Prevention of middle ear barotrauma with oxymetazoline/fluticasone treatment.

Middle ear barotrauma (MEB) is a common complication of hyperbaric oxygen (HBO2) therapy. It has been reported in more than 40% of HBO2 treatments and can interrupt the sequence of HBO2. MEB may lead to pain, tympanic membrane rupture, and even hearing loss. The aim of this study was to determine if pretreatment with intranasal fluticasone and oxymetazoline affected the incidence of MEB. We conducted a retrospective chart review of subjects undergoing HBO2 at our institution between February 1, 2014, and May 31, 2019. Subjects in the fluticasone/oxymetazoline (FOT) treatment group used intranasal fluticasone 50 mcg two times per day and oxymetazoline 0.05% one spray two times per day beginning 48 hours prior to initial HBO2. Oxymetazoline was discontinued after four days. Fluticasone was continued for the duration of HBO2 therapy. A total of 154 unique subjects underwent 5,683 HBO2 treatments: 39 unique subjects in the FOT group underwent 1,501 HBO2; 115 unique subjects in the nFOT (no oxymetazoline or fluticasone treatment) group underwent 4,182 HBO2 treatments. The incidence of MEB was 15.4% in the FOT group and 16.2% in the nFOT group. This was not a statistically significant difference (OR = 0.77; p = 0.636). Treatment pressure, age over 65 years, male sex, and BMI were not associated with a difference in MEB incidence. In summary, pretreatment with intranasal oxymetazoline and fluticasone in patients undergoing HBO2 did not significantly reduce MEB. More investigation with larger numbers of participants and prospective studies could further clarify this issue.

Oxymetazoline and Energy-Based Therapy in Patients with Rosacea: Evaluation of the Safety and Tolerability in an Open-Label, Interventional Study.

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.

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

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. Oxymetazoline 1.0% cream is an α adrenergic agonist, which has shown to reduce facial erythema. The aim of this study was to determine the degree of erythema improvement and telangiectasia clearance after combination treatment with PDL plus oxymetazoline 1.0% cream. STUDY DESIGN/MATERIALS AND METHODS: This retrospective study was conducted at two sites. Pre- and post-treatment cross-polarized images from subjects on combination treatment with PDL and oxymetazoline 1.0% cream were graded by a board-certified dermatologist at each practice. Blinded images were analyzed using the Clinical Erythema Assessment (CEA) Scale (0 = clear and 4 = severe). Unblinded images were analyzed using the five-point Telangiectasia Scale to determine the degree of improvement post-treatment compared with baseline (1 = <5% clearance and 5 = 75-100% clearance). RESULTS: Thirty-one subjects (20 females, 11 males) of age 51 ± 13 years (mean ± standard deviation) were included in the study after an average of 4 months (range: 1-13) of daily oxymetazoline 1.0% cream and two (range: 1-4) PDL treatments. At baseline, 87% of subjects had CEA Grade 2 (mild erythema) or higher. For erythema, 55% of subjects improved by at least one CEA grade and 13% achieved two grades of improvement post-treatment. For telangiectasias, 90% of subjects achieved at least a two-point clearance (5-25%), 62% at least a three-point clearance (25-50%), and 41% at least a four-point clearance (50-75%) post-treatment. Compared with subjects with baseline CEA Grade 1-2 (almost clear to mild erythema), significantly more subjects with baseline CEA Grade 3-4 (moderate to severe erythema) achieved at least one CEA grade of improvement (P = 0.021) and two grades of CEA improvement (P = 0.041). A higher percentage of baseline CEA Grade 3-4 subjects achieved at least a two-point clearance in telangiectasias (P = 0.055). CONCLUSIONS: Combination treatment with PDL and daily oxymetazoline 1.0% cream can safely and effectively reduce erythema and telangiectasias. Limitations include the retrospective design of the study, small sample size, and lack of a control group. Lasers Surg. Med. © 2019 Wiley Periodicals, Inc.

Microvascular Effects of Pulsed Dye Laser in Combination With Oxymetazoline.

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. Each animal was assigned to one of four experimental groups: saline alone, oxymetazoline alone (10 µl applied once daily × 7 days), saline + PDL (saline applied 5 minutes before PDL irradiation [10 mm spot, 1.5 ms pulse duration, 7 J/cm2 delivered to epidermis]), or oxymetazoline + PDL (10 µl oxymetazoline applied 5 minutes before PDL and then once daily × 7 days). Brightfield and laser speckle imaging were performed for 7 days to monitor vascular architectural and functional changes. RESULTS: We observed persistent blood flow in all of the saline-only and oxymetazoline-only experiments. A higher rate of vascular shutdown was observed with oxymetazoline + PDL (66.7%) compared with saline + PDL alone (16.7%). Oxymetazoline application increased venule diameter at 5 minutes post-application and decreased both arteriole and venule diameters at 60 minutes post-application. CONCLUSION: The combination protocol of oxymetazoline + PDL induces persistent vascular shutdown observed 7 days after irradiation. This result may be associated with the acute vascular effects of oxymetazoline. Oxymetazoline + PDL should be evaluated as a treatment for cutaneous vascular disease, including rosacea and port wine birthmarks. Lasers Surg. Med. © 2019 Wiley Periodicals, Inc.

Interventions for rosacea based on the phenotype approach: an updated systematic review including GRADE assessments.

BACKGROUND: Rosacea is a common chronic facial dermatosis. Classification of rosacea has evolved from subtyping to phenotyping. OBJECTIVES: To update our systematic review on interventions for rosacea. METHODS: We searched CENTRAL, MEDLINE, Embase, LILACS, Science Citation Index and ongoing trials registers (March 2018) for randomized controlled trials. Study selection, data extraction, risk-of-bias assessment and analyses were carried out independently by two authors. Grading of Recommendations, Assessment, Development and Evaluations (GRADE) was used to assess certainty of evidence. RESULTS: We included 152 studies (46 were new), comprising 20 944 participants. Topical interventions included brimonidine, oxymetazoline, metronidazole, azelaic acid, ivermectin and other topical treatments. Systemic interventions included oral antibiotics, combinations with topical treatments or other systemic treatments. Several studies evaluated laser or light-based treatment. We present the most current evidence for rosacea management based on a phenotype-led approach. CONCLUSIONS: For reducing temporarily persistent erythema there was high-certainty evidence for topical brimonidine and moderate certainty for topical oxymetazoline; for erythema and mainly telangiectasia there was low-to-moderate-certainty evidence for laser and intense pulsed light therapy. For reducing papules/pustules there was high-certainty evidence for topical azelaic acid and topical ivermectin; moderate-to-high-certainty evidence for doxycycline 40 mg modified release (MR) and isotretinoin; and moderate-certainty evidence for topical metronidazole, and topical minocycline and oral minocycline being equally effective as doxycycline 40 mg MR. There was low-certainty evidence for tetracycline and low-dose minocycline. For ocular rosacea, there was moderate-certainty evidence that oral omega-3 fatty acids were effective and low-certainty evidence for ciclosporin ophthalmic emulsion and doxycycline.

Compound shuanghua tablets combined with Western medicine on serum and secretion inflammatory factors in patients with acute secretory otitis media caused by swimming.

To observe and analyze the effect of compound shuanghua tablets combined with western medicine on serum and secretion inflammatory factors in patients with acute secretory otitis media caused by swimming. The 140 patients who had been treated in our hospital for acute secretory otitis media were selected as research objects, all of which were caused by swimming. The patients were divided into two groups, namely the control group accepting routine western drug therapy and the research group accepting compound shuanghua tablets combined with western drug therapy, each group contains 70 patients. The therapeutic effect of patients in two groups were observed and compared. Through observation, the levels of tumor necrosis factor, interleukin-6 and interleukin-10 were found to be significantly improved in the research group compared with the control group, and the intergroup difference was of statistical significance, p<0.05; The overall treatment efficiency of the research group was significantly higher than that of the control group, with statistical significance, p<0.05. For patients with acute secretory otitis media caused by swimming, the compound shuanghua tablets combined with Western medicine treatment can not only actively reduce various inflammatory factors in middle ear effusion, but also significantly improve the overall treatment efficiency.

Endoscopic-guided coblation treatment of nasal telangiectasias in hereditary hemorrhagic telangiectasia: "How I do it".

INTRODUCTION: Hereditary hemorrhagic telangiectasia (HHT) is an autosomal dominant disease that leads to frequent epistaxis. It can have a significant impact on quality of life. Many reports exist regarding various therapies to address the epistaxis. MATERIALS AND METHODS: We presented our technique for addressing the epistaxis associated with HHT. RESULTS: Patients are treated in the operating room while they are under general anesthesia. A local anesthetic is injected sublabially, and oxymetazoline is dripped into the nose. The coblation wand is used to treat the telangiectasias. Bevacizumab is then injected into the nasal cavity bilaterally. CONCLUSION: The coblation wand, with or without adjunctive bevacizumab injection, is a technically feasible intervention for patients with HHT that all providers can perform.

[Topical anesthesia in flexible nasofibrolaryngoscopy]. / Anestesia tópica en la nasofibrolaringoscopia flexible.

INTRODUCTION: The emergence of flexible nasofibrolaryngoscopy in recent decades has facilitated the development of Otolaryngology and the nasofibrolaryngoscope has become an essential diagnostic tool for the otolaryngologist. However, its use is not without discomfort for the patient, which is why various options for topical anaesthesia have been proposed during the development of the technique. MATERIAL AND METHODS: This was a prospective, double blind, crossover study in patients with no history of nasal disease, through which we compared the use of topical anaesthetic (Lidocaine) + epinephrine, oxymetazoline and placebo. Using a visual analogue scale, the degree of discomfort was assessed during each scan. RESULTS: We evaluated 18 patients, 10 women (55.6%) and 8 men (44.4%), with a mean age of 28±4 years. The degree of disturbance generated by the scan with the application of lidocaine-epinephrine was 1.94; with oxymetazoline it was 3.78, and with placebo, 4.61. When the lidocaine-epinephrine solution was compared with oxymetazoline, there was a statistical significance in favour of lidocaine-epinephrine (P<0.05). When we compared the use of lidocaine-epinephrine with the placebo, the result was also statistically significant in favour of lidocaine-epinephrine (P<0.05). CONCLUSIONS: In this study we demonstrated that using lidocaine associated with epinephrine as a topical anaesthetic prior to flexible nasofibrolaryngoscopy decreases pain and feeling of discomfort for the patient. Consequently, we can recommend the use of topical nasal anaesthesia when performing this exploration.

In vitro metabolism of oxymetazoline: evidence for bioactivation to a reactive metabolite.

Oxymetazoline (6-tert-butyl-3-(2-imidazolin-2-ylmethyl)-2,4-dimethylphenol) has been widely used as a nonprescription nasal vasoconstrictor for >40 years; however, its metabolic pathway has not been investigated. This study describes the in vitro metabolism of oxymetazoline in human, rat, and rabbit liver postmitochondrial supernatant fraction from homogenized tissue (S9) fractions and their microsomes supplemented with NADPH. The metabolites of oxymetazoline identified by liquid chromatography (LC)/UV/tandem mass spectrometry (MS/MS), included M1 (monohydroxylation of the t-butyl group), M2 (oxidative dehydrogenation of the imidazoline to an imidazole moiety), M3 (monohydroxylation of M2), M4 (dihydroxylation of oxymetazoline), and M5 (dihydroxylation of M2). Screening with nine human expressed cytochromes P450 (P450s) identified CYP2C19 as the single P450 isoform catalyzing the formation of M1, M2, and M3. Glutathione conjugates of oxymetazoline (M6) and M2 (M7) were identified in the liver S9 fractions, indicating the capability of oxymetazoline to undergo bioactivation to reactive intermediate species. M6 and M7 were not detected in those liver S9 incubations without NADPH. Cysteine conjugates (M8 and M9) derived from glutathione conjugates and hydroxylated glutathione conjugates (M10 and M11) were also identified. The reactive intermediate of oxymetazoline was trapped with glutathione and N-acetyl cysteine and identified by LC/MS/MS. M6 was isolated and identified by one-dimensional or two-dimensional NMR as the glutathione conjugate of a p-quinone methide. We have shown the tendency of oxymetazoline to form p-quinone methide species via a bioactivation mechanism involving a CYP2C19-catalyzed two-electron oxidation. Nevertheless, we conclude that the formation of this reactive species might not be a safety concern for oxymetazoline nasal products because of the typical low-dose and brief dosage regimen limited to nasal delivery.

Oxymetazoline is equivalent to ciprofloxacin in preventing postoperative otorrhea or tympanostomy tube obstruction.

OBJECTIVE: To compare the effectiveness of ciprofloxacin and oxymetazoline solutions instilled after tympanostomy tube placement in the prevention of postoperative otorrhea and tube occlusion. STUDY DESIGN: Prospective cross-sectional series. METHODS: We reviewed all bilateral myringotomy and tube placement operations performed by two full-time attending pediatric otolaryngologists during a 9 month period. Data from 488 patients who underwent surgery for otitis media were collected. Demographic and clinical variables including age, sex, number of tube insertions in the past, previous adenoidectomy, type of effusion present at surgery, and type of drop prescribed postoperatively were recorded. All patients were evaluated in the office 2 to 4 weeks postoperatively. Multivariate logistic regression analysis was used to estimate the relationship of these variables with the occurrence of otorrhea and tube patency. Odds ratios were calculated. RESULTS: No significant differences in postoperative otorrhea or tube patency were found between ciprofloxacin (Ciloxan) and oxymetazoline solutions (Afrin, Visine LR). CONCLUSION: Oxymetazoline and ciprofloxacin solutions are equivalent in the prevention of postoperative otorrhea and tube occlusion after tympanostomy tube placement. The implications for medication cost and potential adverse reactions are discussed.

Early changes in insulin secretion and action induced by high-fat diet are related to a decreased sympathetic tone.

To evaluate the relationship between the development of obesity, nervous system activity, and insulin secretion and action, we tested the effect of a 2-mo high-fat diet in rats (HF rats) on glucose tolerance, glucose-induced insulin secretion (GIIS), and glucose turnover rate compared with chow-fed rats (C rats). Moreover, we measured pancreatic and hepatic norepinephrine (NE) turnover, as assessment of sympathetic tone, and performed hypothalamic microdialysis to quantify extracellular NE turnover. Baseline plasma triglyceride, free fatty acid, insulin, and glucose concentrations were similar in both groups. After 2 days of diet, GIIS was elevated more in HF than in C rats, whereas plasma glucose time course was similar. There was a significant increase in basal pancreatic NE level of HF rats, and a twofold decrease in the fractional turnover constant was observed, indicating a change in sympathetic tone. In ventromedian hypothalamus of HF rats, the decrease in NE extracellular concentration after a glucose challenge was lower compared with C rats, suggesting changes in overall activity. After 7 days, insulin hypersecretion persisted, and glucose intolerance appeared. Later (2 mo), there was no longer insulin hypersecretion, whereas glucose intolerance worsened. At all times, HF rats also displayed hepatic insulin resistance. On day 2 of HF diet, GIIS returned to normal after treatment with oxymetazoline, an alpha(2A)-adrenoreceptor agonist, thus suggesting the involvement of a low sympathetic tone in insulin hypersecretion in response to glucose in HF rats. In conclusion, the HF diet rapidly results in an increased GIIS, at least in part related to a decreased sympathetic tone, which can be the first step of a cascade of events leading to impaired glucose homeostasis.

Controlling bleeding from superficial wounds by the use of topical alpha adrenoreceptor agonists spray. A randomized, masked, controlled study.

In an attempt to determine whether alpha adrenergic agonists sprayed directly over the wound are able to reduce a superficial bleeding, phenylephrine (0.25%), oxymetazoline (0.05 and 0.25%) and saline (0.9%) were tested in a rat model. The study was randomized, controlled and quantitative. A total of four incisions were made in each rat, and each solution was sprayed directly on the incision according to a specific protocol. The bleeding times were measured and summed up. Biases were minimized by the fact that each rat received all four solutions, including the control, in all possible combinations. The mean bleeding time after spraying phenylephrine (0.25%) was significantly shorter than the mean bleeding time after spraying saline (1.90 +/- 0.14 min versus 4.80 +/- 0.43 min, respectively, P < 0.001) and significantly shorter than the mean bleeding time after spraying oxymetazoline (0.05 or 0.25%: 4.46 +/- 0.54 and 5.50 +/- 0.58 min, respectively, P < 0.001). No statistically significant difference was found between the mean bleeding time after spraying oxymetazoline (0.05 or 0.25%) compared with saline. We conclude that sprayed phenylephrine (0.25%) can be used for reducing superficial bleedings. This method is simple, cost-effective, does not cause further trauma to the tissue, and can be used to treat several bleedings simultaneously (especially abrasions and lacerations) with a single application, without the need for direct physical contact with the bleeding sites. The method is apparently safe, but further studies are needed to test the systemic effect of the sprayed solution.

Effects of acute, repeated and chronic variable stress on in vivo tyrosine hydroxylase activity and on alpha(2)-adrenoceptor sensitivity in the rat brain.

We assessed the effects of a single tail pinch and two chronic stress regimes, repeated and variable, on in vivo tyrosine hydroxylase activity and on alpha2-adrenoceptor sensitivity in two brain regions. After administering a 3,4-dihydroxyphenylalanine (DOPA) decarboxylase inhibitor, tyrosine hydroxylase activity, measured as the accumulation of DOPA, and noradrenaline (NA) content were determined by using high-performance liquid chromatography. A single tail pinch for 5 min induced an enhancement of DOPA content in hippocampus (28%) and hypothalamus (67%) which was still present 24 h later. This increase could account for the lack of changes in NA content in both regions after the application of this stressor. However, tyrosine hydroxylase activity was unmodified 24 h after exposure to both repeated (5 min of tail pinch, twice daily, for 14 days) and chronic variable stress (one of 5 different stressors, once daily, for 14 days) although there was an enhancement of NA levels in hippocampus (45 and 54%, respectively) and hypothalamus (24.5 and 36%, respectively). The sensitivity of the alpha2-adrenoceptors which regulate [3H]-NA release in hippocampal and hypothalamic synaptosomes was not modified by the acute or chronic stress protocols assayed. The results show that both paradigms of chronic stress had similar effects on the noradrenergic indices evaluated.

Topical nasal anesthesia and laryngopharyngeal sensory testing: a prospective, double-blind crossover study.

Laryngopharyngeal sensory discrimination testing (LPSDT) has become a popular means of detecting sensory deficits in patients with voice and/or swallowing complaints. During this procedure, transnasal fiberoptic laryngoscopy (TFL) using a specialized fiberoptic scope is performed in order to deliver discrete pulses of air to the laryngopharyngeal mucosa. Historically, topical anesthesia has been applied to the nasal mucosa to lessen discomfort during TFL. Because of the concern that topical nasal anesthesia could also anesthetize the laryngopharynx, it is usually not used during sensory testing. To prospectively compare LPSDT scores after the nasal administration of cocaine hydrochloride, oxymetazoline hydrochloride, and saline solution, we prospectively evaluated 15 subjects undergoing LPSDT. Each had the procedure performed on 3 separate occasions. Before examination, each patient was administered either 4% cocaine, 0.05% oxymetazoline, or saline solution by atomizer (2 sprays of 1-second duration to each naris). By the conclusion of the study, each patient had undergone sensory testing with each of the test agents. During each examination, the minimal air pulse eliciting the laryngeal adductor reflex was recorded for both sides of the laryngopharynx. Both patient and examiner were blinded to the test agent used. The mean sensory score for saline solution was 3.9 mm Hg. The sensory scores for oxymetazoline and cocaine were 3.4 and 3.5 mm Hg, respectively. When compared to saline solution and oxymetazoline independently, sensory testing of the laryngopharynx during which the nose was anesthetized with cocaine resulted in similar thresholds for eliciting the laryngeal adductor reflex (p = .40 and p = .85). We conclude that topical anesthesia can be applied to the nasal cavity during LPSDT without altering laryngeal sensation.

Segmental analysis of nasal cavity compliance by acoustic rhinometry.

To explore the determinants of possible collapse of the nasal valve region, a common cause of nasal obstruction, we evaluated the mechanical properties of the nasal wall. In this study, we determined the nasal cross-sectional area-to-negative pressure ratio (nasal wall compliance) in the anterior part of the nose in six healthy subjects by measuring nasal area by acoustic rhinometry at pressures ranging from atmospheric pressure to a negative pressure of -10 cmH(2)O. Measurements were performed at baseline and after nasal mucosal decongestion (oxymetazoline). At baseline, nasal wall compliance increased progressively from the nasal valve (0.031 +/- 0.016 cm2/cmH(2)O, mean +/- SD) to the anterior and medial part of the inferior turbinate (0.045 +/- 0.024 cm2/cmH(2)O) and to the middle meatus region (0.056 +/- 0.029 cm2/cmH(2)O). After decongestant, compliances decreased and became similar in the three regions. On the basis of these results, we hypothesize that compliance of the nasal wall is partly related to mucosal blood volume and quantity of vascular tissue, which differ in the three regions, increasing from the nasal valve to the middle meatus.

Desensitization of alpha(2)-adrenoceptors which regulate noradrenaline synthesis and release after chronic treatment with clorgyline in the rat brain.

The sensitivity of alpha(2)-adrenoceptors which regulate synthesis and release of noradrenaline was investigated in hippocampus, parietal cortex, and hypothalamus of rats treated with clorgyline. After administering a DOPA decarboxylase inhibitor, the in vivo tyrosine hydroxylase activity and the noradrenaline content were evaluated. Acute and chronic treatment with clorgyline led to both increases of noradrenaline levels and decreases of tyrosine hydroxylase activity, determined as the accumulation of DOPA. Whereas the alpha(2)-adrenoceptor agonist clonidine induced a similar reduction in tyrosine hydroxylase activity in the group subjected to the acute treatment and in the control group, it failed to do so after chronic clorgyline treatment. In hippocampal and cortical synaptosomes, a reduction in the sensitivity of alpha(2)-adrenoceptors which regulate [(3)H]noradrenaline release, reflected by the shift to the right of the concentration-effect curves for oxymetazoline, was also found after the repeated treatment. These results indicate a desensitization of alpha(2)-adrenoceptors after chronic treatment with clorgyline.

Molecular cloning and functional expression of the guinea pig alpha(1a)-adrenoceptor.

In the present paper, the cloning and expression of the guinea pig alpha(1A)-adrenoceptor is presented. The nucleotide sequence had an open reading frame of 1401 bp that encoded a 466 amino-acid protein with an estimated molecular mass of approximately 51.5 kDa. When the clone was expressed in Cos-1 cells, specific high-affinity binding of [(3)H]prazosin and [(3)H]tamsulosin was observed. Chloroethylclonidine treatment of membranes slightly decreased the total binding with both radioligands. Binding competition experiments using [(3)H]tamsulosin showed the following potency order: (a) for agonists: oxymetazoline >>epinephrine>norepinephrine>methoxamine, and (b) for antagonists: prazosin> or 5-methyl-urapidil=benoxathian>phentolamine>>BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4,5]decane-7,9-dione). Photoaffinity labeling using [(125)I-aryl]azido-prazosin revealed a major broad band with a molecular mass between 70 and 80 kDa. The receptor was functional, as evidenced by an epinephrine-increased production of [(3)H]inositol phosphates that was blocked by prazosin.

Comparison of oxymetazoline and lidocaine versus cocaine for outpatient dacryocystorhinostomy.

PURPOSE: To evaluate the effectiveness of oxymetazoline combined with lidocaine versus cocaine for outpatient dacryocystorhinostomy (DCR). METHODS: Twenty-seven patients underwent DCR with a combination of oxymetazoline 0.05% nasal spray and lidocaine 4% spray/pledgetts (oxy/lido) and were compared with 28 patients who underwent DCR with cocaine 4% pledgetts for nasal anesthesia and vasoconstriction. Most of the patients underwent standard external approach DCR: five patients in the oxy/lido group and four patients in the cocaine group underwent endoscopic DCR. RESULTS: Patients in both groups reported being comfortable during and immediately after surgery. Visualization of the operative field was adequate, and surgery was successfully completed in all cases. Mean blood loss was 6.3 ml (+/-6.0) in the oxy/lido group and 7.3 ml (+/-6.4) in the cocaine group (p = 0.541). There were no cases of postoperative epistaxis requiring nasal packing or hospital admission in the oxy/lido group, whereas one patient in the cocaine group developed epistaxis 8 days after surgery, which required treatment. Success rate was similar in the two groups. CONCLUSIONS: The combination of oxymetazoline and lidocaine is effective for outpatient dacryocystorhinostomy. Patient comfort was adequate and blood loss not significantly different in comparison to cocaine. This combination provides effective nasal anesthesia and vasoconstriction, while avoiding the "hassle" and potentially greater risks associated with cocaine.