Immunosuppressants

Question 1

Cyclosporine

Answer 1

Binds cyclophilin
Inhibits calcineurin
Prevents IL2 transcription —> blocks T cell activation

Psoriasis
RA
Prevents transplant rejection

Nephrotoxic
HTN
Hyperlipidemia
Hyperglicemia
Neurotoxic
Gingival hyperplasia
Hirsutism

Cyp 450 metab

Question 2

Tacrolimus

fk506

Answer 2

Binds FK506 (FKBP)
Inhibits calcineurin
Prevents IL2 Transcription —> blocks T cell activation

Nephrotoxic
Neurotoxic
Risk of diabetes

Metab by p 450

Question 3

Sorolimus

Rapamycin

Answer 3

Binds FK506 (FKBP)
Inhibits mTOR

Prevents response to IL2 —> prevents T cell activation and B cell differentiation

Kidney transplant rejection prophylaxis
+ in drug eluting stents

Pancytopenia
Insulin resistance
Hyperlipidemia

Question 4

Mycophenolate

Mofetil

Answer 4

Reversibly inhibits IMP dehydrogenase in active lymphocytes preventing purine synthesis of B and T cells

Lupus nephritis

GI upset
Pancytopenia
HTN
Hyperglycemia

Invasive CMV infection

Question 5

Glucocorticosteroids

Answer 5

Inhibit MF-KB
Suppress B and T cell function by decreasing transcription of many cytokines
Induce T cell apoptosis

Autoimmune and inflamm disorders
Adrenal insufficiency
Ashtma
CLL
Non hodgkin’s

Artificial increase in WBC
High glucose
Cushinoid Osteoporosis Cataract Myopathy Gastritis Avascular necrosis Paperthin skin
Adrenal insufficiency if stopped abruptly