Immunosuppressant Drugs Flashcards
What is the overall use of immunosuppressant drugs?
to suppress the activation of the immune system
Name four conditions you can manage with immunosuppressants?
rheumatoid/arthiritic disorders, organ rejection, autoimmune disorders, severe IBD
Name the four classes of immunosuppressive drugs
glucocorticoids, azathioprine and mycophenolate mofetil, disease modifying antirheumatic drugs, biologics
Where are glucocorticoids secreted in the body?
middle layer of the adrenal gland
What are some clinical uses of glucocorticoids?
asthma, allergies, eczema, hypersensitivity states, autoimmune diseases, suppression of organ rejection
Name two common oral glucocorticoids
prednisolone and betamethasone
What is the suffix for glucocorticoids?
-one
Do oral or injectable glucocorticoids have a longer duration of action?
injectable
Which part of the immune system do glucocorticoids suppress?
IL-2 transcription which prevents proliferation and activation of T-cells
What does DMARDs stand for?s
Disease Modifying Anti Rheumatic Drugs
Which part of the immune system to DMARDs suppress?
prevent the activation of the cells that erode cartilage and bone
What are some clinical uses for methotrexate (DMARD)?
rheumatoid arthritis
Give an example of a DMARD?
methotrexate
Which part of the immune system do Azathioprine and Mycophenolate mofetil suppress?
purine synthesis which inhibits DNA synthesis which inhibits cell proliferation
Is Mycophenolate mofetil a prodrug or a full drug?
prodrug
What are some clinical uses of azathioprine and mycophenolate mofetil?
prevent organ rejection, rheumatoid arthritis, autoimmune disorders
What are biologics?
active pharmaceutical ingredients that may be living identities
Give some examples of biologics
vaccines, blood, blood components, gene therapy
Are biologics or synthetic small molecules larger?
biologics
Are biologics available for oral administration?
no, injectable only
What are the targets for biologics?
extracellular targets
Can all biologic cross a cell membrane?
no most are too big
Is the precise structure of all biologics the same?
no, it depends on the cell/organism used for production
What are the aims of biologics therapy?
replace an abnormal or deficient protein, alter an existing biological process, provide a new function
What are some examples of ways biologics can replace an abnormal or deficient protein?
insulin therapy
What are some examples of ways biologics can enhance or inhibit an existing biological process?
rheumatoid arthritis
What are some types of biologics?
monoclonal antibodies, proteins, viral vectors, stem cell therapy
What are monoclonal antibodies?
proteins used by the immune system to identify and neutralise foreign proteins and organisms
How can you produce monoclonal antibodies in the lab?
clone individual cells to produce identical antibodies
What are the mechanisms of monoclonal antibody action?
ligand blockade, receptor blockade, receptor downregulation, signalling induction, cell depletion, payload delivery
How do monoclonal antibodies cause ligand blockade?
prevent the ligand interacting with the receptor
How do monoclonal antibodies cause receptor blockade?
don’t activate the receptor, just prevent the ligand binding
How do monoclonal antibodies cause receptor downregulation?
bind to the receptors on the cell surface
How do monoclonal antibodies cause signalling induction?
they can trigger intracellular signalling upon binding
How can monoclonal antibodies cause cell depletion?
start the cell death process
How can monoclonal antibodies help with payload delivery?
they can deliver other drugs into the body
What is an important cytokine in arthritis?
TNF alpha
How do anti-TNF monoclonal antibodies work?
will recognise and bind to TNF alpha which prevents TNF alpha from binding to its receptor. This inhibits gene transcription and therefore inhibits cell proliferation
What can anti-TNF monoclonal antibodies be used to treat?
rheumatoid arthritis
What is the suffix for monoclonal antibodies?
-mab
Give the name of the anti-TNF monoclonal antibody
adalimumab
