prulifloxacin / Generic mfg. - LARVOL DELTA

In vitro inhibition effect of various pharmacologically relevant drugs on recombinant paraoxonase 1. (PubMed, Chem Biol Interact) - "Nine pharmacologically relevant compounds exhibited inhibition constants (Ki) ranging from 10 μM to 1000 μM, while prulifloxacin and efavirenz emerged as the most potent competitive inhibitors of rePON1 with Ki values around 1 μM. Thus, these two drugs bind rePON1 approximately 2- to 3-fold more tightly than 2-hydroxyquinoline, which is the most kinetically and structurally characterized competitive inhibitor of rePON1."

Journal • Preclinical • PON1

Structural insight in understanding the impact of mutation at position 88 and 94 of DNA gyrase A of Mycobacterium tuberculosis in developing resistance against delafloxacin. (PubMed, J Biol Phys) - "Based on literature information on drug-resistance related study for DNA gyrase, we generated 4 different mutant models 3ILW_G88A, 3ILW_G88C, 3ILW_D94G, and 3ILW_D94H by inserting two mutations at each position 88 and 94 in DNA gyrase chain A. Antibiotics Clinafloxacin, Gatifloxacin, Moxifloxacin, Sitafloxacin, Prulifloxacin, Besifloxacin, Delafloxacin, Ozenoxacin were docked with 3ILW_wild to understand their stability, binding affinity, and interaction pattern with the wild-type DNA gyrase (3ILW_wild). It is worth noting that mutation at position 94 of DNA gyrase A has a very profound effect as it shows a positive contribution towards increased resistance due to reduced binding affinity with delafloxacin. This study explains the structural changes and mechanism behind the resistance against Delafloxacin, and may also guide the structural changes required in existing Delafloxacin or other antibiotics to develop new therapeutics to overcome the issue of resistance."

Journal • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis

Medoxomil Prodrug Strategies. (PubMed, J Med Chem) - "Among these, medoxomil promoieties have been judiciously employed in multiple drug discovery campaigns, leading to three prodrugs gaining FDA approval: azilsartan medoxomil (6), olmesartan medoxomil (20), and ceftobiprole medocaril (29), and one approval in Japan: prulifloxacin (35). The approach has been used for drugs spanning multiple classes to improve oral bioavailability, solubility, tissue localization, efflux, and side effect profiles. This Perspective analyzes the history and application of medoxomil prodrugs and discusses their potential for drug development."

Journal • Review

Comparison of treatments for preventing lower urinary tract symptoms after BCG immunotherapy of bladder tumors : a systematic review and network meta-analysis. (PubMed, BMC Urol) - "The NMA indicated that medications such as celecoxib, prulifloxacin and phenazopyridine are effective in reducing the incidence of LUTS after BCG immunotherapy of bladder tumors."

Journal • Retrospective data • Bladder Cancer • Genito-urinary Cancer • Gynecology • Musculoskeletal Pain • Oncology • Pain • Solid Tumor

Quantitative study of ternary polycrystalline mixtures of prulifloxacin based on Raman spectra and Raman imaging maps. (PubMed, J Pharm Biomed Anal) - "Subsequently, the ternary mixed crystal samples were analyzed using a Raman microscope.Then run a partial least squares regression analysis to establish a PLS quantitative model using the average spectra data, and a non-negative least squares analysis to establish an area percentage quantitative model using Raman imaging data.The method validation results showed that the two models successfully predicted the proportion of each crystal form within the prulifloxacin polycrystalline mixtures, with a prediction accuracy of less than ± 10 %. Raman spectroscopy was thus established as an effective method for crystal form analysis and quantitative measurement of prulifloxacin."

Journal

A Randomized, Controlled Trial of Prulifloxacin as Conversion Therapy after Intravenous Carbapenem in the Treatment of Acute Pyelonephritis Caused by Third Generation Cephalosporin Resistant Pathogens: A Pilot Study. (PubMed, Clin Transl Sci) - "The objective was to compare the clinical and bacteriological outcome of oral prulifloxacin with intravenous ertapenem for the treatment of APN caused by 3-GCrEC. The converting to oral prulifloxacin after intravenous antibiotics therapy appears to be an alternative option for treatment of APN caused by 3-GCrEC. A further large randomized controlled trial should be investigated."

Journal • Infectious Disease • Nephrology

D-mannose for preventing and treating urinary tract infections. (PubMed, Cochrane Database Syst Rev) - "There is currently little to no evidence to support or refute the use of D-mannose to prevent or treat UTIs in all populations. This review highlights the severe lack of high-quality RCTs testing the efficacy of D-mannose for UTIs in any population. Despite UTIs being one of the most common adult infections (affecting 50% of women at least once in their lifetime) and the growing global antimicrobial resistance, we found very few studies that adequately test this alternative treatment. Future research in this field requires, in the first instance, a single adequately powered RCT comparing D-mannose with placebo."

Journal • Review • Chronic Kidney Disease • CNS Disorders • Infectious Disease • Multiple Sclerosis • Nephrology • Pain • Renal Disease • Transplantation

Comparison of Fluoroquinolones and Other Antibiotic Prophylaxis Regimens for Preventing Complications in Patients Undergoing Transrectal Prostate Biopsy. (PubMed, Antibiotics (Basel)) - "The population was stratified according to the antibiotic prophylaxis adopted: fluoroquinolones (levofloxacin, ciprofloxacin, prulifloxacin), cephalosporins (cefixime, ceftriaxone) or trimethoprim/sulfamethoxazole. The ceftriaxone/fosfomycin (OR 0.21, 95% CI 0.04-0.92, p = 0.04) and fluoroquinolone (OR 0.07, 95% CI 0.00-0.70, p = 0.048) prophylaxis were associated with a lower risk of infective sequelae. Fluoroquinolone-based prophylaxis was associated with a lower risk of infective complications after TRUSBx compared to other prophylaxis regimens although its clinical application was recently forbidden by European Medical Agency restrictions."

Journal • Infectious Disease • Septic Shock

Computational Approach to Combat COVID-19 Infection: Emerging Tool for Accelerating Drug Research. (PubMed, Curr Drug Discov Technol) - "This review is focused on the study of various aspects of these drugs related to their target sites on virus, binding interactions, physicochemical properties etc."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Repurposing Sitafloxacin, Prulifloxacin, Tosufloxacin, and Sisomicin as Antimicrobials Against Biofilm and Persister Cells of Pseudomonas aeruginosa. (PubMed, Curr Microbiol) - "Tosufloxacin exhibited the greatest in vivo bactericidal activity against P. aeruginosa biofilms with a reduction of 4.54 ΔLog10 CFU/mL compared to the vehicle group, followed by prulifloxacin, sitafloxacin, and sisomicin. Taken together, our results indicate that sitafloxacin, prulifloxacin, tosufloxacin, and sisomicin have great potential as alternatives for the treatment of refractory infections caused by P. aeruginosa biofilms and persister cells."

Journal • Infectious Disease

Phenotypic and genotypic characterization of antimicrobial resistance in clinical isolates of Vibrio cholerae over a decade (2002-2016). (PubMed, Indian J Med Microbiol) - "Our study has shown very high levels of resistance to older antibiotics and the emergence of resistance to some of the newer classes of antibiotics. There is an urgent need for increased surveillance studies, rational use of the antimicrobials and preventive measures to control the disease."

Clinical • Journal • Cholera

Determination of thiourea by terbium (III)/ prulifloxacin sensitized potassium permanganate-sulfite chemiluminescence with quenching method. (PubMed, Spectrochim Acta A Mol Biomol Spectrosc) - "The method was applied satisfactorily to the determination of thiourea in tap water, lake water and rice noodles and the spiked recoveries were between 104.7 ~ 113.4%. The possible mechanism of sensitization and quenching was also proposed."

Journal

Spatiotemporal profiling of antibiotics and resistance genes in a river catchment: Human population as the main driver of antibiotic and antibiotic resistance gene presence in the environment. (PubMed, Water Res) - "All antibiotics, apart from four fluroquinolones (besifloxacin, lomefloxacin, ulifloxacin, prulifloxacin), were detected within all influent wastewater from the 5 cities (1 city = 1 WWTP), as were the corresponding antibiotic resistance genes (ARGs). The efficiency of ABs and ARGs removal by the WWTPs varied according to site (and treatment process utilized) and target, although strong correlations were maintained between the population size served by WWTPs and daily loads of discharged ABs and ARGs into the environment. We therefore conclude that population size is the main determinant of the magnitude of AB and ARG burden in the environment."

Clinical • Journal • Immunology

Prulifloxacin Effectiveness in Moderate-to-Severe Acute Exacerbations of Chronic Bronchitis: Α Noninterventional, Multicentre, Prospective Study in Real-Life Clinical Practice-The "AIOLOS" Study. (PubMed, Can Respir J) - "The rate of adverse events related to prulifloxacin was 1.3% (serious: 0.7%). In the routine care in Greece, prulifloxacin was highly effective in moderate-to-severe AECB, while displaying a predictable safety profile."

Clinical • Journal • Chronic Obstructive Pulmonary Disease • Pulmonary Disease • Respiratory Diseases

Prulifloxacin in Chronic Bacterial Prostatitis (CBP) (clinicaltrials.gov) - P2; N=168; Completed; Sponsor: Aziende Chimiche Riunite Angelini Francesco S.p.A; Active, not recruiting ➔ Completed

Clinical • Trial completion • Infectious Disease

Drug Repurposing Strategy (DRS): Emerging Approach to Identify Potential Therapeutics for Treatment of Novel Coronavirus Infection. (PubMed, Front Mol Biosci) - "The methodologies involved in drug repurposing can be categorized into three groups such as drug-oriented, target-oriented and disease or therapy-oriented depending on the information available related to quality and quantity of the physico-chemical, biological, pharmacological, toxicological and pharmacokinetic property of drug molecules. This review focuses on drug repurposing strategy applied for existing drugs including Remdesivir, Favipiravir, Ribavirin, Baraticinib, Tocilizumab, Chloroquine, Hydroxychloroquine, Prulifloxacin, Carfilzomib, Bictegravir, Nelfinavir, Tegobuvir and Glucocorticoids etc to determine their effectiveness toward the treatment of COVID-19."

Journal • Review • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Cefixime versus prulifloxacin as a prophylactic treatment for prostate biopsy: a randomized study. (PubMed, Cent European J Urol) - "Among the remaining 117 patients (97.5%), nobody presented with a UTI. Prophylactic cefixime could be suggested as effective in preventing severe UTIs after prostate biopsy in the era of high bacterial resistance to fluoroquinolones."

Clinical • Journal • Allergy • Immunology • Infectious Disease • Nephrology • Renal Disease

A systematic review of preventive and therapeutic options for symptoms of cystitis in patients with bladder cancer receiving intravesical bacillus Calmette-Guérin immunotherapy. (PubMed, Anticancer Drugs) - "Potentially effective options to prevent symptoms of cystitis are BCG dose reduction, intravesical hyaluronic acid instillations and oral prulifloxacin or ofloxacin administration...Studies on directed medical interventions did not consider the influence on the BCG efficacy. Among few proposed preventive or therapeutic options for symptoms of cystitis related to BCG, none was proven to be both definitively effective and oncologically safe."

Clinical • Journal • Review • Bladder Cancer • Oncology • Pain • Solid Tumor • Urothelial Cancer

(Fluoro)quinolones and quinolone resistance genes in the aquatic environment: A river catchment perspective. (PubMed, Water Res) - "Ofloxacin, ciprofloxacin, nalidixic acid and norfloxacin were found to be ubiquitous with daily loads reaching a few hundred g/day in wastewater influent and tens of g/day in receiving waters. This was in contrast to other FQs analysed: flumequine, nadifloxacin, lomefloxacin, ulifloxacin, prulifloxacin, besifloxacin and moxifloxacin, which were hardly quantified...Wastewater-based epidemiology (WBE) was also applied to monitor any potential misuse (e.g. direct disposal) of FQs in the catchment. In most cases higher use of antibiotics with respect to official statistics (i.e. ciprofloxacin, ofloxacin) was observed, which suggests that FQs management practice require further attention."

Journal • Complement-mediated Rare Disorders

[VIRTUAL] Comparative in vitro activity of fluoroquinolones against P. aeruginosa isolated from Greek CF patients (ERS 2020) - "Prulifloxacin, the pro-drug of ulifloxacin, has reported to show high anti-pseudomonal in vitro potency but there are few available data in CF patients. Aim : To compare the in vitro activity of ulifloxacin (ULI), ciprofloxacin (CIP) and levofloxacin (LEV) against P.aeruginosa strains in a Greek CF population...Conclusion : ULI showed similar but not higher in vitro potency than CIP while LEV demonstrated the lowest against the isolates studied. These results do not necessarily reflect in vivo efficacy."

Cystic Fibrosis • Fibrosis • Genetic Disorders • Immunology • Respiratory Diseases

[VIRTUAL] Transrectal ultrasound prostate biopsies - if not fluoroquinolone, what else? (EAU-I 2020) - "The most used antibiotics were FQ (ciprofloxacin in 43,01%; prulifloxacin in 23,42%; levofloxacin in 14,51%; norfloxacin in 6,22%). The indiscriminate use of antimicrobial agents has favored a rise in the prevalence of antibiotic resistance and subsequent complications associated-rate. So, the health authorities have proposed a careful adaptation of these agents to the local pattern of resistances and promoted the restrictive use of FQ for prophylaxis in prostate biopsies. However, the post-biopsy infectious complication rate at our hospital is similar to other reports in the medical community and no post-biopsy multidrug resistant UTI was diagnosed in 2017."

Diabetes • Infectious Disease • Metabolic Disorders • Nephrology • Oncology • Pneumonia • Respiratory Diseases • Septic Shock

Prulifloxacin effectiveness in acute excerbation of chronic bronchitis: a post-marketing non-interventional study (ECCMID 2019) - "Results from this study are in agreement with previous studies of prulifloxacin in patients with AECB confirming the effectiveness and safety of prulifloxacin in daily routine treatment of moderate-to-severe AECB, with a potential advantage in patients with COPD, due to its good safety profile for cardiac events. Improvements in QOL assessments and work activities definitely confirmed the value of the use of the adequate treatment for the management of these patients. Physicians complied with the SPC recommended dosage and 98.3% of the effectiveness population assumed the study treatment according to medical prescription."

Clinical • Observational data • P4 data • Chronic Obstructive Pulmonary Disease • Gastroenterology • Gastrointestinal Disorder • Respiratory Diseases

Quantification of fluoroquinolones in wastewaters by liquid chromatography-tandem mass spectrometry. (PubMed, Environ Pollut) - "This work presents a validated analytical method based on solid phase extraction (SPE) using HLB cartridges, followed by liquid chromatography-tandem mass spectrometry (LC-MS/MS) for quantification of seven different fluoroquinolone antibiotics, namely ciprofloxacin (CPF), enrofloxacin (ENR), lomefloxacin (LOM), norfloxacin (NOR), ofloxacin (OFL), prulifloxacin (PLF) and moxifloxacin (MOX) and its application to detect the target compounds in influents and effluents of wastewater treatment plants (WWTP). OFL was the fluoroquinolone found at the highest concentration, up to 4587.0 ng L and 987.9 ng L, in influent and effluent, respectively. NOR and PLF were not detected."

Journal

Enantiomeric profiling of quinolones and quinolones resistance gene qnrS in European wastewaters. (PubMed, Water Res) - "Nalidixic acid, norfloxacin and lomefloxacin were detected in wastewater even though they were not prescribed according to official prescription data. S,S-(-)-moxifloxacin and S,S-(-)-moxifloxacin-N-sulphate were detected in wastewater due to metabolism of moxifloxacin. For the first time, average population-normalised ulifloxacin loads of 22.3 and 1.5 mg day 1000 people were reported for Milan and Castellón as a result of prulifloxacin metabolism...Utrecht, with the lowest quinolones usage (low daily loads) had also one of the lowest daily loads of the qnrS gene. However, a similar trend was not observed in Oslo nor Bristol where higher qnrS gene loads were observed despite low quinolone usage."

Journal

Ototoxic Adverse Drug Reactions: A Disproportionality Analysis Using the Italian Spontaneous Reporting Database. (PubMed, Front Pharmacol) - "Statistically significant adjusted RORs were found for drugs for cardiovascular disorders, urologicals, teriparatide, amikacin, prulifloxacin, rifampicin and isoniazid, cisplatin, hormone antagonists, tacrolimus, pomalidomide, tramadol, and antidepressants. Significant adjusted RORs in relation to tinnitus were also observed for doxazosin (ROR 5.55, 95% CI 2.06-14.93), bisoprolol (4.28, 1.59-11.53), nebivolol (8.06, 3.32-19.56), ramipril (3.96, 2.17-7.23), irbesartan (19.60, 9.19-41.80), betamethasone (4.01, 1.28-12.52), moxifloxacin (4.56, 1.71-12.34), ethambutol (12.25, 3.89-38.57), efavirenz (16.82, 5.34-52.96), sofosbuvir/ledipasvir (5.95, 1.90-18.61), etoposide (7.09, 2.63-19.12), abatacept (6.51, 2.42-17.53), indometacin (6.30, 2.02-19.72), etoricoxib (5.00, 2.23-11.23), tapentadol (4.37, 1.09-17.62), and timolol combinations (23.29, 9.53-56.95). Moreover, significant adjusted RORs for hypoacusis regarded clarithromycin (3.95, 1.86-8.40), azithromycin (10.23,..."

Adverse drug reaction • Journal