Topical anesthesia of tracheal receptors

Camporesi, Enrico M.; Mortola, Jacopo P.; Sant'Ambrogio, F.B.; Sant’Ambrogio, Giuseppe

doi:10.1152/jappl.1979.47.5.1123

Cited by 31 publications

(16 citation statements)

References 14 publications

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“…On the basis of evidence previously reported it seems that concomitant administration of another amide-type anaesthetic would not have a notable effect on the pharmacokinetic parameters of the first (Tucker & Mather, 1979 (Akerman, 1975;Camporesi et al, 1979). It has not been used as a topical agent in man, to our knowledge.…”

Section: Pharmacokinetic Analysismentioning

confidence: 88%

Absorption of lignocaine and bupivacaine from the respiratory tract during fibreoptic bronchoscopy.

McBurney¹,

Jones²,

Stanley³

et al. 1984

Brit J Clinical Pharma

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Absorption of lignocaine and bupivacaine from the upper and lower respiratory tract was studied in patients undergoing fibreoptic bronchoscopy. No significant differences were found between the drugs and between the routes of administration in terms of the time taken to achieve maximum plasma concentrations. The relative availability of lignocaine was greater following administration via the upper respiratory tract, but bupivacaine availability did not differ. The apparent clearance of lignocaine was not affected by the route of administration but bupivacaine clearance was higher following administration via the lower respiratory tract. Bupivacaine, previously unreported as a topical agent in man, produced adequate anaesthesia at one‐eighth of the dose of lignocaine. Plasma bupivacaine concentrations had a very wide safety margin.

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Section: Pharmacokinetic Analysismentioning

confidence: 88%

Absorption of lignocaine and bupivacaine from the respiratory tract during fibreoptic bronchoscopy.

McBurney¹,

Jones²,

Stanley³

et al. 1984

Brit J Clinical Pharma

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“…The lack of effect of RSD931 on histamine‐induced bronchoconstriction in these experiments is not surprising, since histamine contracts airway smooth muscle directly by activating H 1 ‐receptors. The only other classes of compound documented to possess similar activity on Aδ‐fibres, which correlated to an anti‐tussive action, are the peripherally‐acting μ‐opioid‐receptor agonists (Adcock, 1991; 1999) and the local anaesthetics (Camporesi et al ., 1979; Cross et al ., 1976; Karlsson & Fuller, 1999).…”

Section: Discussionmentioning

confidence: 99%

RSD931, a novel anti‐tussive agent acting on airway sensory nerves

Adcock

Douglas

Garabette

et al. 2003

British J Pharmacology

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1 The anti-tussive eects, of the local anaesthetic, lidocaine and carcainium chloride (RSD931) have been investigated in guinea-pigs and rabbits. 2 Pre-treatment of guinea-pigs with aerosols of lidocaine or RSD931 at 0.1, 1.0 and 10 mg ml 71 reduced the number of citric acid-induced coughs by 9.3, 32.6 and 40.9% (P40.05) for lidocaine and by 25.3% (P40.05), 40.4% (P40.05) and 97.6% (P50.01) for RSD931, respectively and increased the latency to onset of cough at 10.0 mg ml 71 only. In addition, RSD931 at 10 mg ml 71 reduced citric acid-evoked cough responses in rabbits (with prior exposure to ozone at 3 p.p.m. for 1 h) from 22.1+5.1 to 2.7+0.9 coughs (P50.01). ) signi®cantly (P50.05 ± 50.01) reduced the spontaneous and histamineevoked discharges in Ad-®bres originating from airway, rapidly adapting stretch receptors (RARs) without aecting histamine-evoked bronchoconstriction. Lidocaine at 10.0 mg ml 71 also signi®cantly (P50.05) inhibited the spontaneous and histamine-induced discharges of RARs without aecting histamine-evoked bronchoconstriction. 5 Aerosols of RSD931 (10.0 mg ml 71 ) caused a transient, but signi®cant (P50.05), activation of pulmonary C-®bre endings 2.5 min after administration started. RSD931 had no signi®cant (P40.05) eects on discharges in bronchial C-®bres originating from bronchial C-®bre endings, capsaicin-evoked discharges of either pulmonary or bronchial C-®bre endings or on capsaicinevoked bronchoconstriction. In contrast, lidocaine (10.0 mg ml 71 ) signi®cantly (P50.05) inhibited spontaneous and capsaicin-induced discharges in both pulmonary and bronchial C-®bres respectively. Lidocaine also signi®cantly (P50.05) reduced capsaicin-evoked bronchoconstriction. 6 These studies suggest that the anti-tussive actions of RSD931 are mediated via inhibition of discharges in Ad-®bres originating from airway RARs. The mechanism of action of RSD931 is distinct from that of the local anaesthetic lidocaine and RSD931 may represent a novel class of antitussive agent.

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“…These points in combination would a priori suggest potential sitespecific sensitivities. Indeed, RARs do exhibit greater responsiveness than SARs to topical applications of anaesthesia (Karlsson, 1987), including aerosolized anaesthetics (Camporesi et al, 1979). Most of the chemical and mechanical irritants that stimulate RARs are bronchoconstrictors, and RARs have been recognized as cough receptors.…”

Section: Discussionmentioning

confidence: 99%

Aerosol Therapy Implications of Particle Deposition Patterns in Simulated Human Airways

Martonen¹

1991

Journal of Aerosol Medicine

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The efficacy of inhalation therapy may be improved by the selective deposition of aerosolized medicines, by explicitly targeting and delivering drugs to prescribed lung sites. This may be accomplished by controlling particle sizes and regulating breathing patterns. Here, the deposition patterns of 1.9-10.6 pm mass median aerodynamic diameter test aerosols, mapped in surrogate respiratory tracts consisting of replica laryngeal casts and fabricated tracheobronchial models, are analyzed.Configurations of the laryngeal casts corresponded to inspiratory flow rates of 15, 30 and 60 Lmin"-"-. Particles were preferentially deposited at bifurcations, specifically at carinal ridges. Evidence from other investigations indicates that mucociliary clearance may be impeded at such sites ¿n vivo.When these two effects, enhanced deposition and impaired clearance, are coupled, the findings suggest that epithelial cells and receptors at airway branching sites may receive concentrated doses of inhaled pharmacological agents. To focus the effects of airborne drugs the lung should, therefore, be considered as a serial network of Y-shaped bifurcation units. The findings have important implications to current aerosol therapy using metered-dose inhalers and nebulizers, and future protocols including:(1) the treatment of bronchogenic carcinomas because malignant tumors have a predilection for upper airway bifurcations; and, (2) lung diseases related to the afferent nervous system since components of neural pathways frequent such locations.

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Topical anesthesia of tracheal receptors

Cited by 31 publications

References 14 publications

Absorption of lignocaine and bupivacaine from the respiratory tract during fibreoptic bronchoscopy.

Absorption of lignocaine and bupivacaine from the respiratory tract during fibreoptic bronchoscopy.

RSD931, a novel anti‐tussive agent acting on airway sensory nerves

Aerosol Therapy Implications of Particle Deposition Patterns in Simulated Human Airways

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