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Roxithromycin (Rulide)
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Roxithromycin

Roxithromycin is part of the family of medications known as macrolide antibiotics and is commonly used in the treatment of bacterial infections. Roxithromycin is generically prescribed as roxithromycin and can cause life threatening heart complications in patients who also take pimozide, astemizole, cisapride, ergot medications, and terfenadine. Roxithromycin is an ineffective treatment option for patients suffering from infections caused by a virus or bacterium.

Other names for this medication:
Biaxsig, Remora, Roxitromicina, Rulid, Rulide

Similar Products:
Dificid, Zmax, Biaxin XL, Zithromax

 

Also known as:  Rulide.

Description

Roxithromycin is a semi-synthetic macrolide antibiotic. It is used to treat respiratory tract, urinary and soft tissue infections. Roxithromycin is derived from erythromycin, containing the same 14-membered lactone ring. However, an N-oxime side chain is attached to the lactone ring. It is also currently undergoing clinical trials for the treatment of male-pattern hair loss.

Roxithromycin is available under several brandnames. Roxithromycin is not available in the United States. Roxithromycin is available in Australia, Israel and New Zealand. Roxithromycin has also been tested to possess antimalarial activity.

Roxithromycin prevents bacteria from growing, by interfering with their protein synthesis. Roxithromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the synthesis of peptides. Roxithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Legionella pneumophila.

Dosage

Roxithromycin is typically prescribed for a period of 7 to 14 days and patients should take the medication for as long as it has been prescribed to prevent the infection from returning even if they become asymptomatic. Patients should not however, take doses larger than has been prescribed as this can result in an overdose. Overdosing requires immediate medical intervention and may present with symptoms which include abdominal pain, nausea, diarrhea, vomiting, and a general and prolonged feeling of illness.

Overdose

Symptomatic treatment should be provided as required. There is no specific antidote.

Storage

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F) away from moisture, light and heat. Do not store in the bathroom. Keep in a tight, light-resistant container. Keep out of the reach of children.

Side effects

The most common side effects associated with Roxithromycin are:

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Side effect occurrence does not only depend on medication you are taking, but also on your overall health and other factors.

Contraindications

The safety of roxithromycin has not been demonstrated in patients with impaired hepatic or renal function. Caution should be exercised if roxithromycin is administered to patients with impaired hepatic or renal function. If administered to patients with severe impaired hepatic function (eg. hepatic cirrhosis with jaundice and/or ascites), consideration should be given to reducing the daily dosage to half the usual dosage.

Prolonged or repeated use of antibiotics including roxithromycin may result in superinfection by resistant organisms. In the event of superinfection, roxithromycin should be discontinued and appropriate therapy instituted.

When indicated, incision, drainage or other appropriate surgical procedures should be performed in conjunction with antibiotic therapy.

Antibiotic associated pseudomembranous colitis has been reported with many antibiotics. A toxin produced by Clostridium difficile appears to be the primary cause. The severity of the colitis may range from mild to life threatening. It is important to consider this diagnosis in patients who develop diarrhoea or colitis in association with antibiotic use (this may occur up to several weeks after cessation of antibiotic therapy). Mild cases usually respond to drug discontinuation alone. However, in moderate to severe cases, appropriate therapy with a suitable oral antibacterial agent effective against Clostridium difficile should be considered. Fluids, electrolytes and protein replacement therapy should be provided when indicated.

Roxithromycin, like erythromycin, has been shown in vitro to elicit a concentration - dependent lengthening in cardiac action potential duration. Such an effect is manifested only at supra – therapeutic concentrations. Accordingly, the recommended doses should not be exceeded. In certain conditions macrolides, including roxithromycin, have the potential to prolong the QT interval. Therefore roxithromycin should be used with caution in patients with congenital prolongation of the QT interval, with ongoing proarrhythmic conditions (ie uncorrected hypokalemia or hypomagnesaemia, clinically significant bradycardia), and in patients receiving Class IA and III antiarrhythmic agents.

biaxsig roxithromycin and alcohol

Noncystic fibrosis bronchiectasis (NCFB) is characterized by airway expansion and recurrent acute exacerbations. Macrolide has been shown to exhibit anti-inflammatory effects in some chronic airway diseases.

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Agar dilution was used to test the activities of HMR 3647, erythromycin A, azithromycin, clarithromycin, roxithromycin, clindamycin, and quinupristin-dalfopristin against 235 strains of Enterococcus faecalis. HMR 3647 was the most active compound (MICs at which 50 and 90% of the isolates are inhibited [MIC50 and MIC90, respectively] of 0.06 and 4.0 microg/ml, respectively). The MIC50 and MIC90 (with the MIC50 given first and the MIC90 given second; both in micrograms per milliliter) for other compounds were as follows: 4.0 and >32.0 for erythromycin A, 16.0 and >32.0 for azithromycin, 2.0 and >32 for clarithromycin, 32.0 and >32.0 for roxithromycin, 32.0 and >32.0 for clindamycin, and 8.0 and 16.0 for quinupristin-dalfopristin. All compounds were only bacteriostatic.

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To test the efficacy of short-term administration of RXM, elder IL-10-deficient mice (16-20 weeks old) with established colitis were orally treated for 10 days with RXM (20 mg/kg per day). To test the long-term preventive effects of RXM, for 20 weeks young adult IL-10-deficient mice (4-5 weeks old) also were administered RXM orally (20 mg/kg per day).

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The infection rates of mycoplasma and chlamydia in children suspected NGU were high. Mycoplasma showed drug resistance to a different degree to 10 common antibiotics. The results of chemosensitivity showed that josamycin had the highest susceptibility rate.

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To study the effect of low-dose erythromycin combined with sinus displacement therapy on treating sinusitis in patients with nasopharyngeal carcinoma after radiotherapy.

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A 48-year-old female was seen at our hospital after having a severe fever of nearly 40 degrees C, for a period of 9 days. She complained of pain in the left side of her chest. An X-ray examination revealed a slight infiltration of the upper and middle lung fields. At this time, it was learned that the women's pet bird had recently died. This case was diagnosed as acute pneumonia due to psittacosis. Therefore the administration of Roxithromycin was started. After a few day her condition improved. During the course of treatment, serum was taken and a throat swab was done. A micro-immunofluorescence (MIF) test was performed to check the serum antibody levels against Chlamydia psittaci. The serum titer rose from 1:8 to 1:256 in 15 days after admission. The final diagnosis was made after positive isolation of C. psittaci by means of the cell culture method.

roxithromycin drug action

Nine structurally similar macrolide antibiotics were tested at a concentration of 0.5 microg/ml for their relative inhibitory effects on ribosome functions in Staphylococcus aureus cells. Eight of the compounds examined inhibited protein synthesis at this concentration. Seven of the nine compounds were also effective in blocking formation of the 50S ribosomal subunit. Roxithromycin and 14-hydroxy clarithromycin inhibited protein synthesis to a greater extent than they affected 50S subunit formation. Conversely, the compound 11, 12-carbonate-3 deoxy-clarithromycin affected 50S assembly more than translation. Only clarithromycin had any effect on 30S ribosomal subunit assembly. The decline in growth rate and cell number was proportional to the effect on ribosome formation or function by each compound. These inhibitory activities can be related to structural differences between these macrolide antibiotics.

roxithromycin antibiotics

Dermatologists must be aware of the adverse effects of antimicrobial agents as well as various drug interactions that may influence the choice of drug as well as specific drug schedules. The development of modern antibacterials has improved the treatment of cutaneous bacterial infections. Macrolide antibacterials continue to be an important therapeutic class of drugs with established efficacy in a variety of skin infections. All macrolides inhibit protein synthesis by reversibly binding to the 23S ribosomal RNA in the 50S-subunit. Erythromycin, the prototype of macrolide antibacterials, was isolated from the metabolic products of a strain of Streptomyces erytherus in 1952. Originally, erythromycin was introduced as an alternative to penicillin because of its activity against the Gram-positive organisms. Numerous studies have demonstrated the efficacy and safety of erythromycin for various infectious diseases. Unfortunately, erythromycin is associated with a number of drawbacks including a narrow spectrum of activity, unfavorable pharmacokinetic properties, poor gastrointestinal tolerability, and a significant number of drug-drug interactions. Newer macrolides have been developed to address these limitations. The pharmacokinetics of azithromycin and clarithromycin allow for shorter dosing schedules because of prolonged tissue levels. The efficacy of azithromycin for the treatment of skin and soft tissue infections in adults and children is well established. The unique pharmakinetics of azithromycin makes it a suitable agent for the treatment of acne. Clarithromycin represents a clear advance in the macrolide management of patients with leprosy and skin infections with atypical mycobacteria. Dirithromycin and roxithromycin display no clinical or bacteriological adcantage over erythromycin despite a superior pharmacokinetic profile. An area of concern is the increasing macrolide resistance that is being reported with some of the common pathogens which may limit the clinical usefulness of this class of antimicrobial agents in future.

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It has been reported that antibodies to oral anaerobic bacteria are elevated in the serum and synovial fluids of patients with rheumatoid arthritis. Macrolide antibiotics are active against oral anaerobic bacteria.

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We conducted a double-blind randomized controlled trial of oral 500 mg amoxicillin 3 times per day vs oral 300 mg roxithromycin once a day for 10 days.

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roxithromycin dose per kg 2016-10-30

Sub-inhibitory Metropast Ovulos 500 Mg concentrations of antibiotics, which are found in environmental water systems and sewage plants due to an increased use in therapeutical and preventive fields, influence bacterial behavior in biofilms. The application of sulfamethoxazole, erythromycin, and roxithromycin induced changes in biofilm dynamics regarding biomass formation, spatial structure and specific gene expression in different Pseudomonas aeruginosa isolates. Exposing multi-resistant environmental isolated strains for 17 h to environmental concentrations of antibiotics or wastewater, directly, an increase in biofilm biomass and thickness could be observed for each strain. Additionally, multi-resistant strains responded to the applied growth conditions with changes in transcriptional activity. Here, sub-inhibitory concentrations of macrolides specifically upregulated expression of quorum sensing genes (rhlR, lasI), whereas sulfonamides and municipal wastewater, instead upregulated expression of specific resistant genes (sul1) and efflux pumps (mexD). Antibiotic sensitive isolates demonstrated an overall higher transcriptionally activity, but did not show a specific gene response to the applied exogenous stimuli. Furthermore, the presence of low concentrated antibiotics induced also phenotypical change in the biofilm architecture observed by 3D-imaging.

roxithromycin with alcohol 2016-02-15

In a double blind randomised investigation in 76 patients, roxithromycin (150 mg bd) and doxycycline (200 mg once daily) were compared in two groups of patients who were well-matched for age, sex, body weight, diagnosis, duration and severity of disease and associated pathological conditions, with infected skin conditions. Clinical effectiveness was 92% for roxithromycin and 82% for doxycycline, and bacteriological effectiveness also 92% and 82% Co Amoxiclav 500mg Dosage respectively, the differences not being statistically significant.

roxithromycin drinking alcohol 2017-03-06

The concentrations of the new macrolide antibiotic roxithromycin in plasma, saliva, gingiva, and alveolar bone were studied in 24 odontoiatric patients treated with a first dose of 300 mg p.o. followed by three maintenance doses of 150 mg p.o., 12-hourly. Samples of blood, saliva, gingiva, and bone were collected at various time points up to 24 h after the last dosing, and the roxithromycin concentration was measured microbiologically, using Bacillus subtilis ATCC 6633 as the reference organism. Pharmacokinetic analysis was performed according to a two-compartment open model with first-order absorption. The plasma, gingiva, and alveolar bone peak concentrations were 6.12 +/- 1.94 mg/l, 6.55 +/- 2.54 mg/kg, and 5.09 +/- 1.60 mg/kg, respectively. Low levels of roxithromycin were detected in saliva (0.67 +/- 0.12 mg/l at the 3rd h). The values of the Sumamed With Alcohol area under the concentration-time curve for plasma, gingiva, and bone were 59.47 mg/l.h, 51.88 mg/kg.h and 46.80 mg/kg.h, respectively; the half-life values were 7.52 h for plasma and 6.36 and 5.20 h for gingiva and bone, respectively. These results indicate that roxithromycin reaches high levels in periodontal tissues.

roxithromycin 300 mg dosage 2015-07-03

This paper illustrates the challenge faced by analytical chemists when trying to measure selected compounds representative of various classes of prescription and hospital drugs. Because hundreds of drugs belonging to a wide variety of chemical groups are allowed for use, an array of analytical methods has to be implemented. As an example, as part of the European Poseidon Project, five different methods were required to measure eight drugs Amoxil Dosing Chart and personal care products. These methods are discussed in detail. Examples of application to surface and ground waters from the Paris area are also reported. The antibiotics roxithromycin and sulfamethoxazole were detected for the first time in the Seine River downstream of Paris. The behaviour of the eight target compounds during aquifer recharge and drinking water treatment is described. An incident involving the detection of micrograms per litre levels of the personal care product Galaxolide in a drinking water distribution system is reported. The value of the pharmaceuticals and personal care products selected as potential indicators is also discussed.

roxithromycin 50mg tablet 2017-03-05

The CC chemokine eotaxin not only attracts eosinophils to inflamed sites but also promotes adhesion, degranulation and reactive oxygen species production of eosinophils. Reactive oxygen species released from Zithromax 250 Z Pak Tab eosinophils are believed to injure epithelial cells at inflamed sites, resulting in airway hyperresponsiveness. Roxithromycin has been reported to have antiasthmatic effects, although its mechanism of action is not thoroughly understood. Therefore, the effect of roxithromycin on eotaxin-primed reactive oxygen species production from eosinophils was studied.

roxithromycin 300 mg bestellen 2016-04-09

Effects of long-term low-dose macrolide administration were studied in patients with chronic sinusitis. Twelve patients with non-allergic chronic sinusitis were orally Julphamox 250 Mg Dosis given 150 mg roxithromycin once a day without other treatments. The patients underwent computed tomography before and after the treatment, and paranasal sinus aeration was analyzed quantitatively. The number of neutrophils in the nasal smear was semiquantitatively assessed on a grading scale, and the IL-8 concentration in the nasal discharge was measured by enzyme immunoassay. The aeration of all four sinuses significantly improved, and recruited neutrophils and the IL-8 level in the nasal discharge were simultaneously reduced after the treatment. These findings suggest that long-term low-dose roxithromycin administration inhibits the positive feedback mechanism of neutrophil recruitment and IL-8 production by the recruited neutrophils, which is considered to be an essential cause of the prolongation of sinusitis.

roxithromycin sandoz 300 mg ja alkoholi 2016-08-28

In a prospective randomized placebo-controlled study 1010 patients with successful coronary stent placement received roxithromycin or placebo for 4 weeks after coronary stent placement, which showed no effect of roxithromycin on early thrombotic events, as expected. Venous blood samples were collected from patients immediately before treatment. Plasma was analyzed for C. pneumoniae-specific IgG antibody levels by microimmuno-fluorescence. Thrombotic events were defined as death, non-fatal myocardial infarction, or urgent target vessel reintervention within 30 days after stent placement. We found no significant difference concerning the frequency of early thrombotic events in patients positive or negative for C. Amoxival De 500 Mg pneumoniae-specific antibodies. If patients were stratified according to their antibody levels, again no significant difference in the frequency of thrombotic events was observed.

roxithromycin 150 mg 2016-04-09

To compare the real-life treatment of acute exacerbations of chronic bronchitis (AECBs) using moxifloxacin tablets or one of the oral macrolides azithromycin, clarithromycin or roxithromycin in terms of symptom relief, time until improvement and cure Is Denvar A Antibiotic , overall efficacy and tolerability.

roxithromycin brand name 2017-05-03

Enucleated human polymorphonuclear leukocytes (PMN cytoplasts), which have no nuclei and only a few granules, retain many of the functions of intact neutrophils. To better define the mechanisms and intracellular sites of antimicrobial agent accumulation in human neutrophils, we studied the antibiotic uptake process in PMN cytoplasts. Entry of eight radiolabeled antibiotics into PMN cytoplasts was determined by means of a velocity gradient centrifugation technique. Uptakes of these antibiotics by cytoplasts were compared with our findings in intact PMN. Penicillin entered both intact PMN and cytoplasts poorly. Metronidazole achieved a concentration in cytoplasts (and PMN) equal to or somewhat less than the extracellular concentration. Chloramphenicol, a lipid-soluble drug, and trimethoprim were concentrated three- to fourfold by cytoplasts. An unusual finding Medazol Gel Rosacea was that trimethroprim, unlike other tested antibiotics, was accumulated by cytoplasts more readily at 25 degrees C than at 37 degrees C. After an initial rapid association with cytoplasts, cell-associated imipenem declined progressively with time. Clindamycin and two macrolide antibiotics (roxithromycin, erythromycin) were concentrated 7- to 14-fold by cytoplasts. This indicates that cytoplasmic granules are not essential for accumulation of these drugs. Adenosine inhibited cytoplast uptake of clindamycin, which enters intact phagocytic cells by the membrane nucleoside transport system. Roxithromycin uptake by cytoplasts was inhibited by phagocytosis, which may reduce the number of cell membrane sites available for the transport of macrolides. These studies have added to our understanding of uptake mechanisms for antibiotics which are highly concentrated in phagocytes.

roxithromycin 600 mg per day 2017-09-15

Roxithromycin sputum and serum concentrations after administration of therapeutic doses (150 mg in a single dose) were evaluated in six patients. Blood samples and pooled sputum samples were collected at corresponding time intervals up to 24 h after drug administration. Roxithromycin sputum levels were found to be almost always above serum concentrations, the highest sputum levels being 5.85 +/- 2.5 micrograms/ml in the interval ranging from 2 to 4 h after drug administration. Due to its antibacterial spectrum and favourable pharmacokinetic properties, roxithromycin, like other macrolide antibiotics, seems to be particularly indicated in the treatment of respiratory tract infections.

roxithromycin drug 2016-03-20

An analytical method for simultaneous determination of erythromycin propionate and its active metabolite, erythromycin base, in human plasma by high-performance liquid chromatography-electrospray mass spectrometry (HPLC-ESI-MS) was developed and validated. Roxithromycin was selected as the internal standard. The samples were directly injected after simple deproteinized procedure only. The separation was achieved on a Johnson Spherigel analytical column packed with 5 microm C18 silica, employing acetonitrile -0.1% formic acid aqueous solution (50:50) as mobile phase. The quantification of target compounds was obtained by using a selected ion monitoring (SIM) at m/z 790.7 for erythromycin propionate, m/z 734.7 for erythromycin base and m/z 837.8 for roxithromycin. The correlation coefficients of the calibration curves were better than 0.997 (n=6), in the ranges from 2 ng/ml to 1 microg/ml, and from 1 to 10 microg/ml for erythromycin propionate and base. The method can provide the necessary sensitivity, precision and accuracy to allow the simultaneous determination of both compounds in a patient's plasma following a single administration of erythromycin stinoprate capsule (500 mg erythromycin base equivalent).