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PubMed1998

Characteristic difference in gastrointestinal excretion of clarithromycin and roxithromycin.

Excretion characteristics of two new macrolides; clarithromycin and roxithromycin, into the intestinal and the gastric lumens was studied by in situ single-pass perfusion and loop methods in rats. Roxithromycin maintained higher serum levels than clarithromycin after their intravenous administrations at a dose of 5 mg kg(-1) each. Radioactivities of clarithromycin and roxithromycin exsorbed into the intestinal lumen were 8.6 and 18.9% of dose in 2 h, respectively, whereas clarithromycin and roxithromycin excreted into the bile were 28.4 and 5.9%, respectively. These results suggest that roxithromycin is transported mainly by exsorption across the intestinal membrane, whereas clarithromycin mainly by excretion through the biliary tract. On the other hand, radioactivities of clarithromycin and roxithromycin exsorbed into the gastric lumen were much less then those into the intestinal lumen and were 0.72 and 1.34% of dose in 4 h, respectively. Thus, the exsorption into the gastric lumen seems to be a minor route for the elimination of both macrolides. Consequently, the transport into the intestinal lumen via the intestinal membrane and/or the bile tract may play a significant role in the overall elimination of both macrolides.

Animals↗
PubMed2005

Determination of roxithromycin in rat lung tissue by liquid chromatography-mass spectrometry.

A liquid chromatography-mass spectrometry (LC-MS) method for the determination of roxithromycin in rat lung tissue is described. Liquid-liquid extraction was adopted for sample preparation with recoveries from 72.5 to 76.9% at levels of 0.1, 5.0 and 20.0 microg/ml. Chromatographic separation was performed on a C18 column using a mixture of methanol, water and formic acid (80:20:1, v/v/v) as mobile phase delivered at a flow rate of 0.5 ml/min. Positive selected ion monitoring (SIM) mode was used for the quantification of roxithromycin at m/z 837.7 and clarithromycin (internal standard) at m/z 748.7. The linearity was obtained over the concentration range of 0.05-20.0 microg/ml and the lower limit of quantification was 0.05 microg/ml. For each QC level of roxithromycin, the intra- and inter-day precisions relative standard deviation (R.S.D.) were less than 4.1 and 7.5%, respectively, and accuracy (RE) was +/-10.0%. The proposed LC-MS method has been successfully used for the determination of roxithromycin in rat lung tissue after oral administration of roxithromycin formulations to 44 SD rats. The present study demonstrates that the concentration of roxithromycin in rat lung tissues can be significantly increased by ambroxol when they are formulated in combination.

Ambroxol↗
PubMed2001

Treatment of Chlamydia pneumoniae infection with roxithromycin and effect on neointima proliferation after coronary stent placement (ISAR-3): a randomised, double-blind, placebo-controlled trial.

BACKGROUND: Vascular infection with Chlamydia pneumoniae might boost inflammatory responses that play a pivotal part in neointima formation, which is the main cause of restenosis after stenting. Our aim was to investigate whether or not treatment of C pneumoniae infection with antibiotics prevents restenosis after coronary stent placement. METHODS: We enrolled 1010 consecutive patients with successful coronary stenting into a randomised, double-blind trial. Patients received the macrolide antibiotic roxithromycin 300 mg once daily for 28 days (506), or placebo (504). Primary endpoint was frequency of restenosis (diameter stenosis >50%) at follow-up angiography, and secondary endpoint was rate of target vessel revascularisation during the year after stenting. A prespecified secondary analysis addressed treatment effect with respect to titre of C pneumoniae in serum. Analysis was by intention to treat. FINDINGS: Rate of angiographic restenosis was 31% (157 lesions) in the roxithromycin group and 29% (148) in the placebo group (relative risk 1.08 [95% CI 0.92-1.26]; p50.43), corresponding to a rate of target vessel revascularisation of 19% (120) and 17% (105), respectively (1.13 [0.95-1.36]; p50.30). The combined 1-year rates of death and myocardial infarction were 7% (36) in the roxithromycin group and 6% (30) in the placebo group (p50.45). We showed a significant interaction between treatment and C pneumoniae antibody titre (p50.038 for restenosis, p50.006 for revascularisation), favouring roxithromycin at high titres (adjusted odds ratios at a titre of 1/512 were 0.44 [0.19-1.06] and 0.32 [0.13-0.81], respectively). INTERPRETATION: Non-selective use of roxithromycin is inadequate for prevention of restenosis after coronary stenting. There is, however, a differential effect dependent on C pneumoniae titres. In patients with high titres, roxithromycin reduced the rate of restenosis.

Aged↗
PubMed1999

Treatment with the antibiotic roxithromycin in patients with acute non-Q-wave coronary syndromes. The final report of the ROXIS Study.

AIMS: Mounting evidence suggests infection, specifically Chlamydia pneumoniae, plays a role in atherosclerosis. We tested whether antibiotic treatment with the macrolide roxithromycin improves clinical outcome in patients with acute non-Q-wave coronary syndromes. Preliminary reports revealed a reduction in events in the roxithromycin group at 30 days. We now report the long-term follow-up results. METHODS AND RESULTS: Sixty-four per cent of the initial 202 patients with unstable angina who were randomly assigned to receive either roxithromycin or placebo for 30 days completed the active treatment period. At day 30, the primary triple and double end-point rates were 9% and 4% in the placebo group compared to 2% and 0% in the roxithromycin group (unadjusted P = 0.032 and 0.058, respectively). The secondary triple and double end-point rates were again higher in the placebo group at day 90 (12.5% and 6.25% vs 4.37% and 0%, unadjusted P = 0.065 and 0.029, respectively), and at day 180 (14.6% and 7.29% vs 8.69% and 2.17%, unadjusted P = 0.259 and 0.17, respectively). Anti-C, pneumoniae IgG titres were unchanged in both groups while C-reactive protein levels decreased in both strategies, with a more significant decrease in the roxithromycin arm (P = 0.03). Elevated C-reactive protein levels predicted the need for revascularization. CONCLUSIONS: In this pilot trial, roxithromycin appears to extend the clinical benefit of preventing death and re-infarction for at least 6 months after initial treatment.

Aged↗
PubMed1996

Economic analysis of antibiotic regimens used in the treatment pharyngitis: a prospective comparison of azithromycin versus roxithromycin.

The economic impacts in terms of cost and effectiveness (speed of resolution of symptoms) of 3- and 5-day courses of azithromycin and a 10-day course of roxithromycin were compared in a randomized, open study in patients with symptoms suggestive of beta-haemolytic streptococcal pharyngitis. Direct medical costs and absence from work were recorded and symptom scores and compliance were used to assess the effectiveness of therapies. Although no differences between treatment groups in terms of overall clinical response rates were detected 2 and 4 weeks after the start of treatment, more rapid resolution of symptoms was achieved with 3- and 5-day courses of azithromycin than with a 10-day course of roxithromycin. There was also a significant reduction in the time absent from work in the azithromycin treatment groups. The total costs of care over the 4-week evaluation period were lower for the 3- and 5-day azithromycin courses (US$193.60 and US$195.30 respectively) than for roxithromycin (US$202.10). The major cost components were absence from work (58.6%), visits to the physician (15.3%) and utilization of antibiotics (14.9%). Compliance was significantly better (P < 0.01) in patients prescribed azithromycin for 3 and 5 days (58.0% and 42.9% respectively) than in those who received roxithromycin (20.3%) and a significantly longer symptom-free period (P < 0.01) was reported in azithromycin- compared with roxithromycin-treated patients. These findings support the hypothesis that a 3- or 5-day course of azithromycin is as effective as a 10 day course of roxithromycin in the treatment of patients with pharyngitis and is associated with lower costs. Furthermore, azithromycin is associated with faster resolution of symptoms and improved patient compliance.

Acute Disease↗
PubMed1998

Roxithromycin: review of its antimicrobial activity.

Roxithromycin is a semi-synthetic 14-membered-ring macrolide antibiotic in which the erythronolide A lactone ring has been altered to prevent inactivation in the gastric milieu. The in-vitro activity of roxithromycin is well documented and similar to that of other macrolide antibiotics. Roxithromycin is active against gram-positive and gram-negative cocci, gram-positive bacilli and some gram-negative bacilli, but has no significant effect on the predominant faecal flora. It also displays good activity against atypical pathogens, such as Mycobacterium avium complex, Helicobacter pylori and Borrelia spp. It penetrates and accumulates within cells, such as macrophages and polymorphonuclear neutrophils (PMNs), where it is distributed between the cytosol and cellular granules. Once inside the cells, it is active against intracellular pathogens, such as Legionella, Chlamydia, Mycobacterium, Rickettsia and Borrelia spp. Like other macrolides, roxithromycin displays a significant post-antibiotic effect which is dependent on the pathogens under study, the concentration of roxithromycin and the duration of exposure. In vivo, roxithromycin is as effective or more effective than other macrolides in a wide range of infections.

Anti-Bacterial Agents↗
PubMed1998

The comparative in-vitro activity of roxithromycin and other antibiotics against Bordetella pertussis.

In spite of vaccination programmes, whooping cough epidemics continue to occur. The disease affects all age groups, although its severity is greatest in the young, with infants being particularly vulnerable. Erythromycin is generally accepted as the drug of choice both for treatment and for prophylaxis during epidemics. Roxithromycin is a macrolide with pharmacokinetic advantages over erythromycin; it is well absorbed, produces high serum concentrations, has a long half-life and penetrates respiratory secretions well. There are no accepted standards for testing the sensitivity of Bordetella pertussis to antibiotics, and reports of the activity of roxithromycin and erythromycin are variable. Using Isosensitest agar supplemented with 5% horse blood and an inoculum of 10(4) cfu, 88 strains of B. pertussis were tested for their sensitivity to roxithromycin, erythromycin, rifampicin and trimethoprim/sulphamethoxazole. The range of MICs was 0.12-0.5 mg/L for both roxithromycin and erythromycin. Roxithromycin was bactericidal, with an MBC of 1 mg/L (as compared with 0.5 mg/L for erythromycin). Since roxithromycin is well tolerated by children when used for respiratory tract infections, the good in-vitro activity against B. pertussis, combined with its favourable pharmacokinetics, suggest it may be a good candidate for use in the treatment and prophylaxis of whooping cough.

Anti-Bacterial Agents↗
PubMed1998

Comparison of roxithromycin with cefixime in the treatment of adults with community-acquired pneumonia.

This study compared the efficacy and tolerability of once-daily dosing with either roxithromycin or cefixime in previously healthy adult patients aged between 18 and 60 with markers of uncomplicated community-acquired pneumonia (CAP) in three outpatient clinics in an open, randomized study. Sixty patients were enrolled: 17 males and 13 females received roxithromycin 300 mg once daily for 8-10 days and 22 males and eight females received 400 mg cefixime once daily for the same period. All patients were assessed clinically, radiologically and bacteriologically before inclusion, immediately after the study and approximately 1 month later. The most common pathogen isolated from sputum was Streptococcus pneumoniae (in 26 (43%) of 60 patients), with mixed organisms isolated from the sputum of 18 (30%) of 60 patients. Staphylococcus aureus, Haemophilus influenzae or Moraxella catarrhalis occurred in 11/60 patients, and atypical pathogens were detected by serology in 7/26 cases in the roxithromycin group and 3/23 in the cefixime group. The severity of infection was rated as mild to moderate at the beginning of the trial. At the end of the study treatment period, clinical cure rates were 30/30 (100%) for roxithromycin and 28/30 (94%) for cefixime, with one patient on cefixime being classed as a partial responder and one patient being classed as a failure and withdrawn. However, radiological abnormalities persisted in three patients on roxithromycin and one on cefixime. Of the 59 patients who completed the study, none required further antibiotic therapy. No abnormal laboratory parameters or adverse events were reported in either group. Roxithromycin at a daily dose of 300 mg was an effective and well-tolerated treatment for the empirical treatment of mild to moderate CAP in this group of patients.

Adolescent↗
PubMed2002

Comparative pharmacodynamics of azithromycin and roxithromycin with S. pyogenes and S. pneumoniae in a model that simulates in vitro pharmacokinetics in human tonsils.

Most macrolides penetrate and persist in peripheral tissues, irrespective of plasma concentrations. For this reason, comparative pharmacodynamics of macrolides might be better based on tissue rather than plasma pharmacokinetics. The present study compares the antimicrobial effects of azithromycin and roxithromycin on Streptococcus pyogenes and Streptococcus pneumoniae using in vitro simulations of steady-state pharmacokinetics in human tonsils expected after a third 500 mg dose of azithromycin administered once a day and after a sixth 150 mg dose of roxithromycin administered twice a day. Clinical isolates of S. pyogenes and S. pneumoniae (MICs 0.12 and 0.47 mg/L of azithromycin, and 0.15 and 0.60 mg/L of roxithromycin, respectively) were used. More pronounced antistreptococcal effects were observed with azithromycin than with roxithromycin. Despite similar rates of initial killing of S. pyogenes and S. pneumoniae, the respective 12 h areas between the control growth curve and the time-kill curve of antibiotic-exposed bacteria (ABBCs) were 22% and 36% greater with azithromycin than roxithromycin. Moreover, with azithromycin, viable bacterial counts reached the theoretically achievable limit of detection (10 cfu/mL) 8-10 h after drug administration, with no regrowth within 48 h. In contrast to azithromycin, S. pyogenes and S. pneumoniae exposed to roxithromycin regrew 26 and 6 h, respectively, after initial reduction of the starting inoculum. Further in vitro simulations of tissue pharmacokinetics might be useful for pharmacodynamic comparisons among other macrolides.

Anti-Bacterial Agents↗
PubMed1994

Activities of roxithromycin used alone and in combination with ethambutol, rifampin, amikacin, ofloxacin, and clofazimine against Mycobacterium avium complex.

Preliminary studies showed that roxithromycin possessed significant in vitro activity against a variety of atypical mycobacteria such as the Mycobacterium avium complex, M. scrofulaceum, M. szulgai, M. malmoense, M. xenopi, M. marinum, and M. kansasii and rare pathogens such as M. chelonae and M. fortuitum. In this investigation, radiometric MICs of roxithromycin, ethambutol, rifampin, amikacin, ofloxacin, and clofazimine for 10 clinical isolates of the M. avium complex (5 each from human immunodeficiency virus [HIV]-positive and HIV-negative patients) were determined. Roxithromycin MICs against all the isolates were below the reported maximum concentration of drug in serum at the routine pH of 6.8, and the MICs were further lowered by 1 to 2 dilutions at a pH of 7.4. In vitro enhancement of roxithromycin activity against all strains was further investigated by the previously established Bactec 460-TB method by combining the drugs at sub-MIC levels. Antibacterial activity of roxithromycin was enhanced in all 10 strains by ethambutol, in 3 strains each by rifampin and clofazimine, in 2 strains by amikacin, and in 1 strain by ofloxacin. In vitro screening of three-drug combinations showed that combinations of roxithromycin, ethambutol, and a third potential anti-M. avium drug (rifampin, amikacin, ofloxacin, or clofazimine) resulted in further enhancement of activity in 13 out of 20 drug combinations screened.

Amikacin↗
PubMed1995

Activities of roxithromycin against Mycobacterium avium infections in human macrophages and C57BL/6 mice.

The activity of roxithromycin against three clinical isolates of Mycobacterium avium was compared with that of clarithromycin both in a model of infection of human monocyte-derived macrophages and in a model of established infection of C57BL/6 mice. In the cell culture model, roxithromycin and clarithromycin were bactericidal for strains MO-1 and N-92159 and bacteriostatic for strain N-93043. For the three strains, the differences between the intracellular activities of roxithromycin and clarithromycin were not singificant after 7 days of treatment. Mice were infected with the MO-1 strain. Drugs were given by gavage at a dosage of 200 mg/kg of body weight 6 days per week for 16 weeks starting 5 weeks after infection. At the end of treatment, clarithromycin was more effective than roxithromycin in lungs; roxithromycin was as effective as clarithromycin in spleens. Thus, the activity of roxithromycin was comparable to that of clarithromycin both in vitro and in vivo.

Animals↗
PubMed1995

Intracellular activities of roxithromycin used alone and in association with other drugs against Mycobacterium avium complex in human macrophages.

Recent reports have shown that roxithromycin possesses significant activity against atypical mycobacteria, including the Mycobacterium avium complex (MAC), and that its extracellular anti-MAC activity is further enhanced in two- or three-drug combinations with ethambutol, rifampin, amikacin, ofloxacin, and clofazimine. In accordance with the above data, the anti-MAC potential of roxithromycin used alone and in combination with the above-mentioned antituberculous drugs was screened intracellularly against five clinical MAC isolates (from both human immunodeficiency virus-positive and human immunodeficiency virus-negative patients), phagocytized by human monocyte-derived macrophages. The results showed that roxithromycin used alone and within clinically achievable levels was active against all of the MAC isolates tested. Screening of two-drug combinations showed that both rifampin and clofazimine further increased the intracellular activity of roxithromycin against all five isolates by 35 to 80% (ethambutol, ofloxacin, and amikacin resulted in increased intracellular activity against one, two, and four isolates, respectively). For the three-drug combinations, the combination of roxithromycin plus ethambutol used with rifampin or clofazimine was the most uniformly active against all five MAC isolates, with activity increases of 42 to 90%, followed by roxithromycin plus ethambutol used with amikacin, which resulted in activity increases of 15 to 90%. The overall level of intracellular killing after 5 days of drug addition, in comparison with growth in untreated controls, varied from 1 to 3 log units depending on the individual MAC isolate and/or drug combination used.

Cells, Cultured↗
PubMed1996

Roxithromycin alone and in combination with either ethambutol or levofloxacin for disseminated Mycobacterium avium infections in beige mice.

Roxithromycin alone reduced the level of bacteremia caused by Mycobacterium avium complex liver and splenic infection (in CFU per gram) of beige mice and mortality compared with untreated controls (P < 0.05). Roxithromycin plus ethambutol resulted in a significant reduction in the number of bacteria in splenic tissue compared with those in control splenic tissues of mice and mice treated with roxithromycin alone and ethambutol alone. Roxithromycin plus levofloxacin was not better than roxithromycin alone. Roxithromycin has in vivo activity against M. avium complex strains, and pilot studies with humans may be considered.

Animals↗
PubMed1990

Interaction between roxithromycin and cyclosporin in heart transplant patients.

Cyclosporin is an immunosuppressive agent commonly used in transplant patients. It is actively metabolised by the cytochrome P450 system and interactions with drugs metabolised by the same system are predictable. This is particularly relevant since cyclosporin has a low therapeutic index and its renal toxicity is concentration-related. Roxithromycin, a new, well-tolerated macrolide with a weak interactive profile, uses the same isoenzyme of the P450 system as cyclosporin. To evaluate its interaction potential in clinical practice, 8 heart transplant recipients treated with cyclosporin for at least 1 month received roxithromycin for 11 days (150 mg twice daily). Bi-weekly controls of plasma cyclosporin concentrations and creatinine levels were carried out before, during and after roxithromycin treatment. A slight nonsignificant rise in cyclosporin concentrations was observed, but creatinine levels remained stable during roxithromycin treatment. Values of cyclosporin concentrations diminished after withdrawal of roxithromycin. Cyclosporin dosage adjustment was not necessary. There was a minor pharmacokinetic interaction, which can be considered safe for the usual therapeutic dosage of roxithromycin used.

Adult↗
PubMed1994

Roxithromycin. An update of its antimicrobial activity, pharmacokinetic properties and therapeutic use.

Roxithromycin is a derivative of the macrolide antibacterial erythromycin with in vitro antibacterial activity resembling that of the parent compound. The drug has activity against some Staphylococcus spp., many Streptococcus spp., Moraxella (Branhamella) catarrhalis, Mycoplasma pneumoniae, Legionella pneumophila and Chlamydia trachomatis as well as many less common organisms. Measured using recently proposed guidelines, roxithromycin has in vitro activity against Haemophilus influenzae. In comparison with that of its parent compound, the pharmacokinetic profile of roxithromycin is characterised by high plasma, tissue and body fluid concentrations and a long half-life permitting an extended dosage interval. Roxithromycin has proven clinical efficacy in upper and lower respiratory infections, skin and soft tissue infections, urogenital infections and orodental infections, and appears to be as effective as more established treatments including erythromycin, amoxicillin/clavulanic acid and cefaclor. The drug has also shown promise in a variety of more specialised indications including opportunistic infections in human immunodeficiency virus (HIV)-positive patients and as part of a Helicobacter pylori eradication regimen. Roxithromycin is very well tolerated with an overall incidence of adverse events of approximately 4%. Thus, roxithromycin is an attractive therapeutic alternative in its established indications, especially when the option of once-daily administration is considered.

Absorption↗
PubMed1993

Roxithromycin versus cefaclor in lower respiratory tract infection: a general practice pharmacoeconomic study.

An economic evaluation comparing roxithromycin 150mg twice daily and cefaclor 250mg thrice daily in the treatment of lower respiratory tract infections (LRTI) was undertaken as part of a randomised clinical trial in New Zealand general practice. The observed statistically significant difference in adverse events, withdrawal rates and extra treatment courses in favour of roxithromycin in the clinical study was translated into medical cost savings. Treatment failures, withdrawals or adverse events resulted in additional costs for 11 of 120 (9%) patients receiving roxithromycin and 19 of 118 (16%) patients receiving cefaclor. In these cases (treatment failures, withdrawals, adverse effects) additional antibiotics and general practitioner visits were required 3 times more often and the cost of additional medication for treating failure or adverse effects was 3 times higher for patients treated with cefaclor than for patients receiving roxithromycin. The total direct medical cost per patient treated with roxithromycin was $NZ9.37 lower (on an incremental basis) than for patients treated with cefaclor, despite a higher drug acquisition cost. An estimate of $NZ656 000 per year in total savings in direct medical costs could be made in New Zealand if roxithromycin were to replace all cefaclor prescriptions in the treatment of LRTI.

Cefaclor↗
PubMed2001

Roxithromycin in prevention of acute coronary syndrome associated with Chlamydia pneumoniae infection: a randomized placebo controlled trial.

The role of Chlamydia pneumoniae infection in precipitating acute coronary syndrome (ACS) is unclear. Some studies have indicated that intervention with macrolide antibiotics might reduce coronary events in patients with ACS. A double blind, randomized, placebo-control trial was conducted on 84 ACS patients. Patients were randomized to 30 days of treatment with roxithromycin (150 mg, twice daily) or matching placebo. The follow-up period was 90 days, and the primary clinical end point included cardiovascular death, unplanned revascularization and recurrent angina/MI. Anti-C. pneumoniae IgG positive in 24 of 43 (55.8%) patients in the roxithromycin group and 23 of 41 (56.1%) patients in the placebo group. Anti-C. pneumoniae IgA positive in 20 of 43 (46.5%) patients in the roxithromycin group and 13 of 41 (31.7%) patients in the placebo group. Thirty-three cardiac events occurred (2 cardiovascular deaths, 9 CABG, 12 PTCA and 10 recurrent angina/MI) with 17 events in the roxithromycin group and 16 events in the placebo group. There was no significant difference of cardiac events between the roxithromycin and placebo groups. The present study suggests that antibiotic therapy with roxithromycin is not associated with reduction of cardiac events as reported by other investigators. However, therapeutic interventions may need to be specifically targeted to a group of patients who are confirmed with chronic C. pneumoniae infection.

Aged↗
PubMed2003

Determination of roxithromycin by liquid chromatography/mass spectrometry after multiple-dose oral administration in broilers.

A highly sensitive and specific method for the determination of roxithromycin in broiler tissues 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 1 ng/g and 5 ng/g. The method has been successfully applied to determine for roxithromycin in various tissues of broilers. Residue concentrations were associated with administered dose. At the termination of treatment, roxithromycin was found in all collected samples for both dose groups. Liver was detected to have the highest residual concentration of roxithromycin. Residue concentrations of roxithromycin were lower than its LOQ in all tissues from both dose groups 10 days after the treatment of roxithromycin mixed with drinking water at a dose rate of 15 mg/L or 60 mg/L to each broiler for 7 days.

Adipose Tissue↗