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Local Anesthetics

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Local anesthetics

Kuliah Blok Traumatology 2018


Objectives
• Recall how an action potential is generated and
propagated
• Classify local anesthtics
• Describe the machanism of action,
pharmacokinetics and toxic effects of local
anesthetics
• Describe the different techniqes of use of LA
• Describe the risks and benefits of using
vasoconstrictors with LA
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
• Local anesthetics gain access to the
inner axonal membrane by

1. traversing sodium channels while they


are more often in an open
configuration

2. passage directly through the plasma


membrane
• Block
inititation
and
propagatio
n 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
LA

• Infiltration anesthesia

• Regional anesthesia

• Surface anesthesia
LA

• Infiltration anesthesia

• Regional anesthesia

• Surface anesthesia
Regional anaesthesia

• Nerve block

• Intravenous

• Extradural

• Intrathecal block/ spinal anaesthesia


Nerve block

• Inject a drug around


the nerve

• 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

• 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

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