immunosuppressive drugs Flashcards
1
Q
immunosuppression drugs
A
- steroid sparing: azathioprine, methotrexate, mycophenolic acid
- cyclophosphamide
- ciclosporin A
- tacrolimus
- basiliximab
- belatacept
- sirolimus
2
Q
mycophenolic acid action
A
inhibits IMPDH needed for de novo guanosine synthesis
3
Q
cyclophosphamide action
A
crosslinks guanine to produce 7-alkylguanine, so substitution of A-T for G-C
4
Q
ciclosporin A action
A
- usually antigen + TCR > [Ca2+] increases, activating CaN, which dephosphorylateds NF-AT, which translocates to the nucleus > upregulation of IL2
- CsA binds to CpN and this inhibits CaN
5
Q
tacrolimus action
A
like CsA, binds to FK-binding protein to inhibit CaN
6
Q
basiliximab action
A
against CD25 alpha subunit of IL2 receptor, so IL2 antagonist
7
Q
belatacept action
A
- fusion of CTLA-4 and Fc of human IgG1
- binds CD80/86 of APC
8
Q
name an anti-CD28 antibody. effect?
A
TGN1412, causes cytokine storm because it doesn’t just activate Treg
9
Q
sirolimus action
A
like tacrolimus, binds to FKBP, but binds to mTOR
10
Q
azathioprine - prodrug for, conversions
A
- 6-mercaptopurine
- converted by HPRT to TIMP then
1. by TPMT into 6-methyl-TIMP, inhibits de novo purine synthesis
2. by IMPDH into 6-TGN, incorporated into cellular nucleus acids > inhibition of nucleotide and protein synthesis
