AIM: To examine eplerenone(Inspra, Pfizer), a mineralocorticoid receptor antagonist, as a treatment option for chronic central serous chorioretinopathy(CSCR).METHODS: A retrospective consecutive case series was conduc...AIM: To examine eplerenone(Inspra, Pfizer), a mineralocorticoid receptor antagonist, as a treatment option for chronic central serous chorioretinopathy(CSCR).METHODS: A retrospective consecutive case series was conducted for patients receiving oral eplerenone for chronic CSCR. At baseline and each follow-up visit,spectral domain optical coherence tomography(SD-OCT)imaging was performed, including manual measurements of the height and diameter size of subretinal fluid. The primary outcome measure was the reduction in subretinal fluid following initiation of therapy.RESULTS: A total of 17 eyes of 13 patients treated with25 and 50 mg of oral eplerenone per day were identified.Subretinal fluid(SRF) decreased over time following eplerenone therapy(P = 0.007 and P =0.002, diameter and height respectively). Maximum SRF height decreased from a mean of 131.5 μm at baseline to 15.3 μm at day181+. SRF diameter decreased from an average of 2174.4μm at baseline to 46.9 μm at day 181 +. Log MAR visual acuity improved from 0.42(Snellen equivalent: 20/53) at baseline to 0.29(Snellen equivalent: 20/39) at day 181 +(P = 0.024). Central subfield thickness(CST) decreased from 339.5 μm at baseline to 270.3 μm at day 181+(P = 0.029).CONCLUSION: Eplerenone therapy resulted in significant anatomic and visual improvements in eyes with chronic CSCR.展开更多
To investigate the protective effects of eplerenone on adriamycin-induced renal injury and the possible mechanisms involved,36 male Sprague-Dawley rats were randomly divided into control group,adriamycin nephropathy...To investigate the protective effects of eplerenone on adriamycin-induced renal injury and the possible mechanisms involved,36 male Sprague-Dawley rats were randomly divided into control group,adriamycin nephropathy（AN） group and eplerenone-treated group（100 mg.kg-1.d-1 eplerenone）.Blood pressure,24-h urinary protein,serum potassium,sodium and creatinine were measured 28 days after adriamycin injection（a single tail intravenous injection of 6.5 mg/kg adriamycin）.The morphological changes of renal tissues were observed by light and electron microscopy.Immunohistochemistry and Western blotting were performed to examine the expression of TGF-β1 and desmin in renal cortex.The results showed that 28 days after adriamycin injection,there were no significant changes in the level of serum potassium,sodium,creatinine concentrations and blood pressure values in the rats of the three groups.Meanwhile,the 24-h proteinuria excretion in the AN group was significantly higher than that in the control group（P0.01）,but that in the eplerenone-treated group was substantially reduced when compared with that in the AN group（P0.05）.Mild mesangial cell proliferation and matrix expansion,diffuse deformation and confluence of foot processes in podocytes were found in the AN group.By contrast,rats in the eplerenone-treated group exhibited obvious attenuation of these morphological lesions.The protein expression of TGF-β1 and desmin in the AN group was markedly up-regulated in contrast to that in the control group（P0.01）,whereas that in the eplerenone-treated group was much lower than in the AN group（P0.05）.It was concluded that eplerenone may ameliorate the proteinuria and the development of pathological alteration in adriamycin-induced nephropathy presumably via the inhibition of cytokine release,and restore the morphology of podocytes independent of its blood pressure-lowing effects.展开更多
A rapid and simple high performance liquid chromatography （HPLC） mcthod wiih a UV detection （241 nm） was developed and validated for estimation of eplerenone from spiked human plasma. The analyte and the internal ...A rapid and simple high performance liquid chromatography （HPLC） mcthod wiih a UV detection （241 nm） was developed and validated for estimation of eplerenone from spiked human plasma. The analyte and the internal standard （valdecoxib） were extracted with a mixture of dichloromethane and diethyl ether. The chromatographic separation was performed on a HiQSil C-18HS column （250 mm × 4.6 mm, 5 um） with a mobile phase consisting of acetonitrile：water （50：50, v/v） at flow rate of 1 mL/min. The calibration curve was linear in the range 100 3200 ng/mL and the heteroscedasticity was minimized by using weighted least squares regression with weighting factor I/X.展开更多
文摘AIM: To examine eplerenone(Inspra, Pfizer), a mineralocorticoid receptor antagonist, as a treatment option for chronic central serous chorioretinopathy(CSCR).METHODS: A retrospective consecutive case series was conducted for patients receiving oral eplerenone for chronic CSCR. At baseline and each follow-up visit,spectral domain optical coherence tomography(SD-OCT)imaging was performed, including manual measurements of the height and diameter size of subretinal fluid. The primary outcome measure was the reduction in subretinal fluid following initiation of therapy.RESULTS: A total of 17 eyes of 13 patients treated with25 and 50 mg of oral eplerenone per day were identified.Subretinal fluid(SRF) decreased over time following eplerenone therapy(P = 0.007 and P =0.002, diameter and height respectively). Maximum SRF height decreased from a mean of 131.5 μm at baseline to 15.3 μm at day181+. SRF diameter decreased from an average of 2174.4μm at baseline to 46.9 μm at day 181 +. Log MAR visual acuity improved from 0.42(Snellen equivalent: 20/53) at baseline to 0.29(Snellen equivalent: 20/39) at day 181 +(P = 0.024). Central subfield thickness(CST) decreased from 339.5 μm at baseline to 270.3 μm at day 181+(P = 0.029).CONCLUSION: Eplerenone therapy resulted in significant anatomic and visual improvements in eyes with chronic CSCR.
基金supported by grants from the National Natu-ral Sciences Foundation of China (Nos. 30500245, 30871174, and 31050110433)a Medicine-technology Interdiscipline grant from Huazhong University of Science and Technology (No. 2010JC041)
文摘To investigate the protective effects of eplerenone on adriamycin-induced renal injury and the possible mechanisms involved,36 male Sprague-Dawley rats were randomly divided into control group,adriamycin nephropathy（AN） group and eplerenone-treated group（100 mg.kg-1.d-1 eplerenone）.Blood pressure,24-h urinary protein,serum potassium,sodium and creatinine were measured 28 days after adriamycin injection（a single tail intravenous injection of 6.5 mg/kg adriamycin）.The morphological changes of renal tissues were observed by light and electron microscopy.Immunohistochemistry and Western blotting were performed to examine the expression of TGF-β1 and desmin in renal cortex.The results showed that 28 days after adriamycin injection,there were no significant changes in the level of serum potassium,sodium,creatinine concentrations and blood pressure values in the rats of the three groups.Meanwhile,the 24-h proteinuria excretion in the AN group was significantly higher than that in the control group（P0.01）,but that in the eplerenone-treated group was substantially reduced when compared with that in the AN group（P0.05）.Mild mesangial cell proliferation and matrix expansion,diffuse deformation and confluence of foot processes in podocytes were found in the AN group.By contrast,rats in the eplerenone-treated group exhibited obvious attenuation of these morphological lesions.The protein expression of TGF-β1 and desmin in the AN group was markedly up-regulated in contrast to that in the control group（P0.01）,whereas that in the eplerenone-treated group was much lower than in the AN group（P0.05）.It was concluded that eplerenone may ameliorate the proteinuria and the development of pathological alteration in adriamycin-induced nephropathy presumably via the inhibition of cytokine release,and restore the morphology of podocytes independent of its blood pressure-lowing effects.
文摘A rapid and simple high performance liquid chromatography （HPLC） mcthod wiih a UV detection （241 nm） was developed and validated for estimation of eplerenone from spiked human plasma. The analyte and the internal standard （valdecoxib） were extracted with a mixture of dichloromethane and diethyl ether. The chromatographic separation was performed on a HiQSil C-18HS column （250 mm × 4.6 mm, 5 um） with a mobile phase consisting of acetonitrile：water （50：50, v/v） at flow rate of 1 mL/min. The calibration curve was linear in the range 100 3200 ng/mL and the heteroscedasticity was minimized by using weighted least squares regression with weighting factor I/X.
