Immunosuppressant Drugs Flashcards
What drug class is methotrexate
Anti-metabolite and anti-folate immunosuppressant and chemotherapeutic
What are the indications of methotrexate
Cancer, autoimmune diseases, including rheumatoid arthritis, psoriasis, psoriatic arthritis, lupus and Crohn’s disease as well as an abortifacient
What is the MOA of methotrexate
Anti-metabolite and anti-folate drug
What are the admin routes for methotrexate
PO, IM, IV, SQ and IT (intra-thecal)
What must be monitored if you are taking methotrexate
CBC, LFT, creatinine
What are side effects of methotrexate
nausea, abdominal pain, fatigue, fever, dizziness, ulcerative stomatitis, low white blood cell count and thus predisposition to infection
What are severe side effects of methotrexate
developing another malignancy, pulmonary fibrosis, acute, pneumonitis
What category is methotraxate
category X, plus never should be used by pregnant women or those trying to conceive
What supplement decreases the efficacy of methotrexate
folic acid or folate
What drug class is azathioprine (Imuran)
purine anti-metabolite immuno-suppressant
What are the indications of azathioprine (imuran)
Prevention of transplant rejection, inflammatory bowel disease, SLE and rheumatoid arthritis
What is the MOA of azathioprine (imuran)
Metabolic breakdown products of Azathioprine act to inhibit purine synthesis which will block protein synthesis, particularly in cells that experience rapid turnover
What are side effects of azathioprine (imuran)
Rapidly growing cells are most readily affected, leading to hair loss, bone marrow suppression (aplastic anemia), GI toxicity, leukopenia, and thrombocytopenia. Decreased ability to fight infection
What drug class is Cyclosporine (Sandimmune)
immunosuppressant derived from a soil fungus
What are the indications for Cyclosporine
Prevent rejection of kidney, liver and heart transplants as well as for treatment of RA and other autoimmune diseases such as severe psoriasis
What is the MOA of Cyclosporine
T-cell inhibition. Blocks the signal to lymphocytes to produce IL-1, IL-2, IL-3, IL-4, and interferon gamma
What will increase blood levels of cyclosporine
grapefruit, because cyclosporin is processed by CYP 450
What drug class is Tacrolimus/ Prograf
An immunosuppressant drug related to the macrolide class of antibiotics extracted from soil microorganism
What are the indication of Tacrolimus
Protection against rejection of organ transplantation. Topical treatment for severe eczema
How does tacrolimus compare to cyclosporine
tacrolimus is like 100x more potent
What strange location is cyclosporine used in low dose
in the eyes when there is reduced tear production (from inflammation) Called Restasis
What drug class is etanercept (enbrel)
DMARD, recombinant-DNA drug
How is etanercept administered
SQ injection 1-2x weekly
Wat are side effects of etanercept
tumors, increased susceptibility to infections,
What drug class is infliximab (remicade)
DMARD, recombinant-DNA drug
What are the indications for infliximab
RA, Crohn’s disease, U.C (etanercept is not approved for IBD)
What is the administration route for infliximab
IV, since gut would destroy the drug
What is the MOA of infliximab
neutralizes the biological activity of TNFα by binding with high affinity to the soluble (free floating in the blood) TNFα and the trans-membrane (located on the outer membranes of T cells and similar immune cells) forms of TNFα, thus preventing the effective binding of TNFα with its receptors.
Which drug is used in DMARDs is also used as an anti-malarial
Hydroxychloroquine (plaquenil)
What is the MOA for hydroxychloroquine’s DMARD activity
blocks activation fo TLRs on plasmacytoid dendritic cells
What are indications for hydroxychloroquine
AI dz, malaria, post lyme
What are signs of hydroxychloroquine overdose
HA, drowsiness, convulsions, SOB, vision problems
Which drug mandates yearly dilated eye exams
hydroxychloroquine (plaquenil)
From whom is hydroxychloroquine contraindicated
Those with G6PD enzyme deficiency
What are gold salts used for
reducing inflammation in AI disease when patient in unresponsive to other drug therapies
