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Pharmacology Exam #2 > Immunosuppresive Agents : ) > Flashcards

Immunosuppresive Agents : ) Flashcards

1
Q

What are 3 type of drugs used for prevention of transplant rejection

A
  1. Glucocorticoids
  2. immunophilin ligands
  3. mycophenolate
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2
Q

what are the 3 types of immunophilin ligands

A
  1. cyclosporine
  2. tacrolimus
  3. sirolimus
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3
Q

explain the MOA of cyclosporine

A

cyclosporine is a peptide that binds intracellular cyclophilin to form a complex that inhibits the phosphatase cacineurin

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4
Q

what is cacineurin/what is it needed for

A

Ca2+ calmodulin activated enzyme. Needed for the activation of NF-AT(transcription factor)

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5
Q

what is NF-AT used for?

A

required for the expression of IL-2

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6
Q

why is IL-2 needed?

A

IL-2 is essential for T-cell maturation which are involved in acute transplant rejection

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7
Q

explain the MOA of tacrolimus

A
  • binds to immunophilin FK-binding protein (FKBP)
  • this inhibits calcineurin
  • this inhibits expression of IL-2
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8
Q

what is the MOA of siromilus

A
  • binds immunophilins and acts similar tocromilus and cyclosporine
  • also inhibits B cells
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9
Q

what is a derivative of sirolimus and what is it used for

A

everolimus: used for cardiac transplantation

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10
Q

what is the MOA of mycophenolate mofetil (MMF, CellCept)

A

inhibits de novo purine synthesis (guanine nucleotide)

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11
Q

CU of thalidomide

A

treatment of multiple myeloma

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12
Q

MOA of thalidomide

A

inhibits angiogenesis and TNF-α. —> has inflammatory activity

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13
Q

S/Es of thalidomide

A

TERATOGENIC

  • Amelia (absence of arm)
  • phocomelia (short stumps for limbs)
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14
Q

what type of agent is azathioprine

A

cytotoxic

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15
Q

mercaptopurine’s prodrug is what?

A

azathioprine

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16
Q

cyclophosphamide is what type of drug

A

cytotoxic agent

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17
Q

describe leflunomide (CU, prodrug of…, )

A

cytotoxic agent : prodrug of pyrimidine biosynthetic inhibitor
-inhibits mitochondrial dihydroorotate dehydrogenase
CU: rheumatoid arthritis

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18
Q

what type of drug is hyroxychloroquine and how does it work

A

cytotoxic agent : interferes with the antigen presentation on major histocompatability complex (MHC)

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19
Q

what is hyroxychloroquine used to treat?

A
  • malaria
  • systemic rheumatic disorders (RA,lupus, jorgen’s syndrome, porphyria)
  • post Lyme arthritis
20
Q

what does hyroxychloroquine do in inflammatory conditions?

A

blocks toll-like receptors on plasmacytoid dendritic cells (PDCs) hehe

21
Q

What is the role of toll like receptors -9?

A

TLR-9 recognize DNA immune complexes leading to the production of interferon
—>causes dendritic cells to mature and present antigen to T cells

22
Q

what happens when hyroxychloroquine decreases TLR signaling?

A

reduces the activation of dendritic cells and the inflammatory process

23
Q

what kind of inhibitor is pentostatin (nipent)

A

adenosine deaminase inhibitor

24
Q

what is pentostatin used for

A
  • lymphoid malignancies
  • hairy cell leukemia
  • steroid refractory acute and chronic graft-versus-host disease
  • chronic lymphocytic leukemia in relapsed patients
25
Q

MOA of pentostatin

A

purine analog that mimics adenosine, inhibiting adenosine deaminase interfering with DNA metabolism

26
Q

heterologous antilymphocyte globulin (HAG) and antithymocyte globulin (ATG) is used for what?

A

transplant rejection. they are monoclonal or polyclonal antibodies (idk which…eep) : (

27
Q

describe Muromonab -CD3 and what it is used for

A

monoclonal antibody against CD3 receptor. Prevents transplant rejection

28
Q

describe Immunoglobulin IV and what it is used for

A

fractionated gamma globulin from pooled serum. used for -passive immunization of certain immunodeficiencies

  • kawasaki disease (inflam of blood vessels)
  • ideopathic immunothrombocytopenic purpura
29
Q

what is Rh(D) Immune Globulin and what is it used for

A

anti Rh antibodies given to Rh (-) mothers within 24-72 hrs of delivery to prevent sensitization

30
Q

what may happen to the newborn if the mother is sensitized

A

hemolytic disease of the newborn (HDN) / erythroblastosis fetalis may occur

31
Q

alemtuzumab (campath)

A

humanized anti CD52 MAB used for B cell chronic lymphocytic leukemia

32
Q

Bevacizumab (Avastin)

A

Humanized anti VEGF MAB is antiangiogenic used for colorectal carcinomas in combination therapy.

33
Q

Cetuximab (Erbitux)

A

humanized anti EGFR MAB

34
Q

Gemtuzumab (Mylotarg)

A

humanized anti CD33 MAB used for acute myelogenous leukemia (AML)

35
Q

Gemtuzumab-ozogomycin (mylotarg)

A

combination is available for targeted delivery. Ozogomycin causes strand scission in DNA

36
Q

Rituximab (Rituxan)

A

Humanized anti CD20 MAB used for B cell non Hodgkin’s lymphoma

37
Q

Trastuzumab (Herceptin)

A

humanized anti Her2 - Neu MAB used for Her2-New positive metastatic breast cancers

38
Q

what radioactive isotopes are targeted and delivered by MABs

A

99Tc, 90Y, 111In, 131I.

39
Q

how do MABS as anti-inflammatory agents work

A

they are anti-tumor necrosis factor (TNF) - alpha antibodies. TNF-alpha is a proinflammatory cytokine

40
Q

what is adalimumab (humira) and what is it used for

A 
humanized monoclonal antibody. 
-rheumatoid arthritis 
- psoriatic arthritis(PsA)
-plaque psoriasis 
ideopathic juvenile ankylosing spondylitis
-crohns disease
41
Q

what is etanercept (enbrel)

A

recombinant fusion protein containing TNF-alpha receptor ligand binding domain and human Fcgamma portion

42
Q

what is etanercept used to treat

A
  • rheumatoid arthritis
  • psoriasis,
  • ankylosing spondylitis,
  • psoriatic arthritis -
  • juvenile rheumatoid arthritis.
43
Q

what does infliximab (remicade) treat

A
  • Crohn’s/ peds chrohn’s disease
  • rheumatoid arthritis
  • psoriatic arthritis
  • plaque psoriasis,
  • ankylosing spondylitis
  • Ulcerative colitis,
44
Q

what is infliximab and what is it composed of

A

chimeric IgG1κ monoclonal antibody.
-It is composed of human constant and murine variable regions. Infliximab binds specifically to human TNFα with an association constant of 1010 M-1.

45
Q

what is Ustekinumab (Stelara) and what is used to treat

A

monoclonal antibody against IL -12 and IL-23. Treats plaque psoriasis.

Pharmacology Exam #2 (4 decks)

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