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Immunosuppressants Flashcards

1
Q

MOA? - Muronomab-OKT3

A

CD3, prevents T cell activation

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2
Q

MOA? - Basiliximab (Simulect)

A

IL-2 receptor (CD25)

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3
Q

MOA? - Rabbit ATG (Thymoglobulin)

A

Sledgehammer (a lot of antigenic targets) (lymphocyte depletion)

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4
Q

MOA? - Belatacept (NULOJIX)

A

CD80/86 …. a.k.a. B7, prevents T cell activation

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5
Q

MOA? - Cyclosporine

A

Calcineurin Inhibitor (prohibits dephosphorylation of NFAT)

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6
Q

MOA? - Tacrolimus

A

Calcineurin Inhibitor (Binds to FKBP12)

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7
Q

MOA? - Methylprednisolone

A

Corticosteroid (Transcriptional modifications)

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8
Q

MOA? - Prednisone

A

Corticosteroid (Transcriptional modifications)

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9
Q

MOA? - Prednisolone

A

Corticosteroid (Transcriptional modifications)

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10
Q

MOA? - Dexamethasone

A

Corticosteroid (Transcriptional modifications)

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11
Q

MOA? - Sirolimus

A

mTOR inhibitor (FKBP12)

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12
Q

MOA? - Everolimus

A

mTOR inhibitor (FKBP12)

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13
Q

MOA? - Mycophenolate

A

Cell-Ctyle disruptors (inosin monophosphate dehydrogenase inhibitor) (more selective than the other cell cycle disruptors)

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14
Q

MOA? - Azathioprine (and 6-MP)

A

Cell-Cycle Disrupter (6-thioguanine triphosphate)

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15
Q

MOA? - Cyclophosphamide

A

Pro-Drug - Alkylating agent

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16
Q

MOA? - Methotrexate (MTX)

A

Cell Cycle Disruptor (Dihydrofolate reductase inhibitor)

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17
Q

MOA? - Three Mentioned CYP3A4 related Immunosuppressants

A

Cyclosporine, Tacrolimus, Sirolimus

18
Q

Metabolized by CYP34A

A

Cyclosporine*****, Tacrolimus, Sirolimus

19
Q

Which two classes are used for high-dose, rescue, rejection therapies?

A

Corticosteroids (“-ones”) and Anti-lymphocyte antibodies)

20
Q

Lecture Question -Which of the following immunosuppressants works by inhibiting cell cycling in T-Lymphocytes? Azathioprine, Cyclosporine, Muromonab, Thymoglobulin, Sirolimus?

A

Azathioprine

21
Q

The use of which of the following drugs would result in a marked reduction in lymphocyte count? Basiliximab, Prednisone, Thymoglobulin, Mycophenolate, Methotrexate

A

Thymoglobulin

22
Q

Side Effects - Causes Hirsutism

A

Cyclosporine*, Spironolactone, Selegiline

23
Q

Side Effects - Causes Gingival Hyperplasia

A

Cyclosporine*, Ca+2 Channel Blockers, Phenytoin

24
Q

What are the seven drug targets for Immunosuppressive therapy?

A

Gene Expression, Clonally Expanding cells, Intraceullular signals, T-Cell Activation receptors/cytokines, Depletion of T-Cells, Co-stimulation inhibitors, Inhibiting lymphocyte-target interaction

25
Q

Immunosuppresive Triple Therapy Scheme

A

Calcineurin inhibitor, anti-proliferative, steroid

26
Q

Monoclonal Antibodies - “o”

A

Murine - entirely

27
Q

Monoclonal Antibodies - “xi”

A

chimeric - Human constant, Murine Variable

28
Q

Monoclonal Antibodies - “zu”

A

Humanized - Human all but complement determining region

29
Q

Monoclonal Antibodies - “u”

A

Human - all human

30
Q

Trademark Side effects - Requires Patient to be Epstein-Barr virus positive

A

Belatascept

31
Q

Trademark Side effects - Black Box Warning for Angioedema, Hypovolemia, Seizures

32
Q

Trademark Side effects - Contraindicated for those with Horse/Rabbit allergies

A

Thymoglobulin

33
Q

Trademark Side effects - Class of Immunosuppressants known for Renal Toxicity

A

Calcineurin inhibitors

34
Q

Trademark Side effects - Black Box Warning for Mild to Moderate HTN, increased sympathetic tone, renal vasoconstriction

A

Cyclosporine

35
Q

Trademark Side effects - Neurotoxicity (headache, insomnia, tremor, paresthesias, dizziness)

A

Tacrolimus

36
Q

Trademark Side effects - Myelosuppressive, Category D drug that should be avoided with UV radiation

A

Azathioprine

37
Q

Trademark Side effects - Dose-related hyperlipidemia

A

Sirolimus (additionally, hepatotoxicity and negative renal function)

38
Q

Trademark Side effects - Increased toxicity due to Allopurinol

A

Azathioprine

39
Q

Trademark Side effects - Fibrosis of bladder, reduced sperm count, cardiovascular toxicity, pulmonary fibrosis

A

Cyclophosphamide

40
Q

Trademark Side effects - Causes numerous hematological events (

A

Methotrexate

41
Q

Trademark Side effects - Category X - Preganancy

A

Methrotrexate

42
Q

Trademark Side effects - Cell Cycle Disruptors can be used in pregnancy?

A

Simply, no. All Cat D except Methrotrexate Cat X

Pharmacology (6 decks)

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