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Pharmacology > Remaining Anti-inflammatory & Autoimmune Drugs > Flashcards

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
Q

What NSAID is associated with increased risk of CV events, especially MI?

A

Indomethacin

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26
Q

NSAID side effects can occur due to…

A

inhibition of COX-1

asprin allergy

Reye’s syndrome

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27
Q

Inhibition of COX-1 causes what side effects?

A

stomach irritation, prolonged bleed time, renal toxicity, CNS effects

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28
Q

Asprin causes what side effects?

A

angioedema, anaphylaxis, respiratory symptoms, skin reactions, increased leukotrienes

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29
Q

What is Reye’s Syndrome and what does it cause?

A

Varicella infection or influenza virus causes liver damage and encephalopathy

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30
Q

COX-2 selective inhibitors are better because…

A

they have significantly fewer severe side effects in the GI tract and patients should experience less dyspepsia

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31
Q

Celecoxib

A

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

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32
Q

Zileuton

A

Leukotriene Pathway Inhibitor

inhibits 5-lipoxygenase and CYP3A4

orally active

mild to moderate asthma

alternative to a low-dose inhaled corticosteroid therapy

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33
Q

Zafirlukast

A

Leukotriene Pathway Inhibitor

LTD4-receptor antagonist

inhibits CYP3A4 and CYP2C9

orally active

mild to moderate asthma

alternative to a low-dose inhaled corticosteroid therapy

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34
Q

Montelukast

A

Leukotriene Pathway Inhibitor

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35
Q

Which drug inhibits 5-lipoxygenase and CYP3A4?

A

Zileuton

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36
Q

Which drugs blocks the LTD4-receptor?

A

Zafirlukast and Montelukast

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37
Q

What drug has to be used in conjunction with COX-2 inhibitors with patients with asthma?

A

Leukotriene pathway inhibitors

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38
Q

Glucocorticoids

A

anti-inflammatory drugs

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39
Q

Cortisol is produced by the…

A

adrenal cortex

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40
Q

What is the pathway of signaling for cortisol production, aka HPA Axis?

A

Hypothalamus –> CRH –> anterior pituitary –> ACTH –> adrenal cortex –> cortisol

Cortisol does negative feedback to both previous steps

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41
Q

Cortisol is synthesized from what precursor?

A

Cholesterol

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42
Q

The secretion of what follows a circadian rhythm and is controlled by pulses of ACTH that peak in early morning and after meals?

A

Cortisol

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43
Q

What physiologic effects do glucocorticoids have?

A

regulation of immune function, growth, carbohydrate, fat and protein metabolism

44
Q

Prednisone

A

Synthetic Glucocorticoid

45
Q

What drug classes are used to treat RA and sometimes other autoimmune diseases?

A 
NSAIDs
DMARDs
Cytokine blockers
Inhibitors of T-cell activation
Inhibitors of B-cell activation
46
Q

Infliximab

A

Cytokine Blocker

inhibits function of TNF-a

chimeric mAb

47
Q

Etanercept

A

Cytokine Blocker

inhibits function of TNF-a

human TNF-receptor linked to the Fc portion of human IgG1

48
Q

Anakinra

A

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
Q

Adalimumab

A

Cytokine Blocker

inhibits function of TNF-a

human mAb specific for TNF-a

50
Q

What drugs lead to increased incidence of infection, lupus, exacerbation of demyelinating diseases (MS), and heart failure?

A

anti-TNF therapy

51
Q

What autoimmune diseases have been successfully treated with anti- TNF therapy?

A

RA, Crohn’s, Ankylosing Spondylitis, Juvenile RA, Psoriatic arthritis, psoriasis
sarcoidosis

52
Q

Abatecept

A

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
Q

What drug is used for patients that do not respond well to methotrexate or TNF antagonists?

A

Abatecept

Increased function of CTLA-4 which inhibits T-cell activation

54
Q

Rituximab

A

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
Q

Which drug causes B-cell depletion?

56
Q

Tofacitinib

A

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
Q

Inflammation of nasal passages and upper pharynx; upper respiratory tract infections; increased risk of TB and lymphoma; and headaches are side effects of….

A

JAK inhibitor- Tofacitinib

58
Q

Apremilast

A

PDE-4 inhibitor

moderate to severe plaque psoriasis

increases intracellular cAMP

decreases TNF-a production

59
Q

Eicosanoids

A

compounds that are derived from arachidonic acid

60
Q

Prostaglandins that are potent vasodilators?

A

PGI2 and PGE2

61
Q

Leukotrienes that cause hypotension due in part to coronary blood flow are…

A

LTC4 and LTD4

62
Q

Thromboxanes

A

potent vasoconstrictors

TXA2- produced by platelets

63
Q

What mediators are involved in bone formation, resorption and calcium release from bone?

A

prostaglandins

64
Q

Which three 1st generation drugs block the action of histamine at the H1 receptors?

A

Chorpheniramine
Diphenhydramine
Promenthazine

65
Q

Which drug class is involved with sedation?

A

H1 receptor antagonists (but many are inverse agonists)

66
Q

What three 2nd/3rd generation drugs block the histamine H1 receptor?

A

Loratidine
Fexofenadine
Cetirizine

67
Q

What is the most common symptom associated with NSAIDs?

A

GI dyspepsia and GI bleeding

Also, reduce renal function and increase blood pressure

68
Q

What NSAID drugs don’t select one COX over the other?

A

Aspirin

Ibuprofen

69
Q

Which COX is selected for more with the NSAID, indomethacin?

A

COX-1 over 2

70
Q

What drug is associated with caution in elderly patients with history of depression?

A

indomethacin

71
Q

Nabumetone is an NSAID that has selectivity for…

A

COX-2 over 1

72
Q

Which NSAID is a prodrug and is associated with less GI dyspepsia?

A

Nabumetone

73
Q

Meloxicam is an NSAID that has selectivity for which COX enzyme?

A

COX-2 over 1

74
Q

Celecoxib (NSAID) is selective for

A

COX-2 only

75
Q

You should be cautious with individuals with known sensitivity to sulfonamide drugs with use of…

76
Q

What three drugs are leukotriene pathway inhibitors?

A

Zileuton
Zarfirlukast
Montelukast

77
Q

What is the target for Zileuton?

A

Inhibition of 5-lipooxygenase

78
Q

What drugs antagonize the LTD4 (CysLT1) receptors?

A

Zafirlukast

Montelukast

79
Q

What drugs inhibit CYP3A4?

A

All the leukotriene inhibitors

80
Q

Prednisone is an anti-inflammatory drug that has what sort of duration?

A

Short to medium

81
Q

What are the five steroidal anti-inflammatory drugs?

A

Prednisone
Fluticasone
Triamcinolone
Dexamethasone

82
Q

Which steroidal anti-inflammatory drug has an intermediate duration of action?

A

Triamcinolone

83
Q

Which steroidal anti-inflammatory drug has an long duration of action?

A

Dexamethason

84
Q

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
A

steroidal anti-inflammatory agents

85
Q

Hydroxychloroquine is used for…

A

Rheumatoid arthritis and psoriatic arthritis

86
Q

What are the possible mechanisms of action for hydroxycholoquine?

A

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
Q

What drug targets the TNF-a receptor?

A

Entanercept

soluble TNF-a receptor fusion protein that blocks TNF-a action

88
Q

What drug blocks the TNF-a action directly?

A

Infliximab

Anti TNF-a antibody that blocks action of TNF-a

89
Q

What are the MOAs of methotrexate?

A
  • 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
Q

What cell synthesizes leukotriene B4?

A

Neutrophils

91
Q

High doses of methotrexate can cause… due to high doses or improper elimination.

A

hepatotoxicity
myelo-suppression
pulmonary damage

92
Q

Anakinra targets…

A

IL-1 function

Inhibits function

93
Q

What drug is NOT recommended in combination with TNF inhibitors?

94
Q

Ustekinumab binds to and interferes with…

A

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
Q

What drug targets the extracellular domain of CTLA-4?

A

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
Q

What drug can result in a falsely elevated serum glucose reading on the day of infusion?

A

Abatacept because it’s powder form has maltose sometimes

97
Q

What is the drug that targets CD20 antigen on B-cells?

98
Q

What are the possible MOAs for rituximab?

A
  • Fb receptor gamme mediated ADCC
  • Ab-mediated complement dependent cell lysis
  • growth arrest
  • B-cell apoptosis
99
Q

Tofacitinib targets…

A

JAK (Jak Kinase)

100
Q

What drug targets the PDE-4 molecule?

A

Apremilast

101
Q

What does apremilast binding to and inhibiting PDE-4 cause?

A

An increase in intracellular cAMP which decreases TNF-a production

102
Q

What drug is only indicated for moderate to severe plaque psoriasis patients?

A

Apremilast

103
Q

What drugs are used for SLE?

A 
Hydroxychloroquine
Azathioprine
Cyclophosphamide
Mycophenolate mofetil (MMF)
Rituximab
104
Q

Azathioprine is a prodrug converted to…

105
Q

Cyclophosphamide is a alkylating agent that…

A

crosslinks to DNA leading to cell death

106
Q

MMF (Mycophenolate mofetil) MOA is…

A

reversibly inhibits IMP dehydrogenase –> decrease B- and T-cell proliferation –> decreased Ab production

107
Q

Inflammation of the pharynx is associated with…

A

Tofacitnib (JAK inhibitor)

Pharmacology (6 decks)

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