Influence of erdosteine, a mucolytic agent, on amoxycillin penetration into sputum in patients with an infective exacerbation of chronic bronchitis.

Ricevuti, G; Mazzone, A.; Uccelli, E; Gazzani, Gabriella; Fregnan, G. B.

doi:10.1136/thx.43.8.585

Cited by 44 publications

(25 citation statements)

References 6 publications

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“…The present study was designed to in vestigate the antioxidant properties of erdosteine, a novel mucolytic and mucoregulator agent possessing two blocked SH groups which can be liberated and may function as reducing radicals [24,25], in an in vitro model where human ctr AT was inactivated by exposure to the gas phase of cigarette smoke. A comparative evaluation was carried out by employing glutathione and ascorbic acid, two physio logical reducing agents.…”

Section: Introductionmentioning

confidence: 99%

In vitro Protection by Erdosteine against Oxidative Inactivation of Alpha-1-Antitrypsin by Cigarette Smoke

Gazzani

Fregnan²,

Vandoni³

1989

Respiration

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Direct exposure in vitro of the protein αrantitrypsin (α₁-AT; human neutrophil elastase inhibitor, α₁-proteinase inhibitor) to gas phase cigarette smoke causes a loss of elastase-inhibitory capacity (EIC). This effect appears to be related to the formation of reactive oxygen species in the smoke that inactivate α₁-AT by oxidizing the methionine terminal amino acid. Reducing agents such as glutathione and ascorbic acid prevent this inactivation. In the present investigation erdosteine, a novel thiol derivative, which contains two blocked SH groups with potential reducing properties, was tested in vitro for its capacity to protect human α₁-AT. For the purpose, the compound, previously hydrolyzed with bicarbonate-carbonate buffer or with microsomal enzymes, was put in contact with α₁-AT and exposed to gas phase cigarette smoke. The EIC of α₁-AT was then measured by incubating the samples with leukocyte elastase and, subsequently, by titrating the residual elastolytic activity against a synthetic substrate. Under these conditions erdosteine effectively protected α₁-AT against the smoke injury and, after alkaline hydrolysis, it appeared to be as active as glutathione and ascorbic acid (EC₅₀ being respectively 6.4, 7.2 and 6.2 mM). This evidence suggests that the erdosteine SH groups, which can become free, may have an important role in the mechanism of action, by blocking highly reactive oxygen-free radicals. Erdosteine may have a therapeutic application in preventing oxidative lung damage induced by cigarette smoke

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Section: Introductionmentioning

confidence: 99%

In vitro Protection by Erdosteine against Oxidative Inactivation of Alpha-1-Antitrypsin by Cigarette Smoke

Gazzani

Fregnan²,

Vandoni³

1989

Respiration

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“…Preliminary studies have pointed out that the drug is endowed with interesting mucomodulator [1,2] and antioxidant properties in vitro and in vivo (in both animals and men) [3][4][5], and that it is also able to favor the penetration of antibiot ics into bronchial secretions [6]. Moreover, other stud ies have demonstrated that the compound and some of its metabolites can increase the bronchial transport of the mucus in pigeons [2], With this background and on the basis of mucocil iary clearance in man being reduced by chronic air way diseases [7,8], we have evaluated the effect of er dosteine on mucociliary transport (MCT) in patients affected by chronic bronchitis.…”

Section: Introductionmentioning

confidence: 99%

Activity of Erdosteine on Mucociliary Transport in Patients Affected by Chronic Bronchitis

Olivieri¹,

Donno²,

Casalini³

et al. 1991

Respiration

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The influence of erdosteine (a mucomodulator endowed with mucolytic and antioxidant properties) on human mucociliary transport (MCT) was investigated in a double-blind placebo controlled study. Sixteen former smokers affected by chronic bronchitis, preselected for their mucociliary responsiveness to an inhaled β₂-agonist, were divided into two groups (matched by number, sex, age and FEV₁%) and orally treated with placebo or erdosteine (300 mg t.i.d.) for 8 days. Their MCT was assessed by the bronchofiberscopy technique just before starting the treatment and at the end of the treatment. The pretreatment mucus transport velocity in these patients was significantly decreased with respect to healthy subjects. The erdosteine treatment induced a significant improvement of MCT while placebo was inactive (mean % variation ± SE against their baseline values being +60.4 ± 18.4 and -3.0 ± 5.9, respectively). This peculiar activity of erdosteine on mucus transport may be of clinical usefulness in chronic bronchitic patients and it can be added to β₂-agonists to restore the decreased MCT

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“…However, it may be assumed that the doses of erdosteine used in this study were higher than the clinically tolerable dose. Previous studies indicate that the tolerable dose of erdosteine without side-effects was 900 mg day −1 in humans and 500-1000 mg kg −1 in rats (Ricevuti et al, 1988;Giovanni antioxidant enzymes such as SOD, CAT and GSH-Px (on indirect indicator of free-radical production; Ozyurt et al, 2001) in the kidney tissue produced by cisplatin were significantly depleted, and the depletion of these enzymes activities was significantly reduced by the erdosteine treatment, especially at doses of 50 and 75 mg kg −1…”

Section: Discussionmentioning

confidence: 99%

Cisplatin‐induced acute renal failure is ameliorated by erdosteine in a dose‐dependent manner

Özyurt

Yıldırım

Kotuk

et al. 2004

J of Applied Toxicology

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The aim of this study was to investigate the optimum dosage of erdosteine to ameliorate cisplatin-induced nephrotoxicity. Three different doses of erdosteine at 25, 50 and 75 mg kg(-1) were studied in rats. Intraperitoneal administration of 7 mg kg(-1) cisplatin led to acute renal failure, as indicated by kidney histology and increases in plasma creatinine and blood urea nitrogen (BUN) levels. At 5 days after cisplatin injection the BUN level was increased significantly from 15.1 +/- 4.3 to 126.7 +/- 152.6 mg dl(-1) and plasma creatinine levels increased from 0.37 +/- 0.005 to 1.68 +/- 1.9 mg dl(-1). When the rats were administered 50 and 75 mg kg(-1) erdosteine 24 h before cisplatin injection that was continued until sacrifice (total of 6 days), the BUN and creatinine levels remained similar to control levels and the grade of histology was similar. Erdosteine at doses of 50 and 75 mg kg(-1) ameliorates cisplatin-induced renal failure. The optimum dose of erdosteine may be 50 mg kg(-1) in this study.

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Influence of erdosteine, a mucolytic agent, on amoxycillin penetration into sputum in patients with an infective exacerbation of chronic bronchitis.

Cited by 44 publications

References 6 publications

In vitro Protection by Erdosteine against Oxidative Inactivation of Alpha-1-Antitrypsin by Cigarette Smoke

In vitro Protection by Erdosteine against Oxidative Inactivation of Alpha-1-Antitrypsin by Cigarette Smoke

Activity of Erdosteine on Mucociliary Transport in Patients Affected by Chronic Bronchitis

Cisplatin‐induced acute renal failure is ameliorated by erdosteine in a dose‐dependent manner

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