Local Anaesthetics

For BDS

Dr.U.P.Rathnakar
MD.DIH.PGDHM

Learning objectives
Classification MOA Factors affecting[Adrenaline] Lignocaine Eutectic mixture Some adverse affects Uses or techniques

LA-Definition
Local anaesthetics (LA) are drugs Which when applied topically or injected locally, Block nerve conduction Cause reversible loss of all sensations in the restricted part supplied by the nerve, Without loss of consciousness Differences between GA & LA???

Chem structure-LAs
Ester linked Amide linked

Cocaine, Procaine, Chloroprocaine, Tetracaine, Benzocaine

Ligno. Bupiva, Dibu, Prilo, Ropiva

Intense, Longer lasting Not hydrolyzed by plasma esterases Less hypersensitivity No cross sensitivity with ester LAs

Clinical classification of LAs

Injectable anesthetics Surface anesthetics

Short acting with low

potency:

Procaine, Chloroprocaine. Intermediate acting

Soluble: Cocaine, Lignocaine, Tetracaine, Benzoxinate

with intermediate potency: Lignocaine,

Insoluble Benzocaine, Oxythazine

Mepivacaine, prilocaine Long acting with high potency: Tetracaine, Bupivacaine, Ropivacaine

MOA
LA-Injected into interstitial space

Enters axonal space Binds to receptors in intracellular half of Na channels Stabilizes the channel in inactive state Reduces the probability of channel opening

Unionized

Ionized

No depolarizationNo AP Conduction block

Factors affecting LA action

Differential sensitivity of nerve fibre Why?

Factors affecting.
Size of nerve fibres[Small & Large] Type[Myelinated or not, Symp & others] Lipophilicity & ph[pKa] Concentration of the drug Proximity to nerve Location of fibres[Outer & Inner] Inflammation Vasoconstrictors

Factors affecting LA action Lipophilic drugs penetrate the neuronal membranes better.

Factors affecting LA action

Concentration of LA
High concn. Provides favourable concentration gradient for penetration Also favors fast absorption into circulation and toxicity!

Proximity of application to nerve

Nearer the faster Not into the nerve!

Factors affecting.
Size of nerve fibres[Small & Large] Type[Myelinated or not, Symp & others] Lipophilicity & ph[pKa] Concentration of the drug Proximity to nerve Location of fibres[Outer & Inner] Inflammation Vasoconstrictors

Vasoconstrictors-Adrenaline
Increase contact period of LAs with nerve Counteracts local vasodilation by LA[Action on Symp.fibers] By decreasing absorption localizes the LA

Factors affecting LA action

[1:50000-200000]

Creates ischemia in field-less bleeding Systemic toxicity Irreversible hypoxic damage, tissue necrosis and gangreneAdrenaline CI in some sites.[Fingers]

Factors affecting.
Size of nerve fibres Lipophilicity & ph Concentration of the drug Proximity to nerve Location of fibres Inflammation Vasoconstrictors

Systemic actions
CNS Stimulation Depression [Cocaine]
Lignocaine Drowsiness Excitation Convulsion treated by BZDP

Systemic actions
Heart CVS toxicity- Inadvertent I.V. Decreases excitability, conduction rate, and force of contraction-Hypotension Lignocaine and procainamideAntiarrhythmics Blood vessels Symp.blockadeVasodilation Cocaine Symp mimetic[Hypertension]

Systemic actions
Hypersensitivity Due to-LA or vasoconstictors Common with esters. Preservatives

Metabolism
Esters metabolized by plasma esterases Amides by CYP enzyme Amides protein bound-Less toxic Neonates defecient in plasma proteins

Individual compounds
COCAINE
Abuse liability Due to inhibition of catecholamine uptake-DA Used only For topical use in Upper Respiratory Tract Toxicity. Drowsiness, tinnitus, dysgeusia, dizziness, and twitching. -seizures, coma, and respiratory depression and arrest. Clinical Uses: Wide range of clinical uses as a local anesthetic; Almost any application where a LA of intermediate duration is needed.

LIGNOCAINE
Faster, Intense, Longer Eutectic mixture with Prilocaine-Intact skin

Anti-arrhythmic agent

Individual compounds
PRILOCAINE
EMLA (EUTECTIC MIXTURE OF LOCAL ANESTHETICS)
Equal quantities of Lignocaine & Prilocaine. USES-EMLA

Topical-5mm depth [One h. before-One h after] By occlusive dressing

IV catheter insertion Blood sampling, Superficial surgical procedures; Leg ulcers for cleansing or debridement Tattooing Laser hair removal Dental-Scaling Dental-Children

Individual compounds
TETRACAINE
Toxic Topical-Eye, throat, Tracheo-bronchial

ROPIVACAINE
Congener of BUPIVACAINE. Longer acting More motor sparing Less cardio toxic

BENOXINATE
Least irritant Topically Eye

BUPIVACAINE
Long acting More sensory than motor Obstetric and post op.pain reief Cardiotoxic

BENZOCAINE/BUTAMBEN
PABA derivative Antagonizes Sulfa action Lozenges-Stomatitis, sore throat, Anelgesic powder-ulcers Suppository-Ano-rectal lesions

Techniques of LA [Clinical uses]

Conduction block

Topical

Infiltration

Field block

Nerve block

Spinal

Epidural

Bier block

Infiltration

Topical [EMLA]

Spinal Epidural Nerve [Conduction]

Field [Conduction]

Individual compounds
PRILOCAINE
EMLA (EUTECTIC MIXTURE OF LOCAL ANESTHETICS)
Equal quantities of Lignocaine & Prilocaine. USES-EMLA

Topical-5mm depth [One h. before-One h after] By occlusive dressing

IV catheter insertion Blood sampling, Superficial surgical procedures; Leg ulcers for cleansing or debridement Tattooing Laser hair removal Dental-Scaling Dental-Children

Topical
Intact skin is not affected To mucus membranes Adrenaline has no effect

Surface

Topical [EML]

EMLA effective in intact skin

Eye, Nose, Ear, Mouth, pharynx Esophagus, Stomach, Intact skin, Urethra, Anal canal, Rectum

Infiltration

Anesthesia

Directly injecting LA into tissues to paralyse sensory nerve endings & small cutaneous nerves, without taking into consideration the course of nerves. Skin and can also include deeper structures, including intra-abdominal organs

Duration doubled by adrenaline

Infiltration

Technically simple Requires more LA for large areas.

Field [Conduction]

Conduction block
Field block Nerve block

S.C. injection of L.A. around superficial nerves-anesthetize the region distal to the injection.

Hand, scalp, the anterior abdominal wall, and the lower extremity Knowledge of neuroanatomy required
Less quantity of L.A.

Field block

Ilio inguinal nerve

Sup.nerves Fore arm

Nerves of scalp

Conduction block
Field block

Nerve block

Injection of L.A.into or about individual peripheral nerves or nerve plexuses Mixed peripheral nerves - anesthetizes somatic motor nerves,-skeletal muscle relaxation Brachial plexus block-U.Limb & Shoulder Intercostal block-Ant abd.wall C.Plexus block-Neck Sciatic, Ulnar, Median nerve etc.

Biers block-I.V.Regional
Extremity is exsanguinated with an Esmarch bandage [Or raise the limb & Block artery] Proximally located tourniquet is inflated to 100 to 150 mm Hg above SBP Esmarch bandage is removed, LA is injected-I.V. Tourniquet Not less than 30mts-not more than2 hrs U.Limb Lignocaine or Prilocaine with adrenaline

Biers Block

L2

L5

Spinal anesthesia

Spinal anesthesia
Injected into the subarachnoid space between Lumbar 2 -3 or L 3-4 Spinal cord terminates above the second lumbar vertebra In this region there is large volume of CSF within which to inject drug Minimum direct nerve trauma.

Pharmacology of Spinal Anesthesia

Commonly used drugs -Lignocaine, Tetracaine, and Bupivacaine Factors affecting hieght and durationVolume, speed of injection, baricity , position of patient, adrenaline Adrenaline prolongs duration

 Baricity [Density] Decides direction of migration in the dural sac Hyperbaric - settle in the dependent portions of the sac, Hypobaric - Migrate in the opposite direction Isobaric -stay in the vicinity where they were injected

Pharmacology of Spinal Anesthesia-Factors

Pt.position- till Fixed Lidocaine and bupivacaine -isobaric and hyperbaric solutions Diluted with distilled water -hypobaric

 Differential= pre ganglionic symp more sensitive Deleterious and some beneficial Symp-TL out flow- T1 to LI Cephalic spread of anesthetic-Position & Baricity Level of blockade is 2 segments higher than anesthesia Dominant Para symp action and poor symp compensation Not important in children!!

Spinal anesthesia and sympathetic blockade

Spinal anesthesia and sympathetic blockade

Vasodilation

Blood pooling

Venous return becomes gravitydependent CO-Organ perfusion

T1-T4-Card.accelerators

BP=surrogate marker

Treatment Head down,I.V.Fluids, Ephedrine, Phenylephrine

Sympathetic blockade- benefits

Sympathetic fibers -T5 to L1 inhibit peristalsis Blockade produces a small, contracted intestine Together with a flaccid abdominal musculature, produces excellent operating conditions

Complications of spinal anesthesia

Hypotension

Respiratory paralysis Rare Poor perfusion of higher centers Cough and expectorati ondefective

Symp.Blockade

Septic meningitis

Head ache
CSF leak Small bore needles

Intercostal paralysis Cough[-]

Cauda equina syndrome

Damage to nerve roots

Traction of viscera

Nausea& Vomiting

Hypotension & Hypovolemia [i.v. bolus NS-preop.] Uncooperative pts Infants and children-small segments Vertebral anomalies Infection at site of injection

Contra indicationsSpinal anesthesia

Dermatome levels for different procedures

Epidural Anesthesia [LA into epidural space]

Ligamentum flavum posteriorly, Spinal periosteum laterally, Dura anteriorly Site of action-spinal roots

Epidural- categories
Thoracic
Narrow space Small vol of LA Post OP pain reliefAbd/Tho. surgeries

Lumbar
Large volume Lower abd, pelvis, lower limbs

Sacral canal Vaginal delivery Anorectal operations

Caudal

EpiduralTechnically difficult Large volume No differential sympathetic blockade Blood concentrations of LA much higher Area covered depends on volume of LA Complications are same as Spinal Head ache & Neurological complications are less

Epidural
1. Different parts of spinal cord 2. Systemic absorption +++ 3. No diff symp block [Advantage offset by systemic absorption] 4. Small dose

Spinal
1. Lumbar only 2. No systemic absorption 3. Diff block+++ 4. Large dose

Epidural anaelgesia
In an epidural, an indwelling catheter may be placed that avails for additional injections later, while a spinal is a one-shot only. The onset of analgesia is approximately 15 30 minutes in an epidural, while it is approximately 5 minutes in a spinal.

Painless labor, Terminal cancer pain control

Local Anesthetics - Ophthalmological Use

Should be non-irritant Proparacaine and tetracaine Instilled a single drop at a time. If anesthesia is incomplete, successive drops are applied until satisfactory conditions are obtained.

Review-LA Def Classification MOA Techniques Topical, Infiltration, Conduction, I.V. Regional, Spinal and epidural Method Advantages Complications Uses Agents