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Frontiers in Public Health 2022For around three decades, the fluoroquinolone (FQ) antibiotic ciprofloxacin has been used to treat a range of diseases, including chronic otorrhea, endocarditis, lower... (Review)
Review
For around three decades, the fluoroquinolone (FQ) antibiotic ciprofloxacin has been used to treat a range of diseases, including chronic otorrhea, endocarditis, lower respiratory tract, gastrointestinal, skin and soft tissue, and urinary tract infections. Ciprofloxacin's main mode of action is to stop DNA replication by blocking the A subunit of DNA gyrase and having an extra impact on the substances in cell walls. Available in intravenous and oral formulations, ciprofloxacin reaches therapeutic concentrations in the majority of tissues and bodily fluids with a low possibility for side effects. Despite the outstanding qualities of this antibiotic, , and have all shown an increase in ciprofloxacin resistance over time. The rise of infections that are resistant to ciprofloxacin shows that new pharmacological synergisms and derivatives are required. To this end, ciprofloxacin may be more effective against the biofilm community of microorganisms and multi-drug resistant isolates when combined with a variety of antibacterial agents, such as antibiotics from various classes, nanoparticles, natural products, bacteriophages, and photodynamic therapy. This review focuses on the resistance mechanisms of bacteria against ciprofloxacin and new approaches for enhancing its efficacy.
Topics: Anti-Bacterial Agents; Ciprofloxacin; Bacteria; Fluoroquinolones
PubMed: 36620240
DOI: 10.3389/fpubh.2022.1025633 -
PloS One 2023Infectious diseases caused by bacteria that have become resistant to antibiotics have increased in prevalence, necessitating new methods for their diagnosis and...
Infectious diseases caused by bacteria that have become resistant to antibiotics have increased in prevalence, necessitating new methods for their diagnosis and treatment. The aim of this study was to compare the efficacy of synthetic ciprofloxacin to that of organic ciprofloxacin produced by cave microorganisms, as well as to evaluate the feasibility of using organic ciprofloxacin radiolabeled with technetium-99m as an imaging agent. Organic ciprofloxacin produced by cave bacteria isolated from sediment taken from the dark zone of Antalya's "Yark Sinkhole," (Turkey's 14th deepest cave), was purified using high-performance liquid chromatography. Purified organic ciprofloxacin and standard ciprofloxacin were radiolabeled with technetium-99m (99mTc), and their uptake by pathogenic microorganisms as well as potential as an imaging agent were examined. According to thin-layer radiochromatography, radiolabeling efficiencies were 98.99 ± 0.34 (n = 7) and 91.25 ± 1.84 (n = 7) for radiolabeled organic ciprofloxacin and standard ciprofloxacin respectively. The binding efficiency of radiolabeled organic ciprofloxacin at the 240th minute was higher compared with radiolabeled standard ciprofloxacin, especially with P.aeruginosa, MRSA, VRE and E.coli. The results demonstrate that radiolabeling with 99mTc does not alter the biological behavior of organic ciprofloxacin, and radiolabeled organic ciprofloxacin has potential as an imaging agent for the detection of bacterial infection. The original value of the study is the monitoring of the antibiofilm effects of untouched cave-derived organic antibiotics by radiolabeling with a radionuclide.
Topics: Ciprofloxacin; Technetium; Radiopharmaceuticals; Radionuclide Imaging; Anti-Bacterial Agents; Escherichia coli
PubMed: 37943851
DOI: 10.1371/journal.pone.0291342 -
Molecules (Basel, Switzerland) Mar 2020Infections caused by bacteria resistant to antibiotics are an increasing problem. Multivalent antibiotics could be a solution. In the present study, a covalent conjugate...
Infections caused by bacteria resistant to antibiotics are an increasing problem. Multivalent antibiotics could be a solution. In the present study, a covalent conjugate between Ciprofloxacin and a G0-PAMAM dendrimer has been synthesized and tested against clinically relevant Gram-positive and Gram-negative bacteria. The conjugate has antimicrobial activity and there is a positive dendritic effect compared to Ciprofloxacin itself.
Topics: Anti-Infective Agents; Ciprofloxacin; Dendrimers; Gram-Negative Bacteria; Gram-Positive Bacteria
PubMed: 32197523
DOI: 10.3390/molecules25061389 -
Current Opinion in Infectious Diseases Oct 2023The emergence of globally resistant enteric Shigella and nontyphoidal Salmonella strains (NTS) has limited the selection of effective drugs, which has become a major... (Review)
Review
PURPOSE OF REVIEW
The emergence of globally resistant enteric Shigella and nontyphoidal Salmonella strains (NTS) has limited the selection of effective drugs, which has become a major challenge for the treatment of infections. The purpose of this review is to provide the current opinion on the antimicrobial-resistant enteric Shigella and nontyphoidal Salmonella .
RECENT FINDINGS
Enteric Shigella and NTS are resistant to almost all classes of antimicrobials in recent years. Those with co-resistance to ciprofloxacin, azithromycin and ceftriaxone, the first-line antibiotics for the treatment of infectious diarrhoea have emerged worldwide. Some of them have caused interregional and international spread by travel, trade, MSM, and polluted water sources. Several strains have even developed resistance to colistin, the last-resort antibiotic used for treatment of multidrug-resistant Gram-negative bacteria infections.
SUMMARY
The drug resistance of enteric Shigella and NTS is largely driven by the use of antibiotics and horizontal gene transfer of mobile genetic elements. These two species show various drug resistance patterns in different regions and serotypes. Hence treatment decisions for Shigella and Salmonella infections need to take into consideration prevalent antimicrobial drug resistance patterns. It is worth noting that the resistance genes such as blaCTX,mph, ermB , qnr and mcr , which can cause resistance to ciprofloxacin, cephalosporin, azithromycin and colistin are widespread because of transmission by IncFII, IncI1, IncI2 and IncB/O/K/Z plasmids. Therefore, continuous global monitoring of resistance in Shigella and Salmonella is imperative.
Topics: Humans; Azithromycin; Colistin; Shigella; Salmonella; Anti-Bacterial Agents; Ciprofloxacin
PubMed: 37594001
DOI: 10.1097/QCO.0000000000000960 -
Molecular Diversity Aug 2023A series of N-4 piperazinyl ciprofloxacin derivatives as urea-tethered ciprofloxacin-chalcone hybrids 2a-j and thioacetyl-linked ciprofloxacin-pyrimidine hybrids 5a-i...
A series of N-4 piperazinyl ciprofloxacin derivatives as urea-tethered ciprofloxacin-chalcone hybrids 2a-j and thioacetyl-linked ciprofloxacin-pyrimidine hybrids 5a-i were synthesized. The target compounds were investigated for their antibacterial activity against S. aureus, P. aeruginosa, E. coli, and C. albicans strains, respectively. Ciprofloxacin derivatives 2a-j and 5a-i revealed broad antibacterial activity against either Gram positive or Gram negative strains, with MIC range of 0.06-42.23 µg/mL compared to ciprofloxacin with an MIC range of 0.15-3.25 µg/mL. Among the tested compounds, hybrids 2b, 2c, 5a, 5b, 5h, and 5i exhibited remarkable antibacterial activity with MIC range of 0.06-1.53 µg/mL against the tested bacterial strains. On the other hand, compounds 2c, 2e, 5c, and 5e showed comparable antifungal activity to ketoconazole against candida albicans with MIC range of 2.03-3.89 µg/mL and 2.6 µg/mL, respectively. Further investigations showed that some ciprofloxacin hybrids have inhibitory activity against DNA gyrase as potential molecular target compared to ciprofloxacin with IC range of 0.231 ± 0.01-7.592 ± 0.40 µM and 0.323 ± 0.02 µM, respectively. Docking studies of compounds 2b, 2c, 5b, 5c, 5e, 5h, and 5i on the active site of DNA gyrase (PDB: 2XCT) confirmed their ability to form stable complex with the target enzyme like that of ciprofloxacin.
Topics: Ciprofloxacin; Topoisomerase II Inhibitors; Molecular Docking Simulation; DNA Gyrase; Escherichia coli; Staphylococcus aureus; Anti-Infective Agents; Anti-Bacterial Agents; Microbial Sensitivity Tests; Structure-Activity Relationship; Molecular Structure
PubMed: 36152132
DOI: 10.1007/s11030-022-10528-z -
Clinical Pharmacokinetics Aug 2022Ciprofloxacin is a fluoroquinolone used for empirical and targeted therapy of a wide range of infections. Despite the increase in obesity prevalence, only very limited...
BACKGROUND AND OBJECTIVE
Ciprofloxacin is a fluoroquinolone used for empirical and targeted therapy of a wide range of infections. Despite the increase in obesity prevalence, only very limited guidance is available on whether the ciprofloxacin dose needs to be adjusted when administered orally or intravenously in (morbidly) obese individuals. Our aim was to evaluate the influence of (morbid) obesity on ciprofloxacin pharmacokinetics after both oral and intravenous administration, to ultimately guide dosing in this population.
METHODS
(Morbidly) obese individuals undergoing bariatric surgery received ciprofloxacin either orally (500 mg; n = 10) or intravenously (400 mg; n = 10), while non-obese participants received semi-simultaneous oral dosing of 500 mg followed by intravenous dosing of 400 mg 3 h later (n = 8). All participants underwent rich sampling (11-17 samples) for 12 h after administration. Non-linear mixed-effects modelling and simulations were performed to evaluate ciprofloxacin exposure in plasma. Prior data from the literature were subsequently included in the model to explore exposure in soft tissue in obese and non-obese patients.
RESULTS
Overall, 28 participants with body weights ranging from 57 to 212 kg were recruited. No significant influence of body weight on bioavailability, clearance or volume of distribution was identified (all p > 0.01). Soft tissue concentrations were predicted to be lower in obese individuals despite similar plasma concentrations compared with non-obese individuals.
CONCLUSION
Based on plasma pharmacokinetics, we found no evidence of the influence of obesity on ciprofloxacin pharmacokinetic parameters; therefore, ciprofloxacin dosages do not need to be increased routinely in obese individuals. In the treatment of infections in tissue where impaired ciprofloxacin penetration is anticipated, higher dosages may be required.
TRIAL REGISTRATION
Registered in the Dutch Trial Registry (NTR6058).
Topics: Administration, Intravenous; Ciprofloxacin; Humans; Infusions, Intravenous; Obesity, Morbid; Prospective Studies
PubMed: 35641862
DOI: 10.1007/s40262-022-01130-5 -
Annals of Palliative Medicine Sep 2021The efficacy of levofloxacin and ciprofloxacin in the treatment of urinary tract infection is not clear yet. This study perform a meta-analysis to explore the... (Meta-Analysis)
Meta-Analysis
BACKGROUND
The efficacy of levofloxacin and ciprofloxacin in the treatment of urinary tract infection is not clear yet. This study perform a meta-analysis to explore the differences between the two against urinary tract infection (UTI).
METHODS
A computerized literature search was conducted of the databases of PubMed, Medline, Embase, and the Cochrane Library. All the retrieved literatures were randomized comparative studies of levofloxacin and ciprofloxacin. The included studies were screened according to the standard of nanofiltration. The risk of bias was assessed with RevMan 5.3.5 software. The treatment effect index and incidence of adverse reactions index were established and compared via meta-analysis.
RESULTS
A total of 5 studies were included, involving 2,877 patients overall. The results showed that levofloxacin was more effective than ciprofloxacin, but the difference between the 2 drugs was not statistically significant [odds ratio (OR) =1.18, 95% confidence interval (CI): 0.94 to 1.46, P=0.15]. There was also no statistical significance in the rate of adverse reactions between the 2 drugs (OR =0.91, 95% CI: 0.78 to 1.07, P=0.27).
DISCUSSION
In the treatment of UTI, the efficacy and safety of levofloxacin and ciprofloxacin are similar statistically. If bacterial resistance is discovered after the treatment of one of the drugs, the other drug might become an alternative.
Topics: Ciprofloxacin; Humans; Levofloxacin; Urinary Tract Infections
PubMed: 34628902
DOI: 10.21037/apm-21-2042 -
Chemical Biology & Drug Design Jun 2021Several rationally designed isoniazid (INH), pyrazinamide (PZA) and ciprofloxacin (CPF) derivatives were conveniently synthesized and evaluated in vitro against H37Rv...
Several rationally designed isoniazid (INH), pyrazinamide (PZA) and ciprofloxacin (CPF) derivatives were conveniently synthesized and evaluated in vitro against H37Rv Mycobacterium tuberculosis (M. tb) strain. CPF derivative 16 displayed a modest activity (MIC = 16 µg/ml) and was docked into the M. tb DNA gyrase. Isoniazid-pyrazinoic acid (INH-POA) hybrid 21a showed the highest potency in our study (MIC = 2 µg/ml). It also retained its high activity against the other tested M. tb drug-sensitive strain (DS) V4207 (MIC = 4 µg/ml) and demonstrated negligible cytotoxicity against Vero cells (IC ≥ 64 µg/ml). Four tested drug-resistant (DR) M. tb strains were refractory to 21a, similar to INH, whilst being sensitive to CPF. Compound 21a was also inactive against two non-tuberculous mycobacterial (NTM) strains, suggesting its selective activity against M. tb. The noteworthy activity of 21a against DS strains and its low cytotoxicity highlight its potential to treat DS M. tb.
Topics: Animals; Antitubercular Agents; Binding Sites; Catalytic Domain; Cell Survival; Chlorocebus aethiops; Ciprofloxacin; DNA Gyrase; Drug Design; Drug Resistance, Bacterial; Isoniazid; Microbial Sensitivity Tests; Molecular Conformation; Molecular Docking Simulation; Mycobacterium tuberculosis; Nontuberculous Mycobacteria; Pyrazinamide; Structure-Activity Relationship; Vero Cells
PubMed: 33638304
DOI: 10.1111/cbdd.13836 -
British Journal of Clinical Pharmacology Feb 2018Ciprofloxacin and fluconazole combination therapy is frequently used as prophylaxis for, and treatment of, infections in patients with haematological malignancies.... (Observational Study)
Observational Study
AIM(S)
Ciprofloxacin and fluconazole combination therapy is frequently used as prophylaxis for, and treatment of, infections in patients with haematological malignancies. However, both drugs are known to prolong the heart rate-corrected QT (QTc) interval, which is a serious risk factor for torsade de pointes (TdP). Therefore, the aim of the current study was to assess the prevalence of QTc prolongation during ciprofloxacin and fluconazole use. The secondary objective was to determine associated risk factors of QTc prolongation in these patients.
METHODS
A prospective observational study was performed in patients admitted to the Erasmus University Medical Centre and treated with ciprofloxacin and fluconazole. A 12-lead electrocardiogram (ECG) was recorded at the estimated time to peak concentration (T ) for the last added drug. The main outcome was the proportion of patients with QTc prolongation during treatment. Data on the following potential risk factors were collected: patient characteristics, serum electrolyte levels, dosage of ciprofloxacin and fluconazole, renal and liver function and concomitant use of other QTc-prolonging drugs and cytochrome P450 3A4 inhibitors.
RESULTS
A total of 170 patients were included, of whom 149 (87.6%) were treated for haematological malignancies. The prevalence of QTc prolongation was 4.7%. No risk factors were found to be associated with QTc prolongation. The QTc interval increased by 10.7 ms [95% confidence interval (CI) 7.2, 14.1 ms] during ciprofloxacin and fluconazole combination therapy.
CONCLUSION
The prevalence of QTc prolongation in patients using ciprofloxacin and fluconazole is low compared with the prevalence in the general population, which varies from 5% to 11%. In addition, no risk factors were found. Given the low prevalence, routine ECG monitoring in patients on this therapy should be reconsidered.
Topics: Ciprofloxacin; Drug Therapy, Combination; Electrocardiography; Female; Fluconazole; Heart Rate; Humans; Long QT Syndrome; Male; Middle Aged; Monitoring, Physiologic; Prevalence; Prospective Studies; Risk Factors
PubMed: 29057492
DOI: 10.1111/bcp.13457 -
Canadian Family Physician Medecin de... Apr 2015My patient has a urinary tract infection and is currently breastfeeding her 9-week-old son. I would like to prescribe her ciprofloxacin. Should I be concerned about... (Review)
Review
QUESTION
My patient has a urinary tract infection and is currently breastfeeding her 9-week-old son. I would like to prescribe her ciprofloxacin. Should I be concerned about osteoarticular toxicity in the infant?
ANSWER
Although there are concerns about the possible risk of osteoarticular toxicity with ciprofloxacin, the amounts excreted into breast milk are low and studies report no substantial increase in osteoarticular toxicity even with the systemic use of ciprofloxacin in neonates and children. Therefore, interrupting breastfeeding during ciprofloxacin treatment appears unnecessary.
Topics: Adult; Animals; Bone Development; Breast Feeding; Child Development; Ciprofloxacin; Female; Fluoroquinolones; Humans; Infant; Infant, Newborn; Lactation; Male; Milk, Human; Pregnancy; Urinary Tract Infections
PubMed: 26052598
DOI: No ID Found