Hormonal contraception has been changing and evolving a lot in these last decades. The most relevant facts are the reduction in the dose of estrogens from the macro dose to the low dose and the developments of preparations combined with natural estrogens such as 17β-estradiol and estetrol that allow better control of the cycle and reduce metabolic effects. As additional facts, the development of progestins with greater antiandrogenic and anti-mineralocorticoid activity and the acquisition of combination where the suspension interval is reduced up to the minimum of 2–4 days give a greater stability in terms of efficacy and compliance. On such basis, the use of hormonal contraceptives will be discussed so as to disclose the real benefits and the most relevant insights to face menstrual cycle impairments and/or diseases where hormonal contraception might be the beneficial treatment.