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Moxifloxacin: a review of its use in the management of bacterial infections
Abstract
Moxifloxacin (Avelox) is a fluoroquinolone antibacterial with a methoxy group in the C-8 position and a bulky C-7 side chain. Moxifloxacin is approved for use in the treatment of acute exacerbations of chronic bronchitis (AECB), community-acquired pneumonia (CAP), acute bacterial sinusitis and uncomplicated skin and skin structure infections (approved indications may differ between countries). Moxifloxacin has a broad spectrum of antibacterial activity, including activity against penicillin-resistant Streptococcus pneumoniae. It achieves good tissue penetration and has a convenient once-daily administration schedule, as well as being available in both intravenous and oral formulations in some markets. Moxifloxacin has good efficacy in the treatment of patients with AECB, CAP, acute bacterial sinusitis and uncomplicated skin and skin structure infections, and is generally well tolerated. Thus, moxifloxacin is an important option in the treatment of bacterial infections.
... In children with mild-to-moderate persistent asthma, a favourable response to inhaler corticosteroid was associated with higher levels of exhaled nitric oxide, total eosinophils counts, levels of serum IgE and other markers of allergic inflammation (3). Moreover, Cai et al. in a study on patients with stable mild to moderate asthma that were treated with montelukast in four-week concluded that there was not significant correlation between the clinical response and serum IgE levels (4). The percentage of patients with asthma and airway responsiveness in general population with higher IgE levels is more than subjects with lower IgE levels (5). ...
... Introduction: Endobronchial ultrasound guided TBNA (EBUS-TBNA) is a minimally invasive real-time procedure which has been shown to have a high yield for the evaluation of the mediastinum (1)(2)(3)(4). Here we reported our experience of EBUS-TBNA for mediastinal lymphadenopathy and also proved the yields by thoracotomy. ...
... Keywords: reverse-phase high-pressure liquid chromatography, intrapulmonary pharmacokinetics Introduction: Moxifloxacin-HCl (BAY 12-8039) is a relatively new 8-methoxyquinolone with a broad spectrum of antimicrobial activity against respiratory tract pathogens, including Gram-positive and Gram-negative organisms, anaerobic bacteria and atypical respiratory tract pathogens [1][2][3] . It showed very rapid bactericidal activity and favourable tissue kinetics, especially the penetration to intra and extravascular compartment of lung tissue [4] [5] . Moreover it has a long-time post antibiotic effect (PAE) [6] [7] . ...
Introduction: Community-Acquired Pneumonia (CAP) continues to be a major cause
of illness among Filipinos. Clinical Guidelines for CAP are available, particularly
the 2004 Updated Version of Philippine Consensus Guidelines on CAP. However,
management of CAP and adherence rate to Guidelines still varies. Hence, the objective
of the study is to assess the impact of the Philippine Consensus Guidelines
among patients diagnosed with CAP at VRP Medical Center. Specifically, compare
patients who were treated in accordance with the Guidelines and those who were not
in terms of demographics, clinical variables and clinical outcomes.
Methods: This is a Propsective Observational study involving patients admitted
with CAP at VRP Medical Center from December 2006 to October 2007 were
included. Inclusion Criteria are: 1) Age of 18 years and above with 2) Clinical signs
and symptoms (i.e. Cough, Sputum Production) and 3) Chest radiograph compatible
with CAP. Exclusion criteria: 1) Immunocompromised Patients, 2) Long-term
steroids use, 3) Concomitant Infections, 4) Cardiopulmonary Arrest and 5) Admitted
in the previous 2 weeks and/or admitted due to other conditions. Pertinent
information including demographic and clinical variables, initial antibiotics and
patient outcomes such as survival, improvement of clinical symptoms and length
of hospital stay were recorded in a data form. Data was encoded and tabulated in
MS-Excel. Student’s t-Test was used for quantitative variables. Chi-Square Test was
used for qualitative variables.
Results: 206 patients were included and majority (71.4%) of these were treated
according to the Guidelines, with both groups showed no significant difference in
terms of demographic & clinical characteristics. Overall, patients treated according
to guidelines had significant correlation with better outcome measures. Those
under Moderate & High Risk group who received guideline-based treatment showed
a significant response in terms of clinical improvement and survival while only in
Moderate Risk Group showed a significant difference in length of stay.
Conclusion: Guideline-concordant treatment of patients with CAP is associated with better clinical outcomes
... Heterocyclic moieties are the most important pharmacologically active structural units and attracted lot of attention among the medicinal chemists and biologists who are involved in the process of developing new drug candidates. [1] Among the heterocyclic moieties, quinoline and its derivatives form a class of such kind of molecular fraction because of their wide variety of pharmacological activities such as antimalarial (quinine, chloroquine), chemotherapeutic activity (topotecan), anti-tubercular activity (mefloquine, moxifloxacin) etc. [2][3][4][5][6] On the other hand, azoles are the most promising five membered nitrogen containing aromatic heterocyclics. From the literature reports it is identified that among all the azoles (imidazole, pyrazole, triazole, tetrazole and pentazole), the 1,2,3-traizoles are the most studied heterocycles. ...
... The combined organic layers was washed with water, brine and dried over anhydrous Na 2 SO 4 . The solvent was removed under reduced pressure and the obtained residue was purified by silica gel column chromatography using 4 : 16 ethyl acetate in hexane as an eluent to afford pure (2-(4-(hydroxymethyl)phenyl)quinolin-3yl)methanol (5) ...
Synthesis of novel 2‐phenylqinoline conjugated bis‐triazole analogues 8(a–n) demonstrated by a series of reactions concerning Vilsmeier‐Haack reaction, Suzuki‐Miyaura cross coupling, reduction of carbonyl groups, and click reaction. The structure of final compounds predicted based on IR, ¹H, ¹³C NMR and Mass spectral data analysis. The title compounds were screened for their in vitro antimicrobial activities against two‐gram positive (S. aureus and S. pyogens) and two‐gram negative (P. aeruginosa and E. coli) bacteria, and two fungal strains (S. rolfs and F. ricini) by employing Amoxicillin and Bavistin as standard drugs, respectively. The compound containing 3‐chlorophenyl, 4‐(trifluoromethyl)phenyl, 3,4‐dimethylphenyl and 3‐fluoro‐4‐chlorophenyl residues, indicated promising antibacterial activity and the best antifungal activity was reported for compounds containing 3‐chlorophenyl, 4‐methoxyphenyl and 4‐(trifluoromethyl)phenyl residues. Further, Insilco screening of these compounds against COVID‐19 main protease of corona virus had displayed good docking scores and binding interactions in its active site pocket.
... The estimated lifetime risk of a person with diabetes mellitus developing a foot ulcer is 15% to 25%, with an annual incidence of 3% to 10% [11]. Major predisposing factors are peripheral neuropathy, peripheral arterial disease, and impaired immunity [12]. More than one-half of non-traumatic lower extremity amputations are related to DFIs, and 85% of all lower extremity amputations in patients with dia betes are preceded by an ulcer [13]. ...
... Moderate to severe infections and wounds previously treated with antibiotics are often polymicrobial, including gram-negative bacilli. Anaerobic pathogens are more commonly present in necrotic wounds and infections of the isch emic foot [12]. In the past 20 years, various fluoroquinolone agents have been used successfully for treating DFIs. ...
... An estimated 140 million prescriptions have been issued for moxifloxacin worldwide, and the drug is included as an effective alternative in guidelines and/or recommendations for each of these indications. [1][2][3][4][5][6][7][8][9][10] The clinical efficacy of moxifloxacin has been unambiguously demonstrated, [11][12][13][14][15][16][17][18][19][20][21][22][23][24][25][26][27][28][29][30] and its safety profile has been analyzed periodically on the basis of pre-marketing studies, [21,[31][32][33][34][35] including populations with risk factors, [36,37] such as the elderly [38,39] and those with hepatic or renal in-sufficiency. [37,40] These data did not show significantly higher toxicity of moxifloxacin compared with commonly used antibiotics if the contraindications and precautions of use mentioned in the Summary of Product Characteristics [41][42][43] are taken into account. ...
... Overall, the distribution of patients among the different indications mirrors the current prescribing patterns and clinical usage. [19,29] The majority of patients receiving oral moxifloxacin were treated for respiratory tract infections, [66] whereas patients receiving intravenous or intravenous/oral therapy (i) were older; (ii) were predominantly treated for CAP, cIAI and cSSSI; and (iii) had a higher incidence of pre-existing risk factors (related to the severity of their infection and their age). ...
Background
Moxifloxacin, a fluoroquinolone antibiotic, is used for the treatment of respiratory tract, pelvic inflammatory disease, skin, and intra-abdominal infections. Its safety profile is considered favorable in most reviews but has been challenged with respect to rare but potentially fatal toxicities (e.g. hepatic, cardiac, or skin reactions).
Objective
To analyze and compare the safety profile of moxifloxacin versus comparators in the entire clinical database of the manufacturer.
Setting
Data on the valid-for-safety population from phase II–IV actively controlled studies (performed between 1996 and 2010) were analyzed. Studies were either double blind (n = 22 369) or open label (n = 7635) and included patients with indications that have been approved in at least one country [acute bacterial sinusitis, acute exacerbation of chronic bronchitis, community-acquired pneumonia, uncomplicated pelvic inflammatory disease, complicated and uncomplicated skin and skin structure infections, and complicated intra-abdominal infections] (n = 27 824) and patients with other indications (n = 2180), using the recommended daily dose (400 mg) and route of administration (oral, intravenous/oral, intravenous only). The analysis included patients at risk (age ≥65 years, diabetes mellitus, renal impairment, hepatic impairment, cardiac disorders, or body mass index <18 kg/m2). Patients with known contraindications were excluded from enrollment by study protocol design, but any patient having entered a study, even if inappropriately, was included in the analysis.
Main Outcome Measure
Crude incidences and relative risk estimates (Mantel-Haenszel analysis) of patients with any adverse event (AE), adverse drug reaction (ADR), serious AE (SAE), serious ADR (SADR), treatment discontinuation due to an AE or ADR, and fatal outcomes related to an AE or ADR.
Results
Overall incidence rates of AEs were globally similar in the moxifloxacin and comparator groups. By filtering the data for differences in disfavor of moxifloxacin (i) at ≥2.5% for events with an incidence ≥2.5% or at ≥2-fold for events with an incidence <2.5% in one or both groups and (ii) affecting ≥10 patients in either group, we observed slightly more (i) AEs in double-blind intravenous-only and open-label oral studies, (ii) SAEs in double-blind intravenous-only studies, (iii) ADRs and SADRs in open-label oral studies, (iv) SADRs in open-label intravenous/oral studies, and (v) premature discontinuation due to AEs in open-label intravenous-only studies. The actual numbers of SADRs (in all studies) were small, with clinically relevant differences noted only in intravenous/oral studies and mainly driven by ‘gastrointestinal disorders’ (15 versus 7 patients) and ‘changes observed during investigations’ (23 versus 7 patients [asymptomatic QT prolongation: 11 versus 4 patients in double-blind studies]). Analysis by comparator (including another fluoroquinolone) did not reveal medically relevant differences, even in patients at risk. Incidence rates of hepatic disorders, tendon disorders, clinical surrogates of QT prolongation, serious cutaneous reactions, and Clostridium difficile-associated diarrhea were similar with moxifloxacin and comparators.
Conclusion
The safety of moxifloxacin is essentially comparable to that of standard therapies for patients receiving the currently registered dosage and for whom contraindications and precautions of use (as in the product label) are taken into account.
... Moxifloxacin is a fourth generation synthetic fluoroquinolone antibacterial agent with powerful activity against both Gram-positive and Gram-negative bacteria, as well as atypical organisms and anaerobes (1). Moxifloxacin is used to treat certain infections caused by bacteria such as pneumonia, and skin, and abdominal (stomach area) infections. ...
The aim of this study was to assess whether the pharmacokinetic profiles of two Moxifloxacin formulations were similar. Moxifloxacin is a fluoroquinolone antibacterial agent with a broad spectrum of activity, encompassing Gram-negative and Gram-positive bacteria. This was a randomized, 2 sequences and 2 periods, crossover comparative study of two medications: Avalox® 400mg coated tablet, manufactured by Bayer S.A (reference), and Moxifloxacin 400mg coated tablet, manufactured by Eurofarma Laboratórios S.A (test). Plasma samples obtained from 36 eligible subjects were analyzed for Moxifloxacin using LC-MS/MS as analytical method and Moxifloxacin-d4 as internal standard. The statistical analysis showed no significant differences for AUC0-t (Avalox® vs. Moxifloxacin Eurofarma test CI [94.25 – 99.28]) and Cmax (Avalox® vs. Moxifloxacin Eurofarma test CI [90.70 – 106.45]). The current pharmacokinetic study demonstrated bioequivalence between the single agents and provided evidence of bioequivalence between Avalox® and Moxifloxacin Eurofarma.
... Moxifloxacin (1-cyclopropyl-7-(2,8-diazo bicyclo [4.3.0.] nonane)-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3-quinolone carboxylic acid), (MOX) is a fluoroquinolone antibacterial with a methoxy group in the C-8 position. Moxifloxacin has antibacterial activity against a broad spectrum of Gram-positive and Gram-negative organisms [39,40]. The structural formulae of metronidazole and moxifloxacin are shown in Figure 2. Several RP-HPLC methods were reported for the assay of metronidazole and moxifloxacin alone or in combination with other drugs using either acetonitrile or methanol in the mobile phase [41][42][43][44][45][46][47]. ...
Cyrene was evaluated for the first time as a potential sustainable mobile phase solvent in re-versed-phase chromatography. As a benign biodegradable solvent, Cyrene is an attractive re-placement to classical non-green organic chromatographic solvents such as acetonitrile and a modifier, co-eluent to known green solvents such as ethanol. Compared to ethanol, Cyrene is less toxic, nonflammable, biobased, biodegradable and cheaper solvent. A fire safety spider Chart was generated to compare the properties of Cyrene to ethanol and show its superiority as a greener solvent. Cyrene's behaviour, advantages, and drawbacks in reversed-phase chromatography, including cut-off value, elution power, selectivity, and effect on the column, were investigated using a model drug mixture of moxifloxacin and metronidazole. A monolithic C18 (10 x 4.6 mm) column was used as a stationary phase. Different ratios of Cyrene: ethanol with an aqueous portion of sodium acetate buffer mobile phases were tested. A mobile phase consisting of Cyrene: ethanol: 0.1 M sodium acetate buffer pH 4.25 (8:13:79, v/v) was selected as most suitable mobile phase system for separating and simultaneously determining metronidazole and moxifloxacin. The greenness and whiteness of the method were evaluated using the qualitative green assessment tool AGREE and the white analytical chemistry assessment tool RGB12. Further potentials of Cyrene as a solvent or modifier in normal phase chromatography, liquid chromatography-mass spectrometry, and supercritical fluid chromatography are discussed.
... Levofloxacin is a bactericidal fluoroquinolone and has been used in first-line and salvage regimens for eradication of H. pylori [3]. Also, moxifloxacin is a bactericidal fluoroquinolone and characterized by fast absorption with a bioavailability of 89% and broad penetration through body fluids and tissues [17]. ...
Background and aim
Eradication of Helicobacter pylori becomes an ongoing challenge worldwide because eradication rates of H. pylori are declining to less than 60% in some countries. As there is no acceptable definite long-standing used therapeutic regimen for H. pylori , clinicians are doing their best to find new regimens to improve eradication rates of H. pylori . Nitazoxanid and fluoroquinolones, including moxifloxacin and levofloxacin, have been used in treatment of H. pylori . The study aimed to assess and compare the efficacy of two nitazoxanide-based quadruple regimens in treatment of patients infected with H. pylori .
Patients and methods
This prospective randomized controlled trial was conducted on 100 patients diagnosed to be infected by H. pylori by stool antigen test (one-step H. pylori Antigen test Device). They were randomized into two groups: group 1: 50 patients were treated for 14 days with quadruple therapy, including nitazoxanide, moxifloxacin, omeprazole, and doxycycline; and group 2: 50 patients were treated for 14 days with quadruple therapy, including nitazoxanide, levofloxacin, omeprazole, and doxycycline. Eradication of H. pylori was assessed 4 weeks after the end of treatment by stool antigen test (one-step H. pylori Antigen test Device).
Results
Eradication rate of H. pylori infection was higher in patients treated with nitazoxanide–moxifloxacin-based quadruple therapy 37 (74%) than in patients treated with nitazoxanide–levofloxacin-based quadruple therapy 32 (64%), but there were no significant differences between the studied groups with P value ( P <0.28). By subgroup analysis of eradication rate among anemic and nonanemic patients treated by nitazoxanide–moxifloxacin and nitazoxanide–levofloxacin-based quadruple therapy, we found that eradication rate was higher in anemic patients 88% and 80% than nonanemic patients 60% and 45%, with significant P values 0.02 and 0.01, respectively.
Conclusions
Use of moxifloxacin instead of levofloxacin in the nitazoxanide-based quadruple regimen improves eradication therapy of H. pylori .
... MF is a fourth-generation fluoroquinolone antibiotic used against bacterial infections [29]. MF belongs to the class I of BCS, where it shows good solubility and permeability [30]. ...
The aim of the study was to investigate the pharmacokinetic parameters of 5-fluorouracil (5FU) and moxifloxacin HCl (MF) after oral administration using layer-by-layer assembled film in enteric-coated capsule. The layer-by-layer (LbL) film was prepared by sequential layering of chitosan and sodium alginate polyelectrolytes containing either 5FU or MF. The films were in vitro evaluated for physical characteristics, drug loading and release behaviour. In vivo pharmacokinetic evaluation was performed in the rat model for three different drug concentrations after oral administration and compared with intravenous administration. The results showed that the thickness of 10-bilayer film was 147 ± 11.66 µm and 212.3 ± 7.19 µm after 5FU and MF loading, respectively. The LbL film with backing layer provided directional release of 5FU and MF, where 63.81 ± 4.52% and 101.38 ± 5.08%, respectively, was released in 24 h. 5FU showed non-linear pharmacokinetics compared with linear pharmacokinetics shown by MF after oral administration. There is a dose-dependent increase in Cmax after oral administration of 5FU and MF LbL film. The Tmax was found to be 720 min and 840 min for 5FU and MF after oral administration. The mean residence time and AUC0–24 at 45 mg/kg were 871.4 ± 6.45 min and 198.6 ± 5.03 × 103 min per ng/mL and 1267 ± 142.4 min and 1590 ± 55.60 103 min per ng/mL for 5FU and MF, respectively. Taken together, colon-targeted LbL film can be developed for oral administration of drugs for local and systemic applications.Graphical Abstract
... Brissette et al. have treated their patients with fourth-generation uoroquinolone that has a different antibacterial spectrum compared to the aminoglycosides we used. 8, 11 In the study by Smadar et al., treatment was given at the ophthalmologist's discretion, making a direct comparison impossible. 9 In this study, we used topical aminoglycosides because they have a broad antibacterial spectrum and are active against most IK-related pathogens. ...
Purpose
To compare the effect of antiseptics and antibiotics on the occurrence of Infectious Keratitis (IK) secondary to Corneal Foreign Body (CFB) removal.
Methods
Multicenter retrospective study conducted between June 2020 and June 2022 in patients referred for CFBs and treated with Picloxydine (Group 1) or Tobramycin (Group 2) for 7 days. A follow-up visit was scheduled on Day 3 (D3) and a phone call on D30. The primary outcome measure was the occurrence of IK.
Results
307 patients (300 men) with a mean age of 42.8 (14.8) years were included. The mean (SD) time to consultation was 43.1 (45.6) hours. Picloxydine and Tobramycin were given to 155 and 152 patients. Half of patients (n = 154, 50.2%) were building workers and 209 (68.1%) did not wear eye protections. CFBs were mainly metallic (n = 292, 95.1%). Upon referral, rust was found in 220 patients (72.1%). A burr was used in 119 (38.9%) patients. IK occurred in 15 (4.9%) patients, 8 (5.3%) in Group 1 and 7 (4.5%) in Group 2 (p = 0.797). IK was successfully treated in all cases. Persistent rust was found in 113 patients (36.9%) on D3 without difference between burr or needle use (p = 0.278). On D3, corneal healing was delayed in 154 patients (47.2%), mainly in burr-treated patients (p = 0.003). The mean (SD) work stoppage duration was 0.32 (0.98) days.
Conclusion
IK rate was 4.9%. The efficacy of antibiotics and antiseptics was similar on CFB removal. Using a burr was associated with a longer healing time. CFBs had a limited social impact.
... Moxifloxacin, a fluoroquinolone of the second generation, is often used to treat bacterial and fungal skin and lung infections [13]. It has a short half-life (between 9 and 16 hours), is readily absorbed after orally administered, and may be given once daily. ...
Objective: The aim of current study was to evaluate effectiveness of moxifloxacin 4th generation quinolones against patients of
H-pylori infection admitted in a tertiary care hospital Peshawar.
Study Design:Observational study
Place and Duration: This study was carried out at Khyber Teaching Hospital, Peshawar from December 2021 to February 2022
Methods: There were 180 patients of both genders had age 18-55 years with H-pylori infection were included. After obtaining
informed written consent detailed demographics of all cases were recorded. Patients were equally divided in two groups. Group
I received 400mg moxifloxacin for 6-days and group II received moxifloxacin for 12-days. All the patients received 1000mg
amoxicillin and lansoprazole 30 mg twice day. Posttreatment results were compared in terms of eradication rate and
complications among both groups.
Results:We found that 105 (58.3%) patients were males and 75 (41.7%) patients were females. Mean age of the patients was
47.6±11.74 years and had mean BMI 25.8±12.34 kg/m2. Majority of the patients 98 (54.4%) were smokers. Most common
comorbidity was hypertension found in 62 (34.4%) cases, diabetes mellitus in 42 (23.3%) cases, chronic pulmonary disease in
28 (15.6%) and ischemic heart disease in 13 (7.2%) cases. We found that eradication rate among cases of group I was lower
found in 59 (65.6%) cases compared to group II found in 80 (88.9%) cases with p value <0.005. Most common complications
were diarrhea, nausea, abdominal pain and dizziness but their frequency was higher in group II but difference was insignificant.
Conclusion: We concluded in this study that the use of moxifloxacin4th generation quinolones against H-Pyloriinfection for 12-
days in reduction of disease severity and higher eradication rate as compared to 7-days treatment. Complications were higher in
10-days of treatment because of excess usage of regular antibiotics but found no any significant difference to 7-days treatment.
... 28 Their effective anti-TB properties has led to the quinolones also becoming the most widely prescribed antibiotic for other bacterial infections, with moxifloxacin used for the treatment of anthrax, cellulitis, endocarditis, intra-abdominal infections, meningitis, and respiratory tract infections. 29 In countries where TB is endemic, quinolones can often be purchased over the counter. Resistance to moxifloxacin by TBcausing Mycobacterium tuberculosis has become a concern and could develop for reasons unrelated to its use in TB treatment. ...
Modified thymine bases, each containing a polymerizable group (either carboxymethylvinyl or acrylamide) at the 5-position, have been incorporated multiple times into an aptamer sequence allowing the sequence to act as...
... Moxifloxacin has demonstrated antibacterial activity against both gram-positive cocci and gram-negative bacteria, and especially against respiratory pathogens (23). Studies have shown that moxifloxacin is effective in the treatment of chronic bronchitis, skin infections, community-acquired pneumonia, and bacterial infections (24,25). In recent years, an increasing number of high-quality clinical studies have focused on the application of moxifloxacin in the treatment of tuberculosis (18,20). ...
Background:
Moxifloxacin is a fourth-generation fluoroquinolone that has shown good antibacterial activity against both gram-positive cocci and gram-negative bacteria. The purpose of this study was to evaluate the safety and efficacy of moxifloxacin in the drug treatment regimen of patients with tuberculosis.
Methods:
We conducted an electronic database search of the PubMed, Embase, the Cochrane Controlled Center Register of Controlled Trials (CENTRAL), Web of Science, Baidu Scholar, and Google Scholar for literature related to clinical randomized controlled trials (RCTs) of tuberculosis patients (from the date of inception of the database to September 25, 2020). The experimental group received moxifloxacin while the control group did not use moxifloxacin. After literature screening, data extraction, and literature quality evaluation, the included studies were meta-analyzed using RevMan software 5.1.
Results:
In total, 13 RCTs involving 7,774 patients were included in this meta-analysis. The negative rate of sputum culture in the experimental group (which received moxifloxacin) was significantly higher than that of the control group after 2 months of treatment [relative risk (RR) =1.12, 95% confidence interval (CI): 1.06-1.18, P<0.0001]. Treatment-related complications in the experimental group were significantly greater than those in the control group (RR =1.34, 95% CI: 1.07-1.67, P=0.01). There was no significant difference in the incidence of serious complications between the two groups (RR =1.09, 95% CI: 0.90-1.33, P=0.38). In addition, there were no significant differences in mortality and recurrence rate between the two groups (RR =0.79, 95% CI: 0.51-1.21, P=0.28; RR =1.41, 95% CI: 0.61-3.25, P=0.42).
Conclusions:
This meta-analysis found that the addition of moxifloxacin to the treatment regimen of pulmonary tuberculosis patients could significantly increase the negative rate of sputum culture after treatment; however, it has no significant effect on the recurrence rate. Also, the addition of moxifloxacin was found to increase the incidence of complications, but did not increase the incidence of mortality or serious complications.
... For the assay of Verapamil in bulk and dosage forms, a gas chromatographic method was recommended by United States Pharmacopoeia and a non-aqueous titration method was given by Indian Pharmacopoeia. Several analytical methods for the determination of VRP are reported in the literature [25][26][27][28][29][30][31][32][33][34]. To the best of our knowledge, data for the estimation of above drugs using UV-Visible spectrophotometric method was not reported. ...
... [12] Moxifloacin binds strongly to both DNA gyrase and poisomerase IV, thus reducing the occurrence of bacterial drug resistance. [30] Nowadays, more and more researches have been focused on the application of moxifloxacin in the treatment of TB. Many meta-analysis and review articles have evaluated the efficacy and safety of moxifloxacin in the treatment of nondrug resistant or the initial therapy of tuberculosis. ...
Background:
Moxifloxacin, a fourth generation fluoroquinolone, which has good antibacterial activity against both Gram-positive cocci and Gram-negative bacteria. To date, there are no meta-analysis to evaluate the efficacy and safety of moxifloxacin for multi-drug resistant tuberculosis (MDR-TB) treatment. This meta-analysis to explore the efficacy and safety of the moxifloxacin in treatment of MDR-TB in adults.
Methods:
Databases of PubMed, Embase, Embase, Ovid, and Google Scholar databases were investigated for eligible literatures from their establishments to August, 2019. Included studies were selected according to precise eligibility criteria: MDR-TB confirmed by the clinical diagnostic criteria (at least 2 or more first-line drugs resistant to isoniazid and rifampicin). Study design was limited to retrospective studies, randomized controlled trials, or prospective cohort studies; the control group was treated with other drugs or no moxifloxacin. Statistical analysis was performed by RevMan 5.3 software.
Results:
Eight studies with a total of 1447 patients were finally eligible for the final systematic review and meta-analysis. Moxifloxacin regimen was related to a significantly elevated treatment success rate compared with levofloxacin or conventional therapy regimen (OR = 1.94; 95% CI = 1.16-3.25, P = .01). No significant difference of sputum culture conversion rate (OR = 1.15; 95% CI = 0.82-1.60; P = 0.43) was found between 2 groups. In addition, there was no significant difference in the increased risks of gastrointestinal trouble (OR = 1.28; 95% CI = 0.98-1.68; P = .05), hepatotoxicity (OR = 0.91; 95% CI = 0.64-1.30; P = .6), dermatologic abnormalities (OR = 1.11; 95% CI = 0.74-1.67; P = .62), and vision change (OR = 1.47; 95% CI = 0.74-2.89; P = .27) between the moxifloxacin-containing regimens and control group.
Conclusions:
This meta-analysis revealed that the addition of moxifloxacin to the recommended regimen significantly improved the rate of treatment success in the treatment of MDR-TB, with no additional adverse moxifloxacin events.
... Moxifloxacin is a fourth generation fluoroquinolone with extended action against gram negative and gram positive bacteria. This antibacterial have methoxy group on position of C-8 while a massive C-7 side chain [1]. Moxifloxacin [2]. ...
Objective: The objective of the current study was to characterize the quality control parameters and cost effective analysis of five selected different brands of moxifloxacin 400 mg tablets. Moxifloxacin is a fourth generation fluoroquinolone antibiotic, having activity against gram-negative (Escherichia coli, Haemophilus influenza, Klebsiella pneumonia, Proteus mirabilis and Moraxella catarrhalis) and gram-positive (Staphylococcus aureus, Streptococcus anginosus, Enterococcus faecalis, Pneumococci, and Streptococcus pyogenes) microorganisms. Methods: All five selected brands were coded as M-1, M-2, M-3, M-4 and M-5 and the price were noted as PKR 805.82 (2.81), 475 (2.25) and 160 ($1.20) per 5 tablets, respectively. By using official and non-official tests, all the brands were evaluated for physical and chemical characteristics such as hardness, weight variation, friability, disintegration, dissolution, content uniformity and assay using already reported HPLC and spectrophotometric methods. The brand M-1 was considered as reference, due to its good physical and chemical properties and its dissolution profile was compared with other brands, using model independent approach (similarity factor-f2), to compare the dissolution profile of generic drug products with reference. There is a large variation in the price of reference and other generic drugs available in the local market of Pakistan. Results: The results of physical and chemical tests showed that that all brands of moxifloxacin were within the specified limits. The amount of moxifloxacin in all five brands was within the USP specification of not less than 80% at 45 minutes. Similarly, the values of f2 for M-2 (77.20), M-3 (69.56), M-4 (76.98) and M-5 (82.17) indicated that all the brands were found to be similar with reference brand. Conclusion: It was concluded that low cost local brands of moxifloxacin 400 mg tablets can be used as an alternative in case of unavailable brands in the market. This study will be helpful to the healthcare practitioners to prescribe other generic brands of moxifloxacin, as the cost is 50% less in comparison with reference which may reduce the medication cost to the patients.
... In the present study, on calculating pharmacokinetic values for plasma concentration of MX, the AUC t was within these limits. The parameters in the one-compartment pharmacokinetic analysis correlated well to data of healthy individuals found in the literature, 26 maybe with the exception of a shorter half-life. ...
In this study, we evaluated a new aspect of negative pressure wound therapy (NPWT) as an analytical tool for pharmacokinetic studies. Twenty‐one patients with soft tissue defects scheduled to receive NPWT were included in this study. Concomitant to NPWT, all patients received intravenous moxifloxacin (MX). At different time intervals, blood plasma levels of MX were sampled and compared with synchronous concentrations of MX in the exudate obtained from the NPWT drainage system. Serial measurements were performed upon initiation of the therapy as well as in the steady state (after 5 days). At steady state, wound tissue was obtained intraoperatively. High‐performance liquid‐chromatography (HPLC) was used for analysis. At 1 hour post‐administration, the exudate/plasma levels (mg/L) were 1.92/3.07; at 12 hours, 0.80/1.14; at 24 hours, 0.26/0.43; and at 120 hours (steady state), 0.42/0.47. There was a correlation between exudate and plasma levels reaching approximately 0.75. Until now, methods for pharmacokinetic studies concerning interstitial fluid are difficult to apply in the clinical context. The presented method showed limitations, but we believe that, after methodological improvements, measurements of substances in the interstitial fluid by means of NPWT are feasible.
... Moxifloxacin ophthalmic solution 0.5% exhibits enhanced bioavailability due to a unique molecular structure that combines high lipophilicity for enhanced corneal penetration with high aqueous solubility at physiological pH. Numerous studies have shown that moxifloxacin ophthalmic solution 0.5% has high potency against a broad range of microbial species and a favorable profile in terms of safety and tolerability [36][37][38]. Moxifloxacin is a bactericidal, concentration-dependent and anti-infective. It interferes with bacterial survival by binding to DNA gyrase (topoisomerase II) and topoisomerase IV, essential bacterial enzymes involved in the replication, translation, repair and recombination of deoxyribonucleic acid. ...
Background:
The objective of this study was to apply Quality by Design (QbD) principles on process parameter optimization for development of hybrid delivery system (combination of (SLNs) and In-situ gelling system) for hydrophilic drug Moxifloxacin Hydrochloride (MOX) to achieve its controlled delivery, which otherwise may not be possible through single type of technology.
Methods:
Risk assessment studies were carried out to identify probable risks influencing CQAs on the product. In design of experiments (DoE), the process parameters (independent variables) i.e., chiller temperature X1, High pressure homogenization (HPH) pressure X2, and HPH cycles X3 were optimized using a three factor two level face centered central composite design to streamline the influence on three responses, namely encapsulation efficiency Y1, particle size Y2 and outlet temperature Y3. Independent and dependent variables were analyzed to establish a full-model second-order polynomial equation. F value used to confirm the omission of insignificant parameters/interactions to derive a reduced-model polynomial equation to predict the Y1, Y2 and Y3 of moxifloxacin in situ gelled nanosuspension.
Results:
Desirability plots showed the effects of X1, X2, and X3 on Y1, Y2 and Y3. The design space generated to obtain optimized process parameters viz. chiller temperature (-5˚C), HPH pressure 800 - 900 bar and 8 cycles that resulted in nanosuspension with ≈ 500 nm size, encapsulation efficiency >65% and final formulation temperature <23˚C that was necessary to maintain the formulation in liquid state.
Conclusion:
Quality by Design (QbD) approach is recently been encouraged by regulatory bodies to improve the quality of the finished product. This approach proved to be a useful tool in the development of robust nanosuspension of highly hydrophilic drugs with improved efficiency. Results indicate that such hybrid gel systems can be used to control the release of SLNs from application site and prolong their action in a sustained manner.
... Newer quinolones like moxifloxacin are possible combination partners, which were supposed to be examined more closely in this study due to their improved spectrum of activity against gram positive, gram negative, and anaerobic pathogens as well as their good oral bioavailability, activity, and safety. 2 The superiority of moxifloxacin compared with vancomycin was demonstrated in the treatment of prosthetic infections. 3 In addition, the oral bioavailability is almost as high as on parenteral administration. ...
The efficacy of antibiotic monotherapy and combination therapy in the treatment of implant-associated infection by Staphylococcus aureus was evaluated in an animal study. The femoral medullary cavity of 66 male Wistar rats was contaminated with S. aureus (ATCC 29213) and a metal device was implanted, of which 61 could be evaluated. Six treatment groups were studied: flucloxacillin, flucloxacillin in combination with rifampin, moxifloxacin, moxifloxacin in combination with rifampin, rifampin, and a control group with aqua. The treatment was applied for 14 days. After euthanasia, the bacterial counts in the periprosthetic bone, the soft tissue, and the implant-associated biofilm were measured. Both antibiotic combination treatments (moxifloxacin plus rifampin and flucloxacillin plus rifampin) achieved a highly significant decrease in microbial counts in the bone and soft tissue and in the biofilm. Mono-antibiotic treatments with either moxifloxacin or flucloxacillin were unable to achieve a significant decrease in microbial counts in bone and soft tissue or the biofilm, whilst rifampin was able to reduce the counts significantly only in the biofilm. Antibiotic resistance was measured in 1/3 of the cases in the rifampin group, whereas no resistance was measured in all other groups. The results show that combinations of both moxifloxacin and flucloxacillin plus rifampin are adequate for the treatment of periprosthetic infections due to infections with S. aureus, whereas monotherapies are not effective or not applicable due to the rapid development of antibiotic resistance. Therefore, moxifloxacin is an effective alternative in combination with rifampin for the treatment of implant-associated infections.
... 24,25 Studies have shown that moxifloxacin has good efficacy in the treatment of acute exacerbations of chronic bronchitis, skin structure infections, intra-abdominal infections, community-acquired pneumonia, and certain other diseases resulting from bacterial infections. 24,26,27 Accumulating research has been focused on the use of moxifloxacin for TB treatment. A review by Thee et al. ...
Background:
To evaluate the efficacy and safety of the introduction of moxifloxacin into the recommended regimen for tuberculosis (TB) treatment.
Methods:
A meta-analysis was performed of nine eligible studies regarding the effect of moxifloxacin plus the recommended regimen compared to the recommended regimen alone for the treatment of TB.
Results:
In the efficacy analysis, the overall odds ratio (OR) for sputum culture conversion was 1.895 (95% confidence interval (CI) 1.355-2.651, p=0.000), indicating that when moxifloxacin is combined with the recommended regimen, the rate of sputum culture conversion is elevated compared to the recommended regimen alone. The overall OR for recurrence was 0.516 (95% CI 0.342-0.920, p=0.022), suggesting that the introduction of moxifloxacin into the recommended regimen reduces TB relapse after treatment. In the safety analysis, the overall OR was estimated to be 1.001 (95% CI 0.855-1.172, p=0.989), demonstrating that adding moxifloxacin to the recommended regimen does not cause more adverse events during TB treatment.
Conclusions:
This meta-analysis suggests that the introduction of moxifloxacin into the recommended regimen for the treatment of non-drug resistant TB improves the clinical outcome by elevating the culture conversion rate and reducing the recurrence rate.
... However, there is modest evidence in animal models that macrolide antibiotics [1][2][3][4][5][6] and, to a lesser extent, fluoroquinolone antibiotics [7] may increase HR, though there is only sparse clinical evidence for an HR effect in humans for these antibiotic classes [8,9]. The fluoroquinolone moxifloxacin is of particular interest because it is often used to treat infections associated with an already-increased HR, such as community-acquired pneumonia [10], and it is used as an active control in thorough QT (TQT) studies [11,12] QT is the electrocardiographic QT interval and reflects the duration of myocardial repolarization. TQT studies are rigidly designed protocols to measure QT interval changes caused by drugs. ...
(1) Background: We assessed the effect of moxifloxacin on heart rate, and reviewed the heart rate effects of other antibiotics; (2) Methods: A total of 335 normal volunteers had 12-lead electrocardiograms recorded at multiple time points before and during treatment with moxifloxacin and with placebo in seven consecutive, thorough QT studies of crossover design; (3) Results: The average baseline heart rate across the seven studies was 61.5 bpm. The heart rate after moxifloxacin dosing was analyzed at five time points shared by all seven studies (hours 1, 2, 3, 12 and 24). The maximum mean heart rate (HR) increase for the seven studies combined was 2.4 bpm (95% CI 1.6, 3.3) at hour 2. The range of mean maximum increases among the seven studies was 2.1 to 4.3 bpm. For the seven studies combined, the increase was statistically significant at all but the 24 h time point. The maximum observed individual increase in HR was 36 bpm and the mean maximum increase was 30 ± 4.1 bpm by time point and 8 ± 6.9 bpm by subject. Many antibiotics increase HR, some several-fold more than moxifloxacin. However, clinicians and clinical investigators give little attention to this potential adverse effect in the medical literature; (4) Conclusions: The observed moxifloxacin-induced increase in HR is large enough to be clinically relevant, and it is a potentially important confounder in thorough QT studies using moxifloxacin as an active control. More attention to heart rate effects of antibiotics is warranted.
... Its spectrum of activity comprises both Gram-positive and Gram-negative bacteria such as Staphylococcus, Streptococcus, and atypical bacteria. [1][2][3][4] It can be commonly used in the treatment of community-acquired pneumonia and it is also used as a second-line agent in treating sensitive and multidrug resistant tuberculosis. The bactericidal effect on slow replicating bacilli is the important factor that shortens the treatment and it is the reason why MOXI is introduced to standard therapy. ...
Moxifloxacin is a representative of the fourth generation of the fluoroquinolones. It posseses bacteriostatic activity against Gram-positive and Gram-negative bacteria. A simple and fast HPLC-UV method was developed for moxifloxacin analysis. The separation was performed on C18 column. The mobile phase was a mixture of acetonitrile and 0.4% triethylamine solution. The regression curve was linear over the range 0.2-10.0 µg/ml. The validation parameters obey the European Medicine Agency limits. The in vivo study confirmed the practical application of the method.
... MOXI is characterized by a wide range of activity. The activity comprises Gram-negative and Gram-positive bacteria, such as Staphylococcus, Streptococcus, Enterococcus, and also atypical bacteria and anaerobes [58][59][60][61]. It is used in the treatment of conjunctivitis, keratitis, pre-and postoperatively to control infections of the eyes. ...
Fluoroquinolones of the third and fourth generation posses wide bactericidal activity. Monitoring concentrations of antibacterial agents provides effective therapy and prevents the increase of bacterial resistance to antibiotics. The pharmacodynamic parameters that best describe fluoroquinalone activity are AUC/MIC and Cmax/MIC. Determining the level of this type of drug is essential to reach the effective concentration that inhibits the growth of bacteria. Determining the pharmaceutical formulation confirms the purity of a substance. Many methods have been developed to determine the level of these substances. They involve mainly the following analytical techniques: chromatography, capillary electrophoresis, and spectroscopy. The separation techniques were combined with different measuring devices, such as ultraviolet (UV), fluorescence detector (FLD), diode array detector (DAD), and mass spectrometry (MS). The analytical procedures require proper sample pre-conditioning such as protein precipitation, extraction techniques, filtration, or dilution. This paper reviews the reported analytical methods for the determining representatives of the third and fourth generation of fluoroquinolones. Attention was paid to pre-conditioning of the samples and the applied mobile phase. This report might be helpful in the selection of the proper procedure in determining the abovementioned drugs in different matrices.
Graphical abstract
... Therre is little information in the literature about the microbial transformations of fourth-generation quinolones except for moxifloxacin (CCCXVII), an 8-methoxyfluoroquinolone (BAY 12-8039) used for treating infections of the skin and respiratory tract (Keating and Scott, 2004). In the biotransformation of moxifloxacin by G. striatum DSM 9592, several metabolites, among them 3-hydroxymoxifloxacin (CCCXVIII), 6-hydroxymoxifloxacin (CCCXIX), and a demethylated derivative (8-hydroxymoxifloxacin) (CCCXX), were produced in 3 days (Wetzstein et al., 1997): ...
The monography describes examples of the application of microbial
technologies for obtaining of derivatives from a series of nitrogen heterocycles
(saturated nitrogen heterocycles, azaarenes and quinolones). It is proposed
alternative ways for synthesize substances that are difficult to obtain by the
methods of organic chemistry. Microbial technologies of synthesis of organic
compounds may find out a practical application in the production of various
drugs.
... Moxifloxacin is a noteworthy drug as it has been shown to be active against Mycobacterium tuberculosis, a bacterial pathogen not killed by most other classes of antibiotics (exception being novobiocin) given as monotherapy. [138][139][140] Furthermore, the fourth-generation fluoroquinolones have been reported to act as more potent and broad-spectrum inhibitors even against anaerobic bacteria. 141 Aminocoumarins ( Fig. 6) (e.g., novobiocin, clorobiocin, and coumermycin A1) and simocyclinones are another group of antibiotics that target bacterial DNA gyrase, however, with a mechanism different from that of quinolones. ...
DNA topoisomerases are ubiquitously present remarkable molecular machines that help in altering topology of DNA in living cells. The crucial role played by these nucleases during DNA replication, transcription, and recombination vis-à-vis less sequence similarity among different species makes topoisomerases unique and attractive targets for different anticancer and antibacterial drugs. However, druggability of topoisomerases by the existing class of molecules is increasingly becoming questationable due to resistance development predominated by mutations in the corresponding genes. The current scenario facing a decline in the development of new molecules further comprises an important factor that may challenge topoisomerase-targeting therapy. Thus, it is imperative to wisely use the existing inhibitors lest with this rapid rate of losing grip over the target we may not go too far. Furthermore, it is important not only to design new molecules but also to develop new approaches that may avoid obstacles in therapies due to multiple resistance mechanisms. This review provides a succinct account of different classes of topoisomerase inhibitors, focuses on resistance acquired by mutations in topoisomerases, and discusses the various approaches to increase the efficacy of topoisomerase inhibitors. In a later section, we also suggest the possibility of using bisbenzimidazoles along with efflux pump inhibitors for synergistic bactericidal effects.
... To benefit from niosomal formulation of antimicrobial agents as well as chitosan-based gel for controlled, localized drug delivery, we developed chitosan gel-embedded moxifloxacin (MFX) loaded niosomal bioadhesive system. MFX is a broad-spectrum fluoroquinolone that has potent activity against a wide range of bacteria [11]. Due to its broad antibacterial spectrum, its high efficiency, and its potential to promote wound healing, MFX is an ideal candidate for wound infection treatment [12]. ...
The purpose of this study was to prepare and characterize a hybrid system of moxifloxacin loaded niosomes incorporated into chitosan gel as a potential carrier for topical antimicrobial delivery. The prepared system was characterized regarding entrapment efficiency, particle size, zeta potential, in vitro drug release kinetics, morphology, FTIR analysis, bioadhesive strength and rheological behavior. The effect of different formulation parameters (surfactant type, surfactant to drug ratio, cholesterol percentage and loading methodology) on moxifloxacin entrapment and drug release was evaluated. The antibacterial effectiveness of various formulations was also assessed by measuring the minimal inhibitory concentrations, minimal bactericidal concentrations and agar diffusion assay using P. aeruginosa and S. aureus as model pathogens. The optimized niosomal formulation showed 73% drug entrapment, 47% drug release in 8 hours and was ∼290 nm in particle diameter and negatively charged (ζ ∼ –23 mV). The gel-embedded niosomes exhibited pseudo-plastic flow behavior and more sustained drug release profile compared to niosomes. The niosomal formulation of moxifloxacin was the most efficient system against P. aeruginosa, while gel based formulations were superior against S. aureus. Taken together, moxifloxacin-in-niosomes-in-gels hold great promise for topical microbial infections.
... [4] These are well-absorbed orally and cannot cross BBB, have major adverse effects GIT related however CNS related ADR are severe but rare. [3,5,6] Heterocyclic quinolones stand for diverse biological and chemical reactivity. [7] The Quinolonecarboxylic acids, carboxyquuinoloes, or 4-quinolones are a group of synthetic antibacterials structurally related to nalidixic acid. ...
INTRODUCTION Fluoroquninolones are a family of broad-spectrum synthetic antimicrobial agents having particular activity against gram-negative organisms especially Pseudomona aeroginosa. These compounds have a fluoro group attached to the central ring system. Nalidixic acid is the parent compound of the group introduced in 1962. They are classified as 1st, 2nd, 3rd and 4th generation fluoroquinolones having nalidixic acid, ciprofloxacin, levofloxacin and moxifloxacin belonging to the classes respectively. These are bactericidals and acts by attacking the DNA gyrase and topoisomerase in gram-negative and –positive bacteria respectively.[1,3] The activity may reduce in acidic media.[4] These are well-absorbed orally and cannot cross BBB, have major adverse effects GIT related however CNS related ADR are severe but rare.[3,5,6] Heterocyclic quinolones stand for diverse biological and chemical reactivity.[7] The Quinolonecarboxylic acids, carboxyquuinoloes, or 4- quinolones are a group of synthetic antibacterials structurally related to nalidixic acid. The term 4- quinolone has been used as a generic name for the common 4-oxo-1, 4- dihydroquinoline skeleton. Under this system nalidxic acid, a napthyridene derivative, is an 8- aza-4 quinolone, cinoxacin, a cinnoline derivative, is a 2-aza-4-quinolone, and pipemidic and piromidic acids, pyridopyrimidine derivatives, 6,8-diaza-4-quinolones.[8]
(PDF) Degradation of selected Fluoroquinolones. Available from: https://www.researchgate.net/publication/285370399_Degradation_of_selected_Fluoroquinolones [accessed Oct 09 2019].
... fig.1(b)] is a synthetic fourth generation floro quinolone antibiotic [26]. The mechanism of action involve inhibition of an enzyme topoisomerase II (DNA gyrase), which is essential for bacterial DNA replication [27]. It is used in ocular infection (conjunctivitis), acute sinusitis, lower respiratory tract infections and urinary tract infection [28][29][30][31][32]. Moxifloxacin is official in BP 2010 [33]. ...
Objective: To develop rapid, accurate, reproducible, validated and economical difference spectroscopy method for the simultaneous determination of moxifloxacin (MFN) and cefixime (CEF) in tablet dosage forms. Methods: The method comprised the measurement of the absorbance of a solution of the tablet extract in 0.1 M NaOH relative to that of an equimolar solution in 0.1 M HC1 at 254 nm for MFN and 292 nm for CEF. The presence of identical isosbestic points for pure drug solutions and tablet extracts indicated the non-interference of excipients in the absorption at these wavelengths. Results: The method was found to be linear over the concentration range of 10-50 μg/ml for CEF and 4-20 μg/ml for MFN. Accuracy was found to be in the range of 99.91-101.18%. Relative standard deviation for precision and intermediate precision was found to be less than 2%. The developed method was successfully applied for the simultaneous estimation of Moxifloxacin and Cefixime in tablet formulation. The results obtained from the validation experiments prove that the developed method is suitable for routine analysis. Conclusion: This method is simple, selective, linear, precise, and accurate and sensitive hence can be successfully employed for the routine quality control of dosage forms containing both the drugs in pharmaceutical industries.
... Furthermore, some studies have attempted to substitute clarithromycin with other antibiotics due to its contribution to treatment failure with moxifloxacin, a second-generation fluoroquinolone mainly used to treat respiratory infections, receiving particular attention. Moxifloxacin is characterized by fast absorption with a bioavailability of 89% due to oral administration and broad penetration through body fluids and tissues [20] . It also has fewer adverse effects and interactions with other drugs compared with other fluoroquinolones [21] . ...
Aim:
To evaluate the efficacy of moxifloxacin-based sequential therapy (MBST) versus hybrid therapy as a first-line treatment for Helicobacter pylori (H. pylori) infection.
Methods:
From August 2014 to January 2015, 284 patients with confirmed H. pylori infection were randomized to receive a 14-d course of MBST (MBST group, n = 140) or hybrid (Hybrid group, n = 144) therapy. The MBST group received 20 mg rabeprazole and 1 g amoxicillin twice daily for 7 d, followed by 20 mg rabeprazole and 500 mg metronidazole twice daily, and 400 mg moxifloxacin once daily for 7 d. The Hybrid group received 20 mg rabeprazole and 1 g amoxicillin twice daily for 14 d. In addition, the Hybrid group received 500 mg metronidazole and 500 mg clarithromycin twice daily for the final 7 d. Successful eradication of H. pylori infection was defined as a negative (13)C-urea breath test 4 wk after the end of treatment. Patient compliance was defined as "good" if drug intake was at least 85%. H. pylori eradication rates, patient compliance with treatment, and adverse event rates were evaluated.
Results:
The eradication rates in the intention-to-treat (ITT) analysis were 91.4% (128/140; 95%CI: 90.2%-92.9%) in the MBST group and 79.2% (114/144; 95%CI: 77.3%-80.7%) in the Hybrid group (P = 0.013). The eradication rates in the per-protocol (PP) analysis were 94.1% (128/136; 95%CI: 92.9%-95.6%) in the MBST group and 82.6% (114/138; 95%CI: 80.6%-84.1%) in the Hybrid group (P = 0.003). The H. pylori eradication rate in the MBST group was significantly higher than that of the Hybrid group for both the ITT (P = 0.013) and the PP analyses (P = 0.003). Both groups exhibited full compliance with treatment (MBST/Hybrid group: 100%/100%). The rate of adverse events was 11.8% (16/136) and 19.6% (27/138) in the MBST and Hybrid group, respectively (P = 0.019). The majority of adverse events were mild-to-moderate in intensity; none were severe enough to cause discontinuation of treatment in either group.
Conclusion:
MBST was more effective and led to fewer adverse events than hybrid therapy as a first-line treatment for H. pylori infection.
... Literature reports many analytical methods for the determination of CEF in single and in combination with other drug, using UV spectroscopy1415 spectro fluorometry [16], HPLC1718192021222324 and HPTLC [25][26]. The mechanism of action involve inhibition of an enzyme topoisomerase II (DNA gyrase), which is essential for bacterial DNA replication [27]. It is used in ocular infection (conjunctivitis), acute sinusitis, lower respiratory tract infections and urinary tract infection2829303132. ...
Objective: To develop rapid, accurate, reproducible, validated and economical difference spectroscopy method for the simultaneous determination of moxifloxacin (MFN) and cefixime (CEF) in tablet dosage forms. Methods: The method comprised the measurement of the absorbance of a solution of the tablet extract in 0.1 M NaOH relative to that of an equimolar solution in 0.1 M HC1 at 254 nm for MFN and 292 nm for CEF. The presence of identical isosbestic points for pure drug solutions and tablet extracts indicated the non-interference of excipients in the absorption at these wavelengths. Results: The method was found to be linear over the concentration range of 10-50 μg/ml for CEF and 4-20 μg/ml for MFN. Accuracy was found to be in the range of 99.91-101.18%. Relative standard deviation for precision and intermediate precision was found to be less than 2%. The developed method was successfully applied for the simultaneous estimation of Moxifloxacin and Cefixime in tablet formulation. The results obtained from the validation experiments prove that the developed method is suitable for routine analysis. Conclusion: This method is simple, selective, linear, precise, and accurate and sensitive hence can be successfully employed for the routine quality control of dosage forms containing both the drugs in pharmaceutical industries. © 2015, International Journal of Pharmacy and Pharmaceutical Science. All rights reserved.
... In the Maastricht IV/Florence Consensus [3] , a fluoro quinolonebased triple therapy such as moxifloxacin or levofloxacin was used as second-line treatment after failure of the standard triple and the bismuth-based quadruple therapies. Moxifloxacin is a secondgeneration fluoroquinolone widely used to treat respiratory and skin infections [11] . Unlike other fluoroquinolones, moxifloxacin has a low incidence of adverse events and fewer interactions with other drugs. ...
To evaluate the efficacy of the 14-d moxifloxacin-based triple therapy for the second-line eradication of Helicobacter pylori (H. pylori) infection.
Between 2011 and 2013, we conducted a retrospective review of the medical records of 160 patients who had experienced failure of their first-line proton pump inhibitor-based eradication therapy and subsequently received the moxifloxacin-based triple therapy as a second-line eradication treatment regimen. The patients who were treated with the moxifloxacin-based triple therapy (oral 20 mg rabeprazole b.i.d., 1000 mg amoxicillin b.i.d., and 400 mg moxifloxacin q.d.) for 7 d were assigned to the RAM-7 group (n = 79) while those who took them for 14 days were assigned to RAM-14 group (n = 81). The eradication rates for both groups were determined by intention-to-treat (ITT) and per-protocol (PP) analyses. ITT analysis compared the treatment groups as originally allocated while the PP analysis including only those patients who had completed the treatment as originally allocated. Successful eradication therapy for H. pylori infection was defined as the documentation of a negative (13)C-urea breath test 4 wk after the end of the eradication treatment.
The overall ITT eradication rate was 76.2% (122/160). The final ITT eradication rates were 70.8% (56/79; 95%CI: 63.3%-77.1%) in the RAM-7 group and 81.4% (66/81; 95%CI: 74.6%-88.3%) in the RAM-14 group (P = 0.034). The overall PP eradication rate was 84.1% (122/145), and the final PP eradication rates were 77.7% (56/72; 95%CI: 70.2%-85.3%) in the RAM-7 group and 90.4% (66/73; 95%CI: 82.8%-98.1%) in the RAM-14 group (P = 0.017). The H. pylori-eradication rates in the RAM-14 group were significantly higher compared with that of the RAM-7 group according to both the ITT (P = 0.034) and the PP analyses (P = 0.017). Both groups exhibited good treatment compliance (RAM-7/RAM-14 group: 100%/100%). The adverse event rates were 19.4% (14/72) and 20.5% (15/73) in the RAM-7 and RAM-14 groups, respectively (P = 0.441). Adverse events occurred in 14 of the 72 patients (19.4) in the RAM-7 group and in 15 of the 73 patients (20.5) in the RAM-14 group. No statistically significant differences (P = 0.441) were observed.
The 14-d moxifloxacin-based triple therapy is a significantly more effective second-line eradication treatment as compared to the 7-d alternative for H. pylori infection in South Korea.
Background
Knowledge regarding CNS pharmacokinetics of moxifloxacin is limited, with unknown consequences for patients with meningitis caused by bacteria resistant to beta-lactams or caused by TB.
Objective
(i) To develop a novel porcine model for continuous investigation of moxifloxacin concentrations within brain extracellular fluid (ECF), CSF and plasma using microdialysis, and (ii) to compare these findings to the pharmacokinetic/pharmacodynamic (PK/PD) target against TB.
Methods
Six female pigs received an intravenous single dose of moxifloxacin (6 mg/kg) similar to the current oral treatment against TB. Subsequently, moxifloxacin concentrations were determined by microdialysis within five compartments: brain ECF (cortical and subcortical) and CSF (ventricular, cisternal and lumbar) for the following 8 hours. Data were compared to simultaneously obtained plasma samples. Chemical analysis was performed by high pressure liquid chromatography with mass spectrometry. The applied PK/PD target was defined as a maximum drug concentration (Cmax):MIC ratio >8.
Results
We present a novel porcine model for continuous in vivo CNS pharmacokinetics for moxifloxacin. Cmax and AUC0–8h within brain ECF were significantly lower compared to plasma and lumbar CSF, but insignificantly different compared to ventricular and cisternal CSF. Unbound Cmax:MIC ratio across all investigated compartments ranged from 1.9 to 4.3.
Conclusion
A single dose of weight-adjusted moxifloxacin administered intravenously did not achieve adequate target site concentrations within the uninflamed porcine brain ECF and CSF to reach the applied TB CNS target.
Microbes in the human body are closely linked to many complex human diseases and are emerging as new drug targets. These microbes play a crucial role in drug development and disease treatment. Traditional methods of biological experiments are not only time-consuming but also costly. Using computational methods to predict microbe-drug associations can effectively complement biological experiments. In this experiment, we constructed heterogeneity networks for drugs, microbes, and diseases using multiple biomedical data sources. Then, we developed a model with matrix factorization and a three-layer heterogeneous network (MFTLHNMDA) to predict potential drug-microbe associations. The probability of microbe-drug association was obtained by a global network-based update algorithm. Finally, the performance of MFTLHNMDA was evaluated in the framework of leave-one-out cross-validation (LOOCV) and 5-fold cross-validation (5-fold CV). The results showed that our model performed better than six state-of-the-art methods that had AUC of 0.9396 and 0.9385 + /- 0.0000, respectively. This case study further confirms the effectiveness of MFTLHNMDA in identifying potential drug-microbe associations and new drug-microbe associations.
Purpose:
To compare the effect of antiseptics and antibiotics on the occurrence of Infectious Keratitis (IK) secondary to Corneal Foreign Body (CFB) removal.
Methods:
Multicenter retrospective study conducted between June 2020 and June 2022 in patients referred for CFBs and treated with Picloxydine (Group 1) or Tobramycin (Group 2) for 7 days. A follow-up visit was scheduled on Day 3 (D3) and a phone call on D30. The primary outcome measure was the occurrence of IK.
Results:
307 patients (300 men) with a mean age of 42.8 (14.8) years were included. The mean (SD) time to consultation was 43.1 (45.6) hours. Picloxydine and Tobramycin were given to 155 and 152 patients. Half of patients (n = 154, 50.2%) were building workers and 209 (68.1%) did not wear eye protections. CFBs were mainly metallic (n = 292, 95.1%). Upon referral, rust was found in 220 patients (72.1%). A burr was used in 119 (38.9%) patients. IK occurred in 15 (4.9%) patients, 8 (5.3%) in Group 1 and 7 (4.5%) in Group 2 (p = 0.797). IK was successfully treated in all cases. Persistent rust was found in 113 patients (36.9%) on D3 without difference between burr or needle use (p = 0.278). On D3, corneal healing was delayed in 154 patients (47.2%), mainly in burr-treated patients (p = 0.003). The mean (SD) work stoppage duration was 0.32 (0.98) days.
Conclusion:
IK rate was 4.9%. The efficacy of antibiotics and antiseptics was similar on CFB removal. Using a burr was associated with a longer healing time. CFBs had a limited social impact.
Hydrophilic interaction liquid chromatography (HILIC) has inherent merits over RP-HPLC in the analyzing of hydrophilic substances. Accordingly, an innovative HILIC-UV methodology is proposed for the simultaneous estimation of ethyl paraben (PRN), fluconazole (FLZ) and moxifloxacin hydrochloride (MOX) in raw materials and pharmaceutical eye gel. The separation process was conducted using Waters XBridge™ HILIC column (100 mm × 4.6 mm, 3.5 μm particle size) at room temperature. Isocratic mobile phase containing acetonitrile: 0.1% triethylamine buffer (90:10, v/v, pH 5.0), was pumped at flow rate 1.0 mL/min and detected at 260 nm. Under these optimized conditions, PRN, FLZ and MOX showed rectilinear relationships with the concentration ranges (0.5–6.0), (5.0–50.0) and (5.0–60.0) μg/mL, respectively. The developed method offered at least fivefold increase in sensitivity within shorter time than the reported methods. Three greenness assessment tools namely: Analytical eco-scale, GAPI and AGREE were exploited to investigate the method's impact on the environment and conduct a comparative study with the reported methods. International council of Harmonization (ICH) guidelines have been followed to calculate validation parameters. The statistical comparison between results of the suggested method and the comparison method showed no discrepancy confirming accuracy of the method.
Topical fluoroquinolones (FQs) are an established treatment for suspected microbial keratitis. An increased FQ resistance in some classes of bacterial pathogens is a concern. Some recently developed FQs have an extended spectrum of activity, making them a suitable alternative for topical ophthalmic use. For example, the new generation FQs, avarofloxacin, delafloxacin, finafloxacin, lascufloxacin, nadifloxacin, levonadifloxacin, nemonoxacin and zabofloxacin have good activity against the common ophthalmic pathogens such as Staphylococcus aureus , Pseudomonas aeruginosa , Streptococcus pneumoniae and several of the Enterobacteriaceae . However, because there are no published ophthalmic break-point concentrations, the susceptibility of an isolated micro-organism to a topical FQ is extrapolated from systemic break-point data and wild type susceptibility. The purpose of this review is to compare the pharmacokinetics and pharmacodynamics of the FQs licensed for topical ophthalmic use with the same parameters for new generation FQs. We performed a literature review of the FQs approved for topical treatment and the new generation FQs licensed to treat systemic infections. We then compared the minimum inhibitory concentrations (MIC) of bacterial isolates and the published concentrations that FQs achieved in the cornea and aqueous. We also considered the potential suitability of new generation FQs for topical use based on their medicinal properties. Notably, we found significant variation in the reported corneal and aqueous FQ concentrations so that reliance on the reported mean concentration may not be appropriate, and the first quartile concentration may be more clinically relevant. The provision of the MIC for the microorganism together with the achieved lower (first) quartile concentration of a FQ in the cornea could inform management decisions such as whether to continue with the prescribed antimicrobial, increase the frequency of application, use a combination of antimicrobials or change treatment.
Novel conjugates (CP) of moxifloxacin (MXF) with fatty acids (1m–16m) were synthesized with good yields utilizing amides chemistry. They exhibit a more pronounced cytotoxic potential than the parent drug. They were the most effective for prostate cancer cells with an IC50 below 5 µM for respective conjugates with sorbic (2m), oleic (4m), 6-heptenoic (10m), linoleic (11m), caprylic (15m), and stearic (16m) acids. All derivatives were evaluated against a panel of standard and clinical bacterial strains, as well as towards mycobacteria. The highest activity towards standard isolates was observed for the acetic acid derivative 14m, followed by conjugates of unsaturated crotonic (1m) and sorbic (2m) acids. The activity of conjugates tested against an expanded panel of clinical coagulase-negative staphylococci showed that the compound (14m) was recognized as a leading structure with an MIC of 0.5 μg/mL denoted for all quinolone-susceptible isolates. In the group of CP derivatives, sorbic (2) and geranic (3) acid amides exhibited the highest bactericidal potential against clinical strains. The M. tuberculosis Spec. 210 strain was the most sensitive to sorbic (2m) conjugate and to conjugates with medium- and long-chain polyunsaturated acids. To establish the mechanism of antibacterial action, selected CP and MXF conjugates were examined in both topoisomerase IV decatenation assay and the DNA gyrase supercoiling assay, followed by suitable molecular docking studies.
The objective of the present study was to develop a nanoemulsion-based in situ gel of Moxifloxacin Hydrochloride for ocular delivery and investigate their diffusion potential and probability of ocular irritancy. Nanoemulsions were prepared by using the water titration method which was further processed to produce in situ gel. Formulations with optimum gelation temperature were evaluated for their physicochemical characteristics and in vitro drug release. The optimum nanoemulsion in situ gel was selected for investigating its surface morphology, sterility, isotonicity, and ocular irritancy. The optimized formulation had the average droplet size and polydispersity index of 28.29 ±0.14 nm and 0.221 ±0.51, respectively. Furthermore, the physicochemical properties and surface morphology were found to be within the acceptable range for ocular administration. The formulation showed sustained drug release and the % cumulative drug release after 12 hours was found to be 84.59%. The ocular irritancy test revealed that the optimum formulation could be easily tolerated by the eyes. Therefore, these outcomes confirmed that the strategy of using nanoemulsion-based in situ for ophthalmic delivery can be a potential alternative for the treatment of ocular conditions.
A newly developed branded generic of a moxifloxacin (MOX) 400‐mg tablet formulation was manufactured prior to this study. A bioequivalence (BE) study was done to assess the pharmacokinetics of the formulation using a randomized, open‐label, 2‐period crossover, 2‐sequence, and single‐dose experiment. Thirty healthy male volunteers were recruited. The test formulation, Flonoxin 400 mg, was compared with the reference formulation, Avelox 400 mg. The pharmacokinetic parameters of MOX were calculated based on the plasma drug concentration‐time profile. Noncompartmental analysis was performed to determine its safety and tolerability. The 90% confidence intervals (CIs) were 88.5%‐104.6%, 96.1%‐101.1%, and 96.8%‐100.7% for Cmax, AUC0‐t, and AUC0‐inf, respectively. All CIs were within the 80.0%‐125.0% boundary, thus fulfilling the acceptable BE criteria according to the ASEAN guidelines.
Managing infections in immunosuppressed and immunodeficient patients in the pediatric intensive care unit (PICU) setting poses ever-increasing challenges. They are a population already susceptible to viral and fungal infections, in addition to severe bacterial sepsis. Resistant bacterial, viral, and fungal isolates are becoming increasingly common, making the management of these patients even more complex.
Simple, fast, and precise reversed-phase (RP)-high-performance liquid chromatography (HPLC) and two ecofriendly spectrophotometric methods were established and validated for the simultaneous determination of moxifloxacin HCl (MOX) and flavoxate HCl (FLX) in formulations. Chromatographic methods involve the separation of two analytes using an Agilent Zorbax SB C18 HPLC column (150 mm × 4.6 mm; 5 µm) and a mobile phase consisting of phosphate buffer (50 mM; pH 5): methanol: acetonitrile in a proportion of 50:20:30 v/v, respectively. Valsartan was used as an internal standard. Analytes were monitored by measuring the absorbance of elute at 299 nm for MOX and 250 nm for FLX and valsartan. Two environmentally friendly spectrophotometric (first derivative and ratio first derivative) methods were also developed using water as a solvent. For the derivative spectrophotometric determination of MOX and FLX, a zero-crossing technique was adopted. The wavelengths selected for MOX and FLX were −304.0 nm and −331.8 nm for the first derivative spectrophotometric method and 358.4 nm and −334.1 nm for the ratio first-derivative spectrophotometric method, respectively. All methods were successfully validated, as per the International Conference on Harmonization(ICH) guidelines, and all parameters were well within acceptable ranges. The proposed analytical methods were successfully utilized for the simultaneous estimation of MOX and FLX in formulations.
Introduction: The number of elderly people is increasing worldwide. The elderly may be at increased risk of bacterial infections in comparison with younger adults. Dosing adaptation of antibiotics in this population may be difficult due to changes in body composition, decline of renal function and/or drug-drug interactions. Lack of dose adaptation may cause unintentional overdosing with the risk of severe adverse effects.
Areas covered: This review is based on a PubMed search of literature published in English language and concerns pharmacokinetic (PK) studies of antibiotics in the elderly performed between 1971 and 2017.
Expert opinion: Appropriateness of drug prescription in the elderly is a major commitment of the health care systems worldwide. This should push more and more clinicians to adjust the dosage of renally-cleared antibiotics in relation to renal function estimates. The situation may become even more complex in frail elderly patients who are receiving polypharmacy due to drug-drug interactions. Development of new antibiotics should include within clinical trials adequate representation of patients aged ≥75 years to determine age-based dosing. Population PK could be helpful in increasing the knowledge of clinical factors influencing the need for dosing adaptation of the currently available antibiotics in the elderly.
Background/aims:
Moxifloxacin-based sequential therapy showed an excellent eradication rate as the first line treatment of Helicobacter pylori (H. pylori) infection. However, to the best of our knowledge, there were only a few studies on the treatment of those with failed moxifloxacin-based sequential therapy. Hence, this study was to investigate the efficacy of bismuth-containing quadruple therapy in those with failed moxifloxacin-based sequential or reverse sequential therapy for H. pylori eradication.
Methods:
Between January 2013 and March 2016, we retrospectively analyzed patients who failed to eradicate H. pylori using moxifloxacin-based sequential (rabeprazole 20 mg bid and amoxicillin 1 g bid for 5-7 days, followed by rabeprazole 20 mg bid, metronidazole 500 mg bid, and moxifloxacin 400 mg qd for 5-7 days) and 10 days moxifloxacin-based reverse sequential therapy as the first line treatment. Then we investigated the eradication rates of bismuth-containing quadruple therapy as the second line treatment. All subjects had no history of H. pylori eradication before. Eradication rates were described as intention-to-treat (ITT) and per-protocol (PP) analyses. H. pylori status was evaluated by ¹³C-urea breath test 6 weeks after the end of the treatment. Moreover, we examined any side effects that caused discontinuation of therapy.
Results:
Twenty-three patients received bismuth-containing quadruple therapy as the second line treatment. The overall eradication rates by ITT and PP analyses were 60.87% (n=14/23) and 73.68% (n=14/19). All the patients showed good compliance, and there were no serious adverse events.
Conclusions:
Bismuth-containing quadruple therapy is insufficient as the second line eradication treatment after a failed attempt of moxifloxacin-based sequential or reverse sequential therapy. Large-scale clinical trials should be performed to establish better clinical evidence.
Background/aims:
Hybrid therapy was successful in eradicating Helicobacter pylori (H. pylori) according to previous reports. However, to the best of our knowledge, there have only been a few studies evaluating the optimal choice after hybrid failure. Hence, we aimed to evaluate the efficacy of moxifloxacin-containing triple therapy after hybrid therapy failure in H. pylori eradication.
Methods:
Between January 2013 and March 2016, we retrospectively reviewed patients who underwent failed hybrid therapy, as first line treatment, in eradicating H. pylori (rabeprazole and amoxicillin b.i.d for 14 days, in addition to clarithromycin and metronidazole b.i.d for final 7 days). Then, we investigated the eradication rates of moxifloxacin-containing triple therapy (rabeprazole, amoxicillin b.i.d and moxifloxacin qd) as the second line of treatment. Intention-to-treat (ITT) and per-protocol (PP) analyses were used to determine the eradication rate. We evaluated the status of H. pylori by using 13C-urea breath test 6 weeks after the final treatment. Moreover, compliance and adverse effects of each patient were analyzed.
Results:
Among those who failed the initial hybrid therapy, 11 patients received moxifloxacin-containing triple therapy. The overall eradication rates, as determined by ITT and PP, were 72.7% (n=8/11) and 80% (n=8/10), respectively. The compliance rate was 100%, and there were no serious adverse effects.
Conclusions:
Moxifloxacin-containing triple therapy can be used as a second line therapy in case of hybrid therapy failure. A large scale study is necessary to confirm the findings of this study and establish clinical evidence.
Antibacterial drugs is a general term that refers to a group of drugs that includes antibiotics, antifungals, antivirals, and antiprotozoals.
The antimicrobial resistance is an antibiotics inherent problem, which goes hand in hand with their discovery, evolution and clinical use. The quest for new valid targets and the development of new drugs is capital in these days, when the latter antibiotic barrier (vancomycin) has been teared down. Thus, the DNA replication machinery (replisome) gathers lot of characteristics and hopes to be a robust antibacterial target. Five enzymes of the replisome focus the research: (i) topoisomerase type II, (ii) DNA primase, (iii) DNA helicase, (iv) DNA polymerase and (v) DNA ligase. These enzymes, which present characteristics that differentiate the replisome of bacteria from that of virus, archaea or eukaryotes, have been extensively studied in the last decades as antibacterial targets with divergence in outcomes as stated in this chapter.
Traditionally, the PK of different anti-infective drugs is evaluated based on the plasma drug concentrations. However, in some cases those concentrations are not identical to those detected at the target site of the infection, i.e., in the affected tissue. In this context, microdialysis is a valuable technique applied for the quantification of free drug in the interstitial space fluid of a great variety of tissues. Considering that generally the infections are located in interstitial space fluid and only the free drug fraction is able to exert the anti-infective effect, it is clear that this approach has the necessary features to quantify the active fraction at the site of action. Using this information for consecutive pharmacokinetic/pharmacodynamic models is increasingly becoming state-of-the-art for optimizing dosing regimens of antibiotics.
