Evaluation of prescribing pattern of phosphodiesterase-5 inhibitors and assessing effectiveness of sildenafil and tadalafil in patients with erectile dysfunction

Several factors may affect identification and treatment of erectile dysfunction by health care providers, this study evaluates prescribing pattern of PDE-5 inhibitors and assess effectiveness of Sildenafil and Tadalafil in patients with erectile dysfunction.This is a descriptive and observational study, observed participants without providing any interventions, after fulfilling inclusion and exclusion criteria, patients were enrolled into study and informed written consent was obtained from all patients, data was obtained from medical records, analysed descriptively. International Index of Erectile Function (IIEF) Questionnaire is used in assessment of erectile dysfunction and treatment outcomes.In our study, 80% of patients were prescribed with phosphodiesterase inhibitors and 20% received nutritional supplements. 80 percent of drugs were prescribed under generic name, subjects treated with Sildenafil/Tadalafil were found to be associated with higher mean scores for questions of International Index of Erectile Function (IIEF). Tadalafil scored high in terms of sexual desire domain.PDE5 inhibitors represent major first-line oral therapy option for men with erectile dysfunction, shift of market from brand to generic products allows more freedom of choice, although multiple reports suggest general equivalency of four major PDE5 inhibitors, tadalafil suggested to be preferable.

Comprehensive Modeling and Molecular Docking of Phosphodiesterase Inhibitors

In the present study, the biological activity of some pharmaceutical molecules was investigated and predicted by using quantitative structure-activity relationship (QSAR) studies and molecular docking. The aim of this study is to apply QSAR and molecular docking methods to predict and calculate the half maximal inhibitory concentration (IC50) of phosphodiesterase (PDE) 10A. To apply QSAR method at first multiple linear regression (MLR), genetic algorithm (GA), and successive projection algorithm (SPA) were used to select the best descriptors related to PDE 10A inhibitory activity. The selected descriptors were then applied as inputs to construct MLR and a non-linear support vector machine (SVM). Also we used molecular docking method to extract the descriptors and then by using MLR and SVM methods a linear and non-linear models developed respectively. Consequently, a comparison of the results of QSAR and docking study indicated that the non-linear SVM-SPA2 in QSAR study and SVM-MLR in molecular docking study had a much better prediction power than the other models. Finally, the Y-scrambling and cross-validation tests were used to evaluate the validity of the obtained model and the results of these tests indicates that the model is appropriate for using in prediction.

Dysfunction in the Cystic Fibrosis Transmembrane Regulator in Chronic Obstructive Pulmonary Disease as a Potential Target for Personalised Medicine

In recent years, numerous pathways were explored in the pathogenesis of COPD in the quest for new potential therapeutic targets for more personalised medical care. In this context, the study of the cystic fibrosis transmembrane conductance regulator (CFTR) began to gain importance, especially since the advent of the new CFTR modulators which had the potential to correct this protein’s dysfunction in COPD. The CFTR is an ion transporter that regulates the hydration and viscosity of mucous secretions in the airway. Therefore, its abnormal function favours the accumulation of thicker and more viscous secretions, reduces the periciliary layer and mucociliary clearance, and produces inflammation in the airway, as a consequence of a bronchial infection by both bacteria and viruses. Identifying CFTR dysfunction in the context of COPD pathogenesis is key to fully understanding its role in the complex pathophysiology of COPD and the potential of the different therapeutic approaches proposed to overcome this dysfunction. In particular, the potential of the rehydration of mucus and the role of antioxidants and phosphodiesterase inhibitors should be discussed. Additionally, the modulatory drugs which enhance or restore decreased levels of the protein CFTR were recently described. In particular, two CFTR potentiators, ivacaftor and icenticaftor, were explored in COPD. The present review updated the pathophysiology of the complex role of CFTR in COPD and the therapeutic options which could be explored.

Study of the Efficiency of Using Type 5 Phosphodiesterase Inhibitors in the Therapy of Ereсtile Dysfunction in Patients with Metabolic Syndrome

Metabolic syndrome is a symptom complex that combines abdominal obesity, insulin resistance, hyperglycemia, dyslipidemia and arterial hypertension. One of the complications of metabolic syndrome is sexual dysfunction in men. The objective: is to evaluate the efficacy and tolerability of udenafil 200 mg in the treatment of erectile dysfunction in patients with metabolic syndrome. Materials and methods. The clinical efficacy of the IV generation PDE-5 inhibitor medicine udenafil in 76 patients with erectile dysfunction of mixed origin and with metabolic syndrome in dynamics was studied. The average age was 51,6±8,2 years. The observation period was 12 weeks, but the control of metabolic syndrome parameters (anthropometry, review, biochemical blood tests) and the assessment of erectile function were carried out for 6 months. Results. After 12 weeks, patients achieved positive results in weight loss, BMI and waist circumference, although not significantly. It is necessary to note the positive changes in the indicators of the cardiovascular system. The downward trend was demonstrated by such indicators as heart. Diet therapy and taking statins have improved the indicators of fat metabolism. Correction of metabolic disorders in patients was accompanied by an increase in total and free testosterone. However, there was no statistically significant difference in the degree of increase in the concentration of androgens. Correction of metabolic disorders in patients was accompanied by an increase in total and free testosterone. During treatment, almost all integrative indices of IIEF increased. Specifically, the index «erectile function» improved 2,26 times (p<0,01), «satisfaction with intercourse» 2,59 times (p<0,001), «orgasm» 2,0 times (p<0,01), «libido» – 2,9 times (p<0,001), «general satisfaction» 2,3 times (p<0,01). According to various indicators, the sexual function of men with metabolic syndrome and erectile dysfunction improved 2–2,9 times. Changes in cavernous blood flow on Doppler ultrasonography showed an increase in peak systolic blood flow rate by 1,5 times, which is associated with the udenafil half-life. Our data indicate that the use of the medicine udenafil is perspective in men with erectile dysfunction and metabolic syndrome and in those who do not have stable family-sexual relations to ensure spontaneity of sexual relations. Conclusions. Udenafil can be considered as a first-line medecine in the treatment of erectile dysfunction in patients with metabolic syndrome.