Drugs of Inflammation Flashcards

1
Q

AKA Aspirin?

A

Acetylsalicylic acid

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2
Q

AKA Acetylsalicylic acid?

A

Aspirin

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3
Q

Acetylsalicylic acid class and mxn?

A

Salicylate; Irr acetylates COX1,2; metabolite (salicylic acid) reversibly inhibits COX1,2

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4
Q

Acetylsalicylic acid for?

A

Antiplatelet, analgesic, antipyretic, anti-inflammatory (in ascending order of amount taken); often taken as “baby aspirin” to prevent MI, CVA

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5
Q

Acetylsalicylic acid side effects?

A

GI irritation, bleeding, anemia, hepatoxicity, salicylate toxicity, nephrotoxicity in eldery/hypovolemic patients, rare hypersensitivity reaction

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6
Q

Diflunisal class and mxn?

A

Salicylate; Difluorophenyl derivative of salicylic acid, reversible inhibits COX1,2

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7
Q

Diflunisal for?

A

Osteoarthritis, MSK, pain after dental extraction, postepisiotomy pain, cancer pain with bone metastasis

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8
Q

Diflunisal side effects?

A

Fewer GI side effects and less effect on platelets than aspirin

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9
Q

Salicylates?

A

Acetylsalicylic acid and Diflunisal

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10
Q

AKA Tylenol?

A

Acetaminophen

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11
Q

AKA Acetaminophen?

A

Tylenol

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12
Q

Acetaminophen class and mxn?

A

Para-amino phenol; Reversibly inhibits COX1,2 (favors 1)

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13
Q

Acetaminophen for?

A

Analgesic, antipyretic, but weak anti-inflammatory

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14
Q

Acetaminophen side effects?

A

GI irritation (less than aspirin), renal tubular necrosis if chronically abused with other NSAIDs, hepatic necrosis with overdose

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15
Q

Does acetaminophen have antiplatelet effects? Why or why not?

A

No, possibly due to poor function in the presence of peroxides (as found in sites of inflammation)

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16
Q

How does acetaminophen end up at a toxic intermediate?

A

Mostly metabolized via conjugation, but minor pathway via P450 enzymes may lead to toxic intermediate (N-acetyl-benzoquinoneimine) – REVERSE WITH ACETYLCYSTEIN

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17
Q

Indomethacin class and mxn?

A

Indole; Reversibly inhibits COX1,2 (favors COX1)

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18
Q

Indomethacin for?

A

RA, ankylosing spondylitis, OA, gout

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19
Q

Indomethacin vs aspirin?

A

Indomethcin is 10X as potent

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20
Q

Indomethacin side effects?

A

Thrombocytopenia, aplastic anemia, severe frontal headaches, nephrotoxicity in elderly/hypovolemic – >25% stop because of toxicities

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21
Q

Sulindac class and mxn?

A

Indole; Reversibly inhibits COX1,2 (favors 1)

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22
Q

Indoles?

A

Indomethacin, Sulindac

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23
Q

Sulindac for?

A

RA, OA, gout, ankylosing spondylitis

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24
Q

Sulindac vs indomethacin?

A

Sulindac is 1/2 as potent, but with less frequent side effects

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25
Q

Sulindac side effects?

A

Thrombocytopenia, aplastic anemia, severe frontal headaches, NO RENAL TOXICITY

26
Q

AKA Advil?

A

Ibuprofen

27
Q

AKA Motrin?

A

Ibuprofen

28
Q

Advil = what other NSAID?

A

Motrin

29
Q

AKA Ibuprofen?

A

Advil, Motrin

30
Q

Proprionic acid derivatives?

A

Ibuprofen, Flurbiprofen, Naproxen, Oxaprozin

31
Q

Ibuprofen class and mxn?

A

Proprionic acid derivative; Reversibly inhibits COX 1,2 (favors 1)

32
Q

Ibuprofen for?

A

analgesic, antipyretic, anti-inflammatory. Rheumatic disorders, OA, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, surgeries

33
Q

Ibuprofen side effects?

A

GI irritation, hepatotoxicity (less frequent than aspirin)

34
Q

Flurbiprofen class and mxn?

A

Proprionic acid derivative; Reversibly inhibits COX 1,2 (favors 1)

35
Q

Naproxen class and mxn?

A

Proprionic acid derivative; Reversibly inhibits COX 1,2 (favors 1)

36
Q

Oxaprozin class and mxn?

A

Proprionic acid derivative; Reversibly inhibits COX 1,2 (favors 1)

37
Q

Piroxicam class and mxn?

A

Enolic acid; Reversibly inhibits COX 1,2 (favors 1)

38
Q

Ketorolac class and mxn?

A

Heteroaryl acetic acid; Reversibly inhibits COX 1,2 (favors 1)

39
Q

Flurbiprofen for?

A

analgesic, antipyretic, anti-inflammatory. Rheumatic disorders, OA, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, surgeries

40
Q

Naproxen for?

A

analgesic, antipyretic, anti-inflammatory. Rheumatic disorders, OA, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, surgeries

41
Q

Oxaproxin for?

A

analgesic, antipyretic, anti-inflammatory. Rheumatic disorders, OA, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, surgeries

42
Q

Flurbiprofen side effects?

A

GI irritation, hepatotoxicity (less frequent than aspirin)

43
Q

Naproxen side effects?

A

GI irritation, hepatotoxicity (less frequent than aspirin)

44
Q

Oxaprozin side effects?

A

GI irritation, hepatotoxicity (less frequent than aspirin)

45
Q

Tell me about Naproxen half-life.

A

Longer half-life than most proprionic acid derivitives (13 hours vs 1-2 hours)

46
Q

Tell me about Oxaprozin half-life.

A

Much longer half-life than most proprionic acid derivatives (50 hours vs 1-2 hours)

47
Q

Piroxicam for?

A

Long-term tx of RA, OA, ankylosing spondylitis, acute MSK disorders, acute gout

48
Q

Piroxicam side effects?

A

Same as aspirin

49
Q

Tell me about Piroxicam half-life.

A

Very long half-life (45 hours) permits single daily use.

50
Q

What is unique about Ketorolac administration?

A

Injectable (one of few NSAIDs available for this)

51
Q

Ketorolac for?

A

Post-operative pain, inflammatory eye conditions

52
Q

Ketorolac side effects?

A

Same as aspirin, but relatively non irritating

53
Q

COX-2 inhibitors?

A

Celecoxib, Etoricoxib

54
Q

Celecoxib class and mxn?

A

COX-2 inhibitor, Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)

55
Q

Etoricoxib class and mxn?

A

COX-2 inhibitor, Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)

56
Q

Celecoxib for?

A

Anti-inflammatory, antipyretic, analgesic

57
Q

Etoricoxib for?

A

Anti-inflammatory, antipyretic, analgesic

58
Q

Side effects of Celecoxib and Etoricoxib (COX2 inhibitors)?

A

Less GI toxicity than traditional NSAIDs, but concerns of thrombogenicity

59
Q

Celecoxib and Etoricoxib are contraindicated in who?

A

Pregnant, heart problems

60
Q

Can indomethacin be used in children? What is the exception?

A

NO! Except for PDA closure

61
Q

Will COX-2 inhibitors provide antiplatelet effects?

A

NO