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The Laryngoscope Mar 2024Oxymetazoline relieves nasal obstructive symptoms via vasoconstriction, however, the changes in nasal structures and aerodynamics that impact symptoms the most remain...
OBJECTIVES
Oxymetazoline relieves nasal obstructive symptoms via vasoconstriction, however, the changes in nasal structures and aerodynamics that impact symptoms the most remain unclear.
METHODS
This prospective, longitudinal, and single blinded cohort study applied Computational Fluid Dynamic (CFD) modeling based on CT scans at baseline and post-oxymetazoline on 13 consecutive patients with chronic nasal obstruction secondary to inferior turbinate hypertrophy from a tertiary medical center. To account for placebo effect, a sham saline spray was administered with subject blindfolded prior to oxymetazoline, with 30 min rest in between. Nasal Obstruction Symptom Evaluation (NOSE) and unilateral Visual Analogue Scale (VAS) scores of nasal obstructions were collected at baseline, after sham, and 30 min after oxymetazoline.
RESULTS
Both VAS and NOSE scores significantly improved from baseline to post-oxymetazoline (NOSE: 62.3 ± 12.4 to 31.5 ± 22.5, p < 0.01; VAS: 5.27 ± 2.63 to 3.85 ± 2.59, p < 0.05), but not significantly from baseline to post-sham. The anatomical effects of oxymetazoline were observed broadly throughout the entire length of the inferior and middle turbinates (p < 0.05). Among many variables that changed significantly post-oxymetazoline, only decreased nasal resistance (spearman r = 0.4, p < 0.05), increased regional flow rates (r = -0.3 to -0.5, p < 0.05) and mucosal cooling heat flux (r = -0.42, p < 0.01) in the inferior but not middle turbinate regions, and nasal valve Wall Shear Stress (WSS r = -0.43, p < 0.05) strongly correlated with symptom improvement.
CONCLUSION
Oxymetazoline broadly affects the inferior and middle turbinates, however, symptomatic improvement appears to be driven more by global nasal resistance and regional increases in airflow rate, mucosal cooling, and WSS, especially near the head of the inferior turbinate.
LEVEL OF EVIDENCE
3: Well-designed, prospective, single blinded cohort trial. Laryngoscope, 134:1100-1106, 2024.
Topics: Humans; Oxymetazoline; Turbinates; Nasal Obstruction; Prospective Studies; Cohort Studies; Hypertrophy; Paranasal Sinus Diseases
PubMed: 37589314
DOI: 10.1002/lary.30968 -
Clinical Pharmacokinetics Sep 2023Nasal esketamine is indicated for the treatment of adults with treatment-resistant depression and depressive symptoms in adults with major depressive disorder with acute... (Clinical Trial)
Clinical Trial
Pharmacokinetics of Nasal Esketamine in Patients with Allergic Rhinitis with and Without Nasal Decongestant Pretreatment and in Healthy Subjects with and Without Nasal Corticosteroid Pretreatment.
BACKGROUND AND OBJECTIVES
Nasal esketamine is indicated for the treatment of adults with treatment-resistant depression and depressive symptoms in adults with major depressive disorder with acute suicidal ideation or behavior. Primary objectives of this study were to evaluate the effect of nasal decongestant pretreatment in patients with allergic rhinitis and the impact of daily nasal corticosteroid administration by healthy subjects on nasal esketamine pharmacokinetics.
METHODS
Patients with allergic rhinitis self-administered 56 mg of nasal esketamine after pretreatment with nasal oxymetazoline (0.05%) at 1 h before esketamine and without oxymetazoline pretreatment. They were exposed to grass pollen in an allergen challenge chamber to induce allergic rhinitis symptoms at approximately 2 h before each esketamine administration until 1 h after. Healthy subjects self-administered esketamine (56 mg) before and after administration for 16 consecutive days of mometasone (200 µg), with the second esketamine dose administered 1 h after the last mometasone dose. The plasma pharmacokinetics of esketamine and noresketamine were assessed after each esketamine administration. The tolerability of esketamine, including effects on dissociative and potential psychotomimetic symptoms and level of sedation and suicidal ideation and behavior, was evaluated.
RESULTS
The rate of esketamine absorption was slightly greater in patients exhibiting symptoms of allergic rhinitis (decrease in median t from 32 min to 22 min). Increases in esketamine C and AUC were also small (mean, ≤ 21%). The pharmacokinetics of esketamine was not affected by oxymetazoline or mometasone pretreatment. Esketamine was well tolerated when it was administered with or without pretreatment of oxymetazoline or mometasone.
CONCLUSIONS
Patients exhibiting symptoms of rhinitis may receive nasal esketamine spray without dose adjustment. In addition, esketamine may be administered 1 h after using a nasal decongestant or corticosteroid.
TRIAL REGISTRATION
The study was registered in the Clinical Trials (NCT02154334) and EudraCT (2014-000534-38) registries.
Topics: Adult; Humans; Administration, Intranasal; Adrenal Cortex Hormones; Depressive Disorder, Major; Double-Blind Method; Healthy Volunteers; Mometasone Furoate; Nasal Decongestants; Nasal Sprays; Oxymetazoline; Rhinitis, Allergic
PubMed: 37402024
DOI: 10.1007/s40262-023-01273-z -
Nature Communications Jun 2023The αadrenergic receptor (αAR) belongs to the family of G protein-coupled receptors that respond to adrenaline and noradrenaline. αAR is involved in smooth muscle...
The αadrenergic receptor (αAR) belongs to the family of G protein-coupled receptors that respond to adrenaline and noradrenaline. αAR is involved in smooth muscle contraction and cognitive function. Here, we present three cryo-electron microscopy structures of human αAR bound to the endogenous agonist noradrenaline, its selective agonist oxymetazoline, and the antagonist tamsulosin, with resolutions range from 2.9 Å to 3.5 Å. Our active and inactive αAR structures reveal the activation mechanism and distinct ligand binding modes for noradrenaline compared with other adrenergic receptor subtypes. In addition, we identified a nanobody that preferentially binds to the extracellular vestibule of αAR when bound to the selective agonist oxymetazoline. These results should facilitate the design of more selective therapeutic drugs targeting both orthosteric and allosteric sites in this receptor family.
Topics: Humans; Oxymetazoline; Cryoelectron Microscopy; Receptors, Adrenergic, alpha-1; Norepinephrine; Tamsulosin
PubMed: 37339967
DOI: 10.1038/s41467-023-39310-x -
Journal of Cosmetic Dermatology Sep 2023Since there is currently no conclusion on the efficacy and adverse effects of oxymetazoline, this meta-analysis attempts to explore its efficacy and adverse events, so... (Meta-Analysis)
Meta-Analysis Review
BACKGROUND
Since there is currently no conclusion on the efficacy and adverse effects of oxymetazoline, this meta-analysis attempts to explore its efficacy and adverse events, so as to provide guidance for clinical medication.
METHODS
We searched PubMed, Embase, and Cochrane Library from the establishment of the database to May 2021. We included studies that patients were randomly assigned to receive oxymetazoline or vehicle, and we excluded duplicate publications, research without full text, incomplete information or inability to conduct data extraction, animal experiments, reviews, and systematic reviews. STATA 15.1 was used to analyze the data.
RESULTS
The pooled results show that the 3 (RR = 1.76, 95% CI: 1.53-2.03), 6 (RR = 1.71, 95% CI: 1.47-2.00), 9 (RR = 1.63, 95% CI: 1.40-1.90), 12 (RR = 1.41, 95% CI: 1.18-1.67) -hours CEA success rate and the 3 (RR = 1.65, 95% CI: 1.34-2.03), 6 (RR = 1.75, 95% CI: 1.43-2.14), 9 (RR = 1.63, 95% CI: 1.33-2.00), 12 (RR = 1.78, 95% CI: 1.45-2.18) -hours SSA success rate after oxymetazoline treatment for rosacea is significantly higher than that of vehicle. Additionally, the pooled results show that the incidence of TEAEs after treatment with oxymetazoline is significantly higher than that of vehicle (RR = 1.34, 95% CI: 1.10-1.2). However, our analysis of specific adverse events found that the oxymetazoline group was only significantly higher than the vehicle group in the incidence of application-site dermatitis (RR = 8.91, 95% CI: 1.76-45.23), and there was no statistical significance in the difference in the incidence of other adverse events.
CONCLUSION
Oxymetazoline is effective and can be selected for the treatment of persistent facial erythema of rosacea. Additionally, application-site dermatitis was the most important one.
Topics: Humans; Oxymetazoline; Treatment Outcome; Skin Cream; Rosacea; Dermatitis; Randomized Controlled Trials as Topic
PubMed: 37128814
DOI: 10.1111/jocd.15747 -
Cureus Mar 2023In this article, we described two patients with myasthenia gravis-related ptosis who experienced sustained improvement with the use of oxymetazoline hydrochloride...
In this article, we described two patients with myasthenia gravis-related ptosis who experienced sustained improvement with the use of oxymetazoline hydrochloride ophthalmic solution 0.1%. Despite the commonly used treatments for ptosis in myasthenia gravis (MG), such as acetylcholinesterase inhibitors and corticosteroids, complete remission of ptosis is not always achieved, and these treatments are often accompanied by systemic side effects. Our case report suggests the long-term efficacy of daily use of oxymetazoline eye drops in improving ptosis, providing a potential alternative or adjunctive treatment option without significant adverse effects. Further research is necessary to confirm these observations across larger cohorts of MG patients and establish the effectiveness of oxymetazoline eye drops in MG-related ptosis.
PubMed: 37082493
DOI: 10.7759/cureus.36351 -
Journal of Plastic, Reconstructive &... May 2023This study assesses the effects of topical oxymetazoline 0.1% on eyelid position, eye redness, and patient-perceived eye appearance in patients without severe ptosis. (Randomized Controlled Trial)
Randomized Controlled Trial
PURPOSE
This study assesses the effects of topical oxymetazoline 0.1% on eyelid position, eye redness, and patient-perceived eye appearance in patients without severe ptosis.
METHODS
This is a randomized double-blinded controlled trial conducted at a single institute. Patients aged 18-100 years were randomized to receive one drop of oxymetazoline hydrochloride 0.1% or placebo bilaterally. Marginal reflex distance (MRD) 1 and 2, palpebral fissure height, eye redness, and patient-perceived eye appearance were assessed at baseline and two hours after drop instillation. Primary outcome measures included the change in MRD1, MRD2, and palpebral fissure height. Secondary outcome measures included changes in eye redness and patient-perceived eye appearance after drop instillation.
RESULTS
In total, 114 patients were included, 57 treatment patients (mean age 36.4 ± 12.7 years, 31.6% male) and 57 controls (mean age 31.3 ± 10.1 years, 33.3% male). Baseline mean MRD1, MRD2, and palpebral fissure were similar between groups (p = 0.24, 0.45, and 0.23, respectively). Changes in MRD1 and eye redness in the treatment group were significantly greater than those in the control group (0.9 ± 0.9 mm vs. - 0.3 ± 0.4 mm, p < 0.001; - 2.6 ± 4.4 vs. - 0.5 ± 2.3, p = 0.002, respectively). Patient-perceived eye appearance was significantly improved in the treatment group compared to the controls (p = 0.002), with more treatment group patients also reporting increased eye size and decreased eye redness (p = 0.008, p = 0.003, respectively). There were 9 treatment-emergent adverse events (TEAEs) in 7 treatment group patients and 5 TEAEs in 5 control patients (p = 0.25), all of which were mild in severity.
CONCLUSIONS
Topical oxymetazoline 0.1% increases MRD1 and palpebral fissure height, decreases eye redness, and improves patient-perceived eye appearance.
Topics: Humans; Male; Young Adult; Adult; Middle Aged; Female; Oxymetazoline; Eyelids; Blepharoptosis; Patient Reported Outcome Measures
PubMed: 36996503
DOI: 10.1016/j.bjps.2023.02.006 -
Aesthetic Surgery Journal Aug 2023
Topics: Humans; Blepharoptosis; Oxymetazoline; Clostridium botulinum; Botulinum Toxins, Type A; Neuromuscular Agents
PubMed: 36978211
DOI: 10.1093/asj/sjad076