| A | B |
|---|
| Azathioprine | Bimodal metabolizers; supressed B cells, T cells, IL-2 |
| Methotrexate | Ist choice tx for RA. Used at much lower doses than in cancer chemotherapy. |
| Cyclophosphamide | Suppresses T/B-cell fx. T-cell suppression impt for rheumatic diseases. |
| Chlorambucil | Suppresses T/B-cell fx. T-cell suppression impt for rheumatic diseases. |
| Cyclosporine | Inhibits IL-1 and IL-2 receptor production, 2ndarily inhibits macrophate-Tcell interaction and T-cell responsiveness |
| Mycophenolate Mofetile (MMF) | Inhibits T-cell proliferation, interferes with leukocyte adhesion to endo cells |
| Chloroquine & Hydroxychloroquine | Supprection of T-cell response to mitogens, ? chemotaxis, stabilizes lysosomal enzymes, inhibts DNA/RNA synthesis, traps free radicls |
| Penicillamine | Rarely used b/c of toxicity |
| Leflunomide | Inhibits T-cell proliferation and production of autoantibodies by B-cells |
| Sulfasalazine | Decr. IgA & IgM rheumatoid factor, Suppresion of T-cells to concanavalin, inhibits B-cell proliferation |
| Abatacept | Prevents T-cell activation |
| Infliximab | AntiTNF. In long term combo with methotrexate it ? formation of new erosions more then methotrexate alone |
| Etanercept | Anti-TNF. Also inhibits lymphotoxin-? |
| adalimumab | Anti-TNF. Down regulates macrophage and T-cell fx |
| Major metabolite= 6-thioguanine which suppresses inosinic acid synthesis, | Azathioprine MOA |
| Inhibits AICAR transformylase and thymidylate synthestase with 2ndary effects on PMN chemotaxis | Methotrexate MOA |
| Cross-links DNA to prevent cell replication. | Cyclophosphamide MOA |
| Cross-links DNA to prevent cell replication. | Chlorambucil MOA |
| Acts through regulation of gene expression. | Cyclosporine MOA |
| Inhibits cytosine monophosphate dehydrogenase. Ihnhibits E-selectin, P-selectin and intercellular adhesion molecule 1 | Mycophenolate Mofetile (MMF) MOA |
| Unclear | Chloroquine & Hydroxychloroquine MOA |
| Metabolite of penicillin/analogy of AA cystine. | Penicillamine MOA |
| Inhibits Dihydroorotate dehydrogenase; arrests stimulated cells in G1 | Leflunomide MOA |
| Sulfapyridine is active metabolite in RA. Low bioavailability | Sulfasalazine MOA |
| Costimulation modulator, binds CD80 & CD86 preventing binding of CD28. | Abatacept MOA |
| Chimeric monoclonal antibody that targets CD20 B-cells | Rituximamb MOA |
| Chimeric IgG1; binds TNF-? | Infliximab MOA |
| fusion protein of two TNF p75 receptor moieties linked to Fc portion of IgG1 | Etanercept MOA |
| Fully human IgG1 anti-TNF monoclonal antibody. Give subcutenously | adalimumab MOA |
| Azathioprine Indications | Rheumatoid arthritis, psoriatic arthritis, reactive arthritis, polymyositis, SLE, Behcet's Disease |
| Methotrexate Indications | RA, SLE, Juvenile arthritis, psriatic arthritis, ankylosing spondylitis, polymyositis, dermatomyositis, giant cell arthritis, |
| Cyclophosphamide Indications | rheumatoid arthritis, SLE, vasculitis, Wegner's granulomatosis, other severe rheumatoid diseases |
| Chlorambucil Indications | RA, Behcet's disease, SLE, vasculitis. |
| Cyclosporine Indications | RA , SLE, polymyosistis, dermatomyosistis, Wegner's granulomatosis, Juvenile Chronic Arthritis |
| Mycophenolate Mofetile (MMF) Indications | Renal disease due to SLE. Useful in vasculitis, & Wegner's syn |
| Chloroquine & Hydroxychloroquine Indications | Rhematoid arthritis, but not very effective against other DMARDs. Primarily for malaria treatment |
| Penicillamine Indications | Rhematoid arthritis |
| Leflunomide Indications | as effective as methotrexate in RA including inhibn of bony damage |
| Sulfasalazine Indications | Rhematoid arthritis, Juvenile chronic arthritis, ankylosing spondylitis |
| Abatacept Indications | RA unresponsive to other DMARDs or TNF antagonists |
| Rituximamb Indications | treats RAs that's refractory to antiTNF agents. in combo with methotrexate |
| Infliximab Indications | RA, ankylosing spondylitis, crohn's disease, psoriatic arthritis |
| Etanercept Indications | RA, juvenile chronic arthritis, psoriasis, psoriatic arthritis, ankylosing spondylitis. Used as monotherapy or with methotrexate |
| adalimumab Indications | RA, ankylosing spondylitis, psoriatic arthritis. Decr. formation of new erosions. |
| Myelosuppresion, GI probs, risk of infection and Lymphoma. Rare allergic reactions. | Azathioprine Side Effects |
| Nausea, Mucosal ulcers, hepatotoxicity from enzyme elevations, rare hypersensitivity lung rx with shortness of breath. CONTRAINDICATED in pregnancy. | Methotrexate Side Effects |
| Infertility in men & women, myelosuppression, alopecia, hemorrhagic cystitis, bladder carcinoma (rare) | Cyclophosphamide Side Effects |
| myelosuppresion, infertility with azoospermia and amenorrhea. risk of neoplasia (10x) | Chlorambucil Side Effects |
| Nephrotoxicity, drugs that inhibit CYP3A, hypertension, hyperkalemia, hepatotoxicity, gingival hyperplasia, hirsutism. (Monitor serum creatinine) | Cyclosporine Side Effects |
| Similar to azathiprine in GI, myelosuppresion, & hepatic toxicity | Mycophenolate Mofetile (MMF) Side Effects |
| Ocular toxicity at high dose (should monitor for this). Dyspepsia, nausea, vomiting, abdominal pain, rashes, nightmares | Chloroquine & Hydroxychloroquine Side Effects |
| GI probs (diarrhea), elevates liver enzymes. CONTRAINDICATED IN PREGNANCY | Leflunomide Side Effects |
| nausea, vomiting, headache, rash. Reversibile infertility in men only. Drug induced lupus, Hemolytic anemia, methemoglobinemia, Neutropenia rarely. NOT teratogenic | Sulfasalazine Side Effects |
| risk of URT infection, DO NOT use with TNF antagonists. Hypersensitivity Rx's. Possible lymphoma & lung cancer risks. | Abatacept Side Effects |
| URT infections, nausea, headache, sinusitis, rash, cough. RARELY causes a lupus like rx. Use antihistamines to minimize infusion site rx's. | Infliximab Side Effects |
| Activation of latent tuberculosis. Can lead to lupus like rx's. | Etanercept Side Effects |
| risk for macrophage-dependent infections (including Tb). Rarely lupus like rx's and leukopenias and vasculitis. | adalimumab Side Effects |
| Infliximab Side Effects | May activate latent tuberculosis (should screen for this). DO NOT use in multiple sclerosis patients |
