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PubMedDate not supplied

[Ambroxol versus betamethasone for stimulating antepartal lung maturity--a multicenter study].

In a multicenter, randomized double-blind study, the effect of Betamethasone and Ambroxol, both used for prenatal prevention of RDS in premature and newborn infants, is compared in a total of 185 patients with premature labour or an induced termination of pregnancy between the 28 and 36th week of gestation. The Ambroxol group of 93 patients is reduced to 77 due to a break up of therapy in 16 patients. The Betamethasone group is likewise reduced from 92 to 85 due to a break up of therapy in 7 patients. The main reason for breaking up therapy in these patients is the impossibility of stopping labour and delivery within 72 hours after admission to the hospital. Both treatment groups show no significant differences with regard to age, weight, history, rate of premature rupture of membranes, gestational age at beginning of therapy and at time of delivery, mode of delivery, rate of tocolytic therapy and prematurity. RDS morbidity, established by a standardized evaluation of the infants considering X-ray, clinical and blood-gas analyses findings, is 9% (7 out of 79 infants) in the Ambroxol group, and 6% (5 out of 86 infants) in the Betamethasone group. Statistically seen, the difference between the two groups is insignificant. Amniotic fluid analyses carried out in a total of 46 patients of both groups show increased surfactant parameters after therapy as compared to initial values before therapy. A significant difference between the two groups is not manifest. The objections against corticosteroids regarding there indications and side effects are generally known. The results of this study indicate that Ambroxol compared to Betamethasone can be considered as an effective drug for prevention of neonatal respiratory distress syndrome.

Ambroxol↗
PubMed1984

Polymorphonuclear leucocytes functions from premature infants after prevention of respiratory distress syndrome with betamethasone and ambroxol.

An increase in the infection rate both in mother and newborn after antenatal administration of corticosteroids for prevention of RDS has been shown. The aim of this study was to compare PMN functions in two groups of premature infants whose mothers had received betamethasone or ambroxol for prevention of RDS. Blood samples were collected within the first four days of life from 40 newborns. Thirteen infants received antenatal administration of 6 mg of betamethasone acetate and 6 mg sodium phosphate i.m., which was repeated 24 hours later. Twelve received antenatal administration of ambroxol, 1 g i.v. every day for 5 days. Fifteen did not receive any antenatal treatment. Mean gestational age and mean birth weight was not significantly different between the betamethasone group (33 +/- 3.1 weeks and 2080 +/- 567 g) and the ambroxol group (32.9 +/- 3.4 weeks and 2164 +/- 793 g). Phagocytosis and killing ability was significantly lower in the betamethasone group in comparison to the ambroxol group (21.3% +/- 2.2 rather than 48.4% +/- 15; p 0.01 and 11.4% +/- 1.7 rather than 20.5% +/- 6.1; p 0.01 respectively). Immunoglobulin or complement levels were not significantly different in the three groups.

Ambroxol↗
PubMed1982

[A comparative morphological and chemical study of the ambroxol and chlorphentermine action on the lung phospholipid content (author's transl)].

The influence of chronic administration of ambroxol on the phospholipid-(PL-) content and ultrastructure of lungs has been studied and compared with the effect of chlorphentermine (chlph.). Both drugs are amphiphilic substances. The causative factor of the well-known chlph. induced phospholipidosis-like alterations was suggested to be an inhibition of enzymatic degradation of PL. Rats were intraperitoneally treated five times per week for two weeks with chlph. (0,2 mMol per kg b.w.) and ambroxol (0.2 mMol per kg b.w.), respectively. Lung, heart, liver, kidney and spleen were light microscopically examined, and the lung was studied by electron microscopy. Furthermore, the PL-content of the whole lung tissue, the proportion of phosphatidylcholine (PC), the lung weight/body weight ratio (LM/KM) as well as the dry weight/wet weight ratio (TM/FM) of the lung was calculated. The application of chlph, induced an excessive PL-storage in the lung as indicated by an increase of the PL-content, of the PC-proportion as well as of the LM/KM and TM/FM ratio. The accumulated PL are detectable by electron microscopy, mainly in the lysosomes of macrophages appearing as lamellar or crystalloid inclusions. On the contrary, chronic application of ambroxol does not cause any substantial changes especially no abnormal lysosomal PL-inclusions. Therefore, it is suggested that ambroxol does not interfere with the PL-metabolism in a way comparable to that of the chlph. action.

Ambroxol↗
PubMedDate not supplied

Ambroxol inhibits endotoxin-induced lipid peroxidation in mice.

Administration of ambroxol (70 mg/kg ip) once a day for 3 days protected lung and heart lipids from lipopolysaccharide (LPS, 17 mg/kg)-induced oxidative stress in mice. Ambroxol as a lipid peroxidation inhibitor was almost as active as an equivalent dose of N-acetylcysteine (27.6 mg/kg), a well known antioxidant. The lung and heart levels of conjugated dienes in animals pretreated with ambroxol were 3.3- and 1.7-times lower (p < 0.05 and p < 0.01) than those observed in the control group which received only buffer and subsequently LPS. These results indicate that ambroxol can sufficiently inhibit the harmful process of lipid peroxidation in vivo.

Ambroxol↗
PubMed1997

Reduction of cytokine release of blood and bronchoalveolar mononuclear cells by ambroxol.

Ambroxol is a mucolytic agent frequently used in the treatment of chronic bronchitis. It has been reported, following clinical and in-vitro studies, that ambroxol exhibits an anti-inflammatory action. This capability was investigated by activating bronchoalveolar lavage cells and peripheral blood mononuclear cells in-vitro to elicit the release of tumor necrosis factor alpha, interleukin-2 and interferon gamma, whilst simultaneously exposing them to varying pharmacological concentrations of ambroxol (10, 1, and 0.1 microM). After 24 h it was observed that the isolated tissue-culture supernatants showed a dose-dependent reduction in the concentration of the tested cytokines; 10 microM (12 to 37% reduction) and 1 microM to (6 to 27% reduction). At 0.1 microM, a significant reduction could only be observed in the release of interleukin-2 by bronchoalveolar lavage cells. These results demonstrate, that ambroxol exhibits anti-inflammatory actions in concentrations achievable in vivo.

Ambroxol↗
PubMedDate not supplied

Ambroxol effect on transepithelial electrical potential difference of isolated tracheal wall.

The effect of ambroxol on ion transport in isolated tracheal wall was studied by the electrophysiological (Ussing) method. It was shown that ambroxol influenced one component of the transepithelial electrical potential difference (PD), which is related to ion transport processes mechanically stimulated by a jet of bathing fluid from a peristaltic pump. The other component of the PD, which represented stable ion transport processes, was not influenced by the drug. The stimulation-dependent component of the PD was deeply inhibited, or sometimes even eliminated, by a change in the pH of the stimulating bathing fluid from 7.4 to 6.4. Ambroxol, in a concentration of 5 microM, restored the mechanical reactivity of tissue stimulated by jet of fluid at pH 6.4. We put forward the hypothesis that ambroxol influences the ion transport processes, which are evoked by stimulation of "cough receptors", in a way that probably augments airway cough clearance.

Ambroxol↗
PubMedDate not supplied

Effect of paraquat intoxication and ambroxol treatment on hydrogen peroxide production and lipid peroxidation in selected organs of rat.

Paraquat (Pq) is a herbicide which is very toxic to all animals and to man. It generates free radicals and leads to acute or chronic lung injury and usually to death. So far, the role of lipid peroxidation of cell membranes in the mechanism of its toxicity has not been proved satisfactorily and therefore in the present study we examined the concentration of hydrogen peroxide (H2O2) and various lipid peroxidation products (LPP) such as conjugated dienes (CD), lipid hydroperoxides (LH), malonyldialdehyde (MDA) and Schiff bases in selected organs of the rat given a single intraperitoneal dose 35 mg kg-1 Pq. We also evaluated the influence of a mucolytic and probably antioxidant drug, ambroxol, on Pq-induced changes in the concentration of H2O2 and LPP. Paraquat increased the hepatic concentration of H2O2, CD, LH and MDA by approximately fourfold. Though the dose of Pq was nearly twice the LD50 dose, we did not notice any changes in the concentration of these substances in the critical organ, lung or heart and kidney. Ambroxol alleviated the increase of H2O2 in the liver but did not reduce the concentration of LPP. Moreover, the drug administered alone induced lipid peroxidation in the liver. Our results indicate that Pq dose not induce H2O2 production and lipid peroxidation in the lung but it increases the concentration of H2O2 and LPP in the liver. Ambroxol inhibits the Pq-induced increase in the concentration of H2O2 in the liver without protecting it against lipid peroxidation. Moreover, the drug alone may act as a pro-oxidant.

Ambroxol↗
PubMed1990

Ambroxol inhibits interleukin 1 and tumor necrosis factor production in human mononuclear cells.

We have studied the effect of Ambroxol on the production of Interleukin-1 (IL-1) and Tumor Necrosis Factor (TNF) in human mononuclear cells (MNC). For this purpose MNC were cultured for 24 h in the presence of endotoxin and different doses of Ambroxol. The results indicate that Ambroxol markedly inhibited IL-1 and TNF production at doses of 10-100 microgram ml, without any apparent toxicity.

Ambroxol↗
PubMed1998

Donor pretreatment with ambroxol or dexamethasone fails to ameliorate reperfusion injury in experimental lung transplantation.

Based on the known properties of ambroxol and dexamethasone to inhibit inflammation and increase endogenous surfactant levels, the potential advantage of donor pretreatment with either drug was investigated in an acute rat double-lung transplant model. Donor animals were randomly assigned to one of three treatment groups: an ambroxol group (AMB; 0.4 mg/kg), a dexamethasone group (DX; 2 mg/kg); or an untreated control group (CN). Drugs were given intraperitoneally 6 h prior to harvest. Following standard preservation and 16 h of cold ischemia, the donor double lung block was implanted into syngeneic recipients using custom-designed stents for the vascular anastomosis. During reperfusion, serial measurements of graft pulmonary vascular resistance and alveolar-arterial oxygen difference were obtained. Separate graft ventilation allowed determination of graft dynamic lung compliance. Final assessment included weight gain and histology. For phospholipid analysis, lung lavages were performed in the three study groups at the end of reperfusion and compared to levels before graft harvest. Donor pretreatment did not significantly affect preharvest phospholipid levels. Survival following graft ischemia and reperfusion was shortest after AMB (92 +/- 5 min) and longest after DX (110 +/- 5 min; DX vs AMB P < 0.03) and CN (116 +/- 4 min; CN vs AMB P < 0.02). DX pretreatment provided better compliance (P < 0.02) and lower vascular resistance (P < 0.0001) than AMB treatment. Airway resistance was lower in the AMB and DX groups than in controls (P < 0.04 and P < 0.02, respectively). The alveolar-arterial oxygen difference was markedly similar in all groups. Graft weight gain amounted to 114% +/- 10% in AMB, 88% +/- 12% in DX, and 98% +/- 13% in CN (P = NS). Thus, in this rat lung transplantation model, donor pretreatment with dexamethasone did not improve graft function compared to untreated controls and donor pretreatment with ambroxol was found to be potentially detrimental to graft function during reperfusion.

Ambroxol↗
PubMed1997

Antenatal ambroxol treatment does not prevent the respiratory distress syndrome in premature infants.

UNLABELLED: The effectiveness of ambroxol in the prevention of neonatal respiratory distress syndrome and in reducing the need for intermittent mandatory ventilation and oxygen therapy was studied in 88 mothers whose infants was born between 24 and 34 weeks of gestation and who were randomized either for treatment with ambroxol (group A = 42) or served as control (group B = 46). There were no significant differences in the mean gestational age, birth weight or Apgar score between the two groups. We found no significant differences in occurrence of respiratory distress syndrome (55% vs 45%), in support by intermittent mandatory ventilation (71% vs 72%) or oxygen therapy (74% vs 75%) at 12 h of age between groups A and B. CONCLUSION: This study does not suggest the efficacy of antenatal ambroxol treatment both for the prevention of neonatal respiratory distress syndrome and for the reduction of its severity.

Ambroxol↗
PubMed1996

The antioxidative activity of the mucoregulatory agents: ambroxol, bromhexine and N-acetyl-L-cysteine. A pulse radiolysis study.

Ambroxol and bromhexine are shown to be scavengers of both superoxide and hydroxyl radicals as determined by pulse radiolysis experiments. The dismutation of superoxide was accelerated 3-fold by bromhexine and 2.5-fold by ambroxol over the rate of spontaneous dismutation. The reaction constants of hydroxyl radicals with bromhexine and ambroxol were determined by competition kinetics to be 1.58 +/- 0.15 x 10(10) M-1S-1 and 1.04 +/- 0.1 x 10(10) M-1S-1, respectively. N-acetyl-L-cysteine also reacted with hydroxyl radicals (1.28 +/- 0.14 x 10(10) M-1S-1) but not with superoxide radical. These effects may be clinically relevant in the treatment of oxidant-associated lung damage induced by inflammatory agents and/or environmental pollutants.

Acetylcysteine↗
PubMed1992

High-performance liquid chromatographic determination of ambroxol in human plasma.

Ambroxol has been determined in biological fluids using a rapid and sensitive high-performance liquid chromatographic method. The samples prepared from plasma by liquid-liquid extraction were analysed on reversed-phase silica gel by competing-ion chromatography with ultraviolet detection. The method was applied to the determination of ambroxol levels in twelve healthy volunteers after oral administration of 90 mg of ambroxol in tablets of Mucosolvan and Ambrosan.

Adult↗
PubMed1992

Lung injury induced by paraquat, hyperoxia and cobalt chloride: effects of ambroxol.

The effects of the surfactant stimulating drug ambroxol were studied in rats given paraquat (PQ, 15 mg/kg, s.c.), intratracheal cobalt chloride (CoCl2, 2.5 or 1.25 mg Co/kg) or exposed for 2 days to oxygen (greater than 95% O2). Ambroxol (50 mg/kg, i.p., twice daily) was given as a pretreatment for 4 days, or up to 7 days following pneumotoxic administration. Besides body weight evolution and lethality, various pulmonary indices were measured 2 days (O2) or 3 days (PQ and CoCl2) and 7 days after pneumotoxic treatment: wet and dry lung weight, total cell count, distribution of inflammatory cells and lactate dehydrogenase in bronchoalveolar lavage fluid, and histological damage assessed by a semiquantitative injury score. Neither form of ambroxol treatment prevented the toxicity of any of the pneumotoxic agents. The use of a combination of different indices of lung damage showed that different pneumotoxic agents may cause quite distinctive patterns of injury.

Ambroxol↗
PubMed2005

The effect of taste masking agents on in situ gelling pectin formulations for oral sustained delivery of paracetamol and ambroxol.

The aim of this study was to examine the influence of polyhydric alcohols (taste masking agents) on the rheological properties of in situ gelling pectin formulations and on the in vitro and in vivo release of paracetamol and ambroxol from these formulations. Gelation of orally administered pectin solutions containing calcium in complexed form occurred on release of calcium in the acidic environment of the stomach. Inclusion of 10% (w/v) sorbitol in 2% (w/v) pectin sols reduced the viscosity and ensured Newtonian flow properties. Xylitol and mannitol in similar concentrations were less effective in reducing viscosity; sucrose increased viscosity and caused non-Newtonian flow. The in vitro release of paracetamol from 2% (w/v) pectin gels formulated with 10% (w/v) of sorbitol, erythritol, xylitol or mannitol, and of ambroxol from 2% (w/v) pectin gels containing 10% (w/v) sorbitol, followed diffusion-controlled kinetics. Pectin gels (2%, w/v) containing sorbitol (10%, w/v) sustained the release of paracetamol in the rat stomach and bioavailabilities of approximately 90% of those from an orally administered paracetamol syrup were achieved. Sustained release of ambroxol from in situ gelling formulations was achieved with pectin concentrations of 1.5 and 1% (w/v) and a sorbitol concentration of 10% (w/v).

Acetaminophen↗
PubMed2005

Nondestructive determination of the ambroxol content in tablets by Raman spectroscopy.

We describe a method for determining the ambroxol content in tablets nondestructively. To obtain a reliable quantitative calibration, we prepared 20 pellet samples (ambroxol content: 8.30-16.25 wt.%) and acquired their Raman spectra while rotating the pellets. The spectra of the rotated samples reflected the compositional variations better than those that were recorded without rotation. To reduce both the baseline variations and the spectral noise simultaneously, the spectra were pre-processed using wavelet transformation (WT). Then, we used the normalization method before partial least-squares (PLS) regression to correct Raman intensity variation from laser power fluctuation. The achieved standard error of cross validation (SECV) was 0.30%. Two different datasets where Raman intensity was artificially changed were prepared and the corresponding spectra were quantitatively analyzed. The result was reproducible even if laser intensity was fairly changed. Additionally, two different commercial tablets were analyzed and the accuracy of measurement was better for a tablet that had the similar spectral features of the standard pellet samples. The proposed method can be utilized for the analysis of commercial tablets if standard tablets of various ambroxol concentrations that have the same chemical components including additives and the same physical shape of tablets are available.

Ambroxol↗
PubMed2000

Identification of CYP3A4 as the predominant isoform responsible for the metabolism of ambroxol in human liver microsomes.

1. In humans, ambroxol is metabolized to dibromoanthranilic acid (DBAA) and 6,8-dibromo-3-(trans-4-hydroxycyclohexyl)-1,2,3,4-tetrahydroquinazoli ne (DHTQ). The formation of DHTQ proceeds non-enzymatically, whereas that of DBAA requires NADPH. Studies have been performed to identify the CYP isozyme(s) involved in the formation of DBAA using human liver microsomes and microsomes expressing recombinant human CYP isozymes (1A1, 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4 and 4A11). 2. The apparent Vmax and Km for the formation of DBAA were 472+/-192 pmol/ min/mg protein and 248+/-40.6 microM respectively (mean +/- S.D., n = 3). 3. Of the recombinant CYP examined, only CYP3A4 metabolized ambroxol to DBAA. The apparent Vmax and Km were 1.42 pmol/min/pmol P450 and 287 microM respectively. 4. Among the CYP inhibitors examined (furafylline, sulphaphenazole, quinidine, diethyldithiocarbamic acid, ketoconazole), only ketoconazole inhibited the production of DBAA (> 80%) at 1 microM and anti-CYP3A antiserum almost completely inhibited the formation of DBAA. 5. These results suggest that CYP3A4 is predominantly involved in the metabolism of ambroxol to DBAA in humans.

Adult↗
PubMedDate not supplied

Protective effects of ambroxol in hypothermic liver preservation: a transplant study.

The bronchosecretolytic agent ambroxol added to histidine-tryptophan-ketoglutarate (HTK) solution has recently been shown to protect cold stored rat hepatocytes. The aim of the present study was to confirm these observations in a rat liver transplantation model. Before orthotopic liver transplantation, donor livers from 30 syngeneic Wistar rats were assigned to three groups (n = 10): (A) in situ flush (ISF) and 1/2-h cold storage (CS) with HTK solution, (B) ISF and 3-h CS with HTK, and (C) ISF and 3-h CS with HTK + 10(-3) mol/L ambroxol. The efficacy of the drug was evaluated by postoperative survival (> 14 days) and liver enzyme release (ALT), bile flow, histomorphological injury, and malondialdehyde (MDA) level in the grafts 15 min after reperfusion. After 1/2-h CS with HTK solution (A), 90% of the transplanted rats survived. In comparison with donor conditions, bile flow in the reperfused grafts decreased to 87 +/- 5.3%, whereas postoperative ALT levels slightly increased. After 3-h HTK preservation (B), the survival rate decreased to 60%, while ALT values markedly increased and bile flow after reperfusion declined to 82 +/- 6.6%. Ambroxol added to HTK solution (C) enhanced bile flow to 106 +/- 3.4%(p < .05), and reduced ALT and MDA levels and histomorphological injury of the transplanted livers, so that its beneficial effect in organ preservation has been confirmed in the transplant model. However, survival rate was not improved by the agent, probably because of the low cold ischemia tolerance of the Wistar rat livers used.

Alanine Transaminase↗
PubMed1994

Ambroxol is a scavenger of hypochlorous acid and monochloramine.

Experimental studies have suggested that ambroxol, a drug clinically used to enhance pulmonary surfactant production, may also exert some anti-inflammatory effects, though specific mechanisms are not yet fully understood. Thus, potential scavenging properties of ambroxol towards the most toxic neutrophil-arising prooxidants hypochlorous acid and monochloramine were investigated. We have found that the drug at 25, 50 and 100 mumol/l exerted a significant, concentration-related antagonizing effect on both chlorine species, with a maximal specific activity detected against hypochlorous acid. These new pharmacological properties of ambroxol may play a role in vivo in disease entities characterized by white blood cell activation and uncontrolled oxidant generation, such as inflammatory/ischemic conditions.

Ambroxol↗