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Pharmacodynamics > DMARDs > Flashcards

DMARDs Flashcards

1
Q

Define DMARDs

A

Disease Modifying : used both to control symptoms and to slow/stop the progression of the disease
Anti-Rheumatic: Used for Rheumatoid Arthritis and other chronic inflammatory diseases as well

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2
Q

Rheumatoid Arthritis (RA) can cause:

A

diabetes

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3
Q

Autoimmune define:

A

The immune system attacks healthy cells in the body—> persistent inflammation (mostly in the joints) = joint damage

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4
Q

List some differences in a healthy joint compared to arthritic joint

A

increased number of inflammatory cells (i.e. B-cell, T-cells, macrophages etc)
Increases level of inflammatory mediators (TNFalpha, IL-1,IL-6)

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5
Q

csDMARDs

A

conventional synthetic DMARDS

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6
Q

bDMARDs

A

biological DMARDS

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7
Q

EXAMPLE of commonly used csDMARD

A

Methotrexate

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8
Q

MECHANISM of action for csDMARDs

A

NON-SPECIFIC

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9
Q

mechanism of Methotrexate

A
  • inhibits dihydrofolate reductase (involved in folate metabolism)= no DNA/RNA synthesis= inhibits cell proliferation/death
  • inhibits the enzyme AICAR transformylase (ATIC) = increased levels of AICAR
    overall less inflammation because decreased levels of inflammatory cells
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10
Q

Adenosine receptor is what type of receptor?

A

G protein coupled receptor

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11
Q

cons of csDMARDs

A

require regular monitoring
takes time for their effects ( 7 months)

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12
Q

Advantages of bDMARDs

A

Highly specific in their mechanism of action
High efficacy (relief symptoms + slow/stop progression of the disease)

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13
Q

Biological DMARDs define + characteristics

A
  • Medicinal products derived from a living organism
    -Mostly proteins
    -Most manufactured using recombinant DNA technology
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14
Q

Most biologics are manufactured using?

A

recombinant DNA technology

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15
Q

csDMARDS define:

A

small synthetic molecules
-originally developed to treat cancer

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16
Q

csDMARDs also used to treat?

A

Psoriasis, Crohn’s disease

17
Q

Biologics vs Conventional drugs

A

-Manufacturing process highly complex and difficult to replicate but csDMARDs its easy to replicate (chemical synthesis)
-biologics are large molecules conventional drugs are small molecules
-Biologics are more unstable and sensitive to external conditions but conventional are stable

18
Q

how might biologics work?

A

B cells depletion
Inhibition of T-cell activation
Cytokine Inhibition : TNF-alpha/ IL inhibitors

19
Q

Examples of TNF- alpha inhibitors

A

Adalimumab,Infliximab

20
Q

TNF-alpha define

A

key pro-inflammatory cytokine
produced predominantly by macrophages

21
Q

How might biologics TARGET PRO-INFLAMMATORY CYTOKINES?

A

-anti TNF-alpha therapy
-inhibit other cytokines (ANTI: IL-1, IL-6 THERAPIES )

22
Q

IL-1, IL-6 define

A

pro-inflammatory cytokines with a central role in the activation of an inflammatory response

23
Q

Anakinra

A

recombinant antagonist of the IL-1 receptor

24
Q

Canakinumab

A

Antibody that binds to IL-1: (SELECTIVELY BLOCKING)

25
Q

Examples of anti IL-1 therapies

A

Anakira
Canakinumab

26
Q

Tocilizumab

A

an antibody that binds to IL-6 receptors (blocking)

27
Q

Rituximab

A

antibody specific for CD20, which is expressed on B cells

28
Q

Biologic that decreases B cells

A

Rituximab

29
Q

Mechanism of action for rituximab

A

targets CD20 on B cells
CDC- complement-dependent cytotoxicity and ADCC :antibody-dependent cell-mediated cytotoxicity lead to apoptosis=promotes cell lysis

B-CELL DEPLETION

30
Q

Abatacept

A

inhibits the “second signal” required for T-cell activation
prevents co-stimulation
prevents activation of T-cells

31
Q

Disadvantages of DMARDs

A

side effects: increased susceptibility to infection, increased risk of malignancy
Mode of administration: IV, subcutaneous
Manufactured using a living organism= manufacturing process highly complex and difficult to replicate
Unstable (storage conditions very important!)
High price

32
Q

side effects of biological DMARDs

A

increased susceptibility to infection, increased risk of malignancy

Pharmacodynamics (17 decks)

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