Immunopharm Flashcards
Dexamethasone
Glucocorticoid
Induce annexin I (inhibit Phospholipase A2)
Repress COX-2 (via NF-kB inhibition)
Induce MAPK phosphatase I (inhibits MAPKs –> antiinflammatory effects)
Treat cancer-related pain.
Prednisone & Methylprednisone
Glucocorticoid
Induce annexin I (inhibit Phospholipase A2)
Repress COX-2 (via NF-kB inhibition)
Induce MAPK phosphatase I (inhibits MAPKs –> antiinflammatory effects)
Treat & Prevent Transplant Rejection
Prednisolone
Glucocorticoid
Induce annexin I (inhibit Phospholipase A2)
Repress COX-2 (via NF-kB inhibition)
Induce MAPK phosphatase I (inhibits MAPKs –> antiinflammatory effects)
Treat autoimmune disorders
Cyclosporine
Calcineurin Inhibitor
Forms complex with cyclophilin which inhibits calcineurin. Inhibits cytokine transcription. Metbolized by CYP3A4. Nephrotoxicity.
Used in organ transplantation, uveitits, RA, psoriasis.
Tacrolimus
Calcineurin Inhibitor
Forms complex with FK-binding protein which inhibits calcineurin. Inhibits cytokine transcription. Nephrotoxicity.
Used in organ transplantation. Topical formulation used for atopic dermatitis & psoriasis.
Sirolimus
T-Cell proliferation inhibitor
Structurally similar to Tacrolimus. Binds FKBP. Complex inhibits mTOR which is needed for IL-2 driven T-Cell proliferation.
Less nephrotoxic than Calcineurin inhibitors.
Used in renal transplantation & coronary stents.
Thalidomide
Unclear mechanism of action.
Inhibits TNF-a synthesis & angiogenesis.
AE: Teratogen, peripheral neuropathy, inc risk of DVT
Treat erythema nodosum leprosum & multiple myeloma.
Azathioprine
Antimetabolite
Pro-drug of 6-mercaptopurine. Inhiits de-novo purine synthesis. Suppresses B & T Cell function.
Inactivated by Xanthine Oxidase –> Adverse interaction with Allopurinol.
Prevent organ transplant rejection & treat severe RA.
Methotrexate
Antimetabolite
Inhibits AICAR transformylase. AICAR accumulates & inhibits AMP deaminase. Leads to accumulation of AMP –> adenosine –> anti-inflammatory.
AE: Nausea, ulcers, leukopenia, anemia, dose-related hepatotoxicity, pneumonitis, stomatitis. AE worse in pt with renal dysfunction.
Treat: DOC for RA, psoriasis, ankylosing spondilitis, lupus, graft vs host disease.
Leucovorin
Helps reduce methotrexate toxicity in RA treatment.
Mycophenolate Mofetil
Antimetabolite
Prodrug of Mycophenolic Acid. Inhibits IMP dehydrogenase –> inhibit GTP synthesis –> suppresses B & T cell activation.
AE: Nausea, vomiting, diarrhea, abd pain, htn, headache, myelosuppression.
Used as prophylaxis of transplant rejection.
Leflunomide
Antimetabolite
Prodrug of teriflunomide. Inhibits dihydroorate dehydrogenase, decreases levels of UMP, inhibits pyrimidine synthesis.
AE: Diarrhea, alopecia, rash, myelosuppression, carcinogenic, teratogenic.
Only approved use is RA. Efficacy seen in Lupus & myasthenia gravis.
Cyclophosphamide
Alkylating Agent
Alkylates DNA molecules, destroys proliferating lymphoid cells.
AE: Dose-limiting infertility, bone marrow suppression, hemorrhagic cystitis, bladder carcinoma. Long term use inc risk of infection & malignancy.
Acrolein is a metabolite, responsible for urinary toxicity.
Treats lupus & other autoimmune diseases.
Tofacitinib
JAK inhibitor
Inhibits JAK thus inhibits hematopoesis & immune cell function in response to cytokines & growth factors.
Treats moderate-severa RA. Similar effect to anti-TNF-a inhibitors.
Hydroxychloroquine
Unclear mechanism of action.
AE: Hemolysis in pt with G6PD def, retinal damage.
Treat mild RA & lupus.
Sulfasalazine
Metabolized to Sulfapyridine & 5-aminosalicylic (5-ASA). Sulfapridine is active metabolite for RA. 5-ASA active for ulcerative colitis.
AE: Nausea, vomiting, headache, rash, neutropenia, thrombocytopenia, lupus, hemolysis in pt with G6PD def.
Used to treat ulcerative colitis, RA, crohn’s, ankylosing spondylitis.
Rho(D) globulin (Rhogam)
Human IgG
Ab against Rho (D) RBC antigen.
Given to R- women with R+ fetus in pregnancy to prevent hemolytic disease of the newborn.
Adalimumab
Human IgG1
Ab against TNF-a.
AE: Cytopenia, inc risk of inection, inc risk of malignancies, ulcers, anti drug abs, exacerbate heart failure. No live vaccines, check for ongoing infection before administering.
Treats RA, psoriatic arthritis, ankylosing spondylitis, Crohn’s, ulcerative colitis
Infliximab
Chimeric monoclonal Ab
Ab against TNF-a
AE: Cytopenia, inc risk of inection, inc risk of malignancies, ulcers, anti drug abs, exacerbate heart failure. No live vaccines, check for ongoing infection before administering.
Treats RA, psoriatic arthritis, ankylosing spondylitis, Crohn’s, ulcerative colitis
Etanercept
Not a true Monoclonal Ab
Ligand binding portion of TNF-a receptor + Fc portion of human IgG1.
AE: Cytopenia, inc risk of inection, inc risk of malignancies, ulcers, anti drug abs, exacerbate heart failure. No live vaccines, check for ongoing infection before administering.
Treats RA, psoriatic arthritis, ankylosing spondylitis, plaque psoriasis.
Omalizumab
Anti IgE antibody
Used in patients >12 for asthma & chronic utricaria.
Rituximab
Anti CD20 antibody
Depletes circulating B Cells
Used to treat non-Hodgkin’s Lymphoma and Chronic Lymphocytic Leukemia.
Also treat RA in combination with methotrexate.
Tocilizumab
Anti IL6 receptor antibody.
Prevents IL6 action.
AE: elevated liver funct tests, hyperlipidemia, neutropenia, htn, infusion related injection site reactions.
Treat RA, giant cell arteritis, juvenile idiopathic arthritis, cytokine release syndrome.
Sarilumab
Anti IL6 receptor antibody.
Prevents IL6 action.
AE: elevated liver funct tests, hyperlipidemia, neutropenia, htn, infusion related injection site reactions.
Treat RA
Abtacept
Fusion protein that interferes with T-cell activation
Treat moderate to severe RA, polyarticular juvenile idiopathic arthritis.
Aldesleukin
Immunostimulant
Recombinant IL-2. Activates NK cells, promotes production of CTLs.
Adjunctive treatment of renal cell carcinoma & malignant melanoma.
Interferons
Interferon-a in leukemias, melanoma, sarcoma, Hep B & C
Interferon-b in relapsing MS
Interferon-y in chronic granulomatous disease
BCG
Live culture of Bacillus Calmette & Guerin strains of mycobacterium.
Active against tumors due to unclear mechanism.
Treatment & prophylaxis of urinary bladder carcinoma.
