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24 Cards in this Set

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Describe the chemistry of local anesthetics
Lipophilic group (Aromatic ring) --Intermediate chain (Ester or amide) -- Ionizable group (Tertiary amine)
The two main subclasses of local anesthetics are:
Amides
Esters
What is the MOA of local anesthetics?
Na channel blockers, reduce sodium influx. This prevents depolarization and blocks conduction of the action potential.
Name two long duration amides
Bupivacaine
Ropivacaine
Medium duration amide
Lidocaine
List 5 drugs that containe esters as intermediate chain in local anesthtics:
Benzocaine
Cocaine
Procaine
Tetracaine
A long duration ester containing local anesthetic:
Tetracaine
A short duration ester containing local anesthetic:
procaine
Medium duration ester containing local anesthetic:
Cocaine
Surface active ester containing local anesthetic:
Benzocaine
Cocaine
True or False:
All local anesthetics are vasodilators
False,
All except cocaine
Why are short acting local anesthetics given with vasoconstrictors?
Reducing blood flow to injection point allows the drug to sit there longer and increases the duration of action.
Which local anesthetics can be used as topical anesthesia?
Benzocaine and cocaine
How are esters metabolized?
Pseudocholinesterase
How are amides metabolized?
Hepatic microsomal enzymes. Therefore liver problems may increase their elimination half-life.
Which nn. fibers are blocked more easily by local anesthetics? Small or large nerve fibers
Small diameter
Which nn. fibers are blocked more easily by local anesthetics? myelinated or unmyelinated nerve fibers
myelinated - electrical signals travel faster in these nerves.
Which nn. fibers are blocked more easily by local anesthetics? peripheral or core nerve fibers
peripheral - Exposed sooner to a higher concentration of the anesthetic.
List the factors that determine the susceptibility of nn fibers to blockade
Size - small/ large diameter
Myelin
Peripheral/core
List the major toxic effects of local anesthetics:
CNS - lightheaded, nystagmus, resp. & cardiovascular collapse.
Cardiovascular - all local anesthetics are vasodilators exc. cocaine.
Allergic Rxns: With ester type allergic reactions.
Prototype drug for Ester subclass
Procaine

Cocaine: Major variant
Prototype drug for amide subclass
Lidocaine
How are convulsions due to local anesthetic toxicity treated?
Diazepam or barbiturates
What are the cardiovascular symptoms seen with cocaine toxicity?
Hypertension, cerebral hemorrhage, cardiac arrhythmias and myocardial infarction.