Adobe Systems
Imunopharmacology
Department of Pharmacology MF MU
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Adobe Systems
                               Immunomodulatory substances
The main function of IS: to remove dead, impaired, or cancerous cells as well as to protect against
infections and inorganic substances and to adequately react to these stimuli
Inadequate reaction may lead to impairment of the organism and to development of disease
Immunomodulatory substances: act on components of immune system by a direct or indirect mechanism
function of the IS can be potentiated (immunostimulation) x supressed (immunosuppression)
                         immunostimulants x immunosuppressants

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Immunosuppressants
used to treat autoimmune diseases (i.e., disorders of immunity caused by pathological reactivity to
internal antigens)
in severe allergic conditions (i.e., pathological hypersensitivity to external antigens)
in transplantation medicine - as prevention of transplantation rejection
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Non-specific immunosuppressants
Glucocorticoids (earlier talk)
Cytostatic drugs with an immunosuppressive effect
Substances that bind to immunophilins:
cyclosporine A: a cyclic polypeptide acquired from soil bacteria
                                 it affects primarily Th1 lymphocytes by decreasing the
                                 production of IL-2
                                 it has significant interactive potential with substances
                                 inhibiting CYP450
AE: nephrotoxicity, hepatotoxicity (TDM recommended)

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Non-specific immunosuppressants

Substances that bind to immunophilins:
tacrolimus - macrolide antibiotic
                        (MoA similar to the action of cyclosporine A)
                        10-100 times more effective than cyclosporine A (but also more
                        nephrotoxic)
                        metabolised in the liver by CYP450 enzymes
AE: the same as with cyclosporine A + alopecia

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Non-specific immunosuppressants

Other substances
mycophenolate mofetil: intervenes with the synthesis of guanosine
                                                 nucleotides and inhibits the proliferation of T
and
                                                 B lymphocytes
                                                 used in combination with cyclosporine A and
                                                 glucocorticoids
AE: diarrhoea, nausea, leukopenia
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Non-specific immunosuppressants

Biologicals
They affect immunocompetent cells by acting as antibodies against T and/or B lymphocytes or IL-2
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Specific immunosuppressants
The use of specific allergen immunotherapy is widespread in practice
Aim: to evoke immunologic tolerance to an allergen, which induces a pathological
        response from the organism
Gradually increasing doses of a specially modified allergen are given for a period of 3-5 years
Administration: sublingually or injections
Indication: pollen allergies, mite allergies, mould spore allergies, pet allergies
                    bronchial asthma mediated by IgE antibodies.
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Immunostimulants

Specific immunostimulants
Vaccination against infectious disease
Vaccines are modified, in so far as that they can induce an immune reaction with immunological
memory, which will prevent the development of an infectious disease. Vaccines are derived from
live, attenuated strains of microorganisms, modified bacterial toxins, and vaccines containing only
a certain immunogenic part of a microorganism.
Anti-tumour vaccines
consist of activated dendritic cells, which provoke an immune response against tumour antigens
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Immunostimulants

Non-specific immunostimulants:
Origin: synthetic or bacterial origin or they can be products of the immune system, which are
acquired by, for example, recombinant techniques
Synthetic immunomodulators
levamisole: originally an anthelmintic drug
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Immunostimulants

Non-specific immunostimulants:
Synthetic immunomodulators
isoprinosine: a purine derivative, which besides immunostimulant properties also has an antiviral
effect
Indication: repeated herpetic infections (today it has been replaced by specific antiviral drugs
against herpes viruses)
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Immunostimulants

Non-specific immunostimulants:
Bacterial immunomodulators
extracts from bacteria or bacterial lysates
Their application activates macrophages.
Indication: repeated infections of airways and the urinary tract
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Immunostimulants

Non-specific immunostimulants:
Products of the immune system
transfer factor: a dialysate of homogeneous leucocyte mixture that has been acquired from healthy
blood donors
It activates both specific and non-specific immunity.
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Immunostimulants

Non-specific immunostimulants:
Products of the immune system
cytokines - have biological effects, which is why they are used.
Interleukin 2 (Il-2): used for antitumor therapy and under certain conditions after bone marrow
transplantation.
Interferon alpha (INF-α): interferes with large number of viruses in the cell and has an antitumor
effect. It is indicated for infectious hepatitis B and C and oncologic diseases.
Interferon beta (INF-β): has similar effects to interferon alpha. It is used to treat multiple
sclerosis, hepatitis B and C, and for oncologic diseases.
Interferon gamma (INF-γ): has the same basic biological properties as other interferons. It is
indicated for immunodeficiency disorders and antitumor therapy.

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