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Antibiotics (Basel, Switzerland) Dec 2022In this study, we report the performance improvement of wound dressings by covering them with magnetite-based nanostructured coatings. The magnetite nanoparticles (FeO...
In this study, we report the performance improvement of wound dressings by covering them with magnetite-based nanostructured coatings. The magnetite nanoparticles (FeO NPs) were functionalized with () powder/essential oil and dicloxacillin and were synthesized as coatings by matrix assisted pulsed laser evaporation (MAPLE). The expected effects of this combination of materials are: (i) to reduce microbial contamination, and (ii) to promote rapid wound healing. The crystalline nature of FeO NPs and coatings was determined by X-ray diffraction (XRD). Differential Scanning Calorimetry (DSC) and Thermo Gravimetric Analysis (TGA) have been coupled to investigate the stability and thermal degradation of nanoparticle components. The coatings' morphology was examined by scanning electron microscopy (SEM). The distribution of chemical elements and functional groups in the resulting coatings was evidenced by Fourier transform infrared (FTIR) spectrometry. In order to simulate the interaction between wound dressings and epithelial tissues and to evaluate the drug release in time, the samples were immersed in simulated body fluid (SBF) and investigated after different durations of time. The antimicrobial effect was evaluated in planktonic (free-floating) and attached (biofilms) bacteria models. The biocompatibility and regenerative properties of the nanostructured coatings were evaluated , at cellular, biochemical, and the molecular level. The obtained results show that magnetite-based nanostructured coatings functionalized with and dicloxacillin are biocompatible and show an enhanced antimicrobial effect against Gram positive and Gram negative opportunistic bacteria.
PubMed: 36671260
DOI: 10.3390/antibiotics12010059 -
Drug Design, Development and Therapy 2015Dicloxacillin, a semisynthetic isoxazolyl penicillin antibiotic, has antimicrobial activity against a wide variety of gram-positive bacteria including Staphylococcus... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Dicloxacillin, a semisynthetic isoxazolyl penicillin antibiotic, has antimicrobial activity against a wide variety of gram-positive bacteria including Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumonia, Streptococcus epidermidis, Streptococcus viridans, Streptococcus agalactiae, and Neisseria meningitidis. The objective of this study was to evaluate the safety and pharmacokinetic profile of dicloxacillin after single and multiple oral dose in healthy Chinese volunteers.
METHODS
A single-center, open-label, randomized, two-phase study was conducted in 16 subjects. In the single-dose phase, subjects were randomly assigned to receive single doses of 0.25, 0.5, 1.0, and 2.0 g of dicloxacillin sodium capsule in a 4-way crossover design with a 5-day washout period between administrations. In the multiple-dose phase, subjects were assigned to receive 0.25 or 0.5 g every 6 hours for 3 days in a 2-way crossover design. Plasma and urine pharmacokinetic samples were assayed by a validated high-performance liquid chromatography-tandem mass spectrometry method. Pharmacokinetic parameters were calculated and analyzed statistically. Safety assessments were conducted throughout the study.
RESULTS
Following a single oral dose of 0.25-2.0 g dicloxacillin sodium, the maximum plasma drug concentration (Cmax) and the corresponding values for the area under the concentration- time curve from 0 to 10 hours (AUC0-10 h) increased in a dose-proportional manner. The mean elimination half-life (t1/2) was in the range of 1.38-1.71 hours. Dicloxacillin was excreted in its unchanged form via the kidney, with no tendency of accumulation, and varied from 38.65% to 50.10%. No appreciable accumulation of drug occurred with multiple oral doses of dicloxacillin. No serious adverse events were reported. Adverse events were generally mild.
CONCLUSION
Dicloxacillin was safe and well tolerated in the volunteers and displayed linear increases in the Cmax and AUC0-10 h values.
Topics: Administration, Oral; Adolescent; Adult; Anti-Bacterial Agents; Area Under Curve; Asian People; China; Chromatography, High Pressure Liquid; Cross-Over Studies; Dicloxacillin; Drug Administration Schedule; Female; Half-Life; Healthy Volunteers; Humans; Linear Models; Male; Metabolic Clearance Rate; Middle Aged; Models, Biological; Renal Elimination; Tandem Mass Spectrometry; Young Adult
PubMed: 26527863
DOI: 10.2147/DDDT.S92117 -
F1000Research 2021Worldwide, chicken meat is widely consumed due to its low cost, high nutritional value and non-interference with religious or cultural beliefs. However, during animal...
Worldwide, chicken meat is widely consumed due to its low cost, high nutritional value and non-interference with religious or cultural beliefs. However, during animal husbandry chickens are exposed to many chemical substances, including tetracyclines and β-lactams, which are used to prevent and cure several infections. Some residues of these compounds may bioaccumulate and be present in chicken meat after slaughtering, promoting oxidative reactions. In order to evaluate carbonylation induced by tetracyclines and β-lactams residues, a proteomic approach was used. For this, chicken muscle was individually contaminated with tetracyclines (tetracycline, chlortetracycline, oxytetracycline, and doxycycline) and β-lactams (ampicillin, benzathine penicillin, dicloxacillin and oxacillin) at 0.5, 1.0 and 1.5 times their maximum residue level (MRL). Then, sarcoplasmic, myofibrillar and insoluble proteins were extracted and their content were measured using the Bradford method. Protein carbonylation was measured using the 2,4-Dinitrophenylhydrazine alkaline method. Residues of tetracyclines and β-lactams induced carbonylation on sarcoplasmic, myofibrillar and insoluble proteins even at 0.5MRL concentrations ( ). When comparing the carbonylation induced by both antibiotics no differences were found ( ). Variables such as the partition coefficient (log P) and the concentration of these antibiotics showed a high correlation with the oxidative capacity of tetracyclines and β-lactams on chicken breast proteins. : This study shows that the presence of tetracyclines and β-lactams residues at MRLs concentrations promotes carbonylation on chicken breast proteins. Our results provide important insights about the impact of antibiotics on the integrity of meat proteins intended for human consumption.
Topics: Animals; Anti-Bacterial Agents; Chickens; Drug Residues; Food Contamination; Meat; Proteomics; Tetracyclines; beta-Lactams
PubMed: 35316938
DOI: 10.12688/f1000research.53863.1 -
Basic & Clinical Pharmacology &... Sep 2018The antibiotic dicloxacillin has been shown to induce drug-metabolizing CYP enzymes to a clinically relevant extent. In this study, we investigated whether the use of...
The antibiotic dicloxacillin has been shown to induce drug-metabolizing CYP enzymes to a clinically relevant extent. In this study, we investigated whether the use of dicloxacillin confers an increased risk of unwanted pregnancy among oral contraceptive users. The study population comprised Danish women falling pregnant (1997-2015) during oral contraceptive use, defined as having filled a prescription for an oral contraceptive within 120 days both before and after the estimated date of conception. Data were analysed using a case-crossover approach. For each woman, we assessed the use of dicloxacillin preceding the date of conception and during 10 previous control periods and estimated the odds ratio for such unintended pregnancies associated with the use of dicloxacillin. Among 364 women using dicloxacillin prior to conception, 40 (11%) were exposed to dicloxacillin at the time of conception, yielding an odds ratio (OR) associating use of dicloxacillin to unintended pregnancy of 1.18 (95% CI 0.84-1.65). Supplementary and sensitivity analyses generally returned similar estimates, except for a slightly increased risk among users of progestogen-only oral contraceptives (OR 1.83, 95% CI 0.63-5.34). Analysis of other antibiotics as negative controls yielded results close to unity (ORs ranging from 0.83 to 1.13). In conclusion, our study found no evidence for an increased risk of oral contraceptive failure when using dicloxacillin. However, acknowledging study limitations, we suggest the use of supplementary barrier methods during treatment with dicloxacillin, until our findings are confirmed in further studies.
Topics: Adult; Anti-Bacterial Agents; Contraceptives, Oral; Cross-Over Studies; Denmark; Dicloxacillin; Drug Interactions; Female; Humans; Pregnancy; Pregnancy, Unplanned; Pregnancy, Unwanted; Risk; Young Adult
PubMed: 29504695
DOI: 10.1111/bcpt.13000 -
Pathogens (Basel, Switzerland) Oct 2022The objectives of the work were (a) to compare the efficacy of two routes for antibiotic administration in the treatment of mastitis in ewes and (b) to assess the...
The objectives of the work were (a) to compare the efficacy of two routes for antibiotic administration in the treatment of mastitis in ewes and (b) to assess the potential importance of the timing of the initiation of the therapeutic regime on the outcome of the treatment. The ewes were allocated at random into three equal groups; intramammary inoculation with a isolate was performed, and clinical mastitis developed. The ewes in groups T1 ( = 6) and T2 ( = 6) were treated by the intramammary administration of ampicillin and dicloxacillin (two administrations with a 12-h interval). The ewes in group T3 ( = 6) were treated by the intramuscular injection of ampicillin and dicloxacillin (0.75 mL per 10 kg bodyweight, three injections with a 24-h interval). In the ewes in groups T1 and T3, treatment started immediately when the clinical signs of mastitis were first detected during the periodic examination of the ewes; in the ewes in group T2, treatment started 24 h after the clinical signs of mastitis were first detected. The animals were monitored clinically; mammary secretion samples were collected for bacteriological and cytological examinations. The median duration of the clinical signs was 4.75, 7.13, and 4.75 d for T1, T2, and T3; significant differences in clinical severity between the groups were seen until the 7th day post-treatment. The median duration of bacterial recovery was 3.25, 8.00, and 8.00 d for T1, T2, and T3; significant differences in the frequency of bacterial recovery between the groups were seen until (64.1%, 94.9%, and 96.2% of the samples) and after (2.9%, 16.7%, and 11.8%) the 7th day post-treatment. The median period required for the complete cure (clinical, bacteriological, and cytological) was shorter in the T1 than in the T2 and T3 ewe groups: 20.0, 32.0, and 24.5 d, respectively. The findings cover a gap in the available literature regarding the treatment of clinical mastitis in ewes. Early treatment resulted in the improved cure of the infection. The comparison of the intramammary and injectable routes for antibiotic administration indicated some benefit for the former, primarily in the post-treatment somatic cell counts.
PubMed: 36297221
DOI: 10.3390/pathogens11101164 -
Antibiotics (Basel, Switzerland) Apr 2020Studies on human and mouse gastrointestinal microbiota have correlated the composition of the microbiota to a variety of diseases, as well as proved it vital to prevent...
Studies on human and mouse gastrointestinal microbiota have correlated the composition of the microbiota to a variety of diseases, as well as proved it vital to prevent colonization with resistant bacteria, a phenomenon known as colonization resistance. Antibiotics dramatically modify the gut community and there are examples of how antibiotic usage lead to colonization with resistant bacteria [e.g., dicloxacillin usage selecting for ESBL-producing carriage], as shown by Hertz et al. Here, we investigated the impact of five antibiotics [cefotaxime, cefuroxime, dicloxacillin, clindamycin, and ciprofloxacin] on the intestinal microbiota in mice. Five different antibiotics were each given to groups of five mice. The intestinal microbiotas were profiled by use of the IS-pro analysis; a 16S-23S rDNA interspace [IS]-region-based profiling method. For the mice receiving dicloxacillin and clindamycin, we observed dramatic shifts in dominating phyla from day 1 to day 5. Of note, diversity increased, but overall bacterial load decreased. For ciprofloxacin, cefotaxime, and cefuroxime there were few overall changes. We speculate that antibiotics with efficacy against the abundant anaerobes in the gut, particularly Bacteroidetes, can in fact be selected for resistant bacteria, disregarding the spectrum of activity.
PubMed: 32316518
DOI: 10.3390/antibiotics9040191 -
Indian Journal of Pharmaceutical... Jan 2013A simple, accurate, rapid and precise reversed-phase high-performance liquid chromatographic method has been developed and validated for simultaneous determination of...
A simple, accurate, rapid and precise reversed-phase high-performance liquid chromatographic method has been developed and validated for simultaneous determination of cefpodoxime proxetil and dicloxacillin sodium in tablet. The chromatographic separation was carried out on kromasil C18 analytical column (250×4.6 mm; 5 μm) with a mixture of acetonitrile:methanol:trifloroacetic acid (0.001%) with pH 6.5 (30:50:20, v/v/v) as mobile phase; at a flow rate of 1.0 ml/min. UV detection was performed at 235 nm. The dicloxacillin sodium and cefpodoxime proxetil were eluted at 1.92 and 3.35 min, respectively. The peaks were eluted with better resolution. Calibration plots were linear over the concentration range 0.5-20 μg/ml for cefpodoxime proxetil (r(2)=0.9996) and 5-50 μg/ml for dicloxacillin sodium (r(2)=0.9987). The method was validated for accuracy, precision, linearity and specificity. The method was very sensitive with limit of detection 0.0726, 0.3685 μg/ml and limit of quantification 0.220, 1.116 μg/ml for cefpodoxime proxetil and dicloxacillin sodium, respectively. The high recovery and low relative standard deviation confirm the suitability of the method for routine determination of cefpodoxime proxetil and dicloxacillin sodium in bulk drug and tablet dosage form.
PubMed: 23901158
DOI: 10.4103/0250-474X.113538 -
Antimicrobial Agents and Chemotherapy Jun 2010Antibiotic treatment of Staphylococcus aureus infections is often problematic due to the slow response and recurrences. The intracellular persistence of the...
Antibiotic treatment of Staphylococcus aureus infections is often problematic due to the slow response and recurrences. The intracellular persistence of the staphylococci offers a plausible explanation for the treatment difficulties because of the impaired intracellular efficacies of the antibiotics. The intra- and extracellular time- and concentration-kill relationships were examined in vitro with THP-1 cells and in vivo by use of a mouse peritonitis model. The in vivo model was further used to estimate the most predictive pharmacokinetic/pharmacodynamic (PK/PD) indices (the ratio of the maximum concentration of drug in plasma/MIC, the ratio of the area under the concentration-time curve/MIC, or the cumulative percentage of a 24-h period that the free [f] drug concentration exceeded the MIC under steady-state pharmacokinetic conditions [fT(MIC)]) for dicloxacillin (DCX) intra- and extracellularly. In general, DCX was found to have similar intracellular activities, regardless of the model used. Both models showed (i) the relative maximal efficacy (1-log-unit reduction in the numbers of CFU) of DCX intracellularly and (ii) the equal relative potency of DCX intra- and extracellularly, with the MIC being a good indicator of the overall response in both situations. Discordant results, based on data obtained different times after dosing, were obtained from the two models when the extracellular activity of DCX was measured, in which the in vitro model showed a considerable reduction in the number of CFU from that in the original inoculum (3-log-unit decrease in the number of CFU after 24 h), whereas the extracellular CFU reduction achieved in vivo after 4 h did not exceed 1 log unit. Multiple dosing of DCX in vivo revealed increased extra- and intracellular efficacies (2.5 log and 2 log units of reduction in the numbers of CFU after 24 h, respectively), confirming that DCX is a highly active antistaphylococcal antibiotic. PK/PD analysis revealed that fT(MIC) is the index that is the most predictive of the outcome of infection both intra- and extracellularly.
Topics: Animals; Anti-Bacterial Agents; Cell Line; Colony Count, Microbial; Dicloxacillin; Doublecortin Protein; Extracellular Space; Female; Humans; In Vitro Techniques; Intracellular Space; Macrophages; Mice; Microbial Sensitivity Tests; Peritonitis; Staphylococcal Infections; Staphylococcus aureus
PubMed: 20308386
DOI: 10.1128/AAC.01400-09 -
Journal of Analytical Methods in... 2021Novel, accurate, selective, and rapid high-performance liquid chromatography mass spectrometry method was developed for simultaneous analysis of amoxicillin trihydrate,...
Novel, accurate, selective, and rapid high-performance liquid chromatography mass spectrometry method was developed for simultaneous analysis of amoxicillin trihydrate, dicloxacillin sodium, and their official impurity 6-aminopenicillanic acid. The chromatographic separation was carried out by applying the mixture on a C column (3.5 m ps, 100 mm × 4.6 mm id) using acetonitrile:water (65 : 35 by volume) as a mobile phase within only 4 min. The quantitative analysis was executed using single quadrupole mass spectrometer in which electrospray ionization, selected ion monitoring, and negative mode were operated. The retention times were 1.61, 2.54, and 3.50 mins for amoxicillin, 6-aminopenicillanic acid, and dicloxacillin, respectively. The method was validated in linear ranges of 2-28 g mL, 2-35 g mL, and 1-10 g mL for amoxicillin, dicloxacillin, and 6-aminopenicillanic acid, respectively. The results obtained from the suggested HPLC/MS were statistically compared with those obtained from the reported HPLC method, where no significant difference appeared respecting accuracy and precision. According to the analytical eco-scale assessment method, the proposed method was proved to be greener than the reported one, where the analysis time and the amount of the wasted effluent decreased.
PubMed: 34221533
DOI: 10.1155/2021/5570938 -
The New Microbiologica Apr 2017We have previously shown that the phenothiazine, thioridazine, acts in synergy with the beta-lactam antibiotic, dicloxacillin, to kill methicillin-resistant...
We have previously shown that the phenothiazine, thioridazine, acts in synergy with the beta-lactam antibiotic, dicloxacillin, to kill methicillin-resistant Staphylococcus aureus. In this study, we investigated whether synergy by combining these two drugs could also be observed in vancomycin intermediate susceptible S. aureus (VISA) and methicillin-resistant Staphylococcus epidermidis (MRSE). Synergy was observed in three of four tested VISA strains, suggesting that the thickening of cell wall does not interfere with the effects of thioridazine. In S. epidermidis, no synergy was observed in all tested strains, suggesting that synergy by combining thioridazine and dicloxacillin is isolated to S. aureus species.
Topics: Anti-Bacterial Agents; Dicloxacillin; Dopamine Antagonists; Drug Synergism; Humans; Microbial Sensitivity Tests; Staphylococcal Infections; Staphylococcus aureus; Staphylococcus epidermidis; Thioridazine
PubMed: 28255602
DOI: No ID Found