Immunosuppressive Agents

Question 1

How does glucocorticoid work to supress immune system?

Answer 1

It interferes with the cell cycle of lymphoid lineage and cause apoptosis in them.
T cells are affected first and then antibody production also decreases.

Question 2

What are glucocorticoids used for?

Answer 2

Immunologically mediated diseases

To prevent allograft rejection

Question 3

Glucocorticoids are used with ____________ or other cytotoxic agent.

Answer 3

cyclosporine

Question 4

What is the MOA of cyclosporine?

Answer 4

Cyclosporin binds to cyclophilin in the T cell. Cyclophilin inhibits calcineurin. Low calcineurin means low NF-AT leading to decreased synthesis of IL-2.

Question 5

What is the ROA of cyclosporin?

Answer 5

Mainly IV

Orally (Neoral) but variable absorption

Question 6

What should we do when giving cyclosporin to the patient?

Answer 6

We should monitor the blood levels of drug

Question 7

1. Half life of cyclosporine?

2. Metabolism and excretion of cyclosporine?

Answer 7

Biphasic half life with terminal phase of 10-25 hrs
Metabolized by the liver
Excreted in feces

Question 8

What are the uses of cyclocporine?

Answer 8

Prevent short and long term rejection of SOT

Induce tears in ophthalmic inflammation caused by keratoconjunctivits sicca

Question 9

What are the adverse effects of cyclosporine?

Answer 9

Nephrotoxicity
Neurotoxicity
Hypertension
Hyperglycemia
Hyperkalemia
Hirsutism
Gingival hyperplasia

Question 10

What is the MOA of tacrolimus?

Answer 10

It binds to FKBP that then binds to calcineurin and inhibits NF-AT. Low NF-AT causes low synthesis of IL-2

Question 11

What is the ROA of tacrolimus?

Answer 11

Oral

Parenteral

Question 12

What is tacrolimus used for?

Answer 12

Liver transplantation

Question 13

What are adverse effects of tacrolimus?

Answer 13

Renal impairement
Headache and tremors
Hypertension
Hyperkalemia
Alopecia