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PPOM1 Block 4 > Lecture 159 > Flashcards

Lecture 159 Flashcards

(67 cards)

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1
Q

What type of immunosuppressant is cyclosporine?

A

Calcineurin inhibitor (CNI)

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2
Q

What type of immunosuppressant is tacrolimus?

A

Calcineurin inhibitor (CNI)

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3
Q

What immunophilin does cyclosporine form a complex with?

A

Cyclophilin

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4
Q

What immunophilin does tacrolimus form a complex with?

A

FKBP

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5
Q

NFAT

A

Nuclear factor of activated T-cells

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6
Q

CNIs form a complex with ____ and ____

A

An immunophilin and a calcineurin

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7
Q

What complex prevents the dephosphorylation and activation of cytosolic NFAT?

A

CNI-immunophilin-calcineurin complex

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8
Q

What transcription factor is critical for regulating gene transcription and the production of cytokines and T-cell receptor-mediated signaling?

A

NFAT

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9
Q

____ is a calmodulin-dependent serine/threonine protein phosphatase

A

Calcineurin

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10
Q

What is the absorption pattern of CNIs?

A

Incomplete and variable absorption

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11
Q

Cyclosporine and tacrolimus are substrates of ____ and _____

A

CYP3A4 and P-gp

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12
Q

How is CNI therapy optimized?

A

Serum level monitoring

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13
Q

What CNI is typically preferred due to lower acute rejection rates?

A

Tacrolimus

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14
Q

What are cyclosporine ophthalmic drops used to treat?

A

Uveitis

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15
Q

What is topical tacrolimus used to treat?

A

Atopic dermatitis and psoriasis

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16
Q
A
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17
Q

What are the therapeutic uses of CNIs?

A

Rejection prophylaxis, GVHD

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18
Q

Why are CNIs prone to causing nephrotoxicity?

A

Vasoconstrictor effect on afferent renal arteriole and interstitial fibrosis of renal parenchyma

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19
Q

Tubular insensitivity to aldosterone and reduced potassium excretion during CNI treatment causes what AE?

A

Hyperkalemia

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20
Q

Gingival hyperplasia and hirsutism are specific AEs of what CNI?

A

Cyclosporine

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21
Q

What metabolic drug interactions are possible with CNI treatment?

A

CYP3A4/P-gp inducers and inhibitors

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22
Q

What CNI reduces mycophenolate serum concentrations?

A

Cyclosporine

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23
Q

Cyclosporine inhibits MRP2 efflux transporter, which inhibits biliary excretion of ____

A

Active mycophenolic acid (MPA)

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24
Q

Mycophenolate mofetil belongs to what class of immunosuppressants?

A

Antimetabolites

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25
Azathioprine belongs to what class of immunosuppressants?
Antimetabolites
26
Mycophenolate mofetil (MMF) is a prodrug of ____
Mycophenolic acid (MPA)
27
What immunosuppressant selectively inhibits inosine monophosphate dehydrogenase (IMPDH)?
Mycophenolate mofetil
28
Inhibition of what enzyme by mycophenolate mofetil blocks the synthesis of guanine monophosphate, suppressing T and B cell proliferation and function?
IMPDH
29
Where is MMF converted to MPA?
In the liver
30
How often is MMF administered?
Twice a day
31
What antimetabolite is typically preferred for transplant rejection prophylaxis?
MMF
32
What are the therapeutic uses of MMF?
Transplant rejection prophylaxis, GVHD, and autoimmune disease
33
What are the main toxicities of MMF?
Bone marrow suppression and GI related symptoms
34
What effect does cyclosporine have on MMF?
Reduces serum level of MMF
35
What effect does cholestyramine have on MMF?
Chelates drug in the gut and reduces absorption
36
What effect do antacids have on MMF?
Reduces absorption, separate administration by two hours
37
Azathioprine is converted to ____ by glutathione-S-transferase
6-mercaptopurine (6-MP)
38
Azathioprine --> 6-MP --> ____ --> 6-TGTP
TIMP
39
How does AZA ultimately lead to cell death?
Downstream toxic nucleotides are incorporated during DNA synthesis
40
What immunosuppressant is metabolized to inactive metabolites by xanthine oxidase (XO) and thiopurine methyltransferase (TPMT)?
AZA
41
How often is AZA dosed?
Once daily
42
Patients deficient in ____ are at risk for severe, life-threatening myelosuppression if treated with AZA
TPMT
43
What are the therapeutic uses for AZA?
Transplant rejection prophylaxis
44
What is the most serious toxicity associated with AZA?
Bone marrow suppression with profound leukopenia
45
What immunosuppressant has been used safely in pregnancy?
AZA
46
What effect do allopurinol/febuxostat have on AZA?
Decrease AZA inactivation, increasing risk of toxicity
47
What class of immunosuppressants does belatacept belong to?
Selective t-cell costimulation blocker
48
What immunosuppressant is a recombinant fusion protein of CTLA-4 that binds to CD80 and CD86 on APCs?
Belatacept
49
Belatacept prevents ____ on T-cells from binding to ____
CD28 from binding to CD80/86
50
How often is belatacept dosed?
IV every 4 weeks
51
What immunosuppressant is used as an alternative for prevention of transplant rejection in EBV seropositive kidney transplant patients with biopsy proven CNI nephrotoxicity?
Belatacept
52
What immunosuppressant has an increased risk of EBV-associated post-transplant lymphoproliferative disorder (PTLD)?
Belatacept
53
Reactivation of JC virus causing PML is an adverse effect of what immunosuppressant?
Belatacept
54
Belatacept is not recommended for use in what specific organ transplant?
Liver transplants
55
Belatacept is contraindicated in patients that are seronegative for ____
EBV
56
What class of immunosuppressants does sirolimus belong to?
mTOR inhibitors
57
What immunosuppressant binds to FK-binding protein (FKBP-12)?
Sirolimus
58
Sirolimus-FKBP complexes block the activity of what cytoplasmic protein kinase?
mTOR
59
What is the ultimate action of sirolimus?
Blocks the IL-2 signal transduction pathway and inhibits T-cell proliferation
60
How is sirolimus metabolized?
CYP3A4, P-gp
61
How is sirolimus dosed?
Orally, twice daily
62
Sirolimus is used as an alternative in patients who cannot tolerate ____
CNIs
63
Sirolimus should not be used in patients who received what two organs?
Liver or lung transplants
64
What immunosuppressant is also used to treat drug-eliminating coronary stents and lymphoangioleiomyomatosis?
Sirolimus
65
What immunosuppressant is known to cause impaired wound healing, hyperlipidemia, and myelosuppression?
Sirolimus
66
Combination of sirolimus and what drug increases the risk of CNI-induced hemolytic uremia syndrome?
Cyclosporine
67
Sirolimus decreases the blood levels and AUC of what other immunosuppressant?
Tacrolimus

PPOM1 Block 4 (44 decks)

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