Immunosuppressive Drugs - Immunology

Overview

Snapshot

A 36-year-old woman presents to the emergency department with worsening weakness and decreased visual acuity of the right eye. She reports that her symptoms progressively worsened over the course of a week and after developing an upper respiratory infection. Medical history is significant for multiple sclerosis (MS) treated with rituximab. Physical examination is significant for 2/5 strength in the lower extremities and an afferent pupillary defect appreciated in the right eye. Magnetic resonance imaging of the brain and spine shows new enhancing lesions when compared to prior imaging. After further evaluation, it was determined she had an MS exacerbation. She is started on intravenous methylprednisolone.

Immunosuppressants

Immunosuppressants
Medication	Clinical Use	Mechanism of Action	Adverse Effects
Cyclosporine	Rheumatoid arthritis Psoriasis Transplant rejection prophylaxis	Calcineurin inhibitor which impairs IL-2 production and release impairs IL-2-induced T-cell activation	Nephrotoxicity Neurotoxicity Hirsutism Gingival hyperplasia Hypertension Hyperlipidemia
Tacrolimus (FK506)	Transplant rejection prophylaxis	Calcineurin inhibitor via binding with intracellular FKBP-12 protein which impairs IL-2 production and release impairs IL-2-induced T-cell activation	Nephrotoxicity Neurotoxicity ↑ risk of diabetes
Sirolimus (Rapamycin)	Lymphangioleiomyomatosis Renal transplantation prophylaxis	mTOR inhibitor via binding with intracellular FKBP-12 protein which ↓ cytokine-induced T-cell proliferation	Pancytopenia Hyperlipidemia Edema Insulin resistance
Basiliximab	Renal transplantation prophylaxis	Targets the α-chain of the IL-2 receptor complex which is expressed on activated T-cells	Edema Tremor Hypertension
Azathioprine	Rheumatoid arthritis Renal transplantation Inflammatory bowel disease	A precursor of 6-mecaptopurine which inhibits purine nucleotide synthesis incorporates itself into the cell's DNA and halts replication	Pancytopenia
Mycophenolate mofetil	Organ transplantation Lupus nephritis	Inosine monophosphate dehydrogenase (IMPDH) inhibitor which impairs guanosine nucleotide synthesis	Gastrointestinal upset Pancytopenia Hypertension
Corticosteroids	A number of autoimmune and inflammatory disorders	NF-κB inhibitor Induces T-cell apoptosis	Hyperglycemia Osteoporosis Cushing syndrome Adrenocortical atrophy Peptic ulcers Cataracts Avascular necrosis Psychosis