immunosuppressive drugs Flashcards

1
Q

immunosuppression drugs

A
  • steroid sparing: azathioprine, methotrexate, mycophenolic acid
  • cyclophosphamide
  • ciclosporin A
  • tacrolimus
  • basiliximab
  • belatacept
  • sirolimus
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

mycophenolic acid action

A

inhibits IMPDH needed for de novo guanosine synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

cyclophosphamide action

A

crosslinks guanine to produce 7-alkylguanine, so substitution of A-T for G-C

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

tacrolimus action

A

like CsA, binds to FK-binding protein to inhibit CaN

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

basiliximab action

A

against CD25 alpha subunit of IL2 receptor, so IL2 antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

belatacept action

A
  • fusion of CTLA-4 and Fc of human IgG1
  • binds CD80/86 of APC
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

name an anti-CD28 antibody. effect?

A

TGN1412, causes cytokine storm because it doesn’t just activate Treg

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

sirolimus action

A

like tacrolimus, binds to FKBP, but binds to mTOR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly