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PubMed1987

The in-vitro activity of roxithromycin, a new macrolide antibiotic, in comparison with that of erythromycin.

A study was made of the in-vitro activity of roxithromycin in comparison with that of erythromycin on selected recent clinical isolates of a wide range of organisms. Minimum inhibitory concentrations (MICs) were determined by an agar dilution method with an inoculum of 10(4) cfu. Minimum bactericidal concentrations (MBCs) and the effect of pH were determined by a broth dilution method on selected strains. In general the in-vitro activity of roxithromycin mirrored that of erythromycin, but it was slightly less active. Most strains of streptococci, with the exception of enterococci, were highly sensitive to roxithromycin, as were isolates of Gardnerella vaginalis. Branhamella catarrhalis and Neisseria gonorrhoeae. Staphylococci and enterococci were only moderately sensitive to both agents as was Haemophilus influenzae. Most anaerobic bacteria were sensitive although Bacteroides fragilis, fusobacteria and some strains of some clostridial species were moderately resistant. The MBCs were usually at least 16-fold higher than MICs for most staphylococci, enterococci, alpha-haemolytic streptococci and B. fragilis; but for beta-haemolytic streptococci, pneumococci, H. influenzae and B. catarrhalis the MBCs were usually only 2- to 4-fold higher than MICs. Roxithromycin was most active at pH 8 and generally for each unit fall in pH there was a 4-fold diminution of activity. However, the effect was less marked for pneumococci, beta-haemolytic streptococci and H. influenzae.

Anti-Bacterial Agents↗
PubMed1996

Modulatory effect of roxithromycin on human neutrophil function.

Neutrophils are thought to play a key role in tissue injury. We investigated the effect of roxithromycin, a 14-membered ring macrolide, on human neutrophil functions. The drug inhibited N-formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide (O2-) production and Ca2+ influx of human neutrophils. The inhibition was overcome by adding an inhibitor of cyclic AMP-dependent protein kinase (PKA), H-89. These results suggest that the drug affects O2- production and intracellular Ca2+ concentration of neutrophils via the action of PKA. Moreover, roxithromycin ameliorated endothelial cell injury induced by neutrophils, which may be, in part, due to the effect of the drug on neutrophils. Thus, roxithromycin may contribute to the treatment of diseases worsened by the excessive action of neutrophils.

Anti-Bacterial Agents↗
PubMed2000

Optimization study on the formulation of roxithromycin dispersible tablet using experimental design.

This study set out to improve the physical and pharmaceutical characteristics of the present formulation using an appropriate experimental design. The work described here concerns the formulation of the dispersible tablet applying direct compression method containing roxithromycin in the form of coated granules. In this study 2(3) factorial design was used as screening test model and Central Composite Design (CCC) associated with response surface methodology was used as optimization study model to develop and to optimize the proper formulation of roxithromycin dispersible tablet. The three independent variables investigated were functional excipients like binder (X1), disintegrant (X2) and lubricant (X3). The effects of these variables were investigated on the following responses: hardness (Y1), friability (Y2) and disintegration time (Y3) of tablet. Three replicates at the center levels of the each design were used to independently calculate the experimental error and to detect any curvature in the response surface. This enabled the best formulations to be selected objectively. The effect order of each term to all response variable was X3> X2> X1> X1*X2> X2*X2> X2*X3> X3*X3> X1*X3> X1*X1 and model equations on each response variables were generated. Optimized compositions of formula were accordingly computed using those model equations and confirmed by following demonstration study. As a result, this study has demonstrated the efficiency and effectiveness of using a systematic formulation optimization process to develop the tablet formulation of roxithromycin dispersible tablet with limited experiment.

Anti-Bacterial Agents↗
PubMed2005

Moxifloxacin monotherapy compared to amoxicillin-clavulanate plus roxithromycin for nonsevere community-acquired pneumonia in adults with risk factors.

The objective of this study was to assess the efficacy and safety of moxifloxacin versus amoxicillin-clavulanate plus roxithromycin (comparator) in adult community-acquired pneumonia (CAP) patients with risk factors. In this comparative, randomized, multicenter, open-label study, patients hospitalized for CAP received a 10-day oral treatment with either moxifloxacin (400 mg o.d.) or amoxicillin-clavulanate (1,000/125 mg t.i.d.) plus roxithromycin (150 mg b.i.d.). Clinical and bacteriological outcomes were assessed during test of cure and follow-up visits (5-7 days and 21-28 days after the end of treatment, respectively). Of 349 randomized patients, 346 were included in the intent-to-treat analysis and 289 in the per-protocol analysis. Their baseline characteristics were comparable. The most frequent risk factors for mortality were age >65 years (50.0%), alcoholism (23.1%), and comorbidities (50.6%); chronic obstructive pulmonary disease (COPD) (25.4%) and diabetes mellitus (13.6%) were the most common associated comorbidities. A causative pathogen was documented in 66 of 346 (19.1%) of the patients (including 21 with positive blood cultures). Respective per-protocol clinical success rates at test-of-cure (primary efficacy endpoint) for moxifloxacin and comparator were 131 of 151 (86.8%) and 120 of 138 (87.0%), with a 95% confidence interval (CI) of -8.0-7.6 for the difference. Bacteriological success rates (eradication) were 23 of 30 (76.7%) and 23 of 31 (74.2%); rates for patients with positive blood cultures were 10 of 14 and 4 of 6. Persistent clinical success rates at follow-up were 118 of 120 (98.3%) and 102 of 106 (96.2%), with a 95%CI of -2.2-6.4 for the difference. The intent-to-treat analysis confirmed these results. Adverse events associated with moxifloxacin and the comparator drug were reported for 42 of 171 (24.6%) and 50 of 175 (28.6%) of the patients, respectively, and comprised predominantly digestive disorders, which occurred in 9.4% and 21.1%. On the basis of these results, once-daily oral moxifloxacin alone is as effective as amoxicillin-clavulanate plus roxithromycin for the treatment of CAP in patients with risk factors.

Adult↗
PubMed2006

Long-term antibiotic treatment with roxithromycin in patients with multiple sclerosis.

BACKGROUND: There are conflicting results concerning an association between Chlamydia pneumoniae and MS (multiple sclerosis). In the present study, we investigated a possible therapeutic option with antibiotics. PATIENTS AND METHODS: In our randomized, placebo-controlled double-blind study, 28 patients with the confirmed diagnosis of MS [61% relapsing-remitting MS (RR-MS), 32% secondary chronic-progressive MS (SP-MS) and 7% primary chronic progressive MS (PP-MS)] were treated over a time period of 12 months with three cycles of a 6-week oral antibiotic therapy with roxithromycin (300 mg per day) or placebo. RESULTS: No significant differences were observed in patients with RR-MS regarding the expanded disability status scale (EDSS) and the relapse rate when comparing treatment with roxithromycin and placebo. CONCLUSION: Our study shows that the patients with MS do not profit from a long-term antibiotic treatment with roxithromycin compared to placebo treatment. A causative connection between bacterial infections with C. pneumonia and MS therefore does seem very unlikely.

Anti-Bacterial Agents↗
PubMedDate not supplied

In vitro activity of roxithromycin against Moraxella catarrhalis.

The in vitro activity of roxithromycin was compared with that of the other antimicrobial agents (erythromycin, tetracycline, ampicillin, and cotrimoxazole) against 188 distinct clinical isolates of Moraxella catarrhalis. Of these, 106 strains (66%) produced beta-lactamase. The MIC90 of roxithromycin was 0.25 micrograms/ml compared with values of 0.5, 1, greater than 8, greater than 8:0.4 micrograms/ml for erythromycin, tetracycline, ampicillin, and sulfamethoxazole-trimethoprim, respectively. These results, allied with its improved pharmacokinetic properties, suggest that roxithromycin should be an effective treatment in children and adults for upper and lower respiratory tract infections caused by M. catarrhalis.

Ampicillin↗
PubMedDate not supplied

Roxithromycin versus amoxicillin-clavulanic acid in the treatment of respiratory tract infections.

A multicenter, double-blind, double-dummy trial was conducted in 96 general practice patients with upper and lower respiratory tract infection to compare the efficacy and tolerance of roxithromycin (150 mg b.i.d.) and amoxicillin-clavulanic acid (500 mg/125 mg t.i.d.). Good clinical response was obtained in 96% and 95% of cases, respectively, but only 4% of patients receiving roxithromycin volunteered adverse events possibly or probably related to their test treatment, as opposed to 17% of those receiving amoxicillin-clavulanic acid. The results indicate that both drugs are equally effective in the treatment of respiratory tract infection, but that roxithromycin is better tolerated.

Adult↗
PubMed2006

Stochastic resonance is applied to quantitative analysis for weak chromatographic signal of roxithromycin in beagle dog plasma.

Based on the theory of stochastic resonance, the signal to noise ratio (SNR) of HPLC/UV chromatographic signal of roxithromycin is enhanced by cooperation of signal, noise and nonlinear system. A simple new method for the determination of low concentration of roxithromycin in beagle dog plasma is presented. Using signal enhancement by stochastic resonance, this method extends the limit of quantitation from the reported 0.5 to 0.1 microg/ml. During validation of the new method, HPLC/MS was used as a comparison technique. The results indicate that the recovery and low concentrations of roxithromycin in beagle dog plasma were equivalent between the two methods (P>0.05). Stochastic resonance may be a promising tool for improving detection limits in trace analysis.

Animals↗
PubMed2006

Construction of universal quantitative models for determination of roxithromycin and erythromycin ethylsuccinate in tablets from different manufacturers using near infrared reflectance spectroscopy.

Universal quantitative models using NIR reflectance spectroscopy were developed for the analysis of API contents (active pharmaceutical ingredient) in roxithromycin and erythromycin ethylsuccinate tablets from different manufacturers in China. The two quantitative models were built from 78 batches of roxithromycin samples from 18 different manufacturers with the API content range from 19.5% to 73.9%, and 66 batches erythromycin ethylsuccinate tablets from 36 manufacturers with the API content range from 28.1% to 70.9%. Three different spectrometers were used for model construction in order to have robust and universal models. The root mean square errors of cross validation (RMSECV) and the root mean square errors of prediction (RMSEP) of the model for roxithromycin tablets were 1.84% and 1.45%, respectively. The values of RMSECV and RMSEP of the model for erythromycin ethylsuccinate tablets were 2.31% and 2.16%, respectively. Based on the ICH guidelines and characteristics of NIR spectroscopy, the quantitative models were then evaluated in terms of specificity, linearity, accuracy, precision, robustness and model transferability. Our study has shown that it is feasible to build a universal quantitative model for quick analysis of pharmaceutical products from different manufacturers. Therefore, the NIR method could be used as an effective method for quick, non-destructive inspection of medicines in the distribution channels or open market.

Anti-Bacterial Agents↗
PubMed2000

Determination of roxithromycin residues in the flounder muscle with electrospray liquid chromatography-mass spectrometry.

A highly sensitive and specific method for the determination of roxithromycin in the flounder muscle by LC-MS was developed and validated. A dichloromethane extract of the sample was separated on C18 reversed-phase column with acetonitrile-50 mM ammonium acetate (80:20, v/v) as the mobile phase and analyzed by LC-MS via atmospheric pressure ionization/electrospray ionization interface. The limit of detection and limit of quantitation were 0.01 and 0.1 ng/g, respectively. Mean recoveries from spiked muscles were 81.1% (ranged from 71.0 to 90.3%) for roxithromycin. The method has been successfully applied to determine roxithromycin in the flounder muscle.

Animals↗
PubMed1991

A comparative NMR study between the macrolide antibiotic roxithromycin and erythromycin A with different biological properties.

1H nuclear Overhauser enhancement studies and 1H NMR 3J analysis establish the similarity between the major solution-state conformation of roxithromycin (1) and the erythromycin (2). A major difference between the structure of antibiotics 1 and 2 is the replacement of the 9-keto group in 2 by a 9-[O-(2,5-dioxahexyl)oxime] group. The NOE studies show that this oxime chain is oriented above the macrocyclic lactone ring and that the oxygen atoms of this chain are engaged in tight hydrogen bonding with a water molecule and with the 6- and 11-hydroxyl groups of the macrocycle. It results in a globular form of the whole roxithromycin molecule. These data explain also a relative hydrophobicity of this antibiotic. Erythromycin A (2), which presents a less rigid macrocycle with two free hydroxyl groups (6-OH and 11-OH), forms a dimer detected by FAB mass spectroscopy. 1H and 13C NMR relaxation measurements (T1) for both antibiotics show that interresidue hydrogen bonds in roxithromycin reduce the rotational freedom of the macrocyclic lactone ring and consequently the motions of desosamine and cladinose sugars. In another way, an ionization of the amino function occurs in the various media according to the nature of the antibiotic. This would allow the reactivity modification of the desosamine unit. In the biological study, the modifications of the 455-nm metabolite-cytochrome P-450 complex formation are observed.

Crystallization↗
PubMed1990

A model to detect interactions between roxithromycin and oral contraceptives.

Twenty-two healthy women participated in a study to determine whether roxithromycin (a new macrolide antibiotic agent) obtunds the activity of a triphasic oral contraceptive. The duration of the study was four menstrual cycles. Medication was given as follows: (1) cycle 1, no medication to demonstrate ovulation; (2) cycle 2, triphasic oral contraceptive daily to suppress ovulation; (3) cycle 3, triphasic oral contraceptive daily plus roxithromycin, 150 mg b.i.d.; and (4) cycle 4, triphasic oral contraceptive daily plus rifampin, 300 mg daily. Sonography of the ovaries was performed on day 13, and serum progesterone was measured on day 21 of each cycle. Elevated progesterone indicated ovulation. The presence of a maturing follicle supported this finding. All volunteers ovulated in the first cycle and no volunteers ovulated in the second and third cycles. However, 11 women ovulated when rifampin and the triphasic oral contraceptive were given concomitantly. The findings suggest there is no reason to believe that roxithromycin interferes with the efficacy of oral contraceptives.

Adolescent↗
PubMed1995

Effect on Pseudomonas aeruginosa alginate expression of direct plating and culture of fresh cystic fibrosis sputum on to pseudomonas isolation agar containing subinhibitory concentrations of roxithromycin and rifampicin.

The effects of subinhibitory concentrations of roxithromycin (16 mg/L) or rifampicin (16 mg/L) on alginate production by Pseudomanas aeruginosa were investigated. The weight of purified alginate from antibiotic-free cultures was significantly greater (52.5 +/- 24.0 mg, range 22.4-109.5), compared with alginate from cultures bacteria exposed to sub-MIC of roxithromycin (21.9 +/- 17.0, 0.0-42.1 (P < or = 0.037)) and to sub-MIC of rifampicin (28.6 +/- 15.0, 2.9-47.5 (P < or = 0.038)). Chromatographic analysis of hydrolysed and chemically transformed sub-units of alginate revealed that the presence and the molar ratio of D-mannuronic acid and L-guluronic acid were not affected in the remnant alginate exposed to sub-MIC of roxithromycin in contrast to that in the remnant alginate exposed to sub-MIC of rifampicin.

Alginates↗
PubMed1998

Comparative anti-inflammatory effects of roxithromycin, azithromycin and clarithromycin.

There are many published reports on the anti-inflammatory effects of macrolides, some dating back to the introduction of erythromycin. Macrolides have been shown to affect a number of the processes involved in inflammation, including the migration of neutrophils, the oxidative burst in phagocytes and the production of various cytokines, although the precise mechanisms are not clear. These effects have been linked to the ability of macrolides to accumulate in mammalian cells. Roxithromycin, a macrolide with better plasma concentrations and higher tissue concentrations than erythromycin, has been tested in a standard animal model used for evaluating anti-inflammatory drugs. When rats were given a prophylactic dose (20 mg/kg), roxithromycin suppressed the oedema produced by injecting carrageenin into the paw with effects almost equal to that seen with the non-steroidal anti-inflammatory drug nimesulide. Azithromycin and clarithromycin, macrolides with better pharmacokinetics than erythromycin, only showed slight anti-inflammatory effects. These results confirm that roxithromycin has anti-inflammatory properties in vivo and encourage the investigation of its mode of action.

Animals↗
PubMed1998

Roxithromycin treatment for diarrhoea caused by Cryptosporidium spp. in patients with AIDS.

In view of the action of newer macrolide antibiotics on intracellular protozoa, we have investigated the efficacy of roxithromycin in the treatment of cryptosporidiosis in 26 patients with AIDS. Cryptosporidiosis was confirmed either by faecal examination for parasites (modified Kinyoun method) or by detection of the parasite in biopsy material obtained by colonoscopy. Patients received oral roxithromycin (300 mg bd) for 4 weeks. Twenty-two patients completed the study. At the end of the study, 15 patients (68%) were considered to be cured and six patients (27%) improved, and treatment failed in one patient (5%). We conclude that roxithromycin is a useful treatment for diarrhoea caused by Cryptosporidium spp. associated with AIDS.

AIDS-Related Opportunistic Infections↗
PubMed2003

Roxithromycin treatment of scrub typhus (tsutsugamushi disease) in children.

BACKGROUND: Although chloramphenicol and doxycycline have been used for the treatment of scrub typhus, a difficulty exists in determining which drug to use in treating children because of such potential complications as aplastic anemia or tooth discoloration. We evaluated the effect of roxithromycin, a macrolide antibiotic, on scrub typhus in children. METHODS: A retrospective analysis was conducted on 39 children with scrub typhus who were treated with doxycycline (DC), chloramphenicol (CM) or roxithromycin (RM) between 1991 and 2000. We divided the patients into the DC-treated group (DC group; 16 children), CM-treated group (CM group; 14 children) and RM- treated group (RM group; 9 children) and compared these groups. RESULTS: Most cases (97%) occurred in October and November. Fever and rash were observed in all 39 cases, and an eschar was noted in 36 cases (92%). No statistical differences could be found between the 3 groups in mean age, duration of fever before admission, white blood cell (WBC) count and complications including abnormal liver enzymes. In most cases defervescence after treatment was within 24 h (34 cases, 87%) and during 24 to 48 h in 2 cases in the DC group, 1 case in the CM group and 2 cases in the RM group (no statistical difference). CONCLUSION: Roxithromycin was as effective as conventional doxycycline or chloramphenicol in children with scrub typhus and may be safer to use.

Adolescent↗
PubMed2006

Roxithromycin inhibits transforming growth factor-beta production by cultured human mesangial cells.

BACKGROUND: Transforming growth factor-beta (TGF-beta) plays an important role in progression of renal injury. However, few materials which inhibit TGF-beta have been known. Roxithromycin (ROX), macrolide antibiotics, is known to have anti-inflammatory, immunomodulatory and tissue reparative effects besides its bacteriostatic activity, although the exact mechanism of its anti-inflammatory and immunomodulatory effects was not defined. We examined the effect of ROX on production of TGF-beta and type IV collagen by cultured human mesangial cells (HMC). METHODS: Human mesangial cells were incubated with several concentrations of ROX and TGF-beta and type IV collagen levels in the culture supernatants were measured by enzyme-linked immunoassay. Amount of TGF-beta mRNA was also quantified by using a colourimetric mRNA quantification kit and semiquantitative reverse transcriptase polymerase chain reaction. We also examined the effect of ROX on tyrosine kinase, MAP kinase and NF-kappaB stimulated by thrombin. RESULTS: Roxithromycin (0.1-10.0 microg/mL) inhibited TGF-beta production by HMC in a dose- and time-dependent manner without inducing cell injury. ROX (10.0 microg/mL) also inhibited mRNA expression of TGF-beta in HMC. Thrombin (5 U/mL) stimulated TGF-beta production by HMC and ROX significantly inhibited the stimulating effect of thrombin on TGF-beta production. ROX also inhibited the increment of type IV collagen production stimulated by thrombin. ROX (10.0 microg/mL) suppressed the thrombin-induced NF-kappaB activation, although ROX did not inhibit the activation of tyrosine kinase and MAP kinase by thrombin. CONCLUSION: Roxithromycin has an inhibitory effect on TGF-beta production by HMC possibly via inhibition of NF-kappaB. ROX may be a potential agent for the treatment of glomerulosclerosis.

Anti-Bacterial Agents↗
PubMed2003

Erythromycin, roxithromycin, and clarithromycin: use of slow-binding kinetics to compare their in vitro interaction with a bacterial ribosomal complex active in peptide bond formation.

In a cell-free system derived from Escherichia coli, it is shown that clarithromycin and roxithromycin, like their parent compound erythromycin, do not inhibit the puromycin reaction (i.e., the peptide bond formation between puromycin and AcPhe-tRNA bound at the P-site of 70S ribosomes programmed with heteropolymeric mRNA). Nevertheless, all three antibiotics compete for binding on the ribosome with tylosin, a 16-membered ring macrolide that behaves as a slow-binding, slowly reversible inhibitor of peptidyltransferase. The mutually exclusive binding of these macrolides to ribosomes is also corroborated by the fact that they protect overlapping sites in domain V of 23S rRNA from chemical modification by dimethyl sulfate. From this competition effect, detailed kinetic analysis revealed that roxithromycin or clarithromycin (A), like erythromycin, reacts rapidly with AcPhe-tRNA.MF-mRNA x 70S ribosomal complex (C) to form the encounter complex CA which is then slowly isomerized to a more tight complex, termed C*A. The value of the overall dissociation constant, K, encompassing both steps of macrolide interaction with complex C, is 36 nM for erythromycin, 20 nM for roxithromycin, and 8 nM for clarithromycin. Because the off-rate constant of C*A complex does not significantly differ among the three macrolides, the superiority of clarithromycin as an inhibitor of translation in E. coli cells and many Gram-positive bacteria may be correlated with its greater rate of association with ribosomes.

Anti-Bacterial Agents↗