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Pharm U2 > 8) Inflammation > Flashcards

8) Inflammation Flashcards

1
Q

What is the class for Acetylsalicylic acid (ASA, Aspirin)

A

Salicylate

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2
Q

What is the mechanism for Acetylsalicylic acid (ASA, Aspirin)

A

Acetyl-salicylic acid irreversibly acetylates COX-1 and -2; metabolite (salicylic acid) reversibly inhibits COX-1 and -2

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3
Q

What are the therapeutics for Acetylsalicylic acid (ASA, Aspirin)

A

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

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4
Q

What are the important side effects for Acetylsalicylic acid (ASA, Aspirin)

A

GI irritation, bleeding and anemia, hepatotoxicity, and salicylate toxicity

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5
Q

What are the other side effects for Acetylsalicylic acid (ASA, Aspirin)

A

Nephrotoxicity in elderly or hypovolemic patients; rare hypersensitivity reaction

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6
Q

What is the class for Diflunisal (Dolobid)

A

Salicylate

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7
Q

What is the mechanism for Diflunisal (Dolobid)

A

Difluorophenyl derivitive of salicylic acid, which reversibly inhibits COX-1 and -2

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8
Q

What are the therapeutics for Diflunisal (Dolobid)

A

Osteoarthritis, musculoskeletal strains/sprains, pain after dental extraction, and postepisiotomy pain

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9
Q

What are the important side effects for Diflunisal (Dolobid)

A

Fewer GI side effects and less effect on platelets than aspirin

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10
Q

What is the class for Acetaminophen (Tylenol)

A

Para-amino phenol

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11
Q

What is the mechanism for Acetaminophen (Tylenol)

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

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12
Q

What are the therapeutics for Acetaminophen (Tylenol)

A

Analgesic and antipyretic effect similar to aspirin, but weak anti-inflammatory effects

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13
Q

What are the important side effects for Acetaminophen (Tylenol)

A

Renal tubular necrosis if chronically abused with other NSAIDs; hepatic necrosis with overdose

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14
Q

What are the other side effects for Acetaminophen (Tylenol)

A

GI irritation (less than aspirin)

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15
Q

What are the miscellaneous for Acetaminophen (Tylenol)

A

Poor function in presence of peroxides (as found in sites of inflammation); mostly metabolized via conjugation, but minor pathway via P450 enzymes may lead to toxic intermediate (N-acetyl-benzoquinoneimine)

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16
Q

What is the class for Indomethacin (Indocin)

A

Indole

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17
Q

What is the mechanism for Indomethacin (Indocin)

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

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18
Q

What are the therapeutics for Indomethacin (Indocin)

A

Rhematoid arthritis (10X as potent as aspirin), ankylosing spondylitis, osteoarthritis, acute gout

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19
Q

What are the important side effects for Indomethacin (Indocin)

A

At times, thrombocytopenia, aplastic anemia, and severe frontal headaches

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20
Q

What are the other side effects for Indomethacin (Indocin)

A

Nephrotoxicity in elderly or hypovolemic patients

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21
Q

What is the class for Sulindac (Clinoril)

A

Indole

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22
Q

What is the mechanism for Sulindac (Clinoril)

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

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23
Q

What are the therapeutics for Sulindac (Clinoril)

A

Rhematoid arthritis, ankylosing spondylitis, osteoarthritis, acute gout

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24
Q

What are the important side effects for Sulindac (Clinoril)

A

At times, thrombocytopenia, aplastic anemia, and severe frontal headaches

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25
Q

What are the other side effects for Sulindac (Clinoril)

A

Nephrotoxicity in elderly or hypovolemic patients

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26
Q

What are the miscellaneous for Sulindac (Clinoril)

A

Half as potent as indomethacin; side effects less frequent

27
Q

What is the class for Ibuprofen (Advil, Motrin)

A

Proprionic acid dervitive

28
Q

What is the mechanism for Ibuprofen (Advil, Motrin)

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

29
Q

What are the therapeutics for Ibuprofen (Advil, Motrin)

A

Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

30
Q

What are the important side effects for Ibuprofen (Advil, Motrin)

A

GI irritation; hepatotoxicity (less frequent than aspirin)

31
Q

What is the class for Flurbiprofen (Ocufen)

A

Proprionic acid dervitive

32
Q

What is the mechanism for Flurbiprofen (Ocufen)

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

33
Q

What are the therapeutics for Flurbiprofen (Ocufen)

A

Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

34
Q

What are the important side effects for Flurbiprofen (Ocufen)

A

GI irritation; hepatotoxicity (less frequent than aspirin)

35
Q

What is the class for Naproxen (Aleve)

A

Proprionic acid dervitive

36
Q

What is the mechanism for Naproxen (Aleve)

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

37
Q

What are the therapeutics for Naproxen (Aleve)

A

Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

38
Q

What are the important side effects for Naproxen (Aleve)

A

GI irritation; hepatotoxicity (less frequent than aspirin)

39
Q

What are the miscellaneous for Naproxen (Aleve)

A

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

40
Q

What is the class for Oxaprozin (Daypro)

A

Proprionic acid dervitive

41
Q

What is the mechanism for Oxaprozin (Daypro)

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

42
Q

What are the therapeutics for Oxaprozin (Daypro)

A

Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

43
Q

What are the important side effects for Oxaprozin (Daypro)

A

GI irritation; hepatotoxicity (less frequent than aspirin)

44
Q

What are the miscellaneous for Oxaprozin (Daypro)

A

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

45
Q

What is the class for Piroxicam (Feldene)

A

Enolic acid

46
Q

What is the mechanism for Piroxicam (Feldene)

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

47
Q

What are the therapeutics for Piroxicam (Feldene)

A

Long-term treatment of rheumatoid arthritis or osteoarthritis; also, ankylosing spondylitis, acute musculoskeletal disorders, acute gout

48
Q

What are the other side effects for Piroxicam (Feldene)

A

Same as aspirin

49
Q

What are the miscellaneous for Piroxicam (Feldene)

A

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

50
Q

What is the class for Ketorolac (Toradol)

A

Heteroaryl acetic acids

51
Q

What is the mechanism for Ketorolac (Toradol)

A

Reversibly inhibits COX-1 and -2 (favors COX-1)

52
Q

What are the therapeutics for Ketorolac (Toradol)

A

Post-operative pain; inflammatory eye conditions

53
Q

What are the other side effects for Ketorolac (Toradol)

A

Same as aspirin; relatively nonirritating

54
Q

What are the miscellaneous for Ketorolac (Toradol)

A

Injectable (one of few NSAIDs available for this)

55
Q

What is the class for Celocoxib (Celebrex)

A

COX-2 inhibitor

56
Q

What is the mechanism for Celocoxib (Celebrex)

A

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

57
Q

What are the therapeutics for Celocoxib (Celebrex)

A

Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs

58
Q

What are the important side effects for Celocoxib (Celebrex)

A

Less GI toxicity than traditional NSAIDs

59
Q

What are the miscellaneous for Celocoxib (Celebrex)

A

Contraindicated in patients with heart problems/pregnancy

60
Q

What is the class for Etoricoxib (Arcoxia)

A

COX-2 inhibitor

61
Q

What is the mechanism for Etoricoxib (Arcoxia)

A

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

62
Q

What are the therapeutics for Etoricoxib (Arcoxia)

A

Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs

63
Q

What are the important side effects for Etoricoxib (Arcoxia)

A

Less GI toxicity than traditional NSAIDs

64
Q

What are the miscellaneous for Etoricoxib (Arcoxia)

A

Contraindicated in patients with heart problems/pregnancy

Pharm U2 (11 decks)

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