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LOCAL ANESTHETICS
Objectives:
5. indicate which drug characteristics best correlates with rate of onset of local
anesthesia. Indicate the relationship between local duration of anesthesia and
vasodilation. Explain how local inflammation my adversely influence the
effectiveness of local anesthetics.
7. indicate which system is most sensitive to systemic effect of local anesthetics and
which system is second most sensitive.
8. indicate in what ways cocaine differs from most local anesthetics with regards to
CNS and vascular effects.
10. list two agents that are not classified as local anesthetics but have local anesthetic
properties.
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I. Local Anesthetics
A. Definition
B. Desirable Characteristics
C. Mechanism of action
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Na+
LA receptor
++ ++ -- -- -- --
-- -- ++ ++
++ ++
Resting Open
(Closed**) inactivated
(brief) LA have highest
affinity for the
Very slow inactivated form
repolarization in
presence of LA Refractory period
**Closed state may exist in various forms as it moves from resting to open. LA have a
high affinity for the different closed forms and may prevent them from opening.
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i. frequent firing pain neurons more affected than
slow firing motoneurons
a. pKa
b. lipid solubility
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2. local duration positively correlated with LS and inversely related
to vasodilation
R-CH2-NH+ R-CH2-N + H+
C2H5 C2H5
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E. Chemical Classification
C O R N
R
ESTER
O R
NH C R N
R
AMIDE
LIPOPHILIC HYDROPHILIC
LIDOCAINE
PROCAINE
lidocaine (Xylocaine)
procaine (Novocaine)
mepivacaine (Carbocaine)
tetracaine (Pontocaine)
bupivacaine (Marcaine)
benzocaine
etidocaine (Duranest)
cocaine
ropivacaine (Naropin)
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a. occurs with drugs in the same chemical class
2. Biotransformation/duration of action
G. Pharmacokinetics
1. Absorption
d. effects of vasoconstrictors
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iii. increase local duration of action (e.g., lidocaine’s
duration may increase twofold with EPI)
2. Distribution
3. Metabolism
a. ester type LA
b. amide type LA
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Comparison of LA characteristics
Relative Relative Onset pKa Local Vasodilation Plasma
lipid potency duration protein
solubility binding
procaine 1 1 slow 8.9 short +++ 5%
Plasma protein binding may be used as an indirect measure of tissue binding tendencies
5. cardiovascular system
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ii. block of postganglionic sympathetic fiber function
d. neurotoxicity
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iv. may account for transient neurological symptoms
after spinal anesthesia
3. a toxic action on heart may induce rapid and lethal cardiac failure
B. benzocaine (Americaine)
C. procaine (Novocaine)
1. topically ineffective
2. used for infiltration because of low potency and short duration but
most commonly used for spinal anesthesia
D. tetracaine (Pentocaine)
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a. frequently used for topical ophthalmogical anesthesia
B. mepivicaine (Carbocaine)
C. bupivacaine (Marcaine)
1. no topical effect
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D. ropivacine (Naropin)
1. enantiomer of bupivacaine
2. no topical effectiveness
a. lidocaine, tetracaine
b. EMLA – mixture of lidocaine and prilocaine
B. infiltration anesthesia
D. spinal anesthesia
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1. injection into subarachnoid space below level of L2 vertebra to
produce effect in spinal roots and spinal cord
3. used for surgery to abdomen, pelvis, or leg when can’t use general
anesthesia.
a. lidocaine, tetracaine
4. problems
a. greater predictability
b. faster onset
c. shorter duration
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