LOCAL ANAESTHETICS
Dr. R. Jamuna Rani MD,
Professor & HOD,
Department of Pharmacology
LOCAL ANAESTHETICS
Local anaesthetics reversibly block
generation and conduction of nerve
impulses
Cocaine is the first naturally derived local
anaesthetic agent discovered in 1860
It was introduced in the clinical use by
Koller by 1884
Because of toxicity produced by cocaine a
synthetic derivative procaine was
discovered by EINHORN 1905
1943 lidocaine was synthesized by
LOFGREN
CHEMISTRY
Most local anaesthetics contains
hydrophilic group on one side and
liphopilic aroamtic group on the other are
connected by the alkyl chain through an
amide or ester linkage
They are weak bases
MECHANISM OF ACTION
The local anaesthetics interact with LA
receptor situated in the voltage sensitive
sodium channel and reduce the entry of
sodium ions
They produce membrane stabilizing
action. The action affecting the process of
depolarization leading to failure of
propagation of impulse without affecting
the resting potential
PHARMACOKINETICS
The ester type local anaesthetics are
metabolized by pseudocholinesterase
present in the plasma.
The amide linked local anaesthetics are
metabolized in the liver by dealkylation
and hydrolysis
LOCAL ACTIONS
They affect both sensory and motorfibres.
Autonomic fibres are more susceptible than
somatic fibres.
Small fibres are affected first than the larger
fibres.
Non myelinated fibres are blocked easily than
myelinated fibres.
Among the somatic afferents order of blockade
is pain – temperature – touch – deep pressure
Applied to the tongue bitter taste is lost first
followed by sweet and salt taste is last of all
LA & VASOCONSTRICTORS
Adrenaline (1:50000 – 1:200000)
Ephedrine, felypressin
The LA is given along with the
vasoconstrictor agent
Prolongs duration of action of LA by
decreasing their rate of removal from the
local site into the circulation
Reduces systemic toxicity
Provides more bloodless field for surgery
(Contd…)
Side effects:
It delay wound healing
Raise BP and promote arrhythmias in
susceptible individuals
C/I: LA + vasoconstrictor combination is
contraindicated in the surgery of toes,
fingers, pinna and penis.
SYSTEMIC ACTIONS
All LA are capable of producing CNS
stimulation followed by depression
The stimulation is due to inhibition of
inhibitory neurons
CLASSIFICATION
I. NATURAL
Cocaine
II. Synthetic
Injectable
INJECTABLE
Low potency, short duration
Procaine (ester)
Chloroprocaine (ester)
INTERMEDIATE POTENCY AND DURATION
Lignocaine (Lidocaine)
Prilocaine
HIGH POTENCY, LONG DURATION
Tetracaine (Amethocaine) (ester)
Bupivacaine
Ropivacaine
Dibucaine (Cinchocaine)
Bucricaine (Acridine derivative)
SURFACE ANAESTHETIC:
Soluble
NATURAL: Cocaine
Synthetic:
Lignocaine
Tetracaine
Benoxinate
Insoluble
Benzocaine (ester)
Butylaminobenzoate (Butamben)
Oxethazaine
BUCRICAINE
Bucricaine is a new LA derived from acridine has
inherent vasopressor action produce longer duration
of action less cardiotoxic. Used in opthalmic, dental
and surgical procedures
Procaine is not a good surface anaesthetic because
it does not penetrate into the intact skin and
mucous membrane
D/I: Procaine contains PABA which decreases the
antimicrobial action of sulphonamides.
Anticholinesterases increase the duration of action
of procaine
It forms poorly soluble salt with benzyl penicillin
procaine penicillin injected IM acts for 24 hrs.
Tetracaine and lignocaine produce skeletal
muscle relaxation very useful in cautery
Cocaine is a protoplasmic poison, drug of
addiction, cause dryness of cornea,
increase blood pressure, produce
mydriasis. It is banned because it is a
drug of addiction
Chlorprocaine produce neurotoxicity
Bupivacaine popularly used in obstetrics
practice (Mother can actively cooperate in
vaginal delivery) administered epidurally, less
likely to reach the foetus to produce neonatal
depression
SHOULD NOT BE GIVEN IV. because it
produces prolongation of QT interval and
induce ventricular tachycardia
Ropivacaine, bupivacaine congener less
cardiotoxic
Dibucaine is a longest acting LA more toxic
occasionally used for spinal anaesthesia
available as ointment, injection, ear drops
Benoxinate good surface anaesthetic for
eye (tonometry) available as 0.4% eye
drops
Benzocaine and butylaminobenzoate PABA
derivative can antagonise sulphonamide
locally. Used as lozenges for stomatits,
sore throat, dusting powder/ointment for
wound and ulcer and as suppository for
anorectal lesion
Oxethazaine (mucaine) it is administered
along with antacids for the symptomatic
relief of gastritis drug induced gastric
irritation, GO reflux and heart burn in
pregnancy. It desensitizes the gastrocolic
reflex and reduce PP urgency in irritable
bowel syndrome
Eutectic lignocaine/prilocaine it is applied
under occlusive dressing for 1hr before IV
cannulation, split skin graft harvesting and
venesection. It bridges between surface and
infiltration anaesthesia
METHODS OF APPLICATION OF
LA
Surface anaesthesia: Endoscopy, colonoscopy
etc.
Infiltration anaesthesia: Incisions, excisions,
hydrocele.
Nerve block anaesthesia: Tooth extraction and
neuralgia
Spinal anaesthesia: For abdominal, pelvic and
orthopaedic procedures
Epidural: Abdominal, pelvic, orthopaedic
procedures and post operative cardiac pain
IV regional anaesthesia: Upper limb surgery.
SYSTEMIC USES OF LA
Lignocaine, IV bolus used to terminate
ventricular arrhythmias, pain due to
cancer and severe pruritis
Procainamide is used orally in ventricular
arrhythmias
COMPLICATIONS OF SPINAL
ANAESTHESIA
Headache, respiratory paralysis,
hypotension, cauda equina syndrome,
meningitis, nausea and vomiting
DRUGS PRODUCING LA ACTION
Some other drug, eg. Propranolol,
chlorpromazine, H1 antihistaminics, quinine
have significant LA activity, but are not
used for this purpose because of local
irritancy or other prominent systemic
activity. Local anaesthesia can be produced
by cooling as well, eg. application of ice,
CO2 snow, ethylchloride spray
TETRODOTOXIN & SAXITOXIN
Biological toxins block the pore of the
sodium channel – prevent depolarization
Cause paralysis of respiratory muscles
requires respiration support in severe
cases
Blockade of vasomotor nerves cause
relaxation of VSM and responsible for
hypotension
TREATMENT
Early gastric lavage & pressor support are
indicated
If the patient survives for 24 hours the
prognosis is good with shellfish poisoning
