Non-Opioid Analgesics And Local Anesthetics

Front 1

mechanism by which aspirin and NSAIDs produce their analgesic and antipyretic effects

Back 1

inihibition of synthesis of prostaglandins by stopping COX
PG's sensitize pain receptors and mediate increase in body temperature

Front 2

ketorolac vs. other NSAID;s

Back 2

moderate to severe pain
as effective as morphine
in and around surgery
no fx on respiration
only 5 day continuous use
monitor kidney functoin

Front 3

why do opioids and NSAIDs work better together?

Back 3

synergy
no ceiling fx of opioids

Front 4

use and advantages of IV acetaminophen

Back 4

manage pain in surgery
decrease opioid need
rapid analgesia

Front 5

-caine's
most cardiotoxic?
most widely used?
most likely to cause CNS sedation?
topical only?
vasoconstriction?

Back 5

cardiotoxic- bupivicaine
most widely used-lidocaine
most likely to cause CNS sedation-lidocaine
topical-coaine, benzocaine
VC-cocaine

Front 6

what are "differential nerve sensivities?"

Back 6

two types of linkages: ester and amide
(amides have 2 eyes!)

Front 7

MOA and site of local anesthetics

Back 7

specific: bind to specific receptors at the intracellular end of the voltage-gated sodium channel
-prevent axonal conduction by a functional blockade

greatest affinity for sodium channel in open and inactivated states and slows its reversion to the resting state
-frequency dependent action- because high affinity forms of Na+ channel are more frequently presented in neurons that are firing more frequently

Front 8

what is the clinical significance of distingushing between the two general chemical classes of local anesthetics in respect to elimination processes, duration of action, and allergic phenomenon

Back 8

cross-sensitivity- occurs with drugs in the same chemical class
allergy doesn't occur with amides
esters are rapidly broken down in the plasma
amides are slowly broken down in the liver by microsomal p450 enzymes

Front 9

which drug characteristics best correlate with the rate of onset?

Back 9

related to pKa- lower is faster
needs to be non-ionized to penetrate

Front 10

local duration of anesthesia, lipid solubility, vasodilation, and protein binding

Back 10

local duration
-positively correlated with LS and protein binding but inversely with vasodilation

Front 11

how does local inflammation adversely affect the effectiveness of local anesthetics

Back 11

tends to lower pH
LA are more ionized
don't penetrate very well
decreased ability of the LA to produce effects

Front 12

Explain the rationale for inclusion of vasoconstrictors in local anesthetic preparations and the potential risks associated with this drug combination. 

Back 12

decrease rate of systemic absorption
increase local drug concentration
increase local duration of action

Front 13

don't use vasoconstrictors:

Back 13

toes
fingers
ear lobes
penis

Front 14

Indicate which physiological system is most sensitive to systemic effects of local anesthetics and which system is second most sensitive.  

Back 14

most sensitive: CNS
CV system- hypotension, arrhythmias

Front 15

indicate in what ways cocaine differs from most local anesthetics with regards to CNS and vascular effects. 

Back 15

CNS- euphoria
causes vasoconstriction

Front 16

compare procaine, lidocaine, bupivacaine, and tetracaine regarding onset and duration of action, lipid solubility, and chemical classification. 

Back 16

esters: procaine, tetracaine
amides: lidocaine, bupivicaine

onset
procaine and tetracaine are slow
lidocaine is fast
bupivicaine is moderate

local duratoin
long: tetracaine, bupivicaine
short: procaine
lidocaine: moderate

relative lipid solubility
1-procaine
4-lidocaine
80-tetracain
30-bupivicaine

Front 17

list two agents that are not classified as local anesthetics but have local anesthetic properties. 

Back 17

propranolol
diphenhydramine
chlorpromazine
corticosteroids

Front 18

indicate which local anesthetic is almost 100% uncharged at physiological pH and used in many OTC preparations as a surface anesthetic. 

Back 18

benzocaine

Front 19

indicate two advantages that prilocaine has over lidocaine.

Back 19

less VD
least toxic amide

Front 20

what is EMLA and what is it used for?

Back 20

eutectic mixture of local anesthetics
lidocaine and prilocaine

make patch for kid to have surgery-skin numbing
premature ejaculation

Front 21

Indicate the chemical relationship between bupivacaine and ropivacaine and indicate the alleged advantage of ropivacaine. 

Back 21

amide
ropivacaine has significantly less CV toxicity

Front 22

Indicate what methemoglobinemia is and its relationship to local anesthetic agents, which LA are most likely to produce this condition, and what agent is used to treat the condition. 

Back 22

rare but life-threatening oxidation of hemoglobin
treat with oxygen and methylene blue

LA: prilocaine, benzocaine, lidocaine

Front 23

Indicate the earliest signss of lidocaine’s CNS toxicity.

Back 23

Sedative 

Front 24

Oraverse is a new local anesthesia reversal agent. How does it work?

Back 24

alpha antagonism of epi vasoconstriction to increase vascular dilation
speeds return to normal sensation and function

Front 25

fibers affected by LA

Back 25

delta
B
C

Front 26

how do LA cause hypotension?

Back 26

arteriolar VD as a result of direct effects and block of sympathetic function as well as CNS depression

Front 27

most toxic and most potent LA

Back 27

tetracaine

Front 28

more toxic to neonates

Back 28

mepivaciaine

Front 29

can provide sensory analgesia with minimal motor block (labor)

Back 29

bupivicaine