Hormonal Contraceptives: Pharmacology Tailored to Women's Health

Hum Reprod Update. 2016 Sep;22(5):634-46. doi: 10.1093/humupd/dmw016. Epub 2016 Jun 15.


Background: In recent years, several new oral contraceptives have become available. In some ways, they represent an evolution in terms of individualization and compliance on the part of women. The new formulations make it increasingly possible to prescribe a specific hormonal contraceptive on an individual basis.

Methods: A systematic literature search of PubMed was performed using the following combination of terms: 'oral contraceptives', 'estroprogestins' and 'combined oral contraceptive'. Only English-language papers published between January 2000 and July 2014 were included in our analysis. The present review analyzes all aspects of the choice of oral contraceptives in the different phases of a woman's life in detail.

Results: Regarding the estrogen component, lowering the dose of ethinylestradiol (EE) helped reduce associated side effects. Natural estradiol is now available and represents a valid alternative to EE. And regarding progestins, the dose has changed over time, as well as the endocrine and metabolic characteristics. These are the fruit of much research into improvement of old products (19-nor-progesterone-derived progestins) with androgenic effects and testing of new molecules with improved metabolic neutrality in terms of insulin sensitivity and lipid parameters. New progestins were a genuine turning point because they greatly reduced major side effects, such as water retention, and their anti-androgenic properties made them indicated for all forms of hyperandrogenism associated with acne and mild hirsutism. The associations of estradiol/dienogest and estradiol/nomegestrol acetate are the most suitable contraceptives for women with abundant menstrual bleeding and can increase the number of potential users of hormonal contraception.

Conclusion: Progress in the provision of new oral contraceptives has improved the risk/benefit ratio, by increasing benefits and reducing risks. The present challenge is to tailor contraceptives to individual needs in terms of efficacy and protection of reproductive health.

Keywords: combined oral contraceptive; estroprogestins; hormonal contraception; oral contraceptives; women's health.

Publication types

  • Review

MeSH terms

  • Chemistry, Pharmaceutical
  • Contraception / methods
  • Contraceptives, Oral, Combined / adverse effects
  • Contraceptives, Oral, Combined / chemistry
  • Contraceptives, Oral, Combined / pharmacology*
  • Contraceptives, Oral, Hormonal / adverse effects
  • Contraceptives, Oral, Hormonal / chemistry
  • Contraceptives, Oral, Hormonal / pharmacology*
  • Drug Combinations
  • Ethinyl Estradiol / administration & dosage
  • Female
  • Humans
  • Menstruation / physiology
  • Norpregnenes / administration & dosage
  • Progestins
  • Risk Assessment
  • Women's Health*


  • Contraceptives, Oral, Combined
  • Contraceptives, Oral, Hormonal
  • Drug Combinations
  • Norpregnenes
  • Progestins
  • estroprogestin
  • Ethinyl Estradiol