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Pharm Exam II Immuno
Immunosuppressants
| Qestion | Answer |
|---|---|
| What drugs are calcineurin Inhibitors? | Cyclosporine and Tacrolimus |
| What is Prednisone's mechanism of action? | Alter gene transcription at glucocorticoid receptors to Increase expression of anti-inflamm genes & dec. expression of Pro-inflamm genes; it also blocks adhesion of inflammatory cells |
| What are some adverse effects of Corticosteroids? | Bone necrosis, increased risk for infection, osteoporosis, hyperglycemia |
| What drug can be combined with prednisone to allow a decrease of side-effects? | Using corticosteroids in combo w/cyclosporine allows for a smaller dose of corticosteroids to be administered & thus reduce negative side-effects |
| Are calcineurin Inhibitors lipophilic? Can they cross the BBB? | They are lipophilic and can therefore cross cell membranes, including CNS |
| What are the most important Rx's in transplantation? | Calcineurin Inhibitors (Cyclosporine & Tacrolimus |
| What is the MOA of Calcineurin Inhibitors? | They block the activation of T cells by inhibiting IL-2 prod. |
| Do Calcineurin Inibitors allow for selective inhibition of T cell activation? | Yes |
| Do calcineurin inhibitors (Cyclosporine & Tacrolimus cause myelosuppression? | Nope |
| What is the most adverse effect of Cyclosporine & Tacrolimus (the calcineurin inhibitors)? | Renal toxicity (happens in about 25% of transplant pts.) |
| How much more potent is Tacrolimus than Cyclosporine? | 100 x's |
| What is Tacrolimus used for? | For rescue therapy during episodes of acute rejection |
| What are other side effects of Cyclosporine and Tacrolimus (Calcineurin Inhibitors)? | Hypertension, Neurotoxicity, Hirutism, Gingival Hyperplasia |
| What type of drug class does Sirolimus belong to? | Anti-proliferative Immunosuppressant |
| What is Sirolimus like? | Like the Calcineurin Inhibitors. |
| What cells do calcineurin inhibitors work in? | In the helper T cell (prevents activation of the T-cells) |
| What type of cell does Sirolimus work on? | Cytotoxic T cells |
| What are the calcineurin inhibitor's receptors? | Cyclophilins/FKBP |
| What does inhibition of calcineurin cause? | Prevents dephosphorylation of NF-AT transcription factor which in turn prevents the production of IL-2 by helper T cells and activation of helper T cells |
| What types of Drugs do calcineurin inhibitors have interactions with? | Agents that affect cytochrome P-450 |
| Like calcineurin inhibitors, the anti-proliferative Sirolimus is lipophilic and therefore what else? | Can cross BBB |
| What does Sirolimus inhibit? | mTOR protein kinase |
| What is the oral availability of cyclosporine? | From 20-50% |
| What is the half-life of the calcineurin inhibitors? | 6 hrs |
| What percent of patients suffer from Nephrotoxicity? | Occurs in 25-75% |
| What drug are calcineurin inhibitors prescribed with? | Prednisone |
| What types of transplants are calcineurin inhibitors used commonly in? | Renal Hepatic Cardiac |
| What does the inhibition of mTOR protein kinase ultimately cause? | Inhibits cytotoxic T-cell proliferation |
| How is sirolimus metabolized? | By cytochrome P-450 |
| What is the half-life of sirolimus? | 2.5 days |
| Does sirolimus cause renal toxicity? | None aparent |
| What is the indication for using sirolimus? | Prevention of acute renal transplant rejection |
| What drugs should sirolimus be taken with? | Cyclosporine and Corticosteroids |
| Using sirolimus with cyclosporine can lead to what? | Reduction in amount of cyclosporine needed & therefore side effects |
| What class does mycophenolate mofetil belong to? | Anti-proliferative |
| What does mycophenolate mofetil do? | Inhibits IMP dehydrogenase. |
| What does inhibiting IMP dehydrogenase do? | Prevents PURINE synthesis and therefore DNA synthesis |
| What does Methotrexate inhibit? | DHFR |
| What does blocking DHFR cause in the cells? | Blocks thymidylate synthase and purine biosynthesis (therefore DNA synthesis) |
| What does 5-Flurorouracil inhibit? | Thymidylate synthase (which converts dUMP into dTMP - w/o it, no T pre-cursors) |
| Does mycophenolate mofetil cause selective suppression of lymphocyte proliferation? | Yes |
| What the the three things mycophenolate mofetil acts on? | DNA Synthesis, Selective suppression of lymphocytes and inhibition of leukocyte recruitment by blocking glycosylation of cell adhesion molecules as a result of loss of GTP) |
| How is mycophenolate mofetil metabolized? | By glucuronylation |
| What are the two Anti-IL-2 Receptor (CD25) Antibody drugs? | Daclizumab & Basiliximab |
| When is the RhoD Immune Globulin administered? | When a mother has an Rh positive fetus to an Rh negative mother to prevent sensitization to to Rh POSITIVE antigens on the RBC's of the fetus/ infent; this prevents erythroblastosis fetalis in subsequent pregnancies |
| When is the Rho(D) Immune Globulin (RhoGAM) administered? | Within 12 hrs. of birth, miscarriage or ectopic pregnancy |
| What do the Anti-IL 2 receptor (CD 25) Antibodies block | block the IL-2 receptor on activated T cells |
| What is the Anti-TNF reagent we studied? | Infliximab |
| What do the anti-TNF's do? | they bind up TNF alpha. In doing so, block TNF alpha from binding to TNF receptor which then inhibits TNF alpha induced-inflammation |
| What are the indications for infliximab? | Used in dzs w/ elevated TNF alpha levels (RA, Crohn's) |
| What are the indications for Etanercept? | Psoriasis, RA, Ankylosing spondylitis, Psoriatic arthritis, Juvenile Arthritis |
| What is the half-life of anti-TNF's? | about 8-10 days |
| What are adverse effects of anti-TNF's? | Inc. susceptibility to infections (usu URI) |
Created by:
doggiekylesmom
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