Antiinflammatory Antirheumatic Antigout Drugs

1. Antiinflammatory AntirheumaticAntigout Drugs

2. NSAIDs • Large and chemically diverse group of drugs with the following properties: • Analgesic • Antiinflammatory • Antipyretic • Antirheumatic • Mechanism of Action: • Activation of the arachidonic acid pathway causes: • Pain • Headache • Fever • Inflammation

4. NSAIDsMechanism of Action • Analgesic: relieves pain • treatment of headaches • mild to moderate pain • inflammation • Block the chemical activity of either or both COX enzymes (prostaglandin [PG] pathway) and lipoxygenase (LT pathway) • Result: limits the undesirable inflammatory effect of PGs Antipyretic: reduce fever • Inhibit prostaglandin E2 within the area of the brain that controls temperature

5. Chemical Categories of NSAIDs Seven structurally related groups • Acetic acids • Carboxylic acids (salicylates) • Acetylated and nonacetylated • Propionic acids • COX-2 inhibitors • Fenamic acids • Napthylalkanones (nonacidic) • Oxicams

6. NSAIDsAcetic Acids • diclofenac sodium (Voltaren) • diclofenac potassium (Cataflam) • indomethacin (Indocin) • sulindac (Clinoril) • tolmetin (Tolectin)

7. NSAIDsCarboxylic Acids Acetylated • aspirin (ASA), choline salicylate (Arthropan) • diflunisal (Dolobid) Nonacetylated • ketorolac (Toradol) • salsalate (Salsitab) • sodium salicylate

8. NSAIDsSalicylates • Salicylates (Aspirin) also have antiplatelet activity • Inhibit platelet aggregation • 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

9. NSAIDsSalicylate Toxicity • Adults: tinnitus and hearing loss, others • Children: hyperventilation and CNS effects • Effects arise when serum levels exceed 40 to 60 mg/dL • Metabolic acidosis and respiratory alkalosis may be present

10. NSAIDsPropionic Acids • fenoprofen (Nalfon) • flurbiprofen (Ansaid) • ibuprofen (Motrin, Advil) • ketoprofen (Orudis KT) • naproxen (Naprosyn, Aleve) • oxaprozin (Daypro)

11. NSAIDsCOX-2 Inhibitor celecoxib (Celebrex) • Little effect on platelet function • Cause fewer GI adverse effects • May pose CV risks- monitored closely by FDA • Severe skin reactions – toxic epidermal necrolysis

12. NSAIDsOther Drugs Oxicams • meloxicam (Mobic) • piroxicam (Feldene) Fenamic acids • meclofenamate • mefenamic acid (Ponstel) Napthylalkanones (Nonacidic) • nabumetone (Relafen)

13. NSAIDs Indications • Analgesia (mild to moderate) • Antigout effects • Antiinflammatory effects • Antipyretic effects • Relief of vascular headache • Platelet inhibition (aspirin) • Relief of mild to moderate pain • Acute gout • Various bone, joint, and muscle pain • Osteoarthritis • Rheumatoid arthritis • Juvenile rheumatoid arthritis • Dysmenorrhea • Fever • Many other conditions

14. NSAIDsInteractions Serious interactions can occur when given with: • Anticoagulants • Aspirin • Corticosteroids and other ulcerogenic drugs • Protein bound drugs • Others

15. NSAIDsAdverse Effects Gastrointestinal • Dyspepsia, heartburn, epigastric distress, nausea • GI bleeding* • Mucosal lesions* (erosions or ulcerations) Renal • Reductions in creatinine clearance • Acute tubular necrosis with renal failure Cardiovascular • Noncardiogenic pulmonary edema *misoprostol (Cytotec) can be used to reduce these dangerous effects

16. Antigout Drugs • Gout: condition that results from inappropriate uric acid metabolism • Underexcretion of uric acid • Overproduction of uric acid • Uric acid crystals are deposited in tissues and joints, resulting in pain

18. AntigoutDrugs allopurinol (Zyloprim) • Used to reduce production of uric acid colchicine • Reduces inflammatory response to the deposits of urate crystals in joint tissue probenecid (Benemid), sulfinpyrazone (Anturane) • Increase excretion of uric acid in the urine

19. Antirheumatoid Arthritis Drugs • Also known as disease-modifying antirheumatic drugs (DMARDs) • Slow onset of action—several weeks • May take 3 to 6 months to see full effects • Can have much more toxic adverse effects than the NSAIDs • Anti-inflammatory, antiarthritic, immunomodulating effects Drugs: Auranofin (Ridaura) Aurothioglucose (Solganal) gold sodium thiomalate (Aurolate) - weekly injection Leflunomide (Arava)

20. NSAIDsNursing 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, and liver function studies, CBC, platelet count) • Perform a medication history to assess for potential drug interactions • Several serious drug interactions exist

21. Nursing ImplicationsPatient Education • Salicylates are NOT to be given to children under age 18 because of the risk of Reye’s syndrome • Administer with food, milk, or an antacid to avoid GI upset • Therapeutic effects may not be seen for 3 to 4 weeks • Various adverse effects of NSAIDs, and to notify their physician if these effects become severe or if bleeding or GI pain occurs • Watch closely for the occurrence of any unusual bleeding – stool, urine, bruising, sclera, skin and mucous membranes • Enteric-coated tablets should not be crushed or chewed

22. 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