1. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 1 Chapter 26 Antiinflammatories and Antihistamines

2. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 2 Objectives  List both generic and trade drug names covered in this chapter.  Describe the symptoms of inflammation.  Differentiate between steroidal and nonsteroidal antiinflammatories.  List the major side effects of the agents discussed.

3. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 3 Objectives (cont’d)  List the major cells that are activated from the immune system to repair damaged cells.  List the major inflammatory conditions.  List the drug action of pain receptors.

4. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 4 Objectives (cont’d)  List the major medications used in the treatment of arthritis, rheumatoid arthritis, osteoarthritis, and other major conditions.

5. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 5 The Inflammatory Response  Inflammation can be caused by infection, allergic reactions, or injury.  Inflammation is a necessary response for healing  Inflammation and pain run hand in hand http://alexanderjamesstockphotography.com/people- travel-and-leisure/stock-photo-kids-at-play-running- hand-in-hand-on-grass-7819-04-131.html

6. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 6 Aspirin  England, 1800s—bark from willow tree effective for pain, fever, inflammation.  Aspirin is acetylsalicylic acid-ASA.  The first company to market Aspirin was Bayer Company in 1899.  Still popular due to effectiveness and low cost

7. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 7 Aspirin (cont’d)  Used to treat pain, fever, inflammation, and gout  Aspirin should not be given to children.  Aspirin causes Reye’s syndrome: vomiting, lethargy, encephalopathy (leads to coma and death).  Side effect can be upset stomach.  If taken with anticoagulants, increased bleeding.

8. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 8 Aspirin (cont’d)  Most common uses: prevention of strokes or heart attacks.  Aspirin decreases platelet aggregation (clotting).  Dose to decrease blood clotting is 81 to 325 mg/day.

9. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 9 NSAIDs  NSAIDs (Nonsteroidal Antiinflammatory Drugs) have analgesic, antipyretic, antiinflammatory properties.  Are available in prescription and OTC forms.  Are used for mild or moderate pain.

10. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 10 Common OTC NSAIDs  Motrin/ibuprofen  Aleve/naproxen

11. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 11 NSAIDs (cont’d)  NSAIDs used to treat muscle pain, rheumatoid arthritis, bone pain, PMS.  Overuse can worsen stomach problems (GERD).  Take with food.  Do not take with anticoagulants.

12. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 12 Cyclooxygenase (COX)  Responsible for synthesizing prostaglandins which are responsible for pain and inflammation  COX-1 (protects gastric mucosa and promotes platelet aggregation)  COX-2 (found at sites of tissue injury and in the brain)

13. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 13 Cyclooxygenase-2 Inhibitors  First-generation NSAIDs  Inhibit COX-1 and COX-2—decrease in inflammation, pain, fever  Negative effect of inhibiting COX-1—gastric erosion, ulceration, bleeding, renal damage  Second-generation NSAIDs—COX-2 selective  Reduce inflammation, pain, fever without side effects of COX-1 inhibitors

14. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 14 COX inhibitors  COX-1 inhibitors taken off the market-too dangerous  Most common COX-2 inhibitor- Celebrex/celecoxib  Auxiliary labels- “May Cause Dizziness or drowsiness”; “Take with food or milk”; “Do not crush or chew capsules”

15. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 15 Steroids  Steroids are produced naturally by the body  Main gland-adrenal gland  Used to decrease inflammation in conditions like RA, OA, asthma, cancer  High doses can cause decreased immune response, increased appetite, bruising, insomnia, restlessness, anxiety, hypotension, headache

16. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 16  Serious side effects—if taken over long period of time, taken inappropriately, or stopped abruptly.  Discontinuing a steroid must be done slowly.

17. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 17 Steroids (cont’d)  To treat asthma-steroids (corticosteroids) available in inhalant or parenteral forms  Cause bronchodilation  Auxiliary label: Shake Well on Inhalers

18. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 18 Common Steroids  prednisone  hydrocortisone  methylprednisolone

19. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 19 Controlled Analgesics  Opiods: to treat pain Oxycodone, Duragesic (fentanyl), Vicodin, Percocet, Tylenol w/ Codeine  May be combined with NSAIDs to intensify their effects

20. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 20 Antihistamines  Histamine causes allergic responses when antigen is found in the body  Allergic response can become anaphylactic shock=death  Antihistamines block histamine receptors

21. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 21 Histamine 1  H 1 receptors are found in the lower resp. tract and skin-  When histamine binds with H 1 receptors= coughing, sneezing, wheezing, urticaria (rash), bronchiolar constriction

22. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 22 Histamine2  H2 receptors are located in GI tract-  When histamine binds with H2 receptors= nausea, vomiting, diarrhea, cramps

23. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 23 Allergic Conditions and Their Treatment  OTC drugs used for short-term relief.  First-generation antihistamines:  Nonspecific—bind both H 1 and H 2  Cause sedation (affect CNS)  Decrease nausea, vomiting, motion sickness.  EX: Benadryl/diphenhydramine

24. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 24 Allergic Conditions and Their Treatment (cont’d)  Second-generation antihistamines  Affect H 1 only  Cromolyn (inhaled), Allegra/fexofenadine, Zyrtec/cetirizine taken to prevent allergic responses.

25. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 25 Antihistamine and Combination Drugs  Used to decrease inflammation and irritation from allergens.  Some antihistamines are combined with decongestants.  Work best when taken before an allergic reaction.  There are OTC nasal sprays and drops.  Steroids used.

26. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 26 Drug Interactions  Do not consume alcohol with antihistamines—will increase drowsiness.  Antibiotics—macrolides (Erythromycin), ketoconazole, itraconazole—intensify effects of second-generation antihistamines.  Only non-drowsy OTC is Claritin.

27. Copyright © 2012, 2007, 2004 by Saunders, an imprint of Elsevier Inc. All rights reserved. 27 Anaphylaxis  Most severe reactions cause swelling of airways.  Epinephrine given by inhalation, injection to open airways.