ch 24 anti inflammatories

Chapter 24: Anti-inflammatories

1. Inflammation Pathophysiology

  • Causes of Inflammation:

  • Trauma, surgery, extreme heat or cold, caustic chemicals, infection.

  • Protective Response:

  • Chemical mediators (prostaglandins, histamines, kinins) neutralize/destroy harmful agents causing tissue injury.

2. Inflammatory Phases

  • Vascular Phase:

  • Occurs 10-15 minutes post-injury; vasodilation and increased capillary permeability.

  • Fluid and substances move to the injured site.

  • Delayed Phase:

  • Leukocytes infiltrate inflamed tissue.

  • Cyclooxygenase (COX) Enzyme:

  • Converts arachidonic acid into prostaglandins.

  • Forms of COX:

    • COX-1: Protects stomach lining, regulates platelets.

    • COX-2: Triggers inflammation and pain.

3. Cardinal Signs of Inflammation

  • Redness

  • Swelling

  • Heat

  • Pain

  • Loss of function

4. Anti-inflammatory Agents

  • Drug Groups:

  • Nonsteroidal anti-inflammatory drugs (NSAIDs)

  • Corticosteroids

  • Disease-modifying antirheumatic drugs (DMARDs)

  • Antigout drugs

5. Actions of NSAIDs

  • Inhibit biosynthesis of prostaglandins

  • Relieve pain, reduce elevated body temperature (antipyretic)

  • Inhibit platelet aggregation

  • Mimic effects of corticosteroids by inhibiting COX enzyme

6. Types of NSAIDs

  • First-generation NSAIDs:

  • Salicylates, parachlorobenzoic acid derivatives, propionic acid derivatives, fenamates, oxicams

  • Second-generation NSAIDs:

  • Selective COX-2 inhibitors

7. Salicylates (Aspirin)

  • Actions:

  • Anti-inflammatory, antiplatelet, antipyretic effects

  • Increases PT, bleeding time, INR, and uric acid

  • Decrease cholesterol, thyroid levels and potassium

  • Toxic level:

  • Greater than 300 mcg/mL

  • Drug Interactions:

  • Increased bleeding risks with anticoagulants/other NSAIDs

  • Risk for hypoglycemia with oral antidiabetics

  • Increased gastric ulcer risk with glucocorticoids

  • Caution:

  • Avoid with other NSAIDs, last trimester of pregnancy, children with virus symptoms (Reye syndrome risk)

  • Side effects:

  • Dizziness, GI distress, bleeding, tinnitus

  • Assessment/Interventions:

  • Monitor salicylate levels, bleeding, avoid alcohol/warfarin, can not be taken a week within of surgery

8. Non-Salicylate NSAIDs

  • Indomethecin (Parachlorobenzoic acid derivatives):

  • Decreases prostaglandin synthesis; used for arthritis

  • Side effects: headache, GI distress, sodium/water retention, n/v

  • Ibuprofen/Naproxen (Propionic acid derivatives):

  • Most widely used; inhibits COX-1 and COX-2 for arthritis and pain

  • Side effects: dizziness, GI distress, increased bleeding risk, insomnia

  • must observe for bleeding gums/black stools. GI distress and peripheral edema, no alcohol

  • Drug Interactions: increased bleeding with warfarin, increased effects of phenytoin

  • Very Protein Bound

  • Fenamates (Meclofenamate):

  • For osteoarthritis/rheumatoid arthritis and pain; side effects include GI distress/bleeding, dizzines, headache, tinnitus and pruritus.

  • avoid if Hx peptic ulcer

  • Oxicams (Piroxicam):

  • Similar action as others; generally well-tolerated

9. Selective COX-2 Inhibitors

  • Celecoxib:

  • Selectively inhibits COX-2 to relieve pain/inflammation; safer GI profile

  • Side Effects:

  • Dizziness, Headache, sinusitis, GI distress, hypertension

10. Corticosteroids

  • Actions:

  • Control inflammation by suppressing inflammatory components

  • Use:

  • Arthritic flare-ups; needs to be taper off over 5-10 days

11. Disease-Modifying Antirheumatic Drugs (DMARDs)

  • Types:

  • Immunosuppressive agents, immunomodulators, antimalarials

  • Uses:

  • Treat rheumatoid arthritis, psoriatic arthritis, inflammatory bowel diseases

  • Side Effects:

  • Headaches, fever, oral ulcerations, infections, hypertension, injection site rxn

  • Immunosuppresive Agents

    • used to supress inflammatory and mainly used for rheumatoid arthritis

  • Immunomodulators

    • Anakinra and Infliximab

      • disrupt inflammatory process and delay disease progression. Used rheumatoid arthritis, ulcerative colitis, and crohn disease

      • infliximab is taken IV

  • Antimalarials

    • used for refractory rheumatoid arthritis

12. Antigout Drugs

Gout: a form of arthritis characterized by sudden and severe episodes of pain, redness, and swelling, typically affecting the big toe or other joints.

  • Colchicine:

  • Inhibits leukocyte migration; side effects include GI distress, should be taken with food

  • Contraindications: renal, cardiac, GI problems

  • Xanthine Oxidase Inhibitors (Allopurinol):

  • Reduces uric acid production/excretion; side effects include GI distress, dizziness, bradycardia and hyperglycemia

  • prevents gout attacks

  • Uricosurics (Probenecid):

  • Promotes uric acid excretion; side effects include kidney stones, GI distress, flushed skin and fever

13. Practice Questions Overview

  • Example Questions:

  • Identify medication types and administration methods for rheumatoid arthritis treatments, ibuprofen instructions, and monitoring for older adult patients taking NSAIDs.