NSAID med chem and clinical

Question 1

define prostaglandin

Answer 1

20 carbon fatty acid derived from cell membrane phospholipids

Question 2

what are the 5 most inflammatory prostaglandins

Answer 2

PGD2, PGE2, PGF2a, G2, H2

Question 3

how are prostaglandins formed

Answer 3

1. phospholipid to arachidonic acid by phospholipase a2 2. arachidonic acid to G2 by COX 3. G2 to H2 rapidly because it is unstable 4. H2 to other prostaglandins

Question 4

how are leukotrienes formed

Answer 4

from arachidonic acid

Question 5

what does PGD2 do

Answer 5

• vasodilation - inhibition of platelet aggregation - GIT/uterine relaxation

Question 6

what does PGF2a do

Answer 6

uterine contraction

Question 7

what does PGE2 do

Answer 7

EP1- broncho/git contraction EP2/4- broncho vasodilation and fluid secretion EP3- smooth muscle contraction and inhibition of gi acid

Question 8

what is cox

Answer 8

• Membrane embedded protein but mainly in cytoplasm - Exists in dimer form with a long hydrophobic tunnel ○ Arachidonic acid is hydrophobic and formed in the membrane Heme active site allows for production of radicals

Question 9

amino acid in cox1

Answer 9

isoleucine

Question 10

amino acid in cox 2

Answer 10

valene

Question 11

what is the MOA of paracetamol

Answer 11

analgesic and antipyretic - cox inhibitor

Question 12

C/I or special patient groups with aspirin

Answer 12

• under 16s - reyes unless indicated in kawasakis - previous or active peptic ulcers, bleeds, cardiac failure, hypersensitivity - elderly

Question 13

MOA of aspirin

Answer 13

antiplatelet: inhibits thrombus formation in 1st and 2nd CVD prevention analgesic: rarely used - risk of side effects

Question 14

C/I or special patient groups with paracetamol

Answer 14

• children - low body weight <50kg - liver impairment

Question 15

counselling points for NSAIDs

Answer 15

• lowest dose shortest time - with/after food- self monitor for side effects

Question 16

side effects with aspirin

Answer 16

• Bronchospasm, dyspepsia, GIT irritation

Question 17

cautions with aspirin

Answer 17

• use with drugs that increase bleeding risk - drugs that increase renal side effects - can increase toxicity of methotrexate - overdose

Question 18

MOA of NSAIDs

Answer 18

COX inhibition - analgesic within 1 week and anti-inflammatory in 3 weeks

Question 19

name a COX 2 selective NSAID

Answer 19

etoricoxib

Question 20

name a COX inhibitor with COX 2 selectivity

Answer 20

diclofenac

Question 21

what are the special patient groups for NSAIDs

Answer 21

• elderly - renal failure - increased CV risk- BP, DM, hypercholesteremia

Question 22

cautions with NSAIDs

Answer 22

renal failure - co prescribed nephrotoxic medicines, anti-hypertensives, lithium and methotrexate CV events - antiplatelet aspirin and antihypertensives

Question 23

side effects of NSAIDs

Answer 23

GIT irritation, kidney disease, CVD, bronchospasm, sodium/water retention

Question 24

NSAID with high GI side effect risk

Answer 24

ketoprofen

Question 25

NSAID with moderate GI side effect risk

Answer 25

naproxen, diclofenac

Question 26

NSAID with low GI side effect risk

Answer 26

ibuprofen, etoricoxib

Question 27

NSAID with high CV side effect risk

Answer 27

diclofenac