Anti histamines

Dr. Haji Bahadar

Assistant Professor
Khyber Medical University-IPMS
Autocoids
Short acting endogenous chemicals produced usually as
a result of an inflammatory response. Examples:
Bradykinin, Prostaglandins, thromboxanes,
leukotrienes, and histamine
histamine is Involved in inflammatory and
anaphylactic reactions.

Histamine
Conditions That Release Histamine
1. Tissue injury: Any physical or chemical agent that injures
tissue, skin or mucosa are particularly sensitive to injury and
will cause the immediate release of histamine from mast
cells(stored).
2. Allergic reactions: exposure of an antigen to a previously
sensitized (exposed) subject can immediately trigger allergic
reactions. If sensitized by IgE antibodies attached to their
surface membranes will degranulate when exposed to the
appropriate antigen and release histamine
3. Drugs and other foreign compounds: morphine,
antimalarial drugs, dyes, antibiotic penicillines etc.
Effects of histamine
Decreased peripheral vascular resistance (mediated by
H1 receptor ( flushing, headache!)
Increased vascular permeability, especially capillaries,
local edema (H1)
Stimulation of nerve endings (pain!
Bronchioles: it causes contraction of nonvascular smooth
muscle. Asthmatics may experience marked bronchial
constriction.
Anaphylaxis
Type I allergic response
(immediate hypersensitivity reaction)
Mediated by IgE antibodies
IgE binds to receptors on mast cells and basophils
Fab portion of antibody binds antigen and causes
(moderate to massive) release of:
histamine
leukotrienes
prostaglandins
Common causes of anaphylactic reacton
IgE-mediated
Anaphylaxis

Peanuts, seafood, eggs, milk, grains

Venoms
Foreign proteins
Some exercise-induced bronchospasm
Signs symptoms and treatment
Decreased blood pressure
Decreased cardiac output
Bronchoconstriction and increased pulmonary secretions
Pruritis
Treatment:
 Epinephrine - not initially antihistamines
(epinephrine is a physiological antagonist of histamine, not a
pharmacological antagonist)
(alpha-1 vasoconstriction, beta-1 increased HR,
beta-2 bronchodilation)
Inhibit the release of histamine (e.g., cromolyn)
Pharmacological antagonism (antihistamines)
Antihistamines
Those drugs which block histamine receptors
two types:
H1 and H2 blockers
Histamine 1 receptor blockers

Advantages of second generation antihistaminics • They have no

anticholinergic side effects • Do not cross blood brain barrier (BBB),
hence cause minimal or no drowsiness and sedation • Do not impair
Psychomotor performance
Mechanism of action?
Clinical uses
Allergic reactions
Motion sickness
Vomiting
Side effects; self study