Penetration of 0. 3% ciprofloxacin, 0. 3% ofloxacin, and 0. 5% moxifloxacin into the cornea and aqueous humor of enucleated human eyes

We aimed to quantify the penetration of ciprofloxacin, ofloxacin, and moxifloxacin into the cornea and aqueous humor of cadaver eyes. A total of 60 enucleated eyes, not eligible for corneal transplantation, were divided into three groups and immersed in commercial solutions of 0.3% ciprofloxacin, 0.3% ofloxacin, or 0.5% moxifloxacin for 10 min. Whole corneas and samples of aqueous humor were then harvested and frozen, and drug concentrations analyzed by liquid chromatography tandem mass spectrometry. The mean corneal concentration of moxifloxacin was twice as high as ofloxacin, and the latter was twice as high as ciprofloxacin. The mean concentration of moxifloxacin in the aqueous humor was four times higher than the other antibiotics, and the mean concentrations of ciprofloxacin and ofloxacin were statistically similar. The amount of drug that penetrated the anterior chamber after a 10-min immersion was far below the safe limit of endothelial toxicity of each preparation. Moxifloxacin demonstrated far superior penetration into the cornea and anterior chamber of cadaver eyes compared to ciprofloxacin and ofloxacin. One should not expect endothelial toxicity with the commercial eye drops of ciprofloxacin, ofloxacin, and moxifloxacin that reach the anterior chamber through the cornea.

Pharmacodynamic profiling of commonly prescribed antimicrobial drugs against Escherichia coli isolates from urinary tract

Since antimicrobial resistance among uropathogens against current first line agents has affected the management of severe urinary tract infection, we determined the likelihood that antibiotic regimens achieve bactericidal pharmacodynamic exposures using Monte Carlo simulation for five antimicrobials (ciprofloxacin, ceftriaxone, piperacillin/tazobactam, ertapenem, and meropenem) commonly prescribed as initial empirical treatment of inpatients with severe community acquired urinary tract infections. Minimum inhibitory concentration determination by Etest was performed for 205 Brazilian community urinary tract infection Escherichia coli strains from 2008 to 2012 and 74 E. coli bloodstream strains recovered from a surveillance study. Pharmacodynamic exposure was modeled via a 5000 subject Monte Carlo simulation. All isolates were susceptible to ertapenem and meropenem. Piperacillin/tazobactam, ceftriaxone and ciprofloxacin showed 100%, 97.5% and 83.3% susceptibility among outpatient isolates and 98.6%, 75.7% and 64.3% among inpatient isolates, respectively. Against outpatient isolates, all drugs except ciprofloxacin (82.7% in aggressive and 77.6% in conservative scenarios) achieved high cumulative fraction of response: car-bapenems and piperacillin/tazobactam cumulative fraction of responses were close to 100%, and ceftriaxone cumulative fraction of response was 97.5%. Similar results were observed against inpatients isolates for carbapenems (100%) and piperacillin/tazobactam (98.4%), whereas ceftriaxone achieved only 76.9% bactericidal cumulative fraction of response and ciprofloxacin 61.9% (aggressive scenario) and 56.7% (conservative scenario) respectively. Based on this model, standard doses of beta-lactams were predicted to deliver sufficient pharmacodynamic exposure for outpatients. However, ceftriaxone should be avoided for inpatients and ciprofloxacin empirical prescription should be avoided in both inpatients and outpatients with complicated urinary tract infection.

Estudio biofarmacéutico comparativo de marcas comerciales de tabletas de ciprofloxacino disponibles en el mercado colombiano / A comparative biopharmaceutical study of brands of ciprofloxacin tablets available on the Colombian market

Objetivo: Determinar la equivalencia biofarmacéutica de marcas comerciales de Ciprofloxacino 500 mg disponibles en el mercado colombiano. Métodos: Se tomaron 12 productos comerciales de Ciprofloxacino tabletas 500 mg, adquiridos en droguerías y farmacias de cuatro de las principales ciudades del país, a los cuales se les realizaron los siguientes ensayos: Identificación del principio activo por HPLC, contenido de ingrediente activo, uniformidad de dosificación, pruebas de desintegración y disolución; además se compararon los perfiles de disolución de los productos frente a uno tomado como referencia. Los resultados se analizaron a fin de establecer diferencias estadísticamente significativas y posible intercambiabilidad entre los productos evaluados. Resultados: El análisis comparativo de los productos, permitió evidenciar marcadas diferencias en cuanto a la liberaciónin vitrodel principio activo, con uno de los productos incumpliendo este importante parámetro de calidad. Todos los productos evaluados cumplen con las especificaciones oficiales de identificación y valoración del principio activo, uniformidad de dosificación y tiempo de desintegración. En cuanto a la cinética de disolución se encontraron diferencias entre las formulaciones, con productos de deficiente Eficiencia de Disolución (ED) y que a pesar de cumplir con la especificación a Q30, se disuelven muy lentamente. Conclusiones: Once productos cumplen con todas las especificaciones establecidas en la USP-33/NF28. Los resultados de este trabajo constituyen un valioso aporte para en un futuro cercano y en función de las políticas nacionales, poder establecer bioequivalencia entre estos productos.

Objective: Determining the biopharmaceutical equivalency of 500 mg ciprofloxacin tablets available on the Colombian market (i.e. comparing different trademarks). Methods: Twelve commercial 500 mg ciprofloxacin tablets were obtained from drugstores and pharmacies in Colombia’s four major cities. They were submitted to the following assays: HPLC identification of active ingredients, active ingredient content, dose uniformity, disintegration and dissolution tests and comparing the products’ dissolution profiles to that of the innovator. The results were analyzed to establish statistically significant differences and possible inter-changeability between the products being tested. Results: Comparative analysis of the products revealed marked differences regardingin vitrorelease of the active principle (one product failing this important quality parameter). All the products tested here complied with the official specifications for identifying and assaying the active principle, dosage unit uniformity and the disintegration test. Regarding dissolution kinetics, differences were found between formulations as some products had poor dissolution efficiency (DE) and dissolved very slowly despite complying with the Q30specification. Conclusions: 11 products complied with USP33-NF28specifications (guidelines on specifications for impurities in antibiotics). This work has made a valuable contribution towards establishing these products’ bioequivalence in the near future regarding national policy.

Therapeutic effects of ciprofloxacin on the pharmacokinetics of carbamazepine in healthy adult male volunteers

Carbamazepine is a [CYP1A2 and CYP3A4 enzyme inducer] medicine which is used by epileptic patients for a long time. During the course of therapy, patients are generally caught by other diseases like urinary tract infections, upper respiratory tract infection, skin and soft tissue infection etc. To cure them, physicians commonly prescribe fluoroquinolones like Ciprofloxacin [CYP1A2 inhibitor] along with Carbamazepine [CBZ]. Interactions may result without recognition which may lead to unforeseen toxicity, untoward effects or even therapeutic failure. Therefore, studies were conducted to investigate the effect of Ciprofloxacin on the pharmacokinetics of Carbamazepine in healthy adult male volunteers. The main objective of this study was to generate new knowledge regarding CBZ and Ciprofloxacin interaction for physicians and research workers dealing with these medicines. Eight healthy adult male volunteers were selected to assess the effect of ciprofloxacin on the pharmacokinetics of Carbamazepine. After overnight fast the selected male volunteers were given CBZ orally. Blood samples were drawn at different time intervals after medication. Then the same volunteers were given CBZ along with ciprofloxacin. Blood samples were again drawn at the same time intervals as done previously. Plasma was separated from the blood samples. Concentration of CBZ in the plasma samples was determined by using HPLC technique. Results of the present study indicated that ciprofloxacin significantly increased the plasma concentration of CBZ when given concurrently to the healthy adult male volunteers. Ciprofloxacin increased C[max], AUC and t [1/2] while it decreased the CL and Vd of CBZ when administered concurrently to the adult volunteers. Change in pharmacokinetic parameters was due to slow metabolism or elimination of CBZ when given concurrently with ciprofloxacin to the adult volunteers. This is probably due to the inhibition of CYP3A4 isoenzyme by ciprofloxacin which is responsible for metabolism of CBZ. Ciprofloxacin increased the plasma concentration of CBZ so dose adjustment as well as drug monitoring of CBZ is required when both the drugs are given concurrently. The knowledge regarding interaction between ciprofloxacin and CBZ would be helpful for the pharmaceutical industries, physicians and a blessing for the patients

Biodistribución y farmacocinética de 99mTc-ciprofloxacina obtenida de una formulación modificada / Biokinetics performance of 99mTc-ciprofloxacin obtained from a new formulation

El propósito de la presente investigación fue evaluar el comportamiento biocinético de la 99mTc-ciprofloxacina obtenida de una nueva formulación. Un ensayo in vitro y un modelo de infección experimental demostraron su afinidad por bacterias vivas. La vida media en sangre fue de 5,89 +/- 0,85 horas. La biodistribución mostró alta acumulación en músculos infectados y baja en tejidos sanos.

The aim of the present investigation was to evaluate the biokinetics performance of 99mTc-ciprofloxacin obtained from a new formulation. Both in vitro assays and experimental infection models demonstrated its affinity for viable bacteria.Half life in blood was 5.89 +/- 0.85 hours. The biodistribution showed high accumulation on infected muscles and low on healthy tissues.

Aqueous and vitreous penetration of oral cefixime and ciprofloxacin in rabbit eye

To investigate the penetration of cefixime and ciprofloxacin to the rabbit eye on the basis of microbial inhibition of aqueous and vitreous humour after oral administration. In this experimental study, 36 rabbits [72 eyes] were randomly divided into two groups; group A consisted of 20 rabbits and group B 16 rabbits. Each group was divided into four equal subgroups. The rabbits in each subgroup of group A received 4, 8, 12, and 20 mg/kg of syrup of cefixime every 12 hr respectively and the rabbits in each subgroup of group B received 20, 40, 60, and 80 mg/kg tablet of ciprofloxacin respectively every 12 hr. Immediately after the first dose of the drugs, the anterior chamber of one eye was irrigated randomly by 30-40 cc of ringer lactate solution alongside with mild traumatization of iris. Then by 4, 8, 12, 24 and 72 hr intervals after the 3rd dose, 0.1 cc of aqueous, 0.2-0.5 cc of vitreous, 3 cc of blood and one standard disk of the used antibiotic was placed on culture media of a known bacteria which was completely sensitive to the respective antibiotic. Forty eight hours later, the microbial inhibition zone of each sample and the standard disk of antibiotic were compared. No microbial inhibition was seen by sample of aqueous and vitreous, although very large zone of inhibition was seen by blood sample and standard disk of antibiotic. It seems that oral cefixime and ciprofloxacin do not produce an effective dose for microbial inhibition in rabbit eye

Pharmacokinetics of ciprofloxacin in patients with liver cirrhosis.

BACKGROUND: Bacterial infections are common in patients with cirrhosis of liver and are frequently treated with ciprofloxacin. Literature on pharmacokinetics of ciprofloxacin in patients with cirrhosis of the liver is scanty. The present study compared the pharmacokinetics of ciprofloxacin in cirrhotic patients with that in healthy volunteers. METHODS: In 20 patients with cirrhosis of liver (all Child-Pugh class B) and 10 healthy volunteers, plasma levels of ciprofloxacin were measured using high-performance liquid chromatography at several time points after a 500-mg oral dose. Various pharmacokinetic parameters were calculated. RESULTS: No significant differences were observed in maximum plasma levels reached (mean [SD] 2.6 [0.6] vs 2.6 [1.3] microg/ml), time taken for maximum plasma levels to be reached (1.3 [0.6] vs 1.5 [0.9] h), t1/2a (0.7 [0.3] vs 0.4 [0.9] h), elimination half-life (3.6 [1.2] vs 3.2 [1.8] h), and area under the curve (19.3 [3.8] vs 21.9 [4.5] microg/mL x h) in healthy volunteers and cirrhotic patients, respectively. CONCLUSIONS: Pharmacokinetics of ciprofloxacin is unaltered in patients with liver cirrhosis. Ciprofloxacin can be safely administered in the usual doses in such patients.

Mecanismos de acción bactericida de ciprofloxacina sobre bacilos gram negativos fermentadores y no fermentadores / Mechanisms of bactericidal action of ciprofloxacin against fermentative and non fermentative gram negative bacilli

Ciprofloxacina es una quinolona con mayor actividad sobre bacilos gram negativos fermentadores que sobre los no fermentadores, lo que puede relacionarse con diferentes mecanismos de acción bactericida descritos en estos compuestos. En este trabajo se investiga la actividad bactericida de ciprofloxacina sobre escherichia coli y klebsiella pneumoniae (bacilos gram negativos fermentadores) y sobre pseudomonas aeruginosa y acinetobacter baumannii (bacilos gram negativos no fermentadores) en ausencia y presencia de rifampicina. Rifampicina inhibió parcialmente la actividad bactericida de ciprofloxacina en los bacilos fermentadore y no tuvo acción sobre la acción bactericida en los bacilos no fermentadores. Esto sugiere que ciprofloxacina ejerce los mecanismos bactericidas A y B en los bacilos fermentadores y solamente el mecanismo B sobre los no fermentadores. Estos resultados podrían explicar las diferencias de acción de ciprofloxacina sobre ambos grupos de bacterias

Effect of Gasex on pharmacokinetic profile of ciprofloxacin in healthy male volunteers.

Effect of Gasex, a herbomineral formulation on the bioavailability of ciprofloxacin was studied in six healthy male volunteers. On day one, single dose of ciprofloxacin (500 mg) was given at fasting state and the plasma Concentrations of ciprofloxacin were estimated after 1, 2 and 4 hr. On day 8 ciprofloxacin (500 mg) was given along with 2 tablets of Gasex and the plasma concentrations of ciprofloxacin estimated at the same time points. No significant difference in the plasma ciprofloxacin levels was found in these two treatments, indicating that the bioavailability of ciprofloxacin was not affected by simultaneous treatment with Gasex.

Indice inhibitorio (II) e índice bactericida (IB): parámetros que favorecen la comparación de la actividad de agentes antimicrobianos / Inhibitory index (II) and bactericidal index (BI): parameters that allow antimicrobial agents activity comparison

Se define el indice inhibitorio (11) como la relación entre la concentración plasmática máxima (CMáx) que alcanza un agente antibacteriano in vivo y su actividad inhibitorio ín vitro, expresada en forma de CIM. Al mismo tiempo, el indice bactericida (IB) se define como la relación entre la CMáx del antibacteriano y su concentración bactericida mínima CBM. Se estudió la actividad inhibitoria, bactericida y la correlación entre la CMáx y la actividad inhibitoria y bactericida de ciprofioxacina, temafloxacina y tosufloxacina sobre cepas de bacilos Gram negativos multiresistentes aislados de diferentes hospitales chilenos y se calcularon los 11 y los lB. Las quinolonas demostraron una elevada actividad inhibitoria y bactericida sobre E. coli y K. pneumoniae multiresistente, pero inferior sobre bacilos Gram negativos ' no fermentadores. Ciprofloxacina mostró mayor acción sobre P. aerugínosa y tosufloxacina sobre A. baumannií. En cambio la actividad inhibitoria y bactericida fue similar para ciprofioxacina y tosufloxacina e inferior para temafloxacina. Los 11 y IB demostraron que ciprofioxacina y temafloxacina tienen actividad comparable, mientras que tosufloxacina es menos eficiente. Estos índices, al relacionar la CMáx con las actividades inhibitoria y bactericida, surgen como interesantes parámetros de comparación entre agentes antimicrobianos, permitiendo obtener una aproximación más adecuada de su probable eficacia ín vivo

Identificación de especies de enterococcus en muestras clínicas y susceptibilidad a agentes antimicrobianos / Identification of enterococcus species from clinical samples and susceptibility to antimicrobial agents

The genus enterococcus has 12 species of which, E faecalis and E faecium are most important in human infections. A progressive resistance to penicillin and ampicillin has been detected in these species. The aim of this work was to identify Enterococcus species isolated in a hospital and to study their antimicrobial susceptibility. We studied 209 Enterococcus species coming from patients admitted to a public hospital. Their susceptibility to penicillin, ampicillin, imipenem, vancomycin, tetracycline, chloramphenicol, ciprofloxacin, gentamycin and streptomycin was determined with the agar dilution technique. Eighty seven percent of species were E faecalis and 7,1 percent were E fecium, other isolated species were E hirae, E casseliflaws, E avium, E solitarius and E faecalis variant. 38 percent of these species were isolated from the urinary tract, 22 percent from the skin and 14 percent from surgical wounds. All E faecalis species were susceptible to penicillin, ampicillin, imipenem and vancomycin; 27,3 percent were susceptible to tetracycline, 54,7 percent to chloramphenicol and 80 percent to ciprofloxacin. Seventy three percent of E faecium species were susceptible to penicillin, 80 percent to ampicillin and 60 percent to imipenem. 62 percent of E faecalis and 42.4 percent of E faecium were resistant to streptomycin. It is concluded that the correct identification of Enterococcus species has therapeutic implications

Actividad inhibitoria y bactericida de ciprofloxacina, temafloxacina y tosufloxacina sobre Staphylococcus spp. Aislados en hospitales de ciudades chilenas / Inhibitory and bactericidal activity of ciprofloxacin, temafloxacin and tosufloxacin against staphylococcus isolated from chilean hospitals

Inhibitory and bactericidal activities of ciprofoxacin, temafloxacin and tosufloxacin were determined against isolates of Staphylococcus aureus and coagulase negative Staphylococci from various chilean hospitals. Time-kill experiments were performed against one selected strain of each of these bacterial isolates. Tosufloxacin showed highest activity against isolates of Staphylococci either methicillin resistant and methicillin susceptible. Ciprofloxacin was slightly less active temafloxacin

Membranas de colágeno como suporte de liberaçäo controlada de antibióticos / Collagen membranes as support the controlled release of antibiotics

Este trabalho estudou a liberação controlada dos antibióticos rolitetraciclina e ciprofloxacina suportados em membranas de colágeno. No caso de membranas com ciprofloxacina, ocorreu liberação total em 10 min, enquanto que a liberação da rolitetraciclina ocorreu durante um período de 90 min, com valores de k e n de respectivamente 0,10 e 0,48, por meio de um processo de difusão comum. Estes resultados sugerem que a rolitetraciclina suportada pode ser utilizada em periodontia e em implantes dentários.

Abstract: This work studied the controlled release of rolitetracycline and ciprofloxacine supported by collagen membranes. While ciprofloxacine was totally released within a time interval of 1 O min, rolitetracycline was released to only 73% after 90 min, with values for k and n of respectively O, 1 O and 0,48, suggesting a normal diffusion release mechanism. These results suggest that supported rolitetracyclines may be useful with periodontal and dental implant surgery

Farmacocinética y aclaramiento de ciprofloxacina y amikacina en hemodiálisis continua / Pharmacokinetics and clearence of ciprofloxacin and amikacin during continuous hemodialysis

We studied the pharmacokinetics and clearence of a 200 mg ciprofloxacin and a 500 mg amikacin intravenous dose during 5 continuous hemodialysis procedures in 5 patients with acute oliguric renal failure. Hourly blood and ultrafiltrate drug concentrations were measured during 8 hours. Dialysate flux (Qd) was 16.6 ml/min during the first hours and 33.2 ml/min thereafter. For each Qd, total ciprofloxacin clearence was 1.13ñ0.99 and 2.8ñ1.71 ml/min (p<0.001), diffusive clearence was 0.96ñ0.87 and 2.47ñ1.56 ml/min (p<0.005) and convective clearence was 0.16ñ0.17 and 0.33ñ0.2 ml/min (p<0.05). Likewise, total amikacin clearence was 3.47ñ1.31 and 4.18ñ0.53 ml/min (p<0.001), diffusive clearence was 2.97ñ1.24 and 3.86ñ0.52 ml/min and convective clearence was 0.50ñ0.47 and 0.32ñ0.29 ml/min (p=NS). Protein binding was 84 percent for ciprofloxacin and 77 percent for amikacin. It is concluded that during continuous hemodialysis with cuprofan membrane, the main transport mechanism of ciprofloxacin and amikacin is diffusive. Very low amounts of ciprofloxacin are depurated by the dialyser. Likewise, the shortening of amikacin half life suggest the presence of other elimination pathway and the need to use suplementary doses every 24 hours

Patrón de susceptibilidad a los antimicrobianos de cepas de enterococos / Pattern of antimicrobial susceptibility of enterococci strains

Enterococci resistance to antimicrobials has increased lately. We studied the susceptibility to 12 antimicrobials of 150 enterococci strains coming from hospitalized and outpatients, using the agar dilution method. Teicoplanin, followed by imipenem and amoxicilin-clavulanic acid had the lower minimal inhibitory concentrations. No strains of E faecalis was resistant to ampicillin, whereas 14 percent of E faecium had minimal inhibitory concentrations over 8 µg/ml. The high minimal inhibitory concentrations of cefpirone (64µg/ml) renders this antimicrobial useless in the treatment of enterococcal infections. Betalactamase production and resistance to glycopeptides were not detected. Antimicrobial susceptibility of strains coming for hospitalized or outpatients were similar

Evaluación prospectiva de los colirios de tobramicina-dexametasona versus ciprofloxacino-dexametasona en cuanto a penetración y tolerancia ocular / Prospective evaluation of tobramycin-dexametasone eye drops versus ciprofloxacin-dexametasone in the ocular penetration and tolerance

El colirio de tobramicina-dexametasona se utiliza frecuentemente en el postoperatorio de la catarata y la combinación de ciprofloxacino-dexametasona parece una combinación interesante por el amplio espectro del antibiótico, sin embargo nomse encuentra disponible actualmente en el mercado. El objetivo de este trabajo fue comparar la capacidad de penetración de ambos antibióticos a cámara anterior y la tolerancia postoperatoria evaluando el grado de conjuntivitis, queratitis e inflamación intraocular. Se obtuvieron muestras de 0.1 cc de humor acuoso media hora después de instilar 2 gotas de uno u otro colirio sobre la córnea y sólo se logró detectar ciprofloxacino con un promedio de 0,35 microgramos por ml. No fue posible detectar niveles de Tobramicina en ninguna de las muestras. la evaluación postoperatoria no demostró diferencias estadísticamente significativas en cuanto a tolerancia, grado de conjuntivitis, queratitis e inflamación intraocular entre ambos colirios con un P<0.05

Infecçåo urinária aguda, nåo complicada, em mulheres com mais de 18 anos, tratadas com ciprofloxacina, por três dias / Three-days treatment with ciprofloxacin for uncomplicated urinary tract infection in women over 18 years

O presente estudo mostra que o uso da ciprofloxacina 250 mg de 12/12h, por três (3) dias, em pacientes do sexo feminino, com mais de 18 anos, portadoras de infecçåo urinária baixa nåo complicada, é efetivo. O índice de cura, neste trinta (30) casos, foi de 100 por cento, comprovado por exames de urina colhidos após o 5§ dia do ínicio do tratamento. Os sintomas típicos de cistite foram apresentando reduçåo de intensidade a partir de 48 horas pós-início do tratamento, com remissåo total após o 5§ dia. Os germes encontrados foram E. coli com 86,66 por cento e Staphylococcus spo com 13,33 por cento

Sensibilidad de la Neisseria gonorrhoeae de cepas aisladas en pacientes del Hospital San Juan de Dios / Sensitivity of the strains of Neisseria gonorrhoeae isolated in patients of the San Juan de Dios Hospital

Se evalúa la sensibilidad de 28 cepas de Neisseria gonorrhoeae por la técnica de difusión en agar para cuatro antimicrobianos. Los resultados demuestran una alta resistencia a tetraciclina y penicilina con un 71,4% y 17,9% respectivamente. Frente a ciprofloxacina y cefotaxima todas las cepas estudiadas fueron sensibles

Efectividad de ciprofloxacina en infecciones respiratorias graves / Effectivenes of ciprofloxacine in severe respiratory diseases

En un estudio clínico abierto y prospectivo se incluyeron 30 pacientes adultos con diversos diagnósticos de infección respiratoria confirmada con cultivo de expectoración y/o líquido pleural. Se le administró a cada paciente ciprofloxacina en dosis de 250 mg cada 12 h por vía oral durane ocho a 15 días. La eficacia clínica se demostró en el 93% de los casos, al obtner mejoría en 43% y curación en 50% de los pacientes; en un sólo caso hubo fracaso y en otro el resultado no pudo ser valorado. La efiacia bacteriológica se verificó por la eliminación bacteriana en 27 casos (90%), en uno hubo una clara disminución en el cultivo (3.3%) en otro no fue valorable (3.3%) y en uno más persistió la infección (3.3%). La ciproflozacina fue bien tolerada por todos los pacientes.