Podcast
Questions and Answers
What is the primary function of inflammation in the body?
What is the primary function of inflammation in the body?
Which of the following is a common use of NSAIDs?
Which of the following is a common use of NSAIDs?
What is the mechanism of action of NSAIDs?
What is the mechanism of action of NSAIDs?
Which NSAID is an irreversible inhibitor of COX-1 receptors within the platelets themselves?
Which NSAID is an irreversible inhibitor of COX-1 receptors within the platelets themselves?
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What is a potential adverse effect of NSAIDs on the gastrointestinal system?
What is a potential adverse effect of NSAIDs on the gastrointestinal system?
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What is a potential interaction of NSAIDs with other medications?
What is a potential interaction of NSAIDs with other medications?
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What is the role of prostaglandins in renal function?
What is the role of prostaglandins in renal function?
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What is a common symptom of inflammation?
What is a common symptom of inflammation?
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What is the anti-inflammatory effect of NSAIDs due to?
What is the anti-inflammatory effect of NSAIDs due to?
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What is a potential adverse effect of NSAIDs on the cardiovascular system?
What is a potential adverse effect of NSAIDs on the cardiovascular system?
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Which of the following is a contraindication for aspirin administration?
Which of the following is a contraindication for aspirin administration?
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Which of the following NSAIDs is used to prevent GI bleeding?
Which of the following NSAIDs is used to prevent GI bleeding?
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What is the primary indication for the use of ketorolac?
What is the primary indication for the use of ketorolac?
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Which of the following is a common adverse effect of NSAIDs?
Which of the following is a common adverse effect of NSAIDs?
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What is the mechanism of action of misoprostol?
What is the mechanism of action of misoprostol?
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Which of the following NSAIDs has a black box warning regarding an increased risk of adverse cardiovascular thrombotic events?
Which of the following NSAIDs has a black box warning regarding an increased risk of adverse cardiovascular thrombotic events?
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What is a common complication of Reye's syndrome?
What is a common complication of Reye's syndrome?
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Which of the following is a characteristic of COX-2 inhibitors?
Which of the following is a characteristic of COX-2 inhibitors?
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What is the primary indication for the use of celecoxib?
What is the primary indication for the use of celecoxib?
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What is the primary mechanism of action of diclofenac sodium?
What is the primary mechanism of action of diclofenac sodium?
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What is the primary mechanism of action of probenecid in the treatment of gout?
What is the primary mechanism of action of probenecid in the treatment of gout?
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Which of the following NSAIDs is better tolerated gastrointestinally than some other NSAIDs?
Which of the following NSAIDs is better tolerated gastrointestinally than some other NSAIDs?
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What is the primary therapeutic effect of colchicine in the treatment of gout?
What is the primary therapeutic effect of colchicine in the treatment of gout?
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Which of the following is a common adverse effect of NSAIDs that patients should be educated about?
Which of the following is a common adverse effect of NSAIDs that patients should be educated about?
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What is the contraindication for giving salicylates to children and teenagers?
What is the contraindication for giving salicylates to children and teenagers?
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Which of the following is a nursing implication for patients taking NSAIDs or antigout drugs?
Which of the following is a nursing implication for patients taking NSAIDs or antigout drugs?
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What is the mechanism of action of lesinurad in the treatment of gout?
What is the mechanism of action of lesinurad in the treatment of gout?
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What is the primary therapeutic effect of allopurinol in the treatment of gout?
What is the primary therapeutic effect of allopurinol in the treatment of gout?
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Which of the following NSAIDs is the most commonly used?
Which of the following NSAIDs is the most commonly used?
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What is the primary therapeutic effect of febuxostat in the treatment of gout?
What is the primary therapeutic effect of febuxostat in the treatment of gout?
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Study Notes
Inflammation
- Inflammation is a localized protective response to tissue injury, which aims to destroy, dilute, or wall off the injurious agent and injured tissue.
- Symptoms of inflammation include pain, fever, loss of function, redness, and swelling.
- Endogenous compounds involved in inflammation include proteins of the complement system, histamine, serotonin, bradykinin, leukotrienes, and prostaglandins.
Nonsteroidal Anti-inflammatory Drugs (NSAIDs)
- NSAIDs are a large and chemically diverse group of drugs with analgesic, anti-inflammatory, antipyretic, and aspirin-platelet inhibition properties.
- Common uses of NSAIDs include:
- Mild to moderate headaches
- Myalgia
- Neuralgia
- Arthralgia
- Postoperative pain
- Pain associated with arthritic disorders (e.g., rheumatoid arthritis, osteoarthritis)
- Gout and hyperuricemia
- All NSAIDs share antipyretic, analgesic, and anti-inflammatory properties.
Salicylates
- Examples of salicylates include aspirin, diflunisal (Dolobid), and others.
- Aspirin is an irreversible inhibitor of COX-1 receptors and reduces thromboxane A2 formation, promoting platelet aggregation.
- Other NSAIDs lack this antiplatelet effect.
Mechanism of Action of NSAIDs
- NSAIDs inhibit the leukotriene pathway, prostaglandin pathway, or both.
- Blocking the chemical activity of the enzyme COX, which has two isoforms:
- COX-1: involved in maintaining the gastrointestinal (GI) mucosa
- COX-2: involved in inflammation
Adverse Effects of NSAIDs
- Gastrointestinal: heartburn to severe GI bleeding
- Renal: acute renal failure
- Cardiovascular: increased risk of myocardial infarction (MI) and stroke
- Hematological: altered hemostasis
- Hepatic: hepatotoxicity
- Dermatological: skin eruption, sensitivity reaction
- Otological: tinnitus, hearing loss
Interactions of NSAIDs
- Serious interactions can occur with:
- Anticoagulants
- Aspirin
- Corticosteroids and other ulcerogenic drugs
- Protein-bound drugs
- Diuretics and ACE inhibitors
- Others
Renal Function and NSAIDs
- Renal function depends partly on prostaglandins, which can be disrupted by NSAIDs, leading to acute or chronic renal failure.
- NSAIDs can compromise existing renal function, especially in patients with dehydration, heart failure, liver dysfunction, or those taking diuretics or ACE inhibitors.
Black Box Warning for NSAIDs
- All NSAIDs (except aspirin) carry a black box warning regarding the increased risk of adverse cardiovascular thrombotic events, including fatal MI and stroke.
- NSAIDs may counteract the cardioprotective effects of aspirin.
Salicylate Toxicity
- Cardiovascular: increased heart rate
- Central nervous system: tinnitus, hearing loss, dimness of vision, headache, dizziness, mental confusion, lassitude, and drowsiness
- Gastrointestinal: nausea, vomiting, diarrhea
- Metabolic: sweating, thirst, hyperventilation, hypoglycemia, or hyperglycemia
Aspirin
- Uses:
- Reduce cardiac death after myocardial infarction (MI)
- Should be administered at the first sign of MI
- Contraindications:
- Known drug allergy
- Conditions that place the patient at risk of bleeding (e.g., vitamin K deficiency, peptic ulcer disease)
- Reye's syndrome: an acute and potentially life-threatening condition involving progressive neurologic deficits, triggered by viral illnesses and salicylate therapy.
Misoprostol (Cytotec)
- Prevents GI bleeding by:
- Inhibiting gastric acid secretion
- Having a cytoprotective component
- Mechanism of action: unclear
Acetic Acid Derivatives
- Examples: diclofenac sodium (Voltaren), indomethacin (Indocin), sulindac (Clinoril), tolmetin (Tolectin), etodolac (Lodine), ketorolac (Toradol)
- Uses:
- Rheumatoid arthritis (RA)
- Osteoarthritis (OA)
- Acute bursitis or tendonitis
- Ankylosing spondylitis
- Acute gouty arthritis
- Patent ductus arteriosus (PDA)
- Treatment of preterm labor
- Adverse effects:
- Renal impairment
- Edema
- GI pain
- Dyspepsia
- Nausea
Cyclooxygenase-2 (COX-2) Inhibitors
- Example: celecoxib (Celebrex)
- Indicated for:
- OA
- RA
- Acute pain symptoms
- Ankylosing spondylitis
- Primary dysmenorrhea
- Adverse effects:
- Headache
- Sinus irritation
- Diarrhea
- Fatigue
- Dizziness
- Lower extremity edema
- Hypertension
- Little effect on platelet function
- Contraindication: known sulfa allergy
Enolic Acid Derivatives
- Examples: nabumetone (Relafen), meloxicam (Mobic), piroxicam (Feldene)
- Uses:
- Mild to moderate OA
- RA
- Gouty arthritis
- Adverse effects:
- GI distress
- Renal impairment
Propionic Acid Derivatives
- Examples: fenoprofen (Nalfon), flurbiprofen (Ansaid), ibuprofen (Motrin, Advil, others)
- Uses:
- Analgesic effects in RA, OA, primary dysmenorrhea, gout, dental pain, musculoskeletal disorders
- Antipyretic actions
- Adverse effects:
- GI distress
- Renal impairment
- Headache
- Dizziness
- Nausea
Gout
- Condition resulting 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 and hyperuricemia.
Antigout Drugs
- Allopurinol (Zyloprim):
- Used to prevent uric acid production and prevent acute tumor lysis syndrome
- Adverse effects: exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis
- Febuxostat (Uloric):
- Nonpurine selective inhibitor of xanthine oxidase
- May pose a greater risk of cardiovascular events than allopurinol
- Colchicine (Colcrys):
- Reduces inflammatory response to the deposits of urate crystals in joint tissue
- Used for short-term management or prevention of gout
- Adverse effects: short-term leukopenia and bleeding into the GI or urinary tracts
- Probenecid (Benemid):
- Inhibits the reabsorption of uric acid in the kidneys and thus increases the excretion of uric acid
- Uricosuric
- Must have good renal function
- Lesinurad (Zurampic):
- Uric acid transporter inhibitors
- Inhibits the transporter proteins involved in renal uric acid reabsorption resulting in lower serum uric acid levels and increased renal clearance of uric acid
- Given in combination with xanthine oxidase inhibitor
- Teaching: at least 2 liters of fluid a day
Nursing Implications
- Assess for conditions that may be contraindications to therapy, especially GI lesions or peptic ulcer disease, bleeding disorders, and sulfa allergy.
- Perform laboratory studies as indicated (cardiac, renal, and liver function studies; complete blood count; platelet count).
- Perform a medication history to assess for potential drug interactions.
- Educate patients about the various adverse effects of NSAIDs and inform them to notify their prescribers 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.
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Description
Learn about the localized protective response of inflammation, its characteristics, and the properties of Nonsteroidal Anti-inflammatory Drugs (NSAIDs).