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PubMed2004

Roxithromycin suppresses mucin gene expression in epithelial cells.

Macrolide antibiotics are believed to inhibit mucus secretion but the mechanism of action is unclear. This study was designed to investigate an effect of roxithromycin on MUC2 gene expression in cultured intestinal epithelial cells (HM3-MUC2 cells). A reporter gene assay was used for analysis. Roxithromycin suppressed MUC2 gene transcriptional activity in a dose-dependent manner in HM3-MUC2 cells. Phorbol 12-myristate 13-acetate (PMA), lipoteichoic acid (LTA), lipopolysaccharide (LPS) and leukotriene D4 (LTD4) significantly increased MUC2 luciferase activities in the following order: PMA > LTA > LTD4 > LPS. Roxithromycin also decreased MUC2 gene transcriptional activity induced by PMA in a dose-dependent manner. NF-kappaB activation, but not AP-1 activation, was significantly suppressed by roxithromycin in HM3-MUC2 cells. A suppression of NF-kappaB activation was also observed in NCI-H292 cells. These results suggest that roxithromycin suppresses MUC2 gene expression in epithelial cells and that this suppression is probably via inhibition of NF-kappaB activation.

Anti-Bacterial Agents↗
PubMed2002

Roxithromycin treatment prevents progression of peripheral arterial occlusive disease in Chlamydia pneumoniae seropositive men: a randomized, double-blind, placebo-controlled trial.

BACKGROUND: Evidence has been provided that the atherosclerotic process may be associated with chronic infection with Chlamydia pneumoniae. The effect of antibiotic treatment on peripheral arterial occlusive disease has not been investigated yet. METHODS AND RESULTS: Forty C pneumoniae seropositive men suffering from peripheral arterial occlusive disease were randomly assigned to receive either roxithromycin (300 mg daily) or placebo for 28 days. During the 2.7-year follow-up, the number of invasive revascularizations per patient, the walking distance before intervention (in patients without intervention at study end), and the change of carotid plaque size were assessed. Five interventions were performed on 4 patients (20%) in the roxithromycin group, and 29 interventions were performed on 9 patients (45%) in the placebo group. Limitation of walking distance to 200 m or less was observed in 4 patients (20%) in the roxithromycin group and in 13 patients (65%) in the placebo group. The effect of macrolide treatment on the number of interventions per patient and on preinterventional walking distance was significant. Possible confounding variables such as classical vascular risk factors were excluded by multiple regression analyses. Carotid plaque areas monitored over 6 months decreased in the roxithromycin group (mean relative value, 94.4%) but remained constant in the placebo group (100.2%). Regression of carotid plaque size observed in roxithromycin-treated patients was significant for soft plaques. CONCLUSIONS: This study indicates that macrolide treatment for 1 month is effective in preventing C pneumoniae seropositive men from progression of lower limb atherosclerosis for several years.

Aged↗
PubMed2001

Trial of roxithromycin in subjects with asthma and serological evidence of infection with Chlamydia pneumoniae.

An association has been reported between chronic infection with Chlamydia pneumoniae and the severity of asthma, and uncontrolled observations have suggested that treatment with antibiotics active against C. pneumoniae leads to an improvement in asthma control. We studied the effect of roxithromycin in subjects with asthma and immunoglobulin G (IgG) antibodies to C. pneumoniae > or = 1:64 and/or IgA antibodies > or = 1:16. A total of 232 subjects, from Australia, New Zealand, Italy, or Argentina, were randomized to 6 wk of treatment with roxithromycin 150 mg twice a day or placebo. At the end of 6 wk, the increase from baseline in evening peak expiratory flow (PEF) was 15 L/min with roxithromycin and 3 L/min with placebo (p = 0.02). With morning PEF, the increase was 14 L/min with roxithromycin and 8 L/min with placebo (NS). In the Australasian population, the increase in morning PEF was 18 L/min and 4 L/min, respectively (p = 0.04). At 3 mo and 6 mo after the end of treatment, differences between the two groups were smaller and not significant. Six weeks of treatment with roxithromycin led to improvements in asthma control but the benefit was not sustained. Further studies are necessary to determine whether the lack of sustained benefit is due to failure to eradicate C. pneumoniae.

Adult↗
PubMedDate not supplied

Concentration of roxithromycin in the lesions of acne vulgaris.

Roxithromycin, a macrolide antibiotic, is used in the treatment of acne vulgaris, although there have been no reports on its concentration in lesions when administered orally. We investigated the concentration of roxithromycin in acne vulgaris lesions in five patients who received 150 mg roxithromycin orally twice daily for 2 weeks. The mean concentration of roxithromycin in the lesions was 0.54 microgram/ml. These results suggest that roxithromycin accumulates at therapeutic levels in the pilosebaceous system.

Acne Vulgaris↗
PubMed1994

Roxithromycin reduces the degree of bronchial hyperresponsiveness in children with asthma.

We evaluated the effects of a new semisynthetic macrolide antibiotic, roxithromycin, on the bronchial hyperresponsiveness to histamine in children with asthma. Twelve hospitalized asthmatic children, aged 11 to 15 years (mean age, 12.9 years), were enrolled in this study. They were treated with 150 mg of roxithromycin once a day orally for 8 weeks without any side effects. The PC20 value 4 or 8 weeks after the administration of roxithromycin increased significantly over the initial values (p < 0.05, p < 0.01, respectively). No significant change was observed in serum theophylline concentrations during this study. Serum cortisol level in the morning did not change after the administration of roxithromycin for 4 weeks. These results suggest that administration of roxithromycin may act favorably in the treatment of childhood asthma.

Adolescent↗
PubMed2006

In vitro monitoring picogram roxithromycin in human urine using flow injection chemiluminescence procedure.

A sensitive chemiluminescence method, based on the enhancive effect of roxithromycin on the chemiluminescence reaction between luminol and hydrogen peroxide in a flow injection system, was proposed for the determination of roxithromycin. The increment of chemiluminescence intensity was linear with roxithromycin concentration in the range 1.0-1000 pg ml(-1) with the detection limit of 0.3 pg ml(-1) (3sigma). At a flow rate of 2.0 ml min(-1), a complete analytical process could be performed within 0.5 min, including sampling and washing, with a relative standard deviation of less than 5%. The proposed procedure was applied successfully in the monitoring of roxithromycin in human urine without any pre-treatment procedures and it was found that roxithromycin in urine reached its maximum after orally administrated for two hours, presenting an excretive ratio of 4.6% in 12 h. With urinary excretion rate method, the total elimination rate constant k and half-life time t(1/2) of roxithomycin was calculated, which was 0.1831, 3.785 h.

Anti-Bacterial Agents↗
PubMed1997

Roxithromycin attenuates acid-induced cough and water-induced bronchoconstriction in children with asthma.

In the present study, we evaluated the effect of roxithromycin, a semisynthetic macrolide antibiotic, on the cough response to inhaled acetic acid (AA) and on the bronchoconstriction induced by ultrasonically nebulized distilled water (UNDW) in children with asthma. Ten hospitalized asthmatic children (8 boys and 2 girls, mean +/- SEM age 12.6 +/- 0.4 years) were enrolled in this study. They were treated with 150 mg of roxithromycin once a day orally for 8 weeks without any side effects. All the patients underwent AA inhalation challenge before and 2, 4, and 8 weeks after the administration of roxithromycin. Seven of the 10 patients, who had a fall in FEV1 of at least 20% after UNDW inhalation, underwent UNDW inhalation challege at the same time. The cough threshold values, the lowest concentrations of AA eliciting coughs, and UNDW provocative dose producing a 20% fall in FEV1 (UNDW PD20) values 4 or 8 weeks after the administration of roxithromycin increased significantly over the initial values (p < 0.05). No significant change was observed in baseline FEV1 or serum theophylline concentrations throughout the study. These results support the notion that administration of roxithromycin may have favorable results in the treatment of childhood asthma.

Acetic Acid↗
PubMed1999

[Diagnosis and ambulatory treatment of patients with community-acquired pneumonia: variability of complementary tests and study of the effectiveness of roxithromycin. Study Group on Ambulatory Treatment of Community-Acquired Pneumonia (NACTA)].

BACKGROUND: Community-acquired pneumonia (CAP) has been the subject of a number of studies. Nevertheless, studies focused on effectiveness of therapy and variability of diagnostic tests are scarce. PATIENTS AND METHODS: Observational study of the diagnostic methodology used in patients attending hospital Emergency Departments for possible CAP and assessment of effectiveness and reliability of empiric ambulatory therapy with roxithromycin (150 mg/12 h, for a minimum of ten days). The only mandated complementary tests included PA and lateral chest X-ray views and blood count. Microbiological tests were left to the discretion of the attending physician. Clinical and biological follow-up of the patient consisted of three outpatient visits. RESULTS: The study was conducted at 18 spanish hospitals from October 1997 to March 1998. The final total of patients with CAP enrolled was 161 (75 women and 86 men). Three patients required hospital admission. In a 3% of patients the Gram staining of the sputum specimen was performed; in 53% of patients blood cultures were obtained (3.4% were positive) and in 23% of patients serological determinations are performed (16.7% were positive). The final microbiological results led to the disclosure of the etiologic agent of CAP in 5.5% of patients. In only one patient did the results prompt a change in antibiotic therapy. The clinical course was favorable in 92.5% of patients. In 12 patients (7.5%) a change of antibiotic was made or a second antibiotic was added. The mean therapy duration with roxithromycin was 11.9 days (range: 7-22 days). In five patients (3.1%), the observed adverse events were attributed to roxithromycin, and in no case was discontinuation of therapy necessary. CONCLUSIONS: The variability of diagnostic tests used in patients with CAP is remarkable but their yield is of little effect. Patients with CAP candidates for ambulatory therapy can receive empiric antibiotic therapy with roxithromycin. In this series, roxithromycin had a high clinical effectiveness and was well tolerated.

Adolescent↗
PubMedDate not supplied

CD8+ cell changes in psoriasis associated with roxithromycin-induced clinical improvement.

We have shown that T cell receptor BV2- and BV8-bearing CD8+ cells are decreased in the peripheral blood of psoriatic patients, while T cells possessing these BVs accumulate in psoriatic lesions. T cells homing to skin express cutaneous lymphocyte-associated antigen (CLA), and bacterial superantigens that trigger psoriasis promote this expression. Roxithromycin has immunomodulatory potency and its effectiveness for psoriasis has been proposed. Therefore, we monitored BV usage and alteration of superantigen-promoted CLA expression in circulating CD8+ cells of psoriatics before and after roxithromycin therapy. After roxithromycin treatment, circulating BV2- and BV8-bearing CD8+ cells were increased and CD8+ cells exhibited reduced expression of CLA when stimulated in vitro with bacterial superantigens. It is suggested that roxithromycin downregulates augmented expression of CLA by CD8+ cells, thereby suppressing their skin-homing and elevating the numbers of circulating BV2- and BV8-positive CD8+ cells. Such events may be included in part in the improvement of psoriasis with roxithromycin.

Adult↗
PubMed2002

Is roxithromycin better than amoxicillin in the treatment of acute lower respiratory tract infections in primary care? A double-blind randomized controlled trial.

OBJECTIVE: To assess the efficacy of roxithromycin relative to amoxicillin. STUDY DESIGN: We conducted a double-blind randomized controlled trial of oral 500 mg amoxicillin 3 times per day vs oral 300 mg roxithromycin once a day for 10 days. POPULATION: We included 196 adults who had presented to a general practitioner with lower respiratory tract infection (LRTI) and, in the physician's opinion, needed antibiotic treatment. OUTCOMES MEASURED: We measured clinical response after 10 and 28 days, defined in 4 ways: (1) decrease in LRTI symptoms; (2) complete absence of symptoms; (3) decrease in signs; and (4) complete absence of signs. Self-reported response included the decrease in symptoms and the time until resumption of impaired or abandoned daily activities on days 1 through 10, 21, and 27. RESULTS: Clinical cure rates after the completion of antibiotic treatment (10 days) were not significantly different for the 2 groups. After 28 days, the roxithromycin group showed no increase in cure rate as evidenced by the decrease in symptoms, indicating a significantly lower cure rate. However, this difference did not alter physicians' overall conclusion after complete follow-up that 90% of patients, regardless of age, had been effectively treated with either amoxicillin or roxithromycin. CONCLUSIONS: The surplus value of roxithromycin was not confirmed. Amoxicillin remains a reliable first-choice antibiotic in the treatment of LRTI in general practice.

Adult↗
PubMedDate not supplied

Experimental estimation of the role of P-Glycoprotein in the pharmacokinetic behaviour of telithromycin, a novel ketolide, in comparison with roxithromycin and other macrolides using the Caco-2 cell model.

PURPOSE: The aim of this study was to examine the transport mechanism of telithromycin in comparison with erythromycin, azithromycin, clarithromycin and roxithromycin. METHODS: These antibiotics were examined in Caco-2 cell monolayers in order to demonstrate the potential involvement of P-GP in the absorption process, using verapamil as a P-GP competitor. A model using concentration equilibrium conditions was developed to delineate passive and active permeability components of telithromycin and roxithromycin transport in order to predict absorption in humans. RESULTS: Comparison of telithromycin Papp(AB)/Papp(BA) ratios with those of the other antibiotics indicated that an efflux pump was involved which limited the transport of the macrolides to a greater extent than that of telithromycin. Modulation of Caco-2 transport of these antibiotics by verapamil and their reciprocal effect upon verapamil transport confirmed the involvement of P-GP and demonstrated that two substrates of P-GP may increase the transport of each other. Under concentration equilibrium conditions, both roxithromycin and telithromycin exhibited high mean Papp values for passive diffusion which extrapolated to 88% and 77% predicted human absorption respectively, if the involvement of P-GP was ignored. Both Km and Vm values suggested that saturation of P-GP by telithromycin may occur at a lower dose level in humans than with roxithromycin (Km= 9.8 microM, Vm= 0.3 microM and Km= 45 microM, Vm= 1.1 microM, respectively). At 4.10(-5) M of either telithromycin or roxithromycin the passive flux was respectively 48% and 16% greater than the active efflux. CONCLUSIONS: The high absorption potential of telithromycin combined with the low Km and Vm values and the high dose level suggest that in humans the efflux pump may not limit ketolide absorption and that the interaction with other P-GP substrates may not significantly increase its oral absorption.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed2003

[Spectrophotometry determination of roxithromycin based on charge transfer reaction].

A spectrophotometric method for the determination of Roxithromycin has been developed based on the charge transfer reaction between Roxithromycin as donor and cresol red as acceptor. The conditions of reaction have been studied. The reaction time, reaction temperature, reaction medium and the concentration of reagent was ten min, 35 degrees C, alcohol-acetone solution and 6 x 10(-4) mol.L-1 respectively. The apparent molar absorptivity of complex was 1.05 x 10(4) L.mol-1.cm-1 at 456 nm. The Beer's law was obeyed in the range of 0-80 mg.L-1 of Roxithromycin with correlation coefficient 0.9997. The recovery was over 98%. The composition of the charge transfer complex between Roxithromycin and cresol red was 1:1. The reaction mechanism has been discussed based on the composition of the complex. The present method has been applied to the determination of Roxithromycin in capsules with satisfactory results.

Anti-Bacterial Agents↗
PubMed2003

[Metabolism of roxithromycin in dogs].

AIM: To investigate the metabolic profile of roxithromycin in dogs and the effects of oral and intravenous administrations on the metabolism of roxithromycin. METHODS: Liquid chromatography-tandem mass spectrometry (LC-MSn) was used for separation and analysis of roxithromycin and its metabolites in dog bile after an oral dose or intravenous dose of roxithromycin. The metabolites were identified by comparisons of their mass spectra and LC behaviors with the references. RESULTS: Totally 13 metabolites were detected in dog bile, including N-demethylated derivatives, N, N-didemethylated derivatives, O-dealkylether derivatives, decladinose derivatives, and the geometric isomers of parent drug and its metabolites. CONCLUSION: Roxithromycin underwent 4 metabolic pathways in which geometric isomerization and decladinose metabolism were found to be markedly different between the two administration routes.

Administration, Oral↗
PubMed1992

[Roxithromycin in dental infections].

Roxithromicin is a semisynthetic macrolide antibiotic, with similar antibacterial activity to erythromycin. It is characterized by an excellent pharmacokinetic profile and a good tissue penetration. Particularly at the dose of 300 mg per day the dental tissue diffusion is extremely good, and this is important to oppose the oral cavity infections. Oral cavity infections can be either odontogenic or non odontogenic. Odontogenic infections are typically primary and are caused by commensal bacteria (oral Streptococci, Bacteroides sp., Veillonella sp. and Fusobacterium sp.). The antibacterial spectrum of roxithromycin is very large and includes many of the most frequent strains responsible for oral cavity infections. A very interesting characteristic of roxithromycin is its penetration in macrophages (uptake) that allow a more rapid inhibition of bacterial activity. To evaluate the clinical efficacy and tolerance of roxithromycin in the treatment of odontogenic infections, an open study was performed. This study evaluated both the microbiological and clinical aspects. Thirty patients (21 females and 9 males) who had not been previously treated with antibiotic or antibacterial drugs, affected by infective dysodontiasis, gingivitis and periodontal diseases, received 300 mg per day (once a day) of roxithromycin for an average period of 6 days. The symptomatology considered was: intumescence, redness, pain, lymphangitis and presence of trismus. Clinical symptomatology was assessed at the start and at the end of the treatment. The symptomatological improvement due to roxithromycin was rapid and very effective. After 6 days of therapy, the improvement was statistically significant (p < 0.01) compared to basal conditions. No adverse reactions or side-effects were complained during the study. No changement were detected in laboratory parameters.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1994

[Susceptibility to roxithromycin of gram-positive cocci isolated from patients with lowered immunity].

The study involved 412 strains of Gram-positive cocci isolated from throat, sputum, urine and stool of patients prepared for bone marrow transplantation at Department of Hematology. Determination of drug susceptibility was performed by disc diffusion method applying discs with roxithromycin, erythromycin, lincomycin, clindamycin and augmentin. Among strains of S. aureus, S. epidermidis and Micrococcus susceptible strains comprised respectively 48, 48 and 45%; among group A, B, C and G streptococci respectively 92 and 52%. Among 108 strains of group D Streptococci only 24% were susceptible to roxithromycin. Comparison of susceptibility of tested strains to roxithromycin and other antibiotics revealed similar susceptibility of staphylococci and streptococci to roxithromycin and erythromycin, while among staphylococci higher percentage of strains and among streptococci lower percentage was susceptible to lincomycin than to roxithromycin.

Anti-Bacterial Agents↗
PubMed1988

Evaluation of roxithromycin (RU-965) versus cephradine in pneumococcal pneumonia.

One hundred and sixty black South African gold miners with acute pneumococcal pneumonia were enrolled in a prospective randomized double-blind trial comparing roxithromycin (150 mg 2 X day) with cephradine (1.0 g 2 X day). Ninety patients with pneumonia caused by Streptococcus pneumoniae were treated for 5-10 days. Forty-three of 46 (93.4%) of the roxithromycin and all 44 (100%) of the cephradine treated groups had satisfactory clinical responses. In eight of the 46 (17%) roxithromycin treated patients and 10 of the 44 (23%) cephradine treated patients, Streptococcus pneumoniae was not eradicated from sputum cultures by the tenth day. Side effects in 18 patients (20%) were mild and were usually manifested by elevation of the transaminases; these were more common in the cephradine group (12) than in the roxithromycin group (5). Roxithromycin appears to be a safe and effective oral antibiotic for treatment of patients with mild to moderate pneumococcal pneumonia.

Adult↗
PubMed1987

Factors affecting the in-vitro activity of roxithromycin.

The effect of human serum and CO2 on the activity of roxithromycin and erythromycin was assessed. Protein binding of roxithromycin in serum from various animal sources, acid alpha 1-glycoprotein and human albumin V was determined. There was a four- to eight-fold increase in MIC and MBC of roxithromycin in the presence of 70 and 100% human serum (minimum effect seen with erythromycin) and for both compounds there was a four- to eight-fold increase in MIC for fastidious organisms in the presence of CO2. Roxithromycin appears to be selectively bound to acid alpha 1-glycoprotein, binding decreases with an increase in roxithromycin concentration (saturable at 10 mg/l) and protein binding is variable depending on animal source (86% human, 10% guinea pig) and this must be considered when data on activity from animal studies are evaluated.

Animals↗
PubMed1987

Activity of roxithromycin against Toxoplasma gondii in murine models.

Investigations into the activity of roxithromycin against murine toxoplasma infections are reviewed. Roxithromycin is an active drug against murine toxoplasmosis after intraperitoneal challenge with the RH strain of Toxoplasma gondii. Roxithromycin protected 100% of mice after five daily doses of 540 mg per kg administered by gavage. The cure rate after treatment of peritoneal infections seemed to be related to the length of the therapy. Roxithromycin also decreased the number of toxoplasma cysts, after intracerebral infection with the C56 strain and showed synergistic activity when combined with gamma interferon. Thus, roxithromycin could be a worthwhile alternative to current therapy against toxoplasma infections. Clinical studies on its activity and safety, especially in pregnancy, are warranted.

Animals↗