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    1 - Immuno Tables1

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    Urugonda Venumadhav
    This document summarizes various immunosuppressive drugs, including their mechanisms of action, pharmacokinetics, uses, and adverse effects. The drugs discussed include cyclosporine, tacrolimus, sirolimus, mycophenolate mofetil, azathioprine, leflunomide, cyclophosphamide, antithymocyte globulins, basiliximab, dacilizumab, Rho(D) immunoglobulin, and corticosteroids. These drugs work through a variety of mechanisms to suppress the immune system and are used to prevent rejection of organ transplants and treat autoimmune diseases. Common adverse effects across many of the drugs include hypertension, hyperlipidemia

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    1 - Immuno Tables1

    Uploaded by

    Urugonda Venumadhav
    60 views4 pages
    This document summarizes various immunosuppressive drugs, including their mechanisms of action, pharmacokinetics, uses, and adverse effects. The drugs discussed include cyclosporine, tacrolimus, sirolimus, mycophenolate mofetil, azathioprine, leflunomide, cyclophosphamide, antithymocyte globulins, basiliximab, dacilizumab, Rho(D) immunoglobulin, and corticosteroids. These drugs work through a variety of mechanisms to suppress the immune system and are used to prevent rejection of organ transplants and treat autoimmune diseases. Common adverse effects across many of the drugs include hypertension, hyperlipidemia

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    1- Immuno Tables1

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    This document summarizes various immunosuppressive drugs, including their mechanisms of action, pharmacokinetics, uses, and adverse effects. The drugs discussed include cyclosporine, tacrolimus, sirolimus, mycophenolate mofetil, azathioprine, leflunomide, cyclophosphamide, antithymocyte globulins, basiliximab, dacilizumab, Rho(D) immunoglobulin, and corticosteroids. These drugs work through a variety of mechanisms to suppress the immune system and are used to prevent rejection of organ transplants and treat autoimmune diseases. Common adverse effects across many of the drugs include hypertension, hyperlipidemia

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    60 views4 pages

    1 - Immuno Tables1

    Uploaded by

    Urugonda Venumadhav
    This document summarizes various immunosuppressive drugs, including their mechanisms of action, pharmacokinetics, uses, and adverse effects. The drugs discussed include cyclosporine, tacrolimus, sirolimus, mycophenolate mofetil, azathioprine, leflunomide, cyclophosphamide, antithymocyte globulins, basiliximab, dacilizumab, Rho(D) immunoglobulin, and corticosteroids. These drugs work through a variety of mechanisms to suppress the immune system and are used to prevent rejection of organ transplants and treat autoimmune diseases. Common adverse effects across many of the drugs include hypertension, hyperlipidemia

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    Immunosuppressives

    Drug Mechanism of action Pharmacokinetics Uses


    -Prevents rejection of kidney, liver and cardiac allogenic transplants -Alternative to methotrexate for severe active rheumatoid arthritis -For autoimmune diseases (Uveitis; RA; early treatment of diabetes mellitus type 1). - Recalcitrant psoriasis and asthma. -Taken orally or i.v -Oral absorption is variable and is decreased if taken with high fat or high carbohydrate meals -Metabolized in the liver -Excreted mainly in the bile

    Adverse affects
    Nephrotoxicity Hepatotoxicity. Hypertension and hyperlipidemia. Infections (viral). Hyperkalemia. Lymphoma and cancer. Glucose intolerance (diabetes). Anaphylacticreaction. Neurotoxicity Hirsutism. Gingival hyperplasia. -More nephrotoxic, neurotoxic -Post-transplant insulin dependent diabetes mellitus -like those of cyclosporine except it doesnt cause hirsutism or gingival hyperplasia.

    Cyclosporine

    forms a complex with cyclophilin which in turn inhibits the calcineurin

    -Orally or parenterally -Excreted through biliary route -Metabolized in liver

    Tacrolimus

    As cyclosporine (calcineurine antagonist) but it binds to different immunophillin (FKBP)

    Prevention of rejection of liver and kidney transplants moderate to severe atopic dermatitis organ transplantation for women

    Drug

    Mechanism of action

    Pharmacokinetics

    uses

    Adverse effects
    Hyperlipidemia Pneumonitis

    Sacrolimus

    Tacrolimus bind to FKBP and forms a complex with mTOR

    -Taken orally fat meals can its absorption -Extensively bound to BP -Eiminated mainly in feces

    Myelosuppression -Prevention of rejection of renal transplant -Hematopoietic stem cell transplant -Used in cardiology Hepatoxicity Diarrhea Hypertension. Leucopenia Thrombocytopenia

    Mycophenolate mofetil

    Uncompetitive inhibition of inosine monophosphate dehydrogenase

    -Taken orally -Hydrolyzed in GIT into mycophenolic acid (MPA) -Glucuronidated in liver -Excreted in urine. Oral Widely distributed Metabolized in the liver Excreted by the kidney

    - Solid organ transplant alternative drug to cyclosporine and tacrolimus - Lupus nephritis, rheumatoid arthritis - As replacement of azathioprine or cyclophosphamide for autoimmune diseases -Severe rheumatoid arthritis. -Non-responding atopic dermatitis. -Can be used for glomerulonephtitis, SLE, Crohns disease and multiple sclerosis. -Maintenance of renal allograft and other transplantations.

    - Pain - Diarrhea - Sepsis - Leukopenia - Lymphoma -Severe bone marrow suppression -Hypersensitivity -Hepatic dysfunction -It is not teratogenic but can be carcinogenic

    Azathioprine

    Prevents denovo synthesis of purines required for cell division

    Drug
    Leflunomide

    Mechanism of action
    Inhibitor of Pyrimidine synthesis rather than purine
    Destroys proliferating lymphoid cells & alkylate some resting cells (very toxic).

    Pharmacokinetics
    Orally active

    Uses
    Used only for rheumatoid arthritis It was the drug of choice for treatment of many autoimmune diseases,

    Adverse effects
    Alopecia increase LFT, nephrotoxicity, teratogenicity
    Pancytopenic, heamorgenic cystitis, Infertility. Chill.

    Cyclophosphamide

    Antithymocyte globulins

    The antibodies bind to T-lymphocytes antibodies-bound cells are phagocytosed in the liver and spleen lymphopenia and impaired T-cells responses.

    IM, IV infusion. T1/2 = 9 days.

    Hyperacute phase of allograft rejection prepare the recipient to the transplantation of bone marrow

    Fever. Leucopenia. Thrombocytopenia. Infections and hypersensitivity. Lymphoma and cancer

    Immune globulin Intravenous Muromonab- CD3

    Has no antigenicity I.V injection extensively metabolized and eliminated predominantly in bile

    Refractory ITP Acute rejection of renal , cardiac & hepatic allograft prior to transplantation of bone marrow

    disruption of T-lymphocytes function.

    Severe hypersensitivity CNS effects as seizures Severe infections

    Drug
    Basiliximab Dacilizumab Rho (D) immunoglobulin microdose

    Mechanism of action
    bind to -chain of the IL-2 receptor on activated T-cells leading to loss of any antigenic stimulus to activate the T-cell response system. Suppress mothers own antibody response to the foreign Rho (D) positive cells she has no memory B-cells that can be activated upon subsequent pregnancies with a Rho (D) positive fetus

    Kinetics
    Given I .V T 1/2 = 7 days Given I .V T 1/2 = 20 days

    uses
    Acute rejection in renal transplantation

    Adverse effects
    - GIT problems - No clinically relavant antibodies to the drugs have been detected -Malignancy not a problem Pain at the site of injection Fever

    2 ml intramuscularly

    Erythroblastosi Faetalis miscarriages

    Corticosteroids

    At biochemical level: act on gene expression, which lead to decrease synthesis of prostaglandins, leukotrienes, cytokines and other signaling molecules that participate in immune response. At the cellular level: they inhibit the proliferation of T lymphocytes (cell mediated) and slightly dampen humoral immunity (by increasing the catabolism of immunoglobulins). At immunosuppressive doses: Corticosteroids are cytotoxic and continuous use lowers IgG.

    - In combination with other immunossppressants for transplanted patients (To prepare the patients as well as maintenance). - To treat acute rejection episodes (high doses) - To treat undesirable immunoreactions (to drugs or asthma). -To autoimmune diseases (Idiopathic thrombocytopenic purpra, inflammatory bowel disease, rheumatoid arthritis, systemic lupus erythematosus and glomerulonephritis)

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