Immunomodulatory RX (lecture) - Does not include antibody Tx from lecture

Question 1

What is the MoA of cyclosporine?

Answer 1

Bind to calcineurin, blocking NFAT activation (a cytokine transcription factor)

Question 2

Cyclosporine is used in ______, _______, and ______.

Answer 2

Organ transplant, RA, psoriasis

Question 3

What is the primary adverse effect of cyclosporin?

Answer 3

Nephrotoxicity

Question 4

How is cyclosporin metabolized?

Answer 4

Liver - CYP450: Look out for drug interactions (too many to list here)

Question 5

What is another name for Tacrolimus?

Answer 5

FK506

Question 6

What is the MoA of tacrolimus?

Answer 6

calcineurin inhibition leads to inhibition of NFAT activation and cytokine gene transcription

Question 7

What CNI may be used for chronic dry eyes?

Answer 7

Cyclosporine

Question 8

What CNI may be used for atopic dermatitis?

Answer 8

Pimercrolimus

Question 9

What is the MoA of sirolimus?

Answer 9

Inhibit mTOR, leading to decrease in IL-2 induced protein synth

Question 10

What type of transplant is sirolimus used for?

Answer 10

Renal

Question 11

What are the toxic effects of sirolimus?

Answer 11

anemia, thrombocytopenia, hyperlipidemia, HTN

Question 12

What two transplant treatments target purine synthesis, inhibiting lymphocyte proliferation?

Answer 12

Mycophenolate Mofetil

Azathioprine

Question 13

How does mycophenolate mofetil inhibit purine synthesis?

Answer 13

inhibit inosine monophosphate dehydrogenase

http://www.nature.com/nrd/journal/v5/n12/fig_tab/nrd2175_F6.html

Question 14

How does azathioprine interfere with purine synthesis?

Answer 14

It is metabolized to 6-mercaptopurine, which competes with purines, preventing purine synthesis
https://en.wikipedia.org/wiki/Mercaptopurine

Question 15

What is the benefit of mycophenolate mofetil over cyclosporine A?

Answer 15

Less nephrotoxicity

Question 16

What is the prefix of gold compounds?

Answer 16

“Au-“ think of the periodic table

Question 17

Chloroquin is what classification of drug?

Answer 17

Antimalaria (also used to suppress immunity)

Question 18

What are the two first line treatments of RA?

Answer 18

Methotrexate and Leflunomide

Question 19

What is the MoA of methotrexate?

Answer 19

Inhibit DHF reductase (needed for nucleoside synth)

Question 20

What is the MoA of leflunomide?

Answer 20

Inhibit dihydroorotate dehydrogenase (needed for pyrimidine synth)

Question 21

What is the MoA of chloroquine as a DMARD?

Answer 21

Interfere with antigen presentation –> decreased T cell activation

Question 22

What is the MoA of D-penicillamine?

Answer 22

Prevent IL-1 generation and collagen maturation

Question 23

What is the MoA of sulfasalazine as a DMARD?

Answer 23

Scavenge ROS produced by neutrophils

Question 24

What is the MoA of Tofacitinib?

Answer 24

JAK inhibition (all “-tinibs” do this)