non-opioids

Question 1

what dos NSAID stand for?

Answer 1

non-steroidal anti-inflammatory drugs

Question 2

which alarmin can produce degranulation of mast cells?

Answer 2

IL-33

Question 3

histamine is an inflammatory mediator released by ________.

Answer 3

mast cells

Question 4

histamine receptor activity on vascular endothelium increases intracellular Ca2+. what are the 2 affects of this?

Answer 4

1. NO produced in endothelium relaxes smooth musc (vasodilation)
2. MLCK mediated contraction of capillary endothelium makes capillary leaky

Question 5

anti-inflammatory properties and pain relief comes from attenuating the production of ________.

Answer 5

prostaglandins

Question 6

prostaglandins increase ________ and _______.

Answer 6

pain sensitization, inflammation

Question 7

prostaglandins are all derived from __________.

Answer 7

arachidonic acid

Question 8

which two enzymes send arachidonic acid down a path to become prostaglandins?

Answer 8

COX1 and COX2 (mainly responsible for inflammation)

Question 9

how many G protein coupled receptors does PGE2 interact with?

Answer 9

4

Question 10

PGE2 activated G-alpha-stimulatory which increases ______ activity, which leads to phosphorylation of the _______ type nociceptor which increases pain sensitivity.

Answer 10

PKA, TRP

Question 11

prostaglandins can also sensitize pain response via _____________.

Answer 11

central sensitization

Question 12

how to all NSAIDs work?

Answer 12

inhibition of COX enzymes

Question 13

acetylsalicylic acid (aspirin) is a ________ inhibitor, about 100x better inhibitor of COX__, which is the ________ selectivity of the commonly used NSAIDs

Answer 13

irreversible, 1, worst

Question 14

what does COX2 produce after inhibition?

Answer 14

hydroxyeicosatetraenoic acid

Question 15

ibuprofen, naproxen, and acetaminophen are all _______ inhibitors of COX1 and COX2.

Answer 15

reversible

Question 16

rank NSAIDs according to COX2 selectivity

Answer 16

acetylsalisylic acid, ibuprofen, acetaminophen, naproxen (most sensitive)

Question 17

aspirin targets _______, _____, ______ and _______.

Answer 17

pain, fever, thrombosis, and inflammation

Question 18

what do ibuprofen and naproxen target?

Answer 18

pain, fever, inflammation

Question 19

what does acetominophen target?

Answer 19

pain and fever

Question 20

regarding aspirin, cox enzymes inhibit _________, which then inhibits _________. since aspirin is an irreversible inhibitor, only a _____ dose is needed.

Answer 20

thromboxane A2, platelet aggregation, low

Question 21

3 possibilities why acetaminophen is not anti-inflammatory

Answer 21

1. unique COX enzyme in CNS is its target
2. MOA on COX enzymes is different and responsible for the effect
3. providing pain relief through a different mechanism (cannabinoid receptor)

Question 22

the most effective analgesia is a combo of what?

Answer 22

optimum dose of NSAID + additional opioid