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COX Inhibitors


What is COX? Cyclooxygenase, the enzyme that converts arachidonic acid into prostanoids: prostaglandins and related compounds
What are the useful effects of COX inhibitors? Suppress inflammation, relieve pain, and reduce fever
What is the only COX inhibitor that can protect against MI and stroke? Aspirin
What are the principal adverse effects of COX inhibitors? Gastric ulceration, bleeding, and renal impairment
What are the two forms of cyclooxygenase? COX-1 and COX-2
Where is COX-1 found? In all tissues
Where is COX-2 found? At sites of tissue injury
What are the actions of COX-2? It mediates inflammation and sensitizes receptors to painful stimuli
What are the actions of COX-1? Supports renal function, protects gastric mucosa, and promotes platelet aggregation
Which is the "bad" COX? COX-2
Which the "good" COX? COX-1
What are the 2 major groups of COX inhibitors? Drugs with antiinflammatory processes (NSAIDs) and drugs without antiinflammatory properties
What is the only COX inhibitor that lacks antiinflammatory processes? Acetaminophen
What are the 2 groups of NSAIDs? First generation and second generation
How do first generation NSAIDs act? By inhibiting COX-1 AND COX-2
What is the indication for use of first generation NSAIDs? To treat inflammatory disorders (e.g., RA), alleviate mild to moderate pain, and to suppress fever
What is the prototype first generation NSAID? Aspirin
What are salicylates associated with? Aspirin
Which NSAID is a nonreversible inhibitor of COX? Aspirin
How is aspirin absorbed after PO dosing? Rapidly and completely from the small intestine
How is aspirin excreted? By the kidneys
What is salicylism? Aspirin toxicity
When does severe salicylism occur? When plasma drug levels of aspirin exceed 400 mcg/mL
How long before surgery should aspirin use be discontinued? At least 1 week
True of False; The renal impairment caused by aspirin is reversible. True
What are signs and symptoms of salicylism? Tinnitus, sweating, headache, and dizziness
Why is aspirin use in children with chicken pox or the flu life threatening? Because it can cause Reye's syndrome
What are the signs and symptoms of Reye's syndrome? Encephalopathy and fatty liver degeneration
What effect can aspirin have on labor? It can prolong it
Does aspirin increase the risk of thrombotic events? No
True of False: Daily use of aspirin is not associated with erectile dysfunction. False
Can the use of COX inhibitors blunt the immune response to vaccines? Yes
What is the lethal dose of aspirin in an adult? 20-25 gm
What is the lethal dose of aspirin in a child? 4 gm
Describe treatment for acute salicysim. Largely supportive
What is the principal use for nonaspirin first generation NSAIDs? RA and osteoarthritis
True or False: The use of nonaspirin first generation NSAIDs increase the risk of thrombotic events? True
What is an example of a nonaspirin first generation NSAID? Ibuprofen
What are coxibs? Second generation NSAIDs
How do second generation NSAIDs act? By inhibiting COX-2
Which NSAID is considered a last-choice drug for treatment of long-term pain? Celebrex
What are the most common adverse effects of Celebrex? Dysepsia and abdominal pain
Which NSAID is contraindicated in patients with a sulfa allergy? Celebrex
How does acetaminophen act? By inhibiting COX only in the CNS; it's inhibition is minimal at peripheral sites
What can acetaminophen overdose cause? Serious liver damage
What 3 medical emergencies are associated with acetaminophen? Stevens-Johnson Syndrome, acute generalized exanthematous pustulosis, and toxic epidermal necrolysis
What are signs and symptoms of acute poisoning from acetaminophen? N/V, diarrhea, sweating, and abdominal discomfort which progress to hepatic necrosis, coma, and death
How can acute acetaminophen poisoning be treated? With Mucomyst
Created by: shrewsbury_sd



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