Chapter 44

Antiinflammatory and Antigout Drugs

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Fall 2012

NSAIDsnon-steroidal anti-inflammatory drugs

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

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NSAIDs: Mechanism of Action

Activation of the arachidonic acid pathway causes: Pain Headache Fever Inflammation

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NSAIDs: Mechanism of Action (cont’d)

Analgesia—treatment of headaches, mild to moderate pain, and inflammation Block the chemical activity of either or both

COX enzymes (prostaglandin [PG] pathway) and lipoxygenase (LT pathway)

Result in limiting the undesirable inflammatory effect of PGs

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NSAIDs: Mechanism of Action (cont’d)

Antipyretic—reduces fever Inhibits prostaglandin within the area of the

brain that controls temperature

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Chemical Categories of NSAIDs

SalicylatesAcetic acid derivativesCyclooxygenase-2 (COX-2)

inhibitorsEnolic acid derivativesPropionic acid derivatives

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NSAIDs: Salicylates

Salicylates also have antiplatelet activity Inhibit platelet aggregation Examples: aspirin, diflunisal (Dolobid),

others

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NSAIDs: Acetic Acids

indomethacin (Indocin)ketorolac (Toradol)diclofenac sodium (Voltaren)sulindac (Clinoril)tolmetin (Tolectin)etodolac (Lodine)

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NSAIDs: COX-2 Inhibitor

celecoxib (Celebrex) First and only remaining COX-2 inhibitor Indicated for osteoarthritis, rheumatoid

arthritis, acute pain symptoms, ankylosing spondylitis, and primary dysmenorrhea

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NSAIDs: Enolic Acid Derivatives

piroxicam (Feldene)meloxicam (Mobic)namumetone (Relafen)

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NSAIDs: Propionic Acids

fenoprofen (Nalfon)flurbiprofen (Ansaid)ibuprofen (Motrin, Advil, others)ketoprofen (Orudis KT)naproxen (Naprosyn, Aleve)oxaprozin (Daypro)

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NSAIDs: Indications

Analgesia (mild to moderate)Antigout effectsAntiinflammatory effectsAntipyretic effectsRelief of vascular headachePlatelet inhibition (aspirin)

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NSAIDs: Indications (cont’d)

Relief of mild to moderate painAcute goutVarious bone, joint, and muscle

painOsteoarthritisRheumatoid arthritis

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NSAIDs: Indications (cont’d)

Rheumatoid arthritis

Dysmenorrhea

Fever

Many other conditions

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Salicylates: Indications

Salicylic acid (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

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Antigout Drugs: Indications

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

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Antigout Drugs: Indications (cont’d)

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

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NSAIDs: Adverse Effects

GastrointestinalDyspepsia, heartburn, epigastric

distress, nausea GI bleeding* Mucosal lesions* (erosions or ulcerations)

* Misoprostol (Cytotec) can be used to reduce these dangerous effects.

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NSAIDs: Adverse Effects (cont’d)

RenalReductions in creatinine clearanceAcute tubular necrosis with renal

failure

CardiovascularNoncardiogenic pulmonary edema

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NSAIDs: Salicylate Toxicity

Adults: tinnitus and hearing lossChildren: hyperventilation and CNS

effectsMetabolic acidosis and respiratory

alkalosis may be present

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NSAIDs: Interactions

Serious interactions can occur when given with:AnticoagulantsAspirinCorticosteroids and other ulcerogenic drugsProtein bound drugsDiuretics and ACE InhibitorsOthers

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Herbal Products: Glucosamine and Chondroitin

Used to treat the pain of osteoarthritis Adverse effects

GI discomfort Drowsiness, headache, skin reactions

(glucosamine)

Drug interactions Enhance effects of warfarin May increase insulin resistance

(glucosamine)

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NSAIDs: Nursing ImplicationsBefore beginning therapy, assess for

conditions that may be contraindications to therapy, especially: GI lesions or peptic ulcer disease Bleeding disorders

Assess for conditions that require cautious usePerform lab studies as indicated (cardiac,

renal, and liver function studies, CBC, platelet count)

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Nursing Implications

Do NOT give salicylates to children and teenagers because of the risk of Reye’s syndrome

Because these drugs generally cause GI distress, they are often better tolerated if taken with food, milk, or an antacid to avoid irritation

Explain to patients that therapeutic effects may not be seen for 3 to 4 weeks

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Nursing Implications (cont’d)

Educate patients about the various adverse effects of NSAIDs, and inform them to notify their physician if these effects become severe or if bleeding or GI pain occurs

Inform patients to watch closely for the occurrence of any unusual bleeding, such as in the stool

Advise patients that enteric-coated tablets should not be crushed or chewed

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Nursing Implications (cont’d)

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

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