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14 Cards in this Set
- Front
- Back
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What is the mechanism of action for adrenocorticosteroids?
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They inhibit gene transcription by directly competing for NF-KB and other nuclear activating factors in promoter regions and are there for very non-specific.
They inhibit pro-inflammatory cytokine release from macs. Suppress antigen presentation Alter neutrophil/lymphocyte traffic patterns to inflammatory cytes |
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What are the important side effects of corticosteroids?
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Impaired T cell responses and poor neutrophil function and a high risk of infection with most classes or organisms.
Osteoperosis (decreased Ca uptake) Diabetes mellitus Obesity HTN |
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What is cyclophosphamide used to treat?
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SLE and WEGENERS GRANULOMATOSIS
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What drug should never be used with azathioprine? Why?
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Allopurinol. 6-mercaptopurine (azathioprine's metabolite) and allopurinol both compete for xanthine oxidase which will lead to higher levels of 6-mercaptopurine and SEVERE BONE MARROW DEPRESSION.
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Describe azathioprine
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Azathioprine is a pro drug that is metabolized to 6-mercaptopurine
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Describe the difference in methotrexate's use in immunomodulation versus oncology.
What is it used to treat? |
At high dose methotrexate inhibits DHF reductase, interfering with de novo synthesis of purines and pyrimidines.
At once a week low dosage it increases adenosine which is anti-inflammatory. It is used to treat rheumatoid arthritis |
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What is the MOA for mycophenolate mofetil? What is it used to treat?
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Mycophenolate mofetil is a prodrug that is converted by plasma eterases into an acid. It inhibits T & B cell proliferation by blocking de novo nucleotide synthesis.
It is being used to reduce the corticosteroid requirements in patients with SLE |
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What is leflunomide?
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Leflunomide inhibits pyrimidine synthesis and has a half-life of 15-18 days.
It is a teratogen and should NEVER be used when pregnant. If a woman becomes pregnant they must washt he drug out with cholestyramine |
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What is the MOA for cyclosporin and tacrolimus?
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a. Both act primarily on T-Lymphocytes
b. Block signal #1 by binding to cyclophilin A (cyclosporin) and FKBP (tacrolimus). The complexes bind to calcineurin and prevent activation of multiple nuclear activation factors that should be turned on at the time of antigen binding to the TCR. c. G1 phase cannot begin without Signal #1 acting in concert with Signal #2 |
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What are calcineurin inhibitors used for?
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Cyclosporin and Tacrolimus are used to prevent rejection in all transplant settings.
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What is the difficulty in using the calcineurin inhibitors?
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Both Cyclosporin and Tacrolimus have very narrow therapeutic windows and a wide inter- and intraindividual variability in adsorption and metabolism.
On top of all that, drugs that increase P450 (phenytoin) or decrease P450 (erithromycin) also play a role in dosage |
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What is the MOA sirolimus? What is it used for?
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Sirolimus is an inhibitor of mammalian target of rapamycin (mTOR) [whatever that means...]
which blocks co-stimulation and IL2-R which is anti-fibrogenic. It is being used in transplants |
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How does Abatacept work?
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Abatacept is a CTLA IgG that binds to CD/80/86 on APC and inhibits CD28 activation
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How does Rituximab work?
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Rituximab depletes B cells by binding to CD20 on their surface and preventing them from presenting antigen.
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