Local Anesthesia Toxicity
Local
Anesthesia
Toxicity
Dr. Firas Kassab
1Page Dr. Firas Kassab
Local Anesthesia Toxicity
*They produce transient loss of sensory, motor and autonomic functions in a
certain portion of the body.
* They act on specific receptors in sodium channels preventing their
activation, so slow the rate of action potential or membrane depolarization.
* Uses: Analgesia (e.g. postoperative) or a safer alternative to general
anesthesia.
*Precautions during Injection of local anesthetic (LA):
Must be pain free
Aspirate before injection
There should be no resistance to injection
Structure of local anesthetics:
Lipophilic group (benzene ring) ---Intermediate chain --- Hydrophilic group
(tertiary amine)
(Ester link) (Amide link)
The nature of the intermediate chain is the basis of classification of local
anesthetics as esters or amide LA.
. Amides LA: Bupivacaine (Marcaine), Lidocaine (Xylocaine or Lignocaine),
Prilocaine
(Citanest), Dubucaine (Nupercaine), Etidocaine (Duranest), Ropivacaine,
Mepivacaine (Carbocaine).
They are metabolized by microsomal enzymes in the liver.
. Esters LA: Procaine, Chloroprocaine (Nesacaine), Cocaine, Tetracaine
(Pontocaine).
They are metabolized by pseudocholinesterase (plasma cholinesterase)
2Page Dr. Firas Kassab
Local Anesthesia Toxicity
Characteristics of common local anesthetic drugs
Drug pKa Relative Relative Protein Onset Duration Maximum Maximum
lipid potency binding dose with
solubility (%) Dose VC
Procaine 8.9 1 1 6 Slow Short 8mg/kg
Amethocaine 8.5 200 8 75 Slow Long
Lidocaine(Lignocaine) 7.7 150 2 65 Fast Medium 4mg/kg 6mg/kg
Prilocaine 7.7 50 2 55 Fast Medium 6mg/kg 8mg/kg
Etidocaine 7.7 5000 6 96 Fast Long 4mg/kg
Mepivacaine 7.6 50 2 78 Fast Medium 4mg/kg 6mg/kg
Ropivacaine 8.1 400 6 94 Medium Long 3mg/kg
Bupivacaine 8.1 1000 8 95 Medium Long 2mg/kg 2mg/kg
Levobupivacaine 8.1 1000 8 95 Medium Long 2mg/kg
*Factors affect the reaction of LA:
Potency is related to lipid solubility
Duration of action is related to protein binding (for postoperative analgesia
use Bupivacaine)
Speed of onset /latency depends on nonionized lipid soluble, ionized water
soluble forms and pKa of LA (pKa associated with slow onset), so for rapid
onset block use Lidocaine.
- Short and long acting LA can be mixed to obtain rapid onset with longer
duration.
The most common drugs used in dental surgery:
Bupivicaine (Marcaine
-Produce very long acting anesthetic effect to delay the post operative pain
from the surgery for as long as possible
3Page Dr. Firas Kassab
Local Anesthesia Toxicity
- Used in 0.5% solution with vasoconstrictor
-Onset time is longer than other drugs b/c most of the radicals (about 80%)
bind to sodium channel proteins effectively
-Most toxic local anesthetic drug
Prilocaine (Citanest)
--Identical pKa and same conc. with lidocaine
--Almost same duration as lidocaine
--Less toxic in higher doses than lidocaine b/c small vasodilatory activity
Articaine (Septocaine )
--newest local anesthetic drug approved by FDA in 2000
--Same pKa and toxicity as lidocaine, but its half-life is less than about of
lidocaine
--Used with vasoconstrictor.
--Enters blood barrier smoothly
--The drug is widely used in most nations today
Lidocaine:
In 1940, the first modern local anesthetic agent was lidocaine, trade name
Xylocaine
It developed as a derivative of xylidine
Lidocaine relieves pain during the dental surgeries
Belongs to the amide class, cause little allergenic reaction; its hypoallergenic
Sets on quickly and produces a desired anesthesia effect for several hours
Its accepted broadly as the local anesthetic in United States today
Unwanted effects of the local anaesthetic:
4Page Dr. Firas Kassab
Local Anesthesia Toxicity
Failure, allergy, systemic effects, toxicity, drug interactions
Causes of toxicity
a. Intravascular injection
b. Too large a dose
c. Commulation
d. Inability to metabolize++
Local anesthetic toxicity:
Causes: overdose, intravascular injection or cumulative
Symptoms and signs:
Mild: tingling around the mouth, metallic taste, tinnitus, visual disturbance
and slurred speech.
Moderate: disturbed level of consciousness, convulsions and coma
Sever: Respiratory arrest, cardiac arrhythmia and cardiovascular collapse
N.B. Cardiovascular collapse is preceded by convulsions and hypoxia
Treatment:
1. Stop injection
2. ABC
3. Prevent convulsions and hypoxia by Midazolam and oxygen.
4. If there is convulsions intubate the patient and ventilate with 100%
oxygen
5. If there is CV collapse start CPR
5Page Dr. Firas Kassab
