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Pharm Exam 4 > Immunosuppressant > Flashcards

Immunosuppressant Flashcards

1
Q

Define: Prednisone Equivalent doses nomenclature?

A

-A 5 mg prednisone dose has equivalent effect to other short, long, or intermediate acting glucocorts regardless of concnetration

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2
Q

glucocorticoids

-MOA?

A

1) genomic effects: direct to DNA = inhibit gene expression = fewer immune and inflammatory cytokines
2) non-genomic: cell signalling pathways affected - rapid immune suppression via signalling (cant be genomic bc that is slow change)

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3
Q

Glucocorticoid effects:

A
  • rapid dec in periph blood lymphs
  • downreg pro inflammatory cytokines IL1, IL6 TNF-a, interferon-y
  • inhibit IL2 = needed for T-cell maturation
  • reduce neutrophil chemotaxis and lysosomal enzyme release
  • LITTLE EFFECT ON HUMORAL
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4
Q

Glucocorticoid therapeutic uses:

A
  • prevent/treat transplant rejectino (combo therapy)
  • treat Graft v hot disease with BM transplant
  • block first dose cytokine storm in transplant recipeints by tx with muromonab-CD3 and antithymocyte globulin
  • tx autoimmune disorder… long list
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5
Q

Glucocorticoids AE:

A

1) disabling/life threatening
- growth retardation
* **-inc risk inf
- poor wound healing
- HTN
- avascular necrosis of bone
- cataracts
- hyperglycemia
* **-adrenal crisis upon rapid discontinuation

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6
Q

Prevent rapid withdrawal or reduced doses of glucocorticoid AE how?

A

-use combined glucocorticoid calcineurin inh protocols

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7
Q

Low dose glucocorticoid definition:

A

less than or equal to 7.5mg of prednisone equiv per day

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8
Q

Medium dose glucocorticoid definition:

A

greater than 7.5 mg, but less than or equal to 30mg prednisone equiv per day

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9
Q

High dose glucocorticoid definition:

A

greater than 30mg but less than or equal to 100mg prednisone equiv per day

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10
Q

Very high dose glucocorticoid definition:

A

> 100mg prednisone equiv per day

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11
Q

Pulse therapy glucocorticoid definition:

A

greater than 250mg prednisone equiv per day for 1 day or a few days

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12
Q

Cyclosporine

-type?

A

Calcineurin inhibitors

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13
Q

Cyclosporine

-MOA?

A
  • suppress t-cell mediated immunity - important for transplant rejection and automimunity
  • complex with cycophillin - cytoplasm protein in cells –> binds calcineurin–>prevents NFAT transcrtiption factor from entering nucleus ===> no IL 2 = no t-cell maturation
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14
Q

Cyclosporine

-Uses:

A
  • prophylaxis for Kidney, liver, heart, and other organ transplant
  • tx of graft vs host disease
  • Rheumatoid arthritis that doesnt respond to methotrexate
  • psoriasis
  • not given prior to renal transplants = nephrotoxic
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15
Q

Cyclosporine

-AE?

A
  • *-Renal dysfunction
  • *-hirsutism
  • HTN
  • hyperlipidemia
  • tremor hands and feet
  • dont drink with grapefruit drinkis = inc cyclosporin concentrations
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16
Q

Tacrolimus

-type?

A

Calcineurin inh

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17
Q

Tacrolimus

-MOA?

A

-binds FK-binding protein –> binds calcineurin –> prevents translocation of NFAT to nucleus –> no IL-2

(similar to cyclosporin)

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18
Q

Prefered calcineurin inh bc easier to monitor blood concentration (cyclosporin or tacrolimus)?

A

Tacrolimus

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19
Q

Tacrolimus

-uses?

A

-prophylaxis of allograft rejection in solid organ transplantation

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20
Q

Tacrolimus

- AE?

A
  • neprotox (careful with renal transplants)
  • HTN
  • diabetes melitus (neg effect on beta cells)
  • neurotox
  • do not take with grapefruit juice = dangerousl high blood oncentrations bc CYP3A enzymes inhibited
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21
Q

Azathioprine

-what is it?type?

A
  • anti-proliferative/metabolic agent

- purine antimetabolite –> inh lymphocyte proliferation

22
Q

Azathioprine

-MOA?

A

1) metabolized 6-MP –> comvereted to other stuff–> this other stuff incorporated into DNA ==> inh lymph proliferation
2) blocks de-novo synth of purine
- -> lymphs do not have a significant pure salvage pathway

23
Q

Azathioprine

-AE?

A

1) BONE MARROW SUPPRESSION
- leukopenia, anemia, thrombocytopenia
2) liver tox
3) inc susceptibility to HSV and VZV
4) Inc risk of cancer -lymphoma

NEED TO MONITOR CBC AND LIVER FUNCTION!

24
Q

Azathioprine

-uses:

A
  • 1) prevention of organ transplant rejection
  • 2) severe cases of rheumatoid arthritis
    3) some CD, MS, and prednisone resistant antibody mediated idiopathic thrombocytopenic purpura and autoimmune hemolytic anemias
25
Q

Mycophenolate mofetil

  • type?
  • characteristics probably not worth knowing?
A
  • Anti-proliferative/metabolic agent
  • newer than azathioprine
  • delayed release tablet releases drug in intestines
26
Q

Mycophenolate mofetil

-MOA?

A
  • prodrug = rapidly hydrolyze to mycophenolic acid (MPA)
  • MPA - selective inh of inosine monophos dehydrogenase –> need to de-novo synth of guanine nucleotides
  • B and T cells use this path and have no salvage compared to other cells
27
Q

Azothioprine inh?

Mycophenolate mofetil inh?

A
  • blocks de-novo synth of purines

- blocks denovo synth of guanine

28
Q

Mycophenolate modefil

-uses?

A
  • prophylaxs of transplant rejection
  • combo with glucocorticoids and calcineurin inh - lower doses of glucocortcoids needed
  • off label to treat lupus
29
Q

Mycophenolate Modefil

-AE?

A

-hematologic issues
-GI usual
^^(better than azathioprine)
-inc infection with CMV
-congenital abnormalities - cleft lip, heart defects and pregnancy loss

30
Q

Inc risk of CMV infectin with?

Inc risk of VZV and HSV inf with?

A
  • Mycophenolate Modefil

- Azathioprine

31
Q

Serolimus

  • type?
  • use?
A
  • Anti-proliferative/metabolic

- protects kidney from nephro toxic effects of calcineurin inh - combo therapy!

32
Q

Serolimus

-MOA?

A
  • binds FKBP (like tacrolimus) –> BUT NOT INHIBITING CALCINEUIN
  • INSTEAD binds to protein kinase mTOR ==> stops cell cycle progression in lymphocytes (G1 to S)
33
Q

mTOR inh=

A

serolimus

34
Q

Serolimus

-uses?

A
  • prophylaxis of organ transplant rejection IN COMBO with glucocorticoids and a reduced dose of calcineurin inh
  • good in renal transplant patients that cant tolerate calcineurin inh bc of kidney toxicity
35
Q

Serolimus

-AE?

A
  • delayed wound healing*
  • hypokalemia
  • anemia,leukopen,thrombocytop
  • GI
  • inc risk of infections
  • increase cancer - lymphoma
36
Q

Antithymocyte globulin

-what is it?

A

-rabbit serum containing purified gama globulin specific to human thymocytes

37
Q

most commonly used llymphocyte depleting agent?

A

antithymocyte globulin

38
Q

Antithymocyte globulin

-MOA?

A

-basically antibodies that bind a whole bucnh of inflammatory and growth factors on T-LYMPHOCYTES
ESP CD3!!!! NEED CD3 TO MAKE T_CELLS WORK- we get rid of this
To get rid of:
-Complement mediated cytotox = lysing lymphocytes
inh of lymph funcitons by bindibg to cell

39
Q

Antithymocyte lobulin

-USES?

A
  • induction immunosuppression - after transplant
  • prophylactic immunosuppression
  • tx of acute rejection of solid organ transplants IN COMBOwith other drugs
40
Q

Antithymocyte globulin AE:

A
  • fever chlls and that shit
  • serum sickness
  • anaphylaxis
  • leukopenia and thrombocytop
  • malignancy -lymphoma probs
  • infection
41
Q

Muromonab-CD3

-type/info?

A
  • biological - from mouse

- CD3 is important for T-cell activation!!

42
Q

Muromonab-CD3

-MOA?

A

-antibodies againsts CD3
Functionally get rid of lymphocytes: bind CD3 on membrane
Literally get rid of lymphocytes complement mediated destruction

43
Q

Great for glucocorticoid resistant organ transplant reaction episodes?

A

muromonab-CD3

44
Q

Muromonab Cd3

-uses:

A
  • glucocorticoid resistant organ transplant reaction episodes
  • repeat treatment course with drug not useful = human makes antibody for the mouse antibodies
45
Q

Muromonab CD3

-AE?

A

-cytokine storm: within 30 min inflammatory cytokines tnf-a and interferon-y = chills, fever… that shit –> helps to give glucocorticoid first

  • vomit, diarrhea,, tha shit
  • anaphylaxis, pumonary arrest….
46
Q

Anti-TNF-alpha reagents

-drugs in this category?

A
  • inflixmab
  • adalimumab
  • etanercept

-good for treating conditions with TNF-alpha mediated inflammation (CD and Rheum arthritis)

47
Q

Anti-TNF-alpha reagents

-MOA?

A

-bindsTNF-alpha = prevent from binding its receptor

48
Q

Infliximab - derived from?

A

-chimeric human constant region and mouse variable (binding) region

49
Q

Adalimumab - what is it?

A

-recomb human IgG1 monoclonal

50
Q

Etanercept - what is it?

A

contains ligand-bidning portion of a human TNF-alpha receptor fused to Fc proteion of IgG1

(part antibody part TNF-a)
ALL HUMAN

51
Q

Anti-TNF-alpha reagents

-uses:

A

-rheumatoid arthritis
-CD
-UC
plaque psoriasis

52
Q

anti-TNF-a reagent AE?

A
  • inc risk for serious infections

- inc risk for lymphomas and other malignancies

Pharm Exam 4 (10 decks)

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