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
Sulindac side effects?
Thrombocytopenia, aplastic anemia, severe frontal headaches, NO RENAL TOXICITY
AKA Advil?
Ibuprofen
AKA Motrin?
Ibuprofen
Advil = what other NSAID?
Motrin
AKA Ibuprofen?
Advil, Motrin
Proprionic acid derivatives?
Ibuprofen, Flurbiprofen, Naproxen, Oxaprozin
Ibuprofen class and mxn?
Proprionic acid derivative; Reversibly inhibits COX 1,2 (favors 1)
Ibuprofen for?
analgesic, antipyretic, anti-inflammatory. Rheumatic disorders, OA, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, surgeries
Ibuprofen side effects?
GI irritation, hepatotoxicity (less frequent than aspirin)
Flurbiprofen class and mxn?
Proprionic acid derivative; Reversibly inhibits COX 1,2 (favors 1)
Naproxen class and mxn?
Proprionic acid derivative; Reversibly inhibits COX 1,2 (favors 1)
Oxaprozin class and mxn?
Proprionic acid derivative; Reversibly inhibits COX 1,2 (favors 1)
Piroxicam class and mxn?
Enolic acid; Reversibly inhibits COX 1,2 (favors 1)
Ketorolac class and mxn?
Heteroaryl acetic acid; Reversibly inhibits COX 1,2 (favors 1)
Flurbiprofen for?
analgesic, antipyretic, anti-inflammatory. Rheumatic disorders, OA, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, surgeries
Naproxen for?
analgesic, antipyretic, anti-inflammatory. Rheumatic disorders, OA, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, surgeries
Oxaproxin for?
analgesic, antipyretic, anti-inflammatory. Rheumatic disorders, OA, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, surgeries
Flurbiprofen side effects?
GI irritation, hepatotoxicity (less frequent than aspirin)
Naproxen side effects?
GI irritation, hepatotoxicity (less frequent than aspirin)
Oxaprozin side effects?
GI irritation, hepatotoxicity (less frequent than aspirin)
Tell me about Naproxen half-life.
Longer half-life than most proprionic acid derivitives (13 hours vs 1-2 hours)
Tell me about Oxaprozin half-life.
Much longer half-life than most proprionic acid derivatives (50 hours vs 1-2 hours)
Piroxicam for?
Long-term tx of RA, OA, ankylosing spondylitis, acute MSK disorders, acute gout
Piroxicam side effects?
Same as aspirin
Tell me about Piroxicam half-life.
Very long half-life (45 hours) permits single daily use.
What is unique about Ketorolac administration?
Injectable (one of few NSAIDs available for this)
Ketorolac for?
Post-operative pain, inflammatory eye conditions
Ketorolac side effects?
Same as aspirin, but relatively non irritating
COX-2 inhibitors?
Celecoxib, Etoricoxib
Celecoxib class and mxn?
COX-2 inhibitor, Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)
Etoricoxib class and mxn?
COX-2 inhibitor, Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)
Celecoxib for?
Anti-inflammatory, antipyretic, analgesic
Etoricoxib for?
Anti-inflammatory, antipyretic, analgesic
Side effects of Celecoxib and Etoricoxib (COX2 inhibitors)?
Less GI toxicity than traditional NSAIDs, but concerns of thrombogenicity
Celecoxib and Etoricoxib are contraindicated in who?
Pregnant, heart problems
Can indomethacin be used in children? What is the exception?
NO! Except for PDA closure
Will COX-2 inhibitors provide antiplatelet effects?
NO