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Local Anesthetics

Local anesthetics work by blocking sodium channels and preventing the propagation of action potentials, resulting in loss of sensation. They are classified as esters or amides. Amides like bupivacaine, levobupivacaine and lidocaine are commonly used. The mechanism of action, duration, and toxicity depend on factors like lipid solubility, protein binding, and metabolism. Local anesthetics can be administered through infiltration, regional techniques like nerve blocks, or intravenously and are used for various procedures with risks managed through proper dosing and addition of vasoconstrictors.

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164 views35 pages

Local Anesthetics

Local anesthetics work by blocking sodium channels and preventing the propagation of action potentials, resulting in loss of sensation. They are classified as esters or amides. Amides like bupivacaine, levobupivacaine and lidocaine are commonly used. The mechanism of action, duration, and toxicity depend on factors like lipid solubility, protein binding, and metabolism. Local anesthetics can be administered through infiltration, regional techniques like nerve blocks, or intravenously and are used for various procedures with risks managed through proper dosing and addition of vasoconstrictors.

Uploaded by

danti
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Local anesthetics

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
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
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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