Immunosupressants

Question 1

Inhibit enzyme in purine synthesis through inhibition of inosine monophosphate dehydrogenase

Answer 1

Mycophenalte motefil (MMF)

Mycophenolate sodium (MPS)

Question 2

Mycophenolate motefil

Answer 2

Anti-proliferative

Inhibits purine synthesis: inhibits inosine monophosphate dehydrogenase

More selective and effective vs azathioprine

Blocks T-cell and B-cell proliferation

Prevents smooth muscle proliferation - also beneficial in preventing chronic rejection

Question 3

Non-specific blockade of nucleic acid synthesis

Answer 3

Azathioprine

Non-specific

Question 4

Azathioprine

Answer 4

Anti-proliferative

Blocks nucleic acid synthesis

Non-specific: affects all rapidly dividing cells
i.e. T cells undergoing clonal expansion

Question 5

Inhibit T cell activation by inhibiting IL-2 gene transcription

Answer 5

Calcineurin inhibitors

Ciclosporin
Tacrolimus

Question 6

Ciclosporin and Tacrolimus

Answer 6

Both drugs are calcineurin inhibitors and fungal products

Inhibit T cell activation by blocking IL-2 gene transcription

–> inhibit cytotoxic T cell generation

Both nephrotoxic - requiring blood level monitoring as nephrotoxicity is level-dependent

Question 7

Macrolide antibiotic that blocks mTOR

Answer 7

Rapamycin (sirolimus)

Blocks mTOR

Question 8

Rapamycin

Answer 8

Macrolide antibiotic

Blocks protein-designated mammalian target of rapamycin (mTOR)

–> inhibition reduces cytokine-dependent cellular proliferation at G1 to S phase of cell division cycle

–> thereby blocking T-cell activation

Non-nephrotoxic
Impairs wound healing

Question 9

Anti-IL-2R

Answer 9

Basiliximab

Daclizumab