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Immunosuppressants/Chemotherapy Flashcards

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1
Q

________ is a corticosteroid used for 2-3 months prior to organ transplant?

A

prednisone

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2
Q

Prednisone can be used for long-term immunosuppression. how long does it take for the immunosuppression to take place?

A

several weeks to develop

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3
Q

What are the short term SFx of CS use?

A

hyperglycemia, steroid diabetes

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4
Q

cushings-like syndrome, weight gain, suppression of pituitary-hypothalmus, osteoporosis are SFx of what drug being used in the short or long term?

A

Long term CS use

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5
Q

What are the two classes of T-Cell suppressant?

A

Calcineurin inhibitors and proliferation signal inhibitors

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6
Q

These two T-Cell inhibitors are also calcineurin inhibitors…

A

Cyclosporine and tacrolimus

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7
Q

_______ is the only T-Cell inhibitor that is also a proliferation signal inhibitor….

A

Sirolimus

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8
Q

Do T-Cell suppressants cause bone marrow suppression?

A

no

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9
Q

How is cyclosporine metabolized?

A

CYP3A4

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10
Q

Which drug has many drug interactions and a narrow therapeutic range?

A

Cyclosporine

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11
Q

Grapefruit juice should be avoided with what drug?

A

cyclosporine

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12
Q

Rifampin should be avoided when administering what drug, and why?

A

Cyclosporine due to CYP3A4 induction by rifampin. causes decrease in cyclosporine concentration

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13
Q

Erythromycin and ketoconazole should be avoided when administering which calcineurin inhibitor and why?

A

cyclosporine due to CYP3A4 inhibition, causing increased concentration of cyclosporine

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14
Q

This drug is used in combo with immunomodulators to prevent rejection in organ transplant, in maintenance following an organ transplant, and common in bone marrow transplant…

A

Cyclosporine

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15
Q

This drug has the following toxicities:

Renal toxicity

causes gingival hyperplasia

HTN

Hyperglycemia

CNS Tremors, hallucinations, seizures

A

Cyclosporine

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16
Q

How do Cyclosporine and Tacrolimus work?

A

selective inhibition of T-cells, prevent T-cell activation

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17
Q

what advantages does tacrolimus have over cyclosporine?

A

less toxic

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18
Q

What is DOC for for most organ transplant programs to prevent rejection?

A

tacrolimus

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19
Q

A patient who recently had a kidney transplant is showing signs of rejection. What drug can be used as a rescue?

A

tacrolimus

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20
Q

Tacrolimus exhibits what major adverse effects?

A

nephrotoxicity, HTN, hyperglycemia, tremor, headache, insomnia

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21
Q

This drug is a T-Cell inhibitor that works by inhibiting proliferation of T-cells through binding to mTOR

A

sirolimus

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22
Q

what happens to the T-Cell when sirolimus binds to mTOR

A

t-cell cycle arrests and inhibition of b cell differentiation

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23
Q

Sirolimus is an excellent choice for kidney transplant rejection prophylaxis in combo for what reason?

A

no renal toxicity

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24
Q

what is the main adverse effect of sirolimus

A

increased cholesterol/TAGs

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25
Mycophenolate-mofetil inhibits what?
inhibits purine synthesis in T and B lymphocytes and Ab formation in B cells
26
The three cytotoxic agents are...
azithioprine MTX Cyclophosphamide
27
Azithioprine and MTX are both what type of drugs...
antimetabolites
28
cyclophosphamide is what type of cytotoxic agent?
alkylating agent
29
What metabolizes azathioprine?
xanthine oxidase
30
what drug for hyperuricemia inhibits xanthine oxidase, and therefore shouldn't be administered with azithioprine?
allopurinol
31
How does Azithioprine achieve cytotoxic status?
inhibits purine synthesis to inhibit DNA/RNA synthesis induces apoptosis of activated T and B lymphocytes
32
azathioprine is used for immunosuppression in what patients?
transplant patients in combo with CS and other cytotoxic agents
33
Azathioprine has what side effects?
bone marrow suppression, teratogenic
34
MTX inhibits purine synthesis how?
inhibits dihydrofolate reductase
35
can MTX be used in pregnancy?
no... can cause fetal death
36
what side effects come with MTX?
bone marrow suppression, stomatitis, fetal death
37
This drug is metabolized to phosphoramide mustard, which forms DNA-DNA crosslinks which inactivate DNA. This blocks the response to new antigens and inhibits established immune response
cyclophosphamide
38
This drug can be combined with Mesna in order to prevent hemorrhagic cystitis, a potentially life threatening side effect.
Cyclophosphamide
39
cyclophosphamide has what two side effects?
hemorrhagic cystitis, infertility
40
MESNA is often administered alongside cyclophosphamide to prevent hemorrhagic cystitis. What is the mechanism of action of MESNA?
acrolein inhibitor
41
simulect, humira, orencia, and enbrel are what type of biologic?
monoclonal antibody immunosuppressives
42
This T-Cell directed drug binds to IL-2 receptors on activated T-cells, which inhibits IL-2 activation
simulect
43
Simulect can reduce renal rejection by what percent?
50%
44
When is simulect administered during transplant?
at the time of transplant to induce immunosuppresion
45
Psoriasis and RA can be treated systemically with what 3 drugs?
cyclosporine, MTX and biologics (enbrel, orencia, humira)
46
This biologic drug competes with CD28 to bind to CD80. This prevents the signal required for T-cell activation
orencia
47
Common side effects of biologics?
infections including and headache
48
these two biologics neutralize the biological activity of TNF-alpha
humira and enbrel
49
humira is a ________ and enbrel is a _________ . They both function to neutralize biological activity of TNF-alpha
Humira = Ab Enbrel = fusion protein
50
enbrel and humira are commonly used to treat what conditions?
plaque psoriasis
51
this drug is a recombinant of G-CSF
Neupogen
52
What is a common side effect of neupogen?
bone pain
53
Neupogen can be used to treat what condition that is induced by stem cell transplant/chemo?
neutropenia (neupo = neutropenia)
54
epogen is a recombinant form of what hormone?
EPO
55
this drug is used for treatment of severe anemia.
epogen
56
what are two side effects of epogen administration?
increased risk of thrombosis/stroke and HTN
57
these drugs generally cause widespread immunosuppression
CS (prednisone)
58
these drugs are useful for organ transplantation because they don't cause bone marrow suppression
t-cell suppressant (cyclosporine, tacrolimus, sirolimus)
59
These drugs have side-effects and will cause bone marrow suppression
cytotoxic drugs (azathioprine, cyclophosphamide, MTX)
60
this category are well tolerated and used to "prime" the immunosuppression just before transplant
monoclonal Abs (simulect, humira, enbrel)
61
``` Cyclophosphamide mechlorethamine carmustine cisplatin doxorubicin... ``` These drugs do what to DNA?
DNA alkylation
62
MTX 6-Merca 5-FU are all examples of __________ inhibitors
antimetabolites, S-phase inhibitors
63
Paclitaxel Vincristine Vinblastine These drugs inhibit the _______ phase of mitosis
mitosis inhibitors, M-phase inhibition "Men pay the clittax for the V"
64
This drug inhibits G2-M phase
bleomycin
65
this drug targets the BCR-ABL mutation
Imantinib
66
_______ targets Ab that binds EGFR
Cetuximab
67
_________ blocks EGFR kinase activity
erlotinib
68
__________ bind VEGF-R
"VEGetable juice is the BEVerage of choice" bevacizumab
69
This drug forms arcolein-hemorrhagic cystitis
cyclophosphamide
70
To avoid hemorrhagic cystitis with cyclophosphamide administration, make sure to administer _________ and ________
MESNA and hydration
71
mechlorethamine is toxic to _________
renal system
72
This drug can cross the BBB
carmustine
73
This drug can cause acoustic nerve damage and is renal toxic
cisplatin
74
To reduce renal toxicity with cisplatin, administer ________
amifostine
75
this drug is cardiotoxic
doxorubicin
76
what further increases the cardiotoxicity of doxorubicin?
iron
77
how do you avoid the cardiotoxicity of doxorubicin?
administer with dexrazoxane
78
The toxic side effects of these two drugs can be counteracted by Leucovorin rescue
MTX, 6-Merca
79
This antimetabolite drug can cause mucositis and thrombocytopenia
MTX
80
This antimetabolite drug can cause bone marrow suppression, jaundice and shouldn't be given with allopurinol
6-Merca
81
leucovorin enhances the activity of this antimetabolite drug...
5-FU
82
this antimetabolite drug causes oral and GI ulcers
5-FU
83
This M phase mitosis inhibitor can cause myelosuppression and anemia
Paclitaxel
84
This is the only neurotoxic M Phase Mitosis inhibitor
Vincristine
85
The other M Phase mitosis inhibitor that causes myelosuppression, but NOT anemia...
Vinblastine
86
This drug is a G2-M Phase inhibitor.
Bleomycin
87
A special consideration that makes bleomycin a good choice is that it has low..
myelosuppression
88
This G2-M phase inhibitor has the common side effects of hypersensitivity and pulmonary fibrosis
Bleomycin
89
Imantinib can cause ________ which is mitigated by its administration with...
ankle and periorbital edema diuretics
90
Imantinib is targeted for what disorder?
leukemias
91
This Ab drug can cause acneiform lesions and hypomagnesemia
Cetuximab
92
These two drugs can be used after testing for EGFR expression and mutation
Cetuximab and erlotinib
93
this drug can cause bleeding and increases risk for thromboembolism
bevacizumab
94
because it doesn't have renal toxicity, which T-Cell inhibitor is a good choice for kindey transplant rejection prophylaxis in combo?
sirolimus
95
which antineoplastic is also an antibiotic?
doxorubicin

Pharmacology (6 decks)

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