NSAIDs and Eicosanoids

Question 1

Corticosteroids

Answer 1

Anti-inflammatory effects.

Question 2

Leukotrienes:

1) LTB4
2) LTC4
3) LTD4

Answer 2

All induce plasma leakage (edema formation).

All are bronchoconstrictors.

Question 3

Misoprostol

Answer 3

EP3 receptor agonist
Mimics PGE2
Stimulates mucus secretion in the GI tract
Stimulates smooth muscle contraction and can cause cramping / diarrhea.

Question 4

Prostaglandins

1) PGI2 (Prostacyclin)
2) PGE2
3) PGF2a

Answer 4

1) Vasodilator, inhibits gastric secretion, promotes mucous secretion.
2) Bronchodilator, same GI effects as PGI.
3) Bronchoconstrictor,

Question 5

TXA2 (Thromboxane A2)

Answer 5

Produced by platelets via COX-I enzyme to promote platelet aggregation.
Inhibition of COX-1 in platelets is irreversible.
Also a bronchoconstrictor.

Question 6

Aspirin

Answer 6

Non-specific NSAID.

Irreversible inhibitor of COX.

Question 7

Acetaminophen (Tylenol)

Paracetamol

Answer 7

Non-specific NSAID.
Analgesic (pain) and antipyretic.
Not an anti-inflammatory.
COX inhibition is not primary means of action, except in the brain to prevent fever.

Question 8

Indomethacin (Indocin)

Answer 8

Non selective COX inhibitor.
Mostly used to treat Rheumatoid Arthritis, gouty arthritis, and ankylosing spondylitis.
Many extra CNS side effects.

Question 9

Ibuprofen (Motrin, Rufen, Advil, Nuprin)

Answer 9

Non-specific NSAID.
Treats RArthitis, OArthritis, analgesia, dysmenorrhea, fever.
In the same class as Naproxen (aleve).

Question 10

Sulindac (Clinoril)

Answer 10

Non-specific NSAID.
Like Indocin, treats OA, RA, Ankylosing spondylitis, acute gouty arthritis.
Less direct GI irritation.

Question 11

Diclofenac (Volatren)

Answer 11

Potent non-selective COX inhibitor.

Treats OA, RA, Ankylosing Spondylities, dysmenorrhea, analgesia and fever.

Question 12

Ketorolac (Toradol)

Answer 12

Non-selective NSAID.
Approved only for analgesia.
Also has typical NSAID properties (antipyretic, antiinflammatory).
Used post-op in IM or IV.

Question 13

Rofecoxib (Vioxx)

Answer 13

COX-2 selective NSAID.
Reduces GI toxicity.
Increases risk of thrombotic event by disrupting the balance of TXA2 / PGI2 inhibition platelets vs. endothelium.

Question 14

Celecoxib (Celebrex)

Answer 14

COX-2 selective NSAID.

Reduces GI toxicity.

Question 15

Diflunisal (Diflucan)

Answer 15

Non-selective NSAID.

Question 16

Mesalamine and sulfasalazine

Answer 16

Non-selective NSAID.
Salicylic Acid derivative.
Treats inflammatory bowel syndrome.

Question 17

Zileuton

Answer 17

Lipoxygenase inhibitor decreases production of bronchoconstricting leukotrienes (LTD4, LTC4). Used to treat asthma.

Question 18

Salsalate (Disalcid)

Answer 18

Salicylic acid derivate.
Non-selective NSAID.
Weaker and reversible COX-inhibitor.
Less GI toxicity than Aspirin.