NSAIDS!

Question 1

3 main effects of NSAIDs

Answer 1

1. Analgesic
2. Antiinflammatory
3. Antipyretic

Question 2

What are the effects of protaglandins

Answer 2

one of the main mediators of inflammation causing sensitization of nociceptors, dilation of peripheral vessels and local edema

Question 3

How do NSAIDs affect the production of protiglandins

Answer 3

inhibits cyclooxagenases stoping production of prostaglandin from arachonic acid

Question 4

What is COX-1 used for and where is it found

Answer 4

found throughout body

Important for the productuon of prostaglandins (PGE, PGI2) that are cytoprotective for gastric mucosa (inhibit acid sec)

Question 5

What is COX 2 and where is it found

Answer 5

Inducable enzyme (low normally but increased w needed) or expressed in kidney, CNS

Responsible for the production of protaglandins that mediate the inflammatory response

Question 6

Salicutic acid drugs (ASA) effects (3)

Answer 6

• Analgesia peripheral and central
• effect on hypothalamus to decrease heat loss
• increases uric acid secretion (to avoid accumulation in jts)

Question 7

ASA duration of action and how is it metabolised in the body

Answer 7

-duration of action 4 hours

Hydrolyzed by estarases in blood/tissues to salicylate and acetic acid

excreted in urine (enhanced by alkaline urin)

Question 8

what is the MOA for antipyretic effects

Answer 8

inhibition of the synthesis of PGE2 (wont be able to increase set point of hypothalamus)

Question 9

what is the MOA for the antiinflammatory effects

Answer 9

inhibits protaglandins leading to decreased vasodialation, edema, decreased leukocyte migration and stabilization of membranes

Question 10

Indications of use of ASA (4)

Answer 10

• mild/mod pain
• relief of fever in febile pts
• antiinflamatory
• prevent clot formation in cerebral + coronary vessels

Question 11

Geneeral Advese affects of ASA

Answer 11

epigastric distress, nausea, vomitting, microscopic bleeding

-gastric ulceration and bleeding due to inhibition of protaglandin protection

Question 12

What has ASA been associated with in children

Answer 12

in children w chickenpox, influenza administratin of ASA has been associated with development of Reyes syndrome

Question 13

How can NSAIDs affect BP

Answer 13

NSAIDs tend to promote sodium retention which may cause an increase in BP

Question 14

What can repeated NSAID taking lead to

Answer 14

tinnitis, mental confusion, kidney tox, prolonged prothrombin time

Question 15

What does NSAIDS do to uric acid at high/ low doses

Answer 15

at high doses: loss of uric acid in urine

at low doses: retention of uric acid

Question 16

What is the benifit of Ibuproden

Answer 16

Generally better tolerated than ASA, though may cause some git probs and bleeding

Question 17

Naproxon use in combonaton

Answer 17

Used in combo with methocarbamol (mm relaxant for tx of mm spasm and backache

Question 18

Oxicams characteristics (4)

Answer 18

Amphoteric- 2 sites for ionazation depending on PH conditions

Long half life*- 2-3x most nsaids

Low dose

Selectively stops COX2 (less git effects)

Question 19

Example of oxicam

Answer 19

Meloxicam

Question 20

What is idomethacin used for/ good at and side effect

Answer 20

Inhibits protaglandin synthesis, very potent anti inflammatory

-may cause more serious git problems and CNS complaints

Question 21

what is an example of a selective cox 2 inhibitor and what does it not have a major impact on

Answer 21

Celecoxib

claimed no sig affect on platelet aggregation or bleeding time

Question 22

What does acetaminophen selectively inhibit and its main effects

Answer 22

V weak inhibitor of COX 1/2
-pot inhibitor of COX 3??

-Little antiinflammatory action but more central analgesia and some antipyeretic

Question 23

Which Nsaids have more Cox 1 selectivity (3) and Cox 2

Answer 23

Cox 1- Ibuprofen, naproxen, asprin

Cox 2- Celecoxib

Question 24

Which is the tx of choice for arthritic diseases

Answer 24

ASA

Question 25

What was used for serious inflammation but now not used due to toxicity

Answer 25

Gold salts