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Dermatology and Therapy Dec 2023Rosacea is a chronic inflammatory disease with a multifactorial pathogenesis. The wide spectrum of clinical phenotypes, including erythema, telangiectasia, inflammatory... (Review)
Review
Rosacea is a chronic inflammatory disease with a multifactorial pathogenesis. The wide spectrum of clinical phenotypes, including erythema, telangiectasia, inflammatory papules and pustules, and phyma, demand an individualized approach to treatment. This narrative review offers an updated reference for rosacea management by covering the latest developments in both topical and systemic treatments, including data from newly approved therapies, updates to current treatment modalities and ongoing clinical trials. Although use of benzoyl peroxide as a treatment for rosacea has typically been limited due to irritation, the improved tolerability due to microencapsulation of benzoyl peroxide 5% cream provides a new therapeutic option for patients with rosacea. Minocycline foam and topical ivermectin cream add to our armamentarium of treatment options, particularly for inflammatory papules and pustules. Sarecycline has a narrower spectrum of antibacterial activity, which might reduce the development of antibiotic resistance and disruption of the microbiome compared to other oral antibiotics. Brimonidine gel and oxymetazoline cream provide topical options for redness and flushing. There is emerging evidence about the role of hydroxychloroquine and intradermal botulinum toxin A, which may improve rosacea through their effects on mast cells. The clinical trials pipeline includes agents with a variety of mechanisms, including mast cell stabilization, antimicrobial, anti-inflammatory, and vasoconstrictive effects. However, the clinical pipeline for rosacea appears limited, and there remain important unmet needs for patients with more recalcitrant rosacea or phymatous disease. In addition, there is a need for comparative effectiveness studies to identify the highest value treatment approaches for patients with rosacea.
PubMed: 37824060
DOI: 10.1007/s13555-023-01048-1 -
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 -
BMJ Clinical Evidence Jun 2008Each year, children suffer up to 5 colds and adults have 2-3 infections, leading to time off school or work, and considerable discomfort. Most symptoms resolve within a... (Review)
Review
INTRODUCTION
Each year, children suffer up to 5 colds and adults have 2-3 infections, leading to time off school or work, and considerable discomfort. Most symptoms resolve within a week, but coughs often persist for longer.
METHODS AND OUTCOMES
We conducted a systematic review and aimed to answer the following clinical question: What are the effects of treatments for common cold? We searched: Medline, Embase, The Cochrane Library and other important databases up to May 2007 (Clinical Evidence reviews are updated periodically, please check our website for the most up-to-date version of this review). We included harms alerts from relevant organisations such as the US Food and Drug Administration (FDA) and the UK Medicines and Healthcare products Regulatory Agency (MHRA).
RESULTS
We found 19 systematic reviews, RCTs, or observational studies that met our inclusion criteria. We performed a GRADE evaluation of the quality of evidence for interventions.
CONCLUSIONS
In this systematic review we present information relating to the effectiveness and safety of the following interventions: analgesics or anti-inflammatory drugs, antibiotics, antihistamines, decongestants (norephedrine, oxymetazoline, or pseudoephedrine), decongestants plus antihistamine, echinacea, steam inhalation, vitamin C, and zinc (intranasal gel or lozenges).
Topics: Acute Disease; Common Cold; Cough; Echinacea; Humans; Nasal Decongestants; Phenylpropanolamine
PubMed: 19450292
DOI: No ID Found -
Lasers in Surgery and Medicine Jan 2021The objectives of this study were to evaluate the safety, tolerability, and efficacy of oxymetazoline hydrochloride cream, 1% (oxymetazoline) when used as an adjunctive...
BACKGROUND AND OBJECTIVES
The objectives of this study were to evaluate the safety, tolerability, and efficacy of oxymetazoline hydrochloride cream, 1% (oxymetazoline) when used as an adjunctive treatment with energy-based therapy for patients with moderate to severe facial erythema associated with rosacea.
STUDY DESIGN/MATERIALS AND METHODS
In this Phase 4, multicenter, interventional, open-label study, eligible patients received one of four energy-based therapies (potassium titanyl phosphate laser, intense pulsed light therapy, pulsed-dye laser Vbeam Perfecta, or pulsed-dye laser Cynergy) on day 1 and day 29 and once-daily application of oxymetazoline on days 3 through 27 and days 31 through 56. Improvement from baseline in Clinician Erythema Assessment (CEA) score, patient satisfaction measures, incidence of treatment-emergent adverse events (TEAEs), and worsening from baseline on dermal tolerability assessments and the Clinician Telangiectasia Assessment (CTA) were assessed. Data were summarized using descriptive statistics.
RESULTS
A total of 46 patients (mean age, 51.1 years; 78.3% female) enrolled in this study. Similar numbers of patients received each of the energy-based therapies in addition to oxymetazoline. All patients demonstrated an improvement from baseline in CEA during the study with 39 of 43 evaluable patients (90.7%) demonstrating an improvement 6 hours posttreatment on day 56. Most patients were satisfied or very satisfied with treatment at the end of the study. All TEAEs were mild or moderate in severity. Some patients experienced worsening in dermal tolerability assessment symptoms (range: 4-21 patients; 8.7-45.7%). Worsening in CEA and CTA were each reported by three patients (6.5%) at any time during the study.
CONCLUSIONS
Treatment with oxymetazoline as adjunctive therapy with energy-based therapy was safe, well tolerated, and reduced facial erythema in patients with moderate to severe persistent facial erythema associated with rosacea. Lasers Surg. Med. © 2020 The Authors. Lasers in Surgery and Medicine published by Wiley Periodicals LLC.
Topics: Erythema; Female; Humans; Male; Middle Aged; Oxymetazoline; Rosacea; Skin Cream; Treatment Outcome
PubMed: 32378241
DOI: 10.1002/lsm.23253 -
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 -
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 -
Biochimica Et Biophysica Acta.... Dec 2017In LNCaP cells that stably express α-adrenergic receptors, oxymetazoline increased intracellular calcium and receptor phosphorylation, however, this agonist was a weak...
In LNCaP cells that stably express α-adrenergic receptors, oxymetazoline increased intracellular calcium and receptor phosphorylation, however, this agonist was a weak partial agonist, as compared to noradrenaline, for calcium signaling. Interestingly, oxymetazoline-induced receptor internalization and desensitization displayed greater effects than those induced by noradrenaline. Phorbol myristate acetate induced modest receptor internalization and minimal desensitization. α-Adrenergic receptor interaction with β-arrestins (colocalization/coimmunoprecipitation) was induced by noradrenaline and oxymetazoline and, to a lesser extent, by phorbol myristate acetate. Oxymetazoline was more potent and effective than noradrenaline in inducing ERK 1/2 phosphorylation. Mass spectrometric analysis of immunopurified α-adrenergic receptors from cells treated with adrenergic agonists and the phorbol ester clearly showed that phosphorylated residues were present both at the third intracellular loop and at the carboxyl tail. Distinct phosphorylation patterns were observed under the different conditions. The phosphorylated residues were: a) Baseline and all treatments: T233; b) noradrenaline: S220, S227, S229, S246, S250, S389; c) oxymetazoline: S227, S246, S381, T384, S389; and d) phorbol myristate acetate: S246, S250, S258, S351, S352, S401, S402, S407, T411, S413, T451. Our novel data, describing the α-AR phosphorylation sites, suggest that the observed different phosphorylation patterns may participate in defining adrenoceptor localization and action, under the different conditions examined.
Topics: Calcium Signaling; Cell Line, Tumor; Gene Expression Regulation, Neoplastic; Humans; MAP Kinase Signaling System; Mass Spectrometry; Norepinephrine; Oxymetazoline; Phosphorylation; Protein Kinase C; Proteolysis; Receptors, Adrenergic, alpha-1; Tetradecanoylphorbol Acetate
PubMed: 28888989
DOI: 10.1016/j.bbamcr.2017.09.002 -
Journal of Clinical Medicine Mar 2021Alpha-adrenergic agonists, such as the Imidazoline derivatives (ImDs) of oxymetazoline and xylometazoline, are highly effective hemostatic agents. ImDs have not been... (Review)
Review
Alpha-adrenergic agonists, such as the Imidazoline derivatives (ImDs) of oxymetazoline and xylometazoline, are highly effective hemostatic agents. ImDs have not been widely used in dentistry but their use in medicine, specifically in ophthalmology and otolaryngology, warrants consideration for pulpal hemostasis. This review presents dental healthcare professionals with an overview of ImDs in medicine. ImD solutions have the potential to be more effective and biocompatible than existing topical hemostatic compounds in pulpal management. Through a comprehensive analysis of the pharmacology of ImDs and the microphysiology of hemostasis regulation in oral tissues, a conceptual model of pulpal management by ImD solutions is presented.
PubMed: 33803990
DOI: 10.3390/jcm10061212 -
The Journal of Clinical and Aesthetic... Mar 2021Rosacea is a chronic, multisymptom, inflammatory condition that affects the centrofacial skin. Facial erythema associated with rosacea can negatively impact a patient's... (Review)
Review
Rosacea is a chronic, multisymptom, inflammatory condition that affects the centrofacial skin. Facial erythema associated with rosacea can negatively impact a patient's quality of life and is often hard to treat. We sought to review the literature on the role of alpha-adrenergic receptors (α-adrenoceptors) in the context of persistent facial erythema in patients with rosacea and the use of oxymetazoline hydrochloride cream 1% as a topical treatment. PubMed was searched; search terms included "alpha adrenoceptor," "oxymetazoline," and "rosacea." Additional articles were identified from the reference lists of the results. Some α-adrenoceptor agonists have vasoconstrictive properties and may be used topically to treat persistent facial erythema in rosacea. Oxymetazoline hydrochloride cream 1% is an α-adrenoceptor agonist approved for the treatment of persistent facial erythema associated with rosacea. Based on our review, we discuss the role of the α-adrenoceptor in persistent facial erythema; provide an overview of the mechanism of action of α-adrenoceptor agonists, such as oxymetazoline, in the treatment of persistent facial erythema; and summarize the clinical development and data to date demonstrating the efficacy and safety of oxymetazoline in the treatment of persistent facial erythema associated with rosacea. The review of available literature suggests that oxymetazoline cream is well-tolerated, safe, and effective for the treatment of persistent facial erythema in rosacea and is an important component of combination treatment regimens, which are likely to become the standard of treatment for rosacea in the future.
PubMed: 33841614
DOI: No ID Found