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Drugs Aug 1998Montelukast is a selective antagonist of the leukotriene D4 (LTD4) receptor. In patients with asthma, montelukast 5 to 250 mg/day attenuated LTD4-induced... (Clinical Trial)
Clinical Trial Randomized Controlled Trial Review
Montelukast is a selective antagonist of the leukotriene D4 (LTD4) receptor. In patients with asthma, montelukast 5 to 250 mg/day attenuated LTD4-induced bronchoconstriction and, at a dosage of 10 mg, significantly reduced early and late airway response to allergen (dust mite extract) relative to placebo. In studies evaluating the effects of various dosages of montelukast on exercise-induced bronchoconstriction the optimal dose of the drug was found to be 10 mg. Montelukast 10 mg/day controlled asthma significantly more effectively than placebo in a 3-month randomised double-blind study. In a 9-month open extension of this trial, during which patients were randomised to treatment with montelukast 10 mg/day or beclomethasone (approximately 400 micrograms/day), daytime symptom score and beta-agonist use decreased to a similar extent in each group. In a further study, treatment with montelukast 10 mg/day permitted clinically significant tapering of corticosteroid dosage in patients with stable asthma. Montelukast (5 mg/day) has also demonstrated efficacy in childhood asthma. The tolerability profile of montelukast was similar to that of placebo in placebo-controlled clinical trials in adults and children; the most common adverse event was headache.
Topics: Acetates; Adult; Anti-Asthmatic Agents; Asthma; Child; Cyclopropanes; Drug Tolerance; Humans; Quinolines; Sulfides
PubMed: 9711449
DOI: 10.2165/00003495-199856020-00010 -
Drug Delivery and Translational Research Feb 2022Dissolving microneedle (MN) patches are usually formulated with a blend of drug and excipients added for mechanical strength and drug stabilization. In this study, we...
Dissolving microneedle (MN) patches are usually formulated with a blend of drug and excipients added for mechanical strength and drug stabilization. In this study, we developed MNs made of pure drug to maximize drug loading capacity. MN patches were fabricated for transdermal delivery of montelukast sodium (MS) which is used to treat asthma and allergic rhinitis. We developed three different fabrication methods - solvent casting, melt casting, and solvent washing - and determined that filling molds with MS powder followed by a solvent washing method enabled MS to be loaded selectively to the MNs. Drug localization was confirmed with Raman imaging. MNs were able to penetrate in vitro and ex vivo skin models, and maintained strong mechanical properties during 6 months' storage at 22 °C. MS was also stable and compatible with the formulation used for the patch backing layer after 3 months' storage at 40 °C. MS delivery efficiency into skin was 55%, which enabled delivery of 3.2 mg MS into porcine skin ex vivo, which is in the range of MS doses in human clinical use. We conclude that the solvent washing method can be used to prepare MNs containing pure drug, such as MS at milligram doses in a ~ 1 cm MN patch.
Topics: Acetates; Administration, Cutaneous; Animals; Cyclopropanes; Drug Delivery Systems; Needles; Pharmaceutical Preparations; Quinolines; Skin; Solvents; Sulfides; Swine
PubMed: 34480297
DOI: 10.1007/s13346-021-01047-9 -
Allergologia Et Immunopathologia 2023Bronchial asthma is a prevalent type of respiratory disease that affects a large proportion of pediatric patients. The purpose of this study is to further investigate... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND AND AIM
Bronchial asthma is a prevalent type of respiratory disease that affects a large proportion of pediatric patients. The purpose of this study is to further investigate the clinical effects of budesonide combined with montelukast sodium in treating bronchial asthma.
METHODS
Eighty six children with bronchial asthma were equally divided into study and control groups via randomized double-blind controlled trial. The control group was treated with aerosol inhalation of budesonide combined with placebo, while the study group was treated with budesonide combined with montelukast sodium. Pulmonary function parameters, immunoglobulin, and recovery of related symptoms, along with the adverse reaction rate, were observed and compared between both groups.
RESULTS
Before treatment, there was no marked difference in pulmonary function parameters and immunoglobulin indexes between both groups ( > 0.05). All pulmonary function indicators and immunoglobulin indexes in both groups improved following therapy, with the study group outperforming the control group ( < 0.05). The recovery time of related symptoms in the study group was shorter than that in the control group ( < 0.05). The incidence of adverse reactions in both groups was compared, with notable differences ( < 0.05).
CONCLUSION
Budesonide combined with montelukast sodium in the treatment of bronchial asthma has the value of clinical application and promotion.
Topics: Humans; Child; Budesonide; Anti-Asthmatic Agents; Asthma; Acetates; Quinolines; Administration, Inhalation
PubMed: 37422792
DOI: 10.15586/aei.v51i4.897 -
Journal of Nanoscience and... Feb 2021Because some asthma patients have different types of inflammatory cells in their bodies, they cannot get relief with traditional drugs. However, the nano drug delivery...
Because some asthma patients have different types of inflammatory cells in their bodies, they cannot get relief with traditional drugs. However, the nano drug delivery system can realize efficient drug delivery, inflammatory cells and intracellular targeting, and the apoptosis of inflammatory cells. This article aims to comprehensively evaluate the effects of montelukast sodium combined with graphene oxide nanomaterials on improving the clinical symptoms and airway inflammation of children with bronchial asthma, with a view to further improving the clinical treatment of children with bronchial asthma. The results show that montelukast sodium can improve lung function in patients with asthma, and also has important effects such as anti-inflammatory and regulating immune function. After exposure to graphene oxide, the level of oxidative stress in mice increased with brightness and humidity, demonstrating the role of T oxidative stress in the development of asthma. In addition, nanocarriers assist co-loaded drugs to deepen and enrich the pulmonary inflammation site, further achieving effective mitochondrial targeted drug delivery, thereby enhancing the inhibitory effect of anti-apoptotic proteins, leading to inflammatory cell apoptosis.
Topics: Acetates; Animals; Anti-Asthmatic Agents; Asthma; Cyclopropanes; Graphite; Humans; Mice; Nanostructures; Quinolines; Sulfides
PubMed: 33183457
DOI: 10.1166/jnn.2021.18705 -
Expert Opinion on Pharmacotherapy Apr 2023Montelukast is a leukotriene inhibitor that is widely used to treat chronic asthma and allergic rhinitis. The drug interferes with molecular signaling pathways produced... (Review)
Review
INTRODUCTION
Montelukast is a leukotriene inhibitor that is widely used to treat chronic asthma and allergic rhinitis. The drug interferes with molecular signaling pathways produced by leukotrienes in a variety of cells and tissues throughout the human body that lead to tightening of airway muscles, production of aberrant pulmonary fluid (airway edema), and in some cases, pulmonary inflammation.
AREAS COVERED
Montelukast has also been noted to have anti-inflammatory properties, suggesting it may have a role in the treatment of coronavirus disease 2019 (COVID-19), the disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which has been noted to induce misfiring of the immune system in some patients. A literature search of PubMed was performed to identify all relevant studies of montelukast and SARS-CoV-2 through 27 January 2023.
EXPERT OPINION
Montelukast has been the subject of small studies of SARS-CoV-2 and will be included in a large, randomized, double-blind, placebo-controlled study of outpatients with COVID-19 sponsored by the United States National Institutes of Health known as Accelerating COVID-19 Therapeutic Interventions and Vaccines-6. This paper reviews what is known about montelukast, an inexpensive, well-tolerated, and widely available medication, and examines the rationale for using this drug to potentially treat patients with COVID-19.
Topics: Humans; COVID-19; Leukotriene Antagonists; SARS-CoV-2; Asthma; Acetates; Quinolines; Cyclopropanes; Sulfides; Double-Blind Method; Randomized Controlled Trials as Topic
PubMed: 36927284
DOI: 10.1080/14656566.2023.2192866 -
Pakistan Journal of Medical Sciences 2022To investigate the effects of Montelukast sodium combined with Budesonide aerosol on airway function and T lymphocytes in asthmatic children.
OBJECTIVES
To investigate the effects of Montelukast sodium combined with Budesonide aerosol on airway function and T lymphocytes in asthmatic children.
METHODS
The records of 86 pediatric asthma patients, treated in Huzhou Maternal and Child Health Hospital from February 2020 to March 2021, were studied retrospectively. Of them, 40 children received routine treatment + budesonide atomizer (Group-I), and 46 patients received routine treatment + budesonide atomizer + montelukast sodium (Group-II). The improvement in airway and lung function, and T-lymphocyte count in both groups after 3 months of corresponding treatment were analyzed.
RESULTS
After three months of treatment, expiratory flow rate (TEF) with the tidal volume of 25%, 50% and 75%, was significantly higher in Group-II than Group-I (P<0.05). CD8+ expression in Group-II was lower, and CD3+, CD4+ and CD4+/CD8+ were higher than those in Group-I (P<0.05). There was a significant difference in the levels of inflammatory factors between the two groups. The levels of IL-4, IL-5 and IFN-γ in Group-II were lower than those in Group-I(P<0.05).
CONCLUSIONS
In the clinical treatment of asthmatic children, in combination with routine treatment, budesonide atomizer and montelukast sodium can effectively promote the improvement of airway function, regulate T lymphocytes levels, reduce inflammatory reaction and improve the total clinical curative effect.
PubMed: 35799724
DOI: 10.12669/pjms.38.5.5749 -
Indian Journal of Pharmacology 2016Allergic rhinitis (AR) is a global health problem. Almost 10%-25% of population worldwide is affected by AR. Oral/intranasal H1-antihistamine, decongestants, leukotriene... (Comparative Study)
Comparative Study Randomized Controlled Trial
Comparison of efficacy, safety, and cost-effectiveness of montelukast-levocetirizine and montelukast-fexofenadine in patients of allergic rhinitis: A randomized, double-blind clinical trial.
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. Therefore, we aimed to compare the efficacy, safety, and cost-effectiveness of montelukast-levocetirizine and montelukast-fexofenadine combination in patients of AR.
MATERIALS AND METHODS
Seventy patients with AR participated in a prospective, randomized, double-blind, parallel, active-controlled, comparative 4-week trial. The patients between the age group of 18-65 years of either gender having moderate-severe intermittent or mild persistent AR were included in the study. The study inclusion criteria required the patients with total nasal symptom score (TNSS) of 5 or higher. The patients were randomly divided into two treatment groups with montelukast-levocetirizine (10 mg and 5 mg) in one group and montelukast-fexofenadine (10 mg and 120 mg) in another group. TNSS parameter was the main effectiveness parameter.
RESULTS
Evaluation of TNSS revealed significant difference ( < 0.05) when compared from baseline to 4 week in both groups. The mean change of TNSS, i.e., 9.46 was significant ( < 0.05) in montelukast-fexofenadine group. The cost-effectiveness ratio was less in montelukast-levocetirizine group than in montelukast-fexofenadine group.
CONCLUSION
The decrease in TNSS was more in montelukast-fexofenadine group, but the cost-effectiveness is more with montelukast-levocetirizine combination.
Topics: Acetates; Anti-Allergic Agents; Anti-Asthmatic Agents; Cetirizine; Cost-Benefit Analysis; Cyclopropanes; Double-Blind Method; Drug Therapy, Combination; Female; Follow-Up Studies; Humans; Male; Prospective Studies; Quinolines; Rhinitis, Allergic; Sulfides; Terfenadine; Treatment Outcome
PubMed: 28066101
DOI: 10.4103/0253-7613.194854 -
Proceedings of the National Academy of... Feb 2021
Topics: Acetates; Atazanavir Sulfate; Benzimidazoles; Biphenyl Compounds; Chloroquine; Cyclopropanes; Dipyridamole; Humans; Oxytetracycline; Pharmaceutical Preparations; Protease Inhibitors; Quinolines; SARS-CoV-2; Sulfides; Tetrazoles; COVID-19 Drug Treatment
PubMed: 33568498
DOI: 10.1073/pnas.2024420118 -
Journal of Chromatographic Science Dec 2023Recently, the aim of analytical community is to reduce the usage of hazardous chemicals; so eco-friendly, rapid, selective and cost-effective methods were developed for...
Recently, the aim of analytical community is to reduce the usage of hazardous chemicals; so eco-friendly, rapid, selective and cost-effective methods were developed for simultaneous determination of montelukast sodium (MKT) and loratadine (LRT). The first method was based on chromatographic separation performed on precoated silica gel 60 GF254 plates with ethyl acetate-ethanol 9: 1 (v/v) as the mobile phase. The developed plates were scanned and quantified at 260 nm. The method gives linear correlation over concentration ranges of 0.3-3.6 μg/spot and 0.2-4.0 μg/spot for MKT and LRT, respectively. It was also successfully applied to analysis of both drugs in their pharmaceutical preparation and human plasma. The other methods are UV-spectrophotometric methods based on smart spectra manipulating to zero order spectrum of each drug. These methods are named response correlation (RC), a-centering and ratio derivative methods. RC and a-centering methods were dependent on the presence of an isosbestic point between the overlapped spectra of both drugs. While ratio derivative method based on manipulation of the ratio spectra of both drugs. The two drugs obey Beer-Lambert law over the concentration ranges of 3.0-30.0 μg/mL in the three spectrophotometric methods. Moreover, the greenness of the developed methods is assessed using suitable analytical Eco-Scale and Green Analytical Procedure Index.
Topics: Humans; Loratadine; Spectrophotometry; Quinolines; Densitometry
PubMed: 37032124
DOI: 10.1093/chromsci/bmad025 -
Expert Opinion on Drug Safety May 2009Suicide is a serious public health problem. Prevention of suicide depends to a great degree on identification and mitigation of its risk factors. Allergy has been... (Review)
Review
BACKGROUND
Suicide is a serious public health problem. Prevention of suicide depends to a great degree on identification and mitigation of its risk factors. Allergy has been associated with mood and anxiety disorders, risk factors for suicidality. Antiallergic medication could modulate or mediate these predictive associations. Recently, the FDA issued a warning raising concerns about the suicidality potential of montelukast and other leukotriene (LT) antagonists.
OBJECTIVE
The purpose of this review is to integrate the emerging interpretations of the link between suicidality, suicide risk factors, allergy and treatment of allergy in particular, with LT antagonists.
METHODS
We reviewed the available reports on the possible relationships between montelukast, allergy, suicide, suicidality and suicide risk factors. We also present the positions of the FDA, manufacturer, and national organizations of allergists and immunologists on the possible role of montelukast in suicidality.
CONCLUSION
At present, there is insufficient data to prove that there is a link between montelukast and suicidality. Inquiring about mood changes and suicidal ideation should be integrated in general medical practice.
Topics: Acetates; Cyclopropanes; Humans; Hypersensitivity; Quinolines; Risk Factors; Suicide; Sulfides; Suicide Prevention
PubMed: 19505261
DOI: 10.1517/14740330902932688