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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 -
Indian Journal of Otolaryngology and... Sep 2023Epistaxis means bleeding from nostrils, nasal cavity or nasopharynx. To summarize the available epistaxis treatment options. Methods: 61 articles published in the last...
Epistaxis means bleeding from nostrils, nasal cavity or nasopharynx. To summarize the available epistaxis treatment options. Methods: 61 articles published in the last 20 years were included. Duplicate records, irrelevant and inaccessible ones were excluded. Epistaxis can be treated with first aid measures such as external pressure and ice packing and applying topical agents, e.g. oxymetazoline that stops 65-75% of nosebleeds in A&E. Also, with electrocautery which is more effective and has fewer recurrences (14.5% vs. 35.1%) than chemical cauterization and applying tranexamic acid that promotes hemostasis in 78% of patients, versus 35% and 31% respectively in patients treated with oxymetazoline and nasal packing. Furthermore, nasal packing can be applied with non-absorbable materials, e.g. petroleum jelly, BIPP gauze, PVA nasal tampons (Merocel), Foley catheter, balloons (Rapid-Rhino), absorbable materials, e.g. nasal tampon (Nasopore), and with newer hemostatic materials which are more effective and with fewer complications, e.g. hemostatic gauzes (Surgicel), thrombin matrix (Floseal), gelatin sponge (Spongostan) and fibrin glue. Moreover, epistaxis can be achieved with endoscopic ligation of arteries, mainly SPA, which is more effective than conventional nasal packing (97% vs. 62%), and with endoscopic cauterization which is more effective than ligation. Finally, for intractable cases embolization can be applied using gelatin sponge, foam, PVA and coils with 80% success rate and comparable efficacy and complications to surgical methods. Epistaxis can be dealt with various methods depending on patient's history and available resources. Newer hemostatic agents in combination with endoscopic methods have advantages over traditional methods.
PubMed: 37636777
DOI: 10.1007/s12070-023-03824-z -
The Annals of Pharmacotherapy Mar 2018To review and summarize topical oxymetazoline's pharmacology, pharmacokinetics, efficacy, safety, cost, and place in therapy for persistent redness associated with... (Review)
Review
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. Relevant materials from government sources, industry, and reviews were also included.
DATA SYNTHESIS
Data support the efficacy of oxymetazoline for persistent facial redness. Little study beyond clinical trials cited in the drug approval process has been conducted. Current data suggest that oxymetazoline is similar in safety and efficacy to brimonidine. Head-to-head comparisons of topical α-agonists for erythema caused by rosacea are needed.
CONCLUSION
The topical α-agonist, oxymetazoline, is safe and effective for reducing persistent facial redness associated with erythematotelangiectatic subtype of rosacea. Health care practitioners selecting among treatments should consider not only the subtype of rosacea but also individual patient response, preference, and cost.
Topics: Administration, Topical; Adrenergic alpha-Agonists; Drug Interactions; Erythema; Humans; Oxymetazoline; Rosacea; Treatment Outcome
PubMed: 29094614
DOI: 10.1177/1060028017740139 -
The Journal of Dermatological Treatment Sep 2022Since medication absorption through the skin and eye tissue seems similar, commercially available eye-drops could be used to treat skin diseases when topical therapies... (Review)
Review
Since medication absorption through the skin and eye tissue seems similar, commercially available eye-drops could be used to treat skin diseases when topical therapies are unavailable or unaffordable. The FDA-approved and off-label applications of various eye drops used as topical treatments in dermatological clinical practice were highlighted in this review. A thorough PubMed and Google Scholar library search using various combinations of the keywords (Eye drop, ocular solution, conjunctival installation, and skin diseases, topical, local, beta-blockers, prostaglandin, cyclosporin, apraclonidine, atropine, oxymetazoline). Based on the findings of the studies reviewed, timolol is highly recommended for infantile hemangioma and other vascular skin conditions such as angiomas, Kaposi sarcoma, acne, rosacea, and wound healing. Bimatoprost is a drug that can be used to treat hypotrichosis of any kind, as well as mild localized alopecia areata and leukoderma. Oxymetazoline ispromising for treating facial erythema. We recommend apraclonidine for mild upper eyelid ptosis induced botulinum neurotoxin. We don't recommend atropine for hyperhidrosis, although it can help with hydrocystomas and pruritis produced by syringomas. Tobramycin will need to be tested in RCTs before it can be confirmed as a viable alternative to systemic treatments for treating green nail syndrome.
Topics: Humans; Ophthalmic Solutions; Oxymetazoline; Dermatology; Timolol; Atropine Derivatives
PubMed: 35652324
DOI: 10.1080/09546634.2022.2079598 -
Current Opinion in Pharmacology Jun 2019Rosacea 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... (Review)
Review
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. The topical alpha adrenergic agonist oxymetazoline reduces rosacea-related erythema. Topical ivermectin improves lesion count, inflammation, and maintenance of remission of rosacea compared to topical metronidazole. Procedural therapies including pulsed dye laser, radiofrequency, and dual frequency ultrasound are promising as both monotherapies or in combination. Although there are several effective treatment modalities for rosacea management, treatments options should be tailored for the specific clinical scenario.
Topics: Administration, Cutaneous; Humans; Rosacea
PubMed: 30639950
DOI: 10.1016/j.coph.2018.12.001 -
Journal of the American Association of... Jan 2021Primary care, urgent care, and emergency department providers periodically treat epistaxis, either as recurrent nosebleed or an acute persistent episode. Silver nitrate...
Primary care, urgent care, and emergency department providers periodically treat epistaxis, either as recurrent nosebleed or an acute persistent episode. Silver nitrate application to the decongested and anesthetized nasal mucosa addresses the former in most cases. The plethora of commercial nasal packing devices testifies to the discomfort, technical difficulty, and frustration associated with traditional gauze-packing methods. Inflatable anterior nasal balloon packs reliably control most nosebleeds. Addition of a Foley catheter nasopharyngeal balloon pack manages most posterior epistaxis. Cautery and the two packing techniques mentioned above should treat most cases not requiring otolaryngology consultation or interventional radiology. Appropriate anesthetic and analgesics lessen the unpleasantness for both the patient and the provider. Topical moisturizing facilitates mucosal healing. Oxymetazoline 0.05% nasal spray provides the patient means to address rebleeding after discharge from treatment.
Topics: Ambulatory Care; Cautery; Emergency Service, Hospital; Epistaxis; Humans
PubMed: 33463979
DOI: 10.1097/JXX.0000000000000527 -
JAMA Ophthalmology Nov 2020
Topics: Blepharoptosis; Humans; Oxymetazoline; Randomized Controlled Trials as Topic; Visual Fields
PubMed: 33001145
DOI: 10.1001/jamaophthalmol.2020.3833 -
American Journal of Clinical Dermatology Dec 2015Rosacea is a common chronic inflammatory disorder that affects approximately 16 million Americans. The multifactorial pathophysiology of rosacea is not fully understood.... (Comparative Study)
Comparative Study Review
Rosacea is a common chronic inflammatory disorder that affects approximately 16 million Americans. The multifactorial pathophysiology of rosacea is not fully understood. Several new treatment options were recently US Food and Drug Administration approved or are in clinical trials. This paper reviews new treatment options including ivermectin, brimonidine, the new foam formulation of azelaic acid, and oxymetazoline. The potential role in therapy, patient selection, and adverse effects of these agents are discussed.
Topics: Administration, Topical; Brimonidine Tartrate; Clinical Trials, Phase III as Topic; Dermatologic Agents; Dicarboxylic Acids; Drug Approval; Female; Follow-Up Studies; Forecasting; Humans; Ivermectin; Male; Oxymetazoline; Patient Satisfaction; Rosacea; Severity of Illness Index; Treatment Outcome; United States; United States Food and Drug Administration
PubMed: 26396117
DOI: 10.1007/s40257-015-0156-2 -
The Medical Letter on Drugs and... Feb 2024
Topics: Humans; Rosacea
PubMed: 38294765
DOI: 10.58347/tml.2024.1695b