Immunosuppressants

Question 1

Toxicities of sirolimus (rapamycin)

Answer 1

Hyperlipidemia, Anemia, Leukopenia, Thrombocytopenia, Fever, GI effects

Question 2

CyclosporineA

Answer 2

1) BLOCKS calcineurin (phosphatase) -> Activates Tx of IL-2R genes
Acts on T cells to inhibit TCR activation and Cytokine Induction
2) BLOCKS IgE mediated mast cell degranulation
3) STIMULATES TGF-beta expression: Inhibitory cytokine
**KIDNEY TOXICITY

Question 3

Tacrolimus (FK506)

Answer 3

BLOCKS calcineurin used for IL-2R Tx activation
Acts on T cells to inhibit TCR activation and induction of cytokines
FKBP/FK506 Complex binds to and blocks calcineurin
**Same action as CsA but used as an alternative since it does not have kidney toxicity

Question 4

Two drugs that can bind to FKBP12 to prevent action of calcineurin

Answer 4

Tacrolimus (FK506)

Sirolimus (rapamycin)

Question 5

Tacrolimus

Answer 5

FK506

Question 6

Sirolimus

Answer 6

Rapamycin

Question 7

Two drugs that block calcineurin

Answer 7

CsA + Tacrolimus (FK506)

Question 8

Immunosuppressant Drugs that blocks T cell proliferation (IL-2)

Answer 8

1) mTOR inhibitors (Sirolimus and Everolimus)
2) Cytotoxic Drugs that inhibit Purine biosynthesis (Azathioprine, Mycophenolate Mofetil)
3) Dacluizmab - Prevents binding of IL-2 to its receptor

Question 9

Drug (acts like CTLA4-IgG) - Binds CD80(B7)/CD86 [APC] and prevents it from binding to CD28 (Tcell)

Answer 9

Abatacept [CTLA4-IgG]

Question 10

Another R.A. drug that acts as an anti-TNFalpha agent

Answer 10

Adalimumab (Humira)

Question 11

Sirolimus (Rapamycin)

Answer 11

T cell blocker by BLOCKING mTOR kinase (Needed for cytokine signaling)
Prophylaxis of organ rejection
Used with Calcineurin inhibitors and glucocorticoids