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Immunomodulators
Classification of anti allergic drugs
1. Drugs that decrease the release of mediators ( histamine, other ABS) from mast cell.
(Stabilization of mast cells)
- glucocorticoids
- sodium cromoglicate
2. Drugs that inhibit the interaction between histamine and its receptors.
H1 histaminoblockers
- diphenhydramine
- clemastine
3. Drugs that diminish the main allergic symptoms:
( hypotension, bronchospasm)
a) adrenomimetics: epinephrine, norepinephrine
b) bronchodilators: I. Musculotropic: aminophylline
II. Sympaphomimetics: salbutamol
III. M-cholinoblockers: ipratropium
IV. Drugs that decrease tissues affection:
- Non steroidal-antiinflammatory drugs
4. Drugs used in cell-mediated immune reactions:
1. Immunosuppressants:
- glucocorticoids
- 4-aminoquinoline derivatives: chloroquine
hydroxichloroquine
- cytostatics :
methotrexate
azathioprine
cyclosporine
mercaptopurine
2. Drugs that diminish the cytotoxic reactions and tissues alteration
- steroid anti-inflammatory drugs
- non steroid anti- inflammatory drugs
Histamine is a biogenic amine involved in local immune responses as well as regulating
physiological function in the gut and acting as a neurotransmitter. As part of an immune response
to foreign pathogens, histamine is produced by basophils and by mast cells found in nearby
connective tissues. Histamine increases the permeability of the capillaries to white blood cells
and other proteins, in order to allow them to engage foreign invaders in the affected tissues. It is
found in virtually all animal body cells.
Types of immune reactions:
Type I reactions: immediate hypersensitivity
Type II reactions: membrane- reactive immunity
Type III reactions: immune complex disease
Type IV reactions: cell-mediated immune reactions.
Histamine exerts its actions by combining with specific cellular histamine receptors. The
four histamine receptors that have been discovered are designated H1 through H4.
Type
Location
Function
H1
histamine
receptor
H2
histamine
receptor
H3
histamine
receptor
H4
histamine
receptor
Unknown role
such cases, a doctor may prescribe diet supplements with folic acid and niacin (which used in
conjunction can increase blood histamine levels and histamine release), or L-histidine.
Schizophrenia
It has been found that about half the patients classified as suffering from schizophrenia have low
histamine levels in the blood. This may be because of antipsychotics that have unwanted effect
on histamine, such as quetiapine. Although, in these cases, as histamine levels were increased,
their health improved.
Disorders
As an integral part of the immune system, histamine may be involved in immune system
disorders and allergies.
Nomenclature
"H substance" or "substance H" are occasionally used in medical literature for histamine or a
hypothetical histamine-like diffusible substance released in allergic reactions of skin and in the
responses of tissue to inflammation.
Antihistamines are inhibitors of histamine receptors. One distinguishes H1 and H2 antagonists.
H1-antihistamines have been used for more than fifty years in treating various allergic
manifestations.
Classification of antihistamines
I. according to the chemical structure
II. according to the generations
1. Ethanolamines:
I generations
a. diphenhydramine
- diphenhydramine
b. clemastine (tavegyl)
- clemastine (tavegil)
2. Ethylendamines:
- chlorophiramine (suprastine)
a. chlorophiramine (suprastine)
- chlorphenamine
3. Alkylamines:
- promethasine
a. chlorphenamine
- antasoline
4. Phenothiasines:
- quiphenamide
a. promethasine
II generation
5. Imidasols:
- astemisole
a. antasoline
- loratadine
6. Hynuclidines:
- terfenadine
quiphenamide (phencarol)
- cetirizine
7. Piperidines:
a. astemisole
b. loratadine
c. terfenadine
8. Piperazines:
a. cetirizine
Antihistamines
It is usual to classify H1-antihistamines into two classes: old ones, called first-generation agents,
which are sedating and recent ones, called second-generation agents which have slight or no
sedating effects because they do not cross the blood-brain barrier. In addition, each compound
can have or not have parallel properties, antimuscarinic effects for example. This distinction
between generations must be taken with caution because a product considered as non sedative or
not antimuscarinic can, in certain circumstances, large doses or particular susceptibility of the
patient ,have these effects. Effect duration deffers but in medium is equal 4-8 hours.
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Theophylline belongs to the methylxanthines. Whereas caffeine (1,3,7trimethylxanthine) predominantly stimulates the CNS and constricts cerebral blood vessels,
theophylline
(1,3-dimethylxanthine)
possesses
additional
marked
bronchodilator,
cardiostimulant, vasorelaxant, and diuretic actions. These effects are attributed to both inhibition
of phosphodiesterase ( c AMP elevation,) and antagonism at adenosine receptors. In bronchial
asthma, theophylline can be given orally for prophylaxis or parenterally to control the attack.
Manifestations of overdosage include tonic-clonic seizures and cardiac arrhythmias as early
signs.
Ipratropium can be inhaled to induce bronchodilation; however, it often lacks sufficient
effectiveness in allergic bronchospasm.
Immunomodulators
A. Biologic origin drugs:
1. drugs from thymus
- thymaline
- T-activine
2. other animal origin drugs
- melopid
3. bacterial origin drugs
pyrogenal
prodigiozane
4. drugs from donators blood
interloc
interferon
5. drugs obtained with genetic engineer method
philgastrine
nolgastrine
reaferon
betaferon
interleukine-2
B. Synthetic drugs
levamisol
imunophan
leucadine
polyoxidoniu
Immunomodulators are natural or synthetic substances that help regulate or normalize the
immune system. Immunomodulators correct immune systems that are out of balance.
Immunomodulators correct weak immune systems and temper immune systems that are
overactive, but they do not boost the immune system the way immune stimulants such as
Echinacea do. Immunomodulators are recommended for people with autoimmune diseases and
they are widely used in chronic illness to restore immune system health in people who have been
on lengthy courses of antibiotics or anti-viral therapies.
The benefits of immunomodulators stem from their ability to stimulate natural and
adaptive defense mechanisms, such as cytokines, which enables the body to help itself.
Natural and Synthetic Immunomodulators
Plant sterols and sterolins are excellent immunomodulators fount in waxy fruits and
vegetables although they are lost when vegetables and fruits are cooked. Several products, such
as Moducare, are patent preparations rich in sterols and sterolins. Other natural
immunomodulators include ginseng root, German chamomile tea, lemon/olive drinks, reishi
mushroom extract and olive leaf extract
Prescription synthetic immunomodulator medications, such as azathioprine, 6mercaptopurine, methotrexate, and mycophenolate mofetil, work by suppressing the immune
system and decreasing inflammation in the digestive tract in people with inflammatory bowel
disease, ulcerative colitis, and Crohn's disease. Tacrolimus can be used in Crohn's disease when
corticosteroids prove ineffective. In children, immunomodulators are less likely to cause growth
failure than corticosteroids.
Topical immunomodulators such as tacrolimus and pimeocrolimus have been found to
offer benefits in patients with eczema, vitiligo and nickel allergy. Topical immunomodulators are
well tolerated even in infants.
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