Lecture 13: Immune System Drugs (RED ONLY) Flashcards
What are the 3 main drug classes with immune effects?
Glucorticoids
Immunomodulators
Biologics
What are the glucocortidoids (ALL END IN ONE)
CHPPD TB
cortisone
hydrocortisone
Prednisone
Prednisolone
Dexamethasone
Betamethasone
what are the four groups of immunumodulators and their subgroups
hint… got milk?
All of my calcium
A milk lover?
Sure, Gotta have flavored milk
even strawberry?
chocolate too.
antimetabolites - azothioprinem methotrexate, leflunomide
Other - Sulsasalazine, glatiramer, hydroxychloriquine, fingolimod, mycophenolate.
mTOR kinase inhib - everlimus, sirolimus
Calcineurin Inhibitors - cyclosporine, tacrolimus.
What are the cytokine inhibitors
go back and learn this
What are the 3 S?
Sugar (glucocorticoids)
Salt (mineralcorticoids)
Sex (Androgens)
What are the main 3 glucocorticoids?
what is the glucocorticoid hormone?
Hydrocortisone (main?)
Cortisone
Prednisolone
hormone is cortisol
What is the main hormone in the mineralcorticoids?
what is the main mineralcorticoid med?
Aldosterone = hormome
med = fludrocortisone
What is the main hormone in the androgens?
what is the main med?
Testosterone = hormone
med = DHEA
What are the effects of GCs?
Widespread effects on carb, protein, and lipid metabolism, and electrolyte/water balance.
in the nervous system:
Excess GC = insomnia/euphoria followed by depression, aka steroid psychosis.
Deficiency GC = Depression
What is the MOA of a GC’s antinflammatory/immune effects?
Inhibits production of precursors to prostaglandins, leukotrienes, and PAF.
Suppresses inflammatory cytokines, chemokines, and other inflammatory mediators.
Inhibits macrophages and other APCs
Reduces synthesis of arachidonic acid, which leads to reduction of COX 2, reducing prostaglandins.
Reduces antibody production in large doses.
Note:
NSAIDs are also COX inhibitors.
Which GC is often prescribed as a cream and has similar anti-inflammatory effects and mineralcorticoid activity?
Hydrocortisone
What is the MOA of methotrexate?
Binds and inhibits dihydrofolate reductase (DHFR)
Inhibiting tetrahydrofolate synthesis (THF)
Inhibiting synthesis of purine nucleotides and amino acids
Interfering with the formation of DNA, RNA, and cellular proteins
What nucleic acids is leflunomide an analog for?
Pyrimidine
What nucleic acids is azathioprine an analog for?
Purine
Note:
Prine purine
What are the indications for MTX?
RA, psoriasis, several types of cancer.
Off-label use in Crohn’s disease, MS, SLE, and multiple conditions.
what drug requires use of birth control and why
methotrexate because it causes birth defects
What are the indications for leflunomide?
RA. PO administration only
What are the indications for azathioprine?
RA, MS, psoriasis, Crohn’s disease, and transplant maintenance.
What are the caclineurin inhibitors and what are their MOAs
cyclosporine, tacrolimus
Inhibiting T-lymphocyte activation.
What are issues of tolerability in cyclosporine?
Gingival hyperplasia
Hirsutism
What are the indications for the calcineurin inhibitors?
Transplant maintenance
RA
Psoriasis
What is the MOA of the mTOR kinase inhibitors?
Inhibiting T-lymphocyte activation & proliferation.
Synergy with calcineurin inhibitors.
What is the indication for the mTOR kinase inhibitors?
Cancer, Organ transplantation, complications of TB.
What is the MOA for mycophenolate?
Inhibits T and B cell proliferation by inhibiting major enzyme involved in nucleotide synthesis.
What are the indications for mycophenolate?
Transplant maintenance, lupus nephritis, autoimmune hepatitis, and myasthenia gravis.
What is the MOA for sulfasalazine?
5-aminosalicyclic acid derivative. Immune modulator with an unknown mechanism.
What are the indications for sulfasalazine?
RA, and ulcerative colitis
What is the MOA for hydroxychloroquine?
Antimalarial drug with immune modulating factors (inhibits neutrophil and eosinophil motility and impairs complement antibody reactions)
What are the indications for hydroxychloroquine?
RA
SLE
Malaria
What is the MOA of fingolimod?
Binds sphingosine receptors and blocks lymphocytes from leaving lymph nodes
What are the indications for fingolimod?
MS
What is the MOA for glatiramer?
Not well defined.
Mixture of polymers that roughly mimics basic myelin protein; it is thought to activate T suppressor cells.
What are the indications for Glatiramer?
MS (Preferred in pregnancy)
What are the two Anti-TNFs?
Etanercept (Enbrel)
Adalimumab (Humira)
What are the indications for etanercept and adalimumab?
RA, psoriasis, Crohn’s disease, and more.
What are the two anti-CD80/86 drugs?
Belatacept
Abatacept
What are the indications for Belatacept and Abatacept?
Transplant (belatacept)
RA, psoriasis (Abatacept)
What is Rituximab and its use?
Anti-CD20 indicated for RA, chronic lymphocytic leukemia, and non-hodgkin lymphomas.
What should you always double check when prescribing an immune system drug?
Pregnancy
Live vaccine candidacy
Drug and disease interactions
Dose adjustments
What should you always do with GCs?
Taper down high or long doses to avoid adrenal insufficiency.
What cancers is MTX for?
Lungs, liver, kidney, bone marrow
What should you always give with MTX and sulfasalazine?
Folic acid
What should you always do when prescribing a biologic?
Parenteral only.
Screen for TB before use.
Avoid live vaccines.
Refrigerate
Don’t combine them!
