Immunosuppressants Flashcards
Identify what immunosuppressants do
- MOA:
- agents that block lymphocyte action and proliferation.
- Reduce acute transplant rejection by suppressing cellular immunity.
- Frequently combined to achieve greater efficacy with dec toxicity.
- Chronic suppresion inc risk of infection and maligancy
Identify the drugs used as immunosuppressants
CTS-BAG
- Cyclosporine
- Tacrolimus
- Sirolimus (Rapamycin)
- Basiliximab
- Azathioprine
- Glucocorticoids
Identify the drugs used as therapeutic antibodies
for cancer therapy
ABC-RT
- Alemtuzumab
- Bevacizumab
- Cetuximab
- Rituximab
- Trastuzumab
Identify the drugs used as therapeutic antibodies
autoimmune disease therapy
IN
- Infliximab, adalimumab
- Natalizumab
Identify the drugs used as therapeutic antibodies
- Other*
- DDOPA*
- Denosumab
- Digoxin immune Fab
- Omalizumab
- Palivizumab
- Abciximab
Identify a drug & MOA
Used for: transplant rejection prophylaxis, psoriasis, rheumatoid arthritis
Toxicity: Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, hirsutism, gingival hyperplasia
- Drug: Cyclosporine
- MOA:
- calcineurin inhibitor, binds cyclophilin.
- blocks T cell activation by preventing IL-2 transcription.
- Notes: both calcineurin inhibitors are highly nephrotoxic
Identify a drug & MOA
Used for: transplant rejectino prophylaxis
Toxicity: Similar to another drug, increase risk of diabetes and neurotoxicity, no gingival hyperplasia or hirsutism.
- Drug: Tacrolimus
- MAO:
- Calcineurin inhibitor, binds FK506 binding protein (FKBP).
- Blocks T cell activation by preventing IL-2 transcription.
- Note: drugs ending with -limus bind to FKBP
Identify a drug & MOA
Used for: Kidney transplant rejection prophylaxis
Toxicity: Anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia, non-nephrotoxic.
- Drug: Sirolimus (Rapamycin)
- MOA:
- mTOR inhibitor, binds FKBP
- Blocks T cell activation and B cell differentation by preventing IL-2 signmal transduction. **vs the others were signal transcription.
- *Notes: Kidney ‘sir-vives’ *
- synergistic with cyclosporine
- also used in drug-eluting stents.
Identify a drug & MOA
Used for: Kidney transplant rejection prophylaxis
Toxicity: Edema, hypertension, tremor
- Drug: Basiliximab
- MOA: monoclonal antibody; blocks IL-2R
Identify a drug & MOA
Used for: Transplant rejection prophylaxis, rheumatoid arthritis, Crohn disease, glomerulonephritis, other autoimmune conditions.
Toxicity: Leukopenia, anemia, thrombocytopenia
- Drug: Azathioprine
- MOA:
- Antimetabolite precursor of 6-mercaptopurine
- Inhibits lymphocyte proliferation by blocking nucleotide synthesis.
- *Notes: *
- 6-MP degraded by xanthing oxidase; toxicity inc by allopurinol
- pronouced ‘azathio-purine’
Identify a drug & MOA
Used for: Transplant rejection prophylaxis (immune suppression), many autoimmune disorders, inflammation.
Toxicity: Hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, hypertension, cataracts, peptic ulcers.
- Drug: Glucocorticoids
- MOA:
- Inhibit NF-kappaB
- suppress both B and T cell function by dec transcription of many cytokines.
Identify the drug and Target for the clinical use of:
CLL
- Drug: Alemtuzumab
- Target: CD52
Identify the drug and Target for the clinical use of:
Colorectal cancer, renal cell carcinoma
- Drug: Bevacizumab
- Tagert: VEGF
Identify the drug and Target for the clinical use of:
Stage IV colorectal cancer, head and neck cancer
- Drug: Cetuximab
- Target: EGFR
Identify the drug and Target for the clinical use of:
B-cell non-hodgkin lymphoma, rheumatoid arthritis (with MTX), ITP
- Drug: Rituximab
- Target: CD20