The Role of Vagal Reflex in Mechanism of Secretagogic Action of Bromhexine

Takeda, Hiroshi; Abe, Youichi; Misawa, Miwa; Yanaura, Saiζo; Kuroiwa, Yukio

doi:10.1254/jjp.35.445

Cited by 4 publications

(4 citation statements)

References 20 publications

(17 reference statements)

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“…BH derivatives 12 and 14 possess M2 cholinergic activity. Although BH shows no binding to serotonin receptors (see table 3), it has been reported that it promotes the release of liposomal enzymes which dissolve acid glycoproteins in canine trachéal secretory cells (21,22). Besides binding to a-receptors, BH binds to muscarinic2 receptors therefore its activity, at least in part, could be partially due to this phenomenon.…”

Section: Discussionmentioning

confidence: 98%

“…Figure 12 shows the results for five of the seven peaks (two peaks were insignificant). Three major peaks (13,22, and 28 min retention times) and two minor peaks (17 and 19 min retention times) were quantified with respect to topical administration of 7A. Of the three major peaks, the peaks with retention times of 19 and 22 minutes show a statistically significant (n=18, p<0.001) increase in the treated eye at 10 minutes and both the treated and fellow eyes at 60 minutes compared to baseline values (see figure 12).…”

Section: Size-exelusion High Pressure Liquid Chromatographymentioning

confidence: 99%

See 1 more Smart Citation

Lacrimal Secretion Stimulants: Sigma Receptors and Drug Implications

Shirolkar

Schoenwald²,

Barfknecht³

et al. 1993

Journal of Ocular Pharmacology and Therapeutics

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3H-DTG (1.3-di(2-[5-3H]tolyl)guanidine) or 3H-haloperidol was added to areceptors (25 nM) in the presence of 25 nM splperone and incubated with increasing concentrations of bromhexine derivatives (phenylalkylamines; 10~9 to 10~2 M) in membrane homogenate suspensions. IC50 values for two derivatives ranged from 3.2 to 8.8 nM for both radioligands. A preferred derivative, 7A (N, N'-dimethy1-2-phenylethylamine) , yielded an IC50 of 7.8 nM for 3H-haloperidol but showed much less affinity in displacing 3H-DTG (IC50=900 nM). Applying the technic of Bromberg [Exp. Eye Res. , 40:313-320, 1985] , in vitro protein secretion rates were measured following stimulation of either lacrimal gland slices or isolated, intact lacrimocytes with the compounds, in vitro protein secretion rates exhibit a dose-response relationship with increases in protein release up to a concentration of 10~8 to 10"4 M for various derivatives of bromhexine and ÎO-4 M for carbachol. By means of Schirmer strips, tear fluid was collected over a five minute period at 10 and 60 minutes post-dosing following the topical application (50/il) to the right eye of New Zealand white rabbits (n=20-24) of 7A at various concentrations. Incubation of lacrimocytes with 7A alone (10"'' M) , with haloperidol (lO"4 M) alone or in combination show that 7A is acting as an agonist to stimulate protein release, whereas haloperidol is acting as an antagonist to inhibit release. In vivo protein secretion rates also show a doseresponse curve (at both 10 and 60 minutes post-dosing) for 7A that reach a statistically significant maximum in the dosed eye at a concentration of 0.15% w/v. Analysis of protein extracts using size exclusion HPLC shows an increase in secretory proteins, particularly tear-specific prealbumin.

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Section: Discussionmentioning

confidence: 98%

Section: Size-exelusion High Pressure Liquid Chromatographymentioning

confidence: 99%

Lacrimal Secretion Stimulants: Sigma Receptors and Drug Implications

Shirolkar

Schoenwald²,

Barfknecht³

et al. 1993

Journal of Ocular Pharmacology and Therapeutics

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“…Ausführliche Studien wurden in der Veterinärmedizin durchgeführt, in der Bromhexin weitverbreitet angewendet wird. Hier sind zum Beispiel bei Haustieren lokale Schleimhautreizungen sowie Reaktivierungen von Magenulzera bekannt (18,19).…”

Section: Diskussionunclassified

“…Die zweite Phase bildet die direkte Wirkung an den submukösen Drüsen. Lysosomale Enzyme werden ins Zytoplasma der sekretorischen Zellen sezerniert, wodurch es zur Auflösung der sauren Glykoproteine kommt, was wiederum klinisch als Mukolyse resultiert (4,18,19).…”

unclassified

Akute Ulkusblutung bei parasuizidaler Intoxikation mit Bromhexin-Saft – ein Fallbericht

Bernhard¹,

Ohlenbusch²,

Bödeker³

et al. 2004

Kinder- und Jugendmedizin

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ZusammenfassungWir berichten von einem 13-jährigen Jungen mit Ulcus ventriculi-Blutung. Der Patient wurde wegen akuten Bluterbrechens, jedoch in stabilem Allgemeinzustand vorgestellt. Endoskopisch imponierte ein florides Ulkus am Angulus ventriculi mit einer Sickerblutung. Anamnestisch ließ sich während des stationären Verlaufs eruieren, dass der Junge am Vortag eine Überdosis Bromhexin-Saft getrunken hatte. Dies führte bei möglicherweise vorgereizter Schleimhaut zu einer akuten Exazerbation mit nachfolgender Ulkusblutung. In der psychologischen Diagnostik zeigten sich als mögliche Ursache für die Intoxikation parasuizidale Tendenzen.

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