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Immunostimulants & immunosuppressants

This document discusses immunomodulators, which are drugs that either suppress (immunosuppressants) or enhance (immunostimulants) the immune system. It describes several classes of immunosuppressants including calcineurin inhibitors like cyclosporine and tacrolimus, antiproliferative agents like azathioprine, mTOR inhibitors like sirolimus, glucocorticoids like prednisolone, and biologics like infliximab. Their mechanisms of action, uses, and adverse effects are summarized. Immunostimulants discussed include levamisole, thalidomide, BCG vaccine, and interferons.

Health & Medicineā—¦
IMMUNOMODULATORS -NIRALI THAKKAR (FROM SMT S.M.SHAH PHARMACY COLLEGE)
IMMUNOMODULATORS IMMUNOSUPPRESSANT IMMUNOSTIMULANT
-These are drugs that suppress the immune response. -Their main therapeutic application is in autoimmune diseases and organ transplantation. IMMUNOSUPPRESSANTS
CLASSIFICATION 1.Calcineurin inhibitors: Cyclosporine ,Tacrolimus 2.Antiproliferative and cytotoxin agents : Azathioprine, methotrexate,cyclophosphamide 3. mTOR(mammalian target of rapamycin)inhibitors:Sirolimus 4.Glucocorticoids : Prednisolone ,methylprednisolone 5.Biologics : (a)TNF-Ī± inhibitors: Etanercept ,Infliximab (b)IL-1 inhibitors: Anakinra (c)Antibodies: Muromonab-CD3 , anti-thymocytes and anti-lymphocyte antibodies
MECHANISM OF ACTION
1.CALCINEURIN INHIBITORS -Cyclosporine: Very lipophilic and essentially not soluble in water administered orally , i.v. and i.v. infusion Mechanism of action : enters in target cells ā†“ binds to cyclophilin ā†“ cyclosporine ā€“ cyclophilin complex ā†“ inhibit calcineurin and blocks activation of T cells and decresed production of IL-2 and other cytokines
1.CALCINEURIN INHIBITORS Uses: -prevent and treat rejection episodes in organ transplantation like kidney,bone marrow,liver etc -treat autoimmune diseases like myasthenia gravis, rheumatoid arthritis etc.
1.CALCINEURIN INHIBITORS Adverse effects: -Nephrotoxicity -Hepatotoxicity -Hypertrophy of Gums -Hypertension -Hyperglycemia -Hyperlipidemia -Increased susceptibility to infections -Bone marrow toxicity is minimal
1.CALCINEURIN INHIBITOR Drug Interaction : -Cyclosporine Ɨ Aminoglycoside/Amphotericin B/Vancomycin/ NSAIDS: Nephrotoxicity is enhanced -Cyclosporine Ɨ Rifampicin/Phenobarbitone/Phenytoin: The blood level of Cyclosporine is reduced due to induction of its metabolism -Cyclosporine Ɨ Erythromycin: The plasma level of Cyclosporine is increased as its metabolism is inhibited by
2. ANTIPROLIFERATIVE AGENTS -Azathioprine: -It is a purine antimetabolite -Incorporation of false nucleotide Mechanism of action : Taken up into the immune cells ā†“ Activated to 6-MP ā†“ Inhibits purine synthesis ā†“ Inhibition of cell Proliferation and impairment of lymphocyte funtion
2. ANTI PROLIFERATIVE AGENTS Uses : -Used in combination with glucocorticoids or cyclosporine for prevention of rejection episodes in organ transplantation -Used in rheumatoid arthritis , Crohnā€™s disease etc Adverse effects : -Hepatotoxicity -Bone marrow suppresion -Gastrointestinal side effects
3. mTOR Inhibitors Sirolimus : It inhibits T-cell activation and Proliferation. -Mechanism of action: It forms complex with an immunophilin ā†“ Inhibits a key enzyme in cell cycle progression ā†“ Inhibits the response of interleukin-2 ā†“ That blocks activation of T-cells and B-cells
3. mTOR Inhibitors Uses : -To treat and prevent graph rejection reaction Adverse effects :-Myelosuppression -Headache -Hepatotoxicity -Hypokalemia -Risk of infection -Thrombocytopenia
4.GLUCOCORTICOIDS Prednisolone : Induce redistribution of lymphocytes that decrease in peripheral blood lymphocyte count . Mechanism of action : Inhibit proliferation of T-lymphocytes ā†“ Decrease expression of interleukines ā†“ Blocks the activation of T-cells and B-cells
4.GLUCOCORTICOIDS Uses : -To prevent and treat rejection episodes during organ transplantation. -Autoimmune diseases. Adverse effects : -Osteoporosis -Hyperglycemia -Risk of Infection -Poor wound healing -A vascular necrosis of bone -Hypertension
5. BIOLOGICS Infliximab : -It is a Chimeric antibody (25% mouse derived, 75% human protein) Mechanism of action : It forms a relatively stable complex ā†“ Binds to soluble and membrane bound TNF ā†“ That blocks activation of T-lymphocytes
5. BIOLOGICS Uses : -Rheumatoid arthritis -Crohnā€™s Disease Adverse Effects : -Infusion reactions like fever,urticaria,hypotension, dysponea -Opportunistic infection like TB , urinart tract infection
IMMUNOSTIMULANTS -These are drugs that enhance the immune response by inducing activation or increasing activity of any of its componants. -It is also called as immunostimulators.
Immuno stimulants specific Non- specific
IMMUNOSTIMULANTS Specific : Provide antigenic specificity in immune response. such as vaccines and any antigen Non-Specific : Many endogenous substances are non-specific. such as female sex hormones , other hormones like prolactin , growth hormone , vitamin D
IMMUNOSTIMULANTS -Levamisole : Use as an adjuvant in colon cancer -Thalidomide: Use in Rheumatoid arthritis , Lepra reaction, Multiple myeloma -BCG vaccine: Use in carcinoma -Interferone : Use in hairy cell leukaemia , malignant melanoma , AIDS related kaposiā€™s sarcoma
IMMUNOSTIMULANTS Thalidomide : -Enhanced T cell production of cytokines IL-2 ,IFN-y -Increase TNF-Ī± in patients who are HIV seropositive -Birth defect . -Contraindicated in women having child bearing potential .
Immunostimulants & immunosuppressants