Non-selective NSAIDS Flashcards
Acetylsalicylic acid
Class: Salicylate
Mech: Acetyl-salicylic acid irreversibly acetylates COX 1 and 2; metabolite (salicylic acid) reversibly inhibits COX 1 and 2
Thera: Antiplatelet, analgesic, antipyretic, anti-inflammatory, (in ascending order of amount taken)
Often taken as a baby aspirin to prevent MI, CVA
Tox: GI irriation, bleeding and anemia, hepatotoxicity, and salicylate toxicity
Nephrotoxicity in elderly or hypovolemic patients, rare hypersensitivity reaction.
Diflunisal
Class: Salicylate
Mech: Difluorophenyl derivative of salicyclic acid, which reversibly inhibits COX 1 and 2
Thera: Osteoarthritis, musculoskeletal strains/sprains, pain after dental extraction, and postepisiotomy pain
Tox: Fewer GI side effects and less effect on platelets than aspirin
Acetaminophen
Class: Para-amino phenol
Mech: Reversibly inhibits COX1 and COX2 (favors COX1)
Thera: Analgesic and antipyretic effect similar to aspirin but has weak anti-inflammatory effects
Tox: Renal tubular necrosis if chronically abused with other NSAIDs Hepatic necrosis with overdose GI irritation (althought less than aspirin)
Misc: Poor function in presence of peroxides (as found in sites of inflammation)
Mostly metabolized via conjugation but minor pathway via P450 enzymes which may lead to toxic intermediate (N-acetyl-benzoquinoeimine)
Indomethacin
Class: Indole
Mech: Reversibly inhibits COX1 and COX2 (favors COX1)
Thera: RA (10x as potent as aspirin), ankylosing spondylitis, osteoarthritis, acute gout
Tox: At times thrombocytopenia, aplastic anemia, and severe frontal headaches
Nephrotoxicity in the elderly or hypovolemic patients
Sulindac
Class: Indole
Mech: Reversibly inhibits COX1 and COX2 (favors COX1)
Thera: RA, ankylosing spondylitis, osteoarthritis, acute gout
Tox: At times thrombocytopenia, aplastic anemia, and severe frontal headaches
Nephrotoxicity in the elderly or hypovolemic patients
Misc: Half as potent as indomethacin; side effects less frequent
Ibuprofen
Class: Proprionic acid
Mech: Reversibly inhibits COX1 and COX2 preferably COX1
Thera: Rheumatic disorders, osteoarthritis, ankylosing spondylitis, post-partum pain, dysmenorrheal pain, and many types of surgery
Tox: GI irritation, hepatotoxicity (less frequent than aspirin)
Flurbiprofen
Class: Proprionic acid
Mech: Reversibly inhibits COX1 and COX2 preferably COX1
Thera: Rheumatic disorders, osteoarthritis, ankylosing spondylitis, post-partum pain, dysmenorrheal pain, and many types of surgery
Tox: GI irritation, hepatotoxicity (less frequent than aspirin)
Naproxen
Class: Proprionic acid
Mech: Reversibly inhibits COX1 and COX2 preferably COX1
Thera: Rheumatic disorders, osteoarthritis, ankylosing spondylitis, post-partum pain, dysmenorrheal pain, and many types of surgery
Tox: GI irritation, hepatotoxicity (less frequent than aspirin)
Misc: Longer half-life than most proprionic acid derivatives (13 hours vs. 1-2 hours)
Oxaprozin
Class: Proprionic acid
Mech: Reversibly inhibits COX1 and COX2 preferably COX1
Thera: Rheumatic disorders, osteoarthritis, ankylosing spondylitis, post-partum pain, dysmenorrheal pain, and many types of surgery
Tox: GI irritation, hepatotoxicity (less frequent than aspirin)
Misc: Longer half-life than most proprionic acid derivatives (13 hours vs. 1-2 hours)
Piroxicam
Class: Enolic acid
Mech: Reversibly inhibits COX-1 and 2 (favors 1)
Thera: Long-term treatment of RA or osteoarthritis; also ankyloid spondylitis, acute musculoskeletal disorders, acute gout
Tox: Same as aspirin
Misc: Very long half-life (45 hours) permits single daily dose
Ketorolac
Class: Heteroaryl acetic acids
Mech: Reversibly inhibits COX 1 and 2 but preferably 1
Thera: Post-op pain, inflammatory eye conditions
Tox: Same as aspirins; relatively non-irritating
Misc: Injectable (one of few NSAIDs available for this)
