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PubMed1987

Roxithromycin in nongonococcal urethritis.

This presentation is a summary of five different studies on the efficacy and tolerance of roxithromycin in the treatment of non-gonococcal genital infections. Three of the studies were double-blind comparative and two were open studies. Of the 924 out-patients whose data were analysed for clinical efficacy, 637 received treatment with roxithromycin 150 mg bd. The standard dose of roxithromycin, 150 mg bd for ten days, was compared with doxycycline 200 mg daily, lymecycline 300 mg bd and roxithromycin 450 mg once daily. The overall clinical success rate was 90% (576 of 637 patients) for roxithromycin 150 mg bd. In the three comparative trials, no significant difference was found between the clinical success rates of roxithromycin 150 mg bd and the other drugs. The overall clinical success rate with roxithromycin 150 mg bd was 92% (512/558) in nongonococcal urethritis and 81% (64/79) in cervicovaginitis. Taking into account all patients treated with roxithromycin 150 mg bd, the bacteriological success rate was 90% (444/492). In the comparative trials, no significant difference could be found between the treatment groups. Roxithromycin 150 mg bd was effective in eradicating 97% (308/316) of the isolates of Chlamydia trachomatis, 88% (149/170) of Ureaplasma urealyticum, 73% (40/55) of Mycoplasma hominis and 57% (13/23) of Gardnerella vaginalis. The present findings show that a high cure rate can be achieved with a ten-day course of treatment with roxithromycin and that it is at least as effective as the tetracyclines commonly used in the treatment of nongonococcal urethritis. A higher dosage than 300 mg/day of roxithromycin did not offer any clear advantage in terms of efficacy.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1987

In-vitro comparison of roxithromycin and erythromycin against 900 anaerobic bacterial strains.

The in-vitro antibacterial activity of roxithromycin was assessed by an agar dilution method against 900 recent clinical anaerobic isolates by five laboratories in England, France, Germany and Japan. Roxithromycin had similar activity to erythromycin against most anaerobic bacteria, the latter being slightly more active against Gram-negative bacilli. Roxithromycin inhibited 53% of the Bacteroides fragilis group strains; the noticeable exception was Bact. thetaiotaomicron, only 17% of strains of which were inhibited by 4 mg/l roxithromycin. In contrast, all isolates of Bacteroides, other than the Bact. fragilis group, and all Mobiluncus isolates were inhibited by 2 mg/l of roxithromycin or less. This compound was inactive against half the Fusobacterium strains. Roxithromycin and erythromycin inhibited 65 and 72%, respectively, of 436 strains of Gram-negative anaerobes (MIC less than or equal to 4 mg/l). Roxithromycin suppressed 97% of non-sporulating Gram-positive to bacilli, 86% of Peptococcoaceae and 95% of clostridia. Two-thirds of Clostridium difficile strains were susceptible to roxithromycin (MIC less than or equal to 1 mg/l). The activity of roxithromycin against Gram-positive bacilli was identical to that of erythromycin. Overall a concentration of 4 mg/l roxithromycin and erythromycin inhibited 79 and 83%, respectively, of the strains investigated.

Bacteria, Anaerobic↗
PubMed1990

Single oral dose pharmacokinetics of erythromycin and roxithromycin and the effects of chronic dosing.

Roxithromycin is a semisynthetic macrolide antibiotic having similar in vitro antibacterial profile and potency to erythromycin but possibly greater in vivo potency. The single and multiple oral dose pharmacokinetics of roxithromycin and erythromycin were studied in 12 healthy volunteers. Plasma concentrations of the two compounds were measured by a sensitive and specific high-performance liquid chromatographic method using electrochemical detection. After single doses, roxithromycin 150 mg gave a Cmax 3.3-fold higher and an area under the curve (AUC) 16.2-fold higher than erythromycin 250 mg. The half-life for roxithromycin was 12.42 +/- 3.94 h compared with 1.53 +/- 0.42 h for erythromycin. On multiple dosing, the AUC over a dosing interval for erythromycin (250 mg, six hourly doses) was increased 2.3-fold compared with the single dose, whereas that for roxithromycin (150 mg, 12 hourly) was decreased by 25.4%. Because of these opposing changes during chronic dosing, the average plasma roxithromycin concentration over the dosing interval was 2.6-fold higher than that for erythromycin, which was a smaller excess than would have been predicted from the single dose data. The results suggest that roxithromycin exerts less inducing and inhibiting effects on human cytochrome P450 than erythromycin. Roxithromycin has a favorable pharmacokinetic profile suitable for twice daily dosing and may have a lower potential than erythromycin for cytochrome P450-mediated drug interactions.

Adolescent↗
PubMed1992

Roxithromycin in Lyme borreliosis: discrepant results of an in vitro and in vivo animal susceptibility study and a clinical trial in patients with erythema migrans.

A new semisynthetic macrolide roxithromycin was evaluated for its potential use in the treatment of Lyme borreliosis. Using a macro-dilution broth technique, Borrelia burgdorferi was shown to be susceptible to roxithromycin with a minimal bactericidal concentration (MBC) of 0.06-0.25 microgram/ml. A systemic B. burgdorferi infection was established in gerbils; a dosage of greater than or equal to 25 mg/kg/day roxithromycin for 10 days eliminated the infection. A single blind, randomized multicenter study was performed to evaluate the efficacy of roxithromycin 150 mg b.i.d. versus phenoxymethyl-penicillin 1 g b.i.d. for 10 days in patients with uncomplicated erythema migrans. The study was interrupted when 19 patients had enrolled because of five treatment failures. All 5 patients had received roxithromycin; three patients had persisting or recurrent erythema migrans, one developed a secondary erythema migrans-like lesion and severe arthralgia and one developed neuroborreliosis. B. burgdorferi was isolated from skin biopsies after roxithromycin therapy from two patients with persistent erythema migrans and both isolates were still highly susceptible to roxithromycin (MBC = 0.03 microgram/ml). No treatment failures were seen in 10 patients treated with phenoxymethyl-penicillin. Roxithromycin is thus not recommended for treatment of Lyme borreliosis.

Adult↗
PubMed1991

Comparative study of clarithromycin and roxithromycin in the treatment of community-acquired pneumonia.

The efficacy and tolerance of clarithromycin (250 mg twice daily) were compared with those of roxithromycin (150 mg twice daily) in an open, multicentre trial of 77 inpatients with community-acquired pneumonia. Sixty-five patients were clinically evaluable (34, clarithromycin; 31 roxithromycin). Efficacy was comparable between treatment groups: 26 of 34 patients (76%) treated with clarithromycin were clinically cured, including four with atypical pneumonia. In the roxithromycin group 25 of 31 patients (81%) were clinically cured and one was improved. Cough, appearance of sputum, and fever improved in most patients in both treatment groups. Chest X-rays after treatment showed resolution or improvement in 76% of patients who received clarithromycin and 87% of those who received roxithromycin. The clinical evaluation of the response generally agreed with the bacteriological response. Among patients who were bacteriologically evaluable for four target organisms (Streptococcus pneumoniae, Haemophilus influenzae, H. parainfluenzae, and Branhamella catarrhalis) the pathogen was eradicated in four of seven (57%) in the clarithromycin-treated group and in five of six (83%) in the roxithromycin-treated group. Adverse events were reported in more patients who received roxithromycin (21.6%) than in those who received clarithromycin (12.5%) although the incidences were not statistically significantly different. The majority of adverse events were transient increases in serum alanine aminotransferase, serum aspartate aminotransferase, and alkaline phosphatase. Clarithromycin was shown to be effective and well-tolerated; the clinical efficacy and safety of clarithromycin and roxithromycin were comparable.

Adult↗
PubMed1987

Roxithromycin, a new macrolide antibiotic, in the treatment of infections in the lower respiratory tract: an overview.

Roxithromycin is a new macrolide antibiotic with good absorption and a longer half-life than erythromycin. Worldwide clinical studies to evaluate its efficacy and safety in the treatment of infections of the lower respiratory tract have achieved a clinical success rate of 89% with few and mild side effects. Double-blind studies comparing roxithromycin with cephradine, erythromycin ethylsuccinate and doxycycline in pneumonia, acute exacerbations of bronchitis in patients with chronic obstructive airways disease, and acute bronchitis have been done. The clinical response to comparative regimens has been similar and ranges from 60% response with either regimen in patients with chronic airways disease to 90% response in patients with acute bronchitis or pneumonia. Roxithromycin appears to be as effective as erythromycin or doxycycline for the treatment of either Streptococcus pneumoniae or Haemophilus influenzae infections. A large double-blind trial comparing cephradine and roxithromycin in 90 cases of bacteriologically confirmed pneumococcal pneumonia in South African gold miners resulted in a 93% and 100% respective clinical response rate. The bacteriological results revealed interesting results in this same study, in that cultures from 17% of patients receiving roxithromycin and 23% of those receiving cephradine remained positive for S. pneumoniae after therapy was finished and an excellent clinical response had been obtained. Side effects in all studies have been transient and mild, with an elevated transaminase value being the most common in both roxithromycin and erythromycin or cephradine regimens. Roxithromycin appears to be a safe and effective oral antibiotic for the treatment of pneumococcal pneumonia and other infections of the lower respiratory tract, and is as effective as erythromycin, doxycycline or cephradine.

Humans↗
PubMed1988

Comparative efficacy and toxicity of roxithromycin and erythromycin ethylsuccinate in the treatment of streptococcal pharyngitis in adults.

Roxithromycin is a novel oxime ether derivative of erythromycin. Previous studies have demonstrated similar in-vitro activity for roxithromycin and erythromycin. Roxithromycin has improved pharmacokinetic properties and may be a useful alternative agent for infections where erythromycin is indicated. We compared the efficacy and toxicity of roxithromycin and erythromycin ethylsuccinate in the treatment of streptococcal pharyngitis in adults. We also assessed compliance with treatment between the two agents. Roxithromycin and erythromycin ethylsuccinate were equally effective in resolving the symptoms and signs of pharyngitis. Erythromycin ethylsuccinate was superior to roxithromycin in achieving microbiological cure (90% vs. 33%, respectively). No differences were observed in toxicity or compliance with treatment between the two agents. Based on this prespective clinical trial, roxithromycin is not considered to be an acceptable alternative agent for acute streptococcal pharyngitis in adults.

Adolescent↗
PubMed1988

No effect of roxithromycin on pharmacokinetic or pharmacodynamic properties of warfarin and its enantiomers.

The macrolide antibiotics are metabolized by cytochrome P-450 enzymes in the liver and interactions with similarly metabolized compounds have been described. Simultaneous treatment with erythromycin and warfarin is known to decrease warfarin clearance and prolong prothrombin time. Roxithromycin (RU 28965), a new erythromycin derivative with improved pharmacokinetic properties, might then, because of structure similarity, be expected to interact with warfarin. In 21 healthy volunteers, the effect of orally administered roxithromycin (150 mg b.i.d.) on warfarin steady-state kinetics, and the effects of warfarin on roxithromycin kinetics, were investigated in a double-blind, randomized study versus placebo. Since the warfarin enantiomers, R- and S-warfarin have both different potency and different metabolism, the ratio between the enantiomers with and without roxithromycin, was also determined. In this study, mean AUC for warfarin increased slightly from day 14 of warfarin treatment to day 28, but no difference was found between the roxithromycin group and the placebo group, and no change appeared in the ratio between the warfarin enantiomers. A moderate increase in dosage was needed to maintain hypocoagulability during warfarin medication, but there was no difference between the roxithromycin group and the placebo groups, respectively. In addition, roxithromycin kinetics appeared to be unaffected by warfarin treatment.

Adult↗
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↗
PubMed1987

An evaluation of tolerance of roxithromycin in adults.

This review deals with tolerance of a new macrolide, roxithromycin from data collected from a number of studies in adults. A total of 2917 adults, 2519 given roxithromycin 150 mg bid, were recruited into 17 multicentre comparative or non-comparative studies. Nine studies were double-blind, against doxycycline, erythromycin estolate (EES), lymecycline or cephradine. Overall the drug was well tolerated: side-effects possibly or probably related to roxithromycin were noted in only 4.1% (120/2917) of all patients, and in 3.1% (15/480) of elderly subjects. The gastrointestinal tolerance of roxithromycin was significantly better than that of doxycycline in four trials, and better than that of erythromycin ethylsuccinate in one study. The incidence of drug-related liver function test abnormalities following roxithromycin therapy was low and compared favourably with data published on erythromycin. Roxithromycin shows a satisfactory safety profile at the recommended daily dosage of 150 mg bid in adults.

Adult↗
PubMed1988

Toxicity, uptake, and subcellular distribution in rat hepatocytes of roxithromycin, a new semisynthetic macrolide, and erythromycin base.

Rat hepatocytes were used to study the toxicity of a new semisynthetic macrolide, roxithromycin, in comparison with erythromycin base and erythromycin estolate. Roxithromycin caused lactate dehydrogenase leakage close to that of erythromycin estolate and higher than erythromycin base after 21 h of exposure to the drugs. This effect was, at least in part, explained by the higher uptake: roxithromycin was two to three times more concentrated by liver cells than erythromycin base. For both roxithromycin and erythromycin base, the uptake depended on time, temperature, and extracellular antibiotic concentration. The accumulated macrolides egressed rapidly when cells were incubated in antibiotic-free medium. No uptake and no loss of accumulated drugs were observed at 4 degrees C. After accumulation by hepatocytes, roxithromycin and erythromycin base underwent similar subcellular distribution, mostly concentrating in cytosol and lysosomes. The small amount accumulated in the other particulate fractions followed the order mitochondria much greater than nuclei greater than microsomes. Roxithromycin, however, was less concentrated than erythromycin base in the microsomes.

Animals↗
PubMed1989

Roxithromycin. A review of its antibacterial activity, pharmacokinetic properties and clinical efficacy.

Roxithromycin is an acid-stable orally administered antibacterial macrolide structurally related to erythromycin. It has an in vitro antibacterial profile similar to that of erythromycin, with activity against Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae, S. pyogenes, Branhamella catarrhalis, Mycoplasma pneumoniae, Legionella pneumophila, Chlamydia trachomatis, Gardnerella vaginalis, Haemophilus ducreyi, some anaerobes and other less common pathogens. Roxithromycin has a pharmacokinetic profile that is characterised by excellent enteral absorption achieving high concentrations in most tissues and body fluids. The results of clinical studies with roxithromycin have confirmed the potential for its use in a variety of infections, which was suggested by its antibacterial activity in vitro and pharmacokinetic profile. Clinical efficacy has been confirmed in the treatment of respiratory tract infections, including community-acquired and atypical pneumonias, ear, nose and throat infections, genitourinary tract infections, and skin and soft tissue infections. In a relatively small number of patients roxithromycin has generally been shown to be as effective as erythromycin and other appropriate antibacterial drugs in some of the above indications. Roxithromycin is well tolerated and has less potential than erythromycin to produce clinically significant drug interactions. Thus, roxithromycin is an orally active drug which should prove a useful alternative when selecting antibacterial therapy for indications where macrolides are appropriate.

Female↗
PubMed1988

[Interaction of roxithromycin with human polymorphonuclear neutrophils in vitro and ex vivo].

Roxithromycin (RU 28965) a new semisynthetic macrolide has been reported to display an antibacterial spectrum and activity in vitro similar to those of others macrolides. However, roxithromycin seems more efficient than erythromycin in in vivo experimental infections (mice). We have previously reported that roxithromycin increases the ability of human neutrophils (PMN) for bactericidal activity (S. aureus) or phagocytosis (K. pneumoniae) in vitro without altering other PMN functional parameters. In this study, roxithromycin (single dose-300 mg) was given to 6 human volunteers. The neutrophils collected 90 min after ingestion display a significant increased ability to phagocytose and kill S. aureus and K. pneumoniae. Furthermore chemotaxis, oxidative burst and myeloperoxidase activity of the PMN after roxithromycin ingestion were enhanced compared to those of PMN before ingestion. This discrepancy between immunomodulating effect of roxithromycin in vitro and in vivo outlines the complexity of in vivo experimental models and requires further studies in vivo in particular in patients suffering from sepsis.

Adult↗
PubMedDate not supplied

Penetration of roxithromycin into gingival tissue.

Roxithromycin is a new macrolide with an antibacterial spectrum similar to that of erythromycin. Absorption is rapid and complete, resulting in high serum levels and a long half-life. Tissue distribution is extensive and sustained, as shown by the high concentrations measured in the lung, prostate, ovaries, liver, kidney, and skin. In this study, we measured the penetration of roxithromycin into gingival tissue at steady state in 30 patients treated orally with 150 mg every 12 hr for 5 days. Tissue specimens were sampled at 2, 4, 6, 8, or 12 hr (n = 6 each time) after dose 10, and blood samples were taken simultaneously. Serum and tissue concentrations of roxithromycin were measured by high-performance liquid chromatography. The peak serum level, reached 4 hr after dosing, was 6.60 +/- 1.15 micrograms/ml. The peak tissue level was 4.63 +/- 1.84 micrograms/g and was reached after 8 hr. From 4 to 10 hr after dosing, tissue concentrations were greater than 2 micrograms/g, that is, higher than the MIC90 of roxithromycin against most oral pathogens. These data support the use of roxithromycin in the treatment of oral infections.

Absorption↗
PubMedDate not supplied

A randomized double-blind controlled trial of roxithromycin and cefaclor in the treatment of acute lower respiratory tract infections in general practice.

A multicenter, randomized, double-blind, single-dummy placebo-controlled study is being undertaken by the Research Unit of the Royal New Zealand College of General Practitioners to compare the efficacy and tolerance of 150 mg twice daily roxithromycin with 250 mg three times daily cefaclor in the treatment of 250 general practice patients with acute lower respiratory tract infections (LRTIs). Interim analysis of 200 patients reveals no statistically significant differences in the study parameters. Of the patients on roxithromycin and cefaclor, 83% and 67%, respectively, had a moderate or severe illness. Based on efficacy criteria, 96% of roxithromycin recipients and 99% of cefaclor recipients had a satisfactory or improved response. On an intention-to-treat basis, this was reduced to 95% for both treatment groups. Sputum grading and semiquantitative culturing was performed according to NCCLS standards. The most common isolates in order were Haemophilus influenzae, Moraxella catarrhalis, and Streptococcus pneumoniae. Efficacy for bacteriologically evaluable cases was 87.5% for roxithromycin and 57% for cefaclor. Four patients on roxithromycin (3.9%) and 11 patients on cefaclor (11.3%) withdrew because of side effects probably or possibly related to the study treatment. The study is ongoing.

Acute Disease↗
PubMedDate not supplied

Roxithromycin versus doxycycline in the treatment of acute exacerbations of chronic bronchitis.

The efficacy and safety of roxithromycin (300 mg once daily) and doxycycline (200 mg once daily) in the treatment of acute exacerbations of chronic bronchitis in general practice were compared in a multicenter, double-blind, double-dummy trial. The data presented here are the results of an interim analysis of 76 patients. A satisfactory clinical response was obtained in 81% of patients treated with roxithromycin and 80% of those treated with doxycycline. Among patients receiving roxithromycin, 12.2% volunteered adverse events, compared with 33% of those receiving doxycycline; the test treatments were considered possibly or probably responsible for the adverse events in 9.8% and 21.2% of cases, respectively. Though patient numbers are too small for statistically significant differences to be detected, we conclude that the results to date suggest that roxithromycin and doxycycline are equivalent in terms of efficacy, but that roxithromycin is better tolerated.

Adult↗
PubMed1991

The diffusion of clarithromycin and roxithromycin into nasal mucosa, tonsil and lung in humans.

The diffusion of clarithromycin and roxithromycin into respiratory tract tissues was studied in 174 adult patients undergoing surgery. Patients received clarithromycin 250 mg orally (500 mg in the case of lung tissue), or roxithromycin 150 mg orally, both given every 12 h, for three days with the last dose administered at different times before surgery. Clarithromycin reached peak tissue levels 4 h after administration and achieved mean peak concentrations of 8.32 mg/kg +/- 2.57 in nasal mucosa, 6.47 mg/kg +/- 2.8 in tonsil, and 17.47 mg/kg +/- 3.29 in lung tissue. Roxithromycin reached peak tissue levels between 4 and 6 h after administration, achieving mean peak concentrations of 1.78 mg/kg +/- 0.73 in nasal mucosa, 2.2 mg/kg +/- 1.21 in tonsil, and 2.14 mg/kg +/- 0.87 in lung tissue. Clarithromycin and roxithromycin demonstrated contrasting pharmacokinetic behaviour. Roxithromycin was characterized by high concentrations in serum and low concentrations in tissues. Clarithromycin on the other hand, is characterized by therapeutic serum concentrations and high tissue concentrations.

Administration, Oral↗
PubMed1991

Treatment of chlamydial conjunctivitis in newborns and adults with erythromycin and roxithromycin.

A randomized single-blind study of the effects of erythromycin and roxithromycin on chlamydial conjunctivitis was performed on a group of patients, comprising 28 newborns and 27 adults. Treatment used was either 200 mg of erythromycin ethylsuccinate or 50 mg of roxithromycin daily, divided into two doses for the neonatal group or for the adult group, 1000 mg of erythromycin stearate or 300 mg of roxithromycin daily divided into two doses. All patients were treated for ten days. Clinically nine of the neonates and 13 of the adults had unilateral conjunctivitis, whilst the remaining cases were bilateral. At follow-up one month after commencing therapy, all but one (erythromycin-treated) of the 28 neonates and three (two of whom were erythromycin-treated) of the 27 adults were cured. However, 16 (nine neonates and seven adults) were culture-positive for Chlamydia trachomatis in samples from eye and/or nasopharynx. The culture-positive group comprised ten cases (four neonates and six adults) who had been treated with erythromycin and six (five neonates and one adult) with roxithromycin. No major side effects of the therapy were seen. The study indicates that there was no difference in the clinical cure rate for the two drugs either in neonates or in adults. However, the isolation rate of chlamydiae in the adult group differed, with 12 (92%) of the 13 roxithromycin-treated cases becoming culture-negative, whilst this was true for only eight (57%) of the 14 erythromycin-treated cases (P less than 0.007).

Adolescent↗