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Pharmacology FINAL (2nd sem) > B29-31 > Flashcards

B29-31 Flashcards

1
Q

Alkylating agent used as immunosuppressive?

A

Cyclophosphamide

(in organ transplantation and rheumatic diseases)

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2
Q

what about cyclophosphamide?

A
  • nitrogen mustard
  • CCNS
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3
Q

Antimetabolite that is used in immunosupressive agent?

A

methotrexate

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4
Q

what about methotrexate?

A

antagonists of folic acid

; give leucovorin rescue to reduce toxicity

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5
Q

methotrexate MOA?

A
  • inhibitor of dihydrofolate reductase
  • interferes with nucleic acid and protein metabolism
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6
Q

methotrexate pharmacoKinetix?

A
  • Oral and I.V.
  • good tissue distribution (except CNS)
  • not metabolized,
  • clearance is dependent on renal function
  • Adequate hydration is needed to prevent crystallization in renal tubules
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7
Q

Clinical uses of methotrexate as immunosupressive agent?

A
  • rheumatoid arthritis
  • psoriasis
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8
Q

drug used in Kidney, Liver and heart transplantation?

A

Mycophenolate Mofetil

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9
Q

Mycophenolate Mofetil MOA

A
  • converted into mycophenolic acid –> inhibits inosine monophosphate dehydrogenase –> blocks denovo GTP synthesis –> supresses both B and T lymphocyte activation
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10
Q

Mycophenolate Mofetil Clinical use?

A

kidney
Liver
heart transplantations
autoimmune disease( SLE, GN, Psoriasis)

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11
Q

Mycophenolate Mofetil Toxicity?

A

G.I disturbances

neutropenia

given with cyclosporine to reduce dose ; reduce toxicity

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12
Q

cytotoxic drug used in IBD, rheumatic diseases and organ transplantation?

A

Azathioprine

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13
Q

Azathioprine MOA?

A

interferes with purine nucleic acid metabolism of immune cells

  • inhibit denovo purine synthesis
  • rapidly converted to 6-MP
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14
Q

give example of disease modifying antirheumatoc drug?

A

leflunomide

MTX (1st line)

sulfasalazine (5-ASA)

cyclosporin

Tofacitinib

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15
Q

Leflunomide MOA?

A

Inhibitor of dihydroorotate dehydrogenase –> inhibits pyrimidine synthesis –> interfere with the activity of T lymphocytes

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16
Q

Leflunomide administration?

A

orally

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17
Q

Leflunomide clinical uses?

A

rheumatoid arthritis
multiple sclerosis

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18
Q

Inhibitors of cytokine gene expression, 5-ASA derivatives?

A
  • calcineurin inhibitors:
    • cyclosporin A: binds cyclophillin
    • tacrolimus: binds FK-binding protein
  • mTOR inhibitors
    • sirolimus (rapamycin): binds FK-binding protein –> inhibit kinase activity of mTOR
  • JAK inhibitors
    • tofacitinib
  • other immunosupressive agent:
    • sulfasalazine
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19
Q

Calcineurin and mTOR Inhibitors?

A

Cyclosporine
tacrolimus

sirolimus

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20
Q

Cyclosporine A MOA?

A

binds to cyclophilin –> inhibits calcineurin –> inhibits the production of IL-2,3 IFN-g

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21
Q

Tacrolimus MOA?

A

binds to FKBP –> inhibit calcineurin –> inhibits the production of IL-2,3 IFN-g

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22
Q

Sirolimus MOA?

A

binds to FKBP –> inhibit the kinase activity of mammalian target of rapamycin (mTOR) –> inhibits the T-cell proliferation response to IL-2

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23
Q

Cyclosporine clinical use?

A
  • in solid organ transplantation
  • to prevent and treat graft-versus-host (GVH) disease in recipients of allogeneic stem cell transplantation
  • rheumatoid arthritis
  • uveitis
  • psoriasis
  • asthma
  • type 1 diabetes
24
Q

Tacrolimus clinical use?

A
  • in solid organ transplantation
  • to prevent and treat graft-versus-host (GVH) disease in recipients of allogeneic stem cell transplantation
  • rheumatoid arthritis
  • uveitis
  • psoriasis
  • asthma
  • type 1 diabetes

(same as cyclosporine)

25
Q

Sirolimus Clinical uses?

A

Sirolimus-eluting stents are used to prevent restenosis after coronary angioplasty

26
Q

Cyclosporine Pharmacokinetix?

A
  • oral or intravenous
  • exhibits erratic bioavailability (serum lvls are routinely monitored)
  • slow hepatic metabolism by the cyt P450 system
  • long 1/2 life
27
Q

Tacrolimus administration?

A

oral or I.V.

28
Q

Sirolimus administration?

A

ONLY oral

29
Q

Cyclosporine Toxicity?

A
  • renal dysfunction
  • hypertension
  • neurotoxicity
30
Q

Tacrolimus Toxicity?

A
  • renal dysfunction
  • hypertension
  • neurotoxicity
31
Q

Sirolimus Toxicity?

A
  • hypertriglyceridemia
  • hepatotoxicity
  • diarrhea
  • myelosuppression
32
Q

other drugs to know for topic immuno II

A

sulfasalazine (5-ASA derivative)
tofacitinib (JAK1, 3 inhibitor)

(they are DMARDs)

33
Q

Antibodies and fusion proteins in immunopharmacology?

A

ATG (antithymocyte-globulin)

infli-ximab (ANTI-TNF-alpha)

Ritu-ximab ( anti CD 20 )

tocili-zumab (Anti-IL6)

natalizumab (Anti-integrin)

adalim-umab (Anti-TNF-a)
ustekin-umab ( Anti-IL12, 23)
dupil-umab (Anti-IL4 receptor)

abatacept (CTLA4 fusion protein)

34
Q

what is ATG?

A

AntiThymocyte Globulin

35
Q

ATG MOA?

A
  • bind to human T cells involved in antigen recognition –> initiate their destruction by serum complement
  • block cellular immunity –> suppress organ graft rejection
36
Q

ATG clinical use?

A
  • used before allogeneic stem cell transplantation to prevent graft-versus-host reaction
  • used in combination with other immunosuppressants for solid organ transplantation
37
Q

ATG toxicity?

A
  • hypersensitivity reactions:
    1. serum sickness
    2. anaphylaxis
  • Pain and erythema (injection sites)
  • lymphoma (late complication)
38
Q

what about rituximab?

A
  • DMARD
  • monoclonal Ab that interfere with the activity of B lymphocytes
39
Q

Rituximab MOA

A

binds to a surface protein CD20 on B lymph. in non-Hodgkin’s lymphoma cells then:

  • complement-mediated lysis
  • direct cytotoxicity
  • induction of apoptosis
40
Q

Rituximab use?

A
  • non-Hodgkin’s lymphoma
  • rheumatoid arthritis (with methotrexate)
41
Q

Rituximab toxicity?

A
  • anemia
  • neutropenia
  • hypotension
  • fever
42
Q

examples of MAbs that target TNF?

A

Infliximab
Adalimumab

43
Q

Infliximab MOA?

A

against TNF-α –> thereby decreases formation of interleukins and adhesion molecules involved in leukocyte activation

44
Q

Infliximab Clinical use?

A
  • in treatment-resistant Crohn’s disease
  • rheumatoid arthritis (with methotrexate)
  • ulcerative colitis
  • psoriatic arthritis
45
Q

Adalimumab MOA?

A

human IgG monoclonal antibody that binds to TNF-α

46
Q

Adalimumab Clinical use?

A

rheumatoid arthritis

47
Q

ustekinumab MOA?

A

Binds and neutralizes the biological activity of IL-12 & IL-23

48
Q

ustekinumab Clinical use?

A

Plaque psoriasis

49
Q

natalizumab MOA?

A
  • Anti-Integrins
  • Humanized IgG4 binds to integrins on leukocytes (except neutrophils)
50
Q

Natalizumab Clinical use?

A

Drug resistant multiple sclerosis

Crohn’s disease

51
Q

What are the risks of using Natalizumab?

A

progressive multifocal leukoencephalopathy (PML)

52
Q

dupilumab

A

Anti-IL4 receptor

  • human monoclonal Ab
  • Parenteral

used for atopic dermatitis

SE: allergic rxn, conjuctivitis, keratitis

53
Q

Abatacept MOA?

A

CTLA-4 Fusion protein!

blocks T-cell activation by interfering with the interaction of T-cell CD28 to APC

54
Q

Abatacept Clinical use?

A

severe rheumatoid arthritis

55
Q

Abatacept SE

A
  • infections
  • production of neutralizing Ab’s

Pharmacology FINAL (2nd sem) (37 decks)

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