History of Oral Contraceptives

Abstract

Progesterone is the naturally occurring female sex hormone acting as nature's contraceptive by preventing women from conceiving during pregnancy. Since it is not orally active, progesterone cannot practically be used as an oral contraceptive. It required the efforts of organic chemists to synthesise steroids that mimic the biological activity of the natural hormone and that are effective by oral administration. The article concludes with the prognosis that the future prospects for developing fundamentally new contraceptives are dim, primarily because the priorities of the international pharmaceutical industry have shifted to diseases of the increasingly geriatric segments of the population of affluent countries.

Key Concepts:

  • The natural female sex hormone progesterone – nature's contraceptive – is not orally active.

  • New synthetic steroids had to be developed, which retained the biological activity of progesterone, but would be orally active.

  • The lead compound, norethindrone, was synthesised in 1951 and all but one of the subsequent steroid oral contraceptives are based on that chemical template.

  • Research in new approaches to contraception has declined dramatically as the pharmaceutical industry has shifted its attention to diseases of the geriatric segment of the population.

  • The prediction is made that the ultimate direction of birth control in the affluent, geriatric countries will consist of cryopreservation of ‘young’ gametes (particularly relevant for females), followed by sterilisation, and recourse to IVF for reproduction, thus completing the divorce of sex from reproduction.

Keywords: norethindrone; progesterone; 19‐norprogesterone; the pill; norgestrel; norethynodrel; birth control; gamete preservation; oral contraception; ethynyloestradiol

Figure 1.

Chemical structures of (a) progesterone, (b) 19‐norprogesterone, (c) testosterone (R=H) and ethisterone (R=CCH), (d) norethindrone (R=CH3) and norgestrel (R=C2H5), (e) oestradiol (R=H) and 17α‐ethynyloestradiol (R=C°CH), (f) norethynodrel and (g) drospirenone.

close

Further Reading

Asbell B (1995) The Pill: A Biography of the Drug that Changed the World. New York: Random House.

Djerassi C (2001) This Man's Pill: Reflections on the 50th birthday of the Pill. Oxford: Oxford University Press.

Haberlandt E (2009) Ludwig Haberlandt – A pioneer in hormonal contraception. Wiener Klinische Wochenschreift 121(23/24): 746–749.

Haberlandt L (1931) Die hormonale Sterilisierung des weiblichen Organismus. Jena: Verlag Gustav Fischer.

Parnham MJ and Bruinvels J (eds) (1984) Discoveries in pharmacology, vol. 2. Haemodynamics, Hormones and Inflammation. Amsterdam: Elsevier.

Pincus G (1965) The Control of Fertility. New York: Academic Press.

Contact Editor close
Submit a note to the editor about this article by filling in the form below.

* Required Field

How to Cite close
Djerassi, Carl(Sep 2010) History of Oral Contraceptives. In: eLS. John Wiley & Sons Ltd, Chichester. http://www.els.net [doi: 10.1002/9780470015902.a0003628.pub2]