scholarly journals Bacterial Infections in the Elderly Patient: Focus on Sitafloxacin

2012 ◽  
Vol 4 ◽  
pp. CMT.S7435 ◽  
Author(s):  
Beniam Ghebremedhin
Keyword(s):  
Bacterial Infections ◽  
Randomized Clinical Trials ◽  
Bacterial Pathogens ◽  
Anaerobic Bacteria ◽  
The Elderly ◽  
Gram Positive ◽  
Double Blind ◽  
Odontogenic Infections ◽  
Tract Infections

Sitafloxacin (DU-6859a) is a new-generation oral fluoroquinolone with in vitro activity against a broad range of Gram-positive and -negative bacteria, including anaerobic bacteria, as well as against atypical bacterial pathogens. Particularly in Japan this antibiotic was approved in 2008 for treatment of a number of bacterial infections caused by Gram-positive cocci and Gram-negative cocci and rods, including anaerobia atypical bacterial pathogens. As compared to oral levofloxacin sitafloxacin was non-inferior in the treatment of community-acquired pneumonia and non-inferior in the treatment of complicated urinary tract infections, according to the results of randomized, double-blind, multicentre, non-inferiority trials. Non-comparative studies demonstrated the efficacy of oral sitafloxacin in otorhinolaryngological infections, urethritis in men, cervicitis in women and odontogenic infections. Most common adverse reactions were gastrointestinal disorders and laboratory abnormalities in patients receiving oral sitafloxacin; diarrhea and liver enzyme elevations were among the common. In the Japanese population sitafloxacin covers broad spectrum of bacteria as compared to carbapenems, whereas in the Caucasians its use is currently limited due to the potential for ultraviolet A phototoxicity. Sitafloxacin is a promising therapeutic agent which merits further investigation in randomized clinical trials of elderly patients.

scholarly journals Fluoroquinolone antimicrobial agents.

1989 ◽  
Vol 2 (4) ◽  
pp. 378-424 ◽  
Author(s):  
J S Wolfson ◽  
D C Hooper
Keyword(s):  
Bacterial Infections ◽  
Deoxyribonucleic Acid ◽  
Bacterial Resistance ◽  
Antimicrobial Agents ◽  
Beta Lactam ◽  
Double Blind ◽  
Gram Negative ◽  
Cutaneous Infections ◽  
Tract Infections

The fluoroquinolones, a new class of potent orally absorbed antimicrobial agents, are reviewed, considering structure, mechanisms of action and resistance, spectrum, variables affecting activity in vitro, pharmacokinetic properties, clinical efficacy, emergence of resistance, and tolerability. The primary bacterial target is the enzyme deoxyribonucleic acid gyrase. Bacterial resistance occurs by chromosomal mutations altering deoxyribonucleic acid gyrase and decreasing drug permeation. The drugs are bactericidal and potent in vitro against members of the family Enterobacteriaceae, Haemophilus spp., and Neisseria spp., have good activity against Pseudomonas aeruginosa and staphylococci, and (with several exceptions) are less potent against streptococci and have fair to poor activity against anaerobic species. Potency in vitro decreases in the presence of low pH, magnesium ions, or urine but is little affected by different media, increased inoculum, or serum. The effects of the drugs in combination with a beta-lactam or aminoglycoside are often additive, occasionally synergistic, and rarely antagonistic. The agents are orally absorbed, require at most twice-daily dosing, and achieve high concentrations in urine, feces, and kidney and good concentrations in lung, bone, prostate, and other tissues. The drugs are efficacious in treatment of a variety of bacterial infections, including uncomplicated and complicated urinary tract infections, bacterial gastroenteritis, and gonorrhea, and show promise for therapy of prostatitis, respiratory tract infections, osteomyelitis, and cutaneous infections, particularly when caused by aerobic gram-negative bacilli. Fluoroquinolones have also proved to be efficacious for prophylaxis against travelers' diarrhea and infection with gram-negative bacilli in neutropenic patients. The drugs are effective in eliminating carriage of Neisseria meningitidis. Patient tolerability appears acceptable, with gastrointestinal or central nervous system toxicities occurring most commonly, but only rarely necessitating discontinuance of therapy. In 17 of 18 prospective, randomized, double-blind comparisons with another agent or placebo, fluoroquinolones were tolerated as well as or better than the comparison regimen. Bacterial resistance has been uncommonly documented but occurs, most notably with P. aeruginosa and Staphylococcus aureus and occasionally other species for which the therapeutic ratio is less favorable. Fluoroquinolones offer an efficacious, well-tolerated, and cost-effective alternative to parenteral therapies of selected infections.

Działanie in vitro olejku cyprysowego (Oleum Cupressi) na bakterie beztlenowe

2019 ◽  
Vol 20 (2) ◽  
Author(s):  
Anna Kędzia ◽  
Elżbieta Hołderna-Kędzia
Keyword(s):  
Anaerobic Bacteria ◽  
Growth Control ◽  
Cupressus Sempervirens ◽  
Tannerella Forsythia ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Gram Positive Cocci ◽  
Porphyromonas Levii

Introduction. Cypress (Cupressus sempervirens L.) belongs to the family Cupressaceae. It is evergreen, and grows in Mediterranean region. The Cypress leaves and young branches are utilized to produce the essential oil. Cypress oil contain a number of components, in it α-pinene, Δ3-carene, α-terpinyl acetate, cedrol, α-terpinolene, β-myrcene, limonene, α-terpineolene, terpinen-4-ol, β-pinene, δ-cadinene and sabinene. The oil is used in therapy different diseases. It to have antimicrobial activity. Aim. The aim of the date was evaluation the susceptibility of anaerobic bacteria to Cypress oil. Material and methods. The anaerobic bacteria were isolated from patients. The 62 microorganisms, in it 36 strains of Gram-negative rods, 14 Gram-positive cocci and 12 Gram-positive rods, and 7 reference strains were tested. Susceptibility (MIC) was determined by means of plate dilution technique in Brucella agar supplemented with 5% defibrynated sheep blood, menadione and hemin. The Cypress oil was dissolved in DMSO and distilled water to obtain final following concentrations: 2.5, 5.0, 7.5, 10.0, 15.0 and 20.0 mg/ml. Inoculum containing 106 CFU per 1 ml was seeded with Steers replicator upon the agar with oil or without the oil (strains growth control). The agar plates was incubated in anaerobic condition in anaerobic jar in 37°C for 48 hrs. The MIC was interpreted as the lowest concentration of Cypress oil inhibiting the growth of tested bacteria. Results. The results indicated that from among Gram-negative rods the most susceptible to Cypress oil was the strains from genus Tannerella forsythia (MIC < 2.5-5.0 mg/ml), Bacteroides uniformis (MIC = 5.0 mg/ml), Bacteroides vulgatus and Porphyromonas asaccharolytica (MIC 5.0-7.5 mg/ml) and Porphyromonas levii (MIC = 7.5 mg/ml). The strains from genera Fusobacterium and of Bacteroides fragilis were the susceptible to 2.5-≥ 20.0 mg/ml. The Cypress oil was least active towards Prevotella and Parabacteroides strains (MIC ≥ 20.0 mg/ml).The tested Gram-positive cocci were more susceptible. The growth of the strains were inhibited by concentrations in ranges ≤ 2.5-7.5 mg/ml. The oil was minor active towards Gram-positive rods (MIC ≤ 2.5-20.0 mg/ml). Among the strains the genus of Actinomyces odontolyticus (MIC = 5.0 mg/ml) and Actinomyces viscosus (MIC ≤ 2.5-7.5 mg/ml) were the most susceptible. The growth of rods of Bifidobacterium breve was inhibited by concentrations 10.0 mg/ml. The data indicates that the Gram-negative rods were the less susceptible than Gram-positive bacteria to cypress oil. Conclusions. Among Gram-negative rods the most susceptible were the strains Tannerella forsythia, Bacteroides uniformis, Bacteroides vulgatus, Porphyromonas asaccharolytica and Porphyromonas levii. The oil was more active against Gram-positive cocci. Gram-positive anaerobic bacteria demonstrate the more susceptible to Cypress oil then Gram-positive rods.

An insight to the toxic effect of Sulfamerazine on Porcine Pancreatic Amylase and Lactate Dehydrogenase Activity: An in vitro study

2021 ◽  
Vol 15 ◽  
Author(s):  
Avirup Malla ◽  
Koel Mukherjee ◽  
Mukulika Mandal ◽  
Aishwarya Mukherjee ◽  
Runa Sur ◽  
...  
Keyword(s):  
Lactate Dehydrogenase ◽  
Lactic Acidosis ◽  
Conformational Changes ◽  
Bacterial Infections ◽  
Titration Calorimetry ◽  
Dependent Manner ◽  
Pancreatic Amylase ◽  
Lactate Dehydrogenase Activity ◽  
Tract Infections

Background: Sulfamerazine, a sulfonamide has been routinely used to treat various bacterial infections namely Pneumonia, Urinary tract infections, Shigellosis, Bronchitis, Prostatitis, and many more. It interferes with the bacterial folic acid biosynthesis albeit higher eukaryotes are not susceptible to its action due to the inherent absence of this specific pathway. Objective: In spite of its constant use, Sulfamerazine administration evokes serious issues like development of antibacterial resistance through environmental contamination although how it affects eukaryotic system, specifically its target identification has not been addressed in detail. Methods: Hela Cells are cultured as per standard method, amylase and lactate dehydrogenase assay are conducted using standard procedure with spectrophotometer. Binding thermodynamics and conformational study has been estimated with isothermal titration calorimetry as well as with docking. Results: Experimental observations reveal that Sulfamerazine inhibits porcine pancreatic amylase in a noncompetitive mode (IC50 of 0.96 mM). Binding of the drug to porcine pancreatic amylase is entropy driven with conformational changes of the protein as indicated by concomitant red shift. It enhances the inhibitory effects of acarbose and cetapin on their in vitro pancreatic amylase activity. It augments lipid peroxidation and promotes lactic acidosis in a dose dependent manner. Docking studies ensure effective interactions between Sulfamerazine and proteins like lactic dehydrogenase and porcine pancreatic amylase. Conclusion: Detailed study is to be conducted to confirm whether molecular scaffold of Sulfamerazine might serve as an effective repurposed drug acting as a lead molecule for the design of antidiabetic drug of future use. Alternatively, it should be prescribed with caution under specific medical situations like diabetes, cancer, hepatic disorders manifesting lactic acidosis to avoid crisis.

An update on cefepime and its future role in combination with novel β-lactamase inhibitors for MDR Enterobacterales and Pseudomonas aeruginosa

2020 ◽  
Author(s):  
Burcu Isler ◽  
Patrick Harris ◽  
Adam G Stewart ◽  
David L Paterson
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Clinical Studies ◽  
Bacterial Infections ◽  
Animal Studies ◽  
Wide Spectrum ◽  
Clinical Development ◽  
Phase Iii ◽  
Lactam Antibiotic ◽  
Tract Infections

Abstract Cefepime, a wide-spectrum β-lactam antibiotic, has been in use for the treatment of serious bacterial infections for almost 25 years. Since its clinical development, there has been a dramatic shift in its dosing, with 2 g every 8 hours being preferred for serious infections to optimize pharmacokinetic/pharmacodynamic considerations. The advent of ESBLs has become a threat to its ongoing use, although future coadministration with β-lactamase inhibitors (BLIs) under development is an area of intense study. There are currently four new cefepime/BLI combinations in clinical development. Cefepime/zidebactam is generally active against MBL-producing Enterobacterales and Pseudomonas aeruginosa, in vitro and in animal studies, and cefepime/taniborbactam has activity against KPC and OXA-48 producers. Cefepime/enmetazobactam and cefepime/tazobactam are potential carbapenem-sparing agents with activity against ESBLs. Cefepime/enmetazobactam has completed Phase III and cefepime/taniborbactam is in Phase III clinical studies, where they are being tested against carbapenems or piperacillin/tazobactam for the treatment of complicated urinary tract infections. While these combinations are promising, their role in the treatment of MDR Gram-negative infections can only be determined with further clinical studies.

scholarly journals 1371. Safety, Tolerability, and Pharmacokinetics of Multiple Doses of TP-6076, a Novel, Fully Synthetic Tetracycline, in a Phase 1 Study

2018 ◽  
Vol 5 (suppl_1) ◽  
pp. S420-S420 ◽  
Author(s):  
Larry Tsai ◽  
Alison Moore
Keyword(s):  
Physical Examination ◽  
Bacterial Infections ◽  
Clinical Laboratory ◽  
Phase 1 ◽  
Geometric Mean ◽  
Vital Signs ◽  
Gastrointestinal Adverse Event ◽  
Double Blind ◽  
Dose Study

Abstract Background TP-6076 is a novel, fully synthetic tetracycline being developed for the treatment of serious bacterial infections, including those caused by multidrug-resistant Acinetobacter baumannii. TP-6076 has demonstrated potent activity in vitro against carbapenem-resistant strains of A. baumannii, with MIC90 64 times lower compared with tigecycline and 256 times lower compared with minocycline. We now report the results of a multiple ascending dose study in normal healthy volunteers. Methods This was a phase 1, single-site, randomized, double-blind, placebo-controlled dose-escalating, multiple dose study in healthy adults who met the inclusion/exclusion criteria and provided informed consent prior to any study procedure. Cohorts of eight subjects each (six active and two placebo) received daily doses of 6.0 to 40.0 mg TP-6076 or placebo for 7 days. Plasma and urine samples for pharmacokinetic (PK) analyses were collected starting immediately prior to dosing until 96 hours after the last dose. Safety was assessed through collection of adverse events (AEs), clinical laboratories, vital signs, ECG, and physical examination data. Results The geometric mean derived PK parameters for TP-6076 were: There were no serious or severe AEs reported. The most frequently reported AEs were gastrointestinal events, including nausea and vomiting, and localized infusion site reactions. There were no clinically significant changes in clinical laboratory values, ECG parameters, or physical examination findings. Conclusion Following multiple IV doses of TP-6076, plasma exposure increased as dose increased. Multiple IV doses of TP-6076 were generally well tolerated, with higher gastrointestinal adverse event rates in the higher dose groups. Disclosures L. Tsai, Tetraphase Pharmaceuticals: Employee and Shareholder, Salary. A. Moore, Tetraphase Pharmaceuticals: Employee, Salary.

scholarly journals TSPphg Lysin from the Extremophilic Thermus Bacteriophage TSP4 as a Potential Antimicrobial Agent against Both Gram-Negative and Gram-Positive Pathogenic Bacteria

Viruses ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 192 ◽  
Author(s):  
Feng Wang ◽  
Xinyu Ji ◽  
Qiupeng Li ◽  
Guanling Zhang ◽  
Jiani Peng ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Pathogenic Bacteria ◽  
Infection Model ◽  
Bacterial Cells ◽  
Skin Damage ◽  
Gram Positive ◽  
Antibiotic Resistant ◽  
Gram Negative

New strategies against antibiotic-resistant bacterial pathogens are urgently needed but are not within reach. Here, we present in vitro and in vivo antimicrobial activity of TSPphg, a novel phage lysin identified from extremophilic Thermus phage TSP4 by sequencing its whole genome. By breaking down the bacterial cells, TSPphg is able to cause bacteria destruction and has shown bactericidal activity against both Gram-negative and Gram-positive pathogenic bacteria, especially antibiotic-resistant strains of Klebsiella pneumoniae, in which the complete elimination and highest reduction in bacterial counts by greater than 6 logs were observed upon 50 μg/mL TSPphg treatment at 37 °C for 1 h. A murine skin infection model further confirmed the in vivo efficacy of TSPphg in removing a highly dangerous and multidrug-resistant Staphylococcus aureus from skin damage and in accelerating wound closure. Together, our findings may offer a therapeutic alternative to help fight bacterial infections in the current age of mounting antibiotic resistance, and to shed light on bacteriophage-based strategies to develop novel anti-infectives.

scholarly journals Comparative In Vitro Activities of Torezolid (DA-7157) against Clinical Isolates of Aerobic and Anaerobic Bacteria in South Korea

2010 ◽  
Vol 54 (12) ◽  
pp. 5381-5386 ◽  
Author(s):  
Jong Hwa Yum ◽  
Sung Hak Choi ◽  
Dongeun Yong ◽  
Yunsop Chong ◽  
Weon Bin Im ◽  
...  
Keyword(s):  
South Korea ◽  
Antimicrobial Agents ◽  
Anaerobic Bacteria ◽  
Clinical Isolates ◽  
Bacterial Isolates ◽  
First Line ◽  
Gram Positive ◽  
The World ◽  
Aerobic And Anaerobic

ABSTRACT Resistance of Gram-positive pathogens to first-line antimicrobial agents has been increasing in many parts of the world. We compared the in vitro activities of torezolid with those of other antimicrobial agents, including linezolid, against clinical isolates of major aerobic and anaerobic bacteria. Torezolid had an MIC90 of ≤0.5 μg/ml for the Gram-positive bacterial isolates tested and was more potent than either linezolid or vancomycin.

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