BACKGROUND Allergic conditions affect about 20-30% of individuals. A survey of hay fever sufferers found, that 54% were self medicating with over the counter preparations and one third of these patients had experienced drowsiness because of their therapy. Antihistamines are one of the options for the symptomatic treatment of allergic disorders such as seasonal and perennial allergic rhinitis an...

The treatment of chronic spontaneous urticaria begins with antihistamines; however, the dose required typically exceeds that recommended for allergic rhinitis. Second-generation, relatively non-sedating H₁-receptor blockers are typically employed up to 4 times a day. First-generation antihistamines, such as hydroxyzine or diphenhydramine (Atarax or Benadryl), were employed similarly in the past...

Background Hypnotic use in children and adolescents is controversial. Objective To describe the of hypnotic drugs (melatonin, z-drugs, sedating antihistamines) among 5- to 24-year-old Scandinavians during 2012 2018. Methods Aggregate-level data were obtained from public sources Sweden, Norway, Denmark. We calculated annual prevalence (users/1000 inhabitants) stratified by age group, sex, countr...

We examined the effects of two over-the-counter H1-antihistamines on the progression of fatty liver disease in male C57Bl/6 wild-type and apolipoprotein E (ApoE)-/- mice. Mice were fed a high-fat diet (HFD) for 3 mo, together with administration of either cetirizine (4 mg/kg body wt) or fexofenadine (40 mg/kg body wt) in drinking water. Antihistamine treatments increased body weight gain, gonad...

This article reviews the molecular biology of the interaction of histamine with its H1-receptor and describes the concept that H1-antihistamines are not receptor antagonists but are inverse agonists i.e. they produce the opposite effect on the receptor to histamine. It then discourages the use of first-generation H1-antihistamines in clinical practice today for two main reasons. First, they are...

In 2003 a consensus group on new-generation antihistamines (CONGA) defined the characteristics required for a third-generation H(1) antihistamine as there had been much controversy about this issue since the early 1990s. One of the antihistamines that had been claimed to belong to such a group is the second-generation antihistamine, ebastine. The objective of this review is to analyze the pharm...

Classic antihistamines, namely diphenhydramine, chlorpheniramine, clemastine, perphenazine, hydroxyzine, and tripelennamine, share structural features with substrates and inhibitors of the polymorphic cytochrome P450 (CYP) isozyme CYP2D6. Therefore, the current study was undertaken to characterize the in vitro inhibition of CYP2D6 by these commonly used, histamine H1 receptor antagonists. Micro...

BACKGROUND Antihistamines are among the most frequently used medications in the United States. Despite dramatically higher cost, second-generation antihistamines are replacing diphenhydramine because of the perception that they are not constrained by its sedating effects. OBJECTIVE We sought to examine, through meta-analytic procedures, the collective evidence regarding the sedating and perfo...

Executive Board, AAP mor appearance in young women. New Eng. J. Med., 284:878, 1971. 2. Greenwald, P., Barlow, J. J., Nasca, P. C., and Burnett, W. S. : Vaginal cancer after maternal treatment with synthetic estrogens. New Eng. J. Med., 285:390, 1971. 3. Herbst, A. L., Ulfelder, H., and Poskanzer, D. C.: Registry of clear-cell carcinoma of genital tract in young women. New Eng. J. Med., 285:407...