duration
Use:
Painless labour
Post-operative pain relief
Individual compounds
Benoxinate
Surface anaesthetic for eye
0.4% solution for tonometry
Benzocaine, Butylaminobenzoate
Not absorbed through mucous membrane or
abraded skin
Long lasting anaesthesia
Used as lozenges, dusting powder,
Individual compounds:
Oxethazaine
Topical anaesthetic
Very low ionisation seen even at low pH
Used to anaesthetise gastric mucosa
Overdose:
More than 100mg/day
Dizziness and drowsiness
Uses: Surface anaesthesia
Lozenges
Mouth wash
Spray
Cream
Uses: Injectable anaesthesia
Infiltration Anaesthesia
Conduction block
Spinal block
Epidural anaesthesia
Intravenous regional anaesthesia
Conclusion
Local Anaesthetics cause reversible loss of
nerve conduction
Used for diminishing pain sensation
LAs binds to voltage gated Na+ channels from
inner side
Prefers activated and inactivated state of the
channel
Conclusion
Sensitivity of nerves for LA differs
LAs chemically are of two types
Inadvertent high dose or accidental intra
venous infusion can lead to CNS and CVS
effects
Depending upon the agent, LAs can be used
topically and by injectable route
Oxethazine can be used to anaesthetise
gastric mucosa
That’s all for LA!
Question???

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Local anaesthetics 2

  • 1. Local Anaesthetics Dr. Pravin Prasad M.B.B.S., MD Clinical Pharmacology Lecturer, Lumbini Medical College 31 July 2018 (15 Shrawan 2075), Tuesday
  • 2. At the end of the class, MBBS Sem IV students will be able to: Review relevant physiology of pain (definition, conducting pathways, fibres, channels and ions involved) Classify local anaesthetics (LA) Explain the mechanism of action of LA List the actions of LAs Discuss the salient features of different LAs
  • 3. Individual compounds: Cocaine Good surface anaesthetic Causes psychological dependence Reverse tolerance might be seen Stimulates most of the centres Blocks uptake of NA in peripheral adrenergic nerves Not used due to higher side effects
  • 4. Individual compounds: Lignocaine Used as surface and injectable anaesthesia Onset of action after injection- 3 minutes Action more intense and longer lasting Cross sensitivity with ester LA not seen Early CNS effects- depressant Overdose: muscle twitching, convulsions, arrhythmia, coma, respiratory arrest
  • 5. Individual compounds: Bupivacaine Used as injectable LA: Infiltration, nerve block Epidural and spinal anaesthesia of long duration Use: Painless labour Post-operative pain relief
  • 6. Individual compounds Benoxinate Surface anaesthetic for eye 0.4% solution for tonometry Benzocaine, Butylaminobenzoate Not absorbed through mucous membrane or abraded skin Long lasting anaesthesia Used as lozenges, dusting powder,
  • 7. Individual compounds: Oxethazaine Topical anaesthetic Very low ionisation seen even at low pH Used to anaesthetise gastric mucosa Overdose: More than 100mg/day Dizziness and drowsiness
  • 9. Uses: Injectable anaesthesia Infiltration Anaesthesia Conduction block Spinal block Epidural anaesthesia Intravenous regional anaesthesia
  • 10. Conclusion Local Anaesthetics cause reversible loss of nerve conduction Used for diminishing pain sensation LAs binds to voltage gated Na+ channels from inner side Prefers activated and inactivated state of the channel
  • 11. Conclusion Sensitivity of nerves for LA differs LAs chemically are of two types Inadvertent high dose or accidental intra venous infusion can lead to CNS and CVS effects Depending upon the agent, LAs can be used topically and by injectable route Oxethazine can be used to anaesthetise gastric mucosa
  • 12. That’s all for LA! Question???