Pharmacology of non-opiate analgesics

Question 1

amine autocoids

Answer 1

histamine

serotonin

Question 2

lipid derived autocoids

Answer 2

prostaglandins

leukotrienes

Question 3

peptide hormones

Answer 3

bradykinin

angiotensin

Question 4

non classified class of autocoids

Answer 4

cytokines

Question 5

timeline of non-opioids for pain

Answer 5

aspirin
acetaminophen
paracetamol
ibuprofen
indomethacin
diclofenac
naproxen
piroxicam

Question 6

Salicylates class of NSAIDs

Answer 6

aspirin

Question 7

Arylpropionic acids class of NSAIDs

Answer 7

ibuprofen

naproxen

Question 8

Arylacetic acids class of NSAIDs

Answer 8

indomethacin
diclofenac
ketorolac
etodolac

Question 9

Enolic acids class of NSAIDs

Answer 9

piroxicam

meloxicam

Question 10

2nd class of non-opioid that isn’t NSAID

Answer 10

p-Aminophenols

Question 11

Only drug of p-aminophenols

Answer 11

acetaminophen

Question 12

NSAIDs for analgesic

Answer 12

> headache: tylenol
chronic postsurgical pain: tylenol + opioid
myalgias/arthralgias/sprains/strains: ibuprofen
inflammatory pain: ibuprofen
dysmenorrhea(specific PGE effect): ibuprofen

Question 13

NSAIDs for antipyretic

Answer 13

> fever: acetaminophen

Question 14

NSAIDs for anti-inflammatory

Answer 14

bursitis and tendonitis
osteoarthritis
RA including ankylosing spondylitis
gout and hyperuricemia
rib fractures

Question 15

5 symptoms of inflammation

Answer 15

rubor: redness
tumor: swelling
calor: heat
dolor: pain
…and loss of function

Question 16

3 phases of inflammation

Answer 16

acute; vasodilation and increased permeability
subacute; infiltration
chronic; proliferation

Question 17

mediators that recruit inflammatory cells

Answer 17

eicosanoids
> arachidonic acid metabolites
> PG; redness, heat
> thromboxanes
> leukotrienes; swelling
> cytokines; pain

Question 18

main function of NSAIDs; inhibit what and what pathway

Answer 18

cox inhibitors in the arachidonic pathway

Question 19

cox-1 produces

Answer 19

prostanoids from arachadonic acid

Question 20

prostanoids metabolites include

Answer 20

TXA2
PGE2
PGI2

Question 21

function of TXA2

Answer 21

> prothombotic; increase platelet activation and clotting via gp2b3a
vasoconstriction
inhibitor acts as blood thinner

Question 22

function of PGE2 and PGI2

Answer 22

> protect stomach lining cox 1 GI expression
inhibit acid secretion
promote mucus secretion
inhibition can lead to stomach ulcers

Question 23

cox-1 expressed where

Answer 23

platelets, kidneys, stomach

Question 24

function of PGI2 in vasculature

Answer 24

vasodilation

reduce platelet aggregation

Question 25

cox-2 expressed where

Answer 25

brain | spinal cord

Question 26

function of cox-2

Answer 26

> induced in setting of inflammation | > induced by cytokines and inflammatory mediators

Question 27

MOA of aspirin

Answer 27

irreversibly inhibits cox-1 and modifies cox-2 by acetylation

Question 28

Aspirin and cox-2

Answer 28

modified by acetylation to turn off its ability to produce PGE and activate its ability to produce protective lipid mediators

Question 29

Arylacetic acids that inhibit leukotriene synthesis

Answer 29

indomethacin | diclofenac

Question 30

Absorption of salicylates

Answer 30

> rapidly absorbed from stomach and jejunum > passive diffusion of free acid; gastric pH > delayed by presence of food

Question 31

distribution of salicylates

Answer 31

> throughout most tissues and fluids > readily crosses placenta > competes with many drugs for protein binding sites

Question 32

metabolism and excretion of salicylates

Answer 32

> aspirin t1/2 15min > salicylate t1/2 12hrs > active secretion and passive reabsorption in renal tubule > increased excretion with increased urinary pH

Question 33

absorption of non-salicylate NSAIDs

Answer 33

> well absorbed from GI tract

Question 34

metabolism of non-salicylate NSAIDs

Answer 34

> little first pass metabolism | > oxidation, demethylation, conjugation for metabolism

Question 35

excretion of non-salicylate NSAIDs

Answer 35

> drugs and metabolites excreted primarly as conjugates | > active secretion of parent drug in renal tubule

Question 36

Aspirin general use

Answer 36

> analgesia, antipyresis, anti-inflammatory > main use of anti-coagulation > no tolerance development > risk in treating children; Reye's syndrome(rash, vomitting, liver necrosis)

Question 37

Arylpropionic acids half life

Answer 37

Ibuprofen: 2hr Naproxen: 14hr

Question 38

NSAID for coronary artery disease

Answer 38

safest is naproxen

Question 39

Diclofenac use

Answer 39

gel for arthritic pain

Question 40

risk of diclofenac

Answer 40

> increased risk of peptic ulcer and renal dysfunction with prolonged use

Question 41

Arthrotec description

Answer 41

> diclofenac/misoprostol mix | > misoprostol = PGE1 analog

Question 42

indomethacin MOA

Answer 42

potent reversible inhibitors of PG biosynthesis

Question 43

use for indomethacin

Answer 43

acute gouty arthritis, ankylosing spondylitis, pericarditis

Question 44

ketorolac

Answer 44

> should not be given longer than 5 days | > available as IV

Question 45

Use of enolic acids(Meloxicam, Piroxicam)

Answer 45

> treat arthritis > great joint penetration > one of the least GI side effects

Question 46

Half lives of enolic acids

Answer 46

> Meloxicam: 20hrs > Piroxicam: 57hrs low dose meloxicam is cox-2 selective

Question 47

ended on page 18

Answer 47

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