H1-antihistamine is generally a well-tolerated and safe drug. However, in resemblance with all other drugs, H1-antihistamines can also prompt adverse drug reactions (ADRs). We recently encountered the very unusual ADR of H1-antihistamine-induced gynecomastia. A 21-year-old man with idiopathic anaphylaxis was treated with ebastine (Ebastel), a second-generation H1-antihistamine, for the preventi...

A structure-activity relationship (QSAR) analysis of 19 thiazole derivatives with H1-antihistamine activity was carried out. The semi-empirical method AMI was employed to calculate a set of physicochemical parameters for investigated compounds. The principal component analysis (PCA), discriminant function analysis (DFA) and regression analysis (RA) were employed to reduce dimensionality and inv...

The therapeutic index of a histamine-1 (H1)antihistamine is the benefit-to-risk ratio of the medication and defines the range of doses and plasma concentrations over which the drug is effective and safe. In allergic rhinoconjunctivitis and urticaria, although the efficacy profiles of currently available H1-antihistamines are similar, these agents differ greatly with regard to safety, and this c...

cyclizine (1-benzhydryl-4-methyl-piperazine, cas 82-92-8, cyc, i), a piperazine derivative, belongs to h1 antihistamine group of drugs that shows such pharmacological properties as anti-inflammatory, anti-allergic and anti-platelet effects, similar to other h1-receptor antagonists. in this study, two new tolyl and cumene derivatives of i (1-ethyl-4-[(p-isopropylphenyl) (p-tolyl) methyl]-piperaz...

Numerous "antihistamines" as well as various psychotropic medications with antihistamine properties are widely utilized to treat insomnia. Over-the-counter sleep aids usually contain an antihistamine and various antidepressants and antipsychotics with antihistamine properties have sedative-hypnotic actions. Although widely used for the treatment of insomnia, many agents that block the histamine...

INTRODUCTION Rational selection of a second-generation H1-antihistamine requires efficacy and safety considerations, particularly regarding central nervous system (CNS) effects (cognitive and psychomotor function), potential for driving impairment, minimal sedative effects and a lack of interactions. This review evaluates the key safety features of the non-sedating antihistamine, bilastine, dur...

Fexofenadine (Allegra® 180) is a second-generation antihistamine. It is widely used as anti-allergic drug, which suppresses various allergic reactions mediated by histamines. A few cases of H1-antihistamine-induced urticaria have been reported. Herein, we report a rare case of fexofenadine-induced urticaria which was confirmed by a prick test, oral provocation test, and flow cytometry assisted-...

Ocular symptoms often accompany allergic rhinitis and can be as or even more bothersome for the patient than the actual nasal symptoms. Ocular manifestations of allergic rhinoconjunctivitis may result from both direct allergen-mediated mast cell stimulation on the surface of the eye and naso-ocular reflexes--histamine being one of the mediators of symptoms onset. An H1 antihistamine would be th...

Promethazine hydrochloride is a first-generation H1 receptor antagonist, antihistamine, and antiemetic medication that can also have strong sedative effects. The apparent ability of topical H1r/2r antagonists to target epidermal H1/2r was translated into increased efficacy in the treatment of inflammatory dermatoses, likely due to decreased inflammation and enhanced barrier function.