In the current study, the potential blocking ability of K+ channels encoded by the human ether-a-go-go related gene (HERG) by the piperazine H1 receptor antagonist cetirizine has been examined and compared with that of other second-generation antihistamines (astemizole, terfenadine, and loratadine). Cetirizine was completely devoid of any inhibitory action on HERG K+ channels heterologously exp...

BACKGROUND Few studies have compared the antihistaminic effect of ebastine at 20 mg/day (maximal recommended daily dose) with the effect found for other antihistamines in human pharmacologic models. OBJECTIVE To compare the inhibition of the histamine-induced skin reaction produced by ebastine (20 mg/day) with that produced by cetirizine (10 mg/day), loratadine (10 mg/day), or placebo in a do...

BACKGROUND The first generation antihistamines, such as diphenhydramine, are fairly potent muscarinic antagonists in addition to being H1 selective antihistamines. The antimuscarinic action is often not desirable since it is in part responsible for the drying of secretions in the airways and the sedative effect. We therefore examined a number of antihistamines for antimuscarinic effects on ion ...

Research & Development in Material Science Controlled Drug Release from Loratadine-Loaded Pectin Film Dosage Forms Yoshifumi Murata*, Sae Sugimoto, Chieko Maida and Kyoko Kofuji Faculty of Pharmaceutical Science, Hokuriku University, Japan *Corresponding author: Murata, Ho-3, Kanagawa-machi, Kanazawa 920-1181, Submission: February 21, 2022;Published: 25, 2022 DOI: 10.31031/RDMS.2022.16.000895 I...

The Front Cover illustrates how the pyridine ring of antihistamine loratadine can be selectively functionalised at ortho-, meta-, or para-position (each them activated by a thunder). Indeed, selective functionalisation this N-heterocycle is often problematic, thus lighthouse guides chemists through late-stage functionalisations pyridine-containing biomolecules. More information found in Review ...

The present study evaluates the impact of P-glycoprotein (P-gp) on plasma-brain disposition and transepithelial transport of sedating versus nonsedating H1-antagonists using multidrug-resistant (mdr) gene 1a and 1b (mdr1a/b) knockout (KO) mice and human MDR1-transfected Madin-Darby canine kidney (MDCK) cells. Three nonsedating (cetirizine, loratadine, and desloratadine) and three sedating (diph...

We present the clinical case of a 8-years-old boy suffering a fixed drug reaction attributed to the oral intake of loratadine. He is an atopic child with perennial rhinitis and asthma and marked hypersensitivity to the house-dust mite Dermatophagoides pteronyssinus who is receiving inhaled corticosteroids and b2-agonists ad libitum plus specific immunotherapy with the mite. When the boy receive...