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STEP 1 > Immunosuppressant Drugs > Flashcards

Immunosuppressant Drugs Flashcards

1
Q

Mechanism of cyclosporine

A

calcineurin inhibitor
binds cyclophilin
Blocks T-cell activation by preventing IL-2 transcription

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2
Q

Use of cyclosporine

A

transplant rejection prophylaxis, psoriasis, rheumatoid arthritis

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3
Q

Toxicity of cyclosporine

A

NEPHROTOXICITY

hypertension, hyperlipidemia, neurotoxicity, gingival hyperplasia, hirsutism

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4
Q

Mechanism of tacrolimus

A

calcineurin inhibitor
binds FK506 binding protein (FKBP)
blocks T-cell activation preventing IL-2 transcription

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5
Q

Use of tacrolimus

A

transplant rejection prophylaxis

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6
Q

Toxicity of tacrolimus

A

NEPHROTOXICITY

increased risk of diabetes and neurotoxicity

NO gingival hyperplasia and NO hirsutism

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7
Q

Mechanism of sirolimus

A

mTOR inhibitor that binds FKBP

blocks T-cell activation and B-cell differentiation by preventing response to IL-2

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8
Q

Difference between mechanism of cyclosporine/tacrolimus versus sirolimus in terms of IL-2

A

cyclosporine/tacrolimus prevent TRANSCRIPTION of IL-2

sirolimus prevents RESPONSE to IL-2

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9
Q

Use of sirolimus

A

kidney transplant rejection prophylaxis (because spares kidney)

synergistic with cyclosporine
Used in drug-eluting stents

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10
Q

Toxicity of sirolimus

A

anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia

NO nephrotoxicity

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11
Q

What are the IL-2R monoclonal antibodies?

A

Daclizumab and Basiliximab

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12
Q

Mechanism of daclizumab and basiliximab

A

monoclonal antibodies against IL-2R

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13
Q

Use of daclizumab and basiliximab

A

kidney transplant rejection prophylaxis

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14
Q

Toxicity of daclizumab and basiliximab

A

edema, hypertension, tremor

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15
Q

Mechanism of azathioprine

A

Antimetabolite precursor of 6-mercaptopurine

inhibits lymphocyte proliferation by blocking nucleotide synthesis

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16
Q

Use of azathioprine

A

transplant rejection prophylaxis, RA, Crohn’s disease, glomerulonephritis, autoimmune conditions

17
Q

Toxicity of azathioprine

A

leukopenia, anemia, thrombocytopenia

18
Q

Special consideration when using azathioprine

A

6-MP degraded by xanthine oxidase; toxicity increased by allopurinol which blocks xanthine oxidase

Do not use in GOUT patients on allopurinol or consider dose reduction

19
Q

Mechanism of glucocorticoids

A

inhibit NF-kappaB

suppress both B and T cell function by decreased transcription of many cytokines

20
Q

Use of glucocorticoids

A

transplant rejection prophylaxis (immunosuppression)
many autoimmune disorders
inflammation

21
Q

Toxicity of glucocorticoids

A

Hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, HTN, cataracts, avascular necrosis

Can cause IATROGENIC Cushing syndrome

STEP 1 (26 decks)

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