Chlorpromazine was the first tricyclic antidepressant used to treat premature ejaculation, and because of the large number of related studies, chlorpromazine has become a reference standard for determining the efficacy of antidepressants in the treatment of premature ejaculation. In 1973, Eaton published the results of a study on the treatment of premature ejaculation with chlorpromazine: only 1 of 13 patients with premature ejaculation was ineffective with chlorpromazine at 30-40 mg/d (maximum 75 mg/d). The treatment response appeared between 2 weeks and 2 months and sexual desire did not increase. The results confirm that tricyclics have a significant effect on the serotonergic system and are effective in the treatment of premature ejaculation. The dose of chlorpromazine in the treatment of premature ejaculation is 1/5 to 1/10 of that in antidepressant treatment, so the side effects are not significant in the treatment of premature ejaculation. The main side effects of chlorpromazine are dry mouth, constipation, nausea, sensory disturbance, sleep disturbance, fatigue and facial flushing. In view of the above side effects and the shortcomings of the relapse rate after discontinuation of the drug, Huaiqing plug et al. proposed that the amount of chlorpromazine for the treatment of premature ejaculation should be 25-50 mg orally, and advocated that all start with 25 mg, because the side effects are positively correlated with the dose, and one daily dose has achieved satisfactory efficacy, and suggested that chlorpromazine with behavioral therapy can significantly reduce the relapse rate after discontinuation of the drug. Many SSRIs such as fluoxetine, sertraline, paroxetine, and citalopram are widely used in the treatment of premature ejaculation; dapoxetine, which is currently in phase III clinical trials, is a promising one in the treatment of premature ejaculation. The possible mechanisms of SSRIs for premature ejaculation can be summarized as follows: ① delay ejaculation by increasing serotonergic neurotransmission and activating 5-HT2C receptors to raise the patient’s IELT threshold; ② increase penile sensory threshold and reduce penile hypersensitivity; ③ block the vicious circle between the two by treating depression and anxiety caused by premature ejaculation. Local anesthetics are one of the options for pharmacological treatment of premature ejaculation, but are less popular in patients with lifelong premature ejaculation. Intra-cavernous sinus injection of vasoactive drugs should not be recommended for the treatment of premature ejaculation for the time being due to the lack of evidence-based medical support. Studies have shown some efficacy of PDE-5 for the treatment of premature ejaculation, but also lack the support of evidence-based medical evidence. Although SSRIs have some side effects in the treatment of premature ejaculation, resulting in reluctance to take them long-term, they are still one of the best treatments for premature ejaculation. The combined use of SSRIs and 5-HT1A receptor antagonists can rapidly show ejaculatory delay effects and shows promise in the development of new drugs for the on-demand treatment of premature ejaculation. If EMEA (European Medicines Evaluation Agency) or FDA (US Food and Drug Administration) can approve dapoxetine for the treatment of premature ejaculation, it will be another addition to the pharmacological treatment of premature ejaculation. However, the relatively weak effect of dapoxetine compared to the stronger ejaculation-delaying effect of daily SSRIs would be a bottleneck limiting its general use in the treatment of lifelong premature ejaculation, where the desire for medical help and pharmacological treatment is often stronger.