Drugs used in Organ Transplantation Flashcards

1
Q

Glucocorticoids MOA is…

A

suppress distribution and reactivity of lymphoid and myloid cells

catabolic actions at GRE

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2
Q

The main use of glucocorticoids is…

A

acute use when needed or early on, or in emergencies

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3
Q

Antithymocyte Globulin (ATG) and Antilymphocyte Globulin (ALG)

A

MOA- polyclonal suppression of thymocytes (T) or lymphocytes (T&B, NK cells)

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4
Q

The administration of what drugs allows early temporary withdrawal of all other drugs?

A

ATG and ALG

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5
Q

Muromonab-CD3 (OKT-3)

A

Is a MAB against the T- cell receptor

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6
Q

Alemtuzumab

A

human MAB against Cd52 on lymphocytes, monocytes, macrophages, NK

Prolonged T and B cell depletion

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7
Q

What drug is used in CLL?

A

Alemtuzumab

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8
Q

Daclizumab and Basiliximab

A

humanized and chimeric MABs against IL-2 receptor on T-cell

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9
Q

Daclizumab and Basiliximab are used more for…

A

acute renal rejections

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10
Q

Abatacept and Belatacept

A

Fusion of Fc of IgG1 and CTLA-4 –> binds to CD80/CD86 –> suppression of T-cell activation

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11
Q

Thalidomide

A
  • stimulates and changes specificity of T-cells
  • suppresses B-cells
  • stimulates T-cells but in an immunomodulatory fashion
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12
Q

What are two calcineurin inhibitors?

A

Cyclosporine (CSA)

Tacrolimus (FK-506)

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13
Q

Calcineurin inhibitors…

A

block signal transduction activating t-cells

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14
Q

What does Cyclosporine bind to?

A

Cyclophilin

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15
Q

What does tacrolimus bind to?

A

FK-506BP12

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16
Q

What are the two antiproliferative agents?

A

Sirolimus (Rapamycin)

Everolimus

17
Q

Sirolimus and Everolimus…

A

inhibit mTOR kinase activity –> prevents CDK2 phosphorylation –> blocks cell cycle progression in T-cells

18
Q

Sirolimus and Everolimus have drug-drug interactions at what enzyme?

19
Q

What antimetabolites are used for organ transplantation?

A

Mycophenolate Mofetil

Azathioprine

20
Q

MMF

A

is a prodrug

21
Q

What is MMF converted to in order to become active?

A

mycophenolic acid

22
Q

What is the MOA of MMF?

A

inhibits T and B cell inosine monophosphate dehydrogenase in purine pathway for GMP synthesis

23
Q

What is the active form of azathioprine?

24
Q

What is the MOA of 6-MP or AZA?

A

inhibits ATP and GTP synthesis

25
What recurrent symptom is seen with cyclosporine use?
gum hyperplasia in heart transplant patients
26
Lip hypertrophy is seen with cyclosporine (CsA) and is reversed with...
Tacrolimus (FK506 inhibitor)
27
Tacrolimus binds FK506 first and then binds and inhibits...
PP2B- phosphatase activity of calcineurin
28
What drug is associated with diabetogenesis when combined with glucocorticoids?
Tacrolimus
29
What is mTOR?
a serine/threonine protein kinase inhibited by sirolimus
30
What drugs prevent de novo purine synthesis which is important for B- and T- cells?
MMF
31
When combined with AZA, what drug needs to have a dose reduction due to inhibition of xanthine oxidase?
Allopurinol- used for hyperuricemia and crystalluria associated with cell death/gout therapy