Anti-Inflammatory Drugs Flashcards
The anti-inflammatories all target what 2 enzymes, which metabolize arachidonic acid?
COX-1 and COX-2
Of the 2 cyclooxygenases, which one is constitutively expressed, which one is induced, and which one can be selectively inhibited?
COX-1 is constitutive, COX-2 is induced and there are COX-2 specific inhibitors
Name the 2 salicylates. Which one causes less GI and platelet inhibiting side effects?
Acetylsalicylic acid and diflunisal; diflunisal has less side effects
Name the para-amino phenol, enolic acid, and heteroaryl acetic acid.
Acetaminophen, piroxicam, and ketorolac, respectively
Name the 4 proprionic acid derivatives.
Ibuprofen, flurbiprofen, naproxen, oxaprozin
Name the 2 COX-2 inhibitors, which are not NSAIDs.
Celocoxib and etoricoxib
Name the only anti-inflammatory drug that irreversibly inhibits COX-1 and COX-2. Also name its metabolite, which acts reversibly, and the site of metabolism.
Acetylsalicylic acid; metabolized to salicylic acid in the liver
Name the 6 groups of non-selective COX inhibitors / NSAIDs.
Salicylic acids, proprionic acids, enolic acids, heteroaryl acetic acids, indoles, and para-amino phenols
Give the 4 actions of acetylsalicylic acid, from lowest to highest dose needed for the effect to be seen.
Antiplatelet, analgesic (for pain), antipyretic (blocks pyrogen-initiated eicosanoid synthesis), and anti-inflammatory
Name the 2 indoles. Which one is more potent? Which one has more side effects?
Indomethacin and sulindac; indomethacin is more potent and has more side effects
Compared to aspirin, how good is diflunisal as an analgesic, antipyretic and anti-inflammatory agent?
Good analgesic and anti-inflammatory, but weak antipyretic
Which NSAID is particularly useful for treating musculoskeletal pain and cancer pain with bone metastases?
Diflunisal
Except for aspirin, are most anti-inflammatories reversible or irreversible, and do they bind better to COX-1 or COX-2?
Reversible, bind better to COX-1 (which is not good, we want COX-2 inhibition)
Acetaminophen has virtually no side effects at therapeutic doses, but an overdose can cause damage to what organ via the toxic intermediate N-acetyl-benzoquinoneimine?
Liver (can also cause renal toxicity and GI irritation, like all the NSAIDs)
Compared to aspirin, how good is acetaminophen as an analgesic, antipyretic, and anti-inflammatory agent?
Good analgesic and antipyretic, but poor anti-inflammatory (acetaminophen has a strong effect on the brain, but is inhibited by peroxides at inflammation sites)
Besides direct salicylate toxicity, give 4 common side effects and 2 less common side effects of taking NSAIDs (especially aspirin).
GI irritation, bleeding, anemia, and hepatotoxicity; less commonly nephrotoxicity (in elderly, hypovolemic patients, or chronic abuse) and hypersensitivity reactions
What feature of the enolic acid piroxicam makes it particularly good for treating long-term rheumatoid conditions?
It has a very long half life (45 hours)
Which NSAID is injectable, relatively non-irritating, and can also be used for inflammatory conditions of the eye?
Ketorolac
Indomethacin should not be used in children except for what therapeutic purpose?
Closure of the ductus arteriosus
Give the major and minor pathways by which acetaminophen is metabolized.
Major: conjugation (with sulfate, glucuronide, or glutathione)
Minor: P450 enzyme
Which class of anti-inflammatory drugs can cause side effects of thrombocytopenia, aplastic anemia, and severe frontal headaches?
Indoles (indomethacin and sulindac)
Rank the 4 proprionic acid derivatives in order from shortest to longest half-life
Ibuprofen and flurbiprofen (1-2h) - naproxen (13h) - oxaprozin (50h)
How do the side effects of the proprionic acid derivatives compare to that of aspirin and indomethacin?
They cause less GI irritation and hepatotoxicity than aspirin or indomethacin
How do the therapeutic effects and side effects of the COX-2 selective inhibitors compare to that of the NSAIDs?
Same analgesic, antipyretic, and anti-inflammatory effects; less GI irritation
