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Ophtho/Derm/Rheum-Pharm
Local Anesthetics
19
Pharmacology
Graduate
12/01/2010

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Cards

Term
What is the molecular mechanism of action of Local anesthetics
Definition

Block Na Conduction into cell

Do not block K conduction

Term
What nerves are typically affected first by local anesthetics
Definition
B and C fibers (small unmyelinated: Autonomic/Sensory)
Term
What factors determine Onset Time, Potency, and Duration of Action
Definition

Onset: Lower Pka or higher blood pH is faster

Potency: More lipid soluble is stronger

Duration: Higher affinity blocks wash out(longer)

Term
How are the local anesthetics metabolized
Definition

Esters: Plasma Pseudocholinesterase produced by liver

Amides: Liver p450's

Term
What is the prodrome to local anesthesia toxicity?
Definition

Lightheaded

Disturbances of Visual/Auditory

Dizziness

Disorientation

Drowsiness

Term
What are the adverse effects of Local anesthetics and which anesthetics are particularly toxic?
Definition

CNS: Excitation followed by depression

Twitching, Convulsions-> CV/Respiratory depression, Coma

Cardiac: (-)Inotrope, Dysrythmias

Bipivacaine is most Cardiotoxic

Vessels: Vasoconstriction(Low dose), Vasodialation(High dose)

Methemoglobinemia: Benzocaine, Prilocaine

Muscle Necrosis

Allergies: Esters

 

Term
What is used to reverse cardiotoxicity of bipivacaine and how do you reverse methimoglobulinemia
Definition

Cardio: Intralipid infusion

Methimo: Methylene Blue reduces to ferrous state

Term
What are drawbacks and advantages of Cocaine use as a local anesthetic
Definition

Dis: Local Nerve Toxicity

Adv:Vasoconstriction by blocking catecholamine reuptake

Term
What are the kinetics of tetracaine and how is it used
Definition

Slow onset, Long Duration

Topical Anesthetic

Term
Which ester anesthetic has the least toxicity, what toxicity is particular to this drug?
Definition

2-chloroprocaine

Never give IV->Thrombophlebitis

Term
What are some drawbacks to benzocaine use and when is it typically used
Definition

Requires high concentration

Causes Methimoglobulinemia

Used in Mucous membrane procedures(Trachea)

Term
what are the advantages/disadvantages of Dibucaine and when is it used
Definition

Adv: High Potency

Dis: High Toxicity and blocks Plasma Cholinesterase

Used Topically usually for hemorroids

Term
When is Mepivacaine used and what are the drawbacks to its use
Definition

Epidural, Spinal, and Peripheral Nerve block

Potential for accumulation

Term
What is Bupivacaine used for and what are the drawbacks
Definition

Spinal anesthesis

Lower doses used in Obstetrics to prevent motor block

Hyperbaric solutions prevent Cardiac block

Dis:Cardiac toxicity

Term
What are the advantages and disadvantages of Ropivacaine
Definition

Adv: Less Cardiotoxic bc pure S isomer, better frequency dependent Block

Dis: Less potent, shorter duration

 

Term
What is typically the only anesthetic that epinephrine is used with
Definition
Lidocaine
Term
What is the most rapidly metabolized Amide and what are its adverse effects
Definition

Prilocaine

Methimoglobulinemia

Term
What are the local anesthetics used in Topical, ENT, Mucosal, Spinal(Labor) procedures
Definition

Topical: Tetracaine, Dibucaine(Cream-Hemorrhoids)

ENT: Cocaine

Mucosal: Benzocaine

Spinal: Bipivucaine

Term
Why do esters cause allergies
Definition
PABA mediated
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