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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
What are the other side effects for Sulindac (Clinoril)
Nephrotoxicity in elderly or hypovolemic patients
26
What are the miscellaneous for Sulindac (Clinoril)
Half as potent as indomethacin; side effects less frequent
27
What is the class for Ibuprofen (Advil, Motrin)
Proprionic acid dervitive
28
What is the mechanism for Ibuprofen (Advil, Motrin)
Reversibly inhibits COX-1 and -2 (favors COX-1)
29
What are the therapeutics for Ibuprofen (Advil, Motrin)
Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries
30
What are the important side effects for Ibuprofen (Advil, Motrin)
GI irritation; hepatotoxicity (less frequent than aspirin)
31
What is the class for Flurbiprofen (Ocufen)
Proprionic acid dervitive
32
What is the mechanism for Flurbiprofen (Ocufen)
Reversibly inhibits COX-1 and -2 (favors COX-1)
33
What are the therapeutics for Flurbiprofen (Ocufen)
Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries
34
What are the important side effects for Flurbiprofen (Ocufen)
GI irritation; hepatotoxicity (less frequent than aspirin)
35
What is the class for Naproxen (Aleve)
Proprionic acid dervitive
36
What is the mechanism for Naproxen (Aleve)
Reversibly inhibits COX-1 and -2 (favors COX-1)
37
What are the therapeutics for Naproxen (Aleve)
Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries
38
What are the important side effects for Naproxen (Aleve)
GI irritation; hepatotoxicity (less frequent than aspirin)
39
What are the miscellaneous for Naproxen (Aleve)
Longer half-life than most proprionic acid derivitives (13 hours vs. 1-2 hours)
40
What is the class for Oxaprozin (Daypro)
Proprionic acid dervitive
41
What is the mechanism for Oxaprozin (Daypro)
Reversibly inhibits COX-1 and -2 (favors COX-1)
42
What are the therapeutics for Oxaprozin (Daypro)
Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries
43
What are the important side effects for Oxaprozin (Daypro)
GI irritation; hepatotoxicity (less frequent than aspirin)
44
What are the miscellaneous for Oxaprozin (Daypro)
Much longer half-life than most proprionic acid derivitives (50 hours vs. 1-2 hours)
45
What is the class for Piroxicam (Feldene)
Enolic acid
46
What is the mechanism for Piroxicam (Feldene)
Reversibly inhibits COX-1 and -2 (favors COX-1)
47
What are the therapeutics for Piroxicam (Feldene)
Long-term treatment of rheumatoid arthritis or osteoarthritis; also, ankylosing spondylitis, acute musculoskeletal disorders, acute gout
48
What are the other side effects for Piroxicam (Feldene)
Same as aspirin
49
What are the miscellaneous for Piroxicam (Feldene)
Very long half-life (45 hours) permits single daily dose
50
What is the class for Ketorolac (Toradol)
Heteroaryl acetic acids
51
What is the mechanism for Ketorolac (Toradol)
Reversibly inhibits COX-1 and -2 (favors COX-1)
52
What are the therapeutics for Ketorolac (Toradol)
Post-operative pain; inflammatory eye conditions
53
What are the other side effects for Ketorolac (Toradol)
Same as aspirin; relatively nonirritating
54
What are the miscellaneous for Ketorolac (Toradol)
Injectable (one of few NSAIDs available for this)
55
What is the class for Celocoxib (Celebrex)
COX-2 inhibitor
56
What is the mechanism for Celocoxib (Celebrex)
Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)
57
What are the therapeutics for Celocoxib (Celebrex)
Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs
58
What are the important side effects for Celocoxib (Celebrex)
Less GI toxicity than traditional NSAIDs
59
What are the miscellaneous for Celocoxib (Celebrex)
Contraindicated in patients with heart problems/pregnancy
60
What is the class for Etoricoxib (Arcoxia)
COX-2 inhibitor
61
What is the mechanism for Etoricoxib (Arcoxia)
Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site)
62
What are the therapeutics for Etoricoxib (Arcoxia)
Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs
63
What are the important side effects for Etoricoxib (Arcoxia)
Less GI toxicity than traditional NSAIDs
64
What are the miscellaneous for Etoricoxib (Arcoxia)
Contraindicated in patients with heart problems/pregnancy

Pharm U2 (11 decks)

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