326 results match your criteria agonist oxymetazoline


Rapid and Sustained Eyelid Elevation in Acquired Blepharoptosis with Oxymetazoline 0.1%: Randomized Phase 3 Trial Results.

Clin Ophthalmol 2021 25;15:2743-2751. Epub 2021 Jun 25.

Department of Ophthalmology, University of South Florida Morsani College of Medicine, Tampa, FL, USA.

Purpose: Oxymetazoline 0.1% is a novel ophthalmic agent for the treatment of acquired blepharoptosis in adults that has been shown to improve upper eyelid elevation and superior visual field deficits. This analysis characterized the rapid onset of upper eyelid elevation with once-daily oxymetazoline 0. Read More

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Topical Oxymetazoline Hydrochloride Cream 1% for the Treatment of Persistent Facial Erythema of Rosacea in Adults: A Comprehensive Review of Current Evidence.

J Clin Aesthet Dermatol 2021 Mar 1;14(3):32-37. Epub 2021 Mar 1.

Dr. Del Rosso is Research Director at JDR Dermatology Research in Las Vegas, Nevada, is with Thomas Dermatology in Las Vegas, Nevada, and is an adjunct clinical professor of dermatology at Touro University Nevada in Henderson, Nevada.

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. Read More

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Update on the Management of Rosacea from the American Acne & Rosacea Society (AARS).

J Clin Aesthet Dermatol 2020 Jun 1;13(6 Suppl):17-24. Epub 2020 Jun 1.

Dr. Del Rosso is Adjunct Clinical Professor of Dermatology at Touro University, Nevada in Henderson, Nevada; and Research Director at JDR Dermatology Research, Clinical Dermatology, Thomas Dermatology in Las Vegas, Nevada.

Previous consensus articles on rosacea from the American Acne and Rosacea Society (AARS) have focused on pathophysiology, clinical assessment based on phenotypic expressions of rosacea, management guidelines, discussions of individual medical therapies, and reviews of physical modalities. Pathophysiologic mechanisms believed to be operative in rosacea have been covered extensively in the literature. This article updates the previously published consensus recommendations from the AARS on the management of rosacea, including systematic literature and evidence-based reviews of available therapeutic agents and physical modalities. Read More

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Involvement of the Hippocampal Alpha2A-Adrenoceptors in Anxiety-Related Behaviors Elicited by Intermittent REM Sleep Deprivation-Induced Stress in Mice.

Biol Pharm Bull 2020 ;43(8):1226-1234

Department of Pharmacology, Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University.

Attention deficit/hyperactivity disorder (AD/HD) is a neurodevelopmental disorder characterized by inattention, hyperactivity, and impulsivity. In patients with AD/HD, a decrease in the total and rapid eye movement (REM) sleep times has been observed. We have previously reported that mice with REM sleep deprivation-induced stress (REMSD) may show the hyperactivity- and inattention-like symptoms of AD/HD. Read More

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Successful treatment of the face post acne erythema using a topically applied selective alpha 1-Adrenergic receptor agonist, oxymetazoline 1.5%, a controlled left to right face comparative trial.

J Dermatolog Treat 2020 Jul 7:1-6. Epub 2020 Jul 7.

Clinical Pharmacy & Pharmacy Practice Department, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt.

Background: Post-inflammatory erythema (PIE) is a common sequalae of acne inflammation, persistent post acne erythema (PAE) is cosmetically unacceptable and sometimes its complete clearance could not be achieved. Oxymetazoline (OXZ) is a synthetic, direct-acting, sympathomimetic agonist that is highly selective for the 1α-adrenoceptor. It is a potent vasoconstrictor and well known for its ability to clinically 'get the red out'. Read More

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Glycogen Synthase Kinase-3 modulates α-adrenergic receptor action and regulation.

Eur J Cell Biol 2020 Apr 22;99(2-3):151072. Epub 2020 Feb 22.

Departamento de Biología Celular y Desarrollo, Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, Ciudad de México, Mexico. Electronic address:

The possibility that glycogen synthase kinase 3 (GSK3) could modulate α-adrenergic receptor (α-AR) function and regulation was tested employing LNCaP and HEK293 cells transfected to express the enhanced green fluorescent protein-tagged human α-AR. Receptor phosphorylation and internalization, intracellular free calcium, α-AR-GSK3 colocalization, and coimmunoprecipitation were studied. The effects of the pharmacological GSK3 inhibitor, SB-216763, and the coexpression of a dominant-negative mutant of this kinase, as well as the signaling, desensitization, and internalization of receptors with S229, S258, S352, and S381 substitutions for alanine or aspartate, were also determined. Read More

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Microvascular Effects of Pulsed Dye Laser in Combination With Oxymetazoline.

Lasers Surg Med 2020 01 22;52(1):17-22. Epub 2019 Nov 22.

Beckman Laser Institute and Medical Clinic, University of California, 1002 Health Sciences Rd, Irvine, California, 92617.

Background And Objective: Oxymetazoline, an α-1A agonist, is approved by the United States Food and Drug Administration (FDA) for treatment of persistent facial erythema associated with rosacea and induces vasoconstriction by interacting with α receptors. The objective of our study was to study the microvascular effects of oxymetazoline and pulsed dye laser (PDL).

Materials And Methods: A dorsal window chamber was surgically installed on 20 mice. Read More

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January 2020

Treatment of Erythematotelangiectatic Rosacea With Pulsed-Dye Laser and Oxymetazoline 1.0% Cream: A Retrospective Study.

Lasers Surg Med 2020 01 10;52(1):38-43. Epub 2019 Nov 10.

Dermatology & Laser Surgery Center, 6400 Fannin St Suite 2720, Houston, Texas, 77030.

Background And Objectives: Pulsed-dye laser (PDL) and oxymetazoline 1.0% cream are each used for the treatment of erythematotelangiectatic (ET) rosacea. PDL targets oxyhemoglobin and can reduce facial erythema and telangiectasias. Read More

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January 2020

Update on the Management of Rosacea from the American Acne & Rosacea Society (AARS).

J Clin Aesthet Dermatol 2019 Jun 1;12(6):17-24. Epub 2019 Jun 1.

Dr. Del Rosso is Adjunct Clinical Professor of Dermatology at Touro University, Nevada in Henderson, Nevada; and Research Director at JDR Dermatology Research, Clinical Dermatology, Thomas Dermatology in Las Vegas, Nevada.

Previous consensus articles on rosacea from the American Acne and Rosacea Society (AARS) have focused on pathophysiology, clinical assessment based on phenotypic expressions of rosacea, management guidelines, discussions of individual medical therapies, and reviews of physical modalities. Pathophysiologic mechanisms believed to be operative in rosacea have been covered extensively in the literature. This article updates the previously published consensus recommendations from the AARS on the management of rosacea, including systematic literature and evidence-based reviews of available therapeutic agents and physical modalities. Read More

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Functional activation of Gα protein via α -adrenoceptor in rat cerebral cortical membranes.

Clin Exp Pharmacol Physiol 2019 06 7;46(6):567-574. Epub 2019 Apr 7.

Department of Psychiatry, Faculty of Medicine, Saitama Medical University, Moroyama-machi, Iruma-gun, Saitama 350-0495, Japan.

Although it is recognized that α -adrenoceptors are coupled to diverse intracellular signalling pathways, its primary transduction mechanisms are evoked by activating phospholipase C in the cell membrane through Gα , resulting in production of inositol 1,4,5-trisphosphate and diacylglycerol. However, there have been few studies that indicate directly the involvement of Gα proteins in this signalling pathway in the central nervous system. In the current study, we tried to pharmacologically characterize (-)-adrenaline-stimulated [ S]GTPγS binding to Gα in rat brain membranes. Read More

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Hemodynamic and pharmacokinetic analysis of oxymetazoline use during nasal surgery in children.

Laryngoscope 2019 12 20;129(12):2775-2781. Epub 2019 Feb 20.

Department of Anesthesiology and Pain Medicine, Nationwide Children's Hospital, Columbus, Ohio, U.S.A.

Objectives/hypothesis: Oxymetazoline is an α-adrenergic agonist that is commonly used as a topical hemostatic agent in the operating room during ear, nose, and throat surgery. There are limited data on oxymetazoline pharmacokinetics in children who undergo general anesthesia. We assessed the hemodynamic effects and systemic absorption of topically applied oxymetazoline in children undergoing various nasal procedures. Read More

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December 2019

Clinical effectiveness of novel rosacea therapies.

Curr Opin Pharmacol 2019 06 11;46:14-18. Epub 2019 Jan 11.

Center for Dermatology Research, Department of Dermatology, Wake Forest School of Medicine, Winston-Salem, NC, United States.

Rosacea is a common inflammatory skin disease that is difficult to manage because of the unknown etiology and due to its variable manifestations. These facts and the few new available treatment options make it difficult to select a really effective treatment. This review aims to assess the efficacy and safety of novel treatment options for rosacea. Read More

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Topical Oxymetazoline for Fecal Incontinence in Patients with Spinal Cord Injury: A Double-Blind Randomized Controlled Crossover Study.

Dis Colon Rectum 2019 02;62(2):234-240

Semmelweis University, 1st Department of Internal Medicine, Budapest, Hungary.

Background: Topical α-agonists contract the internal anal sphincter muscle; therefore, they may serve as treatment for fecal incontinence.

Objectives: The aim of this study was to investigate the effect of the α-agonist oxymetazoline 1.0% on fecal incontinence in patients with spinal cord injury. Read More

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February 2019

Reduction in ultraviolet B light-induced erythema by oxymetazoline and brimonidine is mediated by different α-adrenoceptors.

Exp Dermatol 2018 07 10;27(7):763-768. Epub 2018 May 10.

Research, Allergan plc, Irvine, CA, USA.

When applied topically, oxymetazoline and brimonidine reduce the persistent facial erythema of rosacea; this effect is mediated by cutaneous vasoconstriction induced by postsynaptic activation of α-adrenoceptors. We investigated the α-adrenergic pharmacology of oxymetazoline and brimonidine. Functional activity on α-adrenoceptors was evaluated in vitro in HEK293 cells stably expressing single receptor subtypes using a fluorometric imaging plate reader Ca influx assay. Read More

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Pivotal Trial of the Efficacy and Safety of Oxymetazoline Cream 1.0% for the Treatment of Persistent Facial Erythema Associated With Rosacea: Findings from the Second REVEAL Trial.

J Drugs Dermatol 2018 Mar;17(3):290-298

Rosacea is a chronic dermatologic condition with limited treatment options, particularly for persistent erythema. This pivotal phase 3 study evaluated oxymetazoline, an a1A-adrenoceptor agonist, for the treatment of moderate to severe persistent erythema of rosacea. Eligible patients were randomly assigned 1:1 to receive oxymetazoline cream 1. Read More

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In Vitro Safety Pharmacology Profiling of Topical α-Adrenergic Agonist Treatments for Erythema of Rosacea.

Drugs R D 2018 Mar;18(1):87-90

Department of Physiology, Royal College of Surgeons in Ireland, Dublin, Ireland.

Background: Topical α-adrenergic agonist therapy has been developed to treat the persistent erythema of rosacea patients. Brimonidine and oxymetazoline are both topical α-adrenergic agonists.

Objectives: The objective of this in vitro safety pharmacology study was to compare the potential safety profiles of brimonidine and oxymetazoline. Read More

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Compound action potential inhibition produced by various antidepressants in the frog sciatic nerve.

Eur J Pharmacol 2018 Jan 2;819:122-128. Epub 2017 Dec 2.

Department of Physiology, Saga Medical School, 5-1-1 Nabeshima, Saga 849-8501, Japan. Electronic address:

Although an inhibition of action potential conduction in nerve fibers possibly contributes to at least a part of antinociception produced by analgesics and the adjuvants, it has not been fully examined yet how the conduction inhibition differs in extent among their drugs. We investigated the effects of various antidepressants used as analgesic adjuvants on compound action potentials (CAPs) recorded from the frog sciatic nerve by using the air-gap method. The results were compared with those of the other adjuvants that were reported previously. Read More

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January 2018

α-Adrenoceptors activate mTOR signalling and glucose uptake in cardiomyocytes.

Biochem Pharmacol 2018 02 24;148:27-40. Epub 2017 Nov 24.

Department of Molecular Biosciences, The Wenner-Gren Institute, Stockholm University, SE-106 91 Stockholm, Sweden. Electronic address:

The capacity of G protein-coupled receptors to modulate mechanistic target of rapamycin (mTOR) activity is a newly emerging paradigm with the potential to link cell surface receptors with cell survival. Cardiomyocyte viability is linked to signalling pathways involving Akt and mTOR, as well as increased glucose uptake and utilization. Our aim was to determine whether the α-adrenoceptor (AR) couples to these protective pathways, and increased glucose uptake. Read More

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February 2018

Topical a-Agonist Therapy for Persistent Facial Erythema of Rosacea and the Addition of Oxmetazoline to the Treatment Armamentarium: Where Are We Now?

J Clin Aesthet Dermatol 2017 Jul 1;10(7):28-32. Epub 2017 Jul 1.

Dr. Del Rosso is Research Director at JDR Dermatology Research, Las Vegas, Nevada and at Henderson Dermatology Research in Henderson, Nevada; is Adjunct Clinical Professor (Dermatology) at Touro University Nevada, Las Vegas, Nevada; and practices Dermatology and Cutaneous Surgery at Thomas Dermatology in Las Vegas, Nevada.

The presence of vasoactivity in rosacea-affected skin led to the development of two topical α-adrenergic receptor agonists, brimonidine tartrate 0.5% gel and oxymetazoline hydrochloride 1% cream, both approved by the United States Food and Drug Administration for treatment of persistent facial erythema of rosacea. In this article, the author discusses challenges related to the treatment of persistent facial erythema of rosacea and the use of a-agonist therapy. Read More

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Role of Topical Oxymetazoline for Management of Erythematotelangiectatic Rosacea.

Ann Pharmacother 2018 03 2;52(3):263-267. Epub 2017 Nov 2.

1 Idaho State University, Pocatello, ID, USA.

Objective: To review and summarize topical oxymetazoline's pharmacology, pharmacokinetics, efficacy, safety, cost, and place in therapy for persistent redness associated with erythematotelangiectatic rosacea.

Data Sources: Literature searches of MEDLINE (1975 to September 2017), International Pharmaceutical Abstracts (1975 to September 2017), and Cochrane Database (publications through September 2017) using the terms rosacea, persistent redness, α -agonist, and oxymetazoline.

Study Selection And Data Extraction: Results were limited to studies of human subjects, English-language publications, and topical use of oxymetazoline. Read More

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Noradrenaline, oxymetazoline and phorbol myristate acetate induce distinct functional actions and phosphorylation patterns of α-adrenergic receptors.

Biochim Biophys Acta Mol Cell Res 2017 Dec 6;1864(12):2378-2388. Epub 2017 Sep 6.

Instituto de Fisiología Celular, Universidad Nacional Autónoma de México, Ap. Postal 70-248, Ciudad Universitaria, Ciudad de México 04510, Mexico. Electronic address:

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. Read More

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December 2017

Oxymetazoline hydrochloride cream for facial erythema associated with rosacea.

Expert Rev Clin Pharmacol 2017 Oct 24;10(10):1049-1054. Epub 2017 Aug 24.

a Center for Dermatology Research, Department of Dermatology , Wake Forest School of Medicine , Winston-Salem , NC , USA.

Introduction: Rosacea is a chronic skin condition characterized by transient and persistent erythema of the central face. The symptom of persistent erythema can be particularly frustrating for both patients and physicians as it is difficult to treat. Areas covered: Current treatment options for the treatment of rosacea include metronidazole, azelaic acid, sodium sulfacetamide-sulfur, and brimonidine. Read More

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October 2017

Factors influencing biased agonism in recombinant cells expressing the human α -adrenoceptor.

Br J Pharmacol 2017 Jul 10;174(14):2318-2333. Epub 2017 Jun 10.

Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia.

Background And Purpose: Agonists acting at GPCRs promote biased signalling via Gα or Gβγ subunits, GPCR kinases and β-arrestins. Since the demonstration of biased agonism has implications for drug discovery, it is essential to consider confounding factors contributing to bias. We have examined bias at human α -adrenoceptors stably expressed at low levels in CHO-K1 cells, identifying off-target effects at endogenous receptors that contribute to ERK1/2 phosphorylation in response to the agonist oxymetazoline. Read More

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Mechanistic insight into the norepinephrine-induced fibrosis in systemic sclerosis.

Sci Rep 2016 09 21;6:34012. Epub 2016 Sep 21.

Department of Dermatology, Gunma University Graduate School of Medicine, Japan.

Raynaud's phenomenon is frequently observed in systemic sclerosis (SSc) patients, and cold- or stress-induced norepinephrine (NE) has been speculated to be associated with vasoconstriction. Objective was to elucidate the role of NE in fibrosis in SSc. IL-6 is a potent stimulator of collagen production in fibroblasts. Read More

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September 2016

Oxymetazoline Metered Dose Spray: Factors Affecting Delivery Volume.

J Pediatr Pharmacol Ther 2016 May-Jun;21(3):247-51

Department of Anesthesiology and Pain Medicine, Nationwide Children's Hospital, Columbus, Ohio ; Department of Anesthesiology & Pain Medicine, The Ohio State University, Columbus, Ohio.

Objectives: The current study compared the amount of oxymetazoline delivered by various anesthesia providers when holding the bottle in the upright and inverted position. Additionally, the amount delivered from a full bottle and a half-full bottle was also investigated.

Methods: Using an analytical balance that was calibrated to zero, we evaluated the impact the position of the bottle and the volume of oxymetazoline in the bottle had on the amount being delivered by both anesthesia staff and trainees. Read More

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Effects of the inverse alpha-agonist doxazosin in allergic rhinitis.

Clin Exp Allergy 2016 05;46(5):696-704

Scottish Centre for Respiratory Research, Ninewells Hospital and Medical School, University of Dundee, Dundee, UK.

Background: We examined the paradoxical hypothesis that the alpha-receptor inverse agonist doxazosin might produce beneficial effects in allergic rhinitis.

Objectives: To evaluate single and chronic dosing effects of doxazosin on nasal airflow and symptoms in allergic rhinitis.

Methods: Fifteen patients randomized to receive 3-5 weeks of oral doxazosin 4 mg daily or placebo in crossover fashion. Read More

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Not Just a Drop in the Bucket-Inversion of Oxymetazoline Nasal Decongestant Container Increases Potential for Severe Pediatric Poisoning.

J Pediatr 2016 Jan 30;168:240-241. Epub 2015 Oct 30.

University of California, San Francisco, School of Pharmacy, San Diego, CA.

Oxymetazoline is an over-the-counter nasal decongestant with potent alpha agonist properties. In overdoses as small as 1-2 mL, toxicity can be seen including bradycardia and respiratory depression. We demonstrated that inverting the container increased the volume delivered 20- to 30-fold compared with holding it upright in an in vitro model. Read More

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January 2016

Functional differences between the arteries perfusing gas exchange and nutritional membranes in the late chicken embryo.

J Comp Physiol B 2015 Oct 29;185(7):783-96. Epub 2015 Jun 29.

Department of Pediatrics, Maastricht University Medical Center (MUMC+), Research Institute Growth and Development (GROW) and Cardiovascular Research Institute Maastricht (CARIM), University of Maastricht, P. Debyelaan 25, P.O. Box 5800, 6202 AZ, Maastricht, The Netherlands.

The chicken extraembryonic arterial system comprises the allantoic arteries, which irrigate the gas exchange organ (the chorioallantoic membrane, CAM) and the yolk sac (YS) artery, which irrigates the nutritional organ (the YS membrane). We compared, using wire myography, the reactivity of allantoic and YS arteries from 19-day chicken embryos (total incubation 21 days). The contractions induced by KCl, the adrenergic agonists norepinephrine (NE, nonselective), phenylephrine (α1), and oxymetazoline (α2), electric field stimulation (EFS), serotonin, U46619 (TP receptor agonist), and endothelin (ET)-1 and the relaxations induced by acetylcholine (ACh), sodium nitroprusside (SNP, NO donor), forskolin (adenylate cyclase activator), and isoproterenol (β-adrenergic agonist) were investigated. Read More

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October 2015