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Fexofenadine was also shown to inhibit histamine-induced wheal and flare to a significantly greater degree than loratadine or desloratadine, [21] but was slightly less effective than levocetirizine. [22] Fexofenadine at doses above 120 mg a day does not appear to provide additional efficacy in the treatment of allergic rhinitis. [23] [24]
It contains fexofenadine, as the hydrochloride, an antihistamine; and pseudoephedrine, as the hydrochloride, a nasal decongestant. [ 2 ] In 2021, it was the 279th most commonly prescribed medication in the United States, with more than 800,000 prescriptions.
[22] [27] Subsequently, other non-sedating antihistamines like loratadine (Claritin), cetirizine (Zyrtec), and fexofenadine (Allegra) were developed and introduced. [ 22 ] The introduction of the first-generation antihistamines marked the beginning of medical treatment of nasal allergies. [ 28 ]
Terfenadine acts as a peripherally-selective antihistamine, or antagonist of the histamine H 1 receptor. [3] It is a prodrug, generally completely metabolized to the active form fexofenadine in the liver by the enzyme cytochrome P450 3A4.
The Thorough QT/QTc study was designed to assess the effect on the QT/QTc interval, both of the therapeutic dose (20 mg) and 100 mg of bilastine, but also the coadministration of the therapeutic dose with usual doses of ketoconazol (400 mg/day), a metabolism inhibitor and a P-gP dependent transport system.
In 1977, it was shown that 5-aminosalicylic acid (5-ASA, mesalazine/mesalamine) was the therapeutically active component in sulfasalazine. [111] Many 5-ASA drugs have been developed with the aim of delivering the active compound to the large intestine to maintain therapeutic efficacy but with reduction of the side effects associated with the ...
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