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PHARMACOLOGY - Antibiotics and Immunosuppressives > Anti-inflammatory Drugs > Flashcards

Anti-inflammatory Drugs Flashcards

1
Q

T or T: glucocorticoids and cytotoxic drugs act in a specific manner to prevent inflammation.

A

False, Monoclonal antibodies are examples of more targeted therapy

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2
Q

Are anti-histamines appropriate for controlling asthma?

  • why or why not?
  • What is appropriate for asthma treatment?
A

No, because they do not block histamine release from mast cells, they only prevent histamine binding to receptors

  • Anti-inflammatories are what is needed to control inflammation in asthma patients
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3
Q

What are the two key phases in the asthma response, what molecules are involved in each phase?

A

Bronchospastic Phase:
- Involves Histamine

Inflammatory Phase:

  • PDG2, LTC4, PAF
  • ECP (eosinophil cationic protein), MBP (major basic protein)
  • Proteases, PAF
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4
Q

What is the only drug that currently works on the Nfkb?

  • how does it work?
  • what is the importance of drug design centered around this pathway?
A

Bortezomib
- Prevents Ub being added to Ikb (inhibitor of Ikb) preventing degradation

It allows us to alter a single pathway while leaving others unaffected

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5
Q

What are some downsides of using corticosteriods?

- Specificity

A

Overaching Concept is that they act on too many cellular processes and are very non-specific.

Side effects:
CV risk, Cataract Glaucoma, Hirsutism, Cushings, Insulin resistance, Osteoporosis(necrosis), Infections

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6
Q

What are some ways in which people develop resistance to even powerful coriticosteriods?

A
  • Receptor Modification
  • Compensatory Pathways
  • Upregulation of Counter-regulatory pathways
  • Efflux mechanisms
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7
Q

What enzymes do NSAIDs work on?

A

COX-1/COX-2

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8
Q

What inflammatory Processes are instigated by IL-13, how can these be IL-13 be blocked?.

A
  • IgE secretion by B cells
  • Upregulation of Low-aff. CD 23 FcRII IgE receptor
  • Mucus secretion inc.
  • Eotaxin secretion by Respiratory cells
  • Fibrosis
  • STEROID RESISTANCE.
  • *IL-13 blocked by:
    1. High affinity Shuttle Receptor (ShulL-13R2)
    2. STAT 6 inhibitor
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9
Q

What was the result of using IL-5 antagonists?

A

Only useful in patients with severe, steroid-resistant, eosinophilic asthma

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10
Q

What was the result of using anti-IL-4/IL-3 antibody?

A

not too fruitful, only helped in a subgroup of severely affected patients

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11
Q

What was the result of using anti-TNF-alpha antibody to treat asthma?

A
  • Not effective

- Patients experienced pneumonia and TB and Malignancies

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12
Q

What are the affects of H1 (histamine 1) receptor activation in the following tissues:

  • Lungs
  • Vascular Smooth Muscle
  • Vascular Endothelium
  • Peripheral Nerves
A

Lungs:
- Bronchoconstriction

Vascular Smooth Muscle:

  • Post-capillary venule Dilation
  • Terminal Arteriole Dilation
  • VENOCONSTRICTION

Vascular Endothelium:
- Contraction causing separation

Peripheral Nerves:
- Afferent Nerve Sensitization

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13
Q

What is the difference in first and second generation antihistamines?

A

1st generation antihistamines cross the BBB and act as ANTICHOLINERGICs on CNS

2nd generations don’t pass BBB

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14
Q

What are four 1st generation antihistamines?

A
  • Diphenhydramine
  • Chlorpheniramine
  • Dimenhydrinate
  • Promethazine
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15
Q

What are three 2nd generation antihistamines?

A
  • Cetirizine
  • Fexofenadine
  • Loratadine
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16
Q

How does Roflumilast work?

A
  • PDE4 (phosphodiesterase-4) inhibitor, this prevents PDE4 from turning active cAMP into 5-AMP

this leads to:

  • Relaxation of Airway smooth muscle
  • Suppression of Inflammatory Cell function
  • Inhibition of airways smooth muscle proliferation
17
Q

What group of diseases do TNF-alpha inhibitors work best on?

  • why?
  • What diseases specifically?
A
  • Arthritic type conditions and GI disorders are predominantly the targets for this treatment.
  • TNF-alpha concentrations are elevated in the blood, SYNOVIUM, and JOINTS, which is what these inflammatory conditions involve

Diseases:

  • Ankylosis Spondylitis
  • Crohn’s Disease
  • Juvenile RA or IA
  • Psoriasis
  • Psoriatic Arthritis
  • Rheumatoid Arthritis
  • Ulcerative Colitis
18
Q

What was Telcagepant designed to do?

- why was it dropped off the market?

A
  • CGRP antagonist to reduce migraines but taken off the market because it produced hepatic toxicity
19
Q

What are Pro-resolving molecules?

- why are they the future?

A
  • These mimick the effects of molecules that naturally TERMINATE the production of SPECIFIC inflammatory response.
  • Mimicking these molecules would hopefully lead to more specific effects
20
Q

T or F: Leukotriene inhibitors have no effect on PG pathways

A

True

21
Q

What is the role of the mAb drugs against TNF-alpha?

  • Etancercept
  • Infliximab
  • Adalimumab
  • Certolizumab Pegol
A

All except Certolizumab Pegol the last blocks Soluble TNF-alpha, Binds Transmembrane TNF-alpha, Increase Transmembrane Cytokine Cleavage, Promote ADCC and CDC, Apoptosis, and PMN death (aka OPSONIZATION)

22
Q

What are the COX-2 specific inhibitors?

A

CELECOXIB

23
Q

what are the non-selective COX inhibitors?

A
  1. Ibuprofen
  2. Indometacin (GI toxicity)
  3. Naproxen
24
Q

What drug acts to inhibit the synthesis of Leukotrienes?

A

Zileuton

25
Q

T or F: Antihistamines and Montelukast both work as receptor blockers.

A

True

26
Q

In what two ways doe corticosteroids block GATA-3 from getting to the nucleus?

A
  1. Inhibit p38 MAP kinase (and induce MAP kinase phaosphatase)
    - note: p38 Map Kinase acts to phosphorylate GATA-3
  2. Compete for Nuclear Entry at Importin Alpha
27
Q

T or F: Coricosteroids indiscriminately down regulate NfkB in addition to blocking GATA-3 from the nucleus.

A

True

28
Q

What drug acts to block IkB from getting degraded?

- Preventing NfkB prevents transcription of what genes?

A

Bortezomib

IL-6, VEGF, VCAM-1

29
Q

How do we limit the shitty systemic effects of antiinflammatories?

A
  1. Topical or Inhaled Treatments
  2. Prodrugs that can be targeted to specific tissues
  3. Taper the dose
30
Q

What condition is Roflumilast used to treat?

A

COPD

31
Q

What is the role of Lipoxins in inflammation?

A
  1. They are important for resolving inflammation

***Messing with the Leukotriene pathway could then be messing with potential resolution of the inflammatory response

32
Q

What is Rituximab?

- what does it do?

A

Targets CD20 on B cells

  • Useful in B cell lymphoma
33
Q

Describe the possible outcomes of TNF signaling and the techniques we use to down-regulate this signaling.

A
  1. TNF binding to surface receptors can be activating or pro-apoptotic depending on the amount of signal received

ways to down regulate:

  • Neutralizing TNF-alpha
  • can be done via mAb
  • Also can be done by Soluble Receptor
  • Inhibiting TNF leads to cell death
  • can happen by cytokine deprivation
  • can also happen by anti-body facilitating cell death via ADCC, or CDC
34
Q

What are the TNF-alpha blocking drugs?

A
  • Etancercept
  • Infliximab
  • Adalimumab
  • Certolizumab Pegol
35
Q

What likely plays the biggest role in the TNF blockers, neutralization of TNF or antibody mediated cell death?

A

Neutralizing TNF is likely more important we know this because Certolizumab Pegol lacks and Fc region but is still effective at keeping down inflammation

36
Q

What condition are leukotriene blockers indicated for?

A

asthma

PHARMACOLOGY - Antibiotics and Immunosuppressives (12 decks)

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