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Pharmacology > Immunosuppressants/Chemotherapy > Flashcards

Immunosuppressants/Chemotherapy Flashcards

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
Q

Mycophenolate-mofetil inhibits what?

A

inhibits purine synthesis in T and B lymphocytes and Ab formation in B cells

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26
Q

The three cytotoxic agents are…

A

azithioprine

MTX

Cyclophosphamide

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27
Q

Azithioprine and MTX are both what type of drugs…

A

antimetabolites

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28
Q

cyclophosphamide is what type of cytotoxic agent?

A

alkylating agent

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29
Q

What metabolizes azathioprine?

A

xanthine oxidase

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30
Q

what drug for hyperuricemia inhibits xanthine oxidase, and therefore shouldn’t be administered with azithioprine?

A

allopurinol

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31
Q

How does Azithioprine achieve cytotoxic status?

A

inhibits purine synthesis to inhibit DNA/RNA synthesis

induces apoptosis of activated T and B lymphocytes

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32
Q

azathioprine is used for immunosuppression in what patients?

A

transplant patients in combo with CS and other cytotoxic agents

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33
Q

Azathioprine has what side effects?

A

bone marrow suppression, teratogenic

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34
Q

MTX inhibits purine synthesis how?

A

inhibits dihydrofolate reductase

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35
Q

can MTX be used in pregnancy?

A

no… can cause fetal death

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36
Q

what side effects come with MTX?

A

bone marrow suppression, stomatitis, fetal death

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37
Q

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

A

cyclophosphamide

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38
Q

This drug can be combined with Mesna in order to prevent hemorrhagic cystitis, a potentially life threatening side effect.

A

Cyclophosphamide

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39
Q

cyclophosphamide has what two side effects?

A

hemorrhagic cystitis, infertility

40
Q

MESNA is often administered alongside cyclophosphamide to prevent hemorrhagic cystitis. What is the mechanism of action of MESNA?

A

acrolein inhibitor

41
Q

simulect, humira, orencia, and enbrel are what type of biologic?

A

monoclonal antibody immunosuppressives

42
Q

This T-Cell directed drug binds to IL-2 receptors on activated T-cells, which inhibits IL-2 activation

A

simulect

43
Q

Simulect can reduce renal rejection by what percent?

A

50%

44
Q

When is simulect administered during transplant?

A

at the time of transplant to induce immunosuppresion

45
Q

Psoriasis and RA can be treated systemically with what 3 drugs?

A

cyclosporine, MTX and biologics (enbrel, orencia, humira)

46
Q

This biologic drug competes with CD28 to bind to CD80. This prevents the signal required for T-cell activation

A

orencia

47
Q

Common side effects of biologics?

A

infections including and headache

48
Q

these two biologics neutralize the biological activity of TNF-alpha

A

humira and enbrel

49
Q

humira is a ________ and enbrel is a _________ . They both function to neutralize biological activity of TNF-alpha

A

Humira = Ab

Enbrel = fusion protein

50
Q

enbrel and humira are commonly used to treat what conditions?

A

plaque psoriasis

51
Q

this drug is a recombinant of G-CSF

A

Neupogen

52
Q

What is a common side effect of neupogen?

A

bone pain

53
Q

Neupogen can be used to treat what condition that is induced by stem cell transplant/chemo?

A

neutropenia (neupo = neutropenia)

54
Q

epogen is a recombinant form of what hormone?

A

EPO

55
Q

this drug is used for treatment of severe anemia.

A

epogen

56
Q

what are two side effects of epogen administration?

A

increased risk of thrombosis/stroke and HTN

57
Q

these drugs generally cause widespread immunosuppression

A

CS (prednisone)

58
Q

these drugs are useful for organ transplantation because they don’t cause bone marrow suppression

A

t-cell suppressant (cyclosporine, tacrolimus, sirolimus)

59
Q

These drugs have side-effects and will cause bone marrow suppression

A

cytotoxic drugs (azathioprine, cyclophosphamide, MTX)

60
Q

this category are well tolerated and used to “prime” the immunosuppression just before transplant

A

monoclonal Abs (simulect, humira, enbrel)

61
Q 
Cyclophosphamide
mechlorethamine
carmustine
cisplatin 
doxorubicin...

These drugs do what to DNA?

A

DNA alkylation

62
Q

MTX
6-Merca
5-FU

are all examples of __________ inhibitors

A

antimetabolites, S-phase inhibitors

63
Q

Paclitaxel
Vincristine
Vinblastine

These drugs inhibit the _______ phase of mitosis

A

mitosis inhibitors, M-phase inhibition

“Men pay the clittax for the V”

64
Q

This drug inhibits G2-M phase

A

bleomycin

65
Q

this drug targets the BCR-ABL mutation

A

Imantinib

66
Q

_______ targets Ab that binds EGFR

A

Cetuximab

67
Q

_________ blocks EGFR kinase activity

A

erlotinib

68
Q

__________ bind VEGF-R

A

“VEGetable juice is the BEVerage of choice”

bevacizumab

69
Q

This drug forms arcolein-hemorrhagic cystitis

A

cyclophosphamide

70
Q

To avoid hemorrhagic cystitis with cyclophosphamide administration, make sure to administer _________ and ________

A

MESNA and hydration

71
Q

mechlorethamine is toxic to _________

A

renal system

72
Q

This drug can cross the BBB

A

carmustine

73
Q

This drug can cause acoustic nerve damage and is renal toxic

A

cisplatin

74
Q

To reduce renal toxicity with cisplatin, administer ________

A

amifostine

75
Q

this drug is cardiotoxic

A

doxorubicin

76
Q

what further increases the cardiotoxicity of doxorubicin?

A

iron

77
Q

how do you avoid the cardiotoxicity of doxorubicin?

A

administer with dexrazoxane

78
Q

The toxic side effects of these two drugs can be counteracted by Leucovorin rescue

A

MTX, 6-Merca

79
Q

This antimetabolite drug can cause mucositis and thrombocytopenia

A

MTX

80
Q

This antimetabolite drug can cause bone marrow suppression, jaundice and shouldn’t be given with allopurinol

A

6-Merca

81
Q

leucovorin enhances the activity of this antimetabolite drug…

A

5-FU

82
Q

this antimetabolite drug causes oral and GI ulcers

A

5-FU

83
Q

This M phase mitosis inhibitor can cause myelosuppression and anemia

A

Paclitaxel

84
Q

This is the only neurotoxic M Phase Mitosis inhibitor

A

Vincristine

85
Q

The other M Phase mitosis inhibitor that causes myelosuppression, but NOT anemia…

A

Vinblastine

86
Q

This drug is a G2-M Phase inhibitor.

A

Bleomycin

87
Q

A special consideration that makes bleomycin a good choice is that it has low..

A

myelosuppression

88
Q

This G2-M phase inhibitor has the common side effects of hypersensitivity and pulmonary fibrosis

A

Bleomycin

89
Q

Imantinib can cause ________ which is mitigated by its administration with…

A

ankle and periorbital edema

diuretics

90
Q

Imantinib is targeted for what disorder?

A

leukemias

91
Q

This Ab drug can cause acneiform lesions and hypomagnesemia

A

Cetuximab

92
Q

These two drugs can be used after testing for EGFR expression and mutation

A

Cetuximab and erlotinib

93
Q

this drug can cause bleeding and increases risk for thromboembolism

A

bevacizumab

94
Q

because it doesn’t have renal toxicity, which T-Cell inhibitor is a good choice for kindey transplant rejection prophylaxis in combo?

A

sirolimus

95
Q

which antineoplastic is also an antibiotic?

A

doxorubicin

Pharmacology (6 decks)

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