Anti-inflammatories (Non-opioid pain relievers)

Question 1

NSAID stands for:

Answer 1

Non-steroidal Anti-inflammatory drugs

Question 2

What is the purpose of inflammation?

Answer 2

It identifies the injury, helps to remove noxious materials, wards off infection and repairs damaged tissue to restore function.

Question 3

T/F inflammation adds to the pain felt at the injury site?

Answer 3

True

Question 4

Injured cells release chemicals called alarmins (I assume these are just cytokines)

Answer 4

Okay, got it. It raises the alarm

Question 5

What can alarmin IL-33 do?

Answer 5

It produces degranulation of resident mast cells

Question 6

What is the most important thing that mast cells release?

Answer 6

Histamine- an inflammatory mediator

Question 7

What effect does histamine have?

Answer 7

It acts through a G couple protein receptor to produce local vasodilation and makes the capillaries leaky so that more immune cells can get out of the blood stream and to the injury site (this is what happens in a runny nose!) This results in edema- aka swelling

Question 8

The histamine receptor activity allows for the freeing of phospholipase C from the membrane which gets cleaved into IP3 and DAG. IP3 increases the concentration of intracellular calcium.

Answer 8

Remember that?

Question 9

When intracellular calcium is increased, what else is made? and what does it do?

Answer 9

NO
It is produced in the endothelial cells and travels to the smooth muscles to make them relax, thereby causing vasodilation.

Question 10

What does MLCK mediated contraction do to the capillary endothelium?

Answer 10

It makes the capillary leaky

Question 11

There are a lot of inflammatory mediators that are released from cells, IE prostaglandins. Do anti-inflammatory drugs work on all of these inflammatory mediators?

Answer 11

Nope, they probably just act on one of the inflammatory mediators, most likely prostaglandins

Question 12

T/F the anti-inflammatory properties and pain relief come from attenuating the production of prostaglandins?

Answer 12

True

Question 13

What are the two main acts of prostaglandins?

Answer 13

Pain sensitization and more inflammation

Question 14

Prostaglandins are all derived from what?

Answer 14

arachidonic acid

Question 15

Arachidonic acid is liberated via the result of some signaling event.

Answer 15

Arachidonic acid can be liberated from the cell membrane if I’m not mistaken. If I am mistaken, please edit this card.

Question 16

T/F cell signaling leads to the liberation of arachidonic acid?

Answer 16

TRue

Question 17

Which enzymes send the arachidonic acids down the path that leads to prostaglandin production?

Answer 17

COX1 and COX2

Question 18

Prostaglandins play a key role in generating and maintaining what?

Answer 18

The inflammatory response

Question 19

T/F prostaglandins play a key role in pain sensitization?

Answer 19

Truth

Question 20

What does pain sensitization mean?

Answer 20

It means that after the injury occurs, the prostaglandins make things hurt more. So it makes sense as to why we would want to inhibit them.

Question 21

How is nociceptor activity enhanced?

Answer 21

Prostaglandins activate G proteins that lead to the increased activity of PKA. PKA phosphorylates the TRP type nociceptor and enhances its activity leading to increased pain.

Question 22

NSAIDS all work by inhibition of which enzymes?

Answer 22

COX

Question 23

What do COX enzymes do?

Answer 23

They drive the production of prostaglandins. Inhibit COX enzymes and you inhibit prostaglandins and if you inhibit prostaglandins you inhibit inflammation

Question 24

Aspirin is a 100x better inhibitor of COX___ than COX___.

Answer 24

100x better inhibitor of COX-1 than COX-2

Question 25

Aspirin is a reversible or irreversible inhibitor of COX-1 and COX-2?

Answer 25

Irreversible

Question 26

Ibuprofen, naproxen, and acetaminophen are all _____ inhibitors of COX-1 and COX-2.

Answer 26

reversible

Question 27

Naproxen is most selective for COX-1 or COX-2.

Answer 27

COX-2

Question 28

What are the therapeutic effects of acetylsalicylic acid (aspirin)?

Answer 28

Analgesia, antipyretic (fever), anti-inflammatory, anti-thrombotic

Question 29

What are the therapeutic effects ibuprofen and naproxen?

Answer 29

Analgesia, antipyretic, and anti-inflammatory

Question 30

What are the therapeutic effects of acetaminophen?

Answer 30

Analgesia, antipyretic

Question 31

Aspirin inhibits COX enzymes. Inhibition of COX enzymes inhibits what that is crucial for platelet aggregation?

Answer 31

Thromboxane A2

Question 32

Even though all of the NSAIDS we're talking about inhibit COX enzymes, why is aspirin the only one that has a significant effect on platelet formation?

Answer 32

Because aspirin is the only one that irreversibly binds. Everything else has a small change in platelet activity, but when the drug leaves the plasma, normal thromboxane A2 production can resume.

Question 33

T/F, only low doses aspirin are effective at preventing thrombotic events?

Answer 33

True

Question 34

Is acetaminophen an anti-inflammatory? Why or why not?

Answer 34

No because it never reaches the threshold concentration of the drug necessaryf to produce an anti-inflammatory effect, but it does have enough for pain relief

Question 35

Prostaglandins (made primarily from COX-1 activity) stimulates _____ and ______ secretion that comprise the mucus gel that protects the stomach from digesting itself.

Answer 35

mucus and bicarbonate | Thanks prostaglandins

Question 36

Why are COX inhibitors potentially bad for your stomach?

Answer 36

If you inhibit COX-1, then you inhibit prostaglandins. If you inhibit prostaglandins, then you inhibit the production of the mucous that lines the stomach. This can lead to bleeding, kidney problems, increased blood pressure

Question 37

What is Reye's syndrome?

Answer 37

It is characterized by a fatty change in the liver and edematous encephalopathy following aspirin use. Generally preceded by a mild upper respiratory tract infection that was managed with aspirin at levels that usually aren't toxic, but in a person with Reye's syndrome it is toxic

Question 38

What are some precautions and contraindications for aspirin use?

Answer 38

Ulcers- internal bleeding Diabetes- hyper/hypoglycemia Gout Hypo coagulation conditions- bleeding without clotting

Question 39

Selective COX-2 inhibitors are bad. Except for celebrex.

Answer 39

Liver failure, cardiac problems

Question 40

Which provides more pain relief, opioids or NSAIDS?

Answer 40

Opioids.

Question 41

What is the most effective analgesia?

Answer 41

An optimum dose of NSAID and some opioids