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