Efficacy and tolerability of mirabegron in female patients with overactive bladder symptoms after surgical treatment for stress urinary incontinence

ABSTRACT Purpose To evaluate the efficacy and tolerability of mirabegron in females with overactive bladder (OAB) symptoms after surgical treatment for stress urinary incontinence (SUI). Materials and Methods The study was conducted with a prospective, randomized and double-blinded design. 62 patients over the age of 40 who met the inclusion-exclusion criterias of the study were enrolled and randomly divided into two groups as Group A (mirabegron 50mg) and B (solifenacin 5mg). Patients were compared based on efficacy of treatment [Patient Perception of Bladder Condition (PPBC) scale and micturition diaries], safety of treatment (heart rate, systolic and diastolic blood pressure, adverse events), number of micturitions per day, patient's satisfaction status after treatment [Visual Analog Scale(VAS)] and quality of life. Results The mean age of the population was 48.2±3.8 years and the duration of OAB symptoms was 5.9±2.9 months. Baseline values for the mean number of micturitions, volume voided in each micturition, nocturia episodes, urgency and urgency incontinence episodes were 15.3±0.34, 128±3.88mL, 3.96±1.67, 5.72±1.35 and 4.22±0.69, respectively. After treatment, values for these parameters were 11.7±0.29, 164.7±2.9mL, 2.25±0.6, 3.38±0.71, 2.31±0.49 respectively. Quality of life score, symptom bother score, VAS for treatment satisfaction score, PPBC score after treatment were 66.1±0.85, 43.7±0.77, 4.78±0.14, 4.78±0.14, respectively. There were no significant differences between two groups on any parameter. However, mirabegron showed better tolerability than solifenacin, particularly after 6 months. Conclusion Mirabegron is safe, effective and tolerable in the long-term treatment of females with OAB symptoms after surgery for stress urinary incontinence.

Overactive bladder - pharmacological treatment

The Guidelines Project, an initiative of the Brazilian Medical Association, aims to combine information from the medical field in order to standardize producers to assist the reasoning and decision-making of doctors. The information provided through this project must be assessed and criticized by the physician responsible for the conduct that will be adopted, depending on the conditions and the clinical status of each patient.

Determination of Mirabegron in rat plasma by UPLC-MS/MS after oral and intravenous administration

SUMMARY Mirabegron is a kind of β3 adrenergic receptor agonist which is an effective drug for the treatment of overactive bladder. In this research, a UPLC-MS/MS method is developed and validated for the study of mirabegron pharmacokinetic in rats. A protein precipitation method is applied for sample preparation with acetonitrile. m/z 397.3→379.6, m/z 326.4→121.0 for mirabegron, tolterodine (IS), respectively in the positive ion mode was performed for quantitation. The method is reliable and reproducible in our study (intra-day precision≤11.06%, inter-day precision≤11.43%) with concentration curves linear from 5 to 2500 ng/mL(R2>0.999). Stability studies demonstrated that mirabegron was stable under a variety of storage conditions. This method was successfully applied for determining mirabegron in rats after oral and intravenous administration.

RESUMO Mirabegron é um tipo de agonista do receptor adrenérgico beta 3 que demonstra eficácia no tratamento de bexiga hiperativa. Nesta pesquisa, o método UPLC-MS/MS é desenvolvido e validado para o estudo da farmacocinética mirabegron em ratos. Um método de precipitação de proteínas é aplicado para a preparação de amostras com acetonitrilo. 397.3 → 379.6 M / Z, M / Z 326.4 → 121.0 para mirabegron, tolterodina (IS), respectivamente, para o íon positivo foi realizado para quantificação. O método é fiável e reprodutível em nosso estudo (precisão intradia ≤ 11,06%; precisão entredia ≤ 11.43%), com curvas de concentração linear de 5 a 2 ng/ml (R2 > 0,999). Estudos de estabilidade demonstraram que mirabegron permanece estável sob uma variedade de condições de armazenamento. Este método foi aplicado com sucesso para a determinação de mirabegron em ratos após administração oral e intravenosa.

Thermodinamic aspects of solvation and dilution for acetanilide and phenacetin in some aqueous and organic solvents mutually saturated

Acetanilide (ACN) and phenacetin (PNC) are compounds structurally related with acetaminophen widely used as model drugs in pharmaceutical chemistry. Based on published thermodynamic quantities for dissolution, partitioning and sublimation of ACN and PNC, at 25.0 °C, thermodynamic quantities for drugs solvation in cyclohexane-saturated water (W(CH)) and water-saturated cyclohexane (CH(W)), chloroform-saturated water (W(CLF)) and water-saturated chloroform (CLF(W)), and isopropyl myristate- saturated water (W(IPM)) and water-saturated isopropyl myristate (IPM(W)), as well as the drugs dilution in the organic solvents were calculated. The Gibbs energies of solvation were favourable in all cases. Respective enthalpies and entropies were negative indicating an enthalpy-driving for the solvation process in all cases. Otherwise, the Gibbs energies of dilution were favourable for ACN and PNC in IPM(W) but unfavourable in the other organic solvents, whereas the respective enthalpies and entropies were negative for both drugs in all the organic solvents, except for PNC in CH(W) indicating enthalpy-driving for the dilution process in the former cases and entropy-driving for the later. From obtained values for the transfer processes, an interpretation based on solute-solute and solute-solvent interactions was developed.

Results based on global experience of monitoring crop protection products in water

The pesticides for which the most expensive data on use are currently available are those applied in agricultural settings. Similarly, the majority of information on pesticide detections in ground water has been collected for pesticides used within predominantly agricultural areas. The available data indicate that the pesticides detected most frequently in ground water are also those used widely in agriculture, namely, the triazines and acetanilides. Some of the more heavily used insecticides and fumigants, such as aldicarb, DBCP, and EDB, have also been among the pesticides detected most often in ground water. For those detected, pesticide detections in ground waters generally become more common with greater use and greater analysis. Direct relations between pesticides detection frequencies and use become more evident when data on pesticide use are aggregated over smaller areas. When pesticide use is assessed at comparatively large spatial areas, low use is typically associated with low frequencies of pesticide detection in ground water, while high use is associated with a broad range of detection frequencies. A comprehensive review of published information on the distribution of pesticides in ground water indicates that pesticides from various chemical classes heve been detected in ground water. Many of these compounds are commonly present at low concentrations in shallow ground water immediately beneath agricultural land. Information on pesticides in ground water is not sufficient to provide either a statistically representative view of pesticide occurence in ground water across various countries or an indication of long-term trends or changes in the severity or extent of this contamination over time.This is largely due to wide variations in analytical detection limits, site selection procedures, and other design features among studies conducted in different countries at different times. Past approaches have not been well suited for distinguishing "point source" from "no-point source" pesticide contamination. Among the variety of natural and anthropogenic factors examined, those that appear to be most strongly associated with the intensity of pesticide contamination of ground water are the depth, construction, and age of the sampled wells, the amount of the recharge (precipitation or irrigation), and the depth of the tillage, proximity to surface water (gw/sw interactions) are responsible for a huge number of detections, since surface run-Off...

Síntesis, controles químicos y radioquímicos del "mebrofenin-Tc-99m": estudios radiofarmacológicos y usos en seres humanos / Synthesis, chemical and radiochemical cotrols of mebrofenin-Tc-99m: radiopharmacological studies and uses in humans

En este trabajo se presenta el estudio químico radiofarmacológico y el uso en seres humanos realizado con el "mebrofeini-Tc-99m". La finalidad del trabajo fue determinar el uso potencial de este radiofármaco en seres humanos portadores de distintas entidades clínico patológicas. Para esto, se sintetizó el producto mejorando el rendimiento de reacción, mediante una modificación en la segunda etapa del camino de síntesis, lo que condujo a elevarlo del 70 al 90%. Se determinó la cinética plasmática mediante la circulación extracorpórea realizada en ratas wistar, mientras que la hepática y renal se llevó a cabo en ratones endocriados. Todos los resultados fueron analizados mediante un procesador, obteniéndose las vidas medias plasmáticas y los máximos tiempos de captación