Indication |
For the treatment of the symptoms of the common cold and allergic
rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing. |
Pharmacodynamics |
Brompheniramine is an antihistaminergic medication of the
propylamine class. It is a first-generation antihistamine. 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. Brompheniramine is a histamine H1
antagonist (or more correctly, an inverse histamine agonist) of the
alkylamine class. 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 |
Brompheniramine works by acting as an antagonist of the H1
histamine receptors. It also functions as a moderately effective
anticholingeric agent, likely an antimuscarinic agent similar to other
common antihistamines such as diphenhydramine. Its effects on the
cholinergic system may include side-effects such as drowsiness,
sedation, dry mouth, dry throat, blurred vision, and increased heart
rate. |
Absorption |
Antihistamines are well absorbed from the gastrointestinal tract after oral administration. |
Volume of distribution |
Not Available |
Protein binding |
Not Available |
Metabolism |
Hepatic (cytochrome P-450 system), some renal. |
Route of elimination |
Not Available |
Half life |
Not Available |
Clearance |
Not Available |
Toxicity |
Oral, rat: LD50 = 318 mg/kg. Signs of overdose include
fast or irregular heartbeat, mental or mood changes, tightness in the
chest, and unusual tiredness or weakness. |
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