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Pharmaceutics Jan 2023Mometasone furoate (MF) is a medium-potency synthetic glucocorticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. However, its role in the...
Mometasone furoate (MF) is a medium-potency synthetic glucocorticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. However, its role in the treatment of ocular inflammation has not yet been explored. This work investigated the anti-inflammatory activity of MF in ocular tissues. First, the in vivo safety of the intravitreal (IVT) injection of MF (80, 160, and 240 µg) was evaluated via clinical examination (including the assessment of intraocular pressure), electroretinography (ERG), and histopathology. Second, MF was tested in an experimental model of bacillus Calmette-Guérin (BCG)-induced uveitis in Wistar rats. Intraocular inflammation was then evaluated via a slit-lamp and fundus examination, ERG, histopathology, and the quantification of pro-inflammatory markers. Intravitreal MF showed no toxicity in all the investigated doses, with 160 µg leading to attenuated disease progression and improvement in clinical, morphological, and functional parameters. There was a significant reduction in the levels of inflammatory markers (myeloperoxidase, interleukins 6 and 1β, CXCL-1, and tumor necrosis factor-alpha) when compared to the levels in untreated animals. Therefore, MF should be further investigated as a promising drug for the treatment of ocular inflammation.
PubMed: 36678822
DOI: 10.3390/pharmaceutics15010193 -
Toxicology and Applied Pharmacology Oct 2013Chlorine gas is a widely used industrial compound that is highly toxic by inhalation and is considered a chemical threat agent. Inhalation of high levels of chlorine...
Chlorine gas is a widely used industrial compound that is highly toxic by inhalation and is considered a chemical threat agent. Inhalation of high levels of chlorine results in acute lung injury characterized by pneumonitis, pulmonary edema, and decrements in lung function. Because inflammatory processes can promote damage in the injured lung, anti-inflammatory therapy may be of potential benefit for treating chemical-induced acute lung injury. We previously developed a chlorine inhalation model in which mice develop epithelial injury, neutrophilic inflammation, pulmonary edema, and impaired pulmonary function. This model was used to evaluate nine corticosteroids for the ability to inhibit chlorine-induced neutrophilic inflammation. Two of the most potent corticosteroids in this assay, mometasone and budesonide, were investigated further. Mometasone or budesonide administered intraperitoneally 1h after chlorine inhalation caused a dose-dependent inhibition of neutrophil influx in lung tissue sections and in the number of neutrophils in lung lavage fluid. Budesonide, but not mometasone, reduced the levels of the neutrophil attractant CXCL1 in lavage fluid 6h after exposure. Mometasone or budesonide also significantly inhibited pulmonary edema assessed 1 day after chlorine exposure. Chlorine inhalation resulted in airway hyperreactivity to inhaled methacholine, but neither mometasone nor budesonide significantly affected this parameter. The results suggest that mometasone and budesonide may represent potential treatments for chemical-induced lung injury.
Topics: Animals; Anti-Inflammatory Agents; Bronchoalveolar Lavage Fluid; Budesonide; Chlorine; Glucocorticoids; Mice; Mice, Inbred Strains; Mometasone Furoate; Neutrophil Infiltration; Pneumonia; Pregnadienediols; Pulmonary Edema
PubMed: 23800689
DOI: 10.1016/j.taap.2013.06.009 -
Respiratory Medicine May 2023A novel, once-daily, fixed-dose combination of mometasone furoate/indacaterol acetate/glycopyrronium bromide (MF/IND/GLY) delivered via Breezhaler® is the first inhaled...
Efficacy of once-daily, single-inhaler, fixed-dose combination of mometasone/indacaterol/glycopyrronium in patients with asthma with or without persistent airflow limitation: Post hoc analysis from the IRIDIUM study.
BACKGROUND
A novel, once-daily, fixed-dose combination of mometasone furoate/indacaterol acetate/glycopyrronium bromide (MF/IND/GLY) delivered via Breezhaler® is the first inhaled corticosteroid/long-acting ꞵ-agonist/long-acting muscarinic antagonist (ICS/LABA/LAMA) therapy approved for the maintenance treatment of asthma in adults inadequately controlled on ICS/LABA combination. In patients with asthma and persistent airflow limitation (PAL), maximal treatment, especially with combination is suggested. This post hoc analysis of data from the IRIDIUM study assessed the efficacy of MF/IND/GLY in asthma patients with and without PAL.
METHODS
Patients with post-bronchodilator FEV ≤80% of predicted and FEV/FVC ratio of ≤0.7 were categorised as PAL subgroup and the remaining as the non-PAL subgroup. Lung function parameters (FEV, PEF, and FEF) and annualised asthma exacerbations rates were evaluated in both subgroups across the treatment arms: once-daily high-dose MF/IND/GLY (160/150/50 μg), high-dose MF/IND (320/150 μg) and twice-daily high-dose fluticasone/salmeterol (FLU/SAL; 500/50 μg).
RESULTS
Of the 3092 randomised patients, 64% (n = 1981) met the criteria for PAL. Overall, there was no evidence of treatment difference between PAL and non-PAL subgroups (interaction P-value for FEV, FEF, PEF, moderate or severe exacerbations, severe exacerbations and all exacerbations were 0.42, 0.08, 0.43 0.29, 0.35 and 0.12, respectively). In the PAL subgroup, high-dose MF/IND/GLY versus high-dose MF/IND and high-dose FLU/SAL improved trough FEV (mean difference: 102 mL [P < 0.0001] and 137 mL [P < 0.0001]) and reduced moderate or severe (16% and 32%), severe (25% and 39%) and all exacerbations (19% and 38%), respectively.
CONCLUSIONS
Once-daily fixed-dose MF/IND/GLY was efficacious in asthma patients with and without persistent airflow limitation.
Topics: Adult; Humans; Glycopyrrolate; Mometasone Furoate; Iridium; Pulmonary Disease, Chronic Obstructive; Drug Combinations; Forced Expiratory Volume; Lung; Asthma; Indans; Nebulizers and Vaporizers; Administration, Inhalation; Bronchodilator Agents
PubMed: 36906187
DOI: 10.1016/j.rmed.2023.107172 -
Respiratory Medicine Dec 2012Fixed-dose combinations of inhaled corticosteroids (ICSs) and long-acting β2-agonists (LABAs) have been used to manage asthma for several years. They are the preferred... (Review)
Review
Fixed-dose combinations of inhaled corticosteroids (ICSs) and long-acting β2-agonists (LABAs) have been used to manage asthma for several years. They are the preferred therapy option for patients who do not achieve optimal control of their asthma with low-dose ICS monotherapy. In Europe, four ICS/LABA products are commercially available for asthma maintenance therapy (fluticasone propionate/formoterol fumarate, fluticasone propionate/salmeterol xinafoate, budesonide/formoterol fumarate and beclometasone dipropionate/formoterol fumarate), and other combinations are likely to be developed over the next few years (e.g. mometasone/formoterol fumarate, fluticasone furoate/vilanterol, mometasone/indacaterol). Data from randomized, controlled, clinical trials do not demonstrate a clear overall efficacy difference among ICS/LABA combinations approved for asthma therapy. Conversely, pharmacological data indicate that there may be certain advantages to using one ICS or LABA over another because of the specific pharmacodynamic and pharmacokinetic profiles associated with particular treatments. This review article summarizes the pharmacological characteristics oft he various ICSs and LABAs available for the treatment of asthma, including the potential for ICS and LABA synergy, and gives an insight into the rationale for the development of the latest ICS/LABA combination approved for asthma maintenance therapy.
Topics: Administration, Inhalation; Adrenergic beta-2 Receptor Agonists; Albuterol; Androstadienes; Anti-Asthmatic Agents; Asthma; Beclomethasone; Bronchodilator Agents; Budesonide; Drug Combinations; Drug Therapy, Combination; Ethanolamines; Evidence-Based Medicine; Fluticasone; Fluticasone-Salmeterol Drug Combination; Formoterol Fumarate; Glucocorticoids; Humans; Nebulizers and Vaporizers; Randomized Controlled Trials as Topic; Salmeterol Xinafoate; Time Factors; Treatment Outcome
PubMed: 23273165
DOI: 10.1016/S0954-6111(12)70005-7 -
Drug Delivery and Translational Research Nov 2023Mometasone furoate (MF) is a synthetic glucocorticoid used clinically to treat specific inflammatory disorders including superior and inferior respiratory tract. Due to...
Mometasone furoate (MF) is a synthetic glucocorticoid used clinically to treat specific inflammatory disorders including superior and inferior respiratory tract. Due to its poor bioavailability we further investigated whether nanoparticles (NPs) made of zein protein may constitute a safe and effective choice to incorporate MF. Thus, in this work, we loaded MF into zein NPs aiming to evaluate possible advantages that could result from oral delivery and extend the range of MF application such as inflammatory gut diseases. MF-loaded zein NPs presented an average size in the range of 100 and 135 nm, narrow size distribution (polydispersity index < 0.300), zeta potential of around + 10 mV and association efficiency of MF over 70%. Transmission electron microscopy imaging revealed that NPs had a round shape and presented a smooth surface. The zein NPs showed low MF release in a buffer that mimics the gastric condition (pH = 1.2) and slower and controlled MF release in the intestinal condition (pH = 6.8). The short and intermediate safety of zein NPs was confirmed assessing the incubation against Caco-2 and HT29-MTX intestinal cells up to 24 h. Permeability studies of MF across Caco-2/HT29-MTX co-culture monolayer evidenced that zein NPs modulated MF transport across cell monolayer resulting in a stronger and prolonged interaction with mucus, potentially extending the time of absorption and overall local and systemic bioavailability. Overall, zein NPs showed to be suitable to carry MF to the intestine and future studies can be developed to investigate the use of MF-loaded zein NPs to treat intestinal inflammatory diseases.
Topics: Humans; Mometasone Furoate; Zein; Caco-2 Cells; Nanoparticles; Drug Carriers
PubMed: 37208563
DOI: 10.1007/s13346-023-01367-y -
Journal of Healthcare Engineering 2022The objective is to explore the treatment effect of mometasone furoate cream on lichen sclerosus et atrophicus (LSeA) of external genitalia in boys and its correlation...
Treatment Effect of Mometasone Furoate Cream on Lichen Sclerosus et Atrophicus of External Genitalia in Boys and Its Correlation with Toll-Like Receptor 4 and Myeloid Differentiation Factor 88.
OBJECTIVE
The objective is to explore the treatment effect of mometasone furoate cream on lichen sclerosus et atrophicus (LSeA) of external genitalia in boys and its correlation with Toll-like receptor 4 (TLR4) and myeloid differentiation factor 88 (MyD88).
METHODS
A total of 100 boys treated in our hospital from January 2021 to January 2023 due to clinical manifestations in the external genitalia were selected as the study objects. All boys received redundant circumcision treatment, their protein expression of TLR4 and MyD88 in foreskin tissues was measured by BCA protein assay and western blot, and mometasone furoate cream was applied to those who were pathologically diagnosed with LSeA, so as to compare the levels of serum inflammatory factors and urodynamic indicators in the child patients before and after treatment.
RESULTS
The total clinical efficacy rate of LSeA child patients was up to 90.79%; after treatment, the maximum and mean urinary flow rates of child patients were significantly higher than before treatment ( < 0.001); compared with the non-LSeA group, the protein expression of TLR4, MyD88, and NF-B was increased in the LSeA group ( < 0.001), and the mRNA expression of TLR4, MyD88, and NF-B was significantly increased in the LSeA group ( < 0.001); the results of ROC curves showed that TLR4 had the highest AUC value, and during treatment, the incidence rate of adverse reactions in child patients was 6.58%.
CONCLUSION
LSeA will increase the inflammatory reactions in child patients, and its pathogenesis may be related to the upregulation of TLR4, MyD88, NF-B expression and thus activation of TLR4/MyD88/NF-B signaling pathways. Applying mometasone furoate cream to LSeA patients after redundant circumcision can effectively reduce the inflammatory reactions in the body and improve their urodynamic indicators, with exact efficacy. Further research will be conducive to establishing a better treatment scheme for such child patients.
Topics: Child; Genitalia; Humans; Inflammation; Lichen Sclerosus et Atrophicus; Male; Mometasone Furoate; Myeloid Differentiation Factor 88; NF-kappa B; Toll-Like Receptor 4
PubMed: 35399843
DOI: 10.1155/2022/3495099 -
Iranian Journal of Otorhinolaryngology Mar 2024Adenoid hypertrophy is a common childhood disease; its standard treatment is adenoidectomy. The desire for medical management is increasing due to fewer complications...
INTRODUCTION
Adenoid hypertrophy is a common childhood disease; its standard treatment is adenoidectomy. The desire for medical management is increasing due to fewer complications and more convenience. The present study investigated the effect of adding oral montelukast to mometasone nasal spray in treating adenoid hypertrophy.
MATERIALS AND METHODS
This was a randomized, double-blind, placebo-controlled study conducted at a referral teaching hospital (Tehran, Iran) from September 2020 to September 2021. Children aged 2 to 14 years with clinical and radiological findings of adenoid hypertrophy were enrolled. Patients were randomly divided into two groups: mometasone nasal spray with oral montelukast (case group) or mometasone with placebo (control group). Then, the clinical scores were compared before and two months after the intervention.
RESULTS
Ninety-six patients completed the study [62.5% male (n=60)]. Of these, 51 were in the case and 45 in the control group. The clinical score in each group decreased significantly after the intervention (P<0.001), but the decrease in clinical score in the case group was not significantly different from the control (p=0.576).
CONCLUSION
The results showed that the combination therapy with mometasone and montelukast has the same efficacy as mometasone and placebo in treating adenoid hypertrophy. Adding montelukast to mometasone has no additional effect.
PubMed: 38476566
DOI: 10.22038/IJORL.2024.73906.3490 -
Journal of Pharmacy & Bioallied Sciences Apr 2024Dermoscopy particularly could be helpful in patients with steroid damaged face to assess and look for the damage caused by the steroid creams as also in cases where the...
BACKGROUND AND OBJECTIVES
Dermoscopy particularly could be helpful in patients with steroid damaged face to assess and look for the damage caused by the steroid creams as also in cases where the patient provides improper history.
MATERIALS AND METHODS
Patients attending to dermatology OPD with suspected/diagnosed TSDF between the ages of 18 and 60 years were enrolled and assessed on the basis of age, gender, residence, duration, potency, brand of application topical steroid creams, clinical and dermoscopic features.
RESULTS
Majority abusing the topical steroid creams were females (n-14) with mean age with SD of 34 ± 11 and were from rural areas (57.8%). Red raised lesions were the most common clinical presentation (n-15) with telangiectasias as the most common dermoscopic feature (n-26). Triple combination creams containing hydroquinone 2%, tretinoin 0.025%, and 0.1% mometasone were on the top of the list (n-20).
CONCLUSION
In this study, the importance of dermoscopy in assessing the features of topical steroid damaged face and preventing further damage is highlighted. Various factors causing topical steroid creams misuse and the easy availability of the creams is to be kept on check.
PubMed: 38882848
DOI: 10.4103/jpbs.jpbs_1191_23 -
Journal of Medical Virology Feb 2021
Topics: Administration, Inhalation; Anti-Inflammatory Agents; Beclomethasone; Clinical Trials as Topic; Humans; Lung; Mometasone Furoate; COVID-19 Drug Treatment
PubMed: 32776550
DOI: 10.1002/jmv.26413 -
Respiratory Medicine 2021To evaluate cardiovascular safety of two new inhaled fixed-dose combinations for treatment of asthma: (i) the inhaled corticosteroid/long-acting beta2-agonist (ICS/LABA)...
OBJECTIVE
To evaluate cardiovascular safety of two new inhaled fixed-dose combinations for treatment of asthma: (i) the inhaled corticosteroid/long-acting beta2-agonist (ICS/LABA) mometasone furoate/indacaterol acetate (MF/IND), (ii) the ICS/LABA/long-acting muscarinic antagonist (LAMA) MF/IND/glycopyrronium bromide (GLY).
METHODS
Patient-level data were pooled from four randomized trials, including 52-week studies PALLADIUM (n = 2216) and IRIDIUM (n = 3092), 24-week study ARGON (n = 1426), and 12-week study QUARTZ (n = 802). Cardio-/cerebrovascular (CCV) event frequencies were examined in the following comparisons: (1) LABA effect: pooled-dose MF/IND vs. pooled-dose MF; (2) LAMA effect: pooled-dose MF/IND/GLY vs. pooled-dose MF/IND; (3) ICS-dose effects: (a) high-dose MF/IND vs. medium-dose MF/IND, (b) high-dose MF/IND/GLY vs. medium-dose MF/IND/GLY; (4) intra-class effects: (a) high-dose MF/IND vs. Fluticasone/Salmeterol (F/S), (b) high-dose MF/IND/GLY vs. F/S + Tiotropium (TIO). Risk estimates (percentage of patients with ≥1 CCV event) and risk differences (RDs) with 95% confidence intervals (CIs) were calculated for each comparison.
RESULTS
The frequency of CCV events was low, without notable differences between comparison groups. Risk estimates and corresponding RDs (95% CIs) were as follows: (1) pooled-dose MF/IND = 2.35%, pooled-dose MF = 2.18%, RD = 0.17% (-1.00%, 1.34%); (2) pooled-dose MF/IND/GLY = 3.65%, pooled-dose MF/IND = 3.77%, RD = -0.12% (-1.63%, 1.39%); (3a) high-dose MF/IND = 3.69%, medium-dose MF/IND = 3.35%, RD = 0.34% (-1.25%, 1.94%); (3b) high-dose MF/IND/GLY = 2.84%, medium-dose MF/IND/GLY = 2.02%, RD = 0.82% (-0.49%, 2.13%); (4a) high-dose MF/IND = 3.69%, F/S = 2.82%, RD = 0.87% (-0.66%, 2.40%); (4b) high-dose MF/IND/GLY = 1.26%, F/S + TIO = 1.05%, RD = 0.21% (-1.26%, 1.68%).
CONCLUSIONS
There was no evidence of increased cardiovascular risk attributable to the addition of IND to MF or addition of GLY to MF/IND. Similarly, no evidence of increased cardiovascular risk was observed with an increase in the ICS-dose or relative to F/S ± TIO.
Topics: Administration, Inhalation; Adolescent; Adrenergic beta-2 Receptor Agonists; Adult; Aged; Aged, 80 and over; Asthma; Child; Clinical Trials, Phase III as Topic; Drug Therapy, Combination; Female; Glycopyrrolate; Heart Disease Risk Factors; Humans; Indans; Male; Middle Aged; Mometasone Furoate; Quinolones; Randomized Controlled Trials as Topic; Safety; Treatment Outcome; Young Adult
PubMed: 33711782
DOI: 10.1016/j.rmed.2021.106311