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1.
JAMA Netw Open ; 7(5): e248661, 2024 May 01.
Artículo en Inglés | MEDLINE | ID: mdl-38696172

RESUMEN

Importance: Bacterial vaginosis (BV) is a common cause of vaginal infection. First-line treatments of BV are metronidazole and clindamycin. Due to the increase in antibiotic resistance, effective nonantibiotic treatments for BV are needed. Objective: To examine whether dequalinium chloride, a broad-spectrum antiseptic, is noninferior to oral metronidazole for the treatment of BV. Design, Setting, and Participants: This phase 4, multicenter, triple-blind, double-dummy, parallel, noninferiority randomized clinical trial was conducted from July 29, 2021, to August 25, 2022, with a 1-month follow-up. Participants were premenopausal women 18 years or older with BV from 11 gynecologic practices and 1 hospital in Poland, Slovakia, and the Czech. Intervention: Patients were randomized to treatment with dequalinium chloride vaginal tablets (10 mg once daily for 6 days) or oral metronidazole (500 mg twice daily for 7 days). Double-dummy medication kits contained vaginal and oral tablets with placebo and active medication. Main Outcomes and Measures: The main outcome was the noninferiority margin (of 15 percentage points) in the absolute difference in clinical cure rates between dequalinium chloride and metronidazole 7 to 11 days after start of treatment (visit 1). Noninferiority was met if the lower 95% CI for the difference in clinical cure rate was less than 15 percentage points at visit 1. Results: A total of 147 women (mean [SD] age, 36.7 [9.0] years) were treated with dequalinium chloride (n = 72) or metronidazole (n = 75). The clinical cure rates at visit 1 were 64 of 69 (92.8%) for dequalinium chloride vs 69 of 74 (93.2%) for metronidazole in the intention-to-treat population, whereas in the per-protocol population, cure rates were 54 of 58 (93.1%) for dequalinium chloride vs 48 of 53 (90.6%) for metronidazole. The treatment differences of -0.5 percentage points (95% CI, -10.8 to 9.8 percentage points; P = .002) in the intention-to-treat population and 2.5 percentage points (95% CI, -9.4 to 14.4 percentage points; P = .001) in the per-protocol population confirmed the noninferiority of dequalinium chloride. The tolerability of dequalinium chloride was rated as very good by 30 of 50 patients (60.0%) but only by 21 of 54 (38.9%) for metronidazole. Three patients in the metronidazole group suspended treatment due to an adverse event. Conclusions and Relevance: This randomized clinical trial showed that dequalinium chloride was not inferior to metronidazole for the treatment of BV. Dequalinium chloride had a similarly high cure rate but with better tolerability and fewer adverse events. With a similar efficacy to metronidazole and clindamycin, dequalinium chloride warrants consideration as first-line treatment for BV to help reduce antibiotic consumption. Trial Registration: EudraCT: 2020-002489-15.


Asunto(s)
Decualinio , Metronidazol , Vaginosis Bacteriana , Humanos , Femenino , Metronidazol/uso terapéutico , Vaginosis Bacteriana/tratamiento farmacológico , Adulto , Decualinio/uso terapéutico , Resultado del Tratamiento , Método Doble Ciego , Persona de Mediana Edad , Administración Intravaginal , Antibacterianos/uso terapéutico , Administración Oral , Adulto Joven
2.
Georgian Med News ; (342): 130-132, 2023 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-37991968

RESUMEN

When women with comorbid bacterial vaginosis visit periodontologist, it is essential to understand the presence of cross-infection processes between the oral cavity and vagina in this particular category of subjects. Conducting detection of Gardnerella vaginalis and Atopobium vaginae, which are provocative microbial factors for bacterial vaginosis, is a mandatory step in the laboratory examination of subjects. When choosing an antiseptic for oral cavity disinfection, the use of 0.25% dequalinium chloride is more advisable. Both subjective and objective examination methods thoroughly demonstrate the higher clinical effectiveness of 0.25% dequalinium chloride: patients report a 20% more frequent improvement in subjective indicators, the index assessment of periodontal status improves by 1.2-1.6 times, and the detection rate of Gardnerella vaginalis and Atopobium vaginae is by 20% lower compared to 0.2% chlorhexidine. The specific composition of oral microbiota in this group of subjects necessitates adjustments to treatment protocols and consideration of the specific impact on Gardnerella vaginalis and Atopobium vaginae.


Asunto(s)
Antiinfecciosos Locales , Decualinio , Vaginosis Bacteriana , Humanos , Femenino , Vaginosis Bacteriana/diagnóstico , Vaginosis Bacteriana/tratamiento farmacológico , Vaginosis Bacteriana/microbiología , Gardnerella vaginalis , Decualinio/uso terapéutico , Vagina/microbiología , Antiinfecciosos Locales/uso terapéutico , Boca
3.
J Obstet Gynaecol ; 42(1): 103-109, 2022 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-33629634

RESUMEN

Bacterial vaginosis (BV) represents the most frequent vaginal infection in women of childbearing age. The aim of this study was to characterise episodes of BV among adult Spanish women and their management with dequalinium chloride (DQC). Data from 573 DQC-treated BV adult women was obtained on medical records and questionnaires. The study shows that 20.6% had presented vaginal infections previously. Comorbid candidosis was significantly associated to other symptoms, such as pruritus or leucorrhoea. Most patients (64.3%) indicated a moderate-strong impact of the BV episode on their sexual life. After treatment, 84.8% of patients reported no BV symptoms. Patients were given instructions to prevent relapses. Most patients (83.1%) rated DQC as 'satisfactory' or 'very/extremely satisfactory' regarding symptom relief, prevention or treatment of the episode of BV. In conclusion, this study provides a better understanding of BV episodes and the impact of the treatment with DQC in real clinical practice in Spanish patients.IMPACT STATEMENTWhat is already known on this subject? Bacterial vaginosis (BV) is the most commonly reported vaginal infection among women of childbearing age. Despite the availability of antibiotic medications for the treatment of BV, management of this condition remains challenging. In fact, recurrence of BV has been reported for up to 50% of cases. However, antiseptic agents are considered an effective option for BV treatment.What the results of this study add? The study provides a better understanding of the prevalent symptomatology and the impact on quality of life of women with BV. Moreover, it has been observed that antiseptic dequalinium chloride (DQC) efficiently reduces symptoms and improves quality of life of the patients during episodes of BV.What the implications are of these findings for clinical practice and/or further research? In the context of the World Health Organisation recommendations on the rational use of antibiotics, we believe that the use of DQC may be a good alternative to antibiotics as a therapy for BV.


Asunto(s)
Antiinfecciosos Locales/uso terapéutico , Decualinio/uso terapéutico , Vaginosis Bacteriana/tratamiento farmacológico , Adolescente , Adulto , Anciano , Anciano de 80 o más Años , Femenino , Humanos , Persona de Mediana Edad , Calidad de Vida , Estudios Retrospectivos , España , Resultado del Tratamiento , Vagina/microbiología , Adulto Joven
4.
Arch Gynecol Obstet ; 303(1): 151-160, 2021 01.
Artículo en Inglés | MEDLINE | ID: mdl-32940765

RESUMEN

PURPOSE: To compare the clinical response, microscopic examination and fungal culture between dequalinium chloride (DQC) and clotrimazole (CT) for treating vaginal candidiasis (VC). METHODS: The double-blind, randomized study was conducted from September 2014 to September 2016 at Siriraj Hospital, Thailand. Eligible participants were Thai women diagnosed with VC by microscopic examination. The exclusion criteria included immunocompromised conditions, consumption of antifungal drugs, and having recurrent VC. Each participant was randomized with a 1:1 allocation to receive six vaginal tablets of 100 mg CT or 10 mg DQC. Two visits included 10 ± 2 days (C1) and 38 ± 4 days (C2). Outcome measures were improvement of VC symptoms, microscopic examination, culture, satisfaction and tolerability. RESULTS: Of 155 eligible participants, 150 were randomized and allocated into CT (N = 76) and DQC (N = 74). The average age was 31.1 ± 7.2 years. Comparable improvement of clinical response was demonstrated (OR at C1 0.79, 95% CI 0.56-1.10, p = 0.197; and OR at C2 0.99, 95% CI 0.69-1.43, p = 0.985). Of CT and DQC groups, the microscopic examination was positive at 11/75 (14.9%) vs 18/72 (25.3%) at C1 and 18/74 (24.3%) vs 28/66 (42.4%) at C2. And the culture was positive at 25/75 (33.8%) vs 46/72 (65.7%) at C1 and at 26/74 (36.6%) vs 46/66 (69.7%) at C2. Most participants had high satisfaction and tolerability and none reported any side effects. CONCLUSION: DQC and CT show comparable clinical response but CT results in greater improvement of microscopic examination and fungal culture. CLINICAL TRIAL REGISTRATION: The Clinical Trial Registry number was NCT02242695. (September 17, 2014).


Asunto(s)
Antiinfecciosos Locales/uso terapéutico , Antifúngicos/uso terapéutico , Candidiasis Vulvovaginal/tratamiento farmacológico , Clotrimazol/uso terapéutico , Decualinio/uso terapéutico , Adulto , Candidiasis Vulvovaginal/diagnóstico , Método Doble Ciego , Femenino , Humanos , Persona de Mediana Edad , Evaluación de Resultado en la Atención de Salud , Comprimidos/administración & dosificación , Tailandia , Cremas, Espumas y Geles Vaginales
5.
BMC Cancer ; 19(1): 1224, 2019 Dec 16.
Artículo en Inglés | MEDLINE | ID: mdl-31842863

RESUMEN

BACKGROUND: Mitochondria are considered a primary intracellular site of reactive oxygen species (ROS) generation. Generally, cancer cells with mitochondrial genetic abnormalities (copy number change and mutations) have escalated ROS levels compared to normal cells. Since high levels of ROS can trigger apoptosis, treating cancer cells with low doses of mitochondria-targeting / ROS-stimulating agents may offer cancer-specific therapy. This study aimed to investigate how baseline ROS levels might influence cancer cells' response to ROS-stimulating therapy. METHODS: Four cancer and one normal cell lines were treated with a conventional drug (cisplatin) and a mitochondria-targeting agent (dequalinium chloride hydrate) separately and jointly. Cell viability was assessed and drug combination synergisms were indicated by the combination index (CI). Mitochondrial DNA copy number (mtDNAcn), ROS and mitochondrial membrane potential (MMP) were measured, and the relative expression levels of the genes and proteins involved in ROS-mediated apoptosis pathways were also investigated. RESULTS: Our data showed a correlation between the baseline ROS level, mtDNAcn and drug sensitivity in the tested cells. Synergistic effect of both drugs was also observed with ROS being the key contributor in cell death. CONCLUSIONS: Our findings suggest that mitochondria-targeting therapy could be more effective compared to conventional treatments. In addition, cancer cells with low levels of ROS may be more sensitive to the treatment, while cells with high levels of ROS may be more resistant. Doubtlessly, further studies employing a wider range of cell lines and in vivo experiments are needed to validate our results. However, this study provides an insight into understanding the influence of intracellular ROS on drug sensitivity, and may lead to the development of new therapeutic strategies to improve efficacy of anticancer therapy.


Asunto(s)
Protocolos de Quimioterapia Combinada Antineoplásica/farmacología , Cisplatino/farmacología , Decualinio/farmacología , Mitocondrias/metabolismo , Neoplasias/tratamiento farmacológico , Especies Reactivas de Oxígeno/metabolismo , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapéutico , Línea Celular Tumoral , Supervivencia Celular , Cisplatino/uso terapéutico , Decualinio/uso terapéutico , Femenino , Humanos , Masculino , Potencial de la Membrana Mitocondrial , Mitocondrias/efectos de los fármacos , Neoplasias/metabolismo , Pronóstico , Resultado del Tratamiento
6.
Int J Nanomedicine ; 13: 4209-4226, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30140154

RESUMEN

INTRODUCTION: Multidrug resistance (MDR) of breast cancer is the major challenge to successful chemotherapy while mitochondria-targeting therapy was a promising strategy to overcome MDR. MATERIALS AND METHODS: In this study, HER-2 peptide-PEG2000-Schiff base-cholesterol (HPSC) derivate was synthesized successfully and incorporated it on the surface of the doxorubicin (DOX)-loaded dequalinium (DQA) chloride vesicle (HPS-DQAsomes) to treat drug-resistant breast cancer. Evaluations were performed using human breast cancer cell and DOX-resistant breast cancer cell lines (MCF-7 and MCF-7/ADR). RESULTS: The particle size of HPS-DQAsomes was ~110 nm with spherical shape. In vitro cytotoxicity assay indicated that HPS-DQAsomes could increase the cytotoxicity against MCF-7/ADR cell line. Cellular uptake and mitochondria-targeting assay demonstrated that HPS-DQAsomes could target delivering therapeutical agent to mitochondria and inducing mitochondria-driven apoptosis process. In vivo antitumor assay suggested that HPS-DQAsomes could reach favorable antitumor activity due to both tumor targetability and sub-organelles' targetability. Histological assay also indicated that HPS-DQAsomes showed a strong apoptosis-inducing effect. No obvious systematic toxicity of HPS-DQAsomes could be observed. CONCLUSION: In summary, multifunctional HPS-DQAsomes provide a novel and versatile approach for overcoming MDR via mitochondrial pathway in cancer treatment.


Asunto(s)
Antineoplásicos/farmacología , Decualinio/farmacología , Doxorrubicina/farmacología , Sistemas de Liberación de Medicamentos , Mitocondrias/metabolismo , Péptidos/farmacología , Receptor ErbB-2/metabolismo , Animales , Antineoplásicos/uso terapéutico , Apoptosis/efectos de los fármacos , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Colesterol/química , Citocromos c/metabolismo , Decualinio/uso terapéutico , Doxorrubicina/uso terapéutico , Liberación de Fármacos , Resistencia a Antineoplásicos/efectos de los fármacos , Endocitosis/efectos de los fármacos , Femenino , Humanos , Concentración de Iones de Hidrógeno , Liposomas , Células MCF-7 , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Ratones Desnudos , Mitocondrias/efectos de los fármacos , Tamaño de la Partícula , Polietilenglicoles/química , Bases de Schiff/química , Pruebas de Toxicidad
7.
Drug Ther Bull ; 55(5): 54-57, 2017 May.
Artículo en Inglés | MEDLINE | ID: mdl-28495833

RESUMEN

Bacterial vaginosis is an infection characterised by overgrowth of anaerobic bacteria in the vagina with an accompanying loss of lactobacilli, and is thought to be the most common cause of abnormal vaginal discharge in women of child-bearing age.1 Standard treatment for symptomatic bacterial vaginosis consists of a short course of an oral or topical antibiotic.2 Dequalinium, a topical antiseptic agent, has been available for many years as a treatment for oral infections.3 A new formulation, dequalinium 10mg vaginal tablets (Fluomizin-Kora Healthcare), was licensed in the UK in June 2015 for the treatment of bacterial vaginosis.4 Here, we review evidence for the effectiveness and safety of dequalinium vaginal tablets in the management of bacterial vaginosis.


Asunto(s)
Antibacterianos/administración & dosificación , Decualinio/administración & dosificación , Vaginosis Bacteriana/tratamiento farmacológico , Administración Intravaginal , Antibacterianos/efectos adversos , Antibacterianos/uso terapéutico , Decualinio/efectos adversos , Decualinio/uso terapéutico , Femenino , Humanos , Comprimidos
8.
Oncotarget ; 6(29): 27537-54, 2015 Sep 29.
Artículo en Inglés | MEDLINE | ID: mdl-26348470

RESUMEN

A major therapeutic obstacle in clinical oncology is intrinsic or acquired resistance to therapy, leading to subsequent relapse. We have previously shown that systemic administration of different cytotoxic drugs can induce a host response that contributes to tumor angiogenesis, regrowth and metastasis. Here we characterize the host response to a single dose of local radiation, and its contribution to tumor progression and metastasis. We show that plasma from locally irradiated mice increases the migratory and invasive properties of colon carcinoma cells. Furthermore, locally irradiated mice intravenously injected with CT26 colon carcinoma cells succumb to pulmonary metastasis earlier than their respective controls. Consequently, orthotopically implanted SW480 human colon carcinoma cells in mice that underwent radiation, exhibited increased metastasis to the lungs and liver compared to their control tumors. The irradiated tumors exhibited an increase in the colonization of macrophages compared to their respective controls; and macrophage depletion in irradiated tumor-bearing mice reduces the number of metastatic lesions. Finally, the anti-tumor agent, dequalinium-14, in addition to its anti-tumor effect, reduces macrophage motility, inhibits macrophage infiltration of irradiated tumors and reduces the extent of metastasis in locally irradiated mice. Overall, this study demonstrates the adverse effects of local radiation on the host that result in macrophage-induced metastasis.


Asunto(s)
Neoplasias del Colon/tratamiento farmacológico , Decualinio/análogos & derivados , Decualinio/uso terapéutico , Macrófagos/efectos de los fármacos , Metástasis de la Neoplasia , Animales , Antineoplásicos/uso terapéutico , Línea Celular , Línea Celular Tumoral , Neoplasias del Colon/patología , Medios de Cultivo Condicionados/química , Femenino , Células HCT116 , Células HT29 , Células Endoteliales de la Vena Umbilical Humana , Humanos , Macrófagos/metabolismo , Ratones , Ratones Endogámicos BALB C , Ratones SCID , Trasplante de Neoplasias , Neovascularización Patológica
10.
Biomaterials ; 32(24): 5673-87, 2011 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-21550109

RESUMEN

Intrinsic multidrug resistance (MDR) of cancers remains a major obstacle to successful chemotherapy. A dequalinium polyethylene glycol-distearoylphosphatidylethanolamine (DQA-PEG(2000)-DSPE) conjugate was synthesized as a mitochondriotropic molecule, and mitochondrial targeting resveratrol liposomes were developed by modifying DQA-PEG(2000)-DSPE on the surface of liposomes for overcoming the resistance. Evaluations were performed on the human lung adenocarcinoma A549 cells and resistant A549/cDDP cells, A549 and A549/cDDP tumor spheroids as well as the xenografted resistant A549/cDDP cancers in nude mice. The yield of DQA-PEG(2000)-DSPE conjugate synthesized was about 87% and the particle size of mitochondrial targeting resveratrol liposomes was approximately 70 nm. The mitochondrial targeting liposomes significantly enhanced the cellular uptake, and selectively accumulated into mitochondria when encapsulating coumarin as the fluorescent probe. Furthermore, mitochondrial targeting resveratrol liposomes induced apoptosis of both non-resistant and resistant cancer cells by dissipating mitochondria membrane potential, releasing cytochrome c and increasing the activities of caspase 9 and 3. They also exhibited significant antitumor efficacy in two kinds of cancer cells, in tumor spheroids by penetrating deeply into the core, and in xenografted resistant A549/cDDP cancers in nude mice. Mitochondrial targeting resveratrol liposomes co-treating with vinorelbine liposomes significantly enhanced the anticancer efficacy against the resistant A549/cDDP cells. In conclusion, mitochondrial targeting resveratrol liposomes would provide a potential strategy to treat the intrinsic resistant lung cancers by inducing apoptosis via mitochondria signaling pathway.


Asunto(s)
Apoptosis/efectos de los fármacos , Decualinio/química , Liposomas/química , Liposomas/uso terapéutico , Neoplasias Pulmonares/metabolismo , Mitocondrias/metabolismo , Fosfatidiletanolaminas/química , Polietilenglicoles/química , Estilbenos/química , Estilbenos/uso terapéutico , Animales , Línea Celular Tumoral , Citocromos c/metabolismo , Decualinio/uso terapéutico , Femenino , Humanos , Ratones , Ratones Endogámicos BALB C , Ratones Desnudos , Resveratrol
11.
EMBO Mol Med ; 2(9): 371-84, 2010 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-20721990

RESUMEN

Neuroblastoma (NB) is the most deadly extra-cranial solid tumour in children necessitating an urgent need for effective and less toxic treatments. One reason for the lack of efficacious treatments may be the inability of existing drugs to target the tumour-initiating or cancer stem cell population responsible for sustaining tumour growth, metastases and relapse. Here, we describe a strategy to identify compounds that selectively target patient-derived cancer stem cell-like tumour-initiating cells (TICs) while sparing normal paediatric stem cells (skin-derived precursors, SKPs) and characterize two therapeutic candidates. DECA-14 and rapamycin were identified as NB TIC-selective agents. Both compounds induced TIC death at nanomolar concentrations in vitro, significantly reduced NB xenograft tumour weight in vivo, and dramatically decreased self-renewal or tumour-initiation capacity in treated tumours. These results demonstrate that differential drug sensitivities between TICs and normal paediatric stem cells can be exploited to identify novel, patient-specific and potentially less toxic therapies.


Asunto(s)
Antibióticos Antineoplásicos/uso terapéutico , Decualinio/análogos & derivados , Células Madre Neoplásicas/efectos de los fármacos , Neuroblastoma/tratamiento farmacológico , Sirolimus/uso terapéutico , Bibliotecas de Moléculas Pequeñas/química , Animales , Apoptosis , Decualinio/química , Decualinio/uso terapéutico , Transporte de Electrón , Perfilación de la Expresión Génica , Humanos , Ratones , Ratones Endogámicos NOD , Mitocondrias/genética , Mitocondrias/metabolismo , Células Madre Neoplásicas/metabolismo , Neuroblastoma/genética , Bibliotecas de Moléculas Pequeñas/uso terapéutico , Ensayos Antitumor por Modelo de Xenoinjerto
12.
Exp Parasitol ; 115(1): 19-24, 2007 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-16814285

RESUMEN

Bisquinoline compounds have exhibited remarkable activity in vitro and in vivo against Plasmodium parasites by inhibition of heme detoxification. We have tested the ability of dequalinium 1,1'-(1,10-decanediyl)bis(4-amino-2-methylquinoline), a known antimicrobial agent, to inhibit beta-hematin synthesis using a non-emzymatic colorimetric assay and globin proteolysis by electrophoretic analysis (SDS-PAGE-15%). Dequalinium was able to inhibit both processes in vitro with close correlation to a murine malaria model, reducing parasitemia levels, prolonging the survival time post-infection and curing 40% of infected mice using a combination therapy with a loading dose of chloroquine. These results confirm that dequalinium is a promising lead for antimalarial drug development.


Asunto(s)
Antiinfecciosos/farmacología , Decualinio/farmacología , Malaria/tratamiento farmacológico , Plasmodium berghei/efectos de los fármacos , Animales , Antiinfecciosos/uso terapéutico , Colorimetría , Decualinio/uso terapéutico , Modelos Animales de Enfermedad , Electroforesis en Gel de Poliacrilamida , Globinas/efectos de los fármacos , Globinas/metabolismo , Hemoproteínas/biosíntesis , Hemoproteínas/efectos de los fármacos , Malaria/parasitología , Masculino , Ratones , Parasitemia/tratamiento farmacológico , Parasitemia/parasitología , Plasmodium berghei/metabolismo
13.
Lik Sprava ; (3): 49-51, 2006.
Artículo en Ucraniano | MEDLINE | ID: mdl-17100185

RESUMEN

Urogenital infection being one of etiological factor of the development of miscarriage, physicians regard carrying out complex microbiological diagnostics of pregnant women which are at risk of miscarriage to be very important as well as providing appropriate therapy for women with urogenital infection. The study aimed at investigating the efficacy of local antimicrobial medication Fluomisin in complex treatment of pregnant women which are at risk of miscarriage. Obtained results confirm Fluomisin to be effective, safe and convenient at use-for pregnant women with inferior urogenital infections.


Asunto(s)
Aborto Espontáneo/etiología , Antiinfecciosos Locales/uso terapéutico , Decualinio/uso terapéutico , Enfermedades de los Genitales Femeninos , Complicaciones Infecciosas del Embarazo , Aborto Espontáneo/prevención & control , Administración Intravaginal , Antiinfecciosos Locales/administración & dosificación , Decualinio/administración & dosificación , Femenino , Enfermedades de los Genitales Femeninos/complicaciones , Enfermedades de los Genitales Femeninos/tratamiento farmacológico , Enfermedades de los Genitales Femeninos/microbiología , Edad Gestacional , Humanos , Embarazo , Complicaciones Infecciosas del Embarazo/tratamiento farmacológico , Complicaciones Infecciosas del Embarazo/microbiología , Riesgo
14.
Arzneimittelforschung ; 52(9): 706-15, 2002.
Artículo en Inglés | MEDLINE | ID: mdl-12404887

RESUMEN

This randomised, double-blind, multicentric clinical study compared the efficacy and tolerability of the two vaginal antiseptics, 10 mg dequalinium chloride (CAS 522-51-0, Fluomycin N) and 200 mg povidone iodine (CAS 25655-41-8), in a parallel-group design. A total of 180 patients with vaginal infections of varying etiology participated in this study (bacterial vaginosis, fluor vaginalis, vulvo-vaginal candidiasis, trichomoniasis). Patients were randomly allocated to one of the two treatment groups and were treated once per day for 6 days. Control examinations took place 5 to 7 days after the end of treatment, and 3 to 4 weeks after the first control examination. The total symptoms score, a summary score for the clinical symptoms, discharge, burning, pruritus, redness of vulva/vagina, was defined as primary efficacy parameter. The treatments at the first control examination were compared in the full analysis set using the Wilcoxon-Mann-Whitney U-test, 2-sided, thereby proving equivalence of both treatments at the 5% level. Both treatments strongly improved the symptoms of vaginal infections both on short-term and long-term follow-up. Descriptive analysis of the secondary parameters, vaginal pH, degree of purity of the vaginal flora, and number of lactobacilli in the wet mounts, supported the comparable efficacy of both therapies to restore the vaginal milieu. Analysis of the diagnostic subgroups indicated that irrespective of the diagnosis, both treatments improved the efficacy criteria as observed for the entire population. The global assessment of the therapeutic efficacy by investigators and patients supported the results of the efficacy analysis with good to very good ratings in 70-90% of the cases. A good tolerability of both preparations was observed in this study with a low number of adverse events in the test group (5.8%).


Asunto(s)
Antiinfecciosos Locales/uso terapéutico , Decualinio/uso terapéutico , Povidona Yodada/uso terapéutico , Enfermedades Vaginales/tratamiento farmacológico , Adolescente , Adulto , Anciano , Anciano de 80 o más Años , Antiinfecciosos Locales/administración & dosificación , Antiinfecciosos Locales/efectos adversos , Candidiasis Vulvovaginal/tratamiento farmacológico , Candidiasis Vulvovaginal/microbiología , Decualinio/administración & dosificación , Decualinio/efectos adversos , Método Doble Ciego , Femenino , Humanos , Concentración de Iones de Hidrógeno , Persona de Mediana Edad , Povidona Yodada/administración & dosificación , Povidona Yodada/efectos adversos , Tricomoniasis/tratamiento farmacológico , Tricomoniasis/microbiología , Excreción Vaginal/microbiología , Enfermedades Vaginales/microbiología
15.
Adv Drug Deliv Rev ; 49(1-2): 63-70, 2001 Jul 02.
Artículo en Inglés | MEDLINE | ID: mdl-11377803

RESUMEN

Traditional chemotherapies, aimed at DNA replication in rapidly dividing cells, have achieved only limited success in the treatment of carcinomas due largely to their lack of specificity for cells of tumorigenic origin. It is important, therefore, to investigate treatment strategies aimed at novel cellular targets that are sufficiently different between normal cells and cancer cells so as to provide a basis for selective tumor cell killing. Delocalized lipophilic cations (DLCs) are concentrated by cells and into mitochondria in response to negative inside transmembrane potentials. The higher plasma and/or mitochondrial membrane potentials of carcinoma cells compared to normal epithelial cells account for the selective accumulation of DLCs in carcinoma mitochondria. Since most DLCs are toxic to mitochondria at high concentrations, their selective accumulation in carcinoma mitochondria and consequent mitochondrial toxicity provide a basis for selective carcinoma cell killing. Several of these compounds have already displayed some degree of efficacy as chemotherapeutic agents in vitro and in vivo. The effectiveness of DLCs can also be enhanced by their use in photochemotherapy or combination drug therapy. Discovery of the biochemical differences that account for the higher membrane potentials in carcinoma cells is expected to lead to the design of new DLCs targeted specifically to those differences, resulting in even greater selectivity and efficacy for tumor cell killing.


Asunto(s)
Antineoplásicos/farmacología , Carcinoma/metabolismo , Membranas Intracelulares/efectos de los fármacos , Mitocondrias/efectos de los fármacos , Fosforilación Oxidativa/efectos de los fármacos , Antiinfecciosos Locales/farmacología , Antiinfecciosos Locales/uso terapéutico , Antineoplásicos/uso terapéutico , Carcinoma/tratamiento farmacológico , Cationes/farmacología , Cationes/uso terapéutico , Permeabilidad de la Membrana Celular/efectos de los fármacos , Decualinio/farmacología , Decualinio/uso terapéutico , Sistemas de Liberación de Medicamentos/métodos , Colorantes Fluorescentes/farmacología , Colorantes Fluorescentes/uso terapéutico , Humanos , Membranas Intracelulares/metabolismo , Lípidos de la Membrana/metabolismo , Potenciales de la Membrana/efectos de los fármacos , Potenciales de la Membrana/fisiología , Mitocondrias/metabolismo , Fotoquimioterapia/métodos , Rodamina 123/farmacología , Rodamina 123/uso terapéutico , Células Tumorales Cultivadas/efectos de los fármacos , Células Tumorales Cultivadas/metabolismo
16.
Lin Chuang Er Bi Yan Hou Ke Za Zhi ; 12(7): 334-6, 1998 Jul.
Artículo en Chino | MEDLINE | ID: mdl-11189192

RESUMEN

A qualitative analysis of microflora from pharynx of 100 cases of acute pharyngitis and acute tonsillitis was performed. These patients were randomly divided into two groups so as to assess treatment effect of Taileqi troches vs Amoxycillin. Results showed that beta-hemolytic streptococcus, Klebsiella pneumoniae, staphylococcus aureus were the most common organisms causing diseases. The predominant anaerobic organisms were bacteroides melaninogenicus, eptostrep. These findings suggest that anaerobic bacteria may play a pathogenic role in infection of the pharynx. The effective rate of treatment with troche alone were 86 percent, roughly consistent with Amoxycillin group. No adverse effect was observed.


Asunto(s)
Antibacterianos/uso terapéutico , Decualinio/uso terapéutico , Faringitis/microbiología , Prevotella melaninogenica/aislamiento & purificación , Tonsilitis/microbiología , Enfermedad Aguda , Adolescente , Adulto , Amoxicilina/uso terapéutico , Niño , Preescolar , Femenino , Humanos , Klebsiella pneumoniae/aislamiento & purificación , Masculino , Persona de Mediana Edad , Faringitis/tratamiento farmacológico , Staphylococcus aureus/aislamiento & purificación , Streptococcus/aislamiento & purificación , Tonsilitis/tratamiento farmacológico
17.
Gynecol Oncol ; 50(1): 38-44, 1993 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-8349163

RESUMEN

Dequalinium chloride (DECA) is a cationic, lipophilic compound with structure similar to the dye rhodamine 123. DECA is selectively accumulated and retained within the mitochondria of carcinoma cells where it acts as a mitochondrial poison by blocking mitochondrial enzymes which can then disrupt cellular energy production, eventually resulting in cell death. In this manner it is similar to the antimitochondrial effects observed with tumor necrosis factor (TNF). We have previously shown that DECA can synergize the in vitro antitumor effects of TNF against a panel of human ovarian cancer cell lines. Those drug studies have been extended to a xenogenic tumor system with a resultant increase in animal survival. Athymic mice were injected intraperitoneally with 2.0 x 10(7) PA-1 human ovarian cancer cells and DECA +/- TNF treatments begun either on Days 3 or 7 postinjection. Peritoneal tumor implantation was not histologically confirmed by Day 3 postinjection but confirmed by Day 7 following tumor cell injection. Single-agent DECA (5 mg/kg; qod) increased animal survival by 37% (P = 0.002) whereas recombinant human TNF (0.5 micrograms/mouse; qod) only increased survival by 13% (P = 0.27) relative to control animals for those animals treated 3 days post-tumor-injection. Sequential DECA/TNF enhanced animal survival by 45% (P = 0.0002) in similarly treated animals. When drug treatment was initiated 7 days following tumor injection, DECA increased survival by 23% (P = 0.04) while TNF had no effect on prolonging animal survival (3% increase; P = 0.79). Combination DECA/TNF increased survival by 23% (P = 0.04). In the UCI-101 ovarian tumor model, single-agent DECA increased survival by 28% (P = 0.04) while TNF treatment stimulated tumor growth (11% decrease in survival; P = 0.006). Combination DECA + TNF resulted in a 41% increase in survival (P = 0.003). No statistical differences were detected between survival rates for single-agent DECA vs DECA + TNF except for the UCI-101 tumor which showed potentiation due to the in vivo stimulatory effects of TNF.


Asunto(s)
Carcinoma/tratamiento farmacológico , Decualinio/uso terapéutico , Neoplasias Ováricas/tratamiento farmacológico , Factor de Necrosis Tumoral alfa/uso terapéutico , Animales , Carcinoma/mortalidad , Combinación de Medicamentos , Sinergismo Farmacológico , Femenino , Ratones , Ratones Endogámicos BALB C , Trasplante de Neoplasias , Neoplasias Ováricas/mortalidad , Análisis de Supervivencia , Células Tumorales Cultivadas
18.
Eur J Cancer ; 29A(1): 124-8, 1992.
Artículo en Inglés | MEDLINE | ID: mdl-1445729

RESUMEN

Cationic lipophilic compounds have an antiproliferative effect on certain tumour systems in vitro and in vivo. We have investigated whether the cationic lipophilic compound dequalinium affects not only proliferation but also motility and invasion of the highly metastatic and highly invasive melanoma cell line K1735-M2. Proliferation was assessed in monolayer cultures and in multicellular spheroids, motility was estimated in the assay of directional migration, and invasiveness was tested through confrontation cultures of tumour multicellular spheroids with embryonic chick heart tissue evaluated by computerized image analysis. 2 mumol/l dequalinium impaired melanoma cell proliferation, reduced directional migration and significantly blocked invasion in vitro. On the ultrastructural level, dequalinium caused obvious changes in mitochondria of both melanoma and embryonic chick heart cells. The mechanisms of the antiproliferative, antimigrating and antiinvasive effects remain to be determined. Inhibition of protein kinase C, calmodulin antagonism, DNA intercalation and/or direct effects on mitochondrial functions may be considered.


Asunto(s)
Decualinio/uso terapéutico , Melanoma/tratamiento farmacológico , Animales , Melanoma/ultraestructura , Ratones , Microscopía Electrónica , Mitocondrias/ultraestructura , Mitosis/efectos de los fármacos , Invasividad Neoplásica , Metástasis de la Neoplasia , Células Tumorales Cultivadas/efectos de los fármacos
19.
Oralprophylaxe ; 13(4): 133-41, 1991 Dec.
Artículo en Alemán | MEDLINE | ID: mdl-1818603

RESUMEN

The influence of antimicrobial mouthrinses containing dequalinium chloride or sanguinarine on early plaque formation was assessed in vivo in a clinical-experimental study. Rinses with water served as controls. After 24 and 72 hours, plastic films, which were applied to the buccal surfaces of six upper front teeth at the start of experiment, were removed and processed for transmission electron microscopic study. Dequalinium chloride or sanguinarine applied on plaque resulted in an increased and higher structured surface coating. Degenerated microorganisms were observed and the variety of bacteria seemed to be reduced. Both mouthrinses effected the early supragingival plaque formation. The effect of sanguinarine was more intensive than that of dequalinium chloride.


Asunto(s)
Alcaloides/farmacología , Antibacterianos/farmacología , Placa Dental/prevención & control , Decualinio/farmacología , Antisépticos Bucales/farmacología , Adulto , Alcaloides/uso terapéutico , Antibacterianos/uso terapéutico , Bacterias/efectos de los fármacos , Benzofenantridinas , Placa Dental/microbiología , Placa Dental/ultraestructura , Decualinio/uso terapéutico , Femenino , Humanos , Isoquinolinas , Masculino , Persona de Mediana Edad , Antisépticos Bucales/uso terapéutico
20.
Artículo en Alemán | MEDLINE | ID: mdl-9272987

RESUMEN

A comparative study involving 50 patients of both genders was conducted in order to determine the effect of dequalinium chloride/benzalconium chloride mouthrinse (Dequonal), and of a preparation of herbal essences (Parodontax) on gingival health. Each of the mouthrinses was used during four weeks by a group of 25 patients who were instructed to abstain from any other oral hygiene measure during this period. Approximal plaque index, sulcus bleeding index and saliva pH were significantly enhanced by both preparations. A slightly better effect shown by dequalinium chloride/benzalconium chloride was not significant.


Asunto(s)
Antiinfecciosos Locales/uso terapéutico , Compuestos de Benzalconio/uso terapéutico , Dentífricos/uso terapéutico , Decualinio/uso terapéutico , Encía/efectos de los fármacos , Antisépticos Bucales/uso terapéutico , Extractos Vegetales/uso terapéutico , Bicarbonato de Sodio/uso terapéutico , Adulto , Mezclas Complejas , Combinación de Medicamentos , Evaluación de Medicamentos , Femenino , Humanos , Concentración de Iones de Hidrógeno , Masculino , Compuestos de Quinolinio , Saliva/efectos de los fármacos
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