Pharmacology of contraceptive steroids: a brief review

American Journal of Obstetrics and Gynecology
J W Goldzieher

Abstract

Blood levels from a given oral dose of medication vary widely from patient to patient, even within a relatively homogeneous population, and from group to group across national borders. An important mechanism of inter-individual variation is the first pass through the enterohepatic circulation. When drugs such as ethinyl estradiol and norethindrone undergo this process, part of an orally administered dose is inactivated, which results in wide ranges of bioavailability. In connection with this process, these drugs are also susceptible to various drug-to-drug interactions. Levonorgestrel is not subject to first-pass extraction by the liver, which results in virtually 100% bioavailability. It is unclear whether interpopulation variations in blood levels result from ethnic, geographic, nutritional, or other phenomena. Hepatic mechanisms are qualitatively different as demonstrated by striking differences in urinary patterns of ethinyl estradiol conjugates and hydroxylations of ethinyl estradiol from country to country.

References

Mar 17, 1978·European Journal of Clinical Pharmacology·R A OkerholmA J Glazko
Jul 1, 1985·Contraception·J Newburger, J W Goldzieher
Mar 1, 1983·Clinical Pharmacokinetics·M L OrmeA M Breckenridge

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Citations

Dec 24, 2010·Women's Health·Rogério Bonassi MachadoCassiana Galvão Giribela
Aug 4, 2004·European Journal of Clinical Pharmacology·Ornella BaisiniAlberto Lanzini
Aug 1, 2000·Maturitas·J Marsden
Sep 21, 2010·Contraception·Alison B EdelmanFrank Z Stanczyk
Jul 27, 2010·Contraception·Giuseppe Benagiano
Sep 16, 2003·Journal of Clinical Pharmacology·Thorir D BjornssonCaroline Loew
Apr 17, 2001·American Journal of Obstetrics and Gynecology·W H Kutteh, R D Franklin
Oct 1, 1992·Advances in Contraception : the Official Journal of the Society for the Advancement of Contraception·P J Hillard
Apr 7, 2010·Expert Opinion on Pharmacotherapy·Jeffrey T Jensen
Apr 15, 2005·Studies in Family Planning·Virginia J Vitzthum, Karin Ringheim
Apr 9, 2005·Endocrinology·Ai-Ming YuFrank J Gonzalez
Apr 13, 2005·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·Ingrid DuijkersChristine Klipping
Nov 9, 2004·The American Journal of Clinical Nutrition·Erik J GiltayPeter L Zock

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