Influence of azelastine and some selected drugs on mucociliary clearance

U, Achterrath-Tuckermann; Saano, Veijo; Minker, E.; Stroman, F; Arny, I; Joki, Susanna; Nuutinen, Juhani; Szelenyi, Istvan

doi:10.1007/bf00174117

Cited by 10 publications

(5 citation statements)

References 17 publications

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“…Studies investigating the influence of intranasal antihistamines on mucociliary clearance and ciliary function have provided contradictory results (Table 2). Some studies have demonstrated no adverse effects of intranasal formulations containing azelastine or levocabastine on mucociliary clearance and/or ciliary function, either in vivo or in vitro 1920. In contrast, others have reported that intranasal formulations containing azelastine and levocabastine do produce ciliotoxic effects on human nasal epithelium in vitro 2122.…”

Section: Effects Of Intranasal Antihistaminesmentioning

confidence: 99%

Influence of Intranasal Drugs on Human Nasal Mucociliary Clearance and Ciliary Beat Frequency

Jiao

Zhang

2019

Allergy Asthma Immunol Res

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The nasal mucociliary clearance system, which comprises epithelial cilia and mucus from goblet cells, is an important intrinsic defense mechanism of the upper respiratory tract. Intranasal drugs and additives can have a detrimental effect on ciliary activity and mucociliary clearance, and thus impact the integrity of nasal defense mechanisms. This article discusses the current literature on the effects of different classes of intranasal drugs including intranasal corticosteroids, antihistamines, decongestants, antimicrobials and antivirals, as well as various drug excipients and nasal irrigation solutions on human nasal mucociliary clearance and ciliary beat frequency. Available data indicate that some intranasal formulations tend to hamper nasal ciliary function and mucociliary clearance. Therefore, it is of great importance to assess the effects of intranasal drugs and additives on mucociliary function before they are recommended as therapy for different nasal conditions.

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Section: Effects Of Intranasal Antihistaminesmentioning

confidence: 99%

Influence of Intranasal Drugs on Human Nasal Mucociliary Clearance and Ciliary Beat Frequency

Jiao

Zhang

2019

Allergy Asthma Immunol Res

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“…Both azelastine and levocabastine may cause irreversible ciliostasis at therapeutic concentrations and cause reversible decreases of cilia beating at diluted concentrations [65]. Other studies support the ciliostatic effects of azelastine [66][67][68] while two other studies suggest that azelastine itself may not be ciliostatic but that rather the benzalkonium preservative used in clinical formulations is ciliostatic [69,70]. Regardless, azelastine does not activate NO production from the human nasal cultures, described above, and thus would not be expected to have the same immune-boosting effects as a DPD-derived compound.…”

Section: Discussionmentioning

confidence: 95%

Cilia Stimulatory and Antibacterial Activities of T2R Bitter Taste Receptor Agonist Diphenhydramine: Insights into Repurposing Bitter Drugs for Nasal Infections

Kuek

McMahon

et al. 2022

Pharmaceuticals

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T2R bitter taste receptors in airway motile cilia increase ciliary beat frequency (CBF) and nitric oxide (NO) production. Polymorphisms in some T2Rs are linked to disease outcomes in chronic rhinosinusitis (CRS) and cystic fibrosis (CF). We examined the expression of cilia T2Rs during the differentiation of human nasal epithelial cells grown at air–liquid interface (ALI). The T2R expression increased with differentiation but did not vary between CF and non-CF cultures. Treatment with Pseudomonas aeruginosa flagellin decreased the expression of diphenhydramine-responsive T2R14 and 40, among others. Diphenhydramine increased both NO production, measured by fluorescent dye DAF-FM, and CBF, measured via high-speed imaging. Increases in CBF were disrupted after flagellin treatment. Diphenhydramine impaired the growth of lab and clinical strains of P. aeruginosa, a major pathogen in CF and CF-related CRS. Diphenhydramine impaired biofilm formation of P. aeruginosa, measured via crystal violet staining, as well as the surface attachment of P. aeruginosa to CF airway epithelial cells, measured using colony-forming unit counting. Because the T2R agonist diphenhydramine increases NO production and CBF while also decreasing bacterial growth and biofilm production, diphenhydramine-derived compounds may have potential clinical usefulness in CF-related CRS as a topical therapy. However, utilizing T2R agonists as therapeutics within the context of P. aeruginosa infection may require co-treatment with anti-inflammatories to enhance T2R expression.

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“…(17) Mucociliary clearance also appears to be unaffected by topically administered antihistamine when applied to the nasal epithelium or trachea in vivo and in vitro. (18)(19)(20) In fact, under conditions of excess thin bronchial secretions (bronchorrhea), such as in acute asthma, there is a decrease in mucus clearance and widespread mucus obstruction contributes to small airways obstruction. Reduction of these secretions may be desirable.…”

Section: Effect Of An Antihistamine On Sputum Rheology In Cf 47mentioning

confidence: 99%

The Effect of A First-Generation Antihistamine on Sputum Viscoelasticity in Cystic Fibrosis

Homnick

Marks

Rubin

2007

Journal of Aerosol Medicine

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Tenacious airway secretions are responsible for much of the lung damage in cystic fibrosis (CF). Label warnings on potential secondary effects of some antihistamines include possible drying or thickening of lower airway secretions, suggesting that they are detrimental to individuals with airway disease. We studied the effects of cyproheptadine hydrochloride (CH) on sputum weight, viscoelasticity, and transportability in CF patients participating in a pilot trial of CH as an appetite stimulant to assure no potential adverse secondary effects on mucus clearance. Sixteen clinically stable subjects were randomized to receive either CH (2 mg QID for 1 week followed by 4 mg QID for 11 weeks) or placebo. Sputum was obtained by voluntary forced cough and expectoration prior to starting CH or placebo and at 4 weeks. Viscoelasticity was measured by rheometry and cough transportability by simulated cough machine. Sufficient paired sputum for rheologic analysis was obtained on four placebo and seven CH subjects and for cough transportability analysis on three placebo and six CH subjects. Weight on all specimens was obtained prior to both analyses. There were no significant differences in sputum weight wet, measures of mucus viscoelasticity (rheology), or cough transportability of mucus between baseline and 4 weeks in patients on placebo or CH. From this limited study, CH, a first-generation antihistamine, appears to have no adverse effects in sputum viscoelasticity or cough transportability in CF patients.

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Influence of azelastine and some selected drugs on mucociliary clearance

Cited by 10 publications

References 17 publications

Influence of Intranasal Drugs on Human Nasal Mucociliary Clearance and Ciliary Beat Frequency

Influence of Intranasal Drugs on Human Nasal Mucociliary Clearance and Ciliary Beat Frequency

Cilia Stimulatory and Antibacterial Activities of T2R Bitter Taste Receptor Agonist Diphenhydramine: Insights into Repurposing Bitter Drugs for Nasal Infections

The Effect of A First-Generation Antihistamine on Sputum Viscoelasticity in Cystic Fibrosis

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