Dapoxetine: an evidence-based review of its effectiveness in treatment of premature ejaculation

In the integrated analysis of two Phase III studies by Pryor et al,46 increases from baseline in average IELT at 12 weeks were significantly greater for either dose of dapoxetine (30 mg or 60 mg) than for placebo in the subgroups of patients with baseline average IELTs ≤1 minute and ≤30 seconds. The subanalysis of these studies by Shabsigh et al49 highlighted the importance of perceived control over ejaculation for achieving increases in IELT. Patients who reported at least a two-category improvement in control after 12 weeks of dapoxetine therapy recorded a mean change in IELT of 3.8 (0.9–4.7) minutes, whereas those who reported less than a two-category improvement in control recorded a mean change in IELT of 0.8 (0.9–1.7) minutes (Table 2). Overall, the consistent nature of the results from the studies identified indicates substantial evidence for a significant increase in IELT with dapoxetine 30 mg and 60 mg, compared with placebo, in adult patients with PE. In a second pharmacokinetic study, single doses and multiple doses of dapoxetine (30 mg, 60 mg) were evaluated in a randomized, open-label, two-treatment, two-period, crossover study of 42 healthy male volunteers over 9 days Modi et al. 2006. Subjects received a single dose of dapoxetine 30 mg or 60 mg on day 1 (single-dose phase) and on days 4–9 (multiple-dose phase).

In the evolving landscape of pharmaceuticals, the Dapox 30mg tablet stands out as a significant breakthrough for individuals with specific health conditions. This article delves into the tablet’s myriad benefits, uses, side effects, and how it improves patients’ quality of life. Priligy (Dapoxetine) is rapidly absorbed and has a short half-life which minimizes the adverse effects that are common to the SSRI’s.

SSRIs act to block the axonal reuptake of serotonin from the synaptic cleft of central serotonergic neurons by 5-HT transporters, which desensitize the 5-HT1A and 5-HT1B receptors (64). The delay in ejaculation can occur within a few days; however, chronic administration for at least 2-3 weeks is necessary to maximize the drugs therapeutic effects (10). With the exception of fluvoxamine, most SSRIs have been shown to clinically delay ejaculatory time (Table 1) (75). 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%).

This medication is used to treat male sexual dysfunction such as premature ejaculation. In this study, we used CGIC to evaluate the satisfaction of dapoxetine and sertraline for the treatment of LPE. CGIC is a self-evaluation assay based on patients’ subjective feelings; so, it is not as objective a measure as IELT and may be influenced by physical or psychological factors. However, somehow, PE itself is a kind of subjective concept based on the PE diagnostic criteria14, and we should understand that patients’ satisfaction is our primary treatment target, especially among patients with PE.

More specifically, a novel selective serotonin reuptake inhibitor (SSRI), dapoxetine, will be evaluated for its pharmacokinetics, efficacy, and safety record in light of available preclinical and clinical data. Premature ejaculation (PE) is the most common male sexual disorder, and is estimated to affect up to 30% of men worldwide (Goldstein 2003). PE, unlike erectile dysfunction (ED), affects men of all ages equally, from 18-year-olds to the elderly. However, both PE and ED coexist, and often PE can masquerade or be misdiagnosed as ED in many men. TB 500 2 mg Canada Peptides buy online This is, in part, due to the lack of knowledge about PE, the absence of performing a careful history, and the non-existence of diagnostic tools for PE (Montague et al 2004). Despite its high prevalence and recognized adverse effects on men’s quality of life, only recently has attention been focused on investigating the causes of PE and developing new therapeutic strategies.

Psychological/behavioral therapy

The lack of chronic serotonergic stimulation with on-demand dapoxetine precludes serotonin receptor desensitization and the downregulation of postsynaptic serotonin receptors that typically occurs with chronic SSRI use, so that on-demand dosing for PE may minimize the risk of withdrawal symptoms Waldinger, 2007. The DSM-IV-TR criteria and a baseline IELT of less than 2 min on 75% of at least four sexual intercourse events were used to enrol subjects in four of the five phase III studies Buvat et al. 2009; McMahon et al. 2010; Pryor et al. 2006. However, 58% of subjects also met the ISSM criteria for lifelong PE Porst et al. 2010. Subjects reported having had PE for an average of 15.1 years, with 64.9% of subjects classified by the investigator as having lifelong PE at screening. Demographic and baseline characteristics were similar across studies, allowing analysis of pooled phase III data. Ejaculatory latency time is probably a genetically determined biological variable which differs between populations and cultures, ranging from extremely rapid through average to slow ejaculation.

• More specifically, a novel selective serotonin reuptake inhibitor (SSRI), dapoxetine, will be evaluated for its pharmacokinetics, efficacy, and safety record in light of available preclinical and clinical data.
• A systematic review of PDE-5 inhibitors used in this context failed to provide strong evidence to support a role for PDE-5 inhibitors in the treatment of men with lifelong PE who maintain normal erectile function (55,56).
• Dapoxetine is an effective, safe and well tolerated on-demand treatment for PE and, in the opinion of the author, is likely to fulfil the treatment needs of most patients.
• The involvement of central serotonergic neurotransmission in ejaculation has been investigated in a number of animal studies.

Perceived improvement in control over ejaculation

However, such a strong delay with on-demand treatment in the absence of serotonergic side-effects does not seem likely, as this implies better effects with on-demand treatment than previously reported daily treatment with 20 mg paroxetine (Waldinger 2005). As an absence of ejaculation delay with acute SSRI administration has been demonstrated in a number of animal sexual behavioral studies and based on current knowledge with conventional SSRIs, it is unlikely that on-demand use of SSRIs will delay ejaculation within 1–2 hours of intake (Mos et al 1999; Waldinger 2005). Based on animal studies, Waldinger et al (2005b) postulated that on-demand treatment of PE with conventional SSRIs will only be successful when an SSRI is combined with a 5-HT1A receptor antagonist, or another serotonergic intervention that acutely stimulates serotonergic release. Priligy has been proven effective in treating premature ejaculation, with studies demonstrating its high safety profile and tolerability.

What Is Dapoxetine?

Intraseminal vesicle pressure and electromyograms of bulbospongiosus muscles were used as physiological markers of the emission and ejection phases respectively. At all doses, dapoxetine significantly reduced the proportion of rats displaying PCA-induced ejaculation in a dose-dependent manner, from 78% of rats with vehicle to 33%, 22% and 13% of rats following intravenous dapoxetine 1, 3 and 10 mg/kg, respectively. Dapoxetine significantly decreased the AUC of PCA-induced intraseminal vesicle pressure increases and bulbospongiosus muscle contractile bursts by 78% at all doses, by 91% following dapoxetine 1 and 10 mg/kg, and by 85% following dapoxetine 3 mg/kg.

Seratoninergic neurons originate in the raphe nuclei and adjacent reticular formation of the brainstem (Waldinger 2005). After its production in the cell body, serotonin passes through the serotonergic neuron to the presynaptic membrane, where it is released into the synapse and acts on the postsynaptic receptors. By the action of serotonin transporters (5-HTT) on the presynaptic membrane, serotonin is returned to the presynaptic neuron. The process of serotonin release and its action on postsynaptic receptors is referred to as serotonergic neurotransmission (Waldinger 2005). Pharmacological modulation of ejaculation is a novel concept, radically going beyond the psychosexual model of PE etiopathogenesis. The introduction of serotonin reuptake inhibitors (SSRIs) has revolutionized the approach to the treatment of this disorder.