Exam 6 Arachidonic acid metabolites and NSAIDs Flashcards
What does activation of prostacyclin (PGI2) and thromboxanes lead to?
Platelets, vasoconstriction, clotting
What does activationg of PGE2 lead to?
Pain, fever, vasodilation, uterine contraction
What is the mechanism of action of acetylsalicylic acid (aspirin)?
covalently binds to COX1 enzymes and irreversibly inhibits them
What is the mechanism of action of celecoxib?
Selective COX2 inhibitor
What is the advantage of celecoxib over aspirin?
decreases the risk of gastric ulceration
What is the disadvantage of celecoxib?
inhibits COX2 of endothelium in coronary and cerebral circulations (COX2 also decreases vasodilation)
Why have COX-2 inhibitors been withdrawn from the market?
They increase the risk of cardiovascular thrombosis
What is the mechanism of action of acetaminophen?
Blocks COX enzymes in the central nervous but not in the periphery
T/F: acetaminophen is antiinflammatory?
False
What does acetaminophen decrease?
fever and pain (good arthritis treatment)
What can an overdose of acetaminophen cause?
Hepatotoxicity
How does apirin affect platelets?
inhibits platelet’s ability to produce thromboxane A2 for the duration of the platelet’s life
What is low dose aspirin used for?
decreases thrombosis
What do prostaglandins do?
mediate many inflammatory effects of rheumatoid arthritis
What are drugs that block cyclooxygenase?
Ibuprofen, naproxen, celebrex
What is the action of glucocorticoids
transcriptional regulators that reduce numbers of lymphocytes, eosinophils, monocytes and basophils, but increase number of polymorphonuclear leukocytes, also synthesize proteins inhibiting Phospholipase A2
How do glucocorticoids act on white blood cells?
reduce the release of arachidonic acid and cytokines (IL1 and 6, TNF)
What are examples of corticosteroids?
dexamethasone, hydrocortisone, methylprednisone, prednisone
What are the toxic side effects of corticosteroids?
Osteoporosis, immune suppression, peptic ulcers, myopathy, cataracts, fluid accumulation and hyperglycemia
Are corticosteroids considered DMARDs for rheumatoid arthritis?
No
What do fish oils get turned into in the body?
PGE3, Thromboxane A3, PGI3
What is fish oil promoted as a treatment for?
rheumatoid arthritis
What does prostaglandin E2 cause?
edema, pain, redness, warmth
What is the target in reducing inflammatory symptoms of rheumatoid arthritis?
inhibiting prostaglandin synthesis
