Immunosuppressants

Question 1

Cyclosporin

Answer 1

Calcineurin inhib --> binds cyclophilin
blocks T-cell activation by preventing IL-2 ascription
Ind: xsplant / psoriasis / RA
SE: NEPHROTOXIC
HTN
hyperlipidemia
hyperglycemia
tremor
hirsutism
gingival hyperplasia

Question 2

Tacrolimus (-limus drugs)

Answer 2

Calcineurin inhibitor --> binds FK506 binding protein
prevents IL-2 xscription
Ind: xsplant
SE: sim to cyclosporin
inc risk of DM and neurotic
no gingival hyperplasia or hirsutism

Question 3

Sirolimus (Rapamycin)

Answer 3

mTOR inhib --> binds FKBP
prevents IL-2 signal xsduction
Ind: kidney xsplant
SE: anemia
thrombocytopenia
leukopenia
insulin resistance
hyperlipidemia
non-nephro
synergistic with cyclosporin

Question 4

Basiliximab

Answer 4

monoclonal Ab
blocks IL-2R
Ind: kidney xsplant
SE: edema
HTN
tremor

Question 5

Azathioprine

Answer 5

antimetab precursor of 6-mercaptopurine
inhib lympho prolif –> blocks NT synth
Ind: xsplant / RA / Chrohn Dz / glomerulonephritis / other autoimmune conditions
SE: leukopenia / anemia / thrombocytopenia
deg by xanthine oxidase
allopurinol inc toxicity

Question 6

Glucocorticoids

Answer 6

inhib NF-kB –> suppress T and B cell f(x)
Ind: xsplant / inflammation / autoimmune disorders
SE: you know
also iatrogenic Cushing syndrome