OBJECTIVE: To determine the safety of intracamerally injected preservative-free 0.5% moxifloxacin/0.1% dexamethasone fixed-dose combination on the corneal endothelium in a rabbit model and compare it to intracamerally injected preservative-free 0.5% moxifloxacin.

METHODS: This experimental study included twenty eyes from ten albino rabbits. The eyes were assessed for baseline corneal clarity and anterior chamber (AC) inflammation using slit-lamp biomicroscopy. A specular microscope measured the corneal endothelial cell density (ECC) and corneal thickness (CT). Intracameral injections of 0.1 mL 0.5% moxifloxacin ophthalmic solution were administered to the 10 right eyes (IPFM group) and 0.1 mL of 0.5% moxifloxacin/0.1% dexamethasone fixed-dose preparation were administered to the 10 left eyes (IPFMDex group). In both groups, ECC, CT, corneal clarity, and AC inflammation at Day 1 (one day post-injection) and Day 7 (seven days post-injection) were compared with Day 0 (baseline). The IPFMDex group was also compared with the IPFM group at Days 0, 1, and 7. The endothelial cells of harvested corneas from both groups at Day 1 and 7 were stained with trypan blue and alizarin red, and compared for endothelial cell damage (ECD). Data were analyzed using paired and independent sample t-tests.

RESULTS: In both the IPFM and IPFMDex groups, ECC and CT at Day 1 (IPFM: ECC p=0.07, CT p=0.76; IPFMDex: ECC p=0.41, CT p=0.94) and Day 7 (IPFM: ECC p=0.95, CT p=0.28; IPFMDex: ECC p=0.29, CT p=0.34) were not different from Day 0 (baseline). No significant difference in ECC, CT, and ECD were found between the IPFM and IPFMDex groups at Day 1 (ECC p=0.82, CT p=0.36, ECD p=0.96) and Day 7 (ECC p=0.95, CT p=0.22, ECD p=0.61). Throughout the study, the cornea in both groups were clear and showed no signs of AC inflammation.

CONCLUSION: Intracameral injection of preservative-free moxifloxacin/dexamethasone fixed-dose formulation was safe on the rabbit corneal endothelium and was no different from preservative-free moxifloxacin.

Animal ; Endothelium, Corneal ; Moxifloxacin ; Alizarin ; Dexamethasone ; Slit Lamp ; Aza Compounds ; Anterior Chamber ; Cornea ; Anthraquinones ; Endothelial Cells ; Inflammation ; Ophthalmic Solutions

PURPOSE: To compare the epithelial wound healing response of two preservative-free fluoroquinolones, moxifloxacin and levofloxacin, in patients who underwent cataract surgery. MATERIALS AND METHODS: In this prospective, evaluator-masked, randomized clinical trial, 59 eyes of 50 patients who underwent cataract surgery were enrolled. Patients were randomized to receive moxifloxacin 0.5% (n=32 eyes) or levofloxacin 0.5% (n=27 eyes). All patients instilled moxifloxacin or levofloxain four times daily for 1 week prior to surgery and 2 weeks after surgery. The epithelial wound healing status in the corneal incision site was scanned with a raster scan mode of fourier-domain optical coherence tomography (FD-OCT). The number of eyes showing epithelial defect images and average number of corneal epithelial defect cuts per eye were compared between groups. All patients were evaluated on postoperative days 1, 2, 3, and 10. RESULTS: On postoperative days 1, 2, and 3, the number of eyes showing epithelial defects in FD-OCT was not statistically different (all p>0.05). The average number of corneal epithelial defect cuts was also not statistically different between the two groups (all p>0.05). No eyes showed epithelial defects on postoperative day 10 in either group. CONCLUSION: There were no differences on epithelial wound healing comparing these two different fluoroquinolones at the incision site of cataract surgery.
Aged ; Aza Compounds/therapeutic use ; Cataract Extraction ; Cornea/drug effects/*surgery ; Female ; Fluoroquinolones/*therapeutic use ; Humans ; Levofloxacin/therapeutic use ; Male ; Middle Aged ; Quinolines/therapeutic use ; Tomography, Optical Coherence ; Wound Healing/*drug effects

OBJECTIVE: To determine the safety of intracameral moxifloxacin 0.5% ophthalmic solution in cataract surgery given at a dose of 500 mg/0.1 mL.
METHODS: Medical records of uncomplicated phacoemulsification performed between January 2009 and December 2010 were reviewed. Each eye received 0.1 mL intracameral moxifloxacin (0.5% ophthalmic solution containing 500 mg of moxifloxacin) prophylactically. Outcome measures included anterior chamber cells and flare (Hogan System), corneal thickness, endothelial cell density, visual acuity, and intraocular pressure.
RESULTS: 353 eyes of 244 patients, mean age of 67.51 ± 9.22 years, were included into the study. All patients completed follow-up to 3 weeks, with 79 patients (103 eyes) followed up to 3 months. All eyes had 20/40 or better vision at 3 weeks and 3 months postoperatively. Trace to +2 anterior chamber cells and flares were observed in 96% of eyes on day 1 postsurgery. All had quiet anterior chambers at subsequent follow-up examinations. Intraocular pressures recorded postoperatively were not significantly different. Mean endothelial cell count (ECC) postoperatively were 2473.25 cells/mm2 at 3 weeks and 2468.42 cells/mm2 at 3 months and were not significantly different from baseline (2586.57 cells/mm2) (p = 0.07 and 0.12 respectively). The mean central corneal thickness postoperatively at 3 weeks (551.92 µm) and at 3 months (542.67 µm ) were not different from baseline (546.48 µm) (p = 0.47). Those with diabetes mellitus showed similar results.
CONCLUSION: Intracameral moxifloxacin 0.5% appears to be safe for prophylactic use in cataract surgery. At a dose of 500 mg/0.1 mL, there was minimal anterior chamber reaction, and the corneal thickness and endothelial cell density were not significantly different from preoperative.

Human ; Male ; Female ; Aged ; Middle Aged ; Phacoemulsification ; Moxifloxacin ; Intraocular Pressure ; Aza Compounds ; Anterior Chamber ; Cataract Extraction ; Cataract ; Ophthalmic Solutions ; Diabetes Mellitus ; Endothelial Cells

PARP [poly(ADP-ribose)polymerase] represents a novel potential target in cancer therapy. It is involved in a DNA repair process by catalyzing the transfer of ADP-ribose units from NAD to a number of its substrate proteins. In this work, a series of novel azaindole derivatives was designed and synthesized. Moreover, 16 target molecules were screened and 8 compounds displayed inhibitory activity against PARP-1. It has been demonstrated that these azaindoles bearing cycloamine substituents at 2-position were active to both PARP-1 and PARP-2.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Aza Compounds ; chemical synthesis ; chemistry ; pharmacology ; Indoles ; chemical synthesis ; chemistry ; pharmacology ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; metabolism

Aged ; Arylsulfotransferase ; genetics ; Aza Compounds ; administration & dosage ; Fluoroquinolones ; Genetic Predisposition to Disease ; Humans ; Male ; Multidrug Resistance-Associated Proteins ; genetics ; Multiple Organ Failure ; chemically induced ; genetics ; Mutation ; genetics ; Quinolines ; administration & dosage

Endogenous lipoid pneumonia is an uncommon condition. This is a report of a 29-year-old woman diagnosed with endogenous lipoid pneumonia associated with Legionella pneumophila serogroup 1 infection. The patient's endogenous lipoid pneumonia resolved completely after treatment for Legionella pneumophila infection. This suggests that early diagnosis and aggressive treatment of the underlying infection may prevent any long-term sequelae of lipoid pneumonia.
Adult ; Anti-Bacterial Agents ; therapeutic use ; Aza Compounds ; therapeutic use ; Azithromycin ; therapeutic use ; Female ; Fluoroquinolones ; Humans ; Legionella pneumophila ; classification ; Legionnaires' Disease ; diagnosis ; drug therapy ; microbiology ; Pneumonia, Lipid ; diagnosis ; drug therapy ; microbiology ; Quinolines ; therapeutic use ; Treatment Outcome

PURPOSE: To report a case of fungal keratitis caused by Scedosporium apiospermum. CASE SUMMARY: A 70-year-old man visited our clinic with complaints of redness and decreased visual acuity in his right eye caused by a soil gotten into an eye while gardening 10 days ago. The patient had previously been treated in a local clinic but did not show significant clinical improvement. Bacterial and fungal staining, culture, and an antibiotic sensitivity test were performed from a corneal scrape. The cultures revealed growth of Scedosporium apiospermum. The patient was treated with topical moxifloxacin antibiotics, fluconazole, amphotericin B antifungal agents. However, the lesion was not improved, so antifungal therapy was switched to topical voriconazole. After two months of treatment, the infection was resolved with mild scarring. CONCLUSIONS: Although it is a rare pathogen, Scedosporium apiospermum should be considered as a potential pathogen in patients presenting with corneal ulceration due to trauma from an object contaminated by soil, polluted water, or spoiled plant contact. And we suggest that topical application of voriconazole may be a good alternative treatment for patient with fungal keratitis in which no improvement despite a conventional antifungal agent, fluconazole.
Amphotericin B ; Anti-Bacterial Agents ; Antifungal Agents ; Aza Compounds ; Corneal Ulcer ; Eye ; Fluconazole ; Gardening ; Humans ; Keratitis ; Plants ; Pyrimidines ; Quinolines ; Scedosporium ; Soil ; Triazoles ; Visual Acuity

Aged ; Anemia, Diamond-Blackfan ; complications ; Aza Compounds ; adverse effects ; Female ; Fluoroquinolones ; Humans ; Quinolines ; adverse effects ; Torsades de Pointes ; chemically induced ; complications

BACKGROUND: Binary toxin-producing Clostridium difficile infections (CDI) are known to be more severe and to cause higher case fatality rates than those by binary toxin-negative isolates. There has been few data of binary toxin-producing CDI in Korea. Objective of the study is to characterize clinical and microbiological trait of CDI cause by binary-toxin producing isolates in Korea. MATERIALS AND METHODS: From September 2008 through January 2010, clinical characteristics, medication history and treatment outcome of all the CDI patients were collected prospectively. Toxin characterization, PCR ribotyping and antibiotic susceptibility were performed with the stool isolates of C. difficile. RESULTS: During the period, CDI caused by 11binary toxin-producing isolates and 105 toxin A & toxin B-positive binary toxin-negative isolates were identified. Comparing the disease severity and clinical findings between two groups, leukocytosis and mucoid stool were more frequently observed in patients with binary toxin-positive isolates (OR: 5.2, 95% CI: 1.1 to 25.4, P = 0.043; OR: 7.6, 95% CI: 1.6 to 35.6, P = 0.010, respectively), but clinical outcome of 2 groups did not show any difference. For the risk factors for acquisition of binary toxin-positive isolates, previous use of glycopeptides was the significant risk factor (OR: 6.2, 95% CI: 1.4 to 28.6, P = 0.019), but use of probiotics worked as an inhibitory factor (OR: 0.1, 95% CI: 0.0 to 0.8; P = 0.026). PCR ribotypes of binary toxinproducing C. difficile showed variable patterns: ribotype 130, 4 isolates; 027, 3 isolates; 267 and 122, 1 each isolate and unidentified C1, 2 isolates. All 11 binary toxin-positive isolates were highly susceptible to clindamycin, moxifloxacin, metronidazole, vancomycin and piperacillin-tazobactam, however, 1 of 11 of the isolates was resistant to rifaximin. CONCLUSIONS: Binary toxin-producing C. difficile infection was not common in Korea and those isolates showed diverse PCR ribotypes with high susceptibility to antimicrobial agents. Glycopeptide use was a risk factor for CDI by those isolates.
Anti-Infective Agents ; Aza Compounds ; Clindamycin ; Clostridium ; Clostridium difficile ; Glycopeptides ; Humans ; Korea ; Leukocytosis ; Metronidazole ; Polymerase Chain Reaction ; Probiotics ; Prospective Studies ; Quinolines ; Ribotyping ; Risk Factors ; Sprains and Strains ; Treatment Outcome ; Vancomycin

The aims of this study were to investigate the changing pattern of Helicobacter pylori antibiotic resistance in Jinju over a 15-year period. H. pylori strains were isolated from 170 adults living in Jinju from 1985-1989, 1990-1994 and 1995-1999, and from 23 adults living in Cheongju from 1995 to 1999. Susceptibility to erythromycin, clarithromycin, azithromycin, amoxicillin, tetracycline, metronidazole, furazolidone, levofloxacin, ciprofloxacin, moxifloxacin, and rifabutin was tested using the serial two-fold agar dilution method. Moxifloxacin resistance significantly increased in Jinju from 1985-1989 (0%) to 1995-1999 (14.9%) (p < 0.0001). Resistance to amoxicillin was increasesed trend to decreased trend from 1985 to 1999 (p = 0.033), whereas metronidazole resistance decreased from 37.5% to 21.3%. Resistance to furazolidone was greater from 1985-1989 (9.4%) than in 1995-1999 (2.1%). In comparing Jinju and Cheongju, minimal inhibitory concentrations (MICs) of tetracycline and levofloxacin among H. pylori isolated from Jinju were lower than for isolates from Cheonju (p < 0.05). The levofloxacin resistance rate was higher in Cheongju than in Jinju (p = 0.02). No macrolide resistance was observed in Cheongju. Overall, we did not observe any remarkable antimicrobial resistance increase of H. pylori strains isolated from Jinju over 15 years. The MIC distributions of antimicrobials and antimicrobial resistant rates were time- and region-specific among different strains. Future anti-H. pylori eradication regimens should be designed based on the changing patterns of antimicrobial resistance according to the resident area.
Adult ; Agar ; Amoxicillin ; Anti-Infective Agents ; Aza Compounds ; Azithromycin ; Ciprofloxacin ; Clarithromycin ; Drug Resistance, Microbial ; Erythromycin ; Furazolidone ; Helicobacter ; Helicobacter pylori ; Humans ; Metronidazole ; Ofloxacin ; Quinolines ; Rifabutin ; Tetracycline