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40 Cards in this Set

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This NSAID can be used for severe pain.

-Reported to be as effective as morphine for moderate pain

**EXAM**
Ketoralac
Why should you only use Ketoralac for 5 days?

***
NSAID

-decreases kidney function
IV acetaminophen has become available in the last year, explain its general use and some of the advantages.

**
-Usually used to decrease pain after surgery

-Decreases opioid use

-Rapid analgesia is achieved

-LIVER TOXICITY an issue
MOA of NSAIDs?

****
e inhibition of synthesis of prostaglandins (PG’s) by inhibiting
cyclooxygenase.

Decreasing PGs knocks out pain and fever!
Your patient is allergic to ester local anesthetics. Which of the following could you give her?

procaine
tetracaine
mepivacaine
benzocaine
cocaine

***EXAM***
mepivacaine

**AMIDES have 2 EYES**
Ester vs. Amide LAs:

lidocaine
mepivacaine
bupivacaine
etidocaine
ropivacaine
Amide LAs

**AMIDES have 2 EYES**
Ester vs. Amide LAs:

procaine
tetracaine
benzocaine
cocaine
Ester LAs
Which one of the following is likely to be cardiotoxic?

• cocaine
• benzocaine
• procaine
• tetracaine
• lidocaine
• mepivacaine
• bupivacaine
• prilocaine
• ropivicaine
Bupivacaine
Which one of the following is most widly used clinically

• cocaine
• benzocaine
• procaine
• tetracaine
• lidocaine
• mepivacaine
• bupivacaine
• prilocaine
• ropivicaine
Lidocaine
Which one of the following is more likely to induce CNS sedation?

• cocaine
• benzocaine
• procaine
• tetracaine
• lidocaine
• mepivacaine
• bupivacaine
• prilocaine
• ropivicaine
Lidocaine
Which one of the following drugs is only used topically?

• cocaine
• benzocaine
• procaine
• tetracaine
• lidocaine
• mepivacaine
• bupivacaine
• prilocaine
• ropivicaine
Cocaine
(corneal or nasopharyngeal)
Which is the most likely to produce vasocontriction effects?

• cocaine
• benzocaine
• procaine
• tetracaine
• lidocaine
• mepivacaine
• bupivacaine
• prilocaine
• ropivicaine
Cocaine

(Don't give epi with coacaine!!)
Which types of neurons are most sensitive to local anesthetics?

**EXAM**
Type A-delta

Type B

Type C (dorsal root and Sympathetic)
3. describe the site and proposed mechanism(s) of action of local anesthetics.
bind to INTRACELLULAR voltage gated sodium channel prevent axonal conduction by a functional blockade

**Greatest affinity for OPEN and INACTIVATED Na channels**

Slows return to RESTING STATE
Ester vs. Amide LAs

-rapidly metabolized in the plasma by cholinesterase
Esters
Ester vs. Amide LAs:

-slowly destroyed by liver microsomal p450 enzymes
Amide
The __ form of LAs crosses the membrane to get to intracellular receptors

**EXAM**
Unionized (Cationic/Uncharged)
The __ form of LAs binds to intracellular receptors to inactivate Na+ channels

**EXAM**
Ionized (Charged)
How does local inflammation affect LAs?
Inflammation makes the area acidic!!

-LAs become ionized BEFORE crossing the membrane

-They can get carried off and act on other areas of the body!!
What is the rate limiting factor for LA onset?
Time to cross membranes into the myelin sheath!!
Do LAs with higher PKAs or lower PKAs tend to have a faster onset?
LAs with PKAs nearer to 7.4 (lower) tend to have the fastest onset!
LAs are ______

A) Strong Bases
B) Weak Bases
C) Strong Acids
D) Weak Acids
Weak Bases
LAs with higher or lower lipid solubility have faster onset times?
higher solubility = faster onset
How does vasodilation affect LA onset?
Vasodilation carries LAs away from local area!!

**Use Epi or Alpha-2 agonists**
6. explain the rationale for inclusion of vasoconstrictors in local anesthetic

***
Vasoconstrictors (Epi, Alpha-2 Agonists):

- decrease systemic absorption and toxicity

-increase local drug concentration

-increase local duration of action
Contraindications of vasocontrictor use with LA?
DON'T USE in toes, fingers, ears or penis

-tissue necrosis
-systemic toxicity
which physiological system is most sensitive to systemic effects of local anesthetics and which system is second most sensitive?
1st = CNS

2nd = Cardiovascular
8. indicate in what ways cocaine differs from most local anesthetics with regards to CNS and vascular effects.
CNS = euphoria

Vascular = vasocontriction**
10. list two agents that are not classified as local anesthetics but have local anesthetic properties.
propranolol

diphenhydramine
11. indicate which local anesthetic is almost 100% uncharged at physiological pH and used in many OTC preparations as a surface anesthetic.
Benzocaine
12. Lidocaine and prilocaine are quite similar in many respects, indicate two advantages that prilocaine has over lidocaine.
**Prilocaine**

-causes significantly less vasodilation than lidocaine

-less toxic than lidocaine (rapidly metabolized)
13. Indicate what EMLA is, local anesthetics used in this product, and some of the general uses.
EMLA = eutectic mixture of local anesthetics

lidocaine + prilocaine

Used for dermal anesthesia -->catheter insertion
Ropivacaine and Bupivacaine are very similar structurally. Which has the least cardiovascular toxicity?
Ropivacaine

(No topical effectiveness only is "S" stereoisomer)
-Some LAs have significant oxidizing effects

-may cause a significant conversion of hemoglobin to methemoglobin and compromize
ability to carry oxygen

What is this? Which LAs are most likely to cause it?
Methemoglobinemia

-Prilocaine**, benzocaine, lidocaine
What is the treatment for Methemoglobinemia?

***
Oxygen and ethylene blue
16. Indicate the earliest signs of lidocaine’s CNS toxicity.
visual disturbances
17. Oraverse is a new local anesthesia reversal agent. How does it work?
Alpha antagonism of epi vasoconstriction to increase vascular dilation

(block's epi's effects!!!)
What is the most toxic and potent ester LA?

-10x more toxic than procaine

**EXAM** r
tetracaine
This LA is a popular choice during labor because it causes sensory analgesia with minimal motor block

**EXAM** r
Bupivacaine
This LA:

Effective by all routes except topical

Similar onset and duration as lidocaine

**More toxic to neonates** so not used in obstetrical anesthesia

**EXAM** r
Mepivacaine