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Pharm Quiz 5 Immunosuppressants

Terms in this set (44)

Examples of Non-Pharm Immunosuppressants
1. Irradiation
2. plasmapheresis (remove autoantibodies in MG)
Examples of Pharm Immunosuppressants
1. decrease T and B cels w/ anti-CD3 and anti-CD20 antibodis
2. chemotherapy
3. calcineurin inhibitors, steriods
Side effects of immunosuppression
1. reactivation of latent infections
2. bacterial and fungal infections
3. bone marrow suppression
4. increased cancer risk
5. nephrotoxicity
Uses of corticosteroids
1. broad anti-inflammatory
2. reverse acute transplant rejection
3. prevent acute exacerbations of autoimmune disease
4. suppress allergic rxn to biologics
Activity of Corticosteroids
1. decrease IL1, TNF alpha, IL2, IL4, IL5, CXCL8= anti-inflam
2. decrease NOS= decrease NO
3. decrease prostaglandins and leukotrienes
4. decrease adhesion molecules
5. induce apoptosis in lymphocytes and eosinophils
What cytotoxic agents are used for RA and MS?
1. cyclophosphamide
2. methotrexate
What do cyclophosphamide, methotrexate, and other cytotoxic agents attack?
used in cancer therapy but attack all fast dividing cells in body:
1. immune system
2. gut mucosa
3. hair follicles
What are different calcineurin inhibitors?
1. cyclosporine
2. Tacrolimus
How do calcineurin inhibitors like cyclosporine and tacrolimus work?
-bind immunophilins that for a complex inhibiting calcineurin

-cannot dephosphoryate NFAT so it can't go to nucleus and T cell prolif/ IL2 production inhibited)
What is cylcosporine (A) and its uses?
-cyclic, 11 aa polypeptide effective against T feel dependent responses (less for B)

-uses: organ transplant, severe RA, disabling psoriasis
How is cyclosporin A administered?
-IV or oral (20-50% bioavailable)
-peak at 1.5-2hrs
-half life= 5-18hrs
-metabolized by CYP3A4 and out bile so hepatic insuff. monitored!
What drugs interact with cyclosporine?
-any drug metabolized by CYP3A4:

-blockers increase plasma CsA= ketoconazole, fluconazole, verapamil, idinavir, grapefruit juice

-inducers decrease plamsaCsA = phenobarbital, phenytoin, St. Johns Wort
Side effects of Cyclosporine?
1. nephrotoxicity
2. hypertension in 50% of kidney patients and all heart transplant puts
3. hyperlipidemia
4. tremor
5. hirsutism and hypertrichosis
6. diabetogenic if with glucocortiboids
What is Tacrolimus (FK506)?
-macrolide antibiotic made by Strep tsukunaensis
-half-life is 12 hrs
-also metabolized by CYP3A4
-use for immunosuppression and rescue therapy if CsA doesn't work
-same side effects as CsA
What is Sirolimus (Rapamycin) Rapamune?
-macrocyclic lactone made by Strep. hygroscopic
-immunosuppressant with 15% bioavailability that peaks at 1-2 hrs
-half life= 62 hrs
-CYP3A4 metabolized
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