Skip to main content

Progestins and Oral Contraceptives

  • Chapter
Principles of Endocrine Pharmacology

Abstract

Development and maintenance of the female reproductive system are dependent on the cyclical interaction between estrogens, primarily es-tradiol-17β, and progesterone. The principal target tissues for these steroid hormones include the uterus, vagina, fallopian tubes, and mammary glands, as well as the anterior pituitary and hypothalamus. Although estrogens are recognized as promoters of cellular proliferation, progestins are known to facilitate cellular differentiation. In addition, progesterone and related drugs exert significant antiestrogenic effects. It is the balance between estrogen and progesterone actions that regulates the state of the female reproductive system. Some of the therapeutically useful derivatives of progesterone share a structural similarity to androgens, and these agents in some instances also produce androgenic or antiandrogenic activity.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

eBook
USD 16.99
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 16.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

Recommended Readings

Physiology and Pharmacology of the Progestins

  • Benagiano, G., Zulli, P., and Diczfalusy, E., Progestogens in therapy, Serono Symp. Ser. 3:1–270, 1983.

    Google Scholar 

  • Chan, L., and O’Malley, B. W., Mechanism of action of the sex steroid hormones, N. Engl. J. Med. 294:1322, 1976.

    Article  PubMed  CAS  Google Scholar 

  • Edgren, R. A., Progestagens, in: Clinical Use of Sex Steroids (J. R. Givens, ed.), pp. 1–29, Year Book Medical Publishers, Chicago, 1979.

    Google Scholar 

  • Gambrell, R.D., Menopause: Benefits and risks of estrogen-progestogen replacement therapy, Fertil. Steril. 37:457, 1982.

    PubMed  Google Scholar 

  • Gambrell, R. D., Proposal to decrease the risk and improve the prognosis of breast cancer, Am. J. Obstet. Gynecol. 150:119, 1984.

    PubMed  Google Scholar 

  • Gambrell, R. D., Bagnell, C. A., and Greenblatt, R. B., Role of estrogens and progesterone in the etiology and prevention of endometrial cancer: Review, Am. J. Obstet. Gynecol. 146:696, 1983.

    PubMed  CAS  Google Scholar 

  • Gold, R. B., and Wilson, P. D., Depo-Provera: New development in decade-old controversy, Fam. Plann. Perspect. 13:35, 1981.

    Article  PubMed  CAS  Google Scholar 

  • Grody, W. W., Schrader, W. T., and O’Malley, B. W., Activation, transformation and subunit structure of steroid hormone receptors, Endocrine Rev. 3:141, 1982.

    Article  CAS  Google Scholar 

  • Horowitz, K. B., Wey, L. L., Sedlacek, S. M., and d’Arville, C. N., Progestin action and progesterone receptor structure in human breast cancer: A review, Recent Prog. Horm. Res. 41:249–317, 1985.

    Google Scholar 

  • Keenan, E. J., The physiological and pathophysiological significance of steroid hormone receptors, Gynecol. Obstet. 5:343, 1982.

    Google Scholar 

  • Knobil, E., The neuroendocrine control of the menstrual cycle, Recent Prog. Horm. Res. 36:53, 1980.

    PubMed  CAS  Google Scholar 

  • McCarty, K. S., Jr., Lubahn, D. B., and McCarty, K. S., Sr., Estrogen and progesterone receptors: Physiological and pathological considerations, Clin. Endocrinol. Metab. 12:133, 1983.

    Article  PubMed  CAS  Google Scholar 

  • McGuire, W. L., and Clark, G. M., Role of progesterone receptors in breast cancer, J. Sem. Oncol. 12:12–16, 1985.

    CAS  Google Scholar 

  • Neumann, F., Progestogens: A short review, Postgrad. Med. J. (Suppl. 2) 54:11, 1978.

    CAS  Google Scholar 

  • O’Malley, B. W., Steroid hormone action in eukaryotic cells, J. Clin Invest. 74:307, 1984.

    Article  PubMed  Google Scholar 

  • Renoir, J. M., and Mester, J., Chick oviduct progesterone receptor: Structure, immunology, function, Mol. Cell Endocrinol. 37:1, 1984.

    Article  PubMed  CAS  Google Scholar 

  • Richards, J. S., Maturation of ovarian follicles: actions and interactions of pituitary and ovarian hormones on follicular cell differentiation, Physiol. Rev. 60:51, 1980.

    PubMed  CAS  Google Scholar 

  • Rochefort, H., and Chalbos, D., Progestin-specific markers in human cell lines: Biological and pharmacological applications, Mol. Cell Endocrinol. 36:36, 1984.

    Article  Google Scholar 

  • Whitehead, M. I., Townsend, P. T., Pryse-Davies, J., Ryder, T. A., and King, R. J. B., Effects of estrogens and progestins on biochemistry and morphology of postmenopausal endometrium, N. Engl. J. Med. 305:1599, 1981.

    Article  PubMed  CAS  Google Scholar 

  • Wilson, J. C., and Brent, R. L., Are female sex hormones teratogenic?, Am. J. Obstet. Gynecol. 141:567, 1981.

    PubMed  CAS  Google Scholar 

Pharmacology of the Oral Contraceptives

  • Andrews, W. C., Oral contraception: Physiologic and pathologic effects, Obstet. Gynecol. Ann. 7:325:1981.

    Google Scholar 

  • Back, D. J., Breckenridge, A. M., Crawford, F. E., MacIver, M., Orme, M. L. E., and Rowe, P. H., Interindividual variation and drug interactions with hormonal steroid contraceptives, Drugs 21:46, 1981.

    Article  PubMed  CAS  Google Scholar 

  • Benagiano, G., and Primiero, F. M., Long acting contraceptives: Present status, Drugs 25:570, 1983.

    Article  PubMed  CAS  Google Scholar 

  • Bronson, R. A., Oral contraception: Mechanism of action, Clin. Obstet. Gynecol. 24:869, 1981.

    Article  PubMed  CAS  Google Scholar 

  • Centers for Disease Control, Cancer and Steroid Hormone Study: Oral Contraceptive use and the risk of endometrial cancer, JAMA 249:1600, 1983.

    Article  Google Scholar 

  • Centers for Disease Control, Cancer and Steroid Hormone Study, Oral contraceptive use and the risk of ovarian cancer, JAMA 249:1596, 1983.

    Article  Google Scholar 

  • Centers for Disease Control, Cancer and Steroid Hormone Study, Long-term oral contraceptive use and risk of breast cancer, JAMA 249:1591, 1983.

    Article  Google Scholar 

  • Dalen, J. E., and Hickler, R. B., Oral contraceptives and cardiovascular disease, Am. Heart J. 101:626, 1981.

    Article  PubMed  CAS  Google Scholar 

  • Delia, J. E., and Emery, M. G., Clnical pharmacology and common minor side effects of oral contraceptives, Clin Obstet. Gynecol. 24:879, 1981.

    Article  PubMed  CAS  Google Scholar 

  • Diczfalusy, E., Gregory Pincus and steroidal contraception: A new departure in the history of mankind, J. Steroid Biochem 11:3, 1979.

    Article  PubMed  CAS  Google Scholar 

  • Dixon, G. W., Schlesselman, J. S., Ory, H. W., and Blye, R. P., Ethinylestradiol and conjugated estrogens as postcoital contraceptives, JAMA 244:1336, 1980.

    Article  PubMed  CAS  Google Scholar 

  • Dorflinger, L. J., Relative potency of progestins used in oral contraceptives, Contraception 31:557–570, 1985.

    Article  PubMed  CAS  Google Scholar 

  • Droegemaueller, W., and Bressler, R., Effectiveness and risks of contraception, Annu. Rev. Med. 31:329, 1980.

    Article  Google Scholar 

  • Edgren, R. A. Progestational potency of oral contraceptives: A polemic, Int. J. Fertil. 23:162, 1978.

    PubMed  CAS  Google Scholar 

  • Edgren, R. A., and Sturtevant, F. M., Potencies of oral contraceptives, Am. J. Obstet. Gynecol. 125:1029, 1976.

    PubMed  CAS  Google Scholar 

  • Goldzieher, J. W., Estrogens in oral contraceptives: Historical perspectives, Johns Hopkins Med. J. 150:165, 1982.

    PubMed  CAS  Google Scholar 

  • Greenblatt, R. B., Oral contraceptives: The state of the art, Clin. Ther. 8:6, 1985.

    PubMed  CAS  Google Scholar 

  • McQueen, E. G., Hormonal steroid contraceptives: A further review of adverse reactions, Drugs 16:322, 1978.

    Article  PubMed  CAS  Google Scholar 

  • McQueen, E. G., The long term safety of hormonal steroid contraceptives, Drugs 16:460, 1981.

    Article  Google Scholar 

  • Mishell, D. R., Non-contraceptive health benefits of oral steroid contraceptives, Am. J. Obstet. Gynecol. 142:809, 1982.

    PubMed  Google Scholar 

  • Realini, J. P., and Goldzieher, J. W., Oral contraceptives and cardiovascular disease: A critique of the epidemiologic studies, Am. J. Obstet. Gynecol. 152:729, 1985.

    PubMed  CAS  Google Scholar 

  • Smith, M. A., and Youngkin, E. Q., Current perspectives on combination oral contraceptives, Clin. Pharm. 3:485, 1984.

    PubMed  CAS  Google Scholar 

  • Speroff, L., The formulation of oral contraceptives: Does the amount of estrogen make any clinical difference?, Johns Hopkins Med. J. 150:170, 1982.

    PubMed  CAS  Google Scholar 

  • Stadel, B. V., Oral contraceptives and cardiovascular disease, N. Engl. J. Med. 305:612 (pt. 1), 672 (pt. 2), 1981.

    Article  PubMed  CAS  Google Scholar 

  • Upton, G. V., The phasic approach to oral contraception: The triphasic concept and its application, Int. J. Fertil. 28:121, 1983.

    PubMed  CAS  Google Scholar 

  • Wilson, E. A., Steroid contraception, in: Clinical Use of Sex Steroid (J. R. Givens, ed.), p. 117, Year Book Medical Publishers, Chicago, 1980.

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

Copyright information

© 1986 Plenum Publishing Corporation

About this chapter

Cite this chapter

Thomas, J.A., Keenan, E.J. (1986). Progestins and Oral Contraceptives. In: Principles of Endocrine Pharmacology. Springer, Boston, MA. https://doi.org/10.1007/978-1-4684-5036-1_8

Download citation

  • DOI: https://doi.org/10.1007/978-1-4684-5036-1_8

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-0-306-42143-3

  • Online ISBN: 978-1-4684-5036-1

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics