Inflammation Flashcards
What are 3 drugs that act as inhibit COX-1 and COX-2?
ASA
Diflunisal
Acetaminophen
How does ASA differ from diflunisal & Acetaminophen mechanistically?
Diflunisal & Acetaminophen reversibly inhibits COX-1 and COX-2.
ASA irreversibily acetylates COX-1 and COX-2
What are the therapeutic actions of ASA in ascending order?
Antiplatelet>analgesic>antipyretic>anti-inflammatory
What is a common side effect of aspirin
GI irritation
What are other side effects of aspirin
Nephrotoxicity - Weak acid competes with uric acid for secretion
Tinnitus - indicative of high dose
Reyes syndrome - do not treat virally infected child with ASA
What ASA side effect can be avoided by using Diflunisal & Acetaminophen?
Fewer GI side effects
Less effect on platelets than aspirin
What are the therapeutic benefits of acetaminophen?
Analgesic and antipyretic effect
Weak anti-inflammatory
Explain hepatic necrosis overdose in acetaminophen?
Acetaminophen is conjugated by P450 enzymes which may lead to toxic intermediate N-acetyl-benzoquinoneimine
What is the most potent reversible COX-1 & 2 inhibitor
Indomethacin(10x as potent as aspirin)
What is the therapeutic use of COX-1 & COX-2 inhibitor aside from acetaminophen?
Rheumatic arthritis Ankylosing spondylitis Osteoarthritis Postpartum pain Dysmenorrheal pain
What is side effects of indomethacin?
Causes thrombocytopenia
Aplastic anemia
How can the side effects of indomethacin be avoided?
Sulindac
What are the COX-1 and 2 inhibitors used to treat RA, Osteoarthritis, & ankylosing spondylitis?
Indomethacin Sulindac Ibuprofen Flurbiprofen Naproxen Oxaprozin Piroxicam Ketorolac
What are selective COX-2 inhibitor?
CeloCOXib
EtonCOXib
What are benefit of COX-2 inhibors?
Less GI toxicity
