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PubMed1995

The macrolide antibacterial roxithromycin reduces bronchial hyperresponsiveness and superoxide anion production by polymorphonuclear leukocytes in patients with asthma.

We investigated the effects of a macrolide antibacterial, roxithromycin, on the generation of free radicals by peripheral polymorphonuclear leukocytes (PMNs) and on the severity of bronchial hyperresponsiveness. Ten asthmatic patients were treated for 3 months with roxithromycin, 150 mg orally once daily; such treatment significantly reduced the production of superoxide anion by PMNs (p = 0.0029) and reduced the bronchial hyperreactivity (p = 0.0016), as compared with results in healthy controls. Most of the patients required at least 2 months of treatment with roxithromycin for clinical improvement. We conclude that long-term, low-dose administration of roxithromycin may be useful in treatment of patients with bronchial asthma.

Adult↗
PubMed1999

Bioequivalence evaluation of two roxithromycin formulations in healthy human volunteers by high performance liquid cromatography coupled to tandem mass spectrometry.

The bioequivalence of two different formulations containing roxithromycin (SPE-712-1). Oral suspension 300 mg/15 mL as test formulation and Rotram, tablets 300 mg as reference formulation, both by Schering Plough S.A., Brazil) was evaluated in 24 healthy volunteers of both sexes (12 male and 12 female). The study was conducted open with randomized two-period crossover design and a 14-day washout period. Each subject received 300 mg of each roxithromycin formulation. Plasma samples were obtained over a 72-hour interval and roxithromycin concentrations were analyzed by combined LC-MS/MS with positive ion electrospray ionization using selected ion monitoring method. From the plasma roxithromycin concentration vs time curves the following pharmacokinetic parameters were obtained: AUC(0-72 h), AUC(0-infinity), Cmax, t1/2 ratios and tmax individual differences. The 90% for confidence interval (CI) of geometric mean SPE-712-L/Rotram individual percent ratio were 105.0-128.3% for AUC(0-72 h), and 78.4-96.9 for Cmax. Although this 90% CI were marginally outside the interval proposed by the Food and Drug Administration, the probability assessed by the two-one sided West for ratios was included in the 0.8-1.25 interval, as we concluded that SPE-712-L oral suspension formulation was bioequivalent to Rotram tablet formulation for the extent and rate of absorption.

Adolescent↗
PubMed2002

[Experience with rovamycin and roxithromycin in patients with chronic bronchitis in the presence of posttuberculous changes].

Rovamycin and roxithromycin were comparatively studied for their effects in 25 patients with chronic bronchitis and posttuberculous changes in the lung. Ten patients received oral rovamycin, 3,000,000 IU, twice daily and 15 had oral roxithromycin, 150 mg, twice daily. The therapy averaged 9 days. Clinical cure was observed in 90% of cases on rovamycin and in 86.7% on roxithromycin. There were no adverse effects of these drugs. The findings suggest that due to their high therapeutical and bacteriological activities, both rovamycin and roxithromycin show their good clinical efficacy in the treatment of exacerbations of chronic bronchitis in patients with residual posttuberculous changes.

Adult↗
PubMed1991

Female genital tissue concentrations of roxithromycin.

A new macrolide, roxithromycin, appears to have some interesting pharmacokinetic characteristics dissimilar to those of erythromycin, e.g. it has the unusual property of a long serum half-life and the possibility of once daily dosing. Moreover tissue levels are higher than those obtained with other macrolides, and the drug is still present in the tissues up to 24 h. after dosing. The pharmacokinetics of roxithromycin were studied in 36 women undergoing gynecological surgery, and divided by means of the time of sampling into six different groups. Each group received an initial 300 mg dose followed by 8 successive doses of 150 mg at 12 h intervals. Blood and tissues samples were taken during surgery at 2, 6, 9, 12, 18 and 24 h after the last dose of roxithromycin and the patients were then allocated to one of the six groups by means of the sampling time. Tissue fragments were obtained from ovary, fallopian tubes, endometrium, myometrium, cervix and vagina immediately after the surgical resection of the organs. Tissue and serum concentrations were determined by the microbiological method using Sarcina lutea ATCC 9341; the lowest limit of detection was 0.01 microg/ml or 0.01 microg/g. Roxithromycin reached the highest concentration at the 9th hour after last administration and its tissue levels would encourage a wide use of this drug as a satisfactory alternative to tetracyclines for the therapy of some gynecological infections.

Administration, Oral↗
PubMed1991

Activity of roxithromycin against respiratory pathogens.

The usefulness of macrolides in treating respiratory infections has been established for over thirty years. Currently, a great deal of interest is being focused on roxithromycin, a new semisynthetic derivative of erythromycin which is more stable than erythromycin under acidic conditions and exhibits improved pharmacokinetic properties. In this study, special attention is paid to the results of recent multicenter studies in Italy aimed at evaluating the in vitro activity of roxithromycin versus erythromycin against a wide range of respiratory pathogens. Considering that a high degree of overlap was observed between the roxithromycin-susceptible and the erythromycin-susceptible strains, whereas a significant proportion of erythromycin-resistant strains shifted to the intermediate category with roxithromycin, there appeared to be cross-susceptibility rather than cross-resistance between the two macrolides.

Anti-Bacterial Agents↗
PubMed2002

[Reduction of the expansion rate of small abdominal aortic aneurysms with roxithromycin. Results from a randomized controlled trial].

INTRODUCTION: Macrolide treatment has been reported to reduce the risk of recurrent ischaemic heart disease. The influence of a macrolide on the expansion rate of small abdominal aortic aneurysms (AAA) is unknown at present. The aim of this study was to investigate the effect of roxithromycin on the expansion rate of small AAA. MATERIALS AND METHODS: A total of 92 patients with a small AAA were recruited from two populations. One population consisted of 6.339 men aged 65-73 years who were offered participation in a mass screening programme for AAA at the local hospital. From this population 66 subjects were recruited. The remaining 26 were recruited from among 49 subjects diagnosed at interval screening for an initial aortic diameter between 25 mm and 29 mm. The patients were randomized to receive either oral roxithromycin 300 mg once daily for 28 days or matching placebo, and followed for a mean of 1.5 years. RESULTS: During the first year the mean annual expansion rate of AAA was reduced by 44% in the macrolid group (1.56 mm/year) compared to 2.80 mm/year after placebo (p = 0.02). During the second year the difference was only 5%. Multiple linear regression analysis showed that roxithromycin treatment and initial AAA size were significantly related to AAA expansion when adjusted for smoking, diastolic blood pressure, and IgA level > or = 20. The logistic regression analysis confirmed a significant difference in expansion rates above 2 mm annually between the intervention and placebo groups, OR = 0.09 (95% CI: 0.01-0.83). DISCUSSION: In comparison to placebo, roxithromycin 300 mg daily for four weeks reduced the expansion rate of AAA.

Aged↗
PubMed1990

Pharmacokinetics of roxithromycin in kidney grafted patients under cyclosporin A or azathioprine immunosuppression and in healthy volunteers.

The pharmacokinetics of roxithromycin was studied in 9 kidney grafted patients under cyclosporin A immunosuppression, in 10 transplanted patients with azathioprine, and in 6 healthy volunteers. The biological half-life (beta-phase) of roxithromycin in cyclosporin patients was 34.4 (+/- 12.25) h (mean +/- SD), in azathioprine patients 23.4 (+/- 8.18) h and in healthy volunteers 17.0 (+/- 3.8) h. The total elimination constant (k10) was 0.046 (+/- 0.014), 0.068 (+/- 0.019) and 0.084 (+/- 0.036) h, respectively. The total clearance was 0.79 (+/- 0.21), 1.45 (+/- 0.66) and 1.84 (+/- 0.56) l/h, respectively. The areas under the serum level curves were 407.6 (+/- 118.3), 251.0 (+/- 106.6) and 180.7 (+/- 73.2) mg.h/l, respectively. The differences in these parameters between healthy volunteers and cyclosporin patients were statistically significant, as well as those between cyclosporin and azathioprine patients. The differences between healthy volunteers and azathioprine patients were not statistically significant. The results cannot be interpreted unambiguously as an interaction between roxithromycin and cyclosporin; the effect of cyclosporin on the function of eliminating organs which causes the slowed-down elimination of roxithromycin could be taken into account.

Adult↗
PubMed1993

[Roxithromycin in the treatment of community-acquired pneumonia].

BACKGROUND: The aim of the present study was to prospectively evaluate the efficacy and tolerance of roxithromycin in the empiric treatment of extra-hospitalary pneumonias in immunocompetent adult patients. METHODS: Over a 12 month period 101 patients with extra-hospitalary pneumonia who attended the Emergency Department were studied. Of these, 53 were treated as out patients (5 with amoxicillin-clavulanic, 25 with erythromycin and 23 with roxithromycin at daily doses of 300 mg for 10 days). The treatment was randomly chosen, with no patient selection, thus making heterogeneous groups and, therefore, the study could not be comparative. RESULTS: In patients receiving roxithromycin, an etiologic diagnosis was achieved in 15 cases (65.3%), with Mycoplasma pneumoniae, being the most frequent pathogen (10 cases), followed by Streptococcus pneumoniae (3), Chlamydia pneumoniae (1) and Haemophilus influenzae (1). The mean duration of fever was 1.9 days, 6.7 days for respiratory manifestations and resolution of the radiographic infiltrate 11.6 days. The evolution was good in all the patients with no secondary effects or relapse occurring in any patient. CONCLUSION: Roxithromycin is an effective, safe and comfortable antibiotic in the treatment of infections of the lower respiratory tract acquired in the community.

Adolescent↗
PubMed1993

[Personal experience with the use of Rulid (roxithromycin) in children less than 1 year of age].

The authors give an account of the use of Roxithromycin (preparation Rulide) in children of the youngest age group, i.e. in infants. From January 1989 to April 1992 they treated 24 children under 5 weeks to 12 months of age with Roxithromycin. Roxithromycin was administered in amounts from 5 to 10 mg/kg after 12-hour intervals in the course of 4 to 12 days. In 22 children a favourable clinical effect was observed, in two children antibiotic treatment had to be changes because there was no clinical response. Undesirable effects, i.e. vomiting, during Roxithromycin were observed only in two children. In no instance was it necessary to discontinue treatment.

Bacterial Infections↗
PubMed1989

Pharmacokinetics of a new macrolide, roxithromycin, in infants and children.

The pharmacokinetics of roxithromycin was investigated after oral administration of 2.5 mg/kg doses given 12 hours apart during 6 days in infants and children. These 18 subjects suffering from a respiratory tract infection were divided into three age groups: group I less than 18 months, group II less than 5 years, group III less than 13 years. At day 6, the elimination plasma half-life had an average value (mean +/- SD) of 19.8 +/- 9.7 h (group I), 21.0 +/- 9.4 h (group II) and 20.8 +/- 6.9 h (group III), respectively. The maximum concentration of roxithromycin (Cmax) was attained between 1 and 2 hours after dosing with mean values of 10.1 +/- 3.0 mg/l (group I), 8.7 +/- 4.9 mg/l (group II), 8.8 +/- 7.0 mg/l (group III). All the calculated pharmacokinetic parameters did not significantly differ from one group to another. The kinetics of roxithromycin in infants and children seemed to be age independent and showed no accumulation after repeated doses. During 12 hours, the plasma concentrations were above MIC of microorganisms generally present in respiratory tract infections. Two daily doses of 2.5 mg/kg of roxithromycin 12 hours apart may be proposed in infants and children.

Adolescent↗
PubMed1987

In-vitro activity of roxithromycin against respiratory and skin pathogens.

The activity of roxithromycin was determined by a microdilution method, in comparison with erythromycin, spiramycin and josamycin. Roxithromycin and erythromycin showed very similar MICs against staphylococci, Streptococcus pneumoniae, Str. pyogenes and Haemophilus influenzae. In most cases, spiramycin and josamycin appeared similarly or more active. The activity of roxithromycin against Mycoplasma pneumoniae, Legionella spp., Chlamydia psittaci and, to some extent, against Pasteurella spp. was also assessed, by suitable in-vitro methods. Roxithromycin has a promising potential for treating selected skin and respiratory infections.

Bacteria↗
PubMed1987

Influence of amoxycillin, erythromycin and roxithromycin on colonization resistance and on appearance of secondary colonization in healthy volunteers.

We investigated the influence of oral administration of amoxycillin, erythromycin and roxithromycin on colonization resistance in healthy volunteers. Antibiotics were administered in a randomized cross-over design. No effect on the colonization resistance of the oropharynx could be demonstrated. Amoxycillin decreased the colonization resistance of the bowel against Enterobacteriaceae and yeasts, whose median concentration in faeces increased 100-fold and 30-fold respectively. Roxithromycin and erythromycin decreased the concentration of Enterobacteriaceae in faeces. Secondary colonization with Enterobacteriaceae was detected as often following roxithromycin as following amoxycillin, but the level of colonization with these bacteria was much higher following amoxycillin. Following roxithromycin and erythromycin the level of secondary colonization did not exceed the original concentration of Enterobacteriaceae, showing that these antibiotics did not decrease the colonization resistance against Enterobacteriaceae. The appearance of secondary colonization in faeces at levels equal to or lower than the concentration of Enterobacteriaceae before administration of antibiotics, should not be regarded as proof of disturbance of colonization resistance.

Adult↗
PubMed1987

Cellular uptake and subcellular distribution of roxithromycin and erythromycin in phagocytic cells.

The intracellular accumulation and subcellular distribution of 14C-labelled roxithromycin and erythromycin has been studied in macrophages and polymorphonuclear neutrophils of both human and animal origin. Roxithromycin was consistently and significantly more accumulated than erythromycin, reaching intracellular/extracellular concentration ratios between 14 (in polymorphonuclear neutrophils) and 190 (in alveolar macrophages from smokers). Uptake was reversible, insensitive to anaerobiosis and to the presence of an aminoglycoside, but inhibited by acid pH. Upon subcellular fractionation by isopycnic centrifugation in sucrose gradients., half the roxithromycin or erythromycin recovered in cell homogenates was found associated with the lysosomes in macrophages, and about one third with azurophil granules in polymorphonuclear leucocytes. Inasmuch as cellular uptake is a necessary, albeit not sufficient, condition for antimicrobials to kill or inhibit the growth of intracellular bacteria the properties of roxithromycin may give it a distinct advantage over other antimicrobial agents.

Animals↗
PubMed1999

The effect of carbon dioxide on susceptibility testing of azithromycin, clarithromycin and roxithromycin against clinical isolates of Streptococcus pneumoniae and Streptococcus pyogenes by broth microdilution and the Etest: Artemis Project-first-phase study.

OBJECTIVE: To evaluate the effect of carbon dioxide on the susceptibility testing, using broth microdilution and the Etest (AB Biodisk, Solna, Sweden), of azithromycin, clarithromycin and roxithromycin against Streptococcus pneumoniae and Streptococcus pyogenes. METHODS: Fresh clinical isolates collected from 36 hospital laboratories in 12 countries were evaluated using the Etest in the presence of carbon dioxide. The isolates were retested under ambient conditions (absence of carbon dioxide) using broth microdilution and/or the Etest. RESULTS: Carbon dioxide falsely elevated azithromycin, clarithromycin and roxithromycin MIC90S for S. pneumoniae, determined by the Etest, approximately 12-fold. Also, the azithromycin MIC90 for S. pyogenes was increased fourfold; the effect was less marked for clarithromycin and roxithromycin. When isolates were retested in the absence of carbon dioxide, using the Etest or microdilution, susceptibilities to azithromycin were comparable to those to clarithromycin (S. pneumoniae, 93.4% versus 91.3%; S. pyogenes, 96.4% versus 95.8%). Both organisms were less susceptible to roxithromycin (S. pneumoniae, 71.3%; S. pyogenes, 85.7%). An internal standard control, consisting of 50 isolates each of S. pneumoniae, S. pyogenes and Haemophilus influenzae, confirmed that azithromycin susceptibility testing resulted in falsely elevated MICs. CONCLUSIONS: Carbon dioxide falsely elevated azithromycin MICs for S. pneumoniae and S. pyogenes, with an apparent reduction in susceptibility. When the in vitro activity of azithromycin and other macrolides against S. pneumoniae and S. pyogenes is being evaluated, awareness of the pH effect is essential.

Journal Article↗
PubMed1987

Pulmonary disposition of roxithromycin (RU 28965), a new macrolide antibiotic.

The penetration of roxithromycin (RU 28965), an ether oxime derivative of erythromycin, into the cells and fluid lining the epithelial surface of the lower respiratory tract was studied by performing fiber-optic bronchoscopy with bronchoalveolar lavage on eight patients who had received roxithromycin at 300 mg perorally every 12 h for 5 days. The apparent volume of epithelial lining fluid recovered by bronchoalveolar lavage was determined by using urea as an endogenous marker. There was a significant relationship (r = 0.75; P less than 0.02) between roxithromycin levels in plasma and epithelial lining fluid, with a correlation whose slope suggested that the level of drug penetration into the lining fluid was 0.2. Concentrations of the antibiotic in cells recovered by bronchoalveolar lavage (21 +/- 10 micrograms/ml) were 2 and 10 times higher than in plasma (11.4 +/- 5.7 micrograms/ml) and epithelial lining fluid (2.0 +/- 1.7 micrograms/ml), respectively. Thus, when administered perorally in humans, roxithromycin is markedly accumulated by resident alveolar macrophages in concentrations largely exceeding the MBCs of the drug for most facultative intracellular pathogens including Legionella pneumophila, despite low concentrations in the epithelial lining fluid.

Bronchitis↗
PubMed1988

In vitro effects of four macrolides (roxithromycin, spiramycin, azithromycin [CP-62,993], and A-56268) on Toxoplasma gondii.

The effect of four macrolides against intracellular Toxoplasma gondii was determined in three different in vitro systems. Unactivated murine peritoneal macrophages were infected with the virulent RH strain of T. gondii. The activity of the macrolides was first measured with [3H]uracil, which is incorporated by the parasite but not the host cell. The 50% inhibitory concentrations (IC50s) and 95% confidence limits were calculated at 54 (38 to 73), 140 (98 to 201), 147 (101 to 214), and 246 (187 to 325) micron for roxithromycin, azithromycin (CP-62,993), A-56268, and spiramycin, respectively. Inhibition of Toxoplasma growth was confirmed by microscopic examination of the infected macrophages after treatment with roxithromycin. Compared with untreated controls, roxithromycin concentrations near the IC50s decreased the number of infected cells, the number of tachyzoites per vacuole, and the number of cells containing rosettes (i.e., clusters of more than eight tachyzoites). After treatment with the four macrolides, tachyzoites were released from the macrophages and subcultured in HeLa cells, which are nonprofessional phagocytes, to assess the viability of the remaining parasites. This showed that the macrolides at concentrations corresponding to four times their 90% inhibitory concentrations (IC90s) had no significant killing effect. At 8 times the IC90, roxithromycin showed an incomplete killing effect, similar to that of the combination of pyrimethamine (0.41 microM)-sulfadiazine (99.42 microM). All macrolides tested showed inhibitory effects against intracellular T. gondii, but amounts of azithromycin and A-56268 corresponding to the IC90 appeared to be toxic against the host macrophages, which might have had nonspecific activity against Toxoplasma metabolism.

Animals↗
PubMed1988

Effects of roxithromycin, a new semisynthetic macrolide, and two erythromycins on drug metabolizing enzymes in rat liver.

The effects of a new semisynthetic macrolide, roxithromycin, on drug metabolizing enzymes of rat liver were compared with two erythromycins, the base (EB) and the estolate (EE), after 7 days' treatment with high oral doses (400 and 800 mg/kg daily). Dose-related higher concentrations of roxithromycin were reached in serum and liver than after EB or EE. The two reference erythromycins induced the synthesis of microsomal enzymes and formed inactive cytochrome P-450-metabolite complexes. N-Demethylation of erythromycin itself and aminopyrine was increased by the treatment. Liver microsomal enzyme activities were not induced and the inactive cytochrome P-450-metabolite complex was not formed after 400 mg/kg of roxithromycin and only to a very limited extent after 800 mg/kg (10% vs. 50% after EE). At the higher dose microsomal activities were not changed by roxithromycin and only aminopyrine N-demethylation was reduced.

Animals↗
PubMed1989

[In vitro sensitivity of Mycobacterium avium and Mycobacterium xenopi to erythromycin, roxithromycin and doxycycline].

The comparative in vitro activity of erythromycin, roxithromycin and doxycycline against 20 isolates of M. avium and 20 M. xenopi was evaluated by two technics: a standard macrobroth dilution (7H9) and the 1% standard proportion method on lowenstein medium. M. avium was highly and uniformly resistant to doxycycline (MIC 50: 64 mg/l). For macrolides some strains were moderately susceptible to roxithromycin and at a lower level to erythromycin the MIC 50 and MIC 90 were respectively 8 and 16 mg/l for roxithromycin, 16 and 64 mg/l for erythromycin. Both macrolides were active against most of the strains of M. xenopi MIC 90 and MBC 90 were respectively 0.25 and 1 mg/l for roxithromycin, 0.5 and 2 mg/l for erythromycin. Doxycycline was less active inhibiting 90% of strains only at 16 mg/l.

Doxycycline↗