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Biologic DMARDs Overview
What conditions are treated with Ustekinumab?
Psoriasis and psoriatic arthritis.
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Uses of Conventional Synthetic DMARDs
What are the uses of Azathioprine?
Rheumatoid arthritis and prevention of organ transplant rejection.
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Immunosuppressive Properties of DMARDs
Name some immunosuppressors mentioned.
Azathioprine, Cyclosporine, Mycophenolate Mofetil, Abatacept, and Tofacitinib.
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Toxicities and Risks of DMARDs
What is a significant risk of Rituximab?
High risk of hypersensitivity and may reactivate Hepatitis B.
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Uses of Conventional Synthetic DMARDs
What are the uses of Chloroquine?
Rheumatoid arthritis and malaria (in areas not resistant to chloroquine).
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Biologic DMARDs: Abatacept, Rituximab, and Tocilizumab
What is the mechanism of action of Tocilizumab?
Binds IL-6 receptor, inhibiting IL-6 mediated signaling.
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TNF-alpha Blockers and their Applications
What conditions are treated with TNF-alpha blockers?
Rheumatoid arthritis and inflammatory bowel disease.
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Specific DMARDs: Azathioprine, Cyclophosphamide, and Cyclosporine
What is the mechanism of action of Azathioprine?
Inhibits macrophage-T cell interaction and T-cell responsiveness.
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Toxicities and Risks of DMARDs
What is a significant risk associated with Cyclophosphamide?
Hemorrhagic cystitis due to accumulation of acrolein.
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Toxicities and Risks of DMARDs
What are some side effects of Sulfasalazine?
Hypersensitivity reactions, hemolytic anemia, and reversible infertility in men.
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Specific DMARDs: Azathioprine, Cyclophosphamide, and Cyclosporine
What does Leflunomide inhibit?
Dihydroorotate dehydrogenase.
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Mechanism of Action of DMARDs
What is the mechanism of action of Cyclophosphamide?
Phosphoramide mustard binds DNA, preventing cell replication and suppressing T and B-cell function.
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Uses of Conventional Synthetic DMARDs
How often is Leflunomide administered?
Once a week or every 2 weeks.
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Uses of Conventional Synthetic DMARDs
What conditions is Sulfasalazine used to treat?
Rheumatoid arthritis and inflammatory bowel disease.
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Uses of Conventional Synthetic DMARDs
What conditions is Tocilizumab used for?
Rheumatoid arthritis and COVID-19.
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TNF-alpha Blockers and their Applications
What is the effect of TNF-alpha blockers on macrophage and T-cell function?
They downregulate macrophage and T-cell function.
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Toxicities and Risks of DMARDs
What rescue agent is given with Methotrexate to mitigate toxicity?
Leucovorin (Folinic acid).
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Uses of Conventional Synthetic DMARDs
What conditions is Mycophenolate Mofetil used for?
Rheumatoid arthritis, SLE, and vasculitis.
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Specific DMARDs: Azathioprine, Cyclophosphamide, and Cyclosporine
What is a major use of Tofacitinib?
Prevention of organ transplant rejection.
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Specific DMARDs: Azathioprine, Cyclophosphamide, and Cyclosporine
What is the effect of Leflunomide on T-cell proliferation?
Decreased T-cell proliferation and decreased antibody production by B-cells.
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Toxicities and Risks of DMARDs
What is a significant risk associated with Mycophenolate Mofetil?
Reversible myelosuppression and hepatotoxicity.
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Biologic DMARDs: Abatacept, Rituximab, and Tocilizumab
What is the mechanism of action of Abatacept?
Binds to CD80 and CD86, inhibiting CD28 and T-cell production.
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Toxicities and Risks of DMARDs
What is a notable toxicity of Chloroquine?
Ocular toxicity (corneal and retinal pigmentation).
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Toxicities and Risks of DMARDs
What is a risk associated with Tocilizumab?
May reactivate latent TB.
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Specific DMARDs: Azathioprine, Cyclophosphamide, and Cyclosporine
What condition is Azathioprine used to prevent?
Organ transplant rejection.
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Mechanism of Action of DMARDs
What is the mechanism of action of Chloroquine?
Inhibits DNA and RNA synthesis and binds free radicals.
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Specific DMARDs: Azathioprine, Cyclophosphamide, and Cyclosporine
What does Sulfasalazine inhibit?
Sulfapyridine, leading to inhibition of inflammatory cytokine release.
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Toxicities and Risks of DMARDs
What is a risk associated with Abatacept?
Increased risk of infection and may reactivate latent TB and Hepatitis B.
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Toxicities and Risks of DMARDs
What is a significant risk associated with Azathioprine?
Increased incidence of lymphoma.
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Specific DMARDs: Azathioprine, Cyclophosphamide, and Cyclosporine
What does Mycophenolate Mofetil inhibit?
Cyclophosphamide monophosphate dehydrogenase.
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Mechanism of Action of DMARDs
What is the mechanism of action of Methotrexate?
Inhibits Aminoimidazole carboxamide ribonucleotide (AICAR) transformylase and Thymidylate synthase, leading to increased adenosine and inhibition of inflammation and chemotaxis of PMNs.
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Toxicities and Risks of DMARDs
Who should not be given Tofacitinib?
Patients with severe hepatic disease.
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Toxicities and Risks of DMARDs
What is a common side effect of Leflunomide?
Diarrhea and elevated liver enzymes.
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Mechanism of Action of DMARDs
What is the mechanism of action of Cyclosporine?
Inhibits IL1 and IL2 receptor.
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Toxicities and Risks of DMARDs
What infections may TNF-alpha blockers reactivate?
Latent TB and Hepatitis B.
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Mechanism of Action of DMARDs
What is the mechanism of action of Azathioprine?
Forms 6-thioguanine, which suppresses T and B cell function.
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Uses of Conventional Synthetic DMARDs
What conditions is Abatacept used for?
Rheumatoid arthritis and psoriatic arthritis.
