Immunosuppressants Flashcards
MOA of action of corticosteroids?
Immunosuppressive by inhibiting transcription and therefore gene expression.
Examples of corticosteroids?
Prednisolone Beclomethasone Fluticasone Dipropionate Budenoside
ADRs of corticosteroids?
Cushingoid, suppression HPA axis, osteoporosis, at high concentration will act on mineralocorticoid receptors (salt retention), stunted growth in children
Indications of corticosteroids?
Immunosuppressive, anti inflammatory, replacement of endogenous corticosteroids
Azathioprine indication of use?
RA, IBD, transplant and leukaemia
MOA: Azathioprine
Inhibition of purine metabolism reduces DNA and RNA production. Cytotoxic action of rapidly diving cells
ADRs of azathioprine?
Myelosuppression (bone marrow suppression!) causing thrombocytopenia and anaemia . Increased infection risk, GI disturbance
Give an example of a cytotoxic alkylating agent?
cyclophosphamide
MOA: cyclophosphamide?
Creates cross links between DNA thus preventing replication. It targets cells with a high mitotic rate
ADRs of cyclophosphamide?
Bladder cancer risk due to increase of acrolein metabolite in urine
Lymphoma and leukaemia
Infertility and teratogenic
DDIs of cyclophosphamide?
It is activated by CYP450 so consider CYP inducers and inhibitors
What is the agent of choice for transplant immunosuppression?
Mycophenolate Mofetil
MOA of mycophenolate mofetil?
Inhibition of guanosine synthesis leading to impaired B cell and T cell proliferation
ADRs of mycophenolate mofetil?
My loud suppression leading to leukopenia and neutropenia
Increased risk of infection, especially viral
Calcineurin inhibitors are indicated for..?
Prevention of graft and transplant rejection
Atopic dermatitis
Psoriasis