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Oxymetazoline

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https://www.readbyqxmd.com/read/29603916/phase-1-pharmacokinetics-and-phase-3-efficacy-of-testosterone-nasal-gel-in-subjects-with-seasonal-allergies
#1
Alan D Rogol, Natalia Tkachenko, Philipp Badorrek, Jens M Hohlfeld, Nathan Bryson
INTRODUCTION: NATESTO® testosterone nasal gel (TNG) is a liquid gel that is applied in the nose for the treatment of male hypogonadism. There is a reasonable concern that administration of TNG to patients with active rhinitis could modify absorption. Results from two clinical studies are reported wherein subjects with allergic rhinitis (AR) subjects are treated with TNG. METHODS: The 24-hour pharmacokinetics (PK) and relative bioavailability of serum total testosterone (sTT) from TNG (11 mg tid ) were determined using a phase 1 Latin-square design with 18 eugonadal AR subjects crossed over between asymptomatic, symptomatic-untreated, and symptomatic-treated (oxymetazoline) conditions...
March 19, 2018: Canadian Urological Association Journal, Journal de L'Association des Urologues du Canada
https://www.readbyqxmd.com/read/29602670/topical-tranexamic-acid-for-the-treatment-of-acute-epistaxis-in-the-emergency-department
#2
Asha R Birmingham, Nathan D Mah, Ran Ran, Matthew Hansen
OBJECTIVE: To evaluate the effectiveness and potential benefits of topical tranexamic acid (TXA) in the management of acute epistaxis. METHODS: Retrospective review was performed among all patients presenting to the institution's emergency department (ED) with epistaxis between September 2014 and August 2016. Patients achieving hemostasis with standard of care agents, such as oxymetazoline, lidocaine, or epinephrine were excluded. The primary outcome was the ED length of stay (LOS)...
March 21, 2018: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/29537449/phase-2-randomized-dose-ranging-study-of-oxymetazoline-cream-for-treatment-of-persistent-facial-erythema-associated-with-rosacea
#3
Janet DuBois, Jeffrey S Dover, Terry M Jones, Robert A Weiss, David R Berk, Gurpreet Ahluwalia
BACKGROUND: Rosacea is a chronic dermatologic condition with limited treatment options. OBJECTIVE: This phase 2 study evaluated the optimal oxymetazoline dosing regimen in patients with moderate to severe persistent facial erythema of rosacea. METHODS: Patients were randomly assigned to oxymetazoline cream, 0.5%, 1.0%, or 1.5%, or vehicle, administered once daily (QD) or twice daily (BID) for 28 consecutive days. The primary efficacy endpoint was the proportion of patients with ≥2-grade improvement from baseline on the Clinician Erythema Assessment (CEA) and the Subject Self-Assessment of erythema (SSA-1) on day 28...
March 1, 2018: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/29537447/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
#4
Leslie Baumann, David J Goldberg, Linda Stein Gold, Emil A Tanghetti, Edward Lain, Joely Kaufman, Emily Weng, David R Berk, Gurpreet Ahluwalia
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 1.0% or vehicle applied topically to the face once daily for 29 days. The primary efficacy outcome was ≥2-grade improvement from baseline on both Clinician Erythema Assessment (CEA) and Subject Self-Assessment for rosacea facial redness (SSA) (composite success) at 3, 6, 9, and 12 hours postdose on day 29...
March 1, 2018: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/29462230/clinical-pharmacokinetics-of-oxymetazoline-cream-following-topical-facial-administration-for-the-treatment-of-erythema-associated-with-rosacea
#5
Amy W Kuang, Janet DuBois, Mayssa Attar, Gurpreet Ahluwalia
BACKGROUND: Oxymetazoline cream 1.0% is FDA-approved for the topical treatment of persistent facial erythema associated with rosacea in adults. This phase 2, multicenter, randomized, double-blind, parallel-group study assessed the pharmacokinetics, safety, and tolerability of oxymetazoline in patients with moderate to severe erythema associated with rosacea. METHODS: Eligible patients were randomized to 1 of 8 treatment groups (oxymetazoline cream 0.5%, 1.0%, or 1...
February 1, 2018: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/29409915/efficacy-and-safety-of-topical-oxymetazoline-cream-1-0-for-treatment-of-persistent-facial-erythema-associated-with-rosacea-findings-from-the-two-phase-3-29-day-randomized-controlled-reveal-trials
#6
Linda Stein-Gold, Leon H Kircik, Zoe Diane Draelos, Philip Werschler, Janet DuBois, Edward Lain, Leslie Baumann, David J Goldberg, Joely Kaufman, Emil A Tanghetti, Nancy Alvandi, Emily Weng, David R Berk, Gurpreet Ahluwalia
BACKGROUND: Rosacea is a chronic dermatologic condition with limited treatment options. OBJECTIVE: To evaluate topical oxymetazoline cream 1.0% in patients with moderate to severe persistent erythema of rosacea. METHODS: Data were pooled from two identically designed phase 3 trials. Patients were randomized to receive oxymetazoline 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...
January 30, 2018: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/29409914/efficacy-and-safety-of-oxymetazoline-cream-1-0-for-treatment-of-persistent-facial-erythema-associated-with-rosacea-findings-from-the-52-week-open-label-reveal-trial
#7
Zoe Diana Draelos, Michael H Gold, Robert A Weiss, Leslie Baumann, Steven K Grekin, Deanne Mraz Robinson, Steven E Kempers, Nancy Alvandi, Emily Weng, David R Berk, Gurpreet Ahluwalia
BACKGROUND: Limited treatments are available for persistent erythema of rosacea. OBJECTIVE: To examine long-term safety and efficacy of oxymetazoline cream 1.0% in rosacea patients with moderate to severe persistent erythema. METHODS: Patients applied oxymetazoline once daily for 52 weeks. Safety assessments included treatment-emergent adverse events (TEAEs), skin blanching, inflammatory lesion counts, telangiectasia, disease severity, and rebound effect...
January 30, 2018: Journal of the American Academy of Dermatology
https://www.readbyqxmd.com/read/29374829/in-vitro-safety-pharmacology-profiling-of-topical-%C3%AE-adrenergic-agonist-treatments-for-erythema-of-rosacea
#8
David Piwnica, Atul Pathak, Gregor Schäfer, James R Docherty
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. METHODS: Brimonidine and oxymetazoline underwent pharmacological profiling with a standard panel of 151 assays, including α-adrenergic receptors and 5-hydroxytryptamine (5-HT) receptors...
January 27, 2018: Drugs in R&D
https://www.readbyqxmd.com/read/29320594/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-first-reveal-trial
#9
Leon H Kircik, Janet DuBois, Zoe Diana Draelos, Philip Werschler, Kimberly Grande, Fran E Cook-Bolden, Emily Weng, David R Berk, Gurpreet Ahluwalia
An unmet need exists for a safe, tolerable, effective treatment for moderate to severe persistent facial erythema in patients with rosacea. This pivotal phase 3, multicenter, double-blind study evaluated the efficacy and safety of topical oxymetazoline in patients with facial erythema associated with moderate to severe rosacea. Patients were randomly assigned to treatment with oxymetazoline hydrochloride cream 1.0% or vehicle applied once daily for 29 days, and were followed for 28 days posttreatment. The primary efficacy outcome was having at least a 2-grade decrease from baseline on both the Clinician Erythema Assessment (CEA) and the Subject Self-Assessment for rosacea facial redness (SSA) scales (composite success) at 3, 6, 9, and 12 hours postdose on day 29...
January 1, 2018: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/29203420/compound-action-potential-inhibition-produced-by-various-antidepressants-in-the-frog-sciatic-nerve
#10
Ryo Hirao, Tsugumi Fujita, Aiko Sakai, Eiichi Kumamoto
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...
January 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29176433/drug-updates-and-approvals-2017-in-review
#11
Geoffrey Mospan, Cortney Mospan, Shayna Vance, Alyssa Bradshaw, Kalyn Meosky, Kirklin Bowles
In 2017, the FDA approved several new drugs for use in primary care. This article highlights the following new drugs: brodalumab (Siliq), dapagliflozin and saxagliptin (Qtern), dupilumab (Dupixent), oxymetazoline (Rhofade), safinamide (Xadago), and sarilumab (Kevzara).
December 15, 2017: Nurse Practitioner
https://www.readbyqxmd.com/read/29175420/%C3%AE-1a-adrenoceptors-activate-mtor-signalling-and-glucose-uptake-in-cardiomyocytes
#12
Masaaki Sato, Bronwyn A Evans, Anna L Sandström, Ling Yeong Chia, Saori Mukaida, Bui San Thai, Anh Nguyen, Linzi Lim, Christina Y R Tan, Jo-Anne Baltos, Paul J White, Lauren T May, Dana S Hutchinson, Roger J Summers, Tore Bengtsson
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 α1A -adrenoceptor (AR) couples to these protective pathways, and increased glucose uptake. We characterised α1A -AR signalling in CHO-K1 cells co-expressing the human α1A -AR and GLUT4 (CHOα1A GLUT4myc) and in neonatal rat ventricular cardiomyocytes (NRVM), and measured glucose uptake, intracellular Ca2+ mobilization, and phosphorylation of mTOR, Akt, 5' adenosine monophosphate-activated kinase (AMPK) and S6 ribosomal protein (S6rp)...
February 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29104721/topical-a-agonist-therapy-for-persistent-facial-erythema-of-rosacea-and-the-addition-of-oxmetazoline-to-the-treatment-armamentarium-where-are-we-now
#13
REVIEW
James Q Del Rosso
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. The author also discusses cases of worsening of facial erythema after the application of brimonidine, as well as briefly reviews recently reported clinical data on oxymetazoline...
July 2017: Journal of Clinical and Aesthetic Dermatology
https://www.readbyqxmd.com/read/29094614/role-of-topical-oxymetazoline-for-management-of-erythematotelangiectatic-rosacea
#14
Rebecca M Hoover, John Erramouspe
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...
November 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/29053231/effects-of-common-cold-and-concomitant-administration-of-nasal-decongestant-on-the-pharmacokinetics-and-pharmacodynamics-of-nasal-glucagon-in-otherwise-healthy-participants-a-randomized-clinical-trial
#15
Cristina B Guzman, Helene Dulude, Claude Piché, Marianne Rufiange, Aziz A Sadoune, Emmanouil Rampakakis, Dolores Carballo, Myriam Triest, Michelle Xiaotian Zhang, Shuyu Zhang, Maryam Tafreshi, Eric Sicard
AIMS: Nasal glucagon (NG) is a nasally-administered glucagon powder, absorbed through the nasal mucosa, designed for treatment of severe hypoglycaemia. This study evaluated the safety, pharmacokinetics (PK) and pharmacodynamics (PD) of NG in otherwise healthy participants with common colds and after recovery from cold symptoms, with and without concomitant nasal decongestant. MATERIALS AND METHODS: This was a single-centre, open-label study. Cohort 1 participants (N = 18) received 2 doses of NG: one while experiencing nasal congestion and another after recovery from cold symptoms...
October 20, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28962626/efficacy-and-usability-of-a-novel-nebulizer-targeting-both-upper-and-lower-airways
#16
Daniela Posa, Antonio Pizzulli, Petra Wagner, Serena Perna, Stephanie Hofmaier, Paolo Maria Matricardi, Susanne Lau
BACKGROUND: Upper and lower airways diseases share in part their pathogenic mechanisms and frequently occur simultaneously as "United Airway Disease." Local treatment with nebulizers delivers anti-symptomatic drugs in either the upper or the lower airways, according to the particle size generated by the nebulizer. To our knowledge, no nebulizer combines both application ways. The aim of this study is to test the efficacy and usability of a new nebulizer (OMRON A3 complete), generating aerosols with particles diameters of 2-4...
September 29, 2017: Italian Journal of Pediatrics
https://www.readbyqxmd.com/read/28901959/oxymetazoline-induced-asthma
#17
Siddharth Shah, Kinner Patel, Harvir S Gambhir
No abstract text is available yet for this article.
August 24, 2017: American Journal of Therapeutics
https://www.readbyqxmd.com/read/28888989/noradrenaline-oxymetazoline-and-phorbol-myristate-acetate-induce-distinct-functional-actions-and-phosphorylation-patterns-of-%C3%AE-1a-adrenergic-receptors
#18
Rocío Alcántara-Hernández, Aurelio Hernández-Méndez, M Teresa Romero-Ávila, Marco A Alfonzo-Méndez, André S Pupo, J Adolfo García-Sáinz
In LNCaP cells that stably express α1A -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. α1A -Adrenergic receptor interaction with β-arrestins (colocalization/coimmunoprecipitation) was induced by noradrenaline and oxymetazoline and, to a lesser extent, by phorbol myristate acetate...
December 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28837365/oxymetazoline-hydrochloride-cream-for-facial-erythema-associated-with-rosacea
#19
REVIEW
Nupur U Patel, Shweta Shukla, Jessica Zaki, Steven R Feldman
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. Until recently, brimonidine gel was the only option approved specifically for the treatment of facial erythema. However, oxymetazoline hydrochloride 1% cream is a newly FDA approved topical medication for adult rosacea patients...
October 2017: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/28711215/changes-occurring-in-mucosal-contractility-of-the-inferior-turbinate-and-mucociliary-clearance-following-total-laryngectomy-a-prospective-clinical-trial
#20
Ilker Kocak, Remzi Dogan, Sabri Baki Eren, Selahattin Tugrul, Orhan Ozturan, Aysenur Meric Hafiz
OBJECTIVE: In this study, changes occurring in the contractility capacity of the inferior turbinate and mucociliary clearance time due to the interruption of nasal air flow were examined. MATERIAL & METHODS: A total of 23 patients undergone total laryngectomy between June 2010 and June 2012 were included in the study. Acoustic rhinometry test was performed in the patients before and after 0.05% oxymetazoline nasal topical decongestant administration. In addition, saccharin test was applied in order to measure mucociliary clearance...
July 12, 2017: Auris, Nasus, Larynx
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