Brands, Medical Use, Clinical Data
Drug Category
Dosage Forms
Brands / Synonyms
Actidil; Myidyl; Pseudodine C; Triacin-C; Triprolidine HCL; Triprolidine Hydrochloride; Venen (TN)
Indications
For the treatment of hay fever, urticaria (hives), and other allergic systems.
Pharmacology
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.
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.
Toxicity
Symptoms of overdose include drowsiness, weakness, inco-ordination, difficulty with micturition, respiratory depression, hypotension, agitation, irritability, convulsions, hypertension, palpitation and tachycardia.
Biotrnasformation / Drug Metabolism
Not Available
Contraindications
Should not be administered to patients suffering from cardiovascular
disease (especially coronary insufficiency), hypertension, prostatism, thyrotoxicosis, bladder dysfunction, narrow
angle glaucoma, phaeochromocytoma and during an attack of asthma in asthmatic patients.
Drug Interactions
Triprolidine may enhance the sedative effects of central nervous system
depressants including alcohol, barbiturates, hypnotics, narcotic analgesics, sedatives, and tranquillisers. The
effects of anticholinergic drugs, such as atropine and tricyclic antidepressants may be enhanced by the concomitant
administration of triprolidine. Triprolidine may effect the metabolism of drugs in the liver.
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