252 Pharmacology - NSAIDS and Antigout Flashcards
Done nomogram
A standard plot of graphic data, originally published in 1960 in the journal Pediatrics, for rating the severity of aspirin toxicity following overdose; serum salicylate levels are plotted against time elapsed since ingestion.
Gout
Hyperuricemia (elevated blood uric acid level); the arthritis caused by tissue buildup of uric acid crystals.
Inflammation
A localized protective response stimulated by injury to tissues that serves to destroy, dilute, or wall off (sequester) both the injurious agent and the injured tissue.
Salicylism
The syndrome of salicylate toxicity, including symptoms such as tinnitus, nausea, and vomiting.
Define NSAID.
- A large and chemically diverse group of drugs that have:
- Analgesic activities
- Anti-inflammatory activities
- Antipyretic activities
- aspirin-platelet inhibition
What are the main uses of NSAIDs?
- Relief of mild to moderate headaches
- Relief of myalgia
- Relief of neuralgia
- Relief of arthralgia
- Relief of postoperative pain
- Relief of pain associated with arthritic disorders such as rheumatoid arthritis, juvenile arthritis, ankylosing spondylitis, and osteoarthritis
- Treatment of gout and hyperuricemia
What three properties do all NSAIDs share?
- Antipyretic properties
- Analgesic properties
- Anti-inflammatory properties
What are 3 acetic acid derivatives?
- diclofenac sodium (Voltaren®)
- indomethacin sulindac
- ketorolac (Toradol®)
What are 2 propionic acid derivatives?
ibuprofen
naproxen
Indications re: MI for aspirin.
- Shown to reduce cardiac death after myocardial infarction (MI)
- Should be administered at the first sign of MI
- If aspirin is not given before the patient arrives at the emergency department, it is one of the first drugs given if there are no contraindications.
Mechanisms of action associated with NSAIDs
- Inhibition of the leukotriene pathway, the prostaglandin pathway, or both
- Blocking the chemical activity of the enzyme COX
What are contraindications of NSAIDS?
- Conditions that place the patient at risk for bleeding
- Rhinitis
- Vitamin K deficiency
- Peptic ulcer disease
What are the main adverse effects of NSAIDS?
- Heartburn to severe GI bleeding
- Acute kidney injury
- Noncardiogenic pulmonary edema
- Altered hemostasis
- Hepatotoxicity
- Skin eruption, sensitivity reaction
- Tinnitus, hearing loss
Why is misoprostol used with NSAIDs?
- Many of the adverse effects of NSAIDs are secondary to their inactivation of protective prostaglandins that help maintain the normal integrity of the stomach lining.
- Prevents GI bleed
- A synthetic prostaglandin E1 analogue: inhibits gastric acid secretion and has a cytoprotective component
What effect can NSAIDS have on kidneys?
- Kidney function depends partly on prostaglandins.
- Disruption of prostaglandin function by NSAIDs is sometimes strong enough to precipitate acute or chronic kidney injury or failure.
- Use of NSAIDs can compromise existing kidney function.
- Kidney toxicity can occur in patients with dehydration, heart failure, or liver dysfunction, or with the use of diuretics or angiotensin-converting enzyme inhibitors.
What is the Health Canada warning regarding NSAIDs?
- All NSAIDs (except aspirin) share a Health Canada warning regarding an increased risk of adverse cardiovascular thrombotic events, including fatal MI and stroke.
- NSAIDs cause an increased risk of serious GI adverse events
- Older adults are at greater risk.
Uses for aspirin
- Inhibits platelet aggregation
- Antithrombotic effect: used in the treatment of MI and other thromboembolic disorders
- Headache, neuralgia, myalgia, and arthralgia
- Pain syndromes resulting from inflammation: arthritis, pleurisy, and pericarditis
- Systemic lupus erythematosus: antirheumatic effects
- Antipyretic action
What is salicylate intoxication?
- Salicylate intoxication (when chronic, known as salicylism)
- Increased heart rate
- Tinnitus, hearing loss, dimness of vision, headache, dizziness, mental confusion, drowsiness
- Nausea, vomiting, diarrhea
- Sweating, thirst, hyperventilation, hypoglycemia or hyperglycemia
What are the uses for the acetic acid derivative indomethacin?
Uses: therapy for rheumatoid arthritis (RA), osteoarthritis (OA), acute bursitis or tendonitis, ankylosing spondylitis, acute gouty arthritis
(Analgesic, anti-inflammatory, antirheumatic, and antipyretic properties)
What are the uses for the acetic acid derivative ketorolac?
- Some anti-inflammatory activity
- Used primarily for its powerful analgesic effects, which are comparable to those of narcotic drugs such as morphine sulphate
- Indication: short-term use (up to 5 to 7 days) to manage moderate to severe acute pain
What is the most commonly used NSAID?
ibuprofen
What is the second most commonly used NSAID?
naproxen
Why might naproxen be a better choice than ibuprofen?
- Somewhat better adverse effect profile than ibuprofen
- Fewer drug interactions with angiotensin-converting enzyme inhibitors given for hypertension
With what kind of allergy is celecoxib contraindicated?
sulpha allergy
