Non-opioid Analgesics

Question 1

NSAIDs - Arylpropionic acids

Answer 1

Ibuprofen

Naproxen

Question 2

NSAIDs- Arylacetic Acids

Answer 2

Indomethacin

Diclofenac

Ketorelac

Etodolac

Question 3

For myalgias, arthralgias, sprains, strains

Answer 3

Ibuprofen

Question 4

For Dysmenorrhea

Answer 4

Ibuprofen

Question 5

For Headache

Answer 5

Tylenol

Question 6

May potentially inhibit bone healing (post-ortho)

Answer 6

Tylenol

Question 7

Three therapeutic applications of NSAIDs

Answer 7

Analgesic

Antipyretic

Anti-inflammatory

Question 8

Three phases of inflammation

Answer 8

Acute (vasodil)

Subacute (infiltration)

Chronic (proliferation)

Question 9

___ and ___ protect the stomach lining

–what is the enzyme?

Answer 9

PGE2 and PGI2

(inhibit acid, promote mucus)

COX1

Question 10

COX1 is ___

COX2 is ___

Answer 10

1 = constitutive

2 = Inducible

Question 11

COX2 is present constitutively in..

Answer 11

the brain and spinal cord

Question 12

Aspirin MOA

Answer 12

Acetylates COX (ser529)

Irreversibly Inhibits COX1/2

Question 13

NSAIDs (except aspirin) are ______

Answer 13

competitive, reversible inhibitors of COX1/2

Question 14

These NSAIDs also inhibit LT synthesis

Answer 14

Indomethacin

Dicclofenac

Question 15

Aspirin mainly absorbed here

Answer 15

Jejunum

Question 16

Aspirin distribution

Answer 16

Most tissues/fluids

Crosses placenta

Question 17

Aspirin T1/2

Answer 17

15 minutes

(but metabolite salicylate half life = 12 hr)

Question 18

Is aspirin secreted or reabsorbed in tubule

Answer 18

Yes

Active secretion, Passive reabsorption

Question 19

Non-salicylate NSAID’s show little

Answer 19

first pass metabolism

(Multiple routes of metabolism – Oxidation, Demethylation, Conjugation)

Question 20

Timeline for aspirin analgesic tolerance

Answer 20

no tolerance with analgesic effects!

Question 21

Arylpropionic acids T1/2

Answer 21

Ibuprofen = 2h

Naproxen = 14h

Question 22

_____ is safest Arylpropionic in coronary artery disease

Answer 22

Naproxen

Question 23

Acetic acid derivatives and their risks

Answer 23

Diclofenac (peptic ulcer/kidney dysfxn if prolonged use)

Indomethacin (Gout, ankylosing spond. pericarditis)

Ketorolac (Less than 5 days, low GI effect)

(also etodolac?)

Question 24

Meloxicam at low doses is..

Answer 24

COX-2 selective

(long T1/2 = 20hrs)

Question 25

Has a half life of 57 hours!

Answer 25

Piroxicam

Question 26

Advantages of APAP

Answer 26

No GI tox Liver dz patients ok No platelet effect No Reye's

Question 27

APAP overdose leads to

Answer 27

hepatic necrosis

Question 28

Salicylates - ____ given for GI distress

Answer 28

Misoprostol | (PGE1 analog -- also labor induction)

Question 29

Metabolic derangement on overdose

Answer 29

**Metabolic acidosis** (kids) and **Resp alkalosis** (adults) _MAcid_ = Early decrease in ATP, Late Increase in Lactate and pyruvate _RAlk_ = Direct stimulation of medullary respiratory centers

Question 30

Sakucylism effects

Answer 30

_Mild_ = vertigo, tinnitus, hearing loss _Moderate/Severe_ = N/V, sweating, fever, delirium/psychosis, stupor, coma

Question 31

Tx for aspirin poisoning

Answer 31

1. Increase urinary excretion (dextrose, sodium bicarb) 2. Hemodialysis 3. Charcoal 4. Correct metabolic imbalance

Question 32

Non-salicates labor use

Answer 32

Delay preterm labor by inhibiting uterine motility

Question 33

APAP AE's (kidney and liver)

Answer 33

* Papillary necrosis, Vasoconstriction by inhibition of PGE2 * Dose dependent hepatic necrosis (increased with Alcohol's induction of CYP450)

Question 34

Selective COX2 inhibitors

Answer 34

Rofecoxib (Vioxx - withdrawn!) Celecoxib (Celebrex)

Question 35

All NSAID's CI'd in...

Answer 35

CKD Peptic Ulcer Dz GI bleeding Hx

Question 36

NSAID Cardiovascular risk is highest in ____ and lowest in \_\_\_\_\_

Answer 36

Highest = Diclofenac Lowest = Naproxen

Question 37

NSAIDs that interfere with bone healing

Answer 37

All of 'em | (in high doses)

Question 38

\_\_\_\_ less likely to cause NSAID-induced asthma exacerbations

Answer 38

COX2-specific

Question 39

Antiproliferative DMARD's

Answer 39

MTX Cyclophosphamide Azathioprine Suppress B and T cell proliferation and function