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Local anaesthetic
agents
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Introduction


-First Local Anesthetic-
Cocaine: isolated from Coca leaves
in 1859 by Niemann
-Introduced into ophthalmology &
dentistry in 1880s
- Widely available in the early 1900s.
- Despite its addictive property, cocaine
was used for 30 years.
-Also found to have strong
vasoconstrictive action
- First analog of cocaine synthesized for
use as a local anesthetic: procaine
(1905)
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Local Anesthetics:
Role:
Decrease intraoperative and postoperative
pain
Decrease amount of general anesthetics used
in the OR
Increase patients cooperation
Diagnostic testing/examination
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The Pharmacology of Local Anaesthetic
Agents (LA)

Local anaesthetic agents can be defined as drugs,
which are used clinically to produce reversible
loss of sensation in a circumscribed area of the
body.

Classification :The molecule of the clinically
useful LA agents consists of
1. A tertiary amine attached to an
2. Aromatic ring by an
3. Intermediate chain.
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Classification of LA Agents
There are 2 classes of local anaesthetic
drugs defined by the nature of the
intermediate chain.
1. The ester LA agents include cocaine,
procaine, and chloroprocaine
2. The amide LA agents include lidocaine,
prilocaine, bupivacaine, etidocaine,
mepivacaine
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There are important practical differences
between these 2 groups of LA agents
Esters are relatively unstable in solution
Amides are relatively stable in solution
Esters are rapidly hydrolysed in the body by plasma
cholinesterase (and other esterases)
Amides are slowly metabolised by hepatic amidases and
Esters: One of the main breakdown products is para-
amino benzoate (PABA) which is associated with allergic
phenomena and hypersensitivity reactions
Amides: hypersensitivity reactions to amide local
anaesthetics are extremely rare
In current clinical practice esters have largely been
superseded by the amides.
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Mode of action
Local anesthesia temporarily blocks the normal
generation and conduction action of the nerve impulses.
After injection, the tertiary amine base is liberated by the
relatively alkaline pH of tissue fluids:
These effects are due to blockade of sodium channels,
thereby impairing sodium ion flux, across the
membrane.
Local anaesthetics are relatively inactive when injected
into tissues with an acid pH (e.g. pyogenic abscess),
which is presumably due to reduced release of free
base.
Induction time is the length of time from the injection
of the anesthetic solution to complete and effective
conduction blockage.

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Preparations of LA
LA agents are usually acid (pH range 4.0-5.5)
and contain

1. reducing agent (e.g. sodium metabisulphite) to
enhance the stability of added vasoconstrictors

2. preservative and a fungicide


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What does 1% Lidocain mean?

The dilute preparations are presented as percentage (%)solutions
of LA.

A solution expressed as 1% contains 1g substance in each
100mls
1 g in 100 ml = 1000mg in 100 ml 10 mg in 1 ml
The number of mg/ml can easily be calculated by
multiplying the percentage strength by
10. Therefore a 0.25% solution of lidocaine contains
2.5mg/ml of solution (10 * 0.25=2.5 mg /ml)
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vasoconstrictors
Most LA produce some degree of vasodilation, and
they may be rapidly absorbed after local injection.
vasoconstrictors decrease the systemic toxicity and
increase the safety margin of local anaesthetics by
reducing their rate of absorption
vasoconstrictors are frequently added to LA to
enhance their potency and prolong their duration of
action
Adrenaline is the most commonly used
vasoconstrictorin concentrations ranging from 1 in
80,000 to 1 in 300,000
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How can I prepare Adrenaline 1:200000?

Adrenaline dilution 1:200000 means
1 g in 200000 ml = 1000 mg in 200000 ml
1 mg in 200 ml = 0.1 mg in 20 ml
1:80000..= 0.1 mg in 8 ml

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Agent: Dose: Onset/Duration:

Lidocaine with epi (1 or 2%) 7mg/kg Fast/medium

Lidocaine without epi 4.5mg/kg Fast/short


Mepivacaine without epi (3%) 5.5mg/kg Fast/short

Bupivacaine with epi (0.5%) 1.3mg/kg Long/long

Articaine with epi (4.0%) 7mg/kg Fast/medium

*ADULT DOSES IN PATIENTS WITHOUT CARDIAC HISTORY

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Dosing considerations:

Patient with cardiac history:
Should limit dose of epinephrine
Most local anesthesia uses 1:100,000 epinephrine
concentration (0.01mg/ml)

Pediatric dosing:
Clarks rule:
Maximum dose=
(weight child in lbs/150) X max adult dose (mg)
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contraindication for Adrenaline containing
local anaesthetic agents:
agents
Absolute contraindication (should never be used) for:
1.infiltration around end-arteries i.e. ring block of
fingers, penis or other areas with a terminal vascular
supply as the intense vasoconstriction may lead to
severe ischaemia and necrosis.
2. Intravenous regional anaesthesia (IVRA)
Relative contraindication:
1.Patient with severe hypertension
2.General anaesthesia with halothane

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1. Topical Anaesthesia
2. Infiltration Anaesthesia
3. Intravenous regional anaesthesia
(IVRA)
4. Peripheral Nerve Blockade
5. Extradural Anaesthesia
6. Spinal Anaesthesia
7. Tumescent Anesthesia
Clinical Uses of Local Anaesthetics
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1: Topical Anaesthesia

LA may be applied to the skin, the eye, the ear, the nose

and the mouth as well as other mucous membranes. most

useful and effective: Lidocaine (i.e.gel 2%) and

prilocaine(i.e.EMLA)

Used prior to local anesthetic injection to
decrease discomfort in non-sedated patients

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2: Infiltration Anaesthesia

provide anaesthesia for minor surgical
procedures. commonly used Amide LA are
(Lidocaine prilocaine,mepivacaine and
Bupivacaine)., The site of action is at
unmyelinated nerve endings and onset is almost
immediate
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3: Intravenous regional anaesthesia (IVRA)
IVRA (BIER s Block) analgesia for minor surgical
procedures. The local anaesthetic agent is injected into a
vein of a limb that has been previously exsanguinated
and occluded by a tourniquet.
The site of action is probably the unmyelinated nerve
fibres, Prilocaine and Lidocaine are commonly used.
Bupivacaine and etidocaine should never be used
for IVRA! They are significantly protein bound and once
the tourniquet is released there is a risk of cardiotoxicity.
Several deaths have been reported during IVRA with
bupivacaine.
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4: Peripheral Nerve Blockade :
Regional anesthetic procedures that inhibit conduction in
fibers of the peripheral nervous system. It can be
devided into:

Minor nerve blocks involve the blocking of single nerve
entities such as the inferior alveolar nerve, mental
nerve, ulnar or radial nerve.

Major nerve blocks involve the blocking of deeper nerves
or trunks with a wide dermatomal distribution (e.g.
brachial plexus blockade).

The commonly used LA agents are: Lidocaine, prilocaine,
mepivacaine, and bupivacaine.


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5: Extradural Anaesthesia:LA agent injected in the

epidural space between the dura mater and the

Lig.Flavum. The epidural space contains adipose tissue,

lymphatics and blood vessels. LA produces analgesia by

blocking conduction at the intradural spinal nerve roots.

usually used 0.5% Bupivacaine (mainly) or lidocaine (2.0%)

6.: Spinal Anaesthesia injction directly into the cerebrospinal
fluid (subarachnoid space) produces spinal anaesthesia.
commonly used : Bupivacaine 0.5% (mainly hyperbaric), lidocaine (5%)
7.: Tumescent Anesthesia A technique most commonly employed
by plastic surgeons during liposuction procedures
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Maxillary anesthesia:
3 major types of injections can be performed in the maxilla for
pain control
Local infiltration
Field block
Nerve block
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Maxillary anesthesia:
Infiltration:
Able to be performed in the maxilla due
to the thin cortical nature of the bone
Involves injecting to tissue immediately
around surgical site
Supraperiosteal injections
Intraseptal injections
Periodontal ligament injections
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Maxillary anesthesia:
Field blocks:
Local anesthetic deposited near a larger
terminal branch of a nerve
Periapical injections
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Maxillary anesthesia:
Nerve blocks:
Local anesthetic deposited near main nerve
trunk and is usually distant from operative
site
Posterior superior alveolar -Infraorbital
Middle superior alveolar -Greater palatine
Anterior superior alveolar -Nasopalatine
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Mandibular anesthesia:
Infiltration techniques do not work in the adult
mandible due to the dense cortical bone

Nerve blocks are utilized to anesthetize the
inferior alveolar, lingual, and buccal nerves

Local anesthesia complications:
Needle breakage
Pain on injection
Burning on injection
Persistent anesthesia/parathesia
Trismus
Hematoma
Infection
Edema
Tissue sloughing
Facial nerve paralysis
Post-anesthetic intraoral lesion
Herpes simplex
Recurrent aphthous stomatitis
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Toxicity from Local Anaesthetic Drugs
when excessive blood levels occur. usually due to:
1. Accidental rapid intravenous injection.
2. Rapid absorption, such as from a very vascular site
ie mucous membranes. Intercostal nerve blocks will
give a higher blood level than subcutaneous
infiltration, whereas plexus blocks are associated
with the slowest rates of absorption and therefore
give the lowest blood levels.
3. Absolute overdose if the dose used is excessive.

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Signs and Symptoms of LA Toxicity
It involves the CNS and CVS. In general (CNS) is more
sensitive to LA than the CVS. Therefore CNS
manifestations tend to occur earlier. Brain excitatory
effects occur before the depressant effects.
CNS signs & symptoms
Early or mild toxicity: light-headedness, dizziness, tinnitus,
circumoral numbness, confusion and drowsiness.
Patients often will not volunteer information about these
symptoms unless asked.
Severe toxicity: tonic-clonic convulsion leading to
progressive loss of consciousness, coma, respiratory
depression, and respiratory arrest.

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CVS signs & symptoms
Early or mild toxicity: if LA with Adrenaline tachycardia
with Hypertension
If no Adrenaline : bradycardia with hypotension
Severe toxicity: Usually about 4 - 7 times the
convulsant dose needs to be injected before CV
collapse occurs.
Collapse is due to the depressant effect of the LA
acting directly on the myocardium (e.g. Bupivacaine)
Severe and intractable arrhythmias can occur with
accidental iv injection.
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Essential Precautions and Treatment
Precautions: Secure intravenous access before
injection of any dose that .
Always have adequate resuscitation equipment and drugs
available before starting to inject.
Treatment: stop the injection and assess the patient.
Call for help while treating the patient
Ensure an adequate airway, give O2 in over facemask .
Ventilate the patient if there is inadequate spontaneous
respiration
Intubation : if the patient is unconscious and unable to
maintain an airway.

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Treatment of circulatory failure
with I.V fluids and vasopressors: Ephedrin : If
not available or not effective in correcting the
hypotension .Adrenaline
Treat arrhythmias. Start chest
compressions if cardiac arrest occurs.
Treat Convulsions with anticonvulsant drugs
(Diazepam 0.2-0.4mg/kg , Thiopentone 1-4 mg/kg)