Developing A High-performance Liquid Chromatography Method for Simultaneous Determination of Loratadine and its Metabolite Desloratadine in Human Plasma.
CONCLUSION: The results obtained indicate that the proposed method is rapid, sensitive in the nanogram range, accurate, selective, robust and reproducible compared to other reported methods. PMID: 31774044 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - November 23, 2019 Category: Drugs & Pharmacology Authors: Sebaiy MM, Ziedan NI Tags: Curr Drug Metab Source Type: research

Metabolism of desloratadine by chimeric TK-NOG mice transplanted with human hepatocytes.
Abstract 1. Desloratadine is an antiallergic drug with species-dependent metabolic profiles in mice, rats, monkeys, and humans. We investigated whether humanized-liver mice could reproduce the reported human-specific in vivo metabolic profile for desloratadine in terms of the formation of 3-hydroxydesloratadine and its O-glucuronide.2. Hepatocytes prepared from humans and humanized-liver mice both preferentially catalyzed the formation of 3-hydroxydesloratadine and its O-glucuronide in vitro.3. After a single oral administration of desloratadine, plasma levels of desloratadine and its metabolites (3-hydrox...
Source: Xenobiotica - November 4, 2019 Category: Research Authors: Uehara S, Yoneda N, Higuchi Y, Yoneda N, Yamazaki H, Suemizu H Tags: Xenobiotica Source Type: research

Human H1 receptor (HRH1) gene polymorphism is associated with the severity of side effects after desloratadine treatment in Chinese patients with chronic spontaneous uticaria
The Pharmacogenomics Journal, Published online: 13 August 2019; doi:10.1038/s41397-019-0094-0Human H1 receptor (HRH1) gene polymorphism is associated with the severity of side effects after desloratadine treatment in Chinese patients with chronic spontaneous uticaria (Source: The Pharmacogenomics Journal)
Source: The Pharmacogenomics Journal - August 12, 2019 Category: Drugs & Pharmacology Authors: Juan Li Wangqing Chen Cong Peng Wu Zhu Zhaoqian Liu Wei Zhang Juan Su Jie Li Xiang Chen Source Type: research

Brain histamine H1 receptor occupancy after oral administration of desloratadine and loratadine
We examined brain H1R binding potential ratio (BPR), H1R occupancy (H1RO), and subjective sleepiness after oral desloratadine administration in comparison to loratadine. Eight healthy male volunteers underwent PET imaging with [11C] ‐doxepin, a PET tracer for H1Rs, after a single oral administration of desloratadine (5  mg), loratadine (10 mg), or placebo in a double‐blind crossover study. BPR and H1RO in the cerebral cortex were calculated, and plasma concentrations of loratadine and desloratadine were measured. Subjective sleepiness was quantified by the Line Analogue Rating Scale (LARS) and the Stanford Sleepiness...
Source: Pharmacology Research and Perspectives - July 11, 2019 Category: Drugs & Pharmacology Authors: Tadaho Nakamura, Kotaro Hiraoka, Ryuichi Harada, Takuro Matsuzawa, Yoichi Ishikawa, Yoshihito Funaki, Takeo Yoshikawa, Manabu Tashiro, Kazuhiko Yanai, Nobuyuki Okamura Tags: ORIGINAL ARTICLE Source Type: research

[ASAP] Route to Prolonged Residence Time at the Histamine H < sub > 1 < /sub > Receptor: Growing from Desloratadine to Rupatadine
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b00447 (Source: Journal of Medicinal Chemistry)
Source: Journal of Medicinal Chemistry - July 5, 2019 Category: Chemistry Authors: Reggie Bosma †?, Zhiyong Wang†?, Albert J. Kooistra†#, Nick Bushby§, Sebastiaan Kuhne†, Jelle van den Bor†, Michael J. Waring??, Chris de Graaf†?, Iwan J. de Esch†, Henry F. Vischer†, Robert J. Sheppard‡, Maikel Wijtmans†, and Rob Leu Source Type: research

To switch or not to switch —first Germany-wide study from the perspective of pharmacists in the European environment
ConclusionPharmacists strongly welcome further switches. This leads to high acceptance rates, especially for a switch of desloratadine, as this was the most named active ingredient possible for a switch within the survey.Impact of findings on practice statementsThe outcome of this survey can support pharmaceutical companies in decision-making about which active substances they should submit a switch application for. Additionally, this helps fulfil patient needs, because pharmacists know best what is beneficial for patient self-care. In addition, all other actors involved in this process can see what is required and can ret...
Source: Journal of Public Health - June 28, 2019 Category: Health Management Source Type: research

Histamine and Delirium: Current Opinion
This study indicated that switch from H2 blockers to PPIs reduced delirium and, thus, providing an appropriate strategy to combat drug-induced delirium using antiulcer drugs (Fujii et al., 2012). The ventrolateral preoptic nucleus is a sleep-promoting nucleus located in the basal forebrain. A commonly used intravenous anesthetic, propofol, had been reported to induce sleep and augment the firing rate of neurons in ventrolateral GABAergic preoptic nucleus, but the underlining mechanism is yet to be clearly determined. Interestingly, the propofol-induced inhibition of inhibitory postsynaptic currents on noradrenalin-inhibite...
Source: Frontiers in Pharmacology - April 8, 2019 Category: Drugs & Pharmacology Source Type: research

OTC Drugs for Seasonal Allergies
Date: April 22, 2019 Issue #:  1570Summary:  Patients with seasonal allergies often experience nasal itching and congestion, sneezing, rhinorrhea, and itchy, watery eyes. Oral, intranasal, and ophthalmic preparations are widely available over the counter (OTC) for relief of symptoms. Prescription products for management of allergic rhinitis and allergic conjunctivitis are reviewed separately. (Source: The Medical Letter)
Source: The Medical Letter - March 20, 2019 Category: Drugs & Pharmacology Authors: admin Tags: Aerius Afrin Alavert Alaway Allegra Allergic rhinitis Antihistamines Avamys azelastine Benadryl Budesonide cetirizine Clarinex Claritin conjunctivities Cromolyn Desloratadine diphenhydramine Dristan Drixoral Fexofen Source Type: research

Ecotoxic effects of loratadine and its metabolic and light-induced derivatives.
Abstract Loratadine and desloratadine are second-generation antihistaminic drugs. Because of human administration, they are continuously released via excreta into wastewater treatment plants and occur in surface waters as residues and transformation products (TPs). Loratadine and desloratadine residues have been found at very low concentrations (ng/L) in the aquatic environment but their toxic effects are still not well known. Both drugs are light-sensitive even under environmentally simulated conditions and some of the photoproducts have been isolated and characterized. The aim of the present study was to...
Source: Ecotoxicology and Environmental Safety - December 19, 2018 Category: Environmental Health Authors: Iesce MR, Lavorgna M, Russo C, Piscitelli C, Passananti M, Temussi F, DellaGreca M, Cermola F, Isidori M Tags: Ecotoxicol Environ Saf Source Type: research

Screening and evaluation of fungal resources for loratadine metabolites.
Abstract Loratadine is a selective inverse agonist of peripheral histamine H1-receptors. Microbial biotransformation gained a lot of attention for its ability to convert molecules to valuable medicinally active substances. The main objective of the present research was to investigate the ability of different fungi to biotransform the drug loratadine to its active metabolite desloratadine, because desloratadine is four times more potent, possess longer duration of action than loratadine and is effective at low doses. The screening studies were performed with selected fungi using their respective broth media...
Source: Journal of Biosciences - December 1, 2018 Category: Biomedical Science Authors: Keerthana M, Vidyavathi M Tags: J Biosci Source Type: research

Prolonged intake of desloratadine: mesenteric lymphatic vessel dysfunction and development of obesity/metabolic syndrome.
This study aimed to establish mechanistic links between the prolonged intake of desloratadine, a common H1 receptor blocker (i.e. antihistamine), and development of obesity and metabolic syndrome. Male Sprague-Dawley rats were treated orally for 16 weeks with desloratadine. We analyzed the dynamics of body weight gain; tissue fat accumulation/density; contractility of isolated mesenteric lymphatic vessels; levels of blood lipids, glucose and insulin; together with parameters of liver function. Prolonged intake of desloratadine induced development of an obesity-like phenotype and signs of metabolic syndrome. These alteratio...
Source: American Journal of Physiology. Gastrointestinal and Liver Physiology - November 26, 2018 Category: Physiology Authors: Gasheva OY, Tsoy Nizamutdinova I, Hargrove L, Gobbell C, Troyanova-Wood M, Alpini SF, Pal S, Du C, Hitt AR, Yakovlev VV, Newell-Rogers MK, Zawieja DC, Meininger CJ, Alpini GD, Francis H, Gashev AA Tags: Am J Physiol Gastrointest Liver Physiol Source Type: research

The ameliorative effect of berberine and coenzyme Q10 in an ovalbumin-induced allergic rhinitis model
ConclusionWe think that berberine and coenzyme Q10 can usefully be employed as therapy due to their antioxidant and anti-inflammatory effects in an experimentally induced allergic rhinitis model. (Source: European Archives of Oto-Rhino-Laryngology)
Source: European Archives of Oto-Rhino-Laryngology - October 1, 2018 Category: ENT & OMF Source Type: research

Desloratadine and depression, a drug safety signal based on worldwide spontaneous reporting of side effects.
CONCLUSION: We hypothesize that desloratadine may enter the CNS and that it hence in rare cases may cause a clinically relevant state of depression, a relation that patients and their treating physicians should be made aware of. PMID: 30084285 [PubMed - as supplied by publisher] (Source: Upsala Journal of Medical Sciences)
Source: Upsala Journal of Medical Sciences - August 7, 2018 Category: General Medicine Authors: Boer J, Ederveen E, Grundmark B Tags: Ups J Med Sci Source Type: research