Anti-inflammatory Drugs

Question 1

Cetirizine (Zirtec)

Answer 1

2nd Gen Antihistamine (CANNOT cross the BBB) MOA: Binds to H1 receptor, blocking the effects of histamine (antagonist)

Question 2

Fexofenadine (Allegra)

Answer 2

2nd Gen Antihistamine (CANNOT cross the BBB) MOA: Binds to H1 receptor, blocking the effects of histamine (antagonist)

Question 3

Zileuton

Answer 3

Leukotriene synthesis inhibitor (Anti-inflammatory) MOA: Inhibits 5-lipoxygenase enzyme TX: Asthma

Question 4

Montelukast

Answer 4

Leukotriene receptor blocker (Anti-inflammatory) MOA: Acts as receptor antagonist

Question 5

Omalizumab

Answer 5

• anti-IgE-Ab (Anti-inflammatory)
• MOA: Prevents the release of histamine granules by mast cells by binding to IgE (neutralization)

Question 6

Celecoxib

Answer 6

• NSAID
• Selective (reversible) COX-2* inhibitor - => inhibits synthesis of ecosinoids (PGs and TXA2)

Question 7

Diphenhydramine (Benydryl)

Answer 7

1st Gen Antihistamine (Crosses the BBB - intense sedative) MOA: Binds to H1 receptor, blocking the effects of histamine (antagonist)

Question 8

Loratadine (Claritin)

Answer 8

2nd Gen Antihistamine (CANNOT cross the BBB) MOA: Binds to H1 receptor, blocking the effects of histamine (antagonist)

Question 9

Acetylsalicylic Acid (Asprin)

Answer 9

NSAID Non-selective (irreversible*) COX inhibitor

Question 10

Chloropheniramine

Answer 10

1st Gen Antihistamine (Crosses the BBB - mild sedative) MOA: Binds to H1 receptor, blocking the effects of histamine (antagonist)

Question 11

Prednisone

Answer 11

Oral Corticosteroids (anti-inflammatory) 1. prevent phospholipid release from membrane (no arachidonic acid, and therfore no LTs or PGs) 2. competitive antagonist to importin-alpha (binds to glucocorticoid receptor, preventing GATA-3 from entering nucleus and initiating cytokine synthesis 3. Inhibits p38 MAP kinase

Question 12

MOA of TNF-alpha Inhibitors?

Answer 12

Most are monoclonal Abs that either: 1. Bind and neutralize TNF-alpha 2. Bind and activate ADCC 3. Bind and fix complement examples: Etancercept, Infliximab, Adalimumab, Certolizumab pegol

Question 13

Promethazine

Answer 13

1st Gen Antihistamine (Crosses the BBB- intense sedative) MOA: Binds to H1 receptor, blocking the effects of histamine (antagonist)

Question 14

Ibuprofen

Answer 14

NSAID Non-selective (reversible) COX inhibitor

Question 15

Naproxen

Answer 15

• NSAID - Non-selective (reversible) COX inhibitor - => inhibits synthesis of ecosinoids (PGs and TXA2)

Question 16

Dimenhydrinate

Answer 16

1st Gen Antihistamine (Crosses the BBB- intense sedative) MOA: Binds to H1 receptor, blocking the effects of histamine (antagonist)

Question 17

Beclomethasone

Answer 17

Inhaled Corticosteroids (Anti-inflammatory) 1. prevent phospholipid release from membrane (no arachidonic acid, and therfore no LTs or PGs) 2. competitive antagonist to importin-alpha (binds to glucocorticoid receptor, preventing GATA-3 from entering nucleus and initiating cytokine synthesis 3. Inhibits p38 MAP kinase

Question 18

Roflumilast

Answer 18

• PDE inhibitor
• MOA: inhibits the action of phosphodiesterase-4 which prevents recruitment and activation of key inflammatory cells - used for Tx of COPD

Question 19

Acetaminophen

Answer 19

• NSAID - analgesic & antipyretic - => inhibits synthesis of ecosinoids (PGs and TXA2)