Efficacy of a topical nasal decongestant in different formulations: the effect of viscosity.

Factors affecting the absorption of drugs through the nasal mucosa are increasingly being studied. Dosage form factors, i.e. the viscosity of the excipients, have been claimed to be of importance for enhanced nasal absorption due to prolongation of contact time between drug and mucosa. In the present study, a comparison was made of the effect of a local nasal sympathomimetic when administered intranasally in formulations with different viscosities. Volunteers received the test drugs as nasal sprays in a randomized cross-over design by a rhinomanometric technique, the effect of the drug being recorded for up to 5 h after administration. No significant differences in effects were observed when the test formulations were compared.     

Dose-response relationship of a topical nasal decongestant: phenylpropanolamine

By means of anterior rhinomanometry, the decongestant effect of topically applied phenylpropanolamine (PPA) was evaluated in 40 patients with nasal obstruction. A dose-response relation was obtained for 0.5, 2.5 and 5.0% PPA solution, with the maximum effect (40% decongestion) found with the 2.5% solution. The decongestant effect was comparable to that induced by physical exercise (50% decongestion). It is concluded that PPA nose-drops are effective and offer an attractive alternative to some of the commonly used nasal decongestants.     

Nasal airflow asymmetry and the effects of a topical nasal decongestant.

Nasal airway resistance (NAR) is normally asymmetrical due to the nasal cycle. The aims of this study were to determine the degree of this asymmetry in healthy subjects and those with acute rhinitis associated with common cold, and to investigate how the administration of a topical nasal decongestant (xylometazoline) influenced the asymmetry in NAR. Unilateral NAR was measured by active anterior rhinomanometry, and was shown to be asymmetrical in both healthy subjects and those suffering with acute rhinitis. The asymmetry in NAR was greater in those with acute rhinitis than in the healthy group, with a ratio between "high" and "low" sides of 2.3:1 in the rhinitis group compared to a ratio of 1.7:1 in the healthy subjects. Administration of a topical nasal decongestant caused a significant decrease in total NAR in both groups and abolished the asymmetry in NAR in the healthy subjects (ratio is 1:1 after decongestion). However, significant asymmetry of NAR was still present in the group with acute rhinitis following the administration of decongestant (ratio is 1.5:1 after decongestion). These findings show that the normal asymmetry in NAR was increased during acute rhinitis associated with common cold, and that in healthy subjects (but not in those with rhinitis) the asymmetry was abolished by administration of a topical decongestant. The results are discussed in relation to nasal sympathetic tone and nasal blood flow.     

Oral decongestant in acute otitis media. Results of a double-blind trial.

In order to investigate the influence of an orally administered decongestant, norephedrine, upon the clinical course of acute otitis media and tubal function, a double-blind trial was performed in Copenhagen in December, 1976-February, 1977, in which 93 patients, aged 6 months to 10 years, with 135 ears with acute otitis media, were treated either with norephedrine or placebo in a randomized order. Most other treatment was avoided except for pain-relieving baby aspirins. The effect of norephedrine seemed to be no other than that of placebo. Because of this inefficacy of norephedrine the authors have, therefore, a material of patients with acute otitis media where the main treatment was pain-relieving aspirin. The use and abuse of antibiotics in the treatment of this disease are discussed, and the authors stress the necessity of performing controlled studies of the efficacy of antibiotics in acute otitis media, since such studies do not exist.     

常用减充血剂对鼻黏膜纤毛毒性的观察

目的:观察减充血剂对鼻黏膜纤毛的毒性作用,为临床选择合适的鼻腔减充血剂提供参考。方法:①选健康志愿者100例,分别用0.05%、0.025%盐酸羟甲唑啉,1.0%、0.5%麻黄素喷鼻7d,进行糖精试验以检测鼻黏膜纤毛输送率(MTR),并与对照组进行比较。②用药7d后每组各取1例下鼻甲黏膜进行扫描电镜观察。结果:①用药7d后,0.05%盐酸羟甲唑啉组鼻黏膜纤毛MTR为(7.64±1.56)mm/min;0.025%盐酸羟甲唑啉组为(7.46±1.65)mm/min,其差异无统计学意义(P>0.05);1.0%麻黄素组为(4.73±2.03)mm/min;0.5%麻黄素组为(4.38±2.04)mm/min,其差异亦无统计学意义(P>0.05)。0.05%、0.025%盐酸羟甲唑啉组分别与对照组[(7.14±1.76)mm/min]比较,差异无统计学意义(均P>0.05);1.0%、0.5%麻黄素组分别与对照组比较,差异有统计学意义(均P<0.01)。0.05%、0.025%盐酸羟甲唑啉组分别与1.0%、0.5%麻黄素组比较,差异有统计学意义(均P<0.05)。②电镜观察:1.0%、0.5%麻黄素组黏膜上皮纤毛脱落,0.05%、0.025%盐酸羟甲唑啉组纤毛排列整齐。结论:麻黄素对鼻黏膜纤毛有不良影响;盐酸羟甲唑啉对鼻黏膜纤毛无明显影响,没有破坏鼻黏膜纤毛的正常生理功能,是理想的鼻腔减充血剂。     

局部用减充血剂后出现鼻阻力反弹现象的研究

目的：探讨局部用减充血剂对鼻粘膜血管运动的调控的影响,为研究和防治药物性鼻炎提供理论依据。方法：调查９２例急,慢性鼻炎患者分别使用４种不同减充血剂后鼻塞变化的情况,并通过前鼻测压法观察部分患者用药后鼻阻力的反弹现象。结果：４组被调查者中分别有６３．５％,３１．２％,３２．２％,８．６％的患者出现鼻塞反弹性加重;３组被检测者中分别有５０％,２０％和７５％;出现鼻阻力反弹性升高。     

The nasal decongestant effect of xylometazoline in the common cold

BACKGROUND: Xylometazoline is a nasal decongestant spray that constricts nasal blood vessels and increases nasal airflow, enabling patients with a blocked nose to breathe more easily. The purpose of this study was to characterize objectively and subjectively the decongestant and additional effects of xylometazoline in the common cold. METHODS: A double-blind, placebo-controlled, parallel group study was performed. Patients with a common cold (n = 61) were treated with xylometazoline 0.1% (n = 29) or placebo (saline solution; n = 32; 1 spray three times a day for up to 10 days). The primary objective was to determine the decongestant effect (nasal conductance); the secondary objectives were to determine the peak subjective effect (visual analog scale), duration of relief of nasal congestion, total and individual cold symptoms and general well-being (patients' daily diary), and adverse events (AEs). RESULTS: The decongestant effect of xylometazoline was significantly greater than placebo, as shown by the nasal conductance at 1 hour (384.23 versus 226.42 cm(3)/s; p 相似文献   

No effect of a nasal decongestant on eustachian tube function in children with ventilation tubes

OBJECTIVE: The aim of the study was to assess the effect of a topical decongestant on eustachian tube function in children with ventilation tubes because of persistent otitis media with effusion. STUDY DESIGN: A randomized, double-blinded, placebo-controlled study. METHODS: At the outpatient departments of a secondary referral hospital and a tertiary referral hospital, eustachian tube function was measured before and after intranasal administration of five drops of 0.05% xylometazoline hydrochloride or placebo in 80 randomly selected children with ventilation tubes because of otitis media with effusion. RESULTS: Xylometazoline nose drops had no effect on the ventilatory or the protective function of the eustachian tube. CONCLUSIONS: Topical decongestants do not have a positive effect on eustachian tube function in children. Therefore, the use of topical decongestants to prevent or treat otitis media with effusion in children is not justified and should be discouraged.     

Comparative oral and topical decongestant effects of phenylpropanolamine and d-pseudoephedrine

Nonselective adrenergic alpha-agonists such as phenylpropanolamine and d-pseudoephedrine are widely used as decongestants to treat nasal congestion associated with a variety of nasal diseases. Although the activity of these drugs is well established in clinical studies, a direct comparison of their nasal decongestant effect as determined by changes in nasal cavity dimensions and nasal architecture has not been studied. Using acoustic rhinometry, we evaluated the effects of these drugs on nasal cavity volume, minimum cross-sectional area (Amin), and the distance from the nosepiece to the Amin (Dmin) in a feline, pharmacological model of nasal congestion. Administration of topical compound 48/80 (1%), a mast cell histamine liberator, into the left nasal passageway decreased nasal volume by 66%, reduced Amin by 51%, and increased Dmin by 116%. The congestive responses to compound 48/80 (1%) were reproducible through six weeks. In a subset of cats, the nasal cavity volume effect of repetitive exposure to compound 48/80, given once every two weeks for six weeks, was not different from the nasal responses after the initial exposure to compound 48/80. Pretreatment with oral phenylpropanolamine (10 mg/kg) or oral d-pseudoephedrine (10 mg/kg) attenuated the nasal effects of compound 48/80, but were associated with a pronounced increase in systolic blood pressure of +51 and +82 mmHg, respectively. A similar decongestant profile was observed with phenylpropanolamine (1%) and d-pseudoephedrine (1%) when given topically. Topical phenylpropanolamine (1%) and d-pseudoephedrine (1%) 45 minutes after dosing increased blood pressure +44 and +17 mmHg, respectively, over control animals. We conclude that oral and topical phenylpropanolamine and d-pseudoephedrine display equieffective nasal decongestant activity and produce similar cardiovascular profiles characterized by significant increases in blood pressure.     

A new in vitro method of decongestant assay of nasal mucosa: a preliminary report

BACKGROUND: The calculation of cell planar surface area, successfully used for glomerular mesangial cell-altered contractility, also is a reasonable methodology to assess nasal mucosal contractility. A simple technique that works particularly well with vasoconstriction-inducing agents has been introduced to test the effects of several drugs on patient turbinate nasal mucosa in vitro. This report will introduce this technique and present some of the initial findings. METHODS: We tested epinephrine, norepinephrine, pseudoephedrine HCl, and methoxamine, respectively, for effectiveness as a vasoconstricting drug. We also tested the effectiveness of verapamil as a vasodilating drug. A piece of nasal mucosa approximately 3 x 4 mm in size was mounted with a 27-gauge needle and submersed in a 4-mL muscle bath in a Petri dish at room temperature. The bath consisted of 4 mL of Kreb's solution. We recorded the decrease of nasal mucosa planar surface area in response to the application of vasoconstricting agents, as measured using a digital microscope connected to a Pentium III with morphometric software, as the estimated degree of contraction. A photograph of the same mucosa was taken every 3 minutes for a total period of 18 minutes. RESULTS: Nasal mucosa that was mounted in a muscle bath in a Petri dish and treated with a small dose of a nasal decongestant was l observed to contract. Drug dosage determined the degree of nasal mucosa contraction. Nasal mucosa similarly prepared but treated with a vasodilating agent, such as verapamil, exhibited a relaxation response only when pretreated with a vasoconstricting agent, such as methoxamine. Both vasoconstricting and vasodilating drugs induce dose-related responses in planar surface calculation. CONCLUSION: In this study, drug dosage determined the degree of nasal mucosa contraction. We also found that the rate of contraction and percent of contraction were dose dependent. We believe this new method will prove useful in studying the effects of drugs on nasal blood vessels.     

Efficacy of acupuncture as a treatment for tinnitus: a systematic review

BACKGROUND: Tinnitus is a prevalent condition for which patients may seek treatment with acupuncture since no conventional treatment has been shown to be effective. OBJECTIVE: To summarize and critically review all randomized controlled trials on the efficacy of acupuncture as a treatment for tinnitus. DATA SOURCES: Four independent computerized literature searches (MEDLINE, Cochrane Controlled Trials Register, Embase, and CISCOM) were conducted in December 1998 using the key words acupuncture and tinnitus. STUDY SELECTION: All randomized controlled trials that compared any form of acupuncture with any control intervention in the treatment of tinnitus were included. DATA EXTRACTION: Data were extracted by 2 authors independently. The methodological quality of the included randomized controlled trials was assessed using the Jadad score. DATA SYNTHESIS: Six randomized controlled trials were included in the review, 4 of which used crossover design. Four studies used manual acupuncture and 2 used electroacupuncture. Five of 6 studies used inconsistent acupoints. Three studies scored 3 points or more on the Jadad scale. MAIN OUTCOME MEASURES: Outcome measurements were visual analog scale scores for loudness, annoyance, and awareness of tinnitus; subjective severity scale scores for tinnitus; or Nottingham Health Profile scores. RESULTS: Two unblinded studies showed a positive result, whereas 4 blinded studies showed no significant effect of acupuncture. CONCLUSION: Acupuncture has not been demonstrated to be efficacious as a treatment for tinnitus on the evidence of rigorous randomized controlled trials.