Local Anesthesia

‫يوسف العلوي‬
Overview

• Local anesthetics produce a transient and reversible

loss of sensation (analgesia) in a circumscribed
region of the body without loss of consciousness.

• Normally, the process is completely reversible.

 INTRODUCTION AND HISTORY
Cocaine
• is a naturally
• occurring compound indigenous to the
Andes Mountains, West Indies, and Java.
• It was the first anesthetic to be discovered
and is the only naturally occurring local
anesthetic
• Coca plant as an ophthalmic anesthetic
 INTRODUCTION AND HISTORY
 Procaine, the first derivative of cocaine,
was developed in 1898.

 Nils Lofgren (1913–1967) was a Swedish

chemist developed lidocaine, the most
widely used cocaine derivative, during
World War II.
 What is local anesthetics?
 block transmission of impulses along
nerves

 short to medium duration of action (1-6

hrs)

 useful for pain control

 overdoses may cause convulsions

Local Anesthetics

• Topical Anesthesia provides a temporary

numbing effect on nerve endings that are
located on the surface of the oral mucosa.
• Supplied as:
– Ointments
– Liquids
– Sprays
• These anesthetics are selected for use on the basis
of:
1. the duration of drug action
• Short: 20 min
• Intermediate: 1—1.5 hrs
• Long: 2—4 hrs
2. effectiveness at the administration site
3. potential for toxicity
 What is local anesthetics?

Applied in the vicinity of peripheral nerve ending

or major nerve trunks

inhibits action potential generation and

propagation

Prevent conduction of electrical impulses from

the periphery to the CNS
 ‫أنشئت الهيئة بموجب المرسوم الملكي رقم م‪ 7‬وتاريخ ‪1/2/1391‬هـ الصادر بنظام تأديب الموظفين‬
‫وهي هيئة مستقلة ترتبط مباشرة برئيس مجلس الوزراء وتختص بالرقابة على أداء الموظفين والتحقيق مع‬
‫من ينسب إليه تقصير منهم وفقا ً لما نص عليه نظام تأديب الموظفين والالئحة الداخلية للهيئة واألنظمة‬
‫األخرى ذات العالقة‬
‫هيئة الرقابة والتحقيق بالمملكة العربية السعودية وهي بمثابة النيابة اإلدارية في بعض الدول العربية كما أن لها‬
‫‪.‬اختصاص جنائي وذلك بالتحقيق في بعض القضايا الجنائية واالدعاء فيها أمام المحاكم المختصة‬
 Two basic classes of local anesthetics

 The amino amides and the amino esters.

 Amino amides have an amide link between

the intermediate chain and the aromatic end

 amino esters have an ester link between the

intermediate chain and the aromatic end.
1. Lipophilic group- an aromatic group, usually an unsaturated benzene ring.
2. Intermediate bond- a hydrocarbon connecting chain, either an ester (-CO-) or amide (-
HNC-) linkage. The intermediate bond determines the classification of local anesthetic.
3. Hydrophilic group- a tertiary amine and proton acceptor.
The classification of local anesthetics

Ester
• Cocaine
• Procaine
• Tetracaine

Amides
• Lidocaine
• Bupivicaine
Cocain Procain Lidocain

Articain Bupivacain Mepivacain

• Amino esters and amino amides differ in several
respects.

• Amino esters are metabolized in the plasma via

pseudocholinesterases,

• Amino amides are metabolized in the liver.

• Amino esters are unstable in solution, but amino

amides are very stable in solution.

• Amino esters are much more likely than amino

amides to cause true allergic reactions
 Mechanism of Action
• Local anesthetics work in general by binding to
sodium channel receptors inside the cell and thereby
inhibiting action potentials in a given axon. They
work the best when the axon is firing.
• The Cell membrane consists of ion pumps, most
notably the Na/K pump that create a negative 70mV
resting potential by pumping 2 K+ intracellular for
every 3 Na+ it pumps extracellular.
 Mechanisms of action

• Fig.
 block nerve fiber conduction by acting on
nerve membranes

 inhibit sodium ion activity

 blocks depolarization--> blocks nerve

conduction
Susceptibility to block of types of nerve fibers.
Function Diamet Myelinatio Conduction Sensitivity
Fiber Type er (mm) n Velocity to Block
(m/s)
Type A
Alpha Proprioception, 12-20 Heavy 70-120 +
motor
Beta Touch, pressure 5-12 Heavy 30-70 ++
Gamma Muscle spindles 3-6 Heavy 15-30 ++
Delta Pain, 2-5 Heavy 12-30 +++
temperature
Type B Preganglionic <3 Light 3-15 ++++
autonomic
Type C
Dorsal root pain 0.4-1.2 None 0.5-2.3 ++++
Sympathetic postganglionic 0.3-1.3 None 0.7-2.3 ++++
 Classification of local anesthetics
• Duration of action:
– short acting (< 60 min)
• procaine
– medium acting (60-120 min):
• lidocaine, mepivacaine, prilocaine, trimecaine, articaine
– long acting(> 120 min):
• bupivacaine, tetracaine, etidocaine, ropivacaine
• Chemical structure
– esters:
• procaine, tetracain, cocaine
– amides:
• lidocain, trimecain, mepivacain, bupivacain, ropivacain, articain,
prilocain, etidocain
 Clinical Use
– minor surgical procedures – topical, infiltration
• most commonly
– nerve blockade
– spinal anesthesia
– autonomic blockade in ischemic conditions
– Slow epidural infusion
• at low concentrations has been used successfully for postoperative
analgesia
• in the same way as epidural opioid infusion (bupivacain-sufentanyle)
• Repeated epidural injection in anesthetic doses may lead to
tachyphylaxis.
• Interactions
– High concentrations of extracellular K+ may enhance local
anesthetic activity,
– B-blockers potentiate LA action
– elevated extracellular Ca2+ may antagonize it.
– Ca2+ channel blockers potentiate LA
 Adverse effects:
– overdose, accidental iv administration – always aspirate
• CNS effects - seizures
– initially
• manifest as sedation, lightheadedness, slurred speech, sensory
disturbances, restlessness, nystagmus;
– higher blood levels
• may result in tremor, respiratory depression and tonic-clonic
convulsions. Severe convulsions may be followed by coma with
respiratory and cardiovascular depression.
– Diazepam i.v. (or thipental), hyperventilation with oxygen
• Cardiovascular effects – bradycardia/hypotension
– Vasodilators
• With the exception of cocaine - !!! Adrenalin
– Patients with preexisting cardiovascular disease may develop
heart block
• and other disturbances of cardiac electrical function at high plasma
levels of local anesthetics.
• Bupivacaine may produce severe cardiovascular toxicity, including
arrhythmias and hypotension, if given intravenously.
 Other toxic effects
• Prilocaine
– Methemoglobinemia - by metabolite
• Allergic responses
– to local anesthetics are rare (<1%)
– can usually be avoided by using an agent from the amide subclass.
• The ester-type local anesthetics
– are metabolized to products that can cause antibody formation in some patients.

• Local neurotoxic action

– In high concentrations of LA
– histological damage and permanent impairment of function
Vasoconstrictor
• Criteria for use:
– Prolongs the duration of an anesthetic agent by
decreasing the blood flow in the immediate area
of the injection.
– Decreases bleeding in the area during surgical
procedures.
• Types:
– Epinephrine
– Levonordefrin
– Norepinephrine
Vasoconstrictor- cont’d
• Ratio of vasoconstrictor to anesthetic
solution:
• 1:50,000
• 1:100,000
• 1:200,000
• 1:20,000
Vasoconstrictor- cont’d
• Contraindications for the use of
vasoconstrictors
– Unstable angina.
– Recent myocardial infarction.
– Recent coronary artery bypass surgery.
– Untreated or uncontrolled severe hypertension.
– Untreated or uncontrolled congestive heart
failure.
• Epinephrine:
– should not be coadministered for nerve block in areas such
as fingers and toes that are supplied with end-arteries
because it may cause ischemia or necrosis
– it should be used cautiously in patients in labor and in
patients with thyrotoxicosis or cardiovascular disease.
 Specific drugs and their therapeutic uses
Amides the duration of drug action
1. Short: 20 min
2. Intermediate: 1—1.5 hr
3. Long: 2—4 hr
Lidocaine, articaine
• Lidocaine is the prototype amide
• it has an intermediate duration of action.
• Lidocaine is generally preferred for:
– infiltration blocks
– epidural anesthesia.

• Articaine has a rapid onset of action with the same pKa and
toxicity as lidocaine.
Mepivacaine
• intermediate duration of action that is longer than
that of lidocaine.
• Actions:
– similar to those of lidocaine
– it causes less drowsiness and sedation.
• isotonic solutions (clear, colorless)
• Mepivacaine is not used topically.
Prilocaine
 intermediate duration of action that is longer than
that of lidocaine.
 Actions:
– similar to those of lidocaine
– less toxic than lidocaine .
 Prilocaine should not be used in patients with cardiac
or respiratory disease or in those with idiopathic or
congenital methemoglobinemia
Hgb

methylene blue
Hgb
Prilocaine O-toluidine methemoglobin
Bupivacaine, Ropivacaine, Etidocaine
• These drugs have a long duration of action.
• Bupivacaine has greater cardiotoxicity than other
amide local anesthetics.
• Ropivacaine may have less cardiotoxicity than
bupivacaine.
• Etidocaine has a rapid onset of action.
 Cocaine
• ester
• block norepinephrine reuptake at sympathetic
neuroeffector junctions
– vasoconstricting actions
• When used as a drug of abuse
– cocaine's cardiovascular toxicity includes severe
hypertension with cerebral hemorrhage, cardiac
arrhythmias, and myocardial infarction.
Tetracaine
• Tetracaine is long acting but has a slow onset of action (>10
min).
• Tetracaine is often preferred for:
– spinal anesthesia
– ophthalmologic use.
Dibucaine

• Dibucaine is long acting but has a slow onset of

action (15 min).
• Dibucaine is used only for:
– topical
– spinal anesthesia.
Benzocaine and butamben picrate.
– These anesthetics are used topically only to treat sunburn, minor
burns, and pruritus.

Proparacaine
• used topically for ophthalmology due to:
– rapid onset
– short duration.
Other local anesthetics

a) Dyclonine
• has a rapid onset of action
• used topically.

b) Pramoxine
• used topically
• too irritating for the eye or nose.
The EMLA cream needs to be applied at least 1
hour before a procedure with a needle (taking
blood, inserting a cannula) is due to be done,
or 2 hours before a surgical procedure such as
a skin graft
• 1mg=1000 μ g
• 80ml 1:80,000 = 12.5μg/ml
• 200ml 1:200,000 = 5μg/ml
 ‫غض@ارة‪ ....‬هو إناء غزير‬
‫•‬ ‫َغ@ضارة‪ ( :‬اسم )‬
‫ضائِ ُر‬ ‫الجمع@ ‪َ :‬غ@ َ‬
‫الطين اللَّ ِزج األَخض ُر@ الحُرُّ‬ ‫ُ‬ ‫ضا َرةُ ‪:‬‬ ‫ال َغ َ‬
‫ْش ‪ :‬النِّ ْع َمةُ ‪ِ ،‬طيبُ ال َعي ِ‬
‫ْش‬ ‫ضا َرةُ ال َعي ِ‬ ‫َغ َ‬
‫ت ‪ُ :‬خصُوبَتُهَا@ ‪ ،‬نُعُو َمتُهَا‬ ‫ضا َرةُ النَّبَا ِ‬ ‫َغ َ‬
‫ض َر‬‫مصدر غ@ ُ‬
‫•‬ ‫غ@ضارة‪ ( :‬اسم )‬
‫ض َر‬ ‫غضار@ة ‪ :‬مصدر َغ@ ُ‬
‫•‬ ‫ض َر‪ ( :‬فعل )‬ ‫َغ@ ُ‬
‫ضر و َغ@ ِ‬
‫ضير@‬ ‫ض َر يغضُر ‪ ،‬غضا@رةً ‪ ،‬فهو َغا ِ‬ ‫غ@ ُ‬
‫ب َع ْي ٍ‬
‫ش‬ ‫ض َر ال َّر ُج ُل ‪َ :‬كا@ َن ِفي َس َع ٍة َو ِطي ِ‬ ‫َغ@ ُ‬
‫ات ‪ :‬نَ ُع َم ‪ ،‬أَيْ َك َ‬
‫ان نَا ِع@ما ً‬ ‫ض َر النَّبَ ُ‬ ‫َغ@ ُ‬
‫•‬ ‫َغضار‪ ( :‬اسم )‬
‫ضا ُر ‪ :‬تُر@ابٌ طين ٌّى دقيق الحبيبات ‪ ،‬كثي ُر@االندماج والصالبة ‪ ،‬تتخذ منه األَواني الصِّ ينية‬ ‫ال َغ َ‬
‫ج أَ ْخ َ‬
‫ض َر الَ َر ْم َل ِفي ِه‬ ‫ضا ُر ‪ :‬إِنَا ٌء ُمتَّ َخ ٌذ ِم ْن@ ِطي ٍن لَ ِز ٍ‬ ‫ال َغ َ‬