Antihistamines are known for their sedative effects. However, some studies suggested mild stimulant effects in the case of fexofenadine. The goals of this study are to examine whether fexofenadine possesses stimulating properties and to determine whether such stimulating effects are related to workload. Sixteen healthy volunteers received a single dose of 180 and 360 mg fexofenadine and placebo on separate test days. Drug effects were assessed using a divided attention task (DAT), continuous performance task (CPT) and motor choice reaction time test (MCRT). Sensitivity of the tasks was increased by manipulating the workload during task performance. Event Related brain Potentials (ERPs) were measured in the DAT and CPT to study the underlying neurophysiological processes. An interaction effect of Treatment and Workload was found on tracking performance in the DAT and on movement time in the MCRT. Performance on the DAT was less affected by increments in workload after fexofenadine as compared to placebo. P1 and P3 latency were affected by Treatment x Workload and Treatment respectively and indicated faster attentional and information processing latencies following fexofenadine treatment. Treatment did not influence performance in the CPT task or in the ERPs measured during this task. The MCRT demonstrated faster movement times following fexofenadine treatment. These results suggest that although the neurophysiological data indicate central nervous system (CNS) activation after fexofenadine treatment, the magnitude of the centrally activating effects is too small to produce relevant performance improvement at the behavioural level.
"Fexofenadine inhibited the production of matrix metal - loproteinases ( MMP ) MMP - 2 and MMP - 9 from nasal polyp and mucosal fi broblasts in response to TNF - α , and inhibited MMP mRNA expression and NF - κB , but not tissue inhibitor of metalloproteinase ( TIMP - 1 and TIMP - 2 ) ( Asano et al 2004c ) . Fexofenadine improved performance on the Digit Symbol Substitution Test , but it did not have a blocking effect upon the dopamine transporter ( Theunissen et al 2006a , b ) Fexofenadine is primarily prescribed for its H 1 antagonist activity . However , it appears to have effects upon other mast cell mediators , as well as mediators produced by other cell types . "
[Show abstract][Hide abstract] ABSTRACT: Fexofenadine is a selective, non-sedating H1 receptor antagonist, marketed in the United States since 2000. The FDA approved an oral suspension in 2006, for the treatment of seasonal allergic rhinitis and chronic idiopathic urticaria in children. The tablet, capsule, and oral suspension are bioequivalent. Although fexofenadine does not use P450 CYP 3A4 it does interact with a number of drugs at P-glycoprotein and organic anion transporter polypeptides. The risk of toxicity from other drugs may increase with the administration of fexofenadine. Orange and grapefruit juices reduce the bioavailability of fexofenadine. Fexofenadine has been shown to have an impact on inflammatory mediators, other than histamine, such as decreasing the production of LTC(4), LTD(4), LTE(4), PGE(2), and PGF(2α); inhibiting cyclo-oxygenase 2, thromboxane; limiting iNOS generation of NO; decreasing cytokine levels (ICAM-1, ELAM-1, VCAM-1, RANTES, I-TAC, MDC, TARC, MMP-2, MMP-9, tryptase); and diminishing eosinophil adherence, chemotaxis, and opsonization of particles. These effects may provide benefit to some of the inflammatory responses of an acute allergic reaction and provide a basis for future development of H1 antagonists with stronger anti-inflammatory effects. These studies also support the contention that fexofenadine is effective for the treatment of allergic rhinits and chronic idiopathic urticaria.
Journal of Asthma and Allergy 09/2008; 1(1):19-29. DOI:10.2147/JAA.S3092
[Show abstract][Hide abstract] ABSTRACT: Rupatadine fumarate is a potent, selective, histamine H(1)-receptor antagonist and PAF inhibitor with demonstrated efficacy for the relief of allergic rhinitis. Rupatadine does not easily cross the blood-brain barrier and is believed to be non-sedating at therapeutic doses. Consequently, rupatadine should show no impairment on car driving.
This study compared the acute effects of rupatadine, relative to placebo and hydroxyzine (as an active control), on healthy subjects' driving performance.
Twenty subjects received a single dose of rupatadine 10 mg, hydroxyzine 50 mg, or placebo in each period of this randomized, double-blind, three-way crossover study. Two hours postdosing, subjects operated a specially instrumented vehicle in tests designed to measure their driving ability. Before and after the driving tests ratings of sedation were recorded.
There was no significant difference between rupatadine and placebo in the primary outcome variable: standard deviation of lateral position (SDLP); however, hydroxyzine treatment significantly increased SDLP (p < 0.001 for both comparisons). Objective (Stanford sleepiness scale) and subjective sedation ratings (Visual Analogue Scales) showed similar results: subjects reported negative effects after hydroxyzine but not after rupatadine.
Rupatadine 10 mg is not sedating and does not impair driving performance.
Human Psychopharmacology Clinical and Experimental 07/2007; 22(5):289-97. DOI:10.1002/hup.856 · 2.19 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Antagonists of histamine H(1) receptors (antihistamines) are widely used for the treatment of allergic disorders in children. These drugs' sedative effect on brain function, however, has been mostly examined in adults.
The objective of this study was to examine the effects of anitihistamines on prefrontal cortex activity in young children using near-infrared spectroscopy (NIRS), a novel brain-imaging method.
In 15 healthy children (mean age, 7.7 years), we examined changes of oxygenated hemoglobin concentration in the prefrontal cortex while they performed a verbal fluency task 3 h after taking a sedating antihistamine (ketotifen), nonsedating antihistamine (epinastine), or placebo.
Ketotifen significantly impaired behavioral performance and cortical activation at the lateral prefrontal cortex compared with placebo. There were no sedative effects on neural response or behavioral performance after epinastine administration.
NIRS revealed that sedating and nonsedating antihistamines exert differential effects on brain hemodynamic response in young children.
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