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Ebastine is a H 1 antihistamine with low potential for causing drowsiness. It does not penetrate the blood–brain barrier to a significant amount and thus combines an effective block of the H 1 receptor in peripheral tissue with a low incidence of central side effects, i.e. seldom causing sedation or drowsiness. [1] [2] [3]
Rupatadine fumarate has been approved for the treatment of allergic rhinitis and chronic urticaria in adults and children over 12 years. It is available as round, light salmon coloured tablets containing 10 mg of rupatadine (as fumarate) to be administered orally, once a day.
A positron emission tomography (PET) study found that brain occupancy of the H 1 receptor was 12.6% for 10 mg cetirizine, 25.2% for 20 mg cetirizine, and 67.6% for 30 mg hydroxyzine. [30] (A 10 mg dose of cetirizine equals about a 30 mg dose of hydroxyzine in terms of peripheral antihistamine effect.) [31] PET studies with antihistamines have ...
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.
Comparison of selected sedating antihistamines Antihistamine Dose a Time to peak Half-life b Metabolism Anticholinergic Diphenhydramine: 50 mg 2–3 hours 2–9 hours CYP2D6, others Yes Doxylamine: 25 mg 2–3 hours 10–12 hours CYP2D6, others Yes Hydroxyzine: 25–100 mg 2 hours 20 hours ADH, CYP3A4, others No Doxepin: 3–6 mg 2–3 hours 17 ...
A single bedtime dose after the last feeding of the day may minimize the harmful effects of the medication on the baby and the milk supply. Still, non-sedating antihistamines are preferred. [37] Paradoxical reactions to diphenhydramine have been documented, particularly in children, and it may cause excitation instead of sedation. [38]
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