LOCAL ANAESTHETICS
Dr. Sanjay Kumar
Assistant Professor
Department of Pharmacology
CASE STUDY
CASE STUDY
CASE STUDY
CASE STUDY
Classification Local anaesthetics
Injectables local anaesthetics Surface local anaesthetics
Low potrncy Intermediate High potency Soluble Insoluble
short duration potency
• Procaine • Lidocaine • Tetracaine • Cocaine • Benzocaine
• Chlorprocaine (Lignocaine) • Bupvacaine • Lidocaine • Butylaminobenzocaine
• Ropivacaine • Tetracaine • Oxethzaine
• Prilocaine Proparacaine
• Dibucaine •
Major types of anaesthesia
Local anaesthetics
• A local anesthetic is a medication that causes absence of all sensation in a specific
body part without loss of consciousness, as opposed to a general anesthetic, which
eliminates all sensation in the entire body and causes unconsciousness.
Local anaesthetics
Features
• Cause reversible loss of sensory perception, especially of pain, in a restricted area of
the body.
• They block generation and conduction of nerve impulse at any part of the
neurone with which they come in contact
General Vs Local anaesthesia
S no Feature General anaesthesia Local anaesthesia
1 Site of action CNS Peripheral nerves
2 Aea of body Whole body Restricted area
3 Consciousness Lost Unaltered
4 Care of vital functions Essential Usually not needed
5 Physiological trespass High High Low
6 Poor health patient Risky Safer Risky Safer
7 Use in non-cooperative patient Possible Not possible
8 Major surgery Preferred Cannot be used
9 Minor surgery Not preferred Preferred
Local anaesthetics: Mechanism of action
LAs reversibly inhibit nerve transmission by binding voltage-gated sodium channels (Nav) in the nerve plasma
membrane.
• Na channels are integral membrane proteins, anchored in the plasma membrane. When LAs bind the sodium channel,
they render it impermeable to Na, which prevents action potential initiation and propagation
• Interact with a receptor situated within the voltage sensitive Na+ channel and raise the threshold of channel opening.
Local anaesthetics: effect of inflammation
The LA often fails to afford adequate pain control in inflamed tissues (like infected tooth).
The likely reasons are:
a. Inflammation lowers pH of the tissue—greater fraction of the LA is in the ionized
form hindering diffusion into the
axolemma.
b. Blood flow to the inflamed area is increased—the LA is removed more rapidly from
the site.
c. Effectiveness of Adr injected with the LA is reduced at the inflamed site.
Local anaesthetics: effect of adding vasoconstrictor
Addition of a vasoconstrictor, e.g. adrenaline (1:50,000 to 1:200,000):
ADVANTAGES
Prolongs duration of action of LAs by decreasing their rate of removal
from the local site into the circulation: contact time of the LA with the nerve
fibre is prolonged.
Enhances the intensity of nerve block.
Reduces systemic toxicity of LAs: rate of absorption is reduced and metabolism
keeps the plasma concentration lower.
Provides a more bloodless field for surgery.
DISADVANTAGES
Increases the chances of subsequent local tissue edema and necrosis as well
as delays wound healing by reducing oxygen supply and enhancing oxygen
consumption in the affected area.
May raise BP and promote arrhythmia in susceptible individuals.
Local anaesthetics: Adverse effects
CNS LOCAL HYPERSENSITIVITY
light-headedness, dizziness, CVS
auditory and visual Cardiovascular Rashes, angioedema,
Addition of
disturbances, toxicity of LAs dermatitis, contact
confusion, disorientation,
mental vasoconstrictors
menoinifeste as sensitization, asthma
shivering, twitchings, hypotension, cardiac the local enhances
bradycardia, rarely anaphylaxis occur and
arrhythmias, asystole tissue necrosis results.
rarely damage;
Involuntary methylparaben added as
and vascular collapse. Vasoconstrictors should not
movements, finally preservative in certain LA
convulsions be added for ring block of
hands, feet, fingers, toes, solutions is responsible for
This can be prevented and the allergic reaction.
penis and in pinna.
treated
Local anaesthetics: Precautions
• Before injecting the LA, aspirate lightly to avoid intravascular injection.
• Vasoconstrictor (adrenaline) containing LA should be avoided for patients with
ischaemic heart disease, cardiac arrhythmia, thyrotoxicosis, uncontrolled
hypertension, and those receiving β blockers (rise in BP can occur due to unopposed
α action) or tricyclic antidepressants (uptake blockade and potentiation of Adr).
Lidocaine (Lignocaine)
• Currently the most widely used LA.
• It is a versatile LA, good both for surface application as
well as injection
• Injected around a nerve it blocks conduction within 3
min, anaesthesia is more intense and longer lasting.
• It is used for surface application, infiltration, nerve
block, epidural, spinal and intravenous regional block
anaesthesia.
• Lidocaine 2% with or without adrenaline is the most
popular dental anaesthetic.
• Overdose causes muscle twitching, convulsions, cardiac
arrhythmias, fall in BP, coma and respiratory
Lidocaine (Lignocaine)
2% injection (with or without adrenaline) 5% heavy (for spinal anaesthesia) 2% with adrenaline 1:80,000 in 1.5 ml
cartridge for dental anaesthesia
Eutectic lidocaine/prilocaine
Also called eutectic mixture of local anaesthetics (EMLA)
• Unique preparation which can anaesthetise
intact skin after surface application.
• Lidocaine and prilocaine are mixed in equal
proportion. The resulting oil is emulsified into
water to form a cream
• Applied under occlusive dressing for 1 hr
before i.v. cannulation, split skin graft harvesting
and other superficial procedures.
• Numbness up to a depth of 5 mm lasts for 1–2 hr
after removal.
• It can be used as an alternative to lidocaine
infiltration
Bupivacaine
• More potent long-acting amide-linked LA, which is
used for infiltration, nerve block, epidural and
spinal anaesthesia of long duration
Peripheral nerve block: 0.25–0.5%
Spinal anaesthesia: 0.5% (hyperbaric)
Epidural anaesthesia: 0.25–0.5%
Continuous epidural analgesia: 0.125%.
Bupivacaine in obstetrics practice
• A 0.25% solution injected epidurally produces adequate
analgesia without significant motor blockade.
• Has become very popular in obstetrics (mother can
actively cooperate by ‘bearing down’ during vaginal
delivery)
• Used for postoperative pain relief by continuous epidural
infusion.
• Due to high lipid-solubility it distributes more in tissues
than in blood after spinal/epidural injection.
• Therefore, it is less likely to reach the foetus (when used
during labour) to produce neonatal depression
Bupivacaine in obstetrics practice
Bupivacaine in obstetrics practice
Instillation of Bupivacaine hydrochloride into the
surgical incision is a safe, well-tolerated treatment
and it is superior to traditional systemic pain
medication in both self-reported and clinical
outcomes.
Ropivacaine
• Newer bupivacaine congener, nearly as long
acting but less cardiotoxic.
• Continuous epidural ropivacaine has become
popular for relief of postoperative and labour
pain.
Proparacaine (proxymetacaine)
• Surface anaesthetic is the most commonly used ophthalmic anaesthetic now
• Tonometry can be performed 30 sec. after instilling one drop 0.5% proparacaine in the eye.
• Corneal anaesthesia lasts for 10–20 min.
• Deeper anaesthesia needed for cataract extraction can be obtained by applying 1–2 drops every
• 5–10 min. for a maximum of 5 applications while for foreign body/suture removal 2–3 applications may
be enough.
Benzocaine
• Because of very low aqueous solubility, these Las are not significantly absorbed from mucous
membranes or abraded skin.
• They produce long-lasting numbness without systemic toxicity
• Used as lozenges for stomatitis, sore throat.
Oxethazaine
• A potent topical anaesthetic, unique in ionizing to a very small extent even at low pH values.
• It is, able to anaesthetise gastric mucosa despite acidity of the medium.
• Swallowed along with antacids it affords symptomatic relief in gastritis, drug induced
gastric irritation, gastroesophageal reflux and heartburn of pregnancy.
• MUCAINE Oxethazaine 0.2% in alumina gel + magnesiumhydroxide suspension
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Clinical aspects of local anaesthesia
Surface anaesthesia
• Produced by topical application of a surface anaesthetic to
mucous membranes or abraded skin.
• Only the superficial layer is anaesthetised and there is no loss
of motor function.
• Onset and duration depends on the site, the drug, its
concentration and form, e.g. lidocaine (10%) sprayed in the
throat acts in 2–5 min and produces anaesthesia for 30–45 min.
• Addition of, but phenylephrine cause mucosal vasoconstriction
and prolong topical anaesthesia.
Clinical aspects of local anaesthesia
Infiltration anaesthesia
• Infiltration is used for minor operations,
e.g. incisions, excisions, hydrocele,
herniorrhaphy, etc. when the area to be
anaesthetized is small.
• Motor function is not affected.
• Dilute solution of LA is infiltrated under the
skin in the area of operation so that sensory
nerve endings are blocked
• Onset of action is almost immediate and
duration is shorter than that after nerve
block,
Clinical aspects of local anaesthesia
Local anaesthetic nerve block
• Local anesthetic nerve block (local anesthetic regional nerve blockade,
or often simply nerve block) is a short-term nerve block involving the
injection of local anesthetic as close to the nerve as possible for pain
relief.
• The local anesthetic bathes the nerve and numbs the area of the body
that is supplied by that nerve.
• The goal of the nerve block is to prevent pain by blocking the
transmission of pain signals from the affected area.
• Local anesthetic is often combined with other drugs to potentiate or
prolong the analgesia produced by the nerve block.
• These adjuvants may include epinephrine (or more specific
alpha-adrenergic agonists), corticosteroids, opioids, or ketamine.
Clinical aspects of local anaesthesia
Local anaesthetic nerve block
• Nerve blocks have a number of uses including treating headache disorders and providing anesthesia
during surgery. The pain relief provided by the block is present during the surgery and continues to
last after the procedure.
• This can lead to a reduction in the amount of opiates needed for pain control.
• The advantages of nerve blocks over general anesthesia include faster recovery, monitored anesthesia
care vs. intubation with an airway tube, and much less postoperative pain.
Anaesthesia: relevant anatomy of spinal canal
Spinal anaesthesia
• The LA is injected in the subarachnoid space between L2–3 or
L3–4, i.e. below the lower end of spinal cord.
• The primary site of action is the nerve roots in the cauda
equina rather than the spinal cord.
• Lower abdomen and hind limbs are anaesthetized
and paralysed.
• The level of anaesthesia depends on the volume and speed of
injection, specific gravity of drug solution and posture of the
patient.
• The duration of spinal anaesthesia depends on the drug
used and its concentration
• Addition of 0.2–0.4 mg of adrenaline to the LA prolongs
spinal anaesthesia
Spinal anaesthesia : clinical uses
Spinal anaesthesia
• The Spinal anaesthesia is used
for operations on the lower limbs, pelvis,
abdomen,
lower e.g. prostatectomy, fracture
setting, obstetric procedures, caesarean
section, etc.
Spinal anaesthesia Vs General anaesthesia
Spinal anaesthesia Vs General anaesthesia
Advantages of spinal anaesthesia over general anaesthesia are:
• It is safer.
• Produces good analgesia and muscle relaxation without loss of
consciousness.
• Cardiac, pulmonary, renal disease and diabetes pose less
problem.
Spinal anaesthesia
Complications
1. Respiratory paralysis
2. Hypotension
3. Neurological symptoms Pain and/or paraesthesias
4. Headache It may occur due to seepage of CSF,
which can be minimised by using smaller bore
needle.
5. Cauda equina syndrome
Spinal anaesthesia
Contraindications
1. Hypotension and hypovolemia.
2. Uncooperative or mentally ill patients.
3. Infants and children—control of level is difficult.
4. Bleeding diathesis.
5. Raised intracranial pressure.
6. Vertebral abnormalities e.g. kyphosis, lordosis, etc.
7. Sepsis at injection site.
Epidural anaesthesia
• Epidural anesthesia is a technique for
perioperative pain management with multiple
applications in anesthesiology.
• It is useful as a primary anesthetic, but most
commonly, it is used as a pain management
adjuvant. It can be a single shot or a continuous
infusion for long-term pain relief.
• Lidocaine (1–2%) and bupivacaine (0.25– 0.5%)
are popular drugs for epidural anaesthesia.
• Onset is slower and duration of anaesthesia is
longer with bupivacaine and action of both the
drugs is prolonged by addition of adrenaline.
Epidural catheter kit
Epidural anaesthesia
• Technically epidural anaesthesia is more difficult than spinal
anaesthesia and relatively larger volumes of drug are
needed.
• Cardiovascular complications are similar to those after spinal
anaesthesia, but headache and neurological complications
are less likely, because intrathecal space is not entered and
the LA is not restricted to a small area for long
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