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Dapoxetine is a selective serotonin reuptake inhibitor (SSRI) used to treat premature ejaculation (PE), and is mainly metabolized by CYP2D6, CYP3A4, and flavin‐containing monooxygenase 1. The purpose of the study was to evaluate the effect of CYP2D6 polymorphism on the pharmacokinetics of dapoxetine in healthy Chinese men. Thirty‐nine subjects who received a single oral dose of 30 mg dapoxetine hydrochloride were classified based on their CYP2D6 genotype: *1/*1 (n = 9), *1/*41 (n = 1), *1/*10 (n = 12), *10/*41 (n = 3), or *10/*10 (n = 14). The difference in pharmacokinetic parameters between different genotype groups was analyzed and then scored according to the activity score system. Compared with the wild‐type subjects of CYP2D6 *1/*1, the peak plasma concentration (Cmax) and the area under the plasma drug concentration‐time curve (AUCinf) of dapoxetine in the *10/*10 and *10/*41 groups were notably increased (P ≤.05). Significant differences in Cmax, AUC, volume of distribution/bioavailability (V/F) and clearance/bioavailability (CL/F) were observed among dapoxetine activity score groups (P ≤.05). The AUCinf was increased significantly (154% and 89.73%, P ≤.05) and the Cmax was increased significantly (73.45% and 42.67%, P ≤.05) in CYP2D6 *10/*41 subjects, compared with CYP2D6 *1/*1 and *1/*10 subjects. The results obtained indicated that CYP2D6 *10 and *41 polymorphisms have significant effects on the pharmacokinetic properties of dapoxetine. [ABSTRACT FROM AUTHOR]

To compare the efficacy of tadalafil alone, dapoxetine alone, and tadalafil with dapoxetine as a combination therapy for the treatment of premature ejaculation. Eligible patients attended our andrology clinic with premature ejaculation were randomly allocated into three groups: group A (92 participants) received on-demand tadalafil, 5 mg; group B (91 participants) were given on-demand dapoxetine, 30 mg; and group C (89 participants) received on-demand combination of tadalafil, 5 mg, and dapoxetine, 30 mg. We assessed the changes in the intravaginal ejaculatory latency time (IELT) and the satisfaction scores 1, 2, and 3 months after treatment. Highly statistically significant improvements were found in the mean IELT and satisfaction scores 1, 2, and 3 months post-treatment in all groups (P = <0.001). Post hoc analysis suggested this improvement was more pronounced in group C (P < 0.001). Both tadalafil and dapoxetine are effective in the treatment of patients with premature ejaculation, but the combination of both drugs gives better results. [ABSTRACT FROM AUTHOR]

to compare the results of using Dapoxetine and HA (hyaluronic acid) gel injection by Five puncture technique in the treatment of premature ejaculation (PE). 100 sexually active heterosexuals circumcised males with lifelong PE were included in the study. Group A patients were treated with on-demand Dapoxetine, while group B was treated with HA gel glans penis injection using a five-puncture technique. Both groups were evaluated at 1st,3rd and 6th months post-treatment using IELT. There were no significant differences between both groups regarding patient demographic. Mean pretreatment IELT in groups A and B were 45.82 ± 7.44 and 46.18 ± 7.82 receptively. There was no significant difference between both groups. After treatment, both groups show significant ILET improvement during the 1st,3rd, and 6th months follow-up with a P value < 0.001. However, when comparing the improvement of ILET in group A (Dapoxetine) and group B (HA injection), there were high significance differences in favor of group B in the 1st,3rd, and 6th-month follow-up. Although both treatment modalities have improved IELT and premature ejaculation, but HA injection with five punctures technique was significantly better than oral Dapoxetine with self-limited side effects. [ABSTRACT FROM AUTHOR]

Premature ejaculation (PE), despite its wide prevalence, is largely underdiagnosed and undertreated. Being a multifactorial dysfunction with strong cultural characteristics, PE requires skillful attitudes in the psychosexological support, necessary to manage the patient's and the couple's expectations, as well as in the medical treatment. Dapoxetine is a short‐acting selective serotonin reuptake inhibitor approved for use in lifelong and acquired PE in a number of countries. Opinions, not always generated by the evidence‐based medicine, impacted the attitudes of Western andrologists, as a nocebo effect which produced a drug's Waterloo, characterized by low prescription rates much more built on the patients' and doctors' expectations than on costs, side effects, and efficacy. In the present study, we retrospectively reviewed real‐life data from eight Andrology and Sexual Medicine Public Centers in China to assess the prevalence of PE among attending patients, its association with erectile dysfunction, its subtype, and the proposed treatments. In 2019, among 156,486 patients coming to the centers, 32,667 visits having PE as the chief complaint were performed (20.9%). Almost all patients received treatment prescriptions (32,641 patients, 99.92%); 23,273 patients came back for a follow‐up visit in the subsequent 12 months (71.2% of those who initially received treatment). Dapoxetine, either alone or in combination with another therapy, was the most prevalent treatment, prescribed to 22,767 patients (69.7% of treated patients), followed by traditional Chinese medicine (TCM) (39.4%). At follow‐up, 8174 patients were unsatisfied with treatment, and a new treatment was proposed (35.12%). Dapoxetine was the best treatment, with an overall 27.1% switching rate when used either alone or in combination: Although the switching rate for Dapoxetine alone was 44.2%, the association of the same drug with psychotherapy resulted in much lower rates (19.5%) and reached a minimum of 12% when also combined with TCM demonstrating how cultural aspects and medical attitudes may dramatically impact on the therapy of a multifaceted, complex, and culture‐grounded sexual symptom such as PE. In conclusion, taking switching rates as surrogate markers of treatment failure, this real‐life study—the largest in the field—shows that in a more patient‐oriented (as in Chinese medical culture), and less symptom‐oriented (as in Western medical attitudes), Dapoxetine is a successful treatment for PE patients, with higher reliability when used alone or as part of combined and integrated therapies. [ABSTRACT FROM AUTHOR]

Dapoxetine is a newer anti‐depressant that is used for severe forms of depression via selective serotonin reuptake inhibition conduit. We aimed to evaluate the effect of different doses of dapoxetine lonely or with acetaminophen (AMP). Seven groups of albino rats were used where dapoxetine was administered orally at the doses of 3, 5, and 8 mg/kg body weight for a period of 14 days in groups 2, 4, and 6, respectively. AMP (67.5 mg/kg body weight) was co‐administered with dapoxetine (3, 5, and 8 mg/kg body weight) for 14 days in groups 3, 5 and 7, respectively. Dapoxetine in mid and high dose plus AMP increased body weight and hematological parameters. Ambulation and rearing were declined with mid and high doses of dapoxetine+AMP, contrary to grooming. Struggling was decreased with high doses of dapoxetine+AMP. High dose of dapoxetine+AMP induced lowering of serotonin and dopamine as well as increasing of cholinesterase. Brain derived neurotrophic factor was decreased in all groups. Oxidative stress biomarkers were augmented with high dose of dapoxetine+AMP. High doses of dapoxetine and/or AMP induced loss of the Purkinje cell layer at cerebellum. The high dose of dapoxetine+AMP denotes behavioral, histopathological and neurochemical alterations, even though no serotonin syndrome occurs. [ABSTRACT FROM AUTHOR]

Stroke is a medical emergency that is associated with substantial mortality and functional disability in adults. The most popular class of antidepressants, selective serotonin reuptake inhibitors SSRIs, have recently been shown in studies to have positive effects on post-stroke motor and cognitive function. Thus, we hypothesized that dapoxetine (DAP), a short-acting SSRI, would be effective against cerebral ischemia/reperfusion injury. Adult male Wister rats (200–250 g) were subjected to a sham operation or bilateral common carotid artery occlusion (BCCAO) for 30 min followed by 24 h of reperfusion to induce global cerebral ischemia/reperfusion (I/R) injury. Rats were treated with vehicle or DAP (30 or 60 mg/kg, i.p.) 1 h before BCCAO. The neurobehavioral performance of rats was assessed. The infarct volume, histopathological changes, oxidative stress parameters, and apoptotic and inflammatory mediators were determined in the brain tissues of euthanized rats. Our results confirmed that DAP significantly ameliorated cerebral I/R-induced neurobehavioral deficits, reduced cerebral infarct volume, and histopathological damage. Moreover, DAP pretreatment reduced lipid peroxidation, caspase-3, and inflammatory mediators (TNF-α and iNOS) compared to I/R-injured rats. Thus, DAP pretreatment potentially improves neurological function, and cerebral damage in cerebral ischemic rats may be partly related to the reduction in the inflammatory response, preservation of oxidative balance, and suppression of cell apoptosis in brain tissues. [ABSTRACT FROM AUTHOR]

Zika virus (ZIKV) belongs to the Flavivirus genus of the Flaviviridae family, and is a pathogen posing a significant threat to human health. Currently, there is a lack of internationally approved antiviral drugs for the treatment of ZIKV infection, and symptomatic management remains the primary clinical approach. Consequently, the exploration of safe and effective anti-ZIKV drugs has emerged as a paramount imperative in ZIKV control efforts. In this study, we performed a screening of a compound library consisting of 1789 FDA-approved drugs to identify potential agents with anti-ZIKV activity. We have identified dapoxetine, an orally administered selective serotonin reuptake inhibitor (SSRI) commonly employed for the clinical management of premature ejaculation (PE), as a potential inhibitor of ZIKV RNA-dependent RNA polymerase (RdRp). Consequently, we conducted surface plasmon resonance (SPR) analysis to validate the specific binding of dapoxetine to ZIKV RdRp, and further evaluated its inhibitory effect on ZIKV RdRp synthesis using the ZIKV Gluc reporter gene assay. Furthermore, we substantiated the efficacy of dapoxetine in suppressing intracellular replication of ZIKV, thereby demonstrating a concentration-dependent antiviral effect (EC50 values ranging from 4.20 μM to 12.6 μM) and negligible cytotoxicity (CC50 > 50 μM) across diverse cell lines. Moreover, cell fluorescence staining and Western blotting assays revealed that dapoxetine effectively reduced the expression of ZIKV proteins. Collectively, our findings suggest that dapoxetine exhibits anti-ZIKV effects by inhibiting ZIKV RdRp activity, positioning it as a potential candidate for clinical therapeutic intervention against ZIKV infection. [ABSTRACT FROM AUTHOR]

We aimed to evaluate the efficacy of combined low-intensity extracorporeal shockwave therapy (LI-ESWT) and dapoxetine administration for the treatment of lifelong premature ejaculation (LPE) in comparison to LI-ESWT and dapoxetine alone. In the randomized controlled trial, 212 men diagnosed with LPE were enrolled. The participants were randomized into four subgroups: control (n = 50), dapoxetine (n = 56), LI-ESWT (n = 50) and LI-ESWT + dapoxetine (n = 56). The intravaginal ejaculation latency (IELT), premature ejaculation profile (PEP), and Global Impression of Change (GIC) were evaluated. There were substantial improvements in the fold-increase of the IELT (F-IELT), and PEP and GIC-I scores in both the dapoxetine (p < 0.001) and LI-ESWT + Dapoxetine (p < 0.001) groups than in the control and LI-ESWT groups. Although the LI-ESWT group demonstrated a minor improvement in the F-IELT score (p = 0.04), there were no noticeable improvements in the PEP (p = 0.12) and GIC-I (p = 0.15) scores. In conclusion, a combination of dapoxetine administration and LI-ESWT might be more effective in treating LPE than LI-ESWT or dapoxetine alone, indicating a potential synergistic effect.

Introduction: Premature ejaculation is one of the problems which men are facing. This disorder can affect the quality of life and in many cases, the fertility of couples. Recent studies have shown that the dapoxetine mechanism affects the spermatogenesis. However, so far, no study has been conducted on the impact of dapoxetine on sexual hormones and spermatogenesis. Therefore, the present study was performed with aim to examine the effects of dapoxetine on sexual hormones and spermatogenesis. Methods: In this study, 32 male albino desert rats weighing 200 to 250 gr were used. The rats were randomly divided into four groups. The first group received saline solution (1mg/kg) via gavage. Groups 2 to 4 were subjected to intervention with dapoxetine at doses of 1, 2, and 4 ml/kg, respectively, administered through gavage. Pathological changes in the testicular, levels of luteinizing hormones, follicle-stimulating hormone, and testosterone were investigated in this study. Data analysis was done using SPSS software (version 22) and ANOVA, Fisher and post hoc tests. P

Introduction: Dapoxetine is a novel therapeutic agent employed in treating specific diseases. However, its potential impact on renal excretion processes has yet to be thoroughly investigated, necessitating further exploration in this study. Objectives: This research aimed to assess the effects of dapoxetine on renal function and explore any potential disturbances in kidney excretion processes. Materials and Methods: In this study, 32 male Albino rats weighing between 200-250 g were utilized. The rats were randomly divided into four groups. Group one served as the control and received a normal diet, while groups two to four were administered dapoxetine through gavage at doses of 1 mg/kg, 2 mg/kg, and 4 mg/kg, respectively. The study evaluated blood urea nitrogen (BUN), and serum creatinine levels and examined renal pathological changes in the rats. Results: The results demonstrated a significant increase in average BUN levels in group four compared to other groups (P0.05). Importantly, no indications of apoptosis, necrosis, edema, hydropic degeneration, or glomerular changes were observed in any of the renal cells from the rat groups. Conclusion: Dapoxetine administration led to changes in BUN and creatinine levels; however, it did not adversely affect the renal cells’ pathological outcomes. These results suggest that dapoxetine could be considered for use in the future treatment of certain diseases, considering its minimal impact on renal function. Further investigations and clinical trials are warranted to corroborate these findings and inform medical decision-making.

Background: Recently, dapoxetine has been widely accepted to treat premature ejaculation by fast‐inhibiting 5‐hydroxytryptamine reuptake. However, dapoxetine is not suitable for all premature ejaculation patients in clinical treatment. We need to investigate and reveal the mechanism deeply to solve this problem. Objectives: To investigate and reveal the function of dopamine D4 receptor in dapoxetine medicated premature ejaculation treatment. Materials and methods: A rat model was used to screen rapid ejaculators. The molecular mechanisms of histone serotonylation‐mediated regulation of dopamine D4 receptor were demonstrated by chromatin immunoprecipitation, DNA pull‐down, mass spectrometry analysis, and coimmunoprecipitation experiments. The biological function of dopamine D4 receptor was investigated through in vivo experiments by intrathecal injection of shDRD4 to knockdown dopamine D4 receptor. Results: In this study, we found that dapoxetine increased expression of 5‐hydroxytryptamine and dopamine D4 receptor. We demonstrated that dapoxetine increased levels of 5‐hydroxytryptamine, which promoted histone serotonylation (H3K4me3Q5ser) and transcription factor myeloid zinc‐finger 1 complex binding on the dopamine D4 receptor promoter, upregulated the expression of dopamine D4 receptor and thus delayed ejaculation. Discussion: In this study, we demonstrated that dapoxetine increased the levels of 5‐hydroxytryptamine, which promoted histone serotonylation and myeloid zinc‐finger 1 complex binding to the dopamine D4 receptor promoter and upregulated the expression of dopamine D4 receptor, thus delaying ejaculation. Conclusion: It is a novel mechanism that dapoxetine take effect of premature ejaculation treatment through upregulating the dopamine D4 receptor, which indicated that upregulated dopamine D4 receptor would enhance the dapoxetine effect in premature ejaculation treatment. This may lead to the development of novel therapeutic interventions for premature ejaculation. [ABSTRACT FROM AUTHOR]

Photoinduced electron transfer (PET) is the most common mechanism proposed to account for quenching of fluorophores. Herein, the intrinsic fluorescence of dapoxetine (DPX) hydrochloride is in the "OFF" state, owing to the deactivation effect of PET. When the amine moiety is protonated, the fluorescence is restored. Protonation of the nitrogen atom of the tertiary amine moiety in DPX leads to "ON" state of fluorescence due to hindrance of the deactivating effect of PET by protonation of the amine moiety. This permits specific and sensitive determination of DPX in human plasma [lower limit of quantification (LLOQ) = 30.0 ngmL−1]. The suggested method adopts protonation of DPX using 0.25 M hydrochloric acid in anionic micelles [6.94 mM sodium dodecyl sulfate (SDS)] leads to a marked enhancement of DPX‐fluorescence, after excitation at 290 nm. [ABSTRACT FROM AUTHOR]

An understanding of drug product degradation issues is needed to advise stable formulation and provide a reasonable shelf‐life evaluation for all drug products. For this purpose, we have developed and validated a novel HPLC method for assessing the stability of vardenafil and dapoxetine in a combined pharmaceutical dosage form. The chromatographic separation was accomplished on a ProntoSIL C18 KROMA PLUS column (250×4.6 mm, 5 μm). The column was run under isocratic conditions with a 2.0 mL/min flow rate. The mobile phase was made up of methanol and 20 mM potassium dihydrogen phosphate at 45 : 55 (v/v), which was adjusted to pH 3.0 with phosphoric acid; these two drugs were eluted at retention times of 5.33 and 9.91 min for vardenafil and dapoxetine, respectively. The proposed method shows a linearity of 1–50 ug/ml with a regression of 0.9999 for both drugs. The method was validated for accuracy, precision, linearity, specificity, and sensitivity. The developed HPLC method has been successfully implemented to analyse dapoxetine and vardenafil in tablets. Furthermore, the stress degradation experiments were conducted on the bulk powder of vardenafil and dapoxetine following the International Council for Harmonization (ICH) recommendations. [ABSTRACT FROM AUTHOR]

Introduction. Recent studies have shown that SSRIs have anti-inflammatory effects, and their administration prevents their production by acting on inflammatory cytokines. Emphasizing that we did not find a study on Dapoxetine and its effect on neuropathic pain, in this study, we examined the effect of Dapoxetine on neuropathic pain in rats. Material and methods. 42 rats were divided into six groups of 7, which included: sham, control, gabapentin, Duloxetine and Dapoxetine 1 and 3. Except for the sham group, other groups were induced with neuropathy, and no drug treatment was performed in the sham group. The groups were treated with normal saline, gabapentin (30 mg/kg/day), Duloxetine at (30 mg/kg/day) and Dapoxetine (1 and 3 mg/kg/day), respectively by intraperitoneal injection. Then, thermal hyperalgesia and mechanical and thermal allodynia experiments were performed on rats. Results. The Dapoxetine-treated groups’ mean response to thermal hyperalgesia and mechanical allodynia increased on days 7 and 14. The mean response of the 3 mg/kg Dapoxetine group on day 7 was significantly higher than the control group (P

Objective: Lifelong premature ejaculation (PE) is regarded as one of the most common male sexual dysfunction. We aimed to detect whether insula-related brain functional networks are altered in lifelong PE patients and whether such alterations are "normalised" after selective serotonin reuptake inhibitors (SSRI) administration. Methods: Twenty-three drug-naive lifelong PE patients and 30 healthy controls (HC) were recruited in current study. All subjects underwent resting-state functional magnetic resonance imaging (fMRI) scan at first. One hour after dapoxetine administration, all patients underwent fMRI scanning again. The degree centrality (DC), amplitude of low-frequency fluctuations (ALFF) and regional homogeneity (ReHo) analysis, and ROI-based functional connectivity (FC) analysis were applied to calculate the abnormalities in insula-related functions among three groups. Results: Compared to HC group, PE patients at baseline showed significantly altered DC, ALFF, and ReHo value of the bilateral insula, which subsequently showed a "normalised" trend after dapoxetine administration. Additionally, compared to HC group, PE patients at baseline showed significantly decreased FC between insula and precentral gyrus, inferior frontal gyrus, middle/inferior temporal gyrus, and caudate, while patients after dapoxetine administration showed increased insula-related FC in anterior cingulate cortex and decreased FC in thalamus and middle/inferior temporal gyrus. The main effects of dapoxetine were located in precentral gyrus, inferior frontal gyrus, caudate, and limbic system. Conclusions: Our findings report altered brain mechanism of insula in lifelong PE patients and also indicate that dapoxetine can "normalise" the abnormal function of the insula to certain extent in lifelong PE patients. [ABSTRACT FROM AUTHOR]

Purpose: Premature ejaculation (PE) is a common sexual dysfunction that significantly affects the quality of life of the patient and their partner. We aimed to compare the efficacy and safety of the combination therapy with biofeedback-guided pelvic floor exercise therapy (BFT) and dapoxetine 30 mg. Methods: Sixty-five patients diagnosed with lifelong PE were included in the study. Patients were divided into three groups as BFT, dapoxetine 30 mg and a combination of BFT and dapoxetine 30 mg. The patients were compared with the intravaginal ejaculatory latency time (IELT) pre-treatment and post-treatment 1st and 3rd months. Results: The mean IELTs of the patients in Group 1 were 40 s in pre-treatment, 115 s at the end of the 4th week and 140 s at the end of the 12th week. The IELT values of the patients in Group 2 were 40 s in pre-treatment, 145 s in the 4th week and 170 s in the 12th week. The IELT values were calculated in Group 3 as 42.5 s in pre-treatment, 185 s in the 4th week and 205 s in the 12th week When the IELT was statistically compared between the groups at 1st and 3rd months, the duration in the combination group was found to increase significantly (p < 0.001). Conclusion: Combination therapy with BFT and dapoxetine 30 mg in lifelong PE treatment is a good alternative with a low side effect profile and acceptable continuous efficiency. [ABSTRACT FROM AUTHOR]

Abstract Background Dapoxetine hydrochloride is a selective serotonin reuptake inhibitor drug for treating premature ejaculation. This study was designed to develop and validate a sensitive and selective LC–MS/MS method for trace analysis of genotoxic impurity ethyl methanesulfonate in Dapoxetine hydrochloride. Results Chromatographic separation was achieved on the Shodex RSpak DS-413 column, 150 × 4.6 mm, 3.0 µm using eluent containing a equal volumes of acetonitrile and 0.1% v/v formic acid in water was used in the isocratic elution mode at a pump flow of 1.0 mL/min. No interference was observed at the retention time of ethyl methanesulfonate, indicating that the developed method is specific and selective for trace level quantification.The developed method was found to be linear in the concentration range of 1–50 ppm with coefficient of regression of 0.9997. Detection limit and quantification limit were determined to be 0.6 ppm and 1.0 ppm respectively. Acceptable RSD values ( 90%) obtained from the accuracy and precison experiments indicate that the developed method is precise and accurate in the concentration range of 1–50 ppm. Ethyl methanesulfonate solutions were stable for two days when stored at room and refrigerated temperatures. Conclusion The developed method has the ability to quantify ethyl methanesulfonate in dapoxetine hydrochloride. Thus, the anticipated method has high probability to adopt in the quality testing laboratories of pharmaceutical industry.

Restriction measures enacted during the COVID-19 pandemic had severe effects on male sexual and reproductive health. We aimed to investigate the real-life impact and perception of sexual function in 2020 in Italy, as the first Western country experiencing a national lockdown by measuring relative search volume for keywords pertaining to sexual health and behaviors provided by Google Trends and sales data for pro-erectile treatments. No significant change was observed for erectile dysfunction and premature ejaculation. Interest towards most phosphodiesterase type 5 inhibitors decreased significantly during lockdown (e.g., sildenafil, p = 0.0002; tadalafil p = 0.0016), then reverted to pre-lockdown levels (e.g., sildenafil, p < 0.0001; tadalafil p < 0.0001), mirroring a concomitant sales decrement (p = 0.0292). A subsequent recovery to previous levels at the end of the social confinement was also found (e.g., after vs. before lockdown, sildenafil, p = 0.8459; tadalafil p = 0.1166). During lockdown, interest towards pornography significantly increased during restrictions (p = 0.0053) and remained high (after vs. before lockdown, p = 0.0004), whereas interest towards paid and casual sex declined (p = 0.0015 and p = 0.049, respectively), then reverted to previous levels (after vs. before lockdown, p = 0.3969 and 0.8373, respectively). During the first Italian lockdown, we observed a transient but measurable decrease of sexual health-seeking behaviors and changes in sexual behaviors, with unknown impact for sexual medicine and public health.

To assess dapoxetine discontinuation rates and the reasons for discontinuation in Chinese men with premature ejaculation (PE). Information on 906 PE outpatients was obtained from the hospital information system (HIS) in 2019. Of these, 150 patients were chosen. We analysed the dapoxetine discontinuation rate and the reasons for discontinuation over a 12‐week follow‐up period. The mean age of all patients was 33.6 years (range = 18–55), the mean PE duration was 12.36 ± 9.45 months. The 5‐item International Index of Erectile Function (IIEF‐5) score was 21.51 ± 3.80. A total of 37.3% of all the patients remained on the treatment until the 12th week. The cumulative discontinuation rates at the 4th, 8th and 12th weeks were 12%, 41.3% and 62.7%, respectively. The discontinuation rates for all the patients in weeks 0–4, weeks 4–8 and weeks 8–12 were 19.1%, 46.8% and 34.0%, respectively. After 4 weeks, the discontinuation rates dropped sharply. The reasons for patients' discontinuation were as follows: overexpectation of efficacy (30.9%), relapsing after drug withdrawal (26.6%), high cost (25.5%), side effects (9.6%), fear of drug addiction (4.3%), failure of follow‐up (2.1%) and choosing other treatments (1.1%). The dapoxetine treatment discontinuation rate was very high. The main reasons for discontinuation were overexpectation of efficacy and high cost. [ABSTRACT FROM AUTHOR]

A study was conducted on 58 patients aged from 18-63 years old, they suffering from rapid ejaculation and all their Intravaginal ejaculation latency time (IELT) were less than 2 minutes. This study done at Erectile dysfunction unit in Al-Muthana teaching hospital for a period of 1 month (March/2019). The patients were divided into 2 groups: Group 1: Patient received 30 mg of Dapoxetine 1hr before coitus and 10 mg of Tadalafil 30 min before coitus. Group 2: Patient received Dapoxetine 20 mg + Tadalafil 10 mg mixed in one tablet 1 hr before coitus. The result of our study revealed that the IELT before treatment was less than 2 minutes in both groups, after treatment the IELT increased significantly (P≤0.05) in group 1 and group 2 (337.9±3.72 and 222.4±2.88 seconds) respectively. The IELT in group 1 was increased significantly (P≤0.05) compared to IELT in group 2 after treatment. In conclusion, the administration of Dapoxetine before 1 hr. of coitus and Tadalafil 30 min. before coitus (G1) gave a good results in increasing of IELT as compared to mixture of these drugs in one tablet.

A fast melt tablet (FMT) is well regarded as an alternative delivery system that might help resolve a patient's non-compliance issue. The main objective of this study was to develop a cocoa butter-based FMT. Additives, namely 5–15% of PEG 6000, beeswax, paraffin wax, and corn starch, were incorporated into the cocoa butter-based FMT to study the effects of these additives with the physical characteristic of a cocoa butter FMT. An optimum-based formulation was chosen according to the desired hardness and disintegration time and the taste masking property achieved with the model drug—dapoxetine. The analysis demonstrated that incorporating beeswax (15%) and paraffin wax (15%) could prolong the disintegration time by at least two-fold. On the contrary, the presence of corn starch was found to cause an increase in the hardness and reduction of the disintegration time. The disintegration mechanism might be presumed due to the synergistic effect of starch swelling and cocoa butter melting. The hardness value and in vitro disintegration time of the optimum formulation were recorded at 2.93 ± 0.22 kg and 151.67 ± 6.98 s. In terms of dissolution, 80% of dapoxetine was released within 30 min and the dissolution profile was comparable to the innovator product. The formulation was palatable and stable for at least 1 year. The exposure of the FMT formulation at 30 °C for 12 months was reported to be stable. Along with the sound palatability profile and high drug load capacity, the current formulation possesses the desired characteristics to be scaled up and marketed. [ABSTRACT FROM AUTHOR]

Dapoxetine is used for the treatment of premature ejaculation. The present study developed an HPLC–MS/MS method to determine the levels of dapoxetine in human plasma processed using simple protein precipitation. Dapoxetine-d7 was selected as the internal standard. The established method was performed using a mass spectrometer equipped with an electrospray ionization source in multiple positive ion reactions to monitor the mode using the precursor-to-product ion transitions of m/z 306.2–157.2 and m/z 313.2–164.2 for dapoxetine-d7 and dapoxetine, respectively. The method was evaluated based on its selectivity, linearity, limit of quantification, precision, accuracy, matrix effects, dilution integrity, stability, and extraction recovery. As a result of the model used in the present study, the validated linear ranges of dapoxetine were determined to be 2.00~1000 ng/mL in plasma, and the selectivity, precision, accuracy, dilution integrity, stability, and extraction recovery met the accepted standard. No matrix interference was observed. The method was successfully validated and applied to pharmacokinetic studies in healthy Chinese volunteers during the fasting and postprandial periods, respectively. [ABSTRACT FROM AUTHOR]

Objective To explore clinical efficacy and drug economy of generic and original dapoxetine hydrochloride tablets in the treatment of premature ejaculation. Methods Total of 87 patients with premature ejaculation who were treated in Andrology Department of Reproductive Medicine Center of Shenzhen Hospital of the University of Hong Kong from January 10, 2020 to January 10, 2022 were divided into two groups including the treatment group (55 cases) and the control group(32 cases). The treatment scheme of the treatment group was 30mg of Aishida, and the treatment scheme of the control group was 30mg of Priligy, which was taken orally as needed. The efficacy of the two groups were observed and compared by the scores of premature ejaculation diagnostic tool (PEDT) and international index of erectile function-5(IIEF-5), and their treatment-related costs were also comparatively analyzed. Results There were no significant differences in all indexes between the two groups before treatment (P>0.05). One month after treatment, the PEDT of the two groups was significantly improved, and the effect of the treatment group was not significantly different from that of the control group (P>0.05); One month after treatment, IIEF-5 in the two groups was slightly improved compared with that before treatment, and there was no significant difference between the treatment group and the control group (P>0.05); Further, the correlation analysis between PEDT and IIEF-5 before and after treatment showed that they were positively correlated, that is, the IIEF-5 score also improved with the improvement of PEDT score; The cost of drug treatment in the treatment group was significantly lower than that in the control group (P<0.05). Conclusion The efficacy of generic and original dapoxetine hydrochloride tablets in the treatment of premature ejaculation is equivalent, but the treatment cost of generic product is significantly lower than that of original product, indicating that the national centralized purchase of generic product has more drug economic advantages and is of great significance to improve patient compliance, satisfaction and accessibility; At the same time, with the significant improvement of premature ejaculation, the erectile function of the two groups is also improved. [ABSTRACT FROM AUTHOR]

Purpose: The purpose of this study was to compare the effectiveness of Dapoxetine, and Paroxetine as well as Dapoxetine/Tadalafil and Paroxetine/Tadalafil combinational therapies, for the treatment of patients with premature ejaculation.Materials and Methods: In this clinical trial study, 120 patients with premature ejaculation were randomly divided into 4 groups: The first group was treated with Paroxetine (Pa), while the second group received Dapoxetine(Da). The third group received Paroxetine combined with Tadalafil(PT) whereas the fourth group's treatment involved the use of Dapoxetine and Tadalafil(DT) for one month. In the next 2 and 4 weeks, the cases were evaluated in terms of ejaculation duration, frequency of intercourse per week, and drug side effects.Results: The mean age of the Da, Pa, PT, DT groups was 32 ± 6.9, 32.4 ± 7.2, 31.6 ± 1.9, and 32.9 ± 7.7 years, respectively. There was a significant difference between the Da and DT groups (p = .029) in the ejaculation latency in the 4-week follow-up. In the two weeks follow-up, a significant difference was observed between DA and DT (p = 0.043), Pa and PT (p = 0.006), and Pa and DT groups (p = 0.004) in terms of ejaculation latency. Four weeks after the intervention, a significant difference was detected in the intercourse frequency of Da and PT groups (p =0.033), Pa and PT groups (p = 0.043), Pa and DT groups (p = 0.02), and Da and DT groups (p = 0.016).Conclusion: Combination therapy (Tadalafil plus Paroxetine or Dapoxetine) was more effective in IELT (Intra ejaculation latency time) than mono-therapy especially in younger patients despite its slightly more side effects. [ABSTRACT FROM AUTHOR]

ABSTRACT: Introduction: Before dapoxetine was approved for the treatment of lifelong premature ejaculation (LPE) in China, daily dosing with off-label sertraline was common. Aim: To investigate the efficacy of dapoxetine in the treatment of patients with LPE as an alternative to sertraline therapy. Methods: This prospective study included LPE patients who previously attempted treatment with sertraline and who agree to receive dapoxetine therapy in our hospital from January 2020 to March 2021. Patients who received any PE therapy in the two months prior to the dapoxetine therapy were excluded. All patients received dapoxetine 30 mg (taken 1–3 hours before sexual intercourse) for 12 weeks, and they were not taking sertraline during the trial. Main Outcome Measure: Data on their intravaginal ejaculatory latency time and premature ejaculation profile were recorded before and after the dapoxetine treatment. Clinical Global Impression of Change scores and data on Treatment-Emergent adverse events were collected after treatment. Results: A total of 144 patients with LPE completed this study; including 64 patients who reported that previous sertraline treatment was satisfactory (group A) and 80 patients for whom previous sertraline therapy was unsatisfactory in treating PE (group B). Both groups experienced significantly increased intravaginal ejaculatory latency time. Dapoxetine therapy was reported satisfactory by 67.5% of patients with LPE in whom sertraline therapy unsatisfactory according to their Clinical Global Impression of Change score, which was not different from those who reported this result in group A (62.5%). Similar outcomes were also reported for premature ejaculation profile and treatment-emergent adverse events. Conclusion: : Although both dapoxetine and sertraline are selective serotonin re-uptake inhibitors, dapoxetine therapy is satisfactory in 67.5% of patients with LPE in whom sertraline treatment unsatisfactory, and the effect of dapoxetine was independent of the effect of sertraline.Liu G, Yin Y, Zhang L. et al., Efficacy of Dapoxetine in the Treatment of Patients With Lifelong Premature Ejaculation as an Alternative to Sertraline Therapy. Sex Med 2021;10:100473.

Present study was aimed to formulate solid dispersions (SD) of Dapoxetine (DAPO), a drug with low water solubility with the help of PVP-30, Ploxomer-180 (P-180) and β-cyclodextrin (CD) by physical mixing to enhance the water solubility and dissolution of drug. Binary and Ternary solid dispersions were prepared with different ratios of drug and polymer and were further evaluated the effects of polymer at individual level as well as when used in combination. The solid dispersions were whitish in color, irregular in shape and have some rough surface when illustrated under SEM. Percentage yield of SDs ranged from 81-95% described the method was structured and significant. Solubility studies were carried out in 0.1N Hcl solution and was observed a remarkable increase in solubility of BSD 8, BSD 12 and TSD 6. Furthermore, the formulations were characterized by FTIR and PXRD. P-180 found an exceptional solubility promoter when used alone and in combination with CD as well. A remarkable enhance in Solubility and dissolution of DAPO was investigated in formulation prepared with ternary SD of Pol-180 and CD. [ABSTRACT FROM AUTHOR]

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Premature ejaculation is a male sexual problem that is marked by rapid ejaculation and quick attainment of orgasm. Dapoxetine belongs to the antidepressant category and modulates its action by preventing the reuptake of serotonin by neurons. Dapoxetine is marketed as an off‐label therapy for premature ejaculation. Here, two facile, sensitive, and green compatible approaches were established for dapoxetine assay. The approaches chemically rely on association complex formed between erythrosine‐B and dapoxetine in an acidic buffered medium. The quenching effect of the formed complex on the native erythrosine fluorescence at emission 553.5 nm is simply the main idea of spectrofluorimetric assay, while resonance Rayleigh scattering methodology uses augmentation of resonance Rayleigh scattering spectrum at 345 nm by the added dapoxetine. The current approaches exhibit linearity between response and dapoxetine concentration over 0.2–2.5 μg/ml and 0.3–3.0 μg/ml for spectrofluorimetric and resonance Rayleigh scattering (RRS) methods, respectively. All variables affecting methods and complex formation were studied and precisely optimized. The criteria of validation were performed by the directives provided by International Conference on Harmonization's (ICH) Guidelines and limits of detection were 0.06 and 0.05 μg/ml for spectrofluorimetric and RRS techniques, respectively. Finally, the approaches were applied with acceptable results for pharmaceutical formulation analysis. [ABSTRACT FROM AUTHOR]

Nowadays bioanalytical techniques including liquid and gas chromatography combined with different types of detectors are largely introduced in a practice. They are largely used for detection and control of substances and for monitoring of the whole production process. The type of detector depends on necessary levels of detection, but also on the matrix where aimed compounds have to be determined. Herein are summarized data from the last ten years related to determination of six main prohibited substances sildenafil, tadalafil, vardenafil, dapoxetine, yohimbine and sibutramine as well as their derivatives in food supplements using high performance liquid chromatography combined with mass spectrometric or UV detection. All these compounds are in a large interest because they are introduced often in products freely distributed in the internet market. [ABSTRACT FROM AUTHOR]

Dapoxetine is the first oral medication specifically developed for the on‐demand treatment of premature ejaculation. The pharmacokinetics and safety of 30 mg (n = 40) and 60 mg (n = 38) dapoxetine in healthy Chinese under fasted and fed states were assessed in 2 studies. Both studies are random, single‐center, 2‐period, open‐label, 2‐way crossover designs. Plasma concentration of dapoxetine was determined by high‐performance liquid chromatography–tandem mass spectrometry, and the pharmacokinetic parameters were calculated using noncompartmental analysis. Dapoxetine was quickly absorbed and reached maximum concentration 1 to 3 hours after oral administration. Elimination was biphasic, and the plasma concentration decreased to 3% to 7% of maximum concentration by 24 hours while half‐life was 15 to 18 hours. Meantime, high‐fat meals slightly increased its exposure. Both doses of dapoxetine were well tolerated. The adverse events in the high‐dose group under fasted and fed states were 37.9% and 19.0%, respectively. [ABSTRACT FROM AUTHOR]

This study was to explore whether serotonin transporter gene‐linked polymorphic region polymorphisms (5‐HTTLPR+rs25531) influence the response to dapoxetine treatment in a Chinese population with premature ejaculation (PE). 112 patients with PE re‐enrolled from our previous study received dapoxetine monotherapy. At the endpoint, patients with S'S' had a significant increased risk of nonresponse compared with L' carriers (p <.001). The improvement in S'S' genotype was significantly lower in premature ejaculation profile (PEP) items of 'control over ejaculation' (p =.035) and 'distress related to ejaculation' (p =.017) than that in L' carriers. As to clinical global impression of change (CGIC), results in S'S' subjects showed significantly lower scores (p =.008) and a less satisfaction rate reporting at least 'better' (p =.020) compared with L' carriers. Moreover, our findings suggested that patients with S'S' were more likely to develop adverse effects (AEs) compared with L' carriers (p =.040). This study suggests that PE patients bearing the S'S' genotype have an inferior comprehensive efficacy and safety of dapoxetine treatment, which consist of poorer response in IELTs, less improvement in patient‐reported outcome (PRO) measures and greater incidence of AEs, than L' carriers. Variants of triallelic 5‐HTTLPR may play a major role as a predictor of treatment response to dapoxetine. [ABSTRACT FROM AUTHOR]

Restriction measures enacted during the COVID-19 pandemic had severe effects on male sexual and reproductive health. We aimed to investigate the real-life impact and perception of sexual function in 2020 in Italy, as the first Western country experiencing a national lockdown by measuring relative search volume for keywords pertaining to sexual health and behaviors provided by Google Trends and sales data for pro-erectile treatments. No significant change was observed for erectile dysfunction and premature ejaculation. Interest towards most phosphodiesterase type 5 inhibitors decreased significantly during lockdown (e.g., sildenafil, p = 0.0002; tadalafil p = 0.0016), then reverted to pre-lockdown levels (e.g., sildenafil, p < 0.0001; tadalafil p < 0.0001), mirroring a concomitant sales decrement (p = 0.0292). A subsequent recovery to previous levels at the end of the social confinement was also found (e.g., after vs. before lockdown, sildenafil, p = 0.8459; tadalafil p = 0.1166). During lockdown, interest towards pornography significantly increased during restrictions (p = 0.0053) and remained high (after vs. before lockdown, p = 0.0004), whereas interest towards paid and casual sex declined (p = 0.0015 and p = 0.049, respectively), then reverted to previous levels (after vs. before lockdown, p = 0.3969 and 0.8373, respectively). During the first Italian lockdown, we observed a transient but measurable decrease of sexual health-seeking behaviors and changes in sexual behaviors, with unknown impact for sexual medicine and public health. [ABSTRACT FROM AUTHOR]

Abstract Background The treatment effect of dapoxetine in real-world practice is not well established. This study was to investigate the factors influencing efficacy of dapoxetine for the treatment of Premature ejaculation (PE) in the real-world setting. Methods Altogether 154 patients were followed up between Jan 2015 and Dec 2015. The clinical global impression of change (CGIC), premature ejaculation profile (PEP), the estimated intravaginal ejaculation latency time (eIELT) and estimated number of intravaginal thrusts before ejaculation (NITBE) were collected. The clinical characteristics of patients with CGIC = 0 and CGIC≥1 were compared. Results After 4 weeks treatment, an obvious improvement compared with the baseline was found regarding mean eIELT (2.4 ± 1.6 min vs 1.0 ± 0.7 min, P

Background: Premature ejaculation (PE) isn’t life-threatening, but it has a negative influence on the lives of both the patient and their partners. Varied researches have employed different definitions of PE, which include, for example, the number of intra-vaginal thrusts and the duration of male voluntary control. Dapoxetine is a selective serotonin reuptake inhibitor (SSRI) medication, one of many commonly prescribed for depressive symptoms. Cognitive behavioral therapy (CBT) has been widely utilised to treat PE prior to the availability of dapoxetine. Other than dapoxetine, other Off-label usage of SSRIs in the treatment of PE has increased in recent years. Objective: Assessment of possible role of dapoxetine in premature ejaculation management. Methods: Dapoxetine, serotonin reuptake inhibitors, and premature ejaculation were all looked for in PubMed, Google scholar, and Science direct. References from relevant literature were also evaluated by the authors, but only the most recent or complete studies from February 2001 to May 2021 were included. Due to the lack of sources for translation, documents in languages other than English have been ruled out. Papers that did not fall under the purview of major scientific investigations, such as unpublished manuscripts, oral presentations, conference abstracts, and dissertations, were omitted. Conclusion: Clinical evidence demonstrated that treatment for people with long-term or acquired PE, dapoxetine is highly effective as well as safe, and the unique properties of dapoxetine make it an appropriate choice for on-demand dosage. [ABSTRACT FROM AUTHOR]

Khalid M El-Say,1,2 Osama AA Ahmed,1,3 Amir I Mohamed,4 Martin K Safo,5 Abdelsattar M Omar6,7 1Nanotechnology Laboratory, Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo 11651, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia 61519, Egypt; 4Department of Pharmaceutics and Industrial Pharmacy, Military Medical Academy, Cairo, Egypt; 5Department of Medicinal Chemistry, and the Institute for Structural Biology, Drug Discovery and Development, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA; 6Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia; 7Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo 11884, EgyptCorrespondence: Khalid M El-SayPharmaceutics and Industrial Pharmacy, Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, P.O. Box: 80260, Jeddah, Saudi ArabiaTel +966 126 400 0002 0073Fax +966 12 695 1696Email kelsay1@kau.edu.saBackground: Premature ejaculation (PE) is the most common type of male sexual disorder with important psychological consequences. Dapoxetine (DPX), a recently approved drug for the treatment of PE, suffers from low bioavailability with large variability that ranges from 15–76% (mean 42%) after oral administration. The objective of this study is to optimize the parameters for the preparation of DPX-Zein-alpha lipoic acid (ALA) nanoparticles (NPs) to improve the bioavailability of DPX and consequently decrease therapeutic dose and adverse effect, leading to patient satisfaction and compliance.Methods: We investigated the effect of ALA concentration, PVA concentration and stirring rate on nanoparticle size (Y1), zeta potential (Y2), initial DPX release (Y3) and cumulative DPX release (Y4). In addition, in vivo pharmacokinetic study was performed for the optimized DPX formulation on human healthy volunteers compared with marketed DPX tablet.Results: The optimized DPX-loaded NPs showed Y1, Y2, Y3, and Y4 of 159.24 nm, 19.14 mV, 25.31% and 95.9 %, respectively. A single oral dose of 30 mg of optimized DPX-loaded NPs to human volunteers resulted in 2-fold improvement of AUC (1376.145±339.592 vs 709.178±146.307 in DPX), 4-fold increase in tmax (2.5±0.314 vs 0.583±0.144), prolongation of MRT (7.637±1.373 compared to 6.031±1.826 h), but with reduction in t1/2 (5.283±1.077 vs 8.452±2.813).Conclusion: The clinical findings suggest 194% enhancement of relative bioavailability of the optimized DPX-loaded NPs, potentially leading to a decrease in therapeutic dose and associated side effects in the treatment of PE.Keywords: dapoxetine, premature ejaculation, mathematical experimental design, nanoparticles, clinical pharmacokinetics, bioavailability

Dapoxetine HCl is used for the treatment of premature ejaculation. Dapoxetine is primarily metabolized in the liver and kidney and its metabolites are inactive; resulting in reduced bioavailability. Also, one of the commonly encountered issues in the oral dapoxetine formulae is its bitter taste. Thus, the objective of this study was to develop and to optimize novel dapoxetine taste-masked oral thin films (OTFs), to offer a faster dissolution rate, rapid release pattern, lower liver metabolism, and better patient compliance. To achieve our goal, the applicability of either pullulan or maltodextrin as strip forming polymers were investigated in the preparation of (OTFs), while glycerol was used as a plasticizer. Also, the physicochemical characteristics of dapoxetine in a resinate complex with AmberLiteTM -IRP69 as taste masking were evaluated. Furthermore, a 23 factorial design was used to study and to optimize the effect of the independent variables (strip forming polymer (X1), glycerol (X2) and AmberLiteTM (X3) amounts) on the disintegration time (Y1), degree of elongation (Y2), and degree of in vitro drug release in phosphate buffer pH 6.8 at 5 minutes (Q5min, Y3) as responses. P2 batch (OTF) (pullulan 96 mg, glycerol 12 mg, AmberLiteTM 32 mg, and dapoxetine 30 mg) was identified as an optimized formulation showing an in vitro disintegration time 9.33 s, 35.56% elongation, and 91.43% Q5min; excellent in vivo disintegration time; good overall taste acceptability and stable resinate complex. [ABSTRACT FROM AUTHOR]

Introduction: Dapoxetine on demand has been approved for premature ejaculation (PE) management in China; however, studies on the efficacy and safety of this treatment in the Chinese population are scarce. Aim: The aim of this study was to evaluate the safety and effectiveness of dapoxetine 30 mg and 60 mg on demand in Chinese men with PE. Methods: Phase IV real-world study on 1,252 patients with PE. If men reported no response to dapoxetine 30 mg after 4 weeks treatment, dapoxetine has been uptitrated at 60 mg for 4 weeks more. Main Outcome Measure: Self-reported data were collected for demographics, general and sexual health characteristics, PE severity, and treatment safety and effectiveness, as measured by the PE profile questionnaire. Results: Adverse events (AEs), such as nausea, thirst, headache, and dizziness, similarly to previous literature, were detected. The treatment-emergent AEs rate was higher in the patients treated with 30 and 60 mg (n = 192) compared with those treated with the dapoxetine 30 mg only (n = 1060) (34.4% vs 15.8%, respectively). No new safety concerns were observed. The overall effectiveness rates were 88.2% in subjects using 30 mg of dapoxetine, whereas a rescue from the previous failure was in 55.7% in the patients who received 60 mg after the initial 30 mg. Overall, 83.2% responded to dapoxetine at dosages equal to or lower than 60 mg. Conclusion: The results in this study demonstrated in a large Chinese population that on-demand dapoxetine is a safe and effective symptomatic treatment in patients with PE.J Peng, L Yang, L Liu, et al. Safety and Effectiveness of Dapoxetine On Demand in Chinese Men With Premature Ejaculation: Results of a Multicenter, Prospective, Open-Label Phase IV Study. Sex Med 2021;9:100296.

The inhibiting effect of the dapoxetine drug towards corrosion of aluminum alloy (AA6063) in 1.0 M HCl and 1.0 M NaOH solutions using weight loss, potentiodynamic polarization, and theoretical calculation. The results demonstrated that the inhibition efficiency (IE%) was increased with increasing the concentration of dapoxetine and lowering the temperature. IE% of dapoxetine is higher in 1.0 M HCl than in 1.0 M NaOH solution. The activation parameters of the corrosion process are endothermic, and the formation of the activated compound includes an association process. Inhibition was demonstrated in light of the horizontal adsorption of the complex formed between dapoxetine and the alloy surface on AA6063 according to the Langmuir absorption isotherm. The inhibition performance of Dapxitine on AA6063 was investigated using materials Studio v7.0. The quantum chemical descriptors are found to suitable to explain the performance of title molecule as corrosion inhibitors. Additionally, adsorption of dapoxetine on an aluminum alloy (Al) (111) has been investigated. The results of the current theoretical approach comply with that obtained experimentally. [ABSTRACT FROM AUTHOR]

Objective: To explore the clinical effect of warm acupuncture with large-quantity moxibustion on primary premature ejaculation (kidney deficiency and liver stagnation)., Methods: A total of 240 patients with primary premature ejaculation (kidney deficiency and liver stagnation) were randomly divided into a warm acupuncture group (80 cases, 5 cases dropped out), an acupuncture group (80 cases, 4 cases dropped out) and a western medication group (80 cases, 6 cases dropped out). In the warm acupuncture group, a large quantity of moxibustion was delivered after acupuncture at Baihui (GV 20), Qihai (CV 6), Guanyuan (CV 4) and Zhongji (CV 3), as well as bilateral Fengchi (GB 20), lateral line 3 of forehead (MS 4), neishengzhiqi (TF 2 ), Ganshu (BL 18), Shenshu (BL 23), and etc. One treatment with warm acupuncture took 40 min, once daily; five treatments were given per week and 4 weeks of treatment was required. In the acupuncture group, moxibustion was not delivered, and the rest operation of acupuncture was same as the warm acupuncture group. In the western medication group, dapoxetine hydrochloride tablets were administered orally, 30 mg each time, taken with warm water 1 h to 3 h before sexual intercourse. Medication was administered at most once within 24 h, twice per week, and 6 times within 4 weeks. Before and after treatment, the score of TCM symptoms, the score of premature ejaculation diagnostic tool (PEDT), intravaginal ejaculation latency time (IELT) and the serum sex hormone content (testosterone [T], luteinizing hormone [LH] and follicule stimulating hormone [FSH]) were observed and the clinical effect was evaluated in the three groups., Results: After treatment, the scores for less duration of intercourse (<1 min), post-ejaculation fatigue, low spirit and decreased libido, and the total scores of TCM symptoms, as well as PEDT scores were reduced when compared with those before treatment in each group ( P <0.01, P <0.05), and IELT was prolonged ( P <0.01) in the three groups. The serum T content was increased when compared with that before treatment in the warm acupuncture group ( P <0.05). After treatment, in comparison with the acupuncture group and the western medication group, the scores for post-ejaculation fatigue, soreness and weakness in the lumbar region and knee joints, decreased libido, insomnia, dream-disturbed sleep and frequent nocturnal enuresis, as well as the total score of TCM symptoms were lower ( P <0.05, P <0.01) and the serum T content was increased ( P <0.05) in the warm acupuncture group. When compared with the acupuncture group, PEDT scores were lower and IELT prolonged in the warm acupuncture group and the western medication group ( P <0.05, P <0.01). The total effective rate was 82.7% (62/75) in the warm acupuncture group, higher than that of the acupuncture group (68.4%, 52/76) and the western medication group (64.9%, 48/74, P <0.05) respectively., Conclusion: Warm acupuncture with large-quantity moxibustion ameliorates the clinical symptoms and increases intravaginal ejaculation latency time and the levels of sex hormone in the patients with primary premature ejaculation (kidney deficiency and liver stagnation).

Introduction: Dapoxetine is considered a first-line treatment for patients with lifelong premature ejaculation (PE), and current researches have showed with functional magnetic resonance imaging (fMRI) that patients with lifelong PE might have abnormal brain function, but differences in brain function before and after administration have not been reported. Aim: The aim of this study was to determine some objective differences in brain function between patients with lifelong PE before and after administration and healthy individuals. Methods: In this study, 17 patients with lifelong PE and 11 healthy controls underwent clinical assessments and resting-state fMRI examination. After 4 weeks of treatment with dapoxetine 30 mg as needed, patients with PE underwent the same fMRI examination again 3 hours after dapoxetine administration. Main Outcome Measure: The data were preprocessed using a data processing assistant for resting-state fMRI, and voxelwise amplitude of low-frequency fluctuation (ALFF) maps was calculated to identify abnormal neural activity in the brain. Results: (a) The ALFF of patients with PE was significantly lower in the bilateral hippocampus and thalamus and higher in the left fusiform and lingual gyrus than that of healthy controls; (b) decreased and increased ALFF in patients with PE recovered after dapoxetine administration. Conclusion: We preliminarily identified the relevant sites by analyzing changes in the ALFF in patients with lifelong PE. Analyzing ALFF changes in the brain by resting-state fMRI is an effective method to study PE, and it might provide a reference for disease diagnosis and future research.Yubo M, Lianjia H, Cuiping M, et al. Changes in the Amplitude of Low-Frequency Fluctuation in Patients With Lifelong Premature Ejaculation by Resting-State Functional MRI. Sex Med 2021;9:100287

To evaluate the safety and efficacy of Chinese medicine, Qiaoshao formula combined with dapoxetine was used for the treatment of premature ejaculation in a real‐life setting. Nine hundred and five males diagnosed with premature ejaculation were reviewed in this retrospective cohort study. We divided the patients into two groups: dapoxetine alone and Qiaoshao formula combined with dapoxetine according to actual interventions provided to patients in clinics. The perceived intravaginal ejaculation latency time and the premature ejaculation profile measures markedly improved in both groups. However, in men with severe premature ejaculation (baseline perceived intravaginal ejaculation latency time <1 min) and those with baseline age ≤30 years, the perceived intravaginal ejaculation latency time was slightly but significantly longer with combined therapy than with dapoxetine alone (p <.05). Therefore, combined therapy involving the Qiaoshao formula and dapoxetine proved to safe as well as effective for treating premature ejaculation while prolonging the perceived intravaginal ejaculation latency time, which significantly improved the overall satisfaction of the patient and likely that of the couple. [ABSTRACT FROM AUTHOR]

Premature ejaculation (PE; early ejaculation or rapid ejaculation) is a common sexual problem affecting about 20-30% of men in the sexually active age group. PE can be of four types: Primary, secondary, natural variable, and subjective PE. Various non-pharmacological and pharmacological treatment options are available to treat PE including Dapoxetine, which is specifically developed for the treatment of PE. In this review, we discuss the pathophysiology and management aspects of PE. [ABSTRACT FROM AUTHOR]

INTRODUCTION: Premature ejaculation(PE) decreases sexual pleasure and quality of life, and both Fluoxetine and Dapoxetine were used in PE therapy. Dapoxetine is the first SSRI with a short half-life and fewer side effects, primarily designed for PE therapy. The aim is to evaluate and compare the effects of Fluoxetine and Dapoxetine on PE symptoms and marital satisfaction. MATERIALS AND METHODS: 44 participants aged between 18 and 64 with a PEDT score of ≥9 from Hospital USM's Primary-Care-Clinic, Kelantan Malaysia were selected and randomized into two groups: Fluoxetine(FG) and Dapoxetine Group(DG), and administered for 8 weeks with either regular Fluoxetine(20mg) or Dapoxetine (30mg) on-demand at least once a week. Premature Ejaculation Diagnostics Tool(PEDT) score was used to assess PE symptoms and Dyadic Satisfaction-Dyadic Adjustment Scale (DS-DAS) used to evaluate marital satisfaction at baseline and the 8th week. RESULT: 22 and 21 participants in FG and DG completed the study. For both groups, PEDT scores decreased substantially [from 11.41 to 5.45(P<0.001) among FG, from 13.43 to 3.10(P<0.001) among DG]. After adjustment of the baseline PEDT score, PEDT scores in DG(6.03 vs 2.49, P<0.001) were lower at the 8th week. All groups showed significantly improved DS-DAS scores [from 34.50 to 40.68(P<0.001) in FG, from 36.57 to 44.33(P<0.001) in DG]. No marked difference in DS-DAS was scored after adjustment of the baseline DS-DAS score(41.13 vs 43.86, P=0.055) at the end of the assessment. CONCLUSION: Treatment of PE with either Fluoxetine or Dapoxetine decreases PE symptoms and increases marital satisfaction. [ABSTRACT FROM AUTHOR]

This study compared the safety and efficacy of the on‐demand (OD) use of sertraline (50 mg), sertraline (100 mg) and dapoxetine (30 mg), and the daily use of sertraline (50 mg) in the treatment of patients with premature ejaculation (PE). This prospective randomised study involved 120 lifelong PE patients (intravaginal ejaculatory latency time [IELT]: <1 min; Arabic Index of Premature Ejaculation [AIPE] score: < 30) without secondary causes of PE, identified between March 2018 and May 2020. Patients were divided into 4 groups (30 patients per group) and treated for 8 weeks. Assessments were conducted using the AIPE form as a diagnostic tool. Sertraline (50 mg, daily; 196.7 ± 115.5 s) and sertraline (100 mg, OD; 173.3 ± 97.0 s) had similar IELT and AIPE scores. The latter groups had better results in comparison with sertraline (50 mg, OD; 100.5 ± 54.4 s) and dapoxetine (93.7 ± 53.5 s; p < 0.01). Sertraline (100 mg, OD) had a similar efficacy to that of sertraline (50 mg, daily) and was more effective than sertraline (50 mg, OD) and dapoxetine (30 mg, OD). Sertraline (100 mg, OD) can be considered in the treatment of lifelong PE treatment, having tolerable side effects. [ABSTRACT FROM AUTHOR]

The aim of our study was to compare melatonin levels of patients with lifelong premature ejaculation (LPE) (n:60) with healthy controls (n:30) and to investigate the changes of melatonin levels in the treatment with dapoxetine and sertraline. Age, body mass index, duration of marriage, weekly intercourse number, International Index of Erectile Function scores, Intravaginal Ejaculation Latency Time (IELT) and melatonin levels were recorded. LPE patients were divided into two treatment groups. The first group was included 30 patients, who received 60 mg dapoxetine for six weeks, twice a week, an hour before intercourse. The second group received 50 mg of sertraline daily, for six weeks. IELT and melatonin measures were repeated after the treatment. IELT (dapoxetine group: 41.22 ± 21.3 s, sertraline group: 48 ± 23.11 s, control group: 195.54 ± 84.14 s; p <.001) and melatonin levels (dapoxetine group: 5.75 ± 2.04 pg/mL, sertraline group: 5.49 ± 2.88 pg/mL, control group: 13.4 ± 12.09 pg/mL; p <.001) of both LPE groups were significantly lower than control group. Following the six‐week sertraline (before: 48 ± 23.11 s, after: 101.01 ± 59.55 s; p <.001) and dapoxetine (before: 41.22 ± 21.3 s, after: 97.39 ± 44.1 s; p <.001) treatments, IELT increased. The melatonin levels increased in the sertraline group (before: 5.49 ± 2.88 pg/mL, after: 10.6 ± 7.37 pg/mL; p <.001). Our results indicate that melatonin levels of LPE patients are lower than levels of healthy volunteers. Furthermore, we found a significant increase in melatonin levels following sertraline treatment. [ABSTRACT FROM AUTHOR]

Although the introduction of dapoxetine has ushered in a new era in the treatment of premature ejaculation, many patients with lifelong premature ejaculation (LPE) exhibit an unimproved clinical global impression even after treatment with dapoxetine. To investigate independent predictors of the improvement of Clinical Global Impression (iCGI) in patients with LPE treated with dapoxetine and develop a nomogram to predict a patient's likelihood of achieving iCGI. Data of 243 patients with LPE diagnosed at Xijing Hospital (Xi'an, China) and Northwest Women's and Children's Hospital (Xi'an, China) from January 2019 to May 2020 were analyzed. Independent predictors of iCGI were identified, and a nomogram was developed using R software based on a multivariate logistic regression model. The predictive accuracy of the nomogram was measured using the area under the receiver operating characteristic curve. The nomogram was calibrated by comparing predictions with observations. The primary outcome was the patient-rated Clinical Global Impression of Change scale score after a 4-week course of dapoxetine treatment, which was collected via an online questionnaire. A Clinical Global Impression of Change score of ≥1 was defined as iCGI in this study. Patients with LPE with at least a bachelor's degree, a self-reported intravaginal ejaculation latency time of >1 minute, and an International Index of Erectile Function question 5 score of ≥3 were independent factors associated with achieving iCGI, whereas a Premature Ejaculation Diagnostic Tool question 1 score of ≥2 was an independent factor negatively associated with achieving iCGI. The predictive accuracy of the nomogram, which was developed by integrating all variables with independent predictive significance, was 0.710 (95% confidence interval: 0.702–0.718). In addition, the calibration plot demonstrated excellent agreement between predictions and observations. If the predictive performance of our nomogram is further proven in multiple external validations, it can be used to select suitable patients for dapoxetine treatment, thereby reducing the number of patients discontinuing treatment. This study developed the first nomogram for predicting the likelihood of achieving iCGI in patients with LPE treated with dapoxetine. However, our nomogram was not externally validated using independent cohorts from other institutions. This study identified several independent predictors of iCGI in patients with LPE treated with dapoxetine. An effective nomogram was developed to predict their likelihood of achieving iCGI. External validations using data of Western patients with LPE are required to test the broader applicability of this Chinese patient-based tool. Hou G, Gao M, Zhang L, et al. An Internally Validated Nomogram for Predicting the Likelihood of Improvement of Clinical Global Impression in Patients With Lifelong Premature Ejaculation Treated With Dapoxetine. J Sex Med 2020;17:2341–2350. [ABSTRACT FROM AUTHOR]