A bullous variant of central serous chorioretinopathy treated with oral spironolactone / Uma variante bolhosa da coriorretinopatia serosa central tratada com espironolactona oral

ABSTRACT We report the case of a 39-year-old male patient who presented with visual loss in the right eye for 6 weeks. The best-corrected visual acuity was counting fingers in the right eye and 20/30 in the left eye. The fundus examination demonstrated a right retinal detachment inferiorly extending to the fovea and a left macular serous detachment. After multimodal imaging study, the patient was diagnosed as having a bullous variant of central serous chorioretinopathy and treated with oral spironolactone associated with adjuvant laser photocoagulation. The retinal changes resolved after 6 months. The final visual acuity was 20/20 in both eyes.

RESUMO Relatamos o caso de um homem de 39 anos apresentando perda visual no olho direito há seis semanas. A melhor acuidade visual corrigida foi conta-dedos no olho direito e 20/30 no esquerdo. A fundoscopia demonstrou descolamento de retina direito inferiormente com extensão à fóvea e descolamento macular seroso à esquerda. Após estudos de imagem multimodal, o paciente foi diagnosticado com uma variante bolhosa de coriorretinopatia serosa central e tratado com espironolactona oral associada à fotocoagulação a laser adjuvante. As alterações retinianas resolveram após seis meses. A acuidade visual final foi 20/20 em ambos os olhos.

Nueva evidencia en el tratamiento de la enfermedad renal diabética: ¿qué aporta la finerenona?

Contexto: la enfermedad renal diabética (ERD) es la primera causa a nivel mundial de enfermedad renal crónica (ERC) e impacta directamente en el riesgo cardiovascular y mortalidad de los pacientes con diabetes mellitus (DM). La finerenona, un antagonista selectivo del receptor mineralocorticoide (ARM), ha sido descrito en diversos estudios recientes como un fármaco que contribuye a la reducción de la progresión de la ERD y la disminución del riesgo cardiovascular, con un adecuado perfil de seguridad. Objetivo: realizar una revisión de la literatura sobre el impacto de la finerenona en la progresión del daño renal y el riesgo cardiovascular en los pacientes con ERD. Metodología: se realizó una búsqueda sistemática en diversas fuentes: PubMed (Medline, Biblioteca del Congreso de los Estados Unidos), Science Direct, Scopus, Embase y Lilacs; la búsqueda fue restringida a referencias en idioma español e inglés, sin límites en la fecha de publicación. Se utilizaron las siguientes palabras clave en el idioma inglés: diabetic renal disease, chronic kidney disease, diabetes mellitus, spironolactone, eplerenone, finerenone, mineralocorticoid receptor antagonist y sus correspondientes versiones en español. Resultados: Las referencias encontradas en la búsqueda fueron revisadas entre los diferentes autores para, posteriormente, proceder a realizar la elaboración del documento. Conclusiones: la finerenona es un medicamento que brinda cardio y nefroprotección en pacientes con ERD de fenotipo albuminúrico.

Background: Diabetic kidney disease (DKD) is the leading cause of chronic kidney disease (CKD) worldwide and has a direct impact on cardiovascular risk and mortality in patients with diabetes mellitus (DM). Finerenone, a selective mineralocorticoid receptor (MRA) antagonist, has been described in several recent studies as a drug that contributes to slowing the progression of CKD and reducing cardiovascular risk, with an adequate safety profile. Purpose: To carry out a review of the literature on the impact of finerenone on the progression of renal damage and cardiovascular risk in patients with DKD. Methodology: A systematic search were carried out in various sources: PubMed (Medline, United States Library of Congress), Science Direct, Scopus, Embase and Lilacs; the search was restricted to references in Spanish and English, with no limits on publication date. The following keywords in the English language were used: diabetic renal disease, chronic kidney disease, diabetes mellitus, spironolactone, eplerenone, finerenone, mineralocorticoid receptor antagonist and their corresponding Spanish versions. Results: The references found in the search were reviewed among the different authors to subsequently proceed to prepare the document. Conclusions: Finerenone is a drug that provides cardio and nephroprotection in patients with DKD albuminuric phenotype.

Effect of spironolactone with angiotensin receptor blocker on albuminuria in type 2 diabetic patients with nephropathy

Background:Diabetic nephropathy is the most important cause of the end-stage renal disease (ESRD). The aim of the study is to evaluate the effect of spironolactone 25 mg once daily in addition to losartan 50 mg once daily for 12 weeks for proteinuria reduction in diabetic nephropathy. Methods:This is a prospective clinical trial was carried out in the department of nephrology, national institute of kidney diseases and urology (NIKDU), Dhaka, Bangladesh from March 2015 to April 2016. A total of 60 patients attended the study considering inclusion and exclusion criteria. Proper ethical consent was taken from the relevant. Collected data were classified, edited, and analyzed into the computer for statistical analysis using SPSS version 22. Results:The mean serum creatinine baseline, end of 1st, 4th, 8th,and 12thweeks were significantly low (p<0.05) in the control group and significantly decline (p<0.05) in subsequent follow-up in both Intervention and control groups. The mean serum potassium-baseline, end of 1st, 4th, 8th,and 12weeks were not statistically significant (p>0.05) and significantly increased (p<0.05) in both groups. Improvement of urine albumin creatinine ratio was found 96.7% and 83.3% at end of 12thweeks in both groups respectively. It was observed that mean eGFR-baseline, endof 4thand 12thweeks were statistically significantly higher (p<0.05) in both groups with baseline. Conclusions:The addition of spironolactone 25 mg once daily with losartan potassium 50 mg daily for a 12-week period did not show a significant role in the reduction of proteinuria in diabetic nephropathy patients.

Tratamiento del hiperaldosteronismo primario durante el embarazo: reporte de un caso / Management of primary hyperaldosteronism during pregnancy: Case report

Resumen ANTECEDENTES: El hiperaldosteronismo primario es la principal causa de hipertensión arterial de origen endocrino en la población general; su manifestación durante el embarazo es poco frecuente, casi siempre provocado por un adenoma adrenal productor de aldosterona. De 1962 a la fecha se han descrito alrededor de 50 casos. Objetivo: Reportar un caso de hiperaldosteronismo durante el embarazo y revisar la bibliografía relacionada. CASO CLÍNICO: Paciente de 39 años, con antecedente médico de hipertensión arterial, en curso del segundo trimestre del quinto embarazo, que acudió a consulta por hipertensión no controlada e hipocalemia. El tratamiento incluyó un antagonista del receptor de aldosterona, que permitió el control de la tensión arterial y la finalización del embarazo. Posteriormente se identificó un nódulo adrenal, cuya resección resultó en normalización de las concentraciones de aldosterona, la actividad de renina plasmática, calemia y remisión de la hipertensión hasta la actualidad. CONCLUSIÓN: Las recomendaciones para el tratamiento de pacientes con hiperaldosteronismo durante el embarazo se basan en los casos publicados y los datos de toxicidad generados de estudios en animales. De ahí la importancia de este caso, que aporta información importante y puede considerarse en situaciones similares.

Abstract BACKGROUND: Primary hyperaldosteronism is the main cause of arterial hypertension of endocrine origin in the general population; its presentation during pregnancy is infrequent; having described about 50 cases since 1962, the most common cause is the presence of an adrenal adenoma. OBJECTIVE: To report the first case of hyperaldosteronism treated during pregnancy in Peru and reviews the literature. CLINICAL CASE: A 39-year-old patient with a history of arterial hypertension and poor obstetric history, who was referred to our center in the second trimester of the 5th pregnancy due to uncontrolled hypertension and symptomatic hypokalemia. Management included an aldosterone receptor antagonist, allowing the control of blood pressure and the culmination of the pregnancy with the delivery of a healthy girl. Subsequently, the presence of an adrenal nodule was confirmed, the resection of which resulted in normalization of aldosterone concentration, plasma renin activity, kalemia, and remission of hypertension to date. CONCLUSION: Recommendations on the management of hyperaldosteronism during pregnancy are based only on published cases and drug toxicity data were generated in animal studies. Hence the importance of this report, which provides information that can be considered in similar situations.

Comparison of the anti-androgen effects of cyproterone acetate and spironolactone on male-to-female transsexuals / 中华医学美学美容杂志

Objective:To compare the anti-androgenic effect of cyproterone acetate (CPA) and spironolactone (SPL) on male-to-female transsexuals.Methods:From January 2012 to September 2021, 185 male-to-female transsexuals (95 using CPA and 90 using SPL) who visited the Peking University Third Hospital and under stable medication for ≥3 months were enrolled, aged 16 to 40 (23±5) years. General information and laboratory indicators of the last visit were collected for a cross-sectional study.Results:The median doses of antiandrogens in the CPA group and SPL group were 25 mg/d and 80 mg/d, respectively. And the median dose of oral estradiol valerate in both groups was 2 mg/d. Testosterone level in the CPA group was significantly lower than the SPL group [0.7 (0.7-1.5) nmol/L vs. 13.2(6.7-18.4) nmol/L, U= 6 970.500, P<0.001]. The CPA group also had better subjective effects on testicular atrophy, erection decrease, body hair decrease, skin softening and figure feminization (all P<0.05). The prolactin level of CPA group was significantly higher than that of SPL group [21.5 (12.6-30.1) ng/ml vs. 11.9 (7.7-20.0) ng/ml, U= 2 053.500, P<0.001]. Conclusions:CPA has a more significant effect on lowering testosterone levels than SPL, and is better than SPL in terms of testicular atrophy, erection decrease, body hair decrease, skin softening and figure feminization, albeit with a potentially higher risk of hyperprolactinemia.

Hipertensão resistente: análise dos estudos pathway 2 e 3 / Resistant hypertension: analysis of pathway 2 and 3 studies

A hipertensão arterial resistente (HAR) é definida quando, apesar do tratamento com pelo menos três medicações anti- -hipertensivas (incluindo um diurético) de diferentes classes a meta pressórica não é alcançada. Nesta sequência de fármacos, por muitos anos se utilizou empiricamente ou baseado em pequenos estudos, a espironolactona. Os estudos Pathway 2 e 3 vieram para corroborar a importância deste quarto fármaco, a espironolactona, como o mais eficaz em termos de potencia anti-hipertensiva, como também explicar os aspectos fisiopatológicos que levam o hipertenso a ficar resistente. Nesta revisão e análise crítica dos fármacos anti-hipertensivos na HAR destacamos os principais mecanismos envolvidos no não controle da pressão e as estratégias para um melhor controle pressórico

Resistant arterial hypertension (RAH) is defined when, despite treatment with at least three antihypertensive medications (including a diuretic) of different classes, the pressure target is not achieved. In this sequence of drugs, for many years it was used empirically or based on small studies, spironolactone. Pathway 2 and 3 studies have come to corroborate the importance of this fourth drug, spironolactone, as the most effective in terms of antihypertensive potency, as well explain the pathophysiological aspects that lead hypertensive patients to become resistant. In this review and critical analysis of antihypertensive drugs in hypertension, we highlight the main mechanisms involved in the lack of pressure control and the strategies for better pressure control

Espironolactona ou clonidina como quarto fármaco na hipertensão resistente? / Spironolactone or clonidine as the fourth drug to treat resistant hypertension?

A hipertensão arterial resistente (HAR) é definida como a ausência de controle pressórico nas medidas de pressão arterial (PA) de consultório a despeito do uso de três ou mais anti-hipertensivos em doses adequadas, incluindo-se preferencialmente um diurético, ou o controle pressórico atingido às custas do uso de quatro ou mais medicamentos. O uso de espironolactona, um antagonista dos receptores de aldosterona, como quarto fármaco no tratamento da HAR é indicado pelas principais diretrizes sobre o assunto, e tem a sua eficácia comprovada em ensaios clínicos e meta análises. Um estudo comparou o uso de clonidina, um agonista adrenérgico alfa-2, como quarto fármaco para tratamento da HAR em comparação com a espironolactona. Embora o desfecho primário (taxa de controle da PA no consultório ou na medida ambulatorial da PA) tenha sido similar com as duas medicações, a espironolactona mostrou maior redução na PA de 24h quando comparada à clonidina. Neste contexto, a clonidina pode ser uma alternativa à espironolactona, particularmente em grupos específicos de pacientes que tenham contraindicação ao uso de espironolactona, como os que apresentam hipercalemia ou doença renal crônica pré dialítica.

Resistant Hypertension (RH) is defined as the absence of blood pressure (BP) control despite the use of three antihypertensive drugs in adequate doses, or the achievement of BP control with the use of four or more medications. The use of spironolactone, an antagonist of aldosterone receptors, as the fourth medication in the treatment of RH is recommended by current Management of Hypertension Guidelines, and its efficacy has been proved in clinical trials and meta-analysis. One clinical trial compared the use of clonidine, an adrenergic alpha-2 agonist, versus spironolactone as an option as the fourth drug in the treatment of RH. The results showed similar rates of the primary outcome (BP control at the office and at ambulatory monitoring) with both drugs, although spironolactone promoted greater reduction in 24h BP when compared with clonidine. In this context, clonidine can be used as an alternative to spironolactone, particularly among specific groups of patients that have contraindications to the use of spironolactone, such as patients with hyperkalemia or end stage renal disease.

Oral Spironolactone Treatment in Chronic Central Serous Chorioretinopathy

PURPOSE: To evaluate the effect of oral spironolactone for non-resolving chronic central serous chorioretinopathy after intravitreal bevacizumab injection.METHODS: Seventeen eyes of 17 patients with non-resolving chronic central serous chorioretinopathy after intravitreal bevacizumab injection from September 2017 to December 2018 were treated with oral spironolactone for 6 months, and changes in central macular thickness, subretinal fluid height, and best-corrected visual acuity (BCVA) were analyzed retrospectively.RESULTS: The central macular thickness decreased from 309.94 ± 105.20 µm at baseline to 259.76 ± 81.83 µm at 3 months, and 243.11 ± 61.98 µm at 6 months, which were both statistically significant (Wilcoxon signed-rank test, p = 0.016 and p = 0.001, respectively). The subretinal fluid height decreased from 138.05 ± 95.69 µm at baseline to 70.88 ± 83.13 µm at 3 months, and 54.00 ± 56.25 µm at 6 months, which were both statistically significant (Wilcoxon signed-rank test, p = 0.002 and p = 0.000, respectively). The BCVA (LogMAR) changed from 0.30 ± 0.38 at baseline to 0.35 ± 0.43 at 1 month, 0.29 ± 0.43 at 3 months, and 0.26 ± 0.40 at 6 months. The results at 6 months were statistically significant (Wilcoxon signed-rank test, p = 0.033). There were no side effects in patients treated with oral spironolactone.CONCLUSIONS: In chronic central serous chorioretinopathy, treatment with oral spironolactone significantly reduced the central macular thickness, subretinal fluid height, and the BCVA, without side effects.

Preparation and Preliminary Stability Tests of Extemporaneously Prepared Oral Suspending Vehicle for Children / 中国药学杂志

OBJECTIVEP: To prepare the extemporaneously prepared oral suspending vehicle that can be used in divided doses for children, and preliminary stability experiments are performed. METHODS: Preparation of blank suspending vehicle by prescription screening and optimization. The preparation of suspending vehicle is based on the comprehensive scale of viscosity, redispersibility and appearance traits as the evaluation index, and signal factor study is used. The preliminary stability investigation was carried out.Using propranolole hydrochloride and spironolactone as model drugs, the drug concentration in suspension determined by ultraviolet spectrophotometry and high performance liquid chromatography(HPLC) respectively,which are methods prescribed in Chinese Pharmacopoeia. RESULTS: The dosages of CMC-Na, HPMC, xanthan gum and xylitol in the final formulation of suspension medium were 3.33% (g•mL-1), 1.67% (g•mL-1), 1% (g•mL-1) and 0.1% (g•mL-1),respectively. The extemporaneously prepared oral suspension is uniform, stable and dispersed, and the inspection conforms to the relevant regulations. Average recovery rates of propranolole hydrochloride and spironolactone are meet the relevant regulations. No stratification in the appearance of samples in centrifugal tests. Three batches of test samples remained stable at 4 and 25℃ for 10 d. CONCLUSION: The oral suspending vehicle has a simple and convenient preparation process, the drug dispersion is simple and fast, the content determination method is accurate and reliable, and the stability is good,and can be used as a drug-loading vehicle.

Antagonistas de mineralocorticoides en coriorretinopatía central serosa crónica / Mineralocorticoid receptor antagonists in chronic central serous chorioretinopathy

INTRODUCCIÓN: La coriorretinopatía central serosa consiste en la filtración de fluido desde la coroides y su acumulación en el espacio subretinal. Su forma crónica se asocia a pérdida visual permanente. Los antagonistas de mineralocorticoides son una alternativa de tratamiento para esta patología, aunque no existe evidencia clara sobre su efectividad. MÉTODOS: Realizamos una búsqueda en Epistemonikos, la mayor base de datos de revisiones sistemáticas en salud, la cual es mantenida mediante el cribado de múltiples fuentes de información, incluyendo MEDLINE, EMBASE, Cochrane, entre otras. Extrajimos los datos desde las revisiones identificadas, analizamos los datos de los estudios primarios, realizamos un metanálisis y preparamos una tabla de resumen de los resultados utilizando el método GRADE. RESULTADOS Y CONCLUSIONES: Identificamos tres revisiones sistemáticas que en conjunto incluyeron 22 estudios primarios, de los cuales, cuatro corresponden a ensayos aleatorizados. Concluimos que el uso de antagonistas de mineralocorticoides en coriorretinopatía central serosa crónica probablemente resulta en poca o nula diferencia en la agudeza visual corregida. No es posible establecer con claridad si su uso disminuye el grosor del fluido subretinal, debido a que la certeza de la evidencia ha sido evaluada como muy baja. Además, esta intervención podría resultar en poca o nula diferencia en la aparición de efectos adversos, pero la certeza de la evidencia es baja.

INTRODUCTION: Central serous chorioretinopathy consists of the leakage of fluid from the choroid and its accumulation into the subretinal space. Its chronic form is associated with permanent vision loss. Mineralocorticoid receptor antagonists are an alternative treatment for this condition, although there is no clear evidence about their effectiveness. METHODS: We searched in Epistemonikos, the largest database of systematic reviews in health, which is maintained by screening multiple information sources, including MEDLINE, EMBASE, Cochrane, among others. We extracted data from the systematic reviews, reanalyzed data of primary studies, conducted a meta-analysis and generated a summary of findings table using the GRADE approach. RESULTS AND CONCLUSIONS: We identified three systematic reviews including 22 studies overall and four of them are randomized trials. We concluded that in chronic central serous chorioretinopathy, mineralocorticoid receptor antagonists probably make little or no difference to best-corrected visual acuity. We are uncertain whether this intervention reduces subretinal fluid height because the certainty of the evidence is very low. Furthermore, this intervention may make little or no difference in terms of adverse effects, but the certainty of the evidence is low.

Effect of spironolactone on the progression of coronary calcification in peritoneal dialysis patients: a pilot study / Efeito da espironolactona na progressão da calcificação coronariana em pacientes em diálise peritoneal: um estudo piloto

ABSTRACT Introduction: There is evidence that aldosterone plays a role in the pathogenesis of vascular calcification. The aim of this study was to evaluate the effect of spironolactone, a mineralocorticoid receptor antagonist, on the progression of coronary calcification (CC) in peritoneal dialysis patients and to identify the factors involved in this progression. Methods: Thirty-three patients with a coronary calcium score (CCS) ≥ 30, detected through multi-detector computed tomography (MDCT) and expressed in Agatston units, were randomly assigned to a group receiving 25mg spironolactone per day for 12 months (spironolactone group) and a control group not receiving this drug. The primary outcome was a percentage change in CCS from baseline to end of the study (relative progression), when a further MDCT was conducted. Patients who had progression of CC were compared with those who did not progress. Results: Sixteen patients, seven in the spironolactone group and nine in the control group, concluded the study. The relative progression of the CCS was similar in both groups, 17.2% and 27.5% in the spironolactone and control groups respectively. Fifty-seven percent of the treated patients and 67% of those in the control group presented progression in the CC scores (p = 0.697). Progressor patients differed from non-progressors because they presented higher levels of calcium and low-density lipoprotein cholesterol and lower levels of albumin. Conclusion: In peritoneal dialysis patients, spironolactone did not attenuate the progression of CC. However, large-scale studies are needed to confirm this observation. Disorders of mineral metabolism and dyslipidemia are involved in the progression of CC.

RESUMO Introdução: Existem evidências de que a aldosterona exerça um papel na patogênese da calcificação vascular. O objetivo deste estudo foi avaliar o efeito da espironolactona, um antagonista do receptor mineralocorticoide, na progressão da calcificação coronariana (CC) de pacientes em diálise peritoneal, e identificar os fatores envolvidos nessa progressão. Métodos: Trinta e três pacientes com escore de cálcio coronariano (ECC) ≥ 30, detectado por tomografia computadorizada com múltiplos detectores (TCMD) e expresso em unidades de Agatston, foram randomizados para um grupo que recebeu 25 mg de espironolactona por dia durante 12 meses (grupo espironolactona) e um grupo controle que não recebeu este medicamento. O desfecho primário foi a mudança percentual do ECC do início para o final do estudo (progressão relativa), quando uma nova TCMD foi realizada. Os pacientes que tiveram progressão de CC foram comparados com aqueles que não progrediram. Resultados: Dezesseis pacientes, sete no grupo espironolactona e nove no grupo controle, concluíram o estudo. A progressão relativa do ECC foi semelhante nos dois grupos, 17,2% e 27,5% nos grupos espironolactona e controle, respectivamente. Cinquenta e sete por cento dos pacientes tratados e 67% daqueles no grupo controle apresentaram progressão nos escores de CC (p = 0,697). Os pacientes progressores diferiram dos não progressores porque apresentaram níveis séricos mais elevados de cálcio e LDL-colesterol e menores níveis de albumina. Conclusão: Em pacientes em diálise peritoneal, a espironolactona não atenuou a progressão da CC. No entanto, estudos em grande escala são necessários para confirmar essa observação. Distúrbios do metabolismo mineral e dislipidemia estão envolvidos na progressão da CC.

Actualización en el manejo clínico de la hipertensión hiporreninémica / Update in the clinical management of low renin hypertension

The renin-angiotensin-aldosterone system modulates volume, sodium and potassium homeostasis. In the setting of a high sodium diet, up to 30% of patients with hypertension have a low or suppressed renin and increased volume. This phenotype of low renin hypertension (LRH) is multifactorial and includes infrequent inherited genetic syndromes, milder phenotypes of classic diseases and environmental exposures. All these conditions have in common a higher cardiovascular risk mediated by the over activation of the mineralocorticoid receptor (MR), present not only in the kidney, but also in vasculature, myocardium and adipocytes. Consequently, the aim of LRH treatment goes beyond the control of blood pressure and requires antagonizing MR with specific pharmacologic agents, pursuing normalization of renin as a clinical objective. Due to the unusual evaluation of renin status by non-endocrinologists and lack of disease awareness, only a minority of hypertensive patients receive this pathophysiologically-driven treatment that should reduce cardiovascular outcomes.

Efficacy of triple diuretic treatment in continuous ambulatory peritoneal dialysis patients: A randomized controlled trial

BACKGROUND: The efficacy of combined diuretic treatment in patients undergoing continuous ambulatory peritoneal dialysis (CAPD) is not known. METHODS: In a single-center, double-blinded, randomized controlled trial, we randomly assigned 51 adult CAPD patients to receive furosemide 1,000 mg/day, hydrochlorothiazide 100 mg/day, and spironolactone 50 mg/day (triple diuretics [TD] group) or furosemide 1,000 mg/day plus placebo (single diuretic [SD] group) for 6 months. The primary outcome was the difference in daily urine output at the 3rd and 6th month of the study compared to baseline (ΔUO) between the SD and TD group. Secondary outcomes were urinary sodium (UNa) and potassium (UK) excretion and overhydration (OH) measured by bioimpedance at 3 and 6 months compared to baseline (ΔUNa, ΔUK, and ΔOH, respectively) and daily glucose exposure (g/day). RESULTS: Forty-three of 51 patients completed the 6-month trial. The ΔUO at 3 and 6 months was significantly higher in the TD group compared to the SD group (386.32 ± 733.92 mL/day vs. −136.25 ± 629.08 mL/day, P < 0.001, at 3 months; 311.58 ± 640.31 mL/day vs. 120.00 ± 624.07 mL/day, P < 0.001, at 6 months) but there was no significant difference in ΔUNa and ΔUK excretion. Hydration status was significantly better in the TD group (ΔOH 1.84 ± 2.27 L vs. 0.44 ± 1.62 L, P = 0.03, at 3 months; 1.49 ± 2.82 L vs. −0.48 ± 2.61 L, P = 0.02, at 6 months). There was no serious adverse event in this study. CONCLUSION: For end-stage renal disease patients on CAPD, the combination of furosemide, hydrochlorothiazide, and spironolactone results in higher urine output and better volume control compared to furosemide alone.

Improvement of in vitro dissolution and physical stability for spironolactone solid dispersion formulated with Soluplus / 药学学报

Spironolactone, a class II drug of the biopharmaceutics classification system, has low oral bioavailability due to poor solubility. Spironolactone solid dispersions were prepared using the solvent method in order to improve its aqueous solubility. Optimization studies of spironolactone solid dispersions were performed using in vitro dissolution tests. Differential scanning calorimetry, X-ray diffraction and Fourier transform infrared were used to investigate the physical state of the drug in carrier materials and to detect the possible interactions between the drug and carrier materials in the solid dispersions. In addition, stress tests were employed to elucidate the key factors which have influence on the stability of the spironolactone solid dispersions. Results showed that spironolactone in the solid dispersions formulated with Soluplus and HPMC-E5 were both in amorphous state and the hydrogen bonds between the drug and carrier materials were formed in the solid dispersion. Therefore, the in vitro dissolution of spironolactone was also significantly enhanced. Stress tests demonstrated that the physical stability of spironolactone solid dispersions prepared with Soluplus was greatly improved compared to those formulated with HPMC-E5. Thus, spironolactone solid dispersion formulated with Soluplus using the solvent method could be used to improve the in vitro dissolution and stability of poorly soluble drugs.

Influence of endothelial progenitor cells mobilized by spironolactone on cardiac function in patients with myocardial infarction / 心血管康复医学杂志

Objective :To explore mobilizing effect of spironolactone by spironolactone on peripheral blood endothelial progenitor cells (EPCs) in patients with acute myocardial infarction ,and its impact on cardiac function .Methods :A total of 136 patients with acute ST elevation myocardial infarction treated in our department were randomly and e‐qually divided into routine treatment group and spironolactone group (received spironolactone 20mg／time ,once／d based on routine treatment group ) ,both groups were treated for three months .Peripheral blood EPCs level before and 7d after treatment ,cardiac function indexes before and three months after treatment were compared between two groups.Results :After 7d treatment ,peripheral blood EPCs level in spironolactone group was significantly high‐er than that of routine treatment group [ (1. 12 ± 0. 26)% vs.(0.53 ± 0. 14)%, P＝0. 001].Compared with routine treatment group after three‐month treatment ,there was significant rise in LVEF [ (51. 47 ± 8.23)% vs.(56. 52 ± 8.84)%] ,and significant reductions in LVESd [(34. 52 ± 3. 16) mm vs.(32.90 ± 2. 68) mm] and LVEDd [(57. 82 ± 8.13) mm vs.(53. 65 ± 7.22) mm] in spironolactone group , P＜0. 01 all.There was no significant difference in incidence rate of adverse reactions between two groups , P＝0. 595. Conclusion :Spironolactone can significantly in‐crease peripheral blood EPCs level and cardiac function ,and inhibit myocardial remodeling in AMI patients .

Influence of Rho kinase inhibitor combined furosemide and spironolactone on cardiac function , serum levels of AST , LDH and CK‐MB in patients with acute left heart failure／ / 心血管康复医学杂志

To explore application value of Rho kinase inhibitor (RKI) combined furosemide and spironolactone in patients with acute left heart failure (ALHF).Methods : A total of 94 ALHF patients were randomly and equally divided into diuretic group (received furosemide and spironolactone based on routine treatment ) and triple therapy group (received RKI‐‐fasudil hydrochloride based on diuretic group ) , both groups were continuously treated for 7d.LVESV , LVEDV , LVEF ,serum levels of aspartate transaminase (AST) , lactate dehydrogenase (LDH) and creatine kinase isoenzyme MB (CK‐MB) before and after treatment , therapeutic effects were observed and compared between two groups .Results : Total effective rate of triple therapy group was significantly higher than that of diuretic group (95.75% vs.82.98%) , P＝0.045. Compared with before treatment , there was significant rise in LVEF , and significant reductions in LVESV , LV‐EDV ,serum levels of AST , LDH and CK‐MB in two groups after treatment , P＝0.001 all ;compared with diuretic group after treatment , there was significant rise in LVEF [ (48.27 ± 5.95)% vs.(55.14 ± 6.74)%] , and significant reductions in LVESV [ (86.29 ± 10.41) ml vs.(65.96 ± 9.84) ml] , LVEDV [ (133.71 ± 13.42) ml vs.(120.35 ± 11.25) ml] , serum levels of AST [ (81.23 ± 10.44) U／L vs.(57.58 ± 8.42) U／L] , LDH [ (184.24 ± 13.51) U／Lvs.(124.65 ± 12.42) U／L] and CK‐MB [ (187.84 ± 13.45) U／L vs.(132.54 ± 11.69) U／L] in triple therapy group , P＝0.001 all. There was no significant difference in adverse reactions during treatment between two groups , P＞0.05 both .Conclusion :Rho kinase inhibitor combined furosemide and spironolactone can significantly improve cardiac function and reduce myocar ‐dial damage , and it＇s safe and reliable , which is worth extending .

Therapeutic effect of spironolactone on aged CHD + CHF patients and its influence on BNP and cardi-ac function / 心血管康复医学杂志

Objective :To explore therapeutic effect of spironolactone on aged patients with coronary heart disease (CHD) complicated chronic congestive heart failure (CHF ) and its influence on level of brain natriuretic peptide (BNP) and cardiac function .Methods : A total of 96 aged CHD + CHF patients treated in our hospital were ran-domly and equally divided into routine treatment group and spironolactone group ,both groups were treated for three months.Therapeutic effect ,plasma BNP level and cardiac function before and after treatment were observed and compared between two groups .Results : After three-month treatment ,total effective rate of spironolactone group was significantly higher than that of routine treatment group (95-8% vs.72-9%,P＝0-002).Compare with before treatment , there were significant reductions in plasma BNP level and left ventricular end-diastolic dimension (LVEDd) ,and significant rise in left ventricular ejection fraction (LVEF) in two groups after three-month treat-ment , P＜ 0-01 all ;compared with routine treatment group after treatment ,there were significant reductions in plasma BNP level [ (440-11 ± 76-90) ng／L vs.(359-21 ± 51-21 ) ng／L ] and LVEDd [ (62-91 ± 3-90 ) mm vs. (59-12 ± 2-38) mm] ,and significant rise in LVEF [ (43-23 ± 5-80)% vs.(49-46 ± 5-98)%] in spironolactone group , P＝0-001 all .Incidence rate of complications in spironolactone group was significantly lower than that of routine treatment group (8-3% vs.22-9%, P＝0-049).Conclusion : Spironolactone possesses significant therapeu-tic effect on aged CHD + CHF patients .It can significantly reduce plasma BNP level and improve cardiac function , which is worth extending .

Efficacy of low-dose spironolactone on top of angiotensin receptor blockade in patients with glomerulonephritis

BACKGROUND: Previous studies have shown that aldosterone antagonists have a proteinuria-lowering effect in patients with proteinuria and progressive proteinuric disease not adequately controlled by the use of angiotensin receptor blockers (ARBs). Aldosterone antagonists, in combination with ARBs, might improve proteinuria in patients with glomerulonephritis (GN). METHODS: In the present retrospective study, we evaluated the proteinuria-lowering effect and drug safety of low-dose spironolactone (12.5 mg/day) in 42 patients with GN being treated with an ARB. RESULTS: Proteinuria decreased from a mean total-protein-to-creatinine (TP/Cr) ratio of 592.3 ± 42.0 mg/g at baseline to 335.6 ± 43.3 mg/g after three months of treatment with spironolactone (P < 0.001). After the initial three months, the mean TP/Cr ratio increased progressively at six, nine, and 12 months; however, it was still less than the baseline value (P = 0.001, < 0.001, and < 0.001, respectively). Although serum Cr levels increased significantly at three and nine months compared with baseline (P = 0.036 and 0.026, respectively), there was no time effect of treatment (P = 0.071). Serum potassium levels tended to increase with time (P = 0.118), whereas systolic and diastolic blood pressures decreased with time (P = 0.122 and 0.044, respectively). CONCLUSION: Low-dose spironolactone in combination with an ARB reduced proteinuria in patients with GN, which could represent a novel treatment option in individuals whose proteinuria is not optimally controlled by the use of ARBs alone.

Therapeutic effect of small dose spironolactone combined valsartan and amlodipine on obese patients with hypertension and its influence on serum visfatin and leptin levels / 心血管康复医学杂志

Objective:To observe therapeutic effect of small dose spironolactone combined valsartan and amlodipine on obese patients with hypertension and its influence on serum levels of visfatin and leptin.Methods:A total of 106 obese patients with hypertension treated in our hospital from Mar 2016 to Mar 2017 were selected.They were ran-domly and equally divided into routine treatment group(received valsartan,amlodipine and routine treatment)and combined treatment group(received small dose spironolactone based on routine treatment group),both groups were continuously treated for eight weeks.Systolic blood pressure(SBP),diastolic blood pressure(DBP),body mass in-dex(BMI),waist circumference(WC)and serum levels of aldosterone,visfatin and leptin before and after treat-ment were measured and compared between two groups.Results:Compared with before treatment,there were sig-nificant reductions in levels of SBP,DBP,serum aldosterone,visfatin and leptin in two groups after eight-week treatment,P=0.001 all;compared with routine treatment group after eight-week treatment,there were significant reductions in levels of SBP[(138.67 ± 9.34)mmHg vs.(127.52 ± 8.74)mmHg],DBP[(93.27 ± 8.26)mmHg vs. (86.43 ± 7.98)mmHg],serum aldosterone[(155.73 ± 16.43)ng/L vs.(121.49 ± 13.76)ng/L],visfatin[(28.49± 4.13)ng/ml vs.(22.31 ± 3.64)ng/ml]and leptin[(15.67 ± 4.82)ng/ml vs.(12.43 ± 3.74)ng/ml]in combined treatment group,P=0.001 all.Total effective rate of combined treatment group was significantly higher than that of routine treatment group(96.23% vs.83.02%),P=0.026. There was no significant difference in incidence rate of adverse reactions(11.32% vs.7.55%)between two groups,P=0.740. Conclusion:Small dose spironolactone combined valsartan and amlodipine possesses significant therapeutic effect on obese patients with hypertension,and it can reduce their serum levels of visfatin and leptin,which is worth extending.

Diagnosis, treatment and progress of primary aldosteronism in China / 中华内分泌代谢杂志

Primary aldosteronism is an important cause of secondary hypertension with the prevalence of 10%-20%in hypertensive patients. Compared with essential hypertension, primary aldosteronism patients have more cardiovascular and cerebrovascular complications. In this article, we will make a discussion on the development and current situation of primary aldosteronism by means of its prevalence, case detection, case confirmation, subtype classification, treatment and basic research.