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The Annals of Otology, Rhinology, and... May 2016Determine if the middle ear (ME) trans-mucosal nitrous oxide (N2O) gas exchange rate can be pharmacologically modulated by the nasal application of a vasoconstrictor. (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVE
Determine if the middle ear (ME) trans-mucosal nitrous oxide (N2O) gas exchange rate can be pharmacologically modulated by the nasal application of a vasoconstrictor.
METHODS
In a randomized, double-blind, crossover study, 20 adults received a nasal spray challenge containing either oxymetazoline or saline (placebo). At each session, subjects were fitted with a non-rebreathing mask and breathed room air for 20 minutes, 50% N2O:50% O2 for 20 minutes, and 100% O2 for 10 minutes. Throughout, heart rate, blood pressure (BP), and blood O2 saturation were monitored, and bilateral ME pressure was recorded by tympanometry every minute. The primary outcome measure was the slope of the ME pressure-time function for the experimental period, a direct measure of the transMEM N2O exchange constant. The effects of treatment, session, and period on the measured vital signs and of treatment, session, disease history, and ear on the ME pressure-time slopes were evaluated for statistical significance using repeated measures ANOVAs.
RESULTS
The analysis documented a significant effect of period on O2 saturation (N2O > room air, P = .03) and of treatment on blood pressure (oxymetazoline > placebo, P < .02) and the ME pressure-time slope (placebo > oxymetazoline, P = .05).
CONCLUSION
The exchange rate across the ME mucosa of inert gases can be decreased by topical treatment of the nasal mucosa with oxymetazoline.
Topics: Acoustic Impedance Tests; Administration, Intranasal; Administration, Topical; Adult; Cross-Over Studies; Double-Blind Method; Ear, Middle; Female; Follow-Up Studies; Humans; Male; Nasal Decongestants; Nasal Mucosa; Nitrous Oxide; Oxymetazoline; Pressure; Reference Values; Time Factors
PubMed: 26611245
DOI: 10.1177/0003489415617776 -
The Journal of Allergy and Clinical... Apr 2011In clinical trials, only about 60% of subjects report an excellent response to intranasal steroids, suggesting a need to add therapies to intranasal steroids to provide... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
In clinical trials, only about 60% of subjects report an excellent response to intranasal steroids, suggesting a need to add therapies to intranasal steroids to provide additional efficacy.
OBJECTIVE
To determine whether the combination of fluticasone furoate and oxymetazoline is more efficacious than either agent alone, and to determine whether rhinitis medicamentosa develops after treatment.
METHODS
We performed a double-blind, double-dummy, randomized, placebo-controlled parallel study. Sixty patients with perennial allergy were randomized to 4 weeks of once-a-night treatment with fluticasone furoate, oxymetazoline hydrochloride, the combination, or placebo. They were monitored during treatment and for 2 weeks posttreatment.
RESULTS
The total nasal symptom score over the 4 weeks of treatment was lower with the combination (median, 143; range, 30-316) compared with treatment with placebo (262; 116-358) and oxymetazoline alone (219; 78-385; ANOVA, P = .04). When acoustic rhinometry was compared between the groups at the end of 4 weeks of treatment, the combination resulted in significantly higher nasal volume (mean + SEM, 15.8 + 1.1 mL; P< .03) compared with both placebo (12.1 + 0.9 mL) and oxymetazoline (12.4 + 0.8 mL) alone. The quality of life data showed no significant differences among the groups. Peak flow showed a nonsignificant improvement with the groups on fluticasone furoate. There was no evidence of rhinitis medicamentosa.
CONCLUSION
The addition of oxymetazoline adds to the effectiveness of fluticasone furoate in the treatment of perennial allergic rhinitis. The lack of development of rhinitis medicamentosa suggests the need for a large multicenter study to develop a once-a-day combination of an intranasal steroid and a long-acting topical decongestant.
Topics: Administration, Intranasal; Adult; Androstadienes; Anti-Inflammatory Agents; Double-Blind Method; Drug Therapy, Combination; Female; Humans; Male; Nasal Decongestants; Oxymetazoline; Rhinitis, Allergic, Perennial
PubMed: 21377716
DOI: 10.1016/j.jaci.2011.01.037 -
Aesthetic Surgery Journal May 2022Oxymetazoline hydrochloride 0.1% ophthalmic solution has recently been approved in the United States for the treatment of ptosis.
BACKGROUND
Oxymetazoline hydrochloride 0.1% ophthalmic solution has recently been approved in the United States for the treatment of ptosis.
OBJECTIVES
The aim of this study was to assess the upper and lower eyelid position as well as the brow position and the color of the sclera following the ophthalmic administration of oxymetazoline hydrochloride 0.1%.
METHODS
In this prospective cohort study, consecutive patients presenting with ptosis received topical oxymetazoline 0.1%. The primary outcome was measurement of the upper eyelid height (margin-to-reflex distance 1 [MRD1]) and lower eyelid height (MRD2) relative to the center of pupil, along with assessment of brow height, measured on photographs at baseline and 2 hours after instillation of oxymetazoline. The secondary outcome was the assessment of the color of the sclera (eye whiteness) before and after treatment with a novel color space algorithm.
RESULTS
Twenty-nine patients participated in the study. The mean [SD] MRD1 at baseline was 2.3 [0.6] mm. At 2 hours following oxymetazoline treatment, the mean MRD1 significantly increased to 4.2 [0.9] mm (P < 0.01). The mean MRD2 also significantly increased from 5.3 [0.9] mm to 5.7 [1.0] mm (P < 0.01). Brow position did not change with treatment (P = 0.4). Following treatment, the eye sclera became significantly whiter, with a mean ΔEab (color change) of 9.7 [3.9], with 57 out of 58 eyes experiencing a significant change in color. A change of ΔEab ≥2 is considered visually perceptible to the human eye.
CONCLUSIONS
Within 2 hours of use, oxymetazoline significantly improves the size of the palpebral aperture (MRD1 + MRD2) and also makes the eye appear significantly whiter.
Topics: Blepharoptosis; Esthetics; Eyelids; Humans; Oxymetazoline; Prospective Studies
PubMed: 34962512
DOI: 10.1093/asj/sjab400 -
Current Molecular Pharmacology Oct 2021Rhinitis medicamentosa, also known as 'rebound congestion,' is inflammation of the nasal mucosa caused by the overuse of topical nasal decongestants. Although local...
BACKGROUND
Rhinitis medicamentosa, also known as 'rebound congestion,' is inflammation of the nasal mucosa caused by the overuse of topical nasal decongestants. Although local decongestants resolve the initial nasal obstruction, the overuse causes rebound obstruction. However, how the overuse of the decongestant causes rhinitis medicamentosa is not known.
OBJECTIVES
Here, we show the intracellular effects of oxymetazoline, commonly used a local decongestant, on the cell death pathways. We also investigated the antioxidative effects of erdosteine suspension (175 mg/5mL), an antioxidative agent.
METHODS
Thirty Wistar-albino rats were used to form the rhinitis medicamentosa model. After rhinitis medicamentosa was clinically detected, we removed the whole lungs of animals to perform the molecular analyses of cell death pathways.
RESULTS
We found a statistically significant decrease in the expression levels of Atg5 (p=0.021), Atg7 (p=0.013) and Ulk1 (p=0.036) in the oxymetazoline group compared to the control group (p<0.05); however, Caspase 3 expression level was recorded to be significantly increased in the oxymetazoline group, and the expression level of Beclin1 recorded to be substantially increased in the erdosteine group (p=0.001).
CONCLUSION
Based on these grounds, we suggest that vasoconstriction in capillary vessels caused by oxymetazoline could lead to a decrease in the blood supply, which triggers autophagy to ensure cellular homeostasis.
Topics: Animals; Lung; Nasal Decongestants; Oxymetazoline; Rats; Rats, Wistar; Rhinitis
PubMed: 32718303
DOI: 10.2174/1874467213666200727124105 -
Optometry and Vision Science : Official... Nov 2021Ptosis is often the hallmark finding in ocular and general myasthenia gravis. Reduction of ptosis has been achieved with oral and topical ocular medications. However,...
SIGNIFICANCE
Ptosis is often the hallmark finding in ocular and general myasthenia gravis. Reduction of ptosis has been achieved with oral and topical ocular medications. However, these medications can result in systemic and ocular adverse effects. A novel eye drop seems to be effective in reducing ptosis while minimizing adverse effects.
PURPOSE
This case report aimed to demonstrate the efficacy of topical oxymetazoline hydrochloride 0.1%, an α-adrenergic agonist, in temporary elimination of ptosis associated with myasthenia gravis.
CASE REPORT
A 68-year-old woman with a history of myasthenia gravis and long-standing ptosis in the right eye presented to improve the asymmetrical appearance of her eyelids. One drop of oxymetazoline hydrochloride 0.1% was instilled in the right eye of the patient. Within 2 hours, the ptosis was eliminated, the margin-reflex distance 1 increased by 2.0 mm, and the superior visual field measured by a superior 36-point screening test increased by 15 points. The effect lasted for at least 7 hours. Of note, there was a decrease in elevation of the contralateral nonptotic eyelid that did not receive a drop of oxymetazoline, which might occur only in myasthenia gravis. Further evaluation is warranted.
CONCLUSIONS
Oxymetazoline 0.1% is effective in reducing and potentially eliminating ptosis related to ocular myasthenia gravis for up to 7 hours.
Topics: Aged; Blepharoptosis; Eyelids; Female; Humans; Myasthenia Gravis; Oxymetazoline; Visual Fields
PubMed: 34510144
DOI: 10.1097/OPX.0000000000001800 -
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 -
The Journal of International Medical... 1979In a double-blind study of 141 patients, 0.025% oxymetazoline ophthalmic solution was compared with its vehicle in the treatment of allergic and non-infectious... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
In a double-blind study of 141 patients, 0.025% oxymetazoline ophthalmic solution was compared with its vehicle in the treatment of allergic and non-infectious conjunctivitis. There was a marked difference in response at the first evaluation. By the tenth day (second evaluation) the total improvement in hyperaemia was 95% for oxymetazoline compared to 54% for the placebo. Oxymetazoline's decongestant effect in the eye matches its effect as a nasal vasoconstrictor.
Topics: Adolescent; Adult; Aged; Clinical Trials as Topic; Conjunctivitis; Double-Blind Method; Female; Humans; Imidazoles; Male; Middle Aged; Ophthalmic Solutions; Oxymetazoline; Placebos; Rhinitis, Allergic, Seasonal; Vasoconstrictor Agents
PubMed: 391626
DOI: 10.1177/030006057900700609 -
Current Therapeutic Research, Clinical... Mar 1966
Topics: Adolescent; Adult; Child; Female; Humans; Male; Middle Aged; Nose Diseases; Oxymetazoline; Respiratory Tract Infections; Sympathomimetics
PubMed: 4956581
DOI: No ID Found -
Journal of Drugs in Dermatology : JDD Nov 2018Background: Rosacea is a chronic dermatologic condition with limited treatment options. Methods: Data were pooled from two identically designed phase 3 trials. Patients... (Randomized Controlled Trial)
Randomized Controlled Trial
Background: Rosacea is a chronic dermatologic condition with limited treatment options. Methods: Data were pooled from two identically designed phase 3 trials. Patients with moderate to severe persistent erythema of rosacea were randomized to receive oxymetazoline cream 1.0% or vehicle once daily for 29 days and were followed for 28 days posttreatment. The primary efficacy outcome was the proportion of patients with ≥2-grade improvement from baseline on both Clinician Erythema Assessment (CEA) and Subject Self-Assessment (SSA) at 3, 6, 9, and 12 hours postdose, day 29. Results: The pooled population included 885 patients (78.8% female); 85.8% and 91.2% had moderate erythema based on CEA and SSA, respectively. The primary outcome was achieved by significantly more patients in the oxymetazoline than vehicle group (P<0.001). Individual CEA and SSA scores and reduction in facial erythema (digital image analysis) favored oxymetazoline over vehicle (P<0.001). The incidence of treatment-emergent adverse events was low (oxymetazoline, 16.4%; vehicle, 11.8%). No clinically relevant erythema worsening (based on CEA and SSA) was observed during the 28-day posttreatment follow-up period (oxymetazoline, 1.7%; vehicle, 0.6%). Conclusion: Oxymetazoline effectively reduced moderate to severe persistent facial erythema of rosacea and was well tolerated. J Drugs Dermatol. 2018;17(11):1201-1208.
Topics: Adult; Erythema; Female; Humans; Male; Oxymetazoline; Rosacea; Self-Assessment; Severity of Illness Index; Skin Cream; Sympathomimetics; Treatment Outcome; Young Adult
PubMed: 30500142
DOI: No ID Found -
Lasers in Surgery and Medicine Dec 2021We evaluated if oxymetazoline therapy combined with 595-nm pulsed dye laser (PDL) will be more beneficial than topical oxymetazoline alone for the improvement of... (Randomized Controlled Trial)
Randomized Controlled Trial
A Randomized Controlled Pilot Study: Combined 595-nm Pulsed Dye Laser Treatment and Oxymetazoline Hydrochloride Topical Cream Superior to Oxymetazoline Hydrochloride Cream for Erythematotelangiectatic Rosacea.
BACKGROUND AND OBJECTIVES
We evaluated if oxymetazoline therapy combined with 595-nm pulsed dye laser (PDL) will be more beneficial than topical oxymetazoline alone for the improvement of erythematotelangiectatic rosacea.
STUDY DESIGN/MATERIALS AND METHODS
This was a randomized, controlled, prospective clinical trial approved by an independent Institutional Review Board, which enrolled 34 patients with moderate to severe clinical erythema (CEA) into a two-arm study of PDL with concomitant oxymetazoline cream (Arm 1) and oxymetazoline cream alone (Arm 2). Patients in Arm 1 were treated with 3 monthly laser sessions, which were started after 1 month of topical oxymetazoline cream. Thirty subjects continued with the study, and 25 subjects (Arm 1: 14, Arm 2: 11) completed the 6-month follow-up. With photographic comparison to baseline images, efficacy endpoints were based on clinical on-site grading by both the investigator and the patient, using the grading tools for CEA, Global Aesthetic Improvement (GAI) assessment, vessel size improvement, and subject self-assessment. These scales were assessed at baseline and/or at each clinical follow-up at 1, 2, 3, and 6 months. Subject satisfaction as well as post-treatment immediate response and treatment-associated pain scores were also evaluated.
RESULTS
Statistically significant improvement in CEA was seen in both arms at the 1-, 2-, and 3-month post-baseline visits (P < 0.01). Only Arm 1 presented statistically significant improvement in CEA (P < 0.001) at 6 months post baseline with a mean score of 1.6 (almost clear-mild) compared with 3.2 at baseline. Arm 1 showed significantly greater mean vessel size improvement at 3 months (P < 0.01) and 6 months (P < 0.05) post baseline compared to Arm 2. Significantly greater improvement (P < 0.05) in the investigator GAI score was reported at the 2- and 6-month follow-ups compared with Arm 2. Subject GAI scores showed statistically significant greater improvement in Arm 1 compared with Arm 2 at both the 3- and 6-month follow-ups (P < 0.01). There were no complications or long-term effects associated with PDL or topical oxymetazoline treatments.
CONCLUSION
The prospective trial verifies a safe, enhanced clinical outcome with the combination of PDL therapy and topical oxymetazoline for the treatment of erythematotelangiectatic rosacea patients. Lasers Surg. Med. © 2021 The Authors. Lasers in Surgery and Medicine published by Wiley Periodicals LLC.
Topics: Humans; Lasers, Dye; Oxymetazoline; Pilot Projects; Prospective Studies; Rosacea; Skin Cream; Treatment Outcome
PubMed: 34233378
DOI: 10.1002/lsm.23439