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Pharmacology > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

Antithymocyte globulin drug class

A

Polyclonal IgG

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2
Q

Muromanab-CD3 class

A

co-stimulatory molecules

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3
Q

Belatacept class

A

co-stimulatory molecules

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4
Q

Daclizumab drug class

A

CD25 inhibitors

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5
Q

Basiliximab drug class

A

CD25 inhibitors

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6
Q

Alemtuzumab drug class

A

CD52 inhibitors

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7
Q

Cyclosporine class

A

Calcineurin inhibitors

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8
Q

Tacrolimus drug class

A

Calcineurin inhibitors

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9
Q

Pimecrolimus drug class

A

Calcineurin inhibitors

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10
Q

Methylprednisolone drug class

A

Steroids/nuclear transcription inhibitors

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11
Q

Mycophenolate mofetil class

A

cell cycle disruptors

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12
Q

Azathioprine class

A

cell cycle disruptors

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13
Q

Methotrexate class

A

cell cycle disruptors

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14
Q

Cyclophosphamide class

A

cell cycle disruptors

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15
Q

Name some drug classes used for maintenance transplant therapy

A

Calcineurin inhibitors, anti-proliferatives, steroids

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16
Q

What is the order of transplant organs to generate a rejection response?

A

Lung > heart > kidney > liver

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17
Q

Describe organ responses to immunopharmacologic agents

A

Renal - very good; heart - good; liver - fair; bone marrow - good

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18
Q

Describe common issues for antibody immunosuppressants

A

1) Opportunistic infections; 2) Need anti-infective prophylaxis; 3) Malignancy/LPD; 4) Cytokine-release syndrome

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19
Q

Muromanab target

A

CD3

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20
Q

Belatacept target

A

CD80/86 (B7)

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21
Q

CD25 is also known as

A

IL-2 receptor

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22
Q

Daclizumab target

A

Il-2 receptor (CD25)

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23
Q

Basiliximab target

A

IL-2 receptor (CD25)

24
Q

Alemtuzumab target

A

CD52

25
Q

Cyclosporine target

A

Cyclophilin

26
Q

Tacrolimus target

A

FKBP12

27
Q

Sirolimus target

A

FKBP12

28
Q

Sirolimus class

A

mTOR inhibitors

29
Q

Mycophenolate target

A

inosine monophosphate dehydrogenase

30
Q

Azathioprine target

A

Metabolite blocks DNA synthesis and induces apoptosis

31
Q

Methotrexate target

A

Dihydrofolate reductase

32
Q

If lactating, the patient should avoid these immunosuppressants

A

Cyclophosphamide; methotrexate; azathioprine; tacrolimus; cyclosporine

33
Q

Globulin immunosuppressants are all lymphocyte depleting, except for this class of them (give drug members)

A

CD25 inhibitors Daclizumab and Basilixiumab

34
Q

Calcineurin inhibitors MOA

A

Inhibit first phase of T cell activation (IL-2 and IL-4 production)

35
Q

mTOR inhibitors MOA

A

Inhibits 2nd phase of T-cell activation; prevents B-cell differentiation and decreases IgM, IgG, IgA

36
Q

Cyclosporine MOA

A

Binds to cyclophilin and together inhibits calcineurin which is required for IL-2 transcription

37
Q

Tacrolimus MOA

A

Binds to FKBP12 (similar to cyclophiln) which is required for IL-2 transcription

38
Q

Calcineurin inhibitors side effects

A

Nephrotoxicity; hypertension; secondary malignancies

39
Q

Sirolimus MOA

A

Binds FKBP12 and together complexes with mTOR (whereas cyclosporine binds with calcineurin)

40
Q

Sirolimus side effects

A

Hyperlipidemia; thrombo-problems; azotemia; drug target is expressed widely so variety of problems

41
Q

Azathioprine side effects

A

Bone marrow suppression; secondary malignancies; avoid if lactating; lowers INR (Warfarin complication)

42
Q

How does azathioprine work?

A

It’s a purine analog so it inhibits DNA replication and RNA production, selectively in lymphocytes for the most part

43
Q

Mycophenolate mofetil MOA

A

Metabolite is a nucleotide analog that inhibits DNA/RNA synthesis by halting G-MP production; more selective for lymphocytes than azathioprine so it is preferred over it now

44
Q

Mycophenolate mofetil side effects

A

GI issues (diarrhea; N/V; abdominal pain…)

45
Q

These drugs are used to treat acute rejection

A

Antithymocyte globulin; muromanab; methylprednisolone

46
Q

Muromonab MOA

A

Binds to CD3 (TCR signal transduction unit) and destroys T-cell activity

47
Q

These mABs can cause cytokine release upon infusion

A

Muromonab and Alemtuzumab (so watch for anaphylaxis)

48
Q

Daclizumab and Basiliximab MOA

A

Bind to IL-2 receptor

49
Q

This drug is used to prevent immune responses from coronary stents

A

Sirolimus

50
Q

Methylprednisolone/corticosteroids MOA

A

Inhibits transcription of pro-inflammatory factors esp. IL-2 by binding to cytosolic receptors, translocating to nucleus, and inhibit HAT (histone acetyltransferase) directly and by activating HDAC to reverse acetylation (of these pro-inflamm genes)

51
Q

What does mTOR normally do?

A

Part of clonal expansion pathway downstream from IL-2 receptor stimulation

52
Q

Alemtuzumab MOA

A

Anti-CD52 antibody targets T-cell for antibody/complement destruction

53
Q

Atgam MOA

A

Polyclonal IgG opsonizes human T-cells for complement destruction

54
Q

Atgam generic name

A

Anti-thymocyte globulin (polyclonal IgG anti-T-cell)

55
Q

Corticosteroids side effects

A

Cell-surface receptor targets -> rapid neurological issues (insomnia, depression); protein metabolism issues (impaired wound healing, stunted growth); susceptibility to infection (esp TB); hypercholesterolemia; thromboembolism; hypercorticism; aggravation of DM

56
Q

mTOR inhibitor side effects

A

Stunts proliferation of other cell types, inc. smooth muscle cell, hepatocyte, fibroblast bc mTOR is widely expressed in body

Pharmacology (3 decks)

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