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Xylometazoline

(Synonyms: Ba-11391, Otrivine, Rhinoxilin) 目录号 : GC26085

Xylometazoline (Ba-11391, Otrivine, Rhinoxilin) is a nasal vasoconstricting decongestant drug which is used to improve symptoms of nasal congestion, allergic rhinitis, and sinusitis.

Xylometazoline Chemical Structure

Cas No.:526-36-3

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5mg
¥614.00
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25mg
¥1,874.00
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产品描述

Xylometazoline (Ba-11391, Otrivine, Rhinoxilin) is a nasal vasoconstricting decongestant drug which is used to improve symptoms of nasal congestion, allergic rhinitis, and sinusitis.

Chemical Properties

Cas No. 526-36-3 SDF Download SDF
别名 Ba-11391, Otrivine, Rhinoxilin
分子式 C16H24N2 分子量 244.38
溶解度 DMSO: 49 mg/mL (200.51 mM);Water: Insoluble;Ethanol: 49 mg/mL (200.51 mM) 储存条件 Store at -20°C
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1 mM 4.092 mL 20.4599 mL 40.9199 mL
5 mM 0.8184 mL 4.092 mL 8.184 mL
10 mM 0.4092 mL 2.046 mL 4.092 mL
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Research Update

Effects of intranasal Xylometazoline, alone or in combination with ipratropium, in patients with common cold

Curr Med Res Opin 2010 Apr;26(4):889-99.PMID:20151787DOI:10.1185/03007991003648015.

Background: Common cold is one of the most prevalent conditions that family doctors encounter. One of the first symptoms to occur is nasal congestion, which can have a negative impact on daily life and prompts many patients to seek treatment for relief. Xylometazoline nasal spray (Otrivin*) is a topical decongestant that has been used successfully for many years and is generally recognized as an effective and safe therapy. However, most studies have investigated its clinical efficacy in healthy patients and few have included patients with common cold. Scope: To review the published clinical efficacy and safety of Xylometazoline alone and in combination in the management of nasal congestion in patients with common cold. Literature searches of PubMed and the Cochrane Library were conducted to obtain published open or blinded, randomized, placebo- or active-controlled studies on the use of Xylometazoline hydrochloride for the symptomatic relief of nasal congestion in patients with common cold. Searches included papers published in English only, up to September 2009. Findings: Despite the small number of studies identified in common cold (n = 4), as per search criteria defined, intranasal Xylometazoline quickly and effectively relieved nasal congestion. When used alone, Xylometazoline had a clinically relevant decongestant effect that was significantly superior for up to 10 hours compared with placebo. The superior decongestant effect with Xylometazoline led to high patient satisfaction with treatment. When used in combination with ipratropium bromide, nasal congestion and rhinorrhoea were treated simultaneously, leading to significantly higher patient general impression scores compared with either agent used alone. Xylometazoline was well tolerated, with generally mild to moderate nasal-related side effects (e.g. epistaxis in 3.4% of patients, and blood-tinged mucus in 10-26% of patients) that were easily resolved; the most frequently reported non-nasal AEs were headache (3.4%) and period pain (10.3%); no cases of sedation were reported. As expected, no rhinitis medicamentosa or rebound congestion was noted with short-term use (<10 days). No clinically important differences in ciliary motility and mucociliary clearance were observed. Xylometazoline does not result in sympathomimetic systemic side effects seen with oral decongestants (e.g. pseudoephedrine, phenylephrine). Conclusions: The few studies available in common cold suggest that intranasal Xylometazoline provides fast and effective relief of nasal congestion and is well tolerated. When Xylometazoline is used in combination with ipratropium, patients with common cold experience the additive benefit of nasal congestion and rhinorrhoea being treated simultaneously.

Sinusitis (acute)

BMJ Clin Evid 2011 Dec 21;2011:0511.PMID:22189346doi

Introduction: Acute sinusitis is defined pathologically, by transient inflammation of the mucosal lining of the paranasal sinuses lasting less than 4 weeks. Clinically, it is characterised by nasal congestion, rhinorrhoea, facial pain, hyposmia, sneezing, and, if more severe, additional malaise and fever. It affects 1% to 5% of the adult population each year in Europe. Methods and outcomes: We conducted a systematic review and aimed to answer the following clinical questions: What are the effects of treatments in people with clinically diagnosed acute sinusitis, and in people with radiologically or bacteriologically confirmed acute sinusitis? We searched: Medline, Embase, The Cochrane Library, and other important databases up to June 2011 (Clinical Evidence reviews are updated periodically; please check our website for the most up-to-date version of this review). We included harms alerts from relevant organisations such as the US Food and Drug Administration (FDA) and the UK Medicines and Healthcare products Regulatory Agency (MHRA). Results: We found 19 systematic reviews, RCTs, or observational studies that met our inclusion criteria. We performed a GRADE evaluation of the quality of evidence for interventions. Conclusions: In this systematic review we present information relating to the effectiveness and safety of the following interventions: antibiotics (amoxicillin, amoxicillin-clavulanic acid [co-amoxiclav], doxycycline, cephalosporins, macrolides; different doses, long-course regimens), antihistamines, decongestants (Xylometazoline, phenylephrine, pseudoephedrine), saline nasal washes, steam inhalation, and topical corticosteroids (intranasal).

Efficacy and safety of intranasal Xylometazoline and ipratropium in patients with common cold

Expert Opin Pharmacother 2009 Apr;10(5):889-908.PMID:19351236DOI:10.1517/14656560902783051.

Background: Many over-the-counter medications are available to treat common cold nasal symptoms, but patients may be unsure which one to use. Methods: This review assesses two widely used intranasal treatments for nasal congestion and rhinorrhea in the common cold: Xylometazoline hydrochloride and ipratropium bromide. Results: Xylometazoline quickly and effectively relieves nasal congestion, while ipratropium is effective at reducing rhinorrhea. When used in combination, a novel approach to treatment, nasal congestion and rhinorrhea are treated simultaneously, providing effective relief from two of the most troublesome symptoms of the common cold Both drugs are well tolerated, with only mild to moderate, nasal-related side effects. Conclusions: The efficacy and safety of the combination product suggest that it should be used first-line in the symptomatic relief of nasal congestion and rhinorrhea, before the use of oral treatments.

Use of Xylometazoline in hospitalised infants: is it safe? A retrospective cohort study

Arch Dis Child 2023 Jan;108(1):62-66.PMID:36171065DOI:10.1136/archdischild-2022-324127.

Objective: When infants suffer from nasal congestion, Xylometazoline spray or drops can be effective to facilitate breathing and drinking. However, case reports on side effects have resulted in international warnings regarding use of Xylometazoline in infants. Nevertheless, the incidence of these side effects in hospitalised infants is unknown. Design: Retrospective cohort study. Setting: Teaching hospital between 2017 and 2021. Patients: Infants under 2 years of age. Exposure: Receiving either saline-only (unlimited frequency, concentration 0.9%) or in combination with Xylometazoline (maximum three times daily, concentration 0.025%). Main outcome measures: Predefined potential side effects (events), including among others apnoea, nausea, bradycardia, cyanosis and nosebleeds, were extracted from patient records, and the probability to be caused by saline only or xylometazoline-saline was determined using the ADR Probability Scale. Results: We included 898 admitted children during 1285 treatment episodes who received saline with or without Xylometazoline. 26 events occurred in the saline-only group (incidence 20.0/100 treatment episodes), and 117 events occurred in the Xylometazoline saline group (incidence of 10.5/100 treatment episodes), which was significantly lower (OR 0.47 95% CI 0.29 to 0.75, p=0.002). No definite linked or life-threatening events were found. Three nosebleeds had a probable link to the use of xylometazoline-saline, and all other events could only possibly be linked to saline-only or Xylometazoline saline use. The incidence of all events was higher in the saline-only group as compared with the Xylometazoline saline group, except nausea, which had a similar occurrence (p=0.65). Results were very similar across (gestational) age groups, gender and reasons for admission. Conclusion: The use of low-dose Xylometazoline seems to be safe in hospitalised infants.

Topical nasal Xylometazoline for flexible bronchoscopy (VAIN): A randomized, double-blind, placebo-controlled trial

Respir Investig 2021 May;59(3):350-355.PMID:33518471DOI:10.1016/j.resinv.2020.12.004.

Background: The role of topical nasal vasoconstrictor administration during flexible bronchoscopy is unclear. Methods: Consecutive subjects undergoing flexible bronchoscopy were randomized to receive either topical Xylometazoline (0.1%) or placebo (saline nasal spray, 0.74% w/v isotonic solution) before bronchoscopy. Background topical anesthesia included 2% nasal lignocaine gel, pharyngeal spray of 10% lignocaine, and 1% lignocaine solution for spray-as-you-go administration. The primary outcome was the operator rated ease of nasal negotiation of the bronchoscope on the visual analog scale (Negotiation VAS). Secondary objectives included assistant rated facial pain scale score, patient-rated nasal pain score (Pain VAS), time to reach the vocal cords after bronchoscope insertion, operator rated nasal mucosal trauma score (Trauma VAS), hemodynamic changes, and complications between the groups. Results: In all, 148 subjects were recruited and randomized to the placebo (73) and Xylometazoline groups (75). Operator rated ease of nasal bronchoscope negotiation (Negotiation VAS) was similar in both the groups [Median (IQR), 1 (1-2) in both groups, p = 0.79]. There were no differences in the other outcomes including assistant rated score of facial pain [(Median (IQR), 2 (2-4) placebo and 2 (2-4) Xylometazoline, p = 0.36], Pain VAS [Median (IQR), placebo 2 (1-2) and Xylometazoline 2 (1-3), p = 0.28], Trauma VAS, [Median (IQR), placebo 1 (0-2) and Xylometazoline 1 (0-1), p = 0.28], hemodynamic changes, or complications between the two groups. Conclusion: The findings of this study do not support the administration of topical nasal Xylometazoline in flexible bronchoscopy. Trial registry: Trial registered on Clinicaltrials.gov, www.clinicaltrials.govNCT03424889, on January 02, 2018.