Vascular effects of topical oxymetazoline on human nasal mucosa

Oxymetazoline, a derivative of imidazoline, is a widely used nasal decongestant. In contrast to other topical decongestants related to phenylephrine, sympathomimetic amines, it also induces a reduced nasal mucosal blood flow. The purpose of the present investigation was to evaluate the duration of effect of oxymetazoline on nasal airway resistance and mucosal blood flow. During the eight hours of study, the blood flow was reduced by 30-40 per cent in six hours. A similar decongestant effect of about 30 per cent was found during the same interval. The pharmacological profile of oxymetazoline seems questionable, since a reduced nasal mucosal blood flow might not be of value in the treatment of upper airways infections.     

Effects of sustained-release oral phenylpropanolamine on the nasal mucosa of healthy subjects

Phenylpropanolamine (PPA) is widely used as a nasal decongestant administered orally in sustained release preparations and, in Sweden, the recommended dose nowadays is 50 mg twice daily for adults. The aim of this placebo-controlled, cross-over study was to determine the onset and duration of the decongestive effect of 50 and 100 mg PPA in 15 healthy subjects. All subjects arrived at the laboratory at 07.30 h. After an acclimatisation, the nasal mucosal baseline was established with rhinostereometry and the minimal cross-sectional area was measured using acoustic rhinometry. The systolic and diastolic blood pressures were also determined. Then all subjects were given their study drugs for the day and the measurements were repeated every hour for 8 h. This procedure was repeated for 3 days at 48 h intervals between the days. For purposes of comparison, the decongestive effect of oxymetazoline nasal spray was studied on a separate day. The decongestive effect of 100 mg PPA was similar to that of topical oxymetazoline. It develops after 1 h and lasts for approximately 6 h. The decongestive effect of oxymetazoline was significantly greater than that of 50 mg PPA and that of 100 mg PPA was significantly greater than that of 50 mg PPA using rhinostereometry, but not when using acoustic rhinometry. However, 50 mg PPA had no significant decongestive effect, compared with placebo, with rhinostereometry or acoustic rhinometry. In the first 3 h after administration of PPA, there was a dose-response increase in the systolic and diastolic blood pressures, which then returned to baseline. In conclusion, this study shows that PPA in double the recommended dose, i.e. 100 mg, has a significant decongestive effect on the nasal mucosa in healthy subjects. However, when the dose of PPA is increased the systolic and diastolic blood pressures also increase.     

Ultrastructure of human nasal mucosa

This thesis describes the ultrastructure of human nasal mucosa, based upon surgical biopsy specimens. The intent of the study is to characterize the normal ultrastructure of human nasal mucosa with emphasis upon the difference between olfactory and respiratory epithelia. Other nasal epithelia (anterior, sinus, and posterior) are reviewed briefly for comparison only. Several pathological examples of the olfactory and respiratory epithelia are also briefly presented for contrast.     

Effects of cocaine on human nasal mucosa

Summary The effects of cocaine on the contractile response of isolated human nasal mucosal blood vessels to field stimulation and methoxamine were investigated. Results showed that cocaine antagonized methoxamine and inhibited field stimulation. The drug increased resting tension in human nasal mucosa in vitro through direct actions and potentiated mucosal contractions by norepinephrine and epinephrine. The study indicated that high concentrations of cocaine may actually antagonize -adrenoceptors, but these concentrations are not necessary in eliciting desired degrees of vasoconstriction in nasal blood vessels while being applied as a local anesthetic.     

Effects of amphetamine on human nasal mucosa

The present study was devised to determine the effects of amphetamine on the sympathetic function of human nasal mucosa. A tissue bath method was employed on the vitro preparations of nasal turbinate mucosa from adult patients with nasal allergies or hypertrophic rhinitis. The effects of amphetamine on the contractile response of isolated human nasal mucosal blood vessels were investigated following electrical field stimulation and methoxamine. The results showed that amphetamine inhibited field stimulation and antagonized the effects on mucosal contraction induced by methoxamine. Likewise, the drug increased mucosal basal tension but had local drug toxicity when a 10^–4 M solution was used. Amphetamine could potentiate mucosal contraction induced by norepinephrine or epinephrine. The study indicated that amphetamine may increase sympathetic function by potentiating the effect of norepinephrine and that high concentrations of amphetamine may actually antagonize a-adrenoceptors.     

Effects of glypressin on human nasal mucosa

The effect of intravenous and topical glypressin, a triglycyl hormonogen of vasopressin, on the nasal mucosa was evaluated in healthy subjects. A dose-dependent reduction of nasal blood flow resulted from both intravenous and topical glypressin. The effect of the latter in gel form lasted 2 hours. Glypressin was also found to decongest the nasal mucosa. Topical application of glypressin gel might be an alternative to conventional treatment with intranasal packing in nose-bleed.     

Functional effects of phosphoramidon and captopril on exogenous neuropeptides in human nasal mucosa

The functional effects of the intranasal application of exogenous vasoactive intestinal polypeptide (VIP), substance P (SP) and calcitonin gene-related peptide (CGRP) were evaluated in 12 healthy volunteers before and after neutral endopeptidase (NEP) inhibition with phosphoramidon (PA) and angiotensin-converting enzyme (ACE) inhibition with captopril. The three neuropeptides increased nasal airway resistance (NAR) measured by anterior rhinomanometry and superficial capillary blood flow measured by laser Doppler flowmetry (LDF). After pretreatment of the nasal mucosa with PA, the effects of VIP, SP and CGRP on the LDF signal, NAR and mucus production were potentiated, whereas local pretreatment with captopril did not modify these functional effects. These observations suggest that NEP, but not ACE, may participate in the catabolism of neuropeptides when applied directly to the human nasal mucosa. Furthermore, since these neuropeptides induced nasal obstruction, increased blood flow and rhinorrhea, a decreased activity of the enzymes involved in their degradation could be involved in the physiopathology of rhinitis symptoms.     

Histochemical study of human nasal mucosa

The histochemical study of the fetal nasal mucosa collected from fetus of different months is reported. The concentration of succinic dehydrogenase and acid phosphatase in nasal epithelium kept pace with the fetal growth which explained a steady improving metabolism and secretory activity of the fetal nasal mucosa. On the other hand, activities of alkaline phosphatase in the mesenchymal cells, the fibroblasts and the glandular cells were getting weaker and weaker indicating the functional maturation of the fetal nasal mucosa. During the sixth month, mucins occur red in the glands, which showed the establishment of the secretory function in the nasal mucous glands.     

The effects of saline-induced edema in the human nasal mucosa on laser Doppler flowmetry

The nasal mucosa on the anteromedial surface of the inferior turbinate was studied with laser Doppler flowmetry in ten patients who were under general anaesthesia. A specially designed adapter was used, which held an injection needle with a diameter of 0.4 mm in a fixed position to the tip of the probe. The tip of the needle was inserted to a depth of 0.7 mm below the surface of the mucosa, while the tip of the probe was held at a distance of 0.3 mm from the mucosa. The laser Doppler parameters of perfusion, concentration of moving blood cells (CMBC) and velocity were recorded before and after the injection of 0.8 ml saline, thus inducing an experimental edema. After the injection no change in perfusion was detected but CMBC decreased and velocity increased. The findings agreed with the view that an increase in mucosal edema would reduce CMBC. When studying unanaesthesised subjects we normally use both rhinostereometry and laser Doppler flowmetry. It is then possible to measure the degree of mucosal congestion and micro circulation simultaneously, thus permitting study of the effects of a change in interstitial fluid content on mucosal congestion.     

Immediate and short-term effects of benzalkonium chloride on the human nasal mucosa in vivo

The in vivo effects of benzalkonium chloride, which is a preservative in most nasal sprays and drops, have been investigated in normal human volunteers. Saccharin clearance time was slightly prolonged 10 min after 0.02% benzalkonium chloride was applied, compared to that following 0.9% saline (n = 27, P = 0.04, Wilcoxon test). Sixty-five normal volunteers were randomly assigned to receive saline, fluticasone propionate aqueous nasal spray or placebo (which contained all the ingredients of fluticasone aqueous spray incl. 0.02% benzalkonium chloride, minus the fluticasone propionate) for 2 weeks, two puffs twice a day on a double-blind basis. Symptom scores, acoustic rhinometry, saccharin clearance time and ciliary beat frequency were measured immediately prior to this study and again at 2 weeks. Fifty-eight individuals completed the study with >80% compliance. There was no significant difference between the three groups in any of the variables tested. Benzalkonium chloride causes slight prolongation of mucociliary clearance shortly after application but has no detectable effect on nasal mucosal function after 2 weeks regular use.     

Fluorescein flowmetry in human nasal mucosa

In sixteen patients a relative blood flow, expressed as an index, in the nasal mucosa was measured by fluorescein flowmetry (FF) using an endoscope technique. Duplicate determination showed slightly lower values in the second measurement performed 5 min after the first one. This difference might be due to a too high background fluorescence in the tissue. The blood flow index was reduced to 1/3 of the original blood flow index by the administration of nose drops. These changes in man due to decongestion are comparable to the changes in blood flow index observed in a previous work (2) in rabbit sinus mucosa, using the corresponding technique.     

The effects of autonomotropic drugs on allergic nasal mucosa

The purpose of the present study was to elucidate the effects of different kinds of autonomotropic drugs on the nasal mucosa as well as on the nasal reaction to specific allergens in patients with nasal allergy. First, phenylephrine (alpha-agonist), phentolamine (alpha-antagonist), isoproterenol (beta-agonist), propranolol (beta-antagonist), methacholine (choline agonist), or ipratropium (choline antagonist) was applied to the nasal mucosa with an atomizer using saline as control. Definitive effects appeared at the spray of alpha-agonist or choline agonist. Phenylephrine reduced nasal airway resistance, and methacholine increased nasal secretion. Secondly, after treatment with the drugs, nasal provocations were performed. The statistically significant effects were noted as follows: phenylephrine spray inhibited the increase of nasal airway resistance, while phentolamine or isoproterenol enhanced it. Methacholine enhanced nasal secretion, while ipratropium inhibited it. None of the drugs, however, affected the number of sneezes. The present results suggest that adrenergic receptors are mainly distributed on the walls of vessels and cholinergic receptors mainly on the secretory glands. Pharmacological conditions of the local autonomic nervous system would affect the nasal response in allergy in different ways according to different conditions.     

Efficacy of vardenafil in human nasal mucosa

ObjectiveLevitra, a phosphodiesterase-5 (PDE5) inhibitor, is the trade name of vardenafil. It is applied to treatment of erectile dysfunction. PDE5 inhibitors dilate the penile blood vessels and cause prolonged erections. However, the effects of Levitra on human nasal mucosa are not yet fully explored.Materials and methodsWe examined the effectiveness of Levitra on human nasal mucosa directly in vitro by testing: 1) effect on human nasal mucosa resting tension; 2) effect on contraction caused by 10⁻⁶ M methoxamine as a sympathetic mimetic; 3) effect of the drugs on electrically induced human nasal mucosa contractions.ResultsThe results showed that addition of methoxamine to the incubation medium caused the nasal mucosa to contract in a dose-dependent manner. Addition of Levitra at doses of 10⁻⁴ M elicited a significant relaxation response to 10⁻⁶ M methoxamine-induced mucosa strip contraction. Levitra could not inhibit electrical field stimulation-induced spike contraction and had a minimal effect on the basal tension of nasal mucosa as the concentration increased.ConclusionThis study indicated that high concentrations of Levitra had a significant spasmolytic effect by antagonizing α-adrenoceptors. Moreover, nasal obstruction might not be relieved in patients suffering from erectile dysfunction and stuffy noses who were concomitant using α-adrenergic agonist and Levitra.     

Bioparox effects on nasal mucosa in acute catarrhal rhinosinusitis

An open, randomized, comparative trial of the drug bioparox was made in 50 patients. Nasal cavity function and its changes in response to bioparox administration were studied with the saccharin test and measurement of ciliary motor activity (CMA) using a special computer program. Significant suppression of the transport function and CMA in all the patients with catarrhal rhinosinusitis was observed. SMA on the inferior turbinated bone and septum was minimal, being low on the middle turbinated bone. After 7 days of bioparox administration mean value of CMA rose 2-fold. Thus, it is demonstrated that bioparox inhalations have no negative effect on nasal ciliated epithelium. On the contrary, it enhances its recovery.     

Beta adrenoceptors in human nasal mucosa.

The significance of the beta adrenergic system in the nasal mucosa is unclear. The authors have used the technique of autoradiography to localize and classify beta adrenoceptors in human nasal mucosa. The receptors have been found to be exclusively of the beta-2 subtype and the highest density is found in the glandular ducts. It is suggested that the beta-adrenergic system may have a physiologically important role in controlling the electrolyte composition of nasal secretions.     

Injurious effect of eosinophil extract on the human nasal mucosa

Eosinophils are frequently associated with the manifestation of nasal allergy in the nasal mucosa and nasal secretion. The role of eosinophils in hypersensitivity diseases, however, is still obscure, whether it protects or damages tissues and activates mast cells. The effects of two kinds of human eosinophil extract (biological and physical extracts) on human nasal mucosa by applying them in nasal provocation test and cilia beating test, and also in tracheal ring incubation and skin test in the guinea-pig were measured. The results of the study suggest that eosinophil major protein and other protein components may produce damage to the function of human nasal mucosa and tracheal mucosa of the guinea-pig.     

Measurement of water loss in human nasal mucosa

BACKGROUND: Regulation of the barrier function in the nasal epithelium seems to be affected by the pathogenesis of allergic rhinitis. The measurement of transepidermal water loss has proven to be an important noninvasive method for assessing the efficiency of the skin as a protective barrier. Although the nasal mucosal epithelium also has such a protective function, the precise mechanism still is unknown. METHODS: We studied the alteration of nasal mucosal water loss in the basal state and after the nontraumatic applications of physiological saline, hypertonic saline (10% NaCl), nasal barrier cream, and 10% glycerol on the mucosal surface of the inferior turbinate. RESULTS: We observed that nasal mucosal water loss was increased by hypertonic saline and decreased by nasal cream and glycerol. CONCLUSION: For the first time, we showed the human nasal mucosal water loss both in the basal state and after topical application of various substances.