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Remaining Anti-inflammatory & Autoimmune Drugs Flashcards

1
Q

Asprin is a weak acid called…

A

acetylsalicylic acid

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2
Q

Asprin acts as a….

A

analgesic - anti pain
antipyretic- anti fever
anti-platelet
anti-inflammatory

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3
Q

The classic NSAID is…

A

Asprin

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4
Q

What is the MOA of Asprin?

A

Irreversibly blocks the COX enzyme preventing the production of prostaglandins

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5
Q

COX

A

Cyclooxygenase enzyme

Converts arachidonic acid to prostaglandins

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6
Q

Prostaglandins

A

late phase inflammatory meadiators

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7
Q

Salicylate-like NSAIDs are…

A

weak organic acids

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8
Q

What anti-inflammatory drugs are rapidly absorbed?

A

Salicylate-like NSAIDs

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9
Q

What are characteristics of Salicylate-like NSAIDs?

A
  • Rapidly absorbed orally
  • highly bound to plasma proteins
  • extensively metabolized by the liver
  • have drug-drug interactions
  • inhibit COX
  • Varying degrees of GI toxicity, suppression of platelet aggregation
  • allergic type cross reaction with Asprin
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10
Q

What is the only anti-inflammatory that irreversibly inhibits COX?

A

Asprin

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11
Q

COX 1

A

is activated by physiological stimulus

is constitutive

results in homeostasis

Responsible for platelet aggregation (TXA2)

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12
Q

TXA2, PGI2, PGE2

A

COX-1

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13
Q

COX-2 is stimulated by…

A

inflammation

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14
Q

Which COX is inducible?

A

COX-2

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15
Q

What mediators are associated with COX-2?

A

PGs, other mediators –> inflammation

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16
Q

PGE2

A

inflammation signs - redness, swelling, and pain

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17
Q

What prostaglandin is rapidly produced after tissue injury?

A

PGI2

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18
Q

PGI2

A

involved in edema and pain for acute inflammation

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19
Q

Which prostaglandin is involved in acute inflammation?

A

PGI2

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20
Q

PGD2 is produced by…

A

antigen-presenting dendritic cells and Th2 cells

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21
Q

What prostaglandin is most abundance in synovial fluid of human arthritic knee joints?

A

PGI2

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22
Q

Elevated levels of which prostaglandin are reported in patients with RA, psoriatic arthritis, reactive arthritis, and osteoarthritis?

A

PGF2a

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23
Q

What NSAIDs are linked to inhibition of COX 1 and 2?

A

Traditional NSAIDs

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24
Q

Nabumetone

A

NSAID that shows selectivity for COX-2 (in vitro)

Prodrug

Less GI upset

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25
What NSAID is associated with increased risk of CV events, especially MI?
Indomethacin
26
NSAID side effects can occur due to...
inhibition of COX-1 asprin allergy Reye's syndrome
27
Inhibition of COX-1 causes what side effects?
stomach irritation, prolonged bleed time, renal toxicity, CNS effects
28
Asprin causes what side effects?
angioedema, anaphylaxis, respiratory symptoms, skin reactions, increased leukotrienes
29
What is Reye's Syndrome and what does it cause?
Varicella infection or influenza virus causes liver damage and encephalopathy
30
COX-2 selective inhibitors are better because...
they have significantly fewer severe side effects in the GI tract and patients should experience less dyspepsia
31
Celecoxib
COX-2 Selective Inhibitor sulfonamide the ONLY one that is FDA approved not any better for upper GI, but better for small bowel inflammation and mucosal breaks
32
Zileuton
Leukotriene Pathway Inhibitor inhibits 5-lipoxygenase and CYP3A4 orally active mild to moderate asthma alternative to a low-dose inhaled corticosteroid therapy
33
Zafirlukast
Leukotriene Pathway Inhibitor LTD4-receptor antagonist inhibits CYP3A4 and CYP2C9 orally active mild to moderate asthma alternative to a low-dose inhaled corticosteroid therapy
34
Montelukast
Leukotriene Pathway Inhibitor
35
Which drug inhibits 5-lipoxygenase and CYP3A4?
Zileuton
36
Which drugs blocks the LTD4-receptor?
Zafirlukast and Montelukast
37
What drug has to be used in conjunction with COX-2 inhibitors with patients with asthma?
Leukotriene pathway inhibitors
38
Glucocorticoids
anti-inflammatory drugs
39
Cortisol is produced by the...
adrenal cortex
40
What is the pathway of signaling for cortisol production, aka HPA Axis?
Hypothalamus --> CRH --> anterior pituitary --> ACTH --> adrenal cortex --> cortisol Cortisol does negative feedback to both previous steps
41
Cortisol is synthesized from what precursor?
Cholesterol
42
The secretion of what follows a circadian rhythm and is controlled by pulses of ACTH that peak in early morning and after meals?
Cortisol
43
What physiologic effects do glucocorticoids have?
regulation of immune function, growth, carbohydrate, fat and protein metabolism
44
Prednisone
Synthetic Glucocorticoid
45
What drug classes are used to treat RA and sometimes other autoimmune diseases?
``` NSAIDs DMARDs Cytokine blockers Inhibitors of T-cell activation Inhibitors of B-cell activation ```
46
Infliximab
Cytokine Blocker inhibits function of TNF-a chimeric mAb
47
Etanercept
Cytokine Blocker inhibits function of TNF-a human TNF-receptor linked to the Fc portion of human IgG1
48
Anakinra
Cytokine Blocker Inhibitor of IL-1 function recombinant, nonglycoslyated synthetic form of human IL-1 receptor antagonist (IL-1Ra) endogenous regulator of IL-1 action
49
Adalimumab
Cytokine Blocker inhibits function of TNF-a human mAb specific for TNF-a
50
What drugs lead to increased incidence of infection, lupus, exacerbation of demyelinating diseases (MS), and heart failure?
anti-TNF therapy
51
What autoimmune diseases have been successfully treated with anti- TNF therapy?
RA, Crohn's, Ankylosing Spondylitis, Juvenile RA, Psoriatic arthritis, psoriasis sarcoidosis
52
Abatecept
Inhibitor of T-cell Activation Blocks costimulatory signal required for T-cell activation Fusion protein of extracellular domain of CTLA-4 and Fc domain of human IgG1
53
What drug is used for patients that do not respond well to methotrexate or TNF antagonists?
Abatecept Increased function of CTLA-4 which inhibits T-cell activation
54
Rituximab
Inhibitor of B-cell function Only for patients who don't respond to TNF-a therapy and for non-Hodgkin's lymphoma Chimeric mAb against CD20 antigen on B-cells
55
Which drug causes B-cell depletion?
Rituximab
56
Tofacitinib
JAK inhibitor blocks JAK 3 and JAK 1 To a lesser degree, JAK 2 also Moderate to severe active RA in patients that don't respond to methotrexate
57
Inflammation of nasal passages and upper pharynx; upper respiratory tract infections; increased risk of TB and lymphoma; and headaches are side effects of....
JAK inhibitor- Tofacitinib
58
Apremilast
PDE-4 inhibitor moderate to severe plaque psoriasis increases intracellular cAMP decreases TNF-a production
59
Eicosanoids
compounds that are derived from arachidonic acid
60
Prostaglandins that are potent vasodilators?
PGI2 and PGE2
61
Leukotrienes that cause hypotension due in part to coronary blood flow are...
LTC4 and LTD4
62
Thromboxanes
potent vasoconstrictors TXA2- produced by platelets
63
What mediators are involved in bone formation, resorption and calcium release from bone?
prostaglandins
64
Which three 1st generation drugs block the action of histamine at the H1 receptors?
Chorpheniramine Diphenhydramine Promenthazine
65
Which drug class is involved with sedation?
H1 receptor antagonists (but many are inverse agonists)
66
What three 2nd/3rd generation drugs block the histamine H1 receptor?
Loratidine Fexofenadine Cetirizine
67
What is the most common symptom associated with NSAIDs?
GI dyspepsia and GI bleeding Also, reduce renal function and increase blood pressure
68
What NSAID drugs don't select one COX over the other?
Aspirin | Ibuprofen
69
Which COX is selected for more with the NSAID, indomethacin?
COX-1 over 2
70
What drug is associated with caution in elderly patients with history of depression?
indomethacin
71
Nabumetone is an NSAID that has selectivity for...
COX-2 over 1
72
Which NSAID is a prodrug and is associated with less GI dyspepsia?
Nabumetone
73
Meloxicam is an NSAID that has selectivity for which COX enzyme?
COX-2 over 1
74
Celecoxib (NSAID) is selective for
COX-2 only
75
You should be cautious with individuals with known sensitivity to sulfonamide drugs with use of...
Celecoxib
76
What three drugs are leukotriene pathway inhibitors?
Zileuton Zarfirlukast Montelukast
77
What is the target for Zileuton?
Inhibition of 5-lipooxygenase
78
What drugs antagonize the LTD4 (CysLT1) receptors?
Zafirlukast | Montelukast
79
What drugs inhibit CYP3A4?
All the leukotriene inhibitors
80
Prednisone is an anti-inflammatory drug that has what sort of duration?
Short to medium
81
What are the five steroidal anti-inflammatory drugs?
Prednisone Fluticasone Triamcinolone Dexamethasone
82
Which steroidal anti-inflammatory drug has an intermediate duration of action?
Triamcinolone
83
Which steroidal anti-inflammatory drug has an long duration of action?
Dexamethason
84
What drugs in high dosing or chronic administration are the following side effects related to? - Cushing's Syndrome - Hypertension - Delayed wound healing - acne, cataracts, glaucoma - inhibition of bone formation and stimulation of bone resorption - weight gain - inhibition of growth in children - immunosuppression - thrombosis - behavioral changes
steroidal anti-inflammatory agents
85
Hydroxychloroquine is used for...
Rheumatoid arthritis and psoriatic arthritis
86
What are the possible mechanisms of action for hydroxycholoquine?
1) effects innate immune system by inhibiting TLR-9 activation by DNA-immune complexes and inhibits TLR signaling 2) lysosomotropic activity involving increases in intracellular pH affects protein processing
87
What drug targets the TNF-a receptor?
Entanercept soluble TNF-a receptor fusion protein that blocks TNF-a action
88
What drug blocks the TNF-a action directly?
Infliximab Anti TNF-a antibody that blocks action of TNF-a
89
What are the MOAs of methotrexate?
- reduced neutrophil adhesion - antiproliferative effect on fibroblasts and endothelial cells - inhibition of leukotriene B4 synthesis by neutrophils - reduced IL-1, IL-6 and IL-8 levels - suppression of cell mediated immunity
90
What cell synthesizes leukotriene B4?
Neutrophils
91
High doses of methotrexate can cause... due to high doses or improper elimination.
hepatotoxicity myelo-suppression pulmonary damage
92
Anakinra targets...
IL-1 function Inhibits function
93
What drug is NOT recommended in combination with TNF inhibitors?
Anakinra
94
Ustekinumab binds to and interferes with...
proinflammatory cytokines such as IL-12 and IL-23 AND expression of monocyte chemotactic protein 1 (MCP1), TNF-a, interferon inducible protein 10 (IP10), and IL-8
95
What drug targets the extracellular domain of CTLA-4?
Abatacept blocks the costimulatory pathway for t-cell activation by binding to and preventing CD28 from binding to it's counter receptor CD80/CD86
96
What drug can result in a falsely elevated serum glucose reading on the day of infusion?
Abatacept because it's powder form has maltose sometimes
97
What is the drug that targets CD20 antigen on B-cells?
Rituximab
98
What are the possible MOAs for rituximab?
- Fb receptor gamme mediated ADCC - Ab-mediated complement dependent cell lysis - growth arrest - B-cell apoptosis
99
Tofacitinib targets...
JAK (Jak Kinase)
100
What drug targets the PDE-4 molecule?
Apremilast
101
What does apremilast binding to and inhibiting PDE-4 cause?
An increase in intracellular cAMP which decreases TNF-a production
102
What drug is only indicated for moderate to severe plaque psoriasis patients?
Apremilast
103
What drugs are used for SLE?
``` Hydroxychloroquine Azathioprine Cyclophosphamide Mycophenolate mofetil (MMF) Rituximab ```
104
Azathioprine is a prodrug converted to...
6-MP
105
Cyclophosphamide is a alkylating agent that...
crosslinks to DNA leading to cell death
106
MMF (Mycophenolate mofetil) MOA is...
reversibly inhibits IMP dehydrogenase --> decrease B- and T-cell proliferation --> decreased Ab production
107
Inflammation of the pharynx is associated with...
Tofacitnib (JAK inhibitor)

Pharmacology (6 decks)

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