Dapoxetine: Hoạt chất ức chất tái hấp thu serotonin dùng để điều trị xuất tính sớm

These agents delay ejaculation in theory by reducing the sensitivity of the glans penis. The use of topical anesthetics is a relatively efficacious, user friendly, and inexpensive modality for PE treatment (48). However, they can cause penile glans numbness and condom use or prior washing off before sexual activity is required to prevent transference of the drug to the vaginal mucosa (14). Animal studies using rat experimental models have demonstrated that acute treatment with oral, subcutaneous and intravenous dapoxetine inhibits ejaculation at doses as low as 1 mg/kg. Dapoxetine appears to inhibit the ejaculatory reflex at a supraspinal level with the lateral paragigantocellular nucleus as a necessary brain structure for this effect Clement et al. 2007. To investigate the efficacy of dapoxetine in the treatment of patients with LPE as an alternative to sertraline therapy.

In addition to IELT, both doses of dapoxetine improved patient reported outcome measures compared to placebo (96). Dapoxetine was comparably effective both in men with lifelong and acquired PE (96,101,102). Selective serotonin reuptake inhibitors (SSRIs) are the most commonly prescribed medications for the treatment of a variety of mood disorders such as depression (62). The use of SSRIs to treat PE is based on the observation that delayed ejaculation and anorgasmia are common side effects of this class of drugs (41,63). SSRIs, either alone at low doses or in combination with psychosexual counseling are widely accepted as first line treatments for lifelong PE (14). Men with acquired PE generally receive targeted therapy aimed at resolving the underlying etiology of their PE, either with or without the addition of SSRIs (10).

Table 1. Medical treatment options for premature ejaculation ( .

Dapoxetine was rapidly absorbed, with mean maximal plasma concentrations of 297 and 498 ng/ml at 1.01 and 1.27 h after single doses of dapoxetine 30 and 60 mg, respectively (Table 1). Elimination of dapoxetine was rapid and biphasic, with an initial half life of 1.31 and 1.42 h, and a terminal half life of 18.7 and 21.9 h following single doses of dapoxetine 30 and 60 mg, respectively. The pharmacokinetics of dapoxetine and its metabolites were not affected by repeated daily dosing and steady state plasma concentrations were reached within 4 days, with only modest accumulation of dapoxetine (approximately 1.5 fold) (Figure 2(b)). Recently several studies have suggested that sildenafil may be beneficial in the treatment of PE, either as a single agent or in combination with SSRIs.

• Therefore, more trials are required to add further evidence for the efficacy of long-term dapoxetine use in PE.
• Preclinical safety pharmacology studies did not suggest an adverse electrophysiologic or hemodynamic effect with concentrations of dapoxetine up to twofold greater than recommended doses.
• Kaplan first suggested that PE was primarily a problem of voluntary control over timing of ejaculation, a concept on which most of the current definitions are based (Kaplan et al 1974).
• It is a centrally acting analgesic, which binds to both µ-opioid and gamma-aminobutyric acid (GABA) receptors.

Clinical studies of dapoxetine

In animal studies, the cyclic nucleotides cyclic adenosine monophosphate (cAMP) and/or cyclic guanosine monophosphate (cGMP) relax the smooth muscle of the rat and guinea pig vas deferens (Schultz et al 1977; Stjarne et al 1979; Kato et al 2000). Sildenafil has been shown to cause potent and selective potentiation of nitrergic transmission in the urogenital muscles in male mice (Frith and Gibson 2000). As human seminal vesicle smooth muscle relaxation and modulation of ejaculation were Drostanolone buy online reported to be regulated, in part, by increases of intracellular cGMP (Stjarne et al 1979). It is interesting to speculate on PDE-5 inhibitor action in this part of the body. In this technique the man is asked to pause during sexual stimulation, just prior to impending ejaculation.

Therefore, we used the CGIC as the standard to evaluate the PE therapeutic effect. In this study, we proved that, among patients with LPE in whom sertraline treatment unsatisfactory, dapoxetine treatment was satisfactory for 67.5% of the patients, which indicated that, despite unsatisfactory of sertraline treatment, dapoxetine could still be prescribed for the treatment of these patients with PE. When taken after full elution, 62.5% of patients with LPE, in whom sertraline is satisfactory, reported dapoxetine to be satisfactory, and there were no significant differences between the two groups. This means that the effect of dapoxetine to treat LPE is independent of the satisfaction of sertraline.

The pharmacokinetics of the drug depends on the dose, however, it does not depend on the consumption of food and alcohol. Priligy is metabolized in the liver too, inter alia, desmethyl dapoxetine and dimethyl dapoxetine. It is not recommended for use in patients with liver and kidney damage, as well as in patients taking drugs that affect cytochrome P450 (e.g. ketoconazole, ritonavir) and taking other serotonin reuptake inhibitors.

After taking it for at least six times, you should evaluate the benefits of continued use against the potential risks of frequent dosing. Some authors believe that medications should be taken for the whole period of sexual activity. Currently, the best results are achieved when taking medications for a limited period (60 days) in combination with a couple of sexual therapy; the man gains control over his ejaculation and strengthens himself in overcoming PE.