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https://www.readbyqxmd.com/read/28088523/the-selective-cysteinyl-leukotriene-receptor-1-cyslt1r-antagonist-montelukast-regulates-extracellular-matrix-remodeling
#1
Jingli Peng, Hezheng Zhou, Guoping Kuang, Lilian Xie, Tao Tian, Ru Liu
Scar formation after filtration surgery of glaucoma is mainly caused by excessive synthesis of new extracellular matrix (ECM) and contraction of subconjunctival tissue mediated by human Tenon fibroblasts (HTFs) and the transforming growth factor (TGF-β1). Montelukast, a potent and specific cysteinyl leukotriene receptor 1 (cysLT1R) antagonist, is a licensed drug clinically used for the treatment of bronchial asthma. In this study, we investigated the effects of montelukast on the contractility of HTFs cultured in a three-dimensional collagen gel...
January 11, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28087482/prolonged-acute-suppression-of-cysteinyl-leukotriene-to-reduce-capsular-contracture-around-silicone-implants
#2
Byung Hwi Kim, Min Park, Hyo Jin Park, Seung Ho Lee, Sung Yoon Choi, Chun Gwon Park, Su Min Han, Chan Yeong Heo, Young Bin Choy
: We hypothesize that periodically early, local suppression of cysteinyl leukotrienes (CysLTs), which are potent inflammatory mediators, can reduce the fibrotic capsular contracture around silicone implants. We tested this hypothesis with the silicone implants enabled with the sustained release of montelukast, a CysLT receptor antagonist, for 3 and 15 days. In this work, we inserted each of the distinct implants into the pocket of the subpanniculus carnosus plane of living rats and performed histological and immunofluorescent (IF) analyses of the tissues biopsied at predetermined periods for 12 weeks after implant insertion...
January 10, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28066101/comparison-of-efficacy-safety-and-cost-effectiveness-of-montelukast-levocetirizine-and-montelukast-fexofenadine-in-patients-of-allergic-rhinitis-a-randomized-double-blind-clinical-trial
#3
Mohini Sachin Mahatme, Ganesh Natthuji Dakhale, Kanchan Tadke, Sachin Keshaorao Hiware, S D Dudhgaonkar, Sumit Wankhede
OBJECTIVES: Allergic rhinitis (AR) is a global health problem. Almost 10%-25% of population worldwide is affected by AR. Oral/intranasal H1-antihistamine, decongestants, leukotriene receptor antagonists, and intranasal corticosteroids are the pillars in the management of AR. The combination therapy of montelukast with antihistaminic provides enhancing and complimentary effects, thereby reducing the symptoms effectively, but there are scanty data regarding the comparisons of combinations...
November 2016: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/28057540/low-molecular-weight-heparin-coated-and-montelukast-filled-inhalable-particles-a-dual-drug-delivery-system-for-combination-therapy-in-asthma
#4
Brijeshkumar Patel, Jahidur Rashid, Nilesh Gupta, Fakhrul Ahsan
Montelukast, a cysteinyl leukotriene type 1 receptor antagonist, exhibits secondary anti-inflammatory properties when used at higher concentrations. Low molecular weight heparin (LMWH) evokes pronounced anti-inflammatory effects by interrupting leukocyte adhesion and migration. We hypothesized that inhalable particles containing montelukast plus LMWH release both drugs in a sustained fashion and protect the lungs against allergen-induced inflammation. Large porous particles of montelukast and LMWH were prepared using a double-emulsion-solvent-evaporation method...
January 2, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28051240/clinical-effect-of-treating-secondary-asthma-attacks-of-children-mycoplasma-pneumoniae-with-combined-therapy-of-montelukast-and-azithromycin
#5
L Gong, L Xu, M Diao, F Guo, F-F Bian, J Min, R Liu, C-L Zhang
OBJECTIVE: To discuss the clinical effects of treating secondary asthma attacks of children Mycoplasma pneumoniae with combined therapy of montelukast and azithromycin. PATIENTS AND METHODS: 96 children patients diagnosed with secondary asthma attacks of Mycoplasma pneumonia were enrolled in this study. They were randomly divided into two groups: the control group (n=49) and the observation group (n=47). Patients in the control group received combined therapy using azithromycin and bronchodilators or glucocorticoid, and patients in the observation group received a combined therapy of montelukast, azithromycin and bronchodilators or glucocorticoid...
December 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28002678/transfer-of-montelukast-into-human-milk-during-lactation
#6
Palika Datta, Kathleen Rewers-Felkins, Teresa Baker, Thomas W Hale
AIM: The aim of this study was to determine levels of montelukast in human milk and to develop a simple, sensitive analytical method using mass spectrometry. METHODS: Milk samples were collected from seven breastfeeding mothers, age 26-35 years, at 0, 1, 2, 4, 8, and 12 hours after oral ingestion of 10 mg montelukast. The samples were analyzed using a new Liquid Chromatography-Tandem Mass Spectrometry method. Area under the milk concentration time curve from zero to the time of the last sample (12 hours) was estimated by the linear trapezoidal rule...
December 21, 2016: Breastfeeding Medicine: the Official Journal of the Academy of Breastfeeding Medicine
https://www.readbyqxmd.com/read/27998374/a-four-year-old-boy-with-unusually-severe-obstructive-sleep-apnea
#7
Taomei Li, Guangyao Zhou, Linghui Yang, Lu Tan, Rong Ren, Yuanfeng Sun, Yun Li, Xiangdong Tang
We report a clinical observation of a four-year-old boy who was diagnosed with unusually severe obstructive sleep apnea with an apnea hypopnea index up to 102.5 events/h. After taking montelukast for two months, his AHI was significantly reduced to 2.4 events/h and his adenoidal nasopharyngeal ratio was reduced from 0.92 to 0.80.
December 16, 2016: Journal of Clinical Sleep Medicine: JCSM: Official Publication of the American Academy of Sleep Medicine
https://www.readbyqxmd.com/read/27989858/aerosolizable-modified-release-particles-of-montelukast-improve-retention-and-availability-of-the-drug-in-the-lungs
#8
Brijeshkumar Patel, Jahidur Rashid, Fakhrul Ahsan
Montelukast, a cysteinyl leukotriene receptor antagonist available as oral tablets, is used as a second-line therapy in asthma. In this study, we sought to enhance the availability of montelukast in the lungs by encapsulating the drug in poly (lactide-co-glycolic acid)-based (PLGA) respirable large porous particles. We determined the oral and lung specific availability of montelukast by assessing metabolic stability of the drug in the lung and liver homogenates, respectively. We similarly measured the oral and inhalational bioavailability by monitoring the pharmacokinetics and disposition of the drug in live animals...
October 27, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27965779/asthma-phenotypes-the-intriguing-selective-intervention-with-montelukast
#9
REVIEW
Cottini Marcello, Lombardi Carlo
Asthma is a heterogeneous disease, usually characterized by chronic airway inflammation and a variable course associated with various underlying mechanisms that can differ between individuals. Patients with asthma can therefore exhibit different phenotypes, a term used to define the observable characteristics of an organism resulting from the interaction between its genetic makeup and the environment. The heterogeneity of asthma has received a large amount of attention in the last few years in order to better tailor treatment according to the different clinical and biological phenotypes of the disease...
2016: Asthma research and practice
https://www.readbyqxmd.com/read/27931302/new-insights-into-treatment-of-children-with-exercise-induced-asthma-symptoms
#10
Iwona Stelmach, Anna Sztafiska, Joanna Jerzyska, Daniela Podlecka, Pawe Majak, Wodzimierz Stelmach
BACKGROUND: Exercise is one of the most common triggers of bronchoconstriction and affects up to 80% of children with asthma. OBJECTIVE: The purpose of this randomized, double-blind, placebo-controlled study was to assess the effectiveness of treatment with ciclesonide 160 microgram, either alone, with a higher dose, with a leukotriene receptor antagonist (LTRA), or with a long-acting beta-agonist (LABA) in children with asthma with postexercise-induced symptoms...
November 2016: Allergy and Asthma Proceedings:
https://www.readbyqxmd.com/read/27931141/modulation-of-leukotriene-signaling-inhibiting-cell-growth-in-chronic-myeloid-leukemia
#11
Elham Yektaei-Karin, Ana Zovko, Anders Nilsson, Barbro Näsman-Glaser, Lena Kanter, Olof Rådmark, Jonas Wallvik, Marja Ekblom, Monika Dolinska, Hong Qian, Leif Stenke
Although tyrosine kinase inhibitors (TKIs) have dramatically improved clinical outcome in chronic myeloid leukemia (CML), cure rarely occurs. This may be due to BCR-ABL-independent, aberrant signaling pathways, one of which leads to leukotriene (LT) formation. Well-recognized as inflammatory mediators, LT can also affect oncogenic mechanisms of several tumors. We have previously discovered elevated LT-synthesis and up-regulated cysteinyl-LT-inducing enzyme in CML. Here we report on dose-dependent inhibition of CML cell growth exerted by specific blockers of LT-signaling...
December 8, 2016: Leukemia & Lymphoma
https://www.readbyqxmd.com/read/27912950/a-randomized-placebo-controlled-trial-of-traditional-chinese-medicine-as-an-add-on-therapy-to-oral-montelukast-in-the-treatment-of-mild-persistent-asthma-in-children
#12
Pak-Hong Chan, Ching-Yee To, Eric Yat-Tung Chan, Handong Li, Xiuxia Zhang, Pok-Yu Chow, Po-Ling Liu, Shuk-Yu Leung, Chung-Hong Chan, Ka-Yan Chan, Johnny Yick-Chun Chan, Jonathan Pak-Heng Ng, Daniel Kwok-Keung Ng
OBJECTIVES: Traditional Chinese medicine are commonly used for treatment of asthma. However, there are only very limited data about its efficacy in children. Therefore, we aimed to determine the efficacy of augmented Yu Ping Feng San (aYPFS) as an add-on to oral montelukast compared with montelukast alone for treatment of mild persistent asthma in children. DESIGN: A single centre, placebo-controlled, double-blinded, randomized control trial was carried out. Participants with age 6-18 years who had mild persistent asthma were randomized according to random number list to receive either aYPFS plus montelukast for 24 weeks or placebo plus montelukast for 24 weeks...
December 2016: Complementary Therapies in Medicine
https://www.readbyqxmd.com/read/27909742/the-anti-inflammatory-effect-of-montelukast-a-cysteinyl-leukotriene-receptor-1-antagonist-against-estradiol-induced-nonbacterial-inflammation-in-the-rat-prostate
#13
Mahmoud M Said, Maarten C Bosland
There is no standard treatment of chronic nonbacterial prostatitis in humans. The current study was aimed to investigate the effect of montelukast, an antagonist of cysteinyl leukotriene receptor-1, against estrogen-induced, nonbacterial lateral lobe-specific prostate inflammation in rats. Male Wistar rats were randomized into five groups of six rats, including sham controls (group 1) and castrated rats (group 2), whereas nonbacterial prostatitis (NBP) was induced in groups 3-5 by castration followed by a daily subcutaneous injection of estradiol (0...
December 1, 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27888864/oesophageal-disease-gastroesophageal-reflux-disease-barrett-s-oesophagus-achalasia-and-eosinophilic-oesophagitis
#14
Xavier Calvet
The most interesting conclusions and/or advances presented at Digestive Disease Week 2016 were the following: a) gastroesophageal reflux disease: proton pump inhibitor-refractory reflux disease is frequently associated with poor treatment adherence, psychiatric comorbidities and functional gastrointestinal disorders. These possible entities should be investigated in all cases of proton pump inhibitor-refractory reflux disease; b) Barrett's oesophagus: the efficacy of screening remains unclear; however, new minimally-invasive techniques such as the cytosponge allow more effective detection, both of Barrett's oesophagus and Barrett's oesophagus-associated dysplasia or neoplasia; c) achalasia: evidence indicates that peroral endoscopic myotomy is as effective as surgery and is a safer alternative; d) eosinophilic oesophagitis: high-dose proton pump inhibitors are required to rule out proton pump inhibitor-responsive eosinophilic oesophagitis; montelukast is not clearly effective in the treatment of eosinophilic oesophagitis, although moderate efficacy cannot be ruled out...
September 2016: Gastroenterología y Hepatología
https://www.readbyqxmd.com/read/27887950/cyslt2-receptor-activation-is-involved-in-ltc4-induced-lung-air-trapping-in-guinea-pigs
#15
Tomohiko Sekioka, Michiaki Kadode, Yasuo Yonetomi, Akihiro Kamiya, Manabu Fujita, Takeshi Nabe, Kazuhito Kawabata
CysLT1 receptors are known to be involved in the pathogenesis of asthma. However, the functional roles of CysLT2 receptors in this condition have not been determined. The purpose of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs and use this model to clarify the mechanism underlying response to such trapping. Because LTC4 is rapidly converted to LTD4 by γ-glutamyltranspeptidase (γ-GTP) under physiological conditions, S-hexyl GSH was used as a γ-GTP inhibitor...
January 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27885204/genetic-interactions-between-adrb2-and-ptger4-on-responses-to-salmeterol-or-montelukast-in-japanese-patients-with-mild-persistent-asthma
#16
Hideyasu Yamada, Hironori Masuko, Toshihide Inui, Jun Kanazawa, Yohei Yatagai, Tohru Sakamoto, Hiroaki Iijima, Satoshi Konno, Kaoruko Shimizu, Hironi Makita, Masaharu Nishimura, Fumio Kokubu, Takefumi Saito, Takeo Endo, Hiroki Ninomiya, Norihiro Kaneko, Nobuyuki Hizawa
BACKGROUND: Long-acting β2-agonists (LABA) and leukotriene receptor antagonists (LTRA) are two principal agents that can be added to inhaled corticosteroids (ICS) for patients with asthma that is not adequately controlled by ICS alone. In our previous study, the Gly16Arg genotype of the β2-adrenergic receptor (ADRB2) gene did not influence the differential bronchodilator effect of salmeterol versus montelukast as an add-on therapy to ICS within 16 weeks of follow-up (the J-Blossom study)...
2016: Arerugī, [Allergy]
https://www.readbyqxmd.com/read/27882879/treatment-of-chronic-spontaneous-urticaria-with-an-inadequate-response-to-h1-antihistamines-an-expert-opinion
#17
Christian Vestergaard, Elias Toubi, Marcus Maurer, Massimo Triggiani, Barbara Ballmer-Weber, Alexander Marsland, Marta Ferrer, André Knulst, Ana Giménez-Arnau
Chronic spontaneous urticaria (CSU) is characterized by the sudden, continuous or intermittent appearance of pruritic wheals (hives), angioedema, or both for six weeks or more, with no known specific trigger. The international EAACI/GA(2)LEN/EDF/WAO urticaria guideline advises standard-dose, second-generation H1-antihistamines as first-line therapy. However, H1-antihistamine treatment leads to absence of symptoms in fewer than 50% of patients. Updosing of second-generation H1-antihistamines (up to fourfold) as recommended by the EAACI/GA(2)LEN/EDF/WAO urticaria guideline as second-line therapy, can improve response, but many patients remain symptomatic...
November 23, 2016: European Journal of Dermatology: EJD
https://www.readbyqxmd.com/read/27881050/pharmaceutical-rejuvenation-of-age-associated-decline-in-spatial-memory
#18
Andrew R Mendelsohn, James W Larrick
Spatial memory and cognition decline during aging. Montelukast, an FDA approved drug for the treatment of asthma, can restore spatial memory in old rats to levels similar to those of young animals. Treatment improves three hallmarks of aging in the brain: reducing microglial-mediated neuroinflammation, blood-brain barrier (BBB) permeability, and increasing neurogenesis in the hippocampus although not completely to youthful levels. Other aging-associated parameters, such as reduced synaptic density, are not affected, suggesting that anti-aging therapeutics may be further optimized...
December 2016: Rejuvenation Research
https://www.readbyqxmd.com/read/27857833/design-formulation-and-physicochemical-evaluation-of-montelukast-orally-disintegrating-tablet
#19
Abolfazl Aslani, Maryam Beigi
BACKGROUND: Orally disintegrating tablets (ODTs) are a modern form of tablets that when placed in the oral cavity, disperses rapidly. These tablets have advantages, particularly good applications for children and old patients who have a complication in chewing or swallowing solid dosage forms. The aim of this study was to design, formulate, and evaluate the physicochemical properties of 5 mg montelukast ODTs for the prevention of asthma and seasonal allergies. METHODS: Formulations were prepared with different amounts of super disintegrating agents and effervescent bases as disintegrant agents...
2016: International Journal of Preventive Medicine
https://www.readbyqxmd.com/read/27826703/leukotriene-receptor-antagonists-and-antiallergy-drugs
#20
Tsutomu Tamada, Masakazu Ichinose
As one of the candidates of the therapeutic strategy for asthma in addition to inhaled corticosteroids (ICS), leukotriene receptor antagonists (LTRAs) are known to be useful for long-term management of asthma patients complicated by allergic rhinitis (AR) or exercise-induced asthma (EIA). Currently available LTRAs are pranlukast hydrate, zafirlukast, and montelukast. These LTRAs have a bronchodilator action and inhibit airway inflammation, resulting in a significant improvement of asthma symptoms, respiratory function, inhalation frequency of as-needed inhaled β2-agonist, airway inflammation, airway hyperresponsiveness, dosage of ICSs, asthma exacerbations, and patients' QOL...
November 9, 2016: Handbook of Experimental Pharmacology
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