Indication |
For the symptomatic relief of seasonal or perennial allergic
rhinitis or nonallergic rhinitis; allergic conjunctivitis; and mild,
uncomplicated allergic skin manifestations of urticaria and angioedema.
Also used in combination with other agents for the symptomatic relief of
symptoms associated with the common cold. |
Pharmacodynamics |
In allergic reactions an allergen interacts with and cross-links
surface IgE antibodies on mast cells and basophils. Once the mast
cell-antibody-antigen complex is formed, a complex series of events
occurs that eventually leads to cell-degranulation and the release of
histamine (and other chemical mediators) from the mast cell or basophil.
Once released, histamine can react with local or widespread tissues
through histamine receptors. Histamine, acting on H1-receptors, produces
pruritis, vasodilatation, hypotension, flushing, headache, tachycardia,
and bronchoconstriction. Histamine also increases vascular permeability
and potentiates pain. Triprolidine, is a histamine H1 antagonist that
competes with histamine for the normal H1-receptor sites on effector
cells of the gastrointestinal tract, blood vessels and respiratory
tract. It provides effective, temporary relief of sneezing, watery and
itchy eyes, and runny nose due to hay fever and other upper respiratory
allergies. Triprolidine has anticholinergic and sedative effects. |
Mechanism of action |
Triprolidine binds to the histamine H1 receptor. This blocks the
action of endogenous histamine, which subsequently leads to temporary
relief of the negative symptoms brought on by histamine. |
Absorption |
Rapidly absorbed in the intestinal tract. |
Volume of distribution |
Not Available |
Protein binding |
Not Available |
Metabolism |
Not Available |
Route of elimination |
Not Available |
Half life |
4 to 6 hours. |
Clearance |
Not Available |
Toxicity |
Symptoms of overdose include drowsiness, weakness,
inco-ordination, difficulty with micturition, respiratory depression,
hypotension, agitation, irritability, convulsions, hypertension,
palpitation and tachycardia. |
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