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