Local Anesthetics Flashcards
Local anesthetics produce tranisent loss of _____,_____,_____ ?
Sensory, Motor, Autonomic Function
Local anesthetics produce a conduction block by preventing passage of _____ through selective channels in the nerve membrane?
Na+
What is responsible for the speed of a local anesthetics onset?
PKa
The unionized portion of the drug is _____ and is what actually gets into the cell
Lipophilic
Once the lipophilic portion of the drug gets into the cell it redistributes into _____ and _____ based on the Ph inside the cell and the drugs PKa.
Ionized and Nonionized
Most local anesthetics are _______ and range from _____ to ____ PKa?
Weak Bases
8.0-9.0
Most drugs are weak bases but this drug we give in anesthesia is a weak acid?
Sodium Thiopental
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Base
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Acid
Drug PKa is 8.2 and is injected IV in normal Patient with a PH of 7.4. Does the curve shift to the right or left and what portion increaes Ionized or nonionized?
Shifts to the Left
Increasing nonionized portion
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The primary active sight of a local anesthetic is where?
Intracellular
Which part of the local anesthetic binds to the receptor site the anion or cation?
cation
The charged portion
Potency correlates with what in the local anesthetic?
Lipid solubility therefore the nonionized portion
Durration of action depends on what?
The amount of the drug protein bound to the channel not refering to protein binding intravascularly because the drug is in the cell at this point
Which Local anesthetic is only used in its S enantiomer form?
Ropivacaine
which local anesthetic is achiral?
Lidocaine
Local anesthetics are either ______ or _____?
Esters or Amides
Addition of Epi does 3 things what are they?
Prolong the Block
Increase intensity of the Block
Decrease systemic absorption of the LA
Local anesthetics are composed of 3 parts ?
Lipophilic Group, Amide or Ester, Hydrophilic Group
NO Question Just view it
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NO Answer Just view it
Amides are metabolized where?
Liver
Esters are metabolized where?
Plasma Cholinesterase
Ester or Amide
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ESTER!!!!
Ester or Amide
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ESTER
Ester or Amide
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AMIDE
Ester or Amide
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AMIDE
Amides are Metabolized 3 ways?
N-dealkylation, Amide Hydrolysis, Aromatic Hydroxylation
List all Ester Local anesthetics?
Cocaine, Benzocaine, Procaine, Tetracaine, Chloroprocaine
List local anesthetics that are common Amides
Lidocaine, Bupivacaine, Ropivacaine, Mepivacaine, Prilocaine,