“…Most discussions on sedative effects of different classes of antihistamines ascribe differences in the sedative potentials to receptor occupancy, receptor selectivity, and brain penetration (Handley and Graff, 1998;Simons, 1994). The inability to penetrate the blood-brain barrier has been put forward as the major advantage of 2nd-and the new-generation antihistamines over the older ones (Hindmarch and Shamsi, 1999).…”
“…Most discussions on sedative effects of different classes of antihistamines ascribe differences in the sedative potentials to receptor occupancy, receptor selectivity, and brain penetration (Handley and Graff, 1998;Simons, 1994). The inability to penetrate the blood-brain barrier has been put forward as the major advantage of 2nd-and the new-generation antihistamines over the older ones (Hindmarch and Shamsi, 1999).…”
“…Seasonal allergic rhinitis per se may affect learning ability and concentration. Treatment with first-generation H 1 -antihistamines often has a further reducing effect upon cognitive function (2226). However, use of the newer H 1 -antihistamines counteracts the feeling of malaise caused by allergic rhinitis and may improve learning ability in allergic rhinitis.…”
“…It is well known that the classical (first-generation) antihistamines such as d-chlorpheniramine, diphenhydramine and promethazine, have undesirable side effects including sedation, at therapeutic doses (Simons, 1994;Shamsi and Hindmarch, 2000). Sedation induced by antihistamines impairs cognitive and psychomotor functions (Passalacqua et al, 1993).…”
Since most classical (first-generation) antihistamines have undesirable sedative effects on the central nervous system (CNS), newer (second-generation) antihistamines have been developed to relieve the sedative effects and to improve the patient's quality of life. However, the psychomotor profiles of second-generation antihistamines are not fully elucidated. In this randomized, double-blind, crossover study, the acute effects of single doses of second-generation antihistamines, fexofenadine (120 mg) and olopatadine (10 mg), on cognitive and psychomotor performance were investigated in comparison with those of placebo and d-chlorpheniramine (4 mg), a first-generation antihistamine, using objective and subjective assessments, in 11 healthy Japanese volunteers. In a battery of psychomotor tests, d-chlorpheniramine impaired tracking ability in the compensatory tracking task and caused a reduction in behavioural activity as continuously measured by wrist actigraphy. Olopatadine, like d-chlorpheniramine, reduced the behavioural activity, while fexofenadine had no effect in any of the tests. No significant changes in the subjects' self-ratings of drowsiness were found with the three antihistamines. These results suggest that d-chlorpheniramine and olopatadine, but not fexofenadine, produce sedative effects on psychomotor performance, and that the CNS profile of fexofenadine is different from that of olopatadine.
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