LOCAL ANAESTHETICS
FOR DENTALS
WHAT IS A LOCAL ANAESTHETIC (LA)?
• A LA is a drug which reversibly blocks neural
transmission in the area where it is injected
• Does not necessarily affect the CNS
PHYSIOLOGY OF NERVE IMPULSES
• Neurons maintain a resting membrane potential
(RMP) of -60 to-70mV by active transport and
passive diffusion of ions
• Regulated by Na/K /ATP ase pumps (energy
dependent)
• Creates an ionic disequilibrium- K moves out of
the cells and Na into the cell
• Neuronal tisse –excitable tissue-susceptible to
changes in RMP- nresulting in action potentials
when the cells become more negative
MOA OF LOCAL ANAESTHETICS
• Normal impulse conduction relies on
depolarisation of nerve tissue- Na influx
• Neutral non-ionised fraction of LA crosses cell
membrane of the nerve
• In the lower pH of the neuron (6.9) becomes
ionised
• Ionised fraction binds to the IC binding site of Na
channel – prevents influx of Na and propagation
of impulse
NEWER THEORIES
• Blockage of K channels
• Blockade of Ca channels
• Blockage TRPV -1
STRUCTURE
• Lipophilic group
• Hydrophilic group
• Linked by intermediate chain – amide or ester
• Weak base
FACTORS AFFECTING ONSET
property effect
pKa Closer to normal= faster OOA
Lipid solubility solubility=slower OOA but
potency
Protein binding Binding = prolonged effect
Isomerism L(S) enantiomers = less toxic
Nerve anatomy Myelinated, smaller, increased
activity=easier blockade
Local factors Blood flow= decreased DOA
Vasoconstrictors = Increased
DOA and decreased OOA
CONTENTS OF A CARTRIDGE
• Local anaesthetic
• Vasoconstrictor
• Stabilising reducing agent
• Fungicide
• Preservatives
• MRL- an isotonic fluid
• Dental cartridges generally contain two drugs, namely, a local anaesthetic and a
vasoconstrictor, each having its own dose limitations.
• Serum concentrations are related to the total dosage rather than the concentration of the
solution,e.g. 2% or 4% local anaesthetic. Administering 20ml of 2%or 10ml of 4% (400mg)
produces the same serum concentration.2,3 Thus it is important to consider the dosage
(milligrams) administered and not the volume (milliliters or cartridges) of the local anaesthetic
administered. One should consider anaesthetic cartridges as containing 2ml and not 1.8ml to
simplify calculations, leading also to an overestimation of the dosage, thereby promoting safety
in limiting administration of the drug. Lignocaine 2% contains 36mg and articaine 4% contains
72mg of the drug per cartridge.
• Each local anaesthetic has its own maximum recommended dose (MDR), expressed in mg/kg.
Unfortunately, the mg/kg MDR for each drug varies in the literature from 4.4mg/kg8 to
6.6mg/kg.9
• Recommended maximum doses for healthy adults (Table 1) for lignocaine 2% is 4.4mg/kg,for
articaine 7mg/kg and for mepivicaine 6mg/kg with a ceiling dose approximate to those for a
70kg person.8,10
• Thus, the MDR of 2% lignocaine with adrenaline for a 15kg child = 15kg x 4.4mg/kg = 66mg
maximum dose of lignocaine. Since a lignocaine/cartridge contains 36mg of the drug this
equates to 1.5 cartridges.7
• A general conservative “rule of 10” may be used as a general guideline for maximum dosages
i.e. one cartridge per 10kg body weight (up to a maximum of 70kgs). Thus, the MDR for a 15kg
child would be 1.5 cartridges lignocaine.
SPECIFIC DRUGS USED
• LIGNOCAINE 2% (20MG/ML)
• Most commonly used amide (metabolised in liver)
• Protein bound drug
• OOA: 2-5 min
• DOA: 60-120 min
• XYLOTOX: 1:80 000 ADRENALINE (10MCG/ML)
• 70kg male: 500mg (3-7mg/kg) (10 x 2.2 ml
cartridges)
• NB neurotoxicity with overdose
• PRILOCAINE 3%
• pKa 7.6- protein binding 55%
• Amide group
• Rapid metabolism- least toxic of amides
• O-toluidine (metabolite of prilocaine) – risk of
methaemoglobinemia in dose related manner
• Dependent on renal clearance
• EMLA: ETECTIC MIXTURE OF LOCAL
ANAESTHETIC= 5%PRILOCAINE +5%LIGNOCAINE
(oil in water emulsion)
• Max dose: 8mg/kg
• BUPIVACAINE
• pKa 8.1, protein binding 95%
• OOA 5 – 8 MIN DOA: UP TO 12 HRS
• Metabolised by the liver
• Max dose: 3mg/kg
• Comes in 0.5% solution with adrenaline 1:200
000
ADDITIVES/ADJUVANT THERAPY
• ADRENALINE
• Significant vasoconstrictor- acts on alpha 1
receptors predominantly around blood vessels
• Vasoconstriction localises the LA around the sight
of surgery- increasing the DOA
• RISK OF BETA 1 AND 2 AGONISM = cardiovascular
side effects
• C/I in cardiac patients with unstable angina and
on MAOIs
ADDITIVES/ADJUVANT THERAPY
• NaHCO3
• Clonidine
• Ketamine
• Opioids
COMPLICATIONS AND TOXICITY
• Can be fatal!!!
• Appropriately managed
• CVS AND CNS toxicity depending on which agent
is used
EFFECT CVS CNS
INITIAL Toxic reactions- Circumoral pareshesia
hypertension and Tinnitus
tachycardia confusion
INTERMEDIATE/ Hypotension Convulsions and
EXCITATORY Myocardial seizures
depression Urine retention
Decreased CO
LATE/TERMINAL Vasodilatation Loss of consciousness
Severe Coma
hypotension Respiratory arrest
Bradycardia
Conduction
defects
Arrythmias
lignocaine
TREATMENT
• INTRALIPID 20%
• Lipid emulsion – causes a lipid “sink” to draw out
the LA from Na channel binding
• Provides lipid to cardiac myocyte where it unbinds
the LA allowing for return of myocyte contractility
( increases the concentration of lipid for the
mitochondria to use as energy)
• Dose: 1ml/kg IV stat, followef by
0.25ml/kg/minute until stable
• Can repeat bolus dose twice at 5min intervals
END
