Immunopharmacology Flashcards
Uses of Immunosuppressives?
1) Autoimmune diseases
2) Isoimmune diseases
3) Organ transplantation
4) Prevention of cell proliferation
Classification of Immunosuppressive Agents?
1) Corticosteroids
2) Calcineurin inhibitors
3) Cytotoxic agents
4) Mycophenolate mofetil
5) Proliferative signal inhibitors
6) Biologicals (antibodies)
Steroids are used in the treatment of?
RA SLE Psoriasis Asthma Inflammatory renal disease Inflammatory opthalmic disease Autoimmune hematological disease MS
Immediate side effects of corticosteroids:
Cushingoid features Weight gain (ravenous appetite) Diabetes (transient) Hirsutism (especially pediatrics) Cataracts Mood changes
Corticosteroids are excreted via the ___ as the metabolite ____:
kidneys; dihydroxyketone (17-hydroxysteroids)
Longest acting, most potent corticosteroids?
Bethamethasone
Dexamethasone
Least potent corticosteroid?
Cortisone
Shortest acting corticosteroid?
Hydrocortisone
Long term effects of corticosteroids:
Osteoporosis
Avascular necrosis
Growth retardation
Effects of steroids?
Regulates numerous gene transcription
Curtail NF-KB activation
Downregulation of IL-1 and IL-6
T-cells are inhibited from producing IL-2
CD8 activation is inhibited
Increase in neutrophils, decrease in other leukocytes
Neutrophils and monocytes display poor chemotaxis
The CNI Cyclosporine A is derived from?
Tolypocladium inflatum
The CNI Tacrolimus is derived from?
Streptomyces tsukunbaensis
IC mediator of CsA?
Cyclophilin
IC mediator of TAC?
FKBP-12
Adverse effects unique to CsA?
Hirsutism
Gum hypertrophy
Hypercholesterolemia
Adverse effects unique to TAC?
Hair loss
GI side effects
Adverse effects common to both TAC and CsA?
Nephrotoxicity
Hyperkalemia
Hypomagnesemia
What are the cytotoxic agents?
Azathioprine Methotrexate Cyclophosphamide Leflunomide Hydroxychloroquine
Uses of Azathioprine?
Transplantation RA Crohn's disease Ulcerative colitis GVHD
Methotrexate inhibits____ which leads to ____.
Dihydrofolate reductase; cessation of nucleotide synthesis
Uses of methotrexate?
GVHD
RA
SLE
Psoriasis
Cyclophosphamide is an ____ that forms covalent bonds with DNA and suppresses ___, which inhibits ___ production.
alkylating agent; cellular immunity; Ab and autoAb