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Clinical Pharm Exam 3 > Transplant Therapeutics > Flashcards

Transplant Therapeutics Flashcards

1
Q

What is the goal in general with prescribing drugs for transplant?

A

Use the lowest dose possible

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2
Q

What does triple/maintenance therapy consist of

A
  1. Anti-metabolites: AZA or mycophenolate
  2. Calcineurin inhibitors: cyclosporine or tacrolimus
  3. Prednisone
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3
Q

What drug can be a substitute for 1 and 2 of triple therapy?

A

Sirolimus

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4
Q

What are the anti-metabolite drugs?

A
  • Azathioprine

- Mycophenolate

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5
Q

Azathioprine is a prodrug of

A

6-mercaptopurine

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6
Q

Azathioprine MOA

A

↓ circulating B and T lymphocytes, ↓ IG synthesis, and ↓ IL-2 secretion

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7
Q

Clinical indications azathioprine

A
  • Prophylaxis of organ rejection
  • Active RA
  • Steroid-sparing agent for corticosteroid-dependent IBD
  • Tx of various autoimmune diseases
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8
Q

Where are we more likely to see azathioprine than in transplant pts.?

A

Difficult to manage rheumatologic disorders

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9
Q

What are the various autoimmune disorders AZA can be used to treat?

A
  • Psoriatic arthritis
  • Psoriasis
  • RA
  • Behcet’s dz
  • Polymyositis
  • SLE
  • Sustain remissions in systemic vasculitis
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10
Q

What do we monitor in a pt. on azathioprine?

A
  • CBC w/ diff
  • CMP
  • Thiopurine methyltransferase (TMPT) genotyping or phenotyping
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11
Q

Pt. w/ absent or reduced TMPT are at risk for what?

A

Severe life-threatening myelotoxicity

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12
Q

Why are pt. w/ absent or reduced TMPT at risk for myelotoxicity?

A

These pt. have an inability to degrade the drug fully and clear it; this leads to more immunosuppression

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13
Q

How do we approach prescribing AZA to pt. that are TMPT homozygous for nonfunctional alleles?

A

Do NOT prescribe

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14
Q

How do we approach prescribing AZA to pt. that are TMPT heterozygous for nonfunctional alleles?

A

Reduce dose

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15
Q

Drug interactions with azathioprine

A
  • Additive immunosuppression w/ other agents
  • ACEI
  • Allopurinol/febuxostat
  • Aminosalicylates (e.g. Mesalamine - IBD drug)
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16
Q

What happens if you use azathioprine with ACEI?

A

May induce anemia & severe leukopenia

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17
Q

What happens if you use azathioprine with allopurinol/febuxostat or aminosalicylates?

A

Increase myelosuppression risk

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18
Q

How does concomitant use of AZA and allopurinol/febuxostat cause increase myelosuppression risk?

A

Slows elimination of 6-MP by inhibiting xanthine oxidase (XO)

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19
Q

How does concomitant use of AZA and aminosalicylates cause increase myelosuppression risk?

A

May inhibit TMPT

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20
Q

Azathioprine ADRs

A
  • N/V, anorexia
  • Hepatotoxicity
  • Pancreatitis
  • Myelosuppression (infeciton, malignancy)
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21
Q

Renal transplant pt. have _____ risk of malignant disease

A

50-100x

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22
Q

Most common tumors associated with renal transplant pt.

A
  • SCC of the skin&raquo_space;»

- NHL

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23
Q

Do we use azathioprine or mycophenolate more commonly?

A

Mycophenolate

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24
Q

Mycophenolate MOA

A

↓ B and T cell proliferation

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25
Clinical indications mycophenolate
- Prophylaxis of organ rejection in pts receiving allogenic renal, cardiac, or hepatic transplants - Tx of lupus nephritis, psoriasis, myasthenia gravis - Prevention & tx of GVHD
26
Drug monitoring in a pt. on mycophenolate
CBC w/ diff
27
Drug interactions with mycophenolate
- Additive immunosuppression w/ other agents | - Fe, antacids, cholestyramine
28
Adding Fe, antacids, or cholestyramine to mycophenolate does what to the drug and why is this a problem?
Decreases absorption of mycophenolate, increases rejection risk
29
Mycophenolate ADRs
- N/V/D, abd cramping - Myelosuppression - Miscarriages & birth defects (BLACK BOX)
30
What types if birth defects occur in the fetus of a pregnant women on mycophenolate?
- Cleft lip/palate | - Ear deformities
31
What are the calcineurin inhibitor drugs?
- Cyclosporine | - Tacrolimus
32
Are formulations of cyclosporine interchangable?
NO
33
Cyclosporine is available in what formulations?
Solution, tablet, IV, ophthalmic gtt
34
Are "old" or "new" cyclosporines preferred and why?
"New" preferred b/c they have a more reliable Pk profile
35
Cyclosporine MOA
↓ production/release of IL-2 -> inhibits IL-2-induced activation of resting T-lymphs
36
Clinical indications cyclosporine
- Prophylaxis if organ rejection in kidney, liver, & heart transplants - Severe, refractory RA, psoriasis, & IBD - Keratoconjunctivitis sicca-associated ocular inflammation (ophthalmic emulsion)
37
What do we monitor in pt. on cyclosporine?
- Cyclosporine trough levels - CMP - CBC w/ diff - BP - FLP
38
Drug interactions w/ cyclosporine
- Additive immunosuppression w/ other agents - Additive nephrotoxicity w/ other nephrotoxic agents - CYP interactions
39
Cyclosporine is a substrate of CYP____
3A4, also P-gp
40
Cyclosporine is a moderate inhibitor of CYP____
3A4
41
Cyclosporine ADRs
- Nephrotoxicity (AKI) - HTN - Neurotoxicity - Metabolic abnormalities - Myelosuppression - Gingival hyperplasia - Hirsuitism - N/V/D
42
What cyclosporine ADR is the most common & clinically significant?
Nephrotoxicity (reversible after dose reduction)
43
Cyclosporine-induced HTN
- Caused by renal vasoconstriction & Na+ retention - 1st wks of therapy - Usually responds to dose reductions
44
Cyclosporine-induced neurotoxicity
- Severe HA, visual abnl, seizuers r/t acute HTN | - Mild tremor common (35-55%)
45
Cyclosporine-induced metabolic abnormalities
- Glucose intolerance (=post-transplant DM) - Hyperlipidemia - Hyperuricemia (exacerbate gout)
46
Where does tacrolimus come from?
It is a macrolide ABX produced by the bacteria streptomyces tsukubaensis
47
Tacrolimus MOA
↓ production/release of IL-2 -> inhibits IL-2-induced activation of resting T-lymphs *binds to immunophilin instead of cyclophilin
48
Clinical indications tacrolimus
- Immunosuppression for heart, kidney, or liver transplant - Refractory ulcerative colitis - Moderate-to-severe atopic dermatitis*
49
For what clinical indications is the oral/injection form of tacrolimus used?
- Immunosuppression | - Refractory UC
50
For what clinical indications is the topical form of tacrolimus used?
Atopic dermatitis
51
What do we monitor in a pt. on tacrolimus?
- CBC w/ diff - CMP - BP - Drug concentration*
52
Drug interactions w/ tacrolimus
- Additive nephrotoxicity w/ other nephrotoxins | - CYP interactions
53
Tacrolimus is a substrate of CYP___
3A4, also P-gp
54
Tacrolimus ADRs
Similar to cyclosporine | - Nephrotoxicity, myelosuppression....
55
What ADRs are more common with tacrolimus c/t cyclosporine?
- PTDM | - Alopecia
56
What ADRs are more common with cyclosporine c/t tacrolimus?
- Hirsuitism - Gingival hyperplasia - HTN
57
What is our corticosteroid of choice for transplant therapy?
Prednisone
58
Prednisone is a prodrug of
Prednisolone
59
Where in the body is prednisone converted to prednisolone?
In the liver
60
Prednisone MOA
Not fully understood | - Lower doses inhibit cytokine production
61
High doses of prednisone are believed to be
Lymphotoxic
62
Clinical indication of prednisone
Prevention & tx of organ transplant
63
Drug interactions w/ prednisone
- Additive immunosuppression | - Antagonizes effect of anti-DM meds
64
How does prednisone antagonize DM drugs?
Induces hyperglycemia
65
What do we monitor in a pt. on prednisone?
- BP | - Blood glucose
66
Prednisone "acute" ADRs
- Insomnia, nervousness - Increased appetite - Hyperglycemia
67
Prednisone "chronic" ADRs
- Hirsutism - Cataracts - Fat redistribution* (Cushingoid) - Fluid retention - Osteoporosis*/AVN - Poor wound healing - HPA-axis suppression/growth suppression* - Myopathy
68
Pts. on prednisone have the following sx r/t myopathy:
- Proximal muscle weakness | - Muscle wasting
69
Pts. on prednisone DO NOT have the following sx r/t myopathy:
- Myalgias | - Muscle tenderness
70
Which occurs first in pt. on prednisone r/t myopathy: UE or LE weakness?
LE weakness (more severe)
71
What are the implications of LE weakness in pt. on prednisone?
Interferes w/ ADLs
72
Prendisone-induced myopathy is uncommon at what dose?
<10mg/d
73
Prednisone-induced myopathy is common at what dose?
>40-60mg/d for 1 month
74
Prednisone-induced myopathy is a......
Diagnosis of exclusion
75
Sirolimus is an example of what type of drug?
mTOR inhibitor (mammalian target of rapamycin)
76
Sirolimus MOA
Inhibition of mTOR suppresses cytokine-drive T cell proliferation *binds to immunophilin like tacrolimus
77
Clinical indications sirolimus
- Prophylaxis of organ rejection in pts receiving renal transplants - Used in triple therapy maintenance regimens in place of calcineurin inhibitor or antimetabolitc (depends on transplant center)
78
What do we monitor in a pt. on sirolimus?
- Drug concentration - CBC w/ diff - CMP - FLP - BP
79
Sirolimus is a substrate of CYP____
3A4; also P-gp
80
Sirolimus ADRs
- HA - Tremor - HTN - Edema - PTDM - Renal dysfcn * similar to tacrolimus
81
Belatacept MOA
- Select T-cell costimulation blocker | - Inhibits cytokine production
82
Clinical indications belatacept
Prevention of rejection of renal transplant | - Only indicated for use in EBV seropositive pt.
83
Drug interactions w/ belatacept
- Additive immunosuppression
84
Belatacept ADRs
- Leukopenia/anemia, N/V/D (20%) - Myelosuppression (malignancy, infection) - Post-transplant lymphoproliferative disorder (PTLD) possible

Clinical Pharm Exam 3 (4 decks)

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