Drug mechanisms

Question 1

Aspirin

Answer 1

Irreversibly inhibits COX1 and COX2 by acetylating a serine residue in the active site-blocks entry of substrate

Exhibits 3 A’s (anti-inflammatory, analgesic, antipyretic)

Question 2

Ibuprofen and Naproxen (NSAIDs)

Answer 2

Reversible competitive inhibitors of COX1 and COX2; block the substrate channel of both

Exhibit 3 A’s

Question 3

Celecoxib

Answer 3

COX2 specific-fits in the COX2 active site and inhibits it

Question 4

Zyflo

Answer 4

Inhibits 5-LOX

Used for prophylatic and chronic treatment of asthma

Question 5

Singuilar

Answer 5

Prevents binding of cysteinyl leukotrienes to CycLT receptors on bronchial smooth muscle cells and inflammatory cells

Question 6

Tylenol

Answer 6

Mechanism not clear; not an NSAID

May inhibit splice variant of COX1

Question 7

Glucocorticoids

Answer 7

Reduce synthesis of both leukotrienes and prostanoids

stimulates lipocortin mRNA expression and inhibits PLA2 activity

Question 8

Heparin

Answer 8

Inhibits IXa, Xa, IIa (via ATIII)

Reversal agent: protamine sulfate

Question 9

Warfarin

Answer 9

Inhibits VII, IX, X, II (via decreased GLA residues)

Reversal agent: Vitamin K

Question 10

Xarelto

Answer 10

Reversible competitive inhibitor of free and clot-bound Xa

Reversal agent: AndexXa (Factor Xa)

Question 11

Eliquis

Answer 11

Reversible competitive inhibitor of free and clot-bound Xa

Reversal agent: AndexXa (Factor Xa)

Question 12

Pradaxa

Answer 12

Reversible competitive inhibitor of thrombin

Reversal agent: Praxbind