This document provides an overview of immunomodulators, which are drugs that modulate the immune system by either suppressing or stimulating it. It discusses the components of the immune system and classifies immunomodulators into immunosuppressants and immunostimulants. Examples of immunosuppressants discussed include corticosteroids like prednisolone, antimetabolites like methotrexate, antibiotics like cyclosporine. Their mechanisms of action and uses for suppressing the immune system, such as for organ transplants, are described. Immunostimulants are also briefly introduced as substances that can activate or increase immune system activity.

1. Immunomodulators
Prepared By :-
Arjun S. Dhawale
[Student of B Pharm 4thyear 2018-2019]
Under the guidance of :-
Prof. Pravin Khatale
[M.Pharm ;Prof . S.G.S.P.S IOP, Akola]
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2. Contents:-
1) Introduction.
2) Components of Immunity .
3) Classification of Immunomodulants .
4) Immunosuppressant .
5) Immunostimulant .
6) Reference .
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3. Introduction:-
The immune system constitutes the body’s defense
against infectious agents. It protects the host by identifying and
eliminating or neutralizing agents that are recognized as nonself. The
entire range of immunological responses affects essentially every
organ, tissue, and cell of the body.
Immune responses include, in part, antibody (Ab)
production, allergy, inflammation, phagocytosis, cytotoxicity,
transplant and tumor rejection .
Types of Immunity:-
1) Active Immunity .
2) Passive Immunity .
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4. 1)Active Immunity :-
It can be imparted either naturally by means of a clinical or
subclinical infection or artificially by injection of
appropriate antigen in the form of vaccine or toxides.
These vaccine contains the microbials strains of abnormaly
low pathogenicity.
Their administration lead to antiginic stimulus are
formation of antibodies at much faster rate. This type of
immunity normaly long lasting.
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5. 2) Passive Immunity:-
This type of Immunity can be imparted either naturally by
placental transfer of mother to antibodies to her child.
Passive immunity offers protection immidietly but such a
protection is short duration.
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6. Components Of Immunity:-
1) Lymphocytes
2) Cellular Immunity
3) Humoral Immunity
a) Immunoglobulin G
b) Immunoglobulin A
c) Immunoglobulin M
d) Immunoglobulin D
e) Immunoglobulin E
4) Immunoglobulin (Antibiotics)
5) Lymph nodes
6) Spleen
7) Thymus 6

7. Immunomodulators:-
Defn: These are the drugs or agents which either stimulant
or suppressant effect on immune system.
They are categorised as:-
1) Immunosuppressant.
2) Immunoenhancer.
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8. Classification of Immunomodulator:-
I]Corticosteroids:
Eg. Betamithasone, Prednisolone.
II]Alkylating Agents:
Eg. Cyclophosphamide.
III]Antimetabolites:
Eg. Mercaptopurine, Methotrexate.
IV]Antibiotics:
Eg. Cyclosporines A.
v]Enzymes:
Eg. L- Asparginage.
VI]Antibodies:
Eg. Antithymocyte globulin.
VII]Miscellaneous Agents:
Eg. Bredinin, Niridazole.
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9. Immunosuppressant :-
1]Corticosteroids
Eg. 1) Betamethasone
2) Prednisolone
3) Hydrocortisone
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10. Betamethasone :-
Hydrocortisone :-
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11. SAR of Corticosteroids
1)Substituents of 1- dehydro 6 α - fluro increases anti-
inflammatory and glucocorticoid activity.
2)Substituents of 16 α - hydroxy, 16 α & 16 β-methyl & 17
ketol decrease the mineralocorticoid activity.
3)9 alpha - fluro, 21- hydroxy, 2 α - methyl and 9 α chloro
increases both glucocorticoids and mineralocorticoid
activity
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12. Mechanism of Action
>These drugs reduce the increased
permeability of capillaries.
>They inhibit the leakage of inflammation producing
tissues by stabilizing the lysosomal membrane.
>The reduced permeability of capillaries inhibits the
migration of white cells out of blood stream, which in turn
decreases the number of such cell able to permit leakage
of their lysosomal enzymes into surrounding tissues.
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13. Adverse effects :-
1]Hyperglycemia
2]Ulcer formation
3]Increase the susceptibility for fungal infection
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14. Uses :-
1] It is use in treatment of autoimmune disorders
eg. rheumatic arthritis .
2] It increase the immunosuppressant activity.
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15. Antimetabolites :-
These are the chemical agents which blocks the
action of metabolites or prevents its assimilation by
an organisms.
Drugs:
1) Azathioprine
2) Methotrexate
3) 6- mercaptopurine
4) Cytarabine
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16. Methotrexate :-
Azathioprine :-
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17. Mechanism of action Methotrexate :-
1]Inhibition of cell replication may be the key therapeutic
mechanism of methotrexate in neoplastic conditions.
2]It is the orally active folic acid analog having
antineoplastic mild immunosuppressant activity.
3]It acts by metabolism and affects the phase 11 of the
immune responses.
4]It does not block the expression of established delayed
hypersensitivity reaction but my alter the intensity of these
reactions.
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18. Adverse effect :-
1]Oral ulceration
2]Post-dose reaction(fatigue)
3]Nausea, Diarrhea
4]Skin rash
5]Myelosuppression
6]Alopecia
7]Hepatics fibrosis
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19. Uses :-
1] Treatment of severe psoriasis.
2] In organ transplantation procedure.
3] As Anti-inflammatory.
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20. Anti Biotics :-
Defn:-An antibiotic also called an antibacterial, is a type of antimicrobial
drugs used in the treatment and prevention of bacterial infections. They may either
kill or inhibit the growth of bacteria.
Eg:- Cyclosporine
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21. Cyclosporine :-
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22. Mechanism of action :-
1]Antigen stimulate the T-cell receptor (TCR) Lead to
generation of inositol triphosphate (IP3) increases in
calcium and formation of an activated calcineurin.
2] Calcineurin is a phosphate which dephosphorylates the
phosphorylated transcriptase factor for nuclear factor of
activated T-cell(NF-AT),allowing NF-AT to translocate to
the nucleolus to induce expression of cytokines genes.
3]Cyclosporine C bind to immunophilines to block the
phosphatase action of calciurine & prevent the expression
of cytokine gene induced by NF-AT.
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23. Moa :-
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24. Adverse Effect :-
1]Renal Insufficiency (acute & chronic)
2]Hypertension
3]Hypertrichosis
4]Headache
5]Gingival Hypertrophy
6]Hyperuricemia
7]Nausea
8]Nephrotoxicity
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25. Uses :-
1]It is use along with Glucocorticoid for
prophylaxis and treatment of organ, bone marrow
and heart transplantation.
2]It is use in the treatment of autoimmune diseases
like rheumatic arthritis.
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26. Some more Immunosuppressant :-
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27. Immunostimulants :-
Immunostimulants, are substances that stimulate
the immune system by inducing activation or increasing
activity of any of its components.
Classification :-
1] Specific .
2] Non – specific .
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28. Immunostimulant :-
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29. Reference :-
1]Principle medicinal chemistry by Dr.Kadam, Dr.
Mahadik & Dr. Bothara nirali prakashan volume Pg. no.
18.1 to 18.8 .
2]Book of Medicinal chemistry by Wilson & Gisvold
Pg.no156 to 178 .
3] Immunomodulatory by Arthur & David .
4] Immunostimulants: Types and Functions Sepideh Shahbazi,
Azam Bolhassani Department of Hepatitis and AIDS, Pasteur
Institute of Iran, Tehran, Iran.
5] Immunomodulatory drugs: Oral and systemic adverse effects
Antonio Bascones-Martinez , Riikka Mattila , Rafael Gomez-Font ,
Jukka H. Meurman .
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30. Thank You
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