Anti-Inflammatory Drugs

Question 1

The anti-inflammatories all target what 2 enzymes, which metabolize arachidonic acid?

Answer 1

COX-1 and COX-2

Question 1

Of the 2 cyclooxygenases, which one is constitutively expressed, which one is induced, and which one can be selectively inhibited?

Answer 1

COX-1 is constitutive, COX-2 is induced and there are COX-2 specific inhibitors

Question 1

Name the 2 salicylates. Which one causes less GI and platelet inhibiting side effects?

Answer 1

Acetylsalicylic acid and diflunisal; diflunisal has less side effects

Question 1

Name the para-amino phenol, enolic acid, and heteroaryl acetic acid.

Answer 1

Acetaminophen, piroxicam, and ketorolac, respectively

Question 1

Name the 4 proprionic acid derivatives.

Answer 1

Ibuprofen, flurbiprofen, naproxen, oxaprozin

Question 1

Name the 2 COX-2 inhibitors, which are not NSAIDs.

Answer 1

Celocoxib and etoricoxib

Question 2

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.

Answer 2

Acetylsalicylic acid; metabolized to salicylic acid in the liver

Question 3

Name the 6 groups of non-selective COX inhibitors / NSAIDs.

Answer 3

Salicylic acids, proprionic acids, enolic acids, heteroaryl acetic acids, indoles, and para-amino phenols

Question 4

Give the 4 actions of acetylsalicylic acid, from lowest to highest dose needed for the effect to be seen.

Answer 4

Antiplatelet, analgesic (for pain), antipyretic (blocks pyrogen-initiated eicosanoid synthesis), and anti-inflammatory

Question 5

Name the 2 indoles. Which one is more potent? Which one has more side effects?

Answer 5

Indomethacin and sulindac; indomethacin is more potent and has more side effects

Question 7

Compared to aspirin, how good is diflunisal as an analgesic, antipyretic and anti-inflammatory agent?

Answer 7

Good analgesic and anti-inflammatory, but weak antipyretic

Question 8

Which NSAID is particularly useful for treating musculoskeletal pain and cancer pain with bone metastases?

Answer 8

Diflunisal

Question 9

Except for aspirin, are most anti-inflammatories reversible or irreversible, and do they bind better to COX-1 or COX-2?

Answer 9

Reversible, bind better to COX-1 (which is not good, we want COX-2 inhibition)

Question 10

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?

Answer 10

Liver (can also cause renal toxicity and GI irritation, like all the NSAIDs)

Question 11

Compared to aspirin, how good is acetaminophen as an analgesic, antipyretic, and anti-inflammatory agent?

Answer 11

Good analgesic and antipyretic, but poor anti-inflammatory (acetaminophen has a strong effect on the brain, but is inhibited by peroxides at inflammation sites)

Question 12

Besides direct salicylate toxicity, give 4 common side effects and 2 less common side effects of taking NSAIDs (especially aspirin).

Answer 12

GI irritation, bleeding, anemia, and hepatotoxicity; less commonly nephrotoxicity (in elderly, hypovolemic patients, or chronic abuse) and hypersensitivity reactions

Question 13

What feature of the enolic acid piroxicam makes it particularly good for treating long-term rheumatoid conditions?

Answer 13

It has a very long half life (45 hours)

Question 14

Which NSAID is injectable, relatively non-irritating, and can also be used for inflammatory conditions of the eye?

Answer 14

Ketorolac

Question 15

Indomethacin should not be used in children except for what therapeutic purpose?

Answer 15

Closure of the ductus arteriosus

Question 16

Give the major and minor pathways by which acetaminophen is metabolized.

Answer 16

Major: conjugation (with sulfate, glucuronide, or glutathione)
Minor: P450 enzyme

Question 17

Which class of anti-inflammatory drugs can cause side effects of thrombocytopenia, aplastic anemia, and severe frontal headaches?

Answer 17

Indoles (indomethacin and sulindac)

Question 18

Rank the 4 proprionic acid derivatives in order from shortest to longest half-life

Answer 18

Ibuprofen and flurbiprofen (1-2h) - naproxen (13h) - oxaprozin (50h)

Question 19

How do the side effects of the proprionic acid derivatives compare to that of aspirin and indomethacin?

Answer 19

They cause less GI irritation and hepatotoxicity than aspirin or indomethacin

Question 24

How do the therapeutic effects and side effects of the COX-2 selective inhibitors compare to that of the NSAIDs?

Answer 24

Same analgesic, antipyretic, and anti-inflammatory effects; less GI irritation

Question 25

Name 3 non-selective COX inhibitors that are used to treat acute gout.

Answer 25

Piroxicam, indomethacin, and sulindac

Question 26

Celocoxib and etoricoxib are contraindicated in what 2 patient populations?

Answer 26

Patients with heart problems or who are pregnant