Aim. To provide an overview of current knowledge on pharmacotherapy of premature ejaculation (PE). Materials and Methods. A comprehensive review of the literature was conducted using MEDLINE and analysis of crossreferences. The key points of methodology and pharmacology of various articles have been analysed and critically reviewed. Results. PE may have significant negative impact on quality of life. Various recommendations for drug treatment of PE have been found in the available literature, varying from anesthetic ointments to various antidepressants and phosphodiesterase inhibitors. Due to disturbing side effects, various drugs are not suitable for general use. On the other hand, topical anesthetics, clomipramine and some SSRIs have repeatedly been found safe and effective to delay ejaculation. Conclusions. Remarkable progress has been made in the treatment of PE. Further research into the neural, psychological and molecular mechanisms involved in PE will lead to the development of even safer, more effective and more convenient therapies for men with PE.