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Antiinflammatory Agents
               and Nonsteroidal
            Antiinflammatory Drugs
                    (NSAIDs)


Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs

  • Large and chemically diverse group of drugs
    with the following properties:
         – Analgesic
         – Antiinflammatory
         – Antipyretic




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Mechanism of Action

  • Activation of the arachidonic acid
    pathway causes:
  • pain
  • headache
  • fever
  • inflammation


Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
Instructors may wish to use
                         EIC Image #107:

                      Arachidonic Acid Pathway




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Mechanism of Action

  Analgesia—treatment of headaches and pain
  • Block the undesirable effects of prostaglandins,
    which cause headaches




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Mechanism of Action

  Antipyretic: reduce fever
  • Inhibit prostaglandin E2 within the area of the brain
    that controls temperature




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Mechanism of Action

  Relief of inflammation
  • Inhibit the leukotriene pathway, the prostaglandin
    pathway, or both




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs
  Six structurally related groups:
  • Acetic acids
  • Carboxylic acids
  • Propionic acids
  • Enolic acids
  • Fenamic acids
  • Nonacidic compounds


Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Acetic Acid

  • diclofenac sodium (Voltaren)
  • diclofenac potassium (Cataflam)
  • etodolac (Lodine)
  • indomethacin (Indocin)
  • sulindac (Clinoril)
  • tolmetin (Tolectin)

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Carboxylic Acids
  Acetylated
  • aspirin (ASA)
  • choline magnesium salicylate (Trilisate)
  • diflunisal (Dolobid)

  Nonacetylated
  • salicylamide
  • salsalate (Disalcid)
  • sodium salicylate
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Propionic Acids
  • fenoprofen (Nalfon)
  • flurbiprofen (Ansaid)
  • ibuprofen (Motrin, others)
  • ketoprofen (Orudis)
  • ketorolac (Toradol)
  • naproxen (Naprosyn)
  • oxaprozin (Daypro)
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Other Agents
  Enolic acids
  • phenylbutazone (Butazolidin)
  • piroxicam (Feldene)

  Fenamic acids
  • meclofenamic acid (Meclomen)
  • mefenamic acid (Ponstel)

  Nonacidic compounds
  • nabumetone (Relafen)

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Other Agents

  COX-2 Inhibitors
  • celecoxib (Celebrex)
  • rofecoxib (Vioxx)




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Drug Effects

  • Analgesic (mild to moderate)
  • Antigout
  • Antiinflammatory
  • Antipyretic
  • Relief of vascular headaches
  • Platelet inhibition (ASA)

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Therapeutic Uses
  • Relief of mild to moderate pain
  • Acute gout
  • Various bone, joint, and muscle pain
  • Osteoarthritis
  • Rheumatoid arthritis
  • Juvenile rheumatoid arthritis
  • Dysmenorrhea
  • Fever
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Specific Agents

  salicylates (aspirin)
  • More potent effect on platelet aggregation and
    thermal regulatory center in the brain
         – analgesic
         – antipyretic
         – antiinflammatory
  • Antithrombotic effect: used in the treatment of MI
    and other thromboembolic disorders

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Specific Agents

  phenylbutazone (Butazolidin)
  • Greater effects on uric acid production and
    excretion, in addition to antiinflammatory effects
  • More commonly used for treatment of gout




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Side Effects

  Gastrointestinal
  • dyspepsia, heartburn, epigastric distress, nausea
         **GI bleeding
         **mucosal lesions (erosions or ulcerations)
  • Misoprostol (Cytotec) can be used to reduce these
    dangerous effects.




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Side Effects

  Renal
  • reductions in creatinine clearance
  • acute tubular necrosis with renal failure




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Side Effects

  Cardiovascular
  • noncardiogenic pulmonary edema




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Salicylate Toxicity

  • Adults: tinnitus and hearing loss
  • Children: hyperventilation and CNS effects
  • Effects arise when serum levels exceed
    300µg/mL.
  • Metabolic acidosis and respiratory alkalosis
    may be present.



Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Nursing Implications
  • Before beginning therapy, assess for
    conditions that may be contraindications to
    therapy, especially:
         – GI lesions or peptic ulcer disease
         – Bleeding disorders

  • Assess also for conditions that require
    cautious use.
  • Perform lab studies as indicated (cardiac,
    renal, liver studies, CDC, platelet count).
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Nursing Implications
  • Perform a medication history to assess for
    potential drug interactions.
  • Several serious drug interactions exist:
         – alcohol
         – heparin
         – phenytoin
         – oral anticoagulants
         – steroids
         – sulfonamides
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Nursing Implications

  • Salicylates are NOT to be given to children
    under age 12 because of the risk of Reye’s
    syndrome.
  • Because these agents generally cause GI
    distress, they are often better tolerated if
    taken with food, milk or an antacid to avoid
    GI irritation.
  • Explain to patients that therapeutic effects
    may not be seen for 3 to 4 weeks.
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Nursing Implications

  • Educate patients about the various side
    effects of NSAIDs, and to notify their
    physician if these effects become severe
    or if bleeding or GI pain occur.
  • Patients should watch closely for the
    occurrence of any unusual bleeding,
    such as in the stool.
  • Enteric-coated tablets should not be
    crushed or chewed.
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
NSAIDs: Nursing Implications

  • Monitor for therapeutic effects, which vary
    according to the condition being treated:

             decrease in swelling, pain, stiffness,
             and tenderness of a joint or muscle area




Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

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Anti-inflammatory agents and nsaids

  • 1. Antiinflammatory Agents and Nonsteroidal Antiinflammatory Drugs (NSAIDs) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 2. NSAIDs • Large and chemically diverse group of drugs with the following properties: – Analgesic – Antiinflammatory – Antipyretic Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 3. NSAIDs: Mechanism of Action • Activation of the arachidonic acid pathway causes: • pain • headache • fever • inflammation Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 4. Instructors may wish to use EIC Image #107: Arachidonic Acid Pathway Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 5. NSAIDs: Mechanism of Action Analgesia—treatment of headaches and pain • Block the undesirable effects of prostaglandins, which cause headaches Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 6. NSAIDs: Mechanism of Action Antipyretic: reduce fever • Inhibit prostaglandin E2 within the area of the brain that controls temperature Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 7. NSAIDs: Mechanism of Action Relief of inflammation • Inhibit the leukotriene pathway, the prostaglandin pathway, or both Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 8. NSAIDs Six structurally related groups: • Acetic acids • Carboxylic acids • Propionic acids • Enolic acids • Fenamic acids • Nonacidic compounds Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 9. NSAIDs: Acetic Acid • diclofenac sodium (Voltaren) • diclofenac potassium (Cataflam) • etodolac (Lodine) • indomethacin (Indocin) • sulindac (Clinoril) • tolmetin (Tolectin) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 10. NSAIDs: Carboxylic Acids Acetylated • aspirin (ASA) • choline magnesium salicylate (Trilisate) • diflunisal (Dolobid) Nonacetylated • salicylamide • salsalate (Disalcid) • sodium salicylate Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 11. NSAIDs: Propionic Acids • fenoprofen (Nalfon) • flurbiprofen (Ansaid) • ibuprofen (Motrin, others) • ketoprofen (Orudis) • ketorolac (Toradol) • naproxen (Naprosyn) • oxaprozin (Daypro) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 12. NSAIDs: Other Agents Enolic acids • phenylbutazone (Butazolidin) • piroxicam (Feldene) Fenamic acids • meclofenamic acid (Meclomen) • mefenamic acid (Ponstel) Nonacidic compounds • nabumetone (Relafen) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 13. NSAIDs: Other Agents COX-2 Inhibitors • celecoxib (Celebrex) • rofecoxib (Vioxx) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 14. NSAIDs: Drug Effects • Analgesic (mild to moderate) • Antigout • Antiinflammatory • Antipyretic • Relief of vascular headaches • Platelet inhibition (ASA) Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 15. NSAIDs: Therapeutic Uses • Relief of mild to moderate pain • Acute gout • Various bone, joint, and muscle pain • Osteoarthritis • Rheumatoid arthritis • Juvenile rheumatoid arthritis • Dysmenorrhea • Fever Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 16. NSAIDs: Specific Agents salicylates (aspirin) • More potent effect on platelet aggregation and thermal regulatory center in the brain – analgesic – antipyretic – antiinflammatory • Antithrombotic effect: used in the treatment of MI and other thromboembolic disorders Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 17. NSAIDs: Specific Agents phenylbutazone (Butazolidin) • Greater effects on uric acid production and excretion, in addition to antiinflammatory effects • More commonly used for treatment of gout Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 18. NSAIDs: Side Effects Gastrointestinal • dyspepsia, heartburn, epigastric distress, nausea **GI bleeding **mucosal lesions (erosions or ulcerations) • Misoprostol (Cytotec) can be used to reduce these dangerous effects. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 19. NSAIDs: Side Effects Renal • reductions in creatinine clearance • acute tubular necrosis with renal failure Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 20. NSAIDs: Side Effects Cardiovascular • noncardiogenic pulmonary edema Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 21. NSAIDs: Salicylate Toxicity • Adults: tinnitus and hearing loss • Children: hyperventilation and CNS effects • Effects arise when serum levels exceed 300µg/mL. • Metabolic acidosis and respiratory alkalosis may be present. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 22. NSAIDs: Nursing Implications • Before beginning therapy, assess for conditions that may be contraindications to therapy, especially: – GI lesions or peptic ulcer disease – Bleeding disorders • Assess also for conditions that require cautious use. • Perform lab studies as indicated (cardiac, renal, liver studies, CDC, platelet count). Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 23. NSAIDs: Nursing Implications • Perform a medication history to assess for potential drug interactions. • Several serious drug interactions exist: – alcohol – heparin – phenytoin – oral anticoagulants – steroids – sulfonamides Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 24. NSAIDs: Nursing Implications • Salicylates are NOT to be given to children under age 12 because of the risk of Reye’s syndrome. • Because these agents generally cause GI distress, they are often better tolerated if taken with food, milk or an antacid to avoid GI irritation. • Explain to patients that therapeutic effects may not be seen for 3 to 4 weeks. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 25. NSAIDs: Nursing Implications • Educate patients about the various side effects of NSAIDs, and to notify their physician if these effects become severe or if bleeding or GI pain occur. • Patients should watch closely for the occurrence of any unusual bleeding, such as in the stool. • Enteric-coated tablets should not be crushed or chewed. Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
  • 26. NSAIDs: Nursing Implications • Monitor for therapeutic effects, which vary according to the condition being treated: decrease in swelling, pain, stiffness, and tenderness of a joint or muscle area Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.