Drugs of Inflammation Flashcards
AKA Aspirin?
Acetylsalicylic acid
AKA Acetylsalicylic acid?
Aspirin
Acetylsalicylic acid class and mxn?
Salicylate; Irr acetylates COX1,2; metabolite (salicylic acid) reversibly inhibits COX1,2
Acetylsalicylic acid for?
Antiplatelet, analgesic, antipyretic, anti-inflammatory (in ascending order of amount taken); often taken as “baby aspirin” to prevent MI, CVA
Acetylsalicylic acid side effects?
GI irritation, bleeding, anemia, hepatoxicity, salicylate toxicity, nephrotoxicity in eldery/hypovolemic patients, rare hypersensitivity reaction
Diflunisal class and mxn?
Salicylate; Difluorophenyl derivative of salicylic acid, reversible inhibits COX1,2
Diflunisal for?
Osteoarthritis, MSK, pain after dental extraction, postepisiotomy pain, cancer pain with bone metastasis
Diflunisal side effects?
Fewer GI side effects and less effect on platelets than aspirin
Salicylates?
Acetylsalicylic acid and Diflunisal
AKA Tylenol?
Acetaminophen
AKA Acetaminophen?
Tylenol
Acetaminophen class and mxn?
Para-amino phenol; Reversibly inhibits COX1,2 (favors 1)
Acetaminophen for?
Analgesic, antipyretic, but weak anti-inflammatory
Acetaminophen side effects?
GI irritation (less than aspirin), renal tubular necrosis if chronically abused with other NSAIDs, hepatic necrosis with overdose
Does acetaminophen have antiplatelet effects? Why or why not?
No, possibly due to poor function in the presence of peroxides (as found in sites of inflammation)
How does acetaminophen end up at a toxic intermediate?
Mostly metabolized via conjugation, but minor pathway via P450 enzymes may lead to toxic intermediate (N-acetyl-benzoquinoneimine) – REVERSE WITH ACETYLCYSTEIN
Indomethacin class and mxn?
Indole; Reversibly inhibits COX1,2 (favors COX1)
Indomethacin for?
RA, ankylosing spondylitis, OA, gout
Indomethacin vs aspirin?
Indomethcin is 10X as potent
Indomethacin side effects?
Thrombocytopenia, aplastic anemia, severe frontal headaches, nephrotoxicity in elderly/hypovolemic – >25% stop because of toxicities
Sulindac class and mxn?
Indole; Reversibly inhibits COX1,2 (favors 1)
Indoles?
Indomethacin, Sulindac
Sulindac for?
RA, OA, gout, ankylosing spondylitis
Sulindac vs indomethacin?
Sulindac is 1/2 as potent, but with less frequent side effects