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Journal of Pharmaceutical and... May 2022Tetracaine hydrochloride (TCH) is a nasal anesthetic and oxymetazoline hydrochloride (OZH) is a nasal decongestant. A moderate to acute overdosage of OZH and TCH can...
Rapid and sensitive simultaneous separation and electrochemical detection of tetracaine hydrochloride and oxymetazoline hydrochloride in pharmaceutical formulations via core-shell reversed-phase liquid chromatography.
Tetracaine hydrochloride (TCH) is a nasal anesthetic and oxymetazoline hydrochloride (OZH) is a nasal decongestant. A moderate to acute overdosage of OZH and TCH can lead to mydriasis, nausea, cyanosis, tachycardia, dyspnoea, cardiovascular failure, disorientation, seizures, and even death. Liquid chromatography (LC) has been mainly utilized for the individual determination of either TCH or OZH; however, there is a need for rapid and efficient methods for simultaneous analysis in pharmaceutical formulations and aqueous samples. This study highlights the use of the fast and efficient separation capabilities of core-shell silica particles in liquid chromatography (LC) for the simultaneous determination of TCH and OZH using UV detection and the enhanced selectivity afforded by electrochemical detection at a boron-doped diamond (BDD) electrode. Rapid reversed-phase (RP) separation and detection of OZH and TCH in nasal spray and eye drops was achieved within 45 s using a poroshell 120 EC-C column, by adjusting the ratio of organic solvent, mobile phase pH, detection potential and mobile phase flow rate. Sensitivity was compared using ultraviolet (UV) detection at 280 nm, and ECD at + 1.3 V with detection limits of 40 and 70 nM for TCH and OZH, respectively. The developed rapid method was utilized successfully in the analysis of pharmaceutical formulations, where the estimated levels of TCH and OZH in these formulations are in agreement with the specified values outlined by the manufacturers.
Topics: Chromatography, High Pressure Liquid; Chromatography, Reverse-Phase; Drug Compounding; Oxymetazoline; Pharmaceutical Preparations; Tetracaine
PubMed: 35358771
DOI: 10.1016/j.jpba.2022.114717 -
Structural insights into ligand recognition, activation, and signaling of the α adrenergic receptor.Science Advances Mar 2022The α adrenergic receptor (αAR) is a G protein (heterotrimeric guanine nucleotide-binding protein)-coupled receptor that mediates important physiological functions in...
The α adrenergic receptor (αAR) is a G protein (heterotrimeric guanine nucleotide-binding protein)-coupled receptor that mediates important physiological functions in response to the endogenous neurotransmitters norepinephrine and epinephrine, as well as numerous chemically distinct drugs. However, the molecular mechanisms of drug actions remain poorly understood. Here, we report the cryo-electron microscopy structures of the human αAR-GoA complex bound to norepinephrine and three imidazoline derivatives (brimonidine, dexmedetomidine, and oxymetazoline). Together with mutagenesis and functional data, these structures provide important insights into the molecular basis of ligand recognition, activation, and signaling at the αAR. Further structural analyses uncover different molecular determinants between αAR and βARs for recognition of norepinephrine and key regions that determine the G protein coupling selectivity. Overall, our studies provide a framework for understanding the signal transduction of the adrenergic system at the atomic level, which will facilitate rational structure-based discovery of safer and more effective medications for αAR.
Topics: Cryoelectron Microscopy; GTP-Binding Proteins; Humans; Ligands; Norepinephrine; Signal Transduction
PubMed: 35245122
DOI: 10.1126/sciadv.abj5347 -
Journal of Advanced Pharmaceutical... 2022Metered-dose nasal sprays (MDNS) are the most widely used for treating rhinitis. Medicinal preparations in the pharmaceutical market vary in their characteristics. To...
Metered-dose nasal sprays (MDNS) are the most widely used for treating rhinitis. Medicinal preparations in the pharmaceutical market vary in their characteristics. To identify the most effective drug, it is necessary to compare the preparations regarding various parameters. The purpose of the research was to compare oxymetazoline MDNS of different brands regarding their dispersion qualities. To that end, nine oxymetazoline sprays available in the Russian market were chosen and analyzed considering their dynamic characteristics and the spraying dispersion composition. The research was conducted with the shadow photography method, the selection of which was justified by its simplicity, the possibilities for detecting the spray jet composition, the process of its formation in dynamics, and the possibility for measuring droplets of all forms. Momentary images of spray activation phases, as well as an averaged image of 100 shots of the spraying main phase, were obtained. According to a range of characteristics, such as spraying duration, a cone angle and cone structure, all the preparations were grouped into three categories. It was found out that the sprays from Group 2 had the best dynamic rates of dispersion, with Vicks Sinex having the best results. Regarding the distribution of particles of different size, the most optimal composition was found for the drugs from Group 2, particularly, Vicks Sinex and Afrin preparations. Hence, Vicks Sinex spraying regimen and microsprayer design were found the most effective for delivering the medicinal substance to the destination.
PubMed: 35223438
DOI: 10.4103/japtr.japtr_240_21 -
Journal of Cosmetic Dermatology May 2022Rosacea is a chronic cutaneous disorder affecting primarily the face, characterized by erythema, transient or persistent, telangiectasia, and inflammatory lesions... (Review)
Review
Rosacea is a chronic cutaneous disorder affecting primarily the face, characterized by erythema, transient or persistent, telangiectasia, and inflammatory lesions including papulo-pustules and swelling. The essential component of the disease is the persistent erythema of facial skin. Episodes of flushing (acute-subacute intermittent vasodilation) are common. Swelling and erythema of the nose along with dilatation of the pilosebaceous poral orifices, known as rhinophyma, can be noted in chronic cases. Rosacea affects up to 10% of the world population and is especially noted in fair-skinned individuals aged 35-50. Women are affected more often than men. Several treatment modalities including topical medications, systemic drugs, lasers, and light-based therapies have been used for the management of rosacea with variable results. Topical medications such as azelaic acid, metronidazole, and sulfacetamide/sulfur, oral antibiotics such as tetracyclines, and oral retinoids alone or, most commonly, in combination form the mainstay of treatment. Light therapies such as intense pulsed light and pulsed dye laser are best used for the erythemato-telangiectatic type. Topical brimonidine, oxymetazoline, ivermectin, tacrolimus, pimecrolimus, low-dose modified-release tetracyclines and botulinum toxin are the new additions to the therapeutic armamentarium. This article provides a comprehensive review of the various therapies used for rosacea.
Topics: Anti-Bacterial Agents; Dermatologic Agents; Erythema; Female; Humans; Male; Oxymetazoline; Rosacea; Telangiectasis; Tetracyclines
PubMed: 35104917
DOI: 10.1111/jocd.14816 -
Journal of Cosmetic Dermatology Apr 2022Post-acne erythema (PAE) is a common sequela of acne inflammation, and it refers to telangiectasia and erythematous lesions remaining after the acne treatment. Although... (Review)
Review
Post-acne erythema (PAE) is a common sequela of acne inflammation, and it refers to telangiectasia and erythematous lesions remaining after the acne treatment. Although some PAE lesions may improve over time, persisting PAE might be esthetically undesirable for patients. The efficacy of various treatment options for PAE has been investigated in many studies but there exists no gold standard treatment modality. In this study, we aimed to give a systematic literature review on various treatment options for PAE, the advantage of each modality, and compare their efficacy, safety, and feasibility. By using the selected keywords, we carried out a systematic search for articles published from the inception to 28 April 2021 in PubMed/Medline and Embase databases. Of the 5796 initially retrieved articles, 18 of them were fully eligible to be enrolled in our study. In this study, we found that light and laser-based devices were the most frequently used treatments for PAE. Generally, pulsed-dye lasers were the most commonly used laser devices for PAE. Neodymium:yttrium aluminum-garnet lasers were the second most commonly used modalities in treating PAE. Topical treatments such as oxymetazoline, tranexamic acid, and brimonidine tartrate are promising treatments in reducing PAE lesions. In our study, no severe side effects were found. In conclusion, both laser devices and topical agents seem to be effective for PAE lesions; however, further randomized clinical trials are needed in this field.
Topics: Acne Vulgaris; Brimonidine Tartrate; Erythema; Humans; Lasers, Dye; Lasers, Solid-State; Treatment Outcome
PubMed: 35076997
DOI: 10.1111/jocd.14804 -
Dermatologic Therapy Apr 2022Persistent post acne erythema (PAE) is common cosmetically unacceptable and challenging sequelae of acne lesions. Tranexamic acid (TXA) is an antifibrinolytic agent that...
Persistent post acne erythema (PAE) is common cosmetically unacceptable and challenging sequelae of acne lesions. Tranexamic acid (TXA) is an antifibrinolytic agent that shows a positive effect on wound healing in several studies, and it showed benefits in treating skin diseases like melasma, rosacea erythema and ultraviolet induced pigmentations. Oxymetazoline (OXZ) is a synthetic, highly selective agonist for alpha 1A-adrenoceptor. It is a potent vasoconstrictor. OXZ hydrochloride 1% cream was approved by the FDA in January 2017 as a topical treatment for persistent facial erythema in rosacea patients. Brimonidine tartrate (BMT) is highly selective α adrenergic receptor agonist, results in direct, potent vasoconstriction of small arterioles and veins. In 2013, brimonidine 0.33% gel was the first topical therapy to be FDA approved for the treatment of persistent facial erythema from rosacea. To evaluate the efficacy and safety of topical triple combination (TXA 5% + OXZ 1.5% + BMT 0.33%) in the treatment of PAE planned as split face comparative study. This study was conducted on 40 patients diagnosed with persistent PAE for at least 3 months, the right side of the face was treated with topical triple combination in liposomal base and was compared to the left side to which topical lipocream (placebo) was applied as a control. Our treatment plan lasted for 3 months. According to the investigator's global assessment of photographs and computerized analysis of erythema using image analysis software, topical triple combination applied on the right side of face was significantly effective in diminishing PAE when compared to topical placebo left side. Topical triple combination is a safe and cost-effective treatment for PAE.
Topics: Acne Vulgaris; Administration, Topical; Brimonidine Tartrate; Drug Therapy, Combination; Erythema; Humans; Oxymetazoline; Rosacea; Treatment Outcome
PubMed: 35060229
DOI: 10.1111/dth.15327 -
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 -
International Journal of Pediatric... Feb 2022Topical intranasal decongestants are essential in nasal surgery to improve operative field. There are concerns regarding safety in paediatric population. Data on safety...
OBJECTIVES
Topical intranasal decongestants are essential in nasal surgery to improve operative field. There are concerns regarding safety in paediatric population. Data on safety and safe dosage are limited. This systematic review evaluated the literature on safety and dosage of intranasal decongestant in paediatric population.
METHODS
We performed a systematic search of PubMed, EMBASE, Cochrane library for relevant articles. Quality assessment was done on included articles.
RESULTS
A total of 10 articles were included: five case reports; three observational studies; and two randomised control trials. Decongestants evaluated were phenylephrine, oxymetazoline, epinephrine, xylometazoline, and cocaine. In total, 209 patients were included. Side effects reported included bradycardia, tachycardia and hypertension. These were mostly self-limiting and of no clinical compromise to the patients. A total of 4/209 (1.9%) of patients required treatment for these reported effects. No mortality was reported in the included studies.
CONCLUSION
In the paediatric population, the literature suggests that when delivered in a pre-specified, controlled dosage, the haemodynamic effects of phenylephrine, oxymetazoline, xylometazoline are minimal and of no clinical significance. There is scope for further studies to establish safe dosage in the paediatric population given the paucity of current literature.
Topics: Administration, Intranasal; Administration, Topical; Child; Humans; Nasal Decongestants; Nasal Surgical Procedures; Oxymetazoline; Vasoconstrictor Agents
PubMed: 34942425
DOI: 10.1016/j.ijporl.2021.111010 -
Clinical and Experimental Dermatology Apr 2022Erythromelalgia is an infrequent syndrome with a profound impact on quality of life. Its management is usually challenging and multiple treatments have been reported...
Erythromelalgia is an infrequent syndrome with a profound impact on quality of life. Its management is usually challenging and multiple treatments have been reported with variable response rates. To the best of our knowledge, we present the first case of erythromelalgia successfully treated with topical oxymetazoline.
Topics: Erythromelalgia; Humans; Oxymetazoline; Quality of Life
PubMed: 34905256
DOI: 10.1111/ced.15060 -
Histology and Histopathology Mar 2022Our aim in this study is to reveal the expression of Vascular Endothelial Growth Factor (VEGF) and Inducible Nitric Oxide Synthase (iNOS) in the pathogenesis of rhinitis...
The importance of vascular epithelial growth factor (VEGF) and inducible nitric oxide synthase (INOS) in rhinitis medicamentosa pathogenesis: An experimental rat model study.
OBJECTIVE
Our aim in this study is to reveal the expression of Vascular Endothelial Growth Factor (VEGF) and Inducible Nitric Oxide Synthase (iNOS) in the pathogenesis of rhinitis medicamentosa (RM), which occurs as a result of the overdose and long-term use of topical nasal decongestants.
METHODS
In this study, 24 Wistar albino rats were divided into two groups as experimental and control groups. In the experimental group, 50 µl of 0.05% oxymetazoline (iliadin® merck) was applied intranasally to each nostril three times a day for 2 months with the help of a micropipette. 50 µl saline was applied to the control group. At the end of the second month, the rats were examined. RM was detected in the experimental group. Then the nasal tissues of the rats were removed and fixed with 10% phosphate buffered neutral formaldehyde (pH=7.4). Nasal tissues were decalcified in Morse's solution (10% sodium citrate and 22.5% formic acid). Histopathological evaluations of the preparations were stained using Masson Trichrome (TCM) and Hematoxylin Eosin (H&E) techniques and immunohistochemical examinations of the preparations were stained with VEGF and iNOS antibodies and photographed using the Leica DM6000B microscope and the Leica Application Suite Program.
RESULTS
In the RM group, we found a significant increase in VEGF and iNOS expression in the nasal mucosa compared to the control group (p<0.001). We also observed the main histopathological changes in the nasal mucosa under a light microscope, including squamous metaplasia in the epithelium of the tunica mucosa, submucosal perivascular edema and degeneration of the submucosal glands.
CONCLUSIONS
According to these results, increased expression levels of VEGF and iNOS play an important role in rebound swelling in RM pathogenesis.
Topics: Animals; Edema; Nasal Mucosa; Nitric Oxide Synthase Type II; Oxymetazoline; Rats; Rats, Wistar; Rhinitis; Vascular Endothelial Growth Factor A
PubMed: 34842278
DOI: 10.14670/HH-18-399