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Local Anesthetics
N/A
32
Medical
Professional
02/20/2010

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Term
Amide anesthetics
Definition
Lidocaine
Prilocaine
Mepivacaine
Bupivacaine
Ropivacaine
Term
Amide metabolism
Definition
Amides are metabolized in liver by P450s

Contraindicated in severe hepatic failure pts
Term
Benzocaine
Definition
Most common topical OTC anesthetic

Low solubility
Term
Benzocaine side effects
Definition
Potential methemoglobinemia
Term
Bupivacaine
Definition
Long acting local infiltration anesthetic

Sensory blockade occurs much faster than motor blockade

Typically not used topically

Levo-bupivicaine (S-enantiomer)
Term
Central n. blockade rxs
Definition
Lidocaine
Prilocaine
Bupivacaine (long Sgx, but cardiotoxic)
Ropivacaine (fewer CV effects than Bupivacaine)
Term
Central neural blockade
Definition
Done either via epidural or intrathecal

Can block ANS

Baricity determines direction of rx flow
Term
Cocaine
Definition
Local topical anesthetic used only in ears, nose, throat bc of vasoconstriction dec bleeding

Systemic absorption can occur

Blocks NE uptake
Term
Ester anesthetics
Definition
Procaine
Cocaine
Tetracaine
Benzocaine
Term
Ester metabolism
Definition
Esters form PABA (para amino benzoic acid), which can INHIBIT SULFONAMIDES
and can cx ALLERGIC RXNS

Degraded by plasma esterases
Term
Important Spinal anesthetics
Definition
Lidocaine
Tetracaine
Bupivacaine
Term
Intermediate duration LA
Definition
Lidocaine
Prilocaine
Mepivacaine
Term
Intravenous regional anesthesia
Definition
IV administration into tourniquet-occluded limb

Lidocaine w/o EPI used most frequently

Used for forearm and hand sgx
Term
LA duration
Definition
determined by protein binding and hydrophobicity
Term
LA onset time
Definition
determined by pKa
Term
Lidocaine
Definition
Most popular local anesthetic

Infiltrative and topical

Used topically in combo w prilocaine can achieve anesthesia at 5mm
Term
Lidocaine toxicity
Definition
Doses cxing CNS toxicity cx CV depression
Term
Local anesthetic potency
Definition
determined mainly by lipid solubiity
Term
Local anesthetics mechanism
Definition
Block "fast" voltage-gated Na channels in the inactivated state
Term
Longest duration LA
Definition
Bupivacaine
Ropivacaine
Tetracaine
Etidocaine
Term
Mepivacaine
Definition
Local anesthetic
Term
Mepivacaine contraindications
Definition
More toxic in neonates
Term
Order of functional block
Definition
1. pain, autonomic C-fibers
2. cold
3. warmth
4. touch
5. deep pressure
6. motor

*Recovery in reverse order

Small fibers more susceptible
(autonomic)> pain fibers> sensory> motor
Term
Peripheral n. blockade
Definition
Used to produce greater areas of anesthesia than infiltration

Minor blocks involve single nerve

Major blocks involve multiple nn

Brachial plexus most commonly
Term
Prilocaine
Definition
In combo w lidocaine can achieve anesthesia 5 mm deep topically
Term
Prilocaine side effects
Definition
potential methemoglobinemia
Term
Procaine
Definition
Local infiltration anesthetic

Slow onset, short duration
Term
Ropivacaine
Definition
Local anesthetic

Typically not used topically
Term
Shortest duration LA
Definition
Procaine
Term
Spinal anesthesia
Definition
Sympathetic block

Vasodilation common
Blood pooling
Redcued Cardiac ouput
Age dependent
Term
Tetracaine
Definition
Local anesthetic

Slower metabolism
More systemic toxicity
Term
Toxicity of Local anesthetics
Definition
CNS stimulation => depression
Dec CV activity (conduction, force, excitability)
Dec BP
Dec GI activity
Hypersensitivity rxns (dermatitis, asthma)
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