Local Anesthesia CHEMISTRY

à Agent that interrupts pain impulses in a specific region of the body Esters:
without a loss of patient consciousness. à cocaine, procaine, tetracaine, and
à Completely reversible--the agent does not produce any residual chloroprocaine.
effect on the nerve fiber à hydrolyzed in plasma by pseudo-
à 1800-cocaine isolated from coca leaves shown to have local cholinesterase. One of the by-products of
anaesthetic properties metabolism is para-aminobenzoic acid, the
à 1884- Sigmund Freud noticed its anaesthetic effect while trying to common cause of allergic reactions seen
wean a patient from morphine addiction. Kollar first introduced it to with these agents
clinical ophthalmology as a topical ocular anaesthetic. Amides:
à 1884, Dr. William Stewart Halsted was the first to describe the à lidocaine, mepivicaine, prilocaine,
injection of cocaine into a sensory nerve trunk to create surgical bupivacaine, and etidocaine.
anesthesia. à Metabolized in the liver to inactive
à 1905-procaine: synthetic agent agents. Allergic reactions are rare
(especially with lidocaine)
à Local anaesthetics block nerve conduction 1. slow rate of depolarization
• reducing the influx of sodium ions into the 2. reduce height of action potential
nerve cytoplasm by binding directly to 3. reduce rate of rise of action potential
intracellular voltage-dependent sodium 4. slow axonal conduction
channels 5. ultimately prevent propagation of action potential
• Block primarily open and inactive sodium 6. do not alter resting membrane potential
channels, at specific sites
• Sodium ions cannot flow into the neuron,
thus the potassium ions cannot flow out,
thereby inhibiting the depolarization of the
nerve.
• If this process can be inhibited for just a few
Nodes of Ranvier along the way, then nerve
impulses generated downstream from the
blocked nodes cannot propagate (pass on) to
the ganglion.

Factors affecting local anaesthetic action Local Infiltration (Local Anaesthesia).

à Lipid solubility: primary determinant of intrinsic à Nerve endings in the skin and subcutaneous
anaesthetic potency. More lipophilic agents are more tissues are blocked by direct contact with a local
potent as local anesthetics anaesthetic
à Effect of pH: charged (cationic) form binds to receptor à Used primarily for surgical procedures involving a
site. Uncharged form penetrates membrane ,efficacy of small area of tissue (for example, suturing a cut).
drug can be changed by altering extracellular or intracellular à Lidocaine;benzocaine;tetracaine
pH
à Effect of protein binding - increased binding increases Surface Anaesthesia
duration of action à Application of a local anesthetic to skin or
à Effect of diffusibility - increased diffusibility = decreased mucous membranes.
time of onset à Surface anesthesia is used to relieve itching,
à Effect of vasodilator activity - greater vasodilator activity burning, and surface pain (for example, as seen in
= decreased potency and decreased duration of action minor sunburns).
• Lidocaine; benzocaine; tetracaine
Susceptibility to block by local anaesthetics of 1. pain
types of nerve fibres 2. cold Topical Block
à small nerve fibers are more susceptible than 3. warmth à Anaesthetic agent applied directly to
large fibers 4. touch mucous membrane surface (cornea;
- the type of fiber 5. deep pressure respiratory tract; oral mucosa)
- degree of myelination 6. motor à Used during examination procedures
- fiber length and ORDER OF (often in spray form)
- frequency- dependence are also SENSORY BLOCK • Lidocaine; tetracaine; benzocaine
important in determining susceptibility
 Epidural Anaesthesia VASOCONSTRICTERS:
Nerve Block à Accomplished by injecting a à Vasoconstrictors sometimes
à Local anaesthetic is injected local anaesthetic into the epidural combined with LA
around a nerve that leads to the space. à By decreasing blood flow =>
operative site. à The epidural space is above the decrease the rate of vascular
à More concentrated forms of dura (one of the coverings of the absorption of LA => allows more
local anaesthetic solutions are spinal cord). anaesthetic to reach the nerve
used for this type of anesthesia. • Lidocaine; bupivacaine membrane and improves the
à Used for surgery or dentistry
depth of anesthesia.
• Lidocaine;bupivacaine
à Epinephrine appears to be
the best vasoconstrictor
Spinal Anaesthesia
à Local anesthetic is injected into
the subarachnoid space of the
spinal cord to act on spinal roots
and spinal nerves
à Used for surgery to abdomen,
pelvis or leg if GA is contra-
indicated
• Mainly lidocaine

TOXICITIES OF LA
Hypersensitivity
à Such allergies are very rare
à There are two basic types of local anesthetics (the amide type and
the ester type). A patient who is allergic to one type may or may not
be allergic to the other type

Central Nervous System Toxicities

à if absorbed systematically in excessive amounts, can cause central
nervous system (CNS) excitement or, if absorbed in even higher
amounts, can cause CNS depression.
à excitement. Tremors, shivering, and convulsions characterize the
CNS excitement.
à depression. The CNS depression is characterized by respiratory
depression and, if enough drug is absorbed, respiratory arrest.

Cardiovascular Toxicities
à depression of the cardiovascular system.
à arteriolar dilation (except cocaine which is vasoconstrictive
à hypotension and a certain type of abnormal heartbeat
(atrioventricular block) characterize such depression.
à ultimately result in both cardiac and respiratory arrest.