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In-silico discovery of efficient second-generation drug derivatives with enhanced antihistamine potency and selectivity.
Comput Biol Chem
January 2025
Department of Chemistry, University of Agriculture Faisalabad, Faisalabad 38000, Pakistan.
The current study focuses on the potential of second-generation antihistamines, which exhibit fewer side effects compared to first-generation drugs, to block the Histamine H receptor (HR) and mitigate allergic responses. We screened several derivatives of second-generation drugs taking Desloratadine (Deslo) and Acrivastine (Acra) as seed compounds. We performed molecular docking, drug-likeness, quantum chemical calculations, UV-visible and infrared spectroscopy, molecular electrostatic potential (MEP) mapping for understanding drug derivatives potential as efficient drugs and molecular dynamics (MD).
View Article and Find Full Text PDFData mining in FAERS: association of newer-generation H1-antihistamines with nervous system disorders.
BMC Pharmacol Toxicol
December 2024
Department of Pharmacy, West China Second University Hospital, Sichuan University, Chengdu, Sichuan, 610041, China.
Background: H1-antihistamines are widely used to treat symptoms depending on histamine release in a variety of conditions. However, neurological adverse events have been reported in post-marketing surveillance studies and there are limited literatures comparing the neurological disorders associated with newer-generation H1-antihistamines from real-world datasets.
Aims: We performed a comparative analysis of nervous system disorders and several newer-generation H1-antihistamines including: cetirizine, loratadine, levocetirizine, desloratadine and fexofenadine.
Comparative Efficacy of Mometasone Nasal Spray Combined with Different Doses of Desloratadine, and Montelukast in Childhood Allergic Rhinitis: A Randomized Clinical Trial.
Iran J Allergy Asthma Immunol
July 2024
Division of Allergy and Clinical Immunology, Department of Pediatrics, Bahrami Children's Hospital, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran.
Article Synopsis
- Allergic rhinitis is a common issue in children, and while several medications like nasal corticosteroids and antihistamines are used to treat it, there's ongoing debate about the best dosage and combinations for maximum effectiveness.* -
- A study involving 64 children compared the effects of different drug combinations alongside mometasone furoate nasal spray, measuring symptoms like nasal congestion and sneezing.* -
- Results showed that using desloratadine twice daily or a combination of desloratadine and montelukast significantly improved symptom control compared to other treatment options.*
Combining dipyridamole and cilostazol with up-dosing antihistamines improves outcomes in chronic spontaneous urticaria with high D-dimer levels: A randomized controlled trial.
Exp Dermatol
August 2024
Division of Allergy and Clinical Immunology, Department of Medicine, Faculty of Medicine, Chulalongkorn University, Bangkok, Thailand.
Article Synopsis
- * Patients were split into two groups: one received both antiplatelet therapy (cilostazol and dipyridamole) and antihistamine, while the other group only received antihistamine for four weeks.
- * Results showed that the antiplatelet group had a significantly greater reduction in Urticaria Activity Scores, improved quality of life, and decreased D-dimer levels, suggesting the combination treatment is more effective for certain CSU patients.
Spectroscopic, electrochemical, and molecular docking studies of the interaction between the antihistamine drug desloratadine and dsDNA.
Anal Biochem
November 2024
Ankara University, Faculty of Pharmacy, Department of Analytical Chemistry, 06560, Ankara, Turkey. Electronic address:
Through the utilization of fluorescence spectroscopy, electrochemical, and molecular docking methods, this research investigates the interaction between the antihistamine drug desloratadine and calf thymus double-stranded DNA (ct-dsDNA). Deoxyguanosine (dGuo) and deoxyadenosine (dAdo) oxidation signals were diminished by incubation with varying concentrations of desloratadine, as determined by differential pulse voltammetry (DPV). This change was ascribed to desloratadine's binding mechanism to ct-dsDNA.
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