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Drug Name: Leflunomide
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:
USES: Rheumatoid arthritis, Wegener's, SLE, Gyasthenia, GVHD
MECHANISM: Antimetabolite-- inhibits de novo pyrimidine synthesis. Inhibits Uridine monophosphate
SIDE EFFECTS: Diarrhea, reversible alopecia
TOXICITY: GI toxicity
ANTIDOTES:
CONTRAINDICATIONS: Quick removal when cholestyramine administered
INTERACTIONS:
OTHER: Significant effect on B & T cells
Drug Name: Methotrexate
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Other info:
USES: Anticancer, GVHD, rheumatoid arthritis, psoriasis
MECHANISM: Antimetabolite- Inhibition of folate results in cytotoxicity. Apoptosis in activated T-cells. Anti-inflammatory (via adenosine?)
SIDE EFFECTS: GI, myelosuppression, thrombocytopenia, pneumonitis,
TOXICITY: Embryo toxcitiy
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS: Plasma binding drugs, tubular secretion, reduced renal blood flow, weak organic acids
OTHER:
Drug Name: Cyclophosphamide
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Antidotes or treatment of toxic effects:
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Other info:
USES: Anticancer, childhood nephritic syndrome, SLE, vasculitis, Wegener's
MECHANISM: Alkylation of guanine residues -> miscoding and mutation, disrupts purine ring, DNA replication
SIDE EFFECTS: Leukipenia, cardiotoxicity, alopecia, repro problems
TOXICITY: Severe!
Bladder cancer (via acrolein), teratogenic, leukemia, ADH secretion
ANTIDOTES: Reduce bladder cancer risk by taking in day, co-administer mesna
CONTRAINDICATIONS:
INTERACTIONS: P-450 enzymes, myelosuppressive, nephrotoxic agents
OTHER: Derivative of nitrogen mustard; prodrug that requires P450
Drug Name: Cyclosporine A
Where applicable list:

Therapeutic Uses:
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USES: transplant, rheumatoid arthritis, psoriasis, atopic dermatitis, uveitis, IBD, nephrotic syndrome
MECHANISM: Calcineurin Inhibitor - Stops activiation (dephosphorylation) of NFAT via binding to calcineurin. NFAT activates transcription of IL-2. Also incr exp of TGF beta.
SIDE EFFECTS: Hypertension (esp in renal/cardiac transplant), incr LDL, tremor, hirsutism
TOXICITY: Nephrotoxicity, renal dysfunction,
ANTIDOTES: Cessate if nephrotoxicity evident
CONTRAINDICATIONS:
INTERACTIONS: Diabetogenic when combined w/ glucocorticoids; other: P-450, NSAIDS, methotrexate, sirolimus, prednisolone, digoxin, statins, mTOR inhibitors
OTHER: Suppresses humoral immunity; more effective against T-cell mechanisms.
Drug Name: Tacrolimus
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Toxicity:
Antidotes or treatment of toxic effects:
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Other info:
USES: Transplant, atopic eczema
MECHANISM: Calcineurin Inhibitor - Stops activiation (dephosphorylation) of NFAT via binding to calcineurin. NFAT activates transcription of IL-2. Also incr exp of TGF beta.
SIDE EFFECTS: Hypertension, hyperkalemia, does NOT affect uric acid or LDL (unlike cyclosporine)
TOXICITY: Nephrotoxicity, hyperglycemia and diabetes, 2ndary tumors, infx
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS: P-450 enzymes, co-dmin w/ cyclosporine causes additive nephrotoxicity
OTHER: Macrolide
Drug Name: Sirolimus & Everolimus
Where applicable list:

Therapeutic Uses:
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USES: Transplant Rx, coronary artery disease,
MECHANISM: mTOR inhibitor - blocks IL-2 receptor. Complexes with FKBP but does not affect calcineurin
SIDE EFFECTS: Incr. triglycerides/chol., anemia, fever, GI problems, low potassium, infx, neoplasia
TOXICITY: Renal function, delay graft function. Lymphocele
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS: P-450, P-glycoprotein transport, cyclosporine
OTHER: Everolimus has shorter 1/2 life
Drug Name: Etanercept
Where applicable list:

Therapeutic Uses:
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USES: Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis
MECHANISM: TNF-alpha inhibitor- (binds both TNF's), prevents binding to TNF receptor
SIDE EFFECTS: Injection site reactions in 1/3 px
TOXICITY: Serious infections
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Infliximab
Where applicable list:

Therapeutic Uses:
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USES: Rheumatoid arthritis plus methotrexate, unresponsive Crohn's disease
MECHANISM: TNF-alpha inhibitor- Partially humanized anti-TNF-alpha antibody
SIDE EFFECTS: Infusion reaction, anti-infliximab antibodies
TOXICITY: lupus-like rxn (rare), serious infections
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Adalimumab
Where applicable list:

Therapeutic Uses:
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USES: Rheumatoid arthritis + methotrexate, psoriatic arthritis, HIV arthropathy, wasting syndromes
MECHANISM: TNF-alpha inhibitor- Fully humanized anti-TNF-alpha antibody
SIDE EFFECTS: Infusion reaction, anti-adalimumab antibodies
TOXICITY: lupus-like rxn (rare), serious infections
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Certolizumab
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Other info:
USES: Moderate to severe Crohn's, methotrexate for rheumatoid arthritis
MECHANISM: TNF-alpha inhibitor-Humanized recombinant Fab fragment specific for TNF-alpha
SIDE EFFECTS: Headache, abdominal pain, cough, althralgia, infections, UTI, nasopharyngitis
TOXICITY: Malignancies, aggrevated Crohn's
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Thalidomide
Where applicable list:

Therapeutic Uses:
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USES: Severe refractory RA, SLE, Crohn's, HIV, cancer
MECHANISM: TNF-alpha inhibitor- Who knows?
SIDE EFFECTS:
TOXICITY: Teratogenic
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Highly regulated use
Drug Name: TACE inhibitors
Where applicable list:

Therapeutic Uses:
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USES: Investigatory
MECHANISM: TNF-alpha inhibitor- inhibits TNF-alpha converting enzyme (TACE), inhibits processing of pro-TNF-a
SIDE EFFECTS:
TOXICITY:
ANTIDOTES:
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INTERACTIONS:
OTHER: Not proving effective for RA
Drug Name: Anakinra
Where applicable list:

Therapeutic Uses:
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Other info:
USES: Rheumatoid arthritis combined with methotrexate
MECHANISM: IL-1 inhibitor - Recombinant IL-1 receptor antagonist
SIDE EFFECTS: Injection site rxn, headache, GI distress, infections, allergic reaction
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Tocilizumab
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Toxicity:
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Other info:
USES: Rheumatoid arthritis (with or with out methotrexate use)
MECHANISM: IL-6 receptor inhibitor. (Humanized monoclonal IgG antibody)
SIDE EFFECTS: Incr. choleserol. Leukopenia,
TOXICITY: Liver dysfunction
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: More effacious when used with methotrexate. May reduce structural damage. No anti-DNA antibodies
Drug Name: Antithymocyte and antilymphocyte globulin (ATG/ALG
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Antidotes or treatment of toxic effects:
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USES: Transplant therapy (suppression, initial rejection, steroid-resistant rejection)
MECHANISM: Polyclonal antibody- recognizes multiple epitopes on T-cells and opsonizes T-cells via macrophages
SIDE EFFECTS: Injection site rxn, fever, infections, cytokine release syndro
TOXICITY: Anaphylactic and serum sickness rxn
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Antibodies obtained from large animals.
Drug Name: Immune Globulin Intravenous (IGIV)
Where applicable list:

Therapeutic Uses:
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USES: Autoimmune diesorders, asthma
MECHANISM: Polyclonal antibody- no specific antigen targeted. Normalizing effect upon immune network.
SIDE EFFECTS:
TOXICITY: Renal failure, aseptic meningits,Anaphylactic and serum sickness rxn
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Rho (D) immune globulin microdose
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Toxicity:
Antidotes or treatment of toxic effects:
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Other info:
USES: Prevent hymolytic disease in Rh(-) mothers
MECHANISM: Polyclonal antibody- human IgG with antibodies against Rho(D) antigen on RBC's
SIDE EFFECTS: Temperature elevation (rare); discomfort at injection site
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Won't work in Rh sensitized mothers; mother must not already be immunized to Rho.
Drug Name: OKT3
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Toxicity:
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USES: Transplant therapy (prevent acute renal rejection)
MECHANISM: Monoclonal antibody - Mouse antibody to CD3 (on T-cells)
SIDE EFFECTS:
TOXICITY: cytokine release syndrome (via activation of CD3); infection, neoplasia, rapid clearance of host to mouse antibody
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Second line when Cyclosporine A or glucocorticoids fail
Drug Name: Daclizumab & Basiliximab
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Antidotes or treatment of toxic effects:
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Other info:
USES: Transplant therapy (acute renal rejection, induction therapy)
MECHANISM: Monoclonal antibody - Binds to CD-25 (subunit of IL-2 receptor)
SIDE EFFECTS:
TOXICITY: Hypersensitivity and anaphylaxis, infx, neoplasia
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Daclizumab = humanized, Basiliximab = partially humanized
Drug Name: Rituximab
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
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Other info:
USES: Non-Hodgkin's lymphoma, rheumatoid arthritis
MECHANISM: Monoclonal antibody - Chimeric IgG against CD-20 (cell surface molecule and signal transducer on mature B cells) decreases pop of circulating B cells
SIDE EFFECTS: Infusion rxn
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: No disruption of B cell lineage or normal plasma cells
Drug Name: Alemtuzumab
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
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Other info:
USES: B cell chronic lymphocytic leukemia, rheumatoid arthritis (not approved)
MECHANISM: Monoclonal antibody - IgG against CD52 expressed on B, T, NK, monocytes. ADCC
SIDE EFFECTS: Lymphopenia, neutropenia, thrombocytopenia, anemia, infections
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Belimumab
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
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Other info:
USES: SLE, rheumatoid arthritis
MECHANISM: Costimulation inhibitor/ monoclonal antibody - binds B-cell BLyS (responsible for BLySR stimulation),
SIDE EFFECTS:
TOXICITY: Not characterized
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Anti-CD40L antibody
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
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Drug Interactions:
Other info:
USES: Long-term graft survival, SLE, lupus nephritis
MECHANISM: Costimulation inhibitor/ monoclonal antibody - anti CD40L (on T-cells). Inhibits B cell activation, isotype switching. Inhibits B7 expr on macrophages
SIDE EFFECTS:
TOXICITY: Thromboembolic events
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Study stopped early due to toxicity
Drug Name: Alefacept
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:
USES: Plaque psoriasis
MECHANISM: Costimulation inhibitor - Chimeric protein of the CD2-binding portion of LFA-3 fused to FC portion of human IgG. Inhibits activation of T cells
SIDE EFFECTS: Dose dependent reduction of circulating T-cells
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Abatacept
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Antidotes or treatment of toxic effects:
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Other info:
USES: Transplant therapy, rheumatoid arthritis
MECHANISM: Costimulation inhibitor - Chimeric protein of the B7 binding region of CTLA-4 fused to Fc portion of IgG. Inhibits CD28 preving delivery of B7 costim signal. T-cell anergy
SIDE EFFECTS: Infusion rxn, infection
TOXICITY: neoplasia
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: binds to B7 (costimulating found on APC's)
Drug Name: Belatacept
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
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Other info:
USES: Acute renal transplant rejection
MECHANISM: Costimulation inhibitor - Chimeric protein of the B7 binding region of CTLA-4 fused to Fc portion of IgG. Inhibits CD28 preving delivery of B7 costim signal. T-cell anergy
SIDE EFFECTS:
TOXICITY: Less toxic than cyclosporine A
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Higher affinity for B7 than abatacept. (B7 is found on APC's and is a costimulator for T-cell proliferation)
Drug Name: Efalizumab
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:
USES: Psoriasis, possibly IBD, MS, organ transplant
MECHANISM: Inhibitor of lymphocyte trafficking (antibody)- Inhibits interaction betw LFA-1 and ICAM (cell migration)
SIDE EFFECTS: Infections
TOXICITY:
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER:
Drug Name: Natalizumab
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Toxicity:
Antidotes or treatment of toxic effects:
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Drug Interactions:
Other info:
USES: Relapsing MS
MECHANISM: Inhibitor of lymphocyte trafficking (antibody)- inhibits interactions of VLA-4:VCAM-1 & LPAM-1:MAdCAM
SIDE EFFECTS:
TOXICITY: Multifocal leukoencephalopathy (rare fatal viral disease)
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Leukoencephalopathy occurred when used for Crohn's and MS. Withdrawn and reapproved
Drug Name: FTY720
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
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Toxicity:
Antidotes or treatment of toxic effects:
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Other info:
USES: Acute rejection (combo therapy)
MECHANISM: Inhibitor of Lymphocyte trafficking. Agonist for Sphingosine 1-phosphate receptor (expressed on T and B cells). Sequesters cells away from circulation
SIDE EFFECTS:
TOXICITY: Lymphopenia, negative chronotropic effect.
ANTIDOTES: Treat chronotropic effect with B1-receptor antagonist or atropine
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Chronotropic effect due to S1P-R expression on atrial myocytes.
Drug Name: Glucocorticoids
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
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Drug Interactions:
Other info:
USES: Transplant, GVH, Autoimmune disorders, asthma, allergies
MECHANISM: Transcription inhibitor of many inflammatory cytokines
SIDE EFFECTS: Infections, poor wound healing, growth retardation, hypertension, adrenal insufficiency
TOXICITY:
ANTIDOTES: None, taper as carefuly possible
CONTRAINDICATIONS:
INTERACTIONS:
OTHER: Use with caution
Drug Name: Azathioprine (AZA)
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
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Drug Interactions:
Other info:
USES: Transplant, IBD, rheumatoid arthritis
MECHANISM: Antimetabolite-Inhibition of de novo purine synthesis (production of 6-mercaptopurine)
SIDE EFFECTS: Bone marrow suppression, susceptibility to infx.
TOXICITY: Neoplasia, pancreatitis, GI, alopecia
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS: Allopurinal, ACEi
OTHER:
Drug Name: Mycophenolate mofetil
Where applicable list:

Therapeutic Uses:
Mechanism of Action:
Side Effects:
Toxicity:
Antidotes or treatment of toxic effects:
Contraindications:
Drug Interactions:
Other info:
USES: Transplant, Steroid refract GVH, lupos, nephritis, dermatologic disorders
MECHANISM: Antimetabolite- Noncompetitive, reversible inhibitr of IMPDH
SIDE EFFECTS: Leukopenia, diarrhea, vomiting
TOXICITY: Sepsis w/ CMV, bad viral infx.
ANTIDOTES:
CONTRAINDICATIONS:
INTERACTIONS: Acyclovir/ganciclovir, tacrolimus, some antacids, cholestyramine
OTHER: B&T cells are highly dependent on de novo purine synth pathway