Immunopharm Flashcards
Glucocorticoids
MOA: bind cytosolic glucocorticoid receptor which translocates to nucleus and alters gene expression, inhibits PLA2 and COX-2
Effect: down-regulation of inflammatory mediator expression
Use: prevent transplant rejection, autoimmune dz’s, alleviate pain/nausea/fatigue
SE: HTN, hyperglycemia, psych sx’s, Cushing’s, myopathy, osteoporosis
Cyclosporine
Calcineurin inhibitor
Metabolism: CYP3A4
MOA: binds and forms complex with cyclophilin (an immunophilin) which inhibits calcineurin
Effect: no activation of NFAT (T-cell specific transcription factor) decreased production of cytokines
SE: nephrotoxicity, tremor, HTN, hyperglycemia, hyperlipidemia, osteoporosis, hirsutism, gum hyperplasia
Use: organ transplantation, uveitis, RA, psoriasis
Tacrolimus
MOA: binds to FK-binding protein (immunophilin)
Effect: complex inhibits calcineurin and decreases synthesis of inflammatory cytokines
SE: nephrotoxicity, neurotoxicity, hyperglycemia, HTN, hyperkalemia, GI sx’s
Use: transplant, atopic dermatitis, psoriasis
Sirolimus
MOA: binds to FKBP forming complex inhibiting the serine-threonine kinase mTOR
Effect: blocks IL-2 driven T-cell proliferation
Use: renal transplant, severe CAD
SE: myelosuppression, hepatotoxicity, diarrhea, hyperTGs, pneumonitis, HA
Thalidomide
MOA: inhibits synthesis of TNF-α
Effect: inhibits angiogenesis
Use: erythema nodosum, MM
Azathioprine
Purine antimetabolite (analogue)
MOA: prodrug of 6-mercapgtopurine, converted to 6-MP (activation depends on xanthine oxidase)
Effect: inhibits purine synthesis, suppressing B and T cell function of IG production and IL-2 secretion
SE: BM suppression, GI sx’s, increased infections and malignancies
CI: pt’s receiving allopurinol should have lower doses of Azathioprine
Methotrexate
MOA: @ low doses inhibits AICAR transformylase
Effect: accumulation of AMP which is converted to adenosine (potent inhibitor of inflammation)
Use: RA, psoriasis, ankylosing spondylitis, SLE
SE: nausea, mucosal ulcers, leukopenia, anemia, GI ulcers, hepatotoxicity, HS pneumonitis
CI: pregnancy 🤰🏽
Mycophenolate Mofetil
MOA: inhibits IMP dehydrogenase in the de novo pathway
Effect: decreased GTP production by B and T cells
Use: prophylaxis of transplant rejection, SLE
SE: N/V/D/abd pn, HA, HTN, myelosuppression (reversible)
Leflunomide
Prodrug of teriflunomide
MOA: inhibits dihydroorate dehydrogenase
Effect: decreases levels of UMP so decreased pyrimidines produced
Use: RA, SLE, MG
SE: diarrhea, allopecia, rash, myelosuppression, increased aminotransferase
CI: pregnancy🤰🏽
Cyclophosphamide
MOA: destroys proliferating lymphoid cells and alkylate DNA and other molecules in resting cells
Effect: immunosuppression
Use: SLE and other autoimmune dz’s
SE: infertility, BM suppression, hemorrhagic cystitis, bladder ca
Hydroxychloroquine
MOA: anti-inflamatory / immunosuppressive
Use: RA, SLE (often used w/ other drugs like Methotrexate and Sulfasalazine)
SE: hemolysis in pt’s w/ G6PD, retinal damage
Sulfasalazine
MOA: metabolized by bacteria in colon
Use: RA (sulfapyridine moiety), ulcerative colitis (5-ASA moiety), Crohn’s, Ankylosing spondylitis
SE: N/V, HA, rash, neutropenia, thrombocytpopenia, drug induced SLE, hemolysis in G6PD
ANtilymphocyte and Antithymocyte Ab’s
MOA: Ab’s bind to T cells involved in ag recognition and initiate complement destruction
Use: before stem cell transplant to prevent graft v host, solid organ transplants
RHo(D) Ig
Effect: prevention of primary immune response
Use: prevention of Rh hemolytic dz of the newborn in RHo(D) -ve mother
TNF-α Inhibitors
Adalimumab / Infliximab / Etanercept
MOA: bind TNF-α preventing its interaction w/ receptors
SE: cytopenias, increased risk of infection, ulcers, bowel perforation, can exacerbate HF
