Postmenopausal symptoms are systemic symptoms associated with estrogen deficiency after menopause. At present, treatments for postmenopausal symptoms include hormonal therapy (HT) and non-HT. However, the optimal regimen for balancing the benefits and risks remains unclear. This article reviewed the characteristics, regimens, and side effects of drugs used in hormonal and non-HT. However, HT is still the most effective treatment with safety in early initiation since menopause onset. Nevertheless, it is essential to evaluate the risks of related chronic diseases and customize individualized treatments. Possible estetrol preparations and more types of Tissue Selective Estrogen Complex formulations are potential directions of drug development in the future of HT. Regarding non-HT, fezolinetant, currently in phase III clinical trials, is poised to become a first-in-class therapy for vasomotor symptoms. Ospemifene, dehydroepiandrosterone (DHEA), and vaginal lasers can also be used for moderate-to-severe genitourinary syndrome of menopause. Recent data suggest a superior ef-ficacy and safety of vaginal lasers, but more validated evidence of long-term tolerability is needed to respond to the United States Food and Drug Administration warning. Herbal medication commonly used in Asia is effective in alleviating menopausal symptoms; however, its adverse effects still require more detailed reports and stan-dardized observation methods. This review contributes to a better understanding of drugs for the treatment of postmenopausal symptoms and provides useful information for clinical drug selection.