Drug used in treatment of rheumatoid arthritis that acts by inhibition of T-cell proliferation?
Correct Answer: Leflunomide
Description: Ans. d (Leflunomide) (Ref. H - 16th ed. Table 295-14 & p. 1968).# LEFLUNOMIDE metabolized to an active metabolite that acts to inhibit dihydroorotate dehydrogenase, an essential enzyme in the pyrimidine biosynthetic pathway.# Its predominant action is to inhibit the proliferation of T lymphocytes.# It is as effective as methotrexate.# Leflunomide can be given alone or with methotrexate.# The major side effect is the associated increase in liver function enzymes.DMARDs# May slow or reverse joint damage# Indicated for the treatment of RA when an ati-inflammatory therapy insufficient to control patient's symptomatology# DMARDs usually do not show benefit for 6-8 weeks or longer; so, bridging therapy# DMARDs have severe and potentially fatal side effectsHydrochloroquine# Stabilizes lysosomes, chemotaxis# Also an antimalarialOphthalmic abnormalities, dermatologic reactions hematotoxicity, GI reactionsMethotrexate# Inhibits dihydrofolate reductase, immunosuppressant# Also an antineoplasticHemotoxicity, ulcerative stomatitis, renaltoxicity, elevated LFTsSulfasalazine# Metabolized to 5-aminosalicylic acid (5 ASA) and sulfapyridine; parent drug and/or metabolites have anti-inflammatory and/or immunomodulatory properties# Used in inflammatory bowel diseaseRash, GI distress, headache, hematotoxicityGold compounds# Macrophage and lysosomal functionsDermatitis, hematotoxicity, nephrotoxicityAzathioprine# Purine metabolism and nucleic acid synthesis# ImmunosuppressantHematologic, GI disturbance, secondary infection, increased risk of neoplasiaPenicillamine# T-cell activity and rheumatoid factor# Also a chelating agentGI disturbances, proteinuria, bone marrow suppression, neurotoxicityEtanerceptBinds TNFInjection site reactionsLeflunomideInhibits cell proliferation and anti-inflammatoryHepatotoxicity, immunosuppression, GI disturbance, alopecia, rash,teratogenInfliximab# Monoclonal antibody to TNF-a# Also used in inflammatory bowel diseaseInfusion reactions, infections, activation of latent TB Immunomodulatory Agents1Recombinant TNF-receptor-Ig fusion protein (etanercept)# Inhibit TNF-alpha# FDA approved for rheumatoid arthritis, juvenile rheumatoid arthritis, psoriasis2Anti-IL-6 monoclonal antibody# Inhibit IL-6, Tested in phase 1 trial in rheumatoid arthritis3Inferferon-ss# Inhibit IL-1, decrease synovial T cells# In trials for use in rheumatoid arthritis4Interferon-gamma# Induce monocyte/macrophage activation Agents# Effective in treating monocyte/macrophage phagocytic defects in chronic granulomatous disease.5IL-11# Inhibit TNF-a and IL-1 production# In trials for Crohn's colitis6IL-12# Stimulate anti-tumor and anti-viral or bacterial cytotoxic T lymphocyte responses# Trials underway for use in cancer patients# Trials planned in humans to prevent/treat severe infections7Anakinra # Inhibit IL-la and -ss FDA approved for rheumatoid arthritis. Anakinra is a recombinant IL2-1 receptor antagonist that competitively blocks the binding of IL-1ss and IL-la to the IL-1 receptor and thereby inhibits the activity of these two related proinflammatory cytokines.# Anakinra has been shown to improve the signs and symptoms of RA, to decrease disability, and to slow progression of articular damage associated radiographically.8Etanercept# A recombinant fusion protein consisting of two soluble TNF p75 receptor moieties linked to the Fc portion of human IgGl; it binds TNF-alpha molecules and also inhibits lymphotoxin- alpha.# Etanercept is approved for the treatment of rheumatoid arthritis, juvenile chronic arthritis, and psoriatic arthritis and ankylosing spondylitis.# While etanercept is ineffective for treatment of ulcerative colitis, it is being used in many rheumatic syndromes such as scleroderma, Wegener's granulomatosis, giant cell arteritis, and sarcoidosis.9Adalimumab# Adalimumab is a fully humanized antibody (IgGl) used in treatment of rheumatoid arthritis.# A recombinant human anti-TNF monoclonal antibody.# This compound complexes with soluble TNF-a and prevents its interaction with p55 and p75 cell surface receptors.# This results in down-regulation of macrophage and T cell function.# The compound is indicated for the treatment of rheumatoid arthritis and decreases the rate of formation of new erosions.# It is effective both as monotherapy and in combination with methotrexate.# The usual dose is 40 mg every other week, though increased responses may be evident at higher dosages.# Adalimumab is presently being tested in psoriasis, psoriatic arthritis, ankylosing spondylitis, and juvenile chronic arthritis.10Infliximab# A chimeric (25% mouse, 75% human) monoclonal antibody that binds with high affinity to soluble and possibly membrane-bound TNF-a.# Its mechanism of action probably is the same as that of Adalimumab.# Infliximab is effective in rheumatoid arthritis and ulcerative colitis and is being used in other diseases, including psoriasis, psoriatic arthritis, juvenile chronic arthritis, Wegener's granulomatosis, giant cell arteritis, and sarcoidosis.# Infliximab, etanercept, and adalimumab are new biologic agents that bind TNF-a, a proinflammatory cytokine. # Infliximab is currently approved for use in Crohn's disease of the colon and in rheumatoid arthritis.11 Leflunomide# Inhibits T cell proliferation and production of autoantibodies by B cells.# Effects include increases of interleukin-10 receptor mRNA, decreased interleukin-8 receptor type A mRNA, and decreased TNF-a-dependent NF-B activation.# Used in treatment of RA.RITUXIMAB (anti-CD20 antibody)# It is an anti-CD20 antibody that also has clinical activity: CLL, NHL (relapsed or refractory low-grade or follicular B cell non-Hodgkin's lymphoma.) and Ca colon.# Rituximab may be used in treatment of:- B cell chronic lymphoid leukemia,- Follicular lymphoma,- Mantle cell lymphoma,- Cold agglutinin disease,- Idiopathic thrombocytopenic purpura, and- Waldenstrom's macroglobulinemia- Rituximab is also used with methotrexate to treat moderate-to-severe forms of rheumatoid arthritis.
Category:
Medicine
Get More
Subject Mock Tests
Practice with over 200,000 questions from various medical subjects and improve your knowledge.
Attempt a mock test nowMock Exam
Take an exam with 100 random questions selected from all subjects to test your knowledge.
Coming SoonGet More
Subject Mock Tests
Try practicing mock tests with over 200,000 questions from various medical subjects.
Attempt a mock test now