Immunosuppressant Drugs Flashcards Preview

STEP 1 > Immunosuppressant Drugs > Flashcards

Flashcards in Immunosuppressant Drugs Deck (21)
1

Mechanism of cyclosporine

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

2

Use of cyclosporine

transplant rejection prophylaxis, psoriasis, rheumatoid arthritis

3

Toxicity of cyclosporine

NEPHROTOXICITY

hypertension, hyperlipidemia, neurotoxicity, gingival hyperplasia, hirsutism

4

Mechanism of tacrolimus

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

5

Use of tacrolimus

transplant rejection prophylaxis

6

Toxicity of tacrolimus

NEPHROTOXICITY

increased risk of diabetes and neurotoxicity

NO gingival hyperplasia and NO hirsutism

7

Mechanism of sirolimus

mTOR inhibitor that binds FKBP
blocks T-cell activation and B-cell differentiation by preventing response to IL-2

8

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

cyclosporine/tacrolimus prevent TRANSCRIPTION of IL-2

sirolimus prevents RESPONSE to IL-2

9

Use of sirolimus

kidney transplant rejection prophylaxis (because spares kidney)

synergistic with cyclosporine
Used in drug-eluting stents

10

Toxicity of sirolimus

anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia

NO nephrotoxicity

11

What are the IL-2R monoclonal antibodies?

Daclizumab and Basiliximab

12

Mechanism of daclizumab and basiliximab

monoclonal antibodies against IL-2R

13

Use of daclizumab and basiliximab

kidney transplant rejection prophylaxis

14

Toxicity of daclizumab and basiliximab

edema, hypertension, tremor

15

Mechanism of azathioprine

Antimetabolite precursor of 6-mercaptopurine
inhibits lymphocyte proliferation by blocking nucleotide synthesis

16

Use of azathioprine

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

17

Toxicity of azathioprine

leukopenia, anemia, thrombocytopenia

18

Special consideration when using azathioprine

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

Mechanism of glucocorticoids

inhibit NF-kappaB
suppress both B and T cell function by decreased transcription of many cytokines

20

Use of glucocorticoids

transplant rejection prophylaxis (immunosuppression)
many autoimmune disorders
inflammation

21

Toxicity of glucocorticoids

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

Can cause IATROGENIC Cushing syndrome