Pharmacokinetic and Pharmacologic Variation Between Different Estrogen Products

  title={Pharmacokinetic and Pharmacologic Variation Between Different Estrogen Products},
  author={Mary Beth O’Connell},
  journal={The Journal of Clinical Pharmacology},
  • M. O’Connell
  • Published 1 September 1995
  • Biology, Medicine
  • The Journal of Clinical Pharmacology
Due to the complex nature of endogenous and exogenous hormone concentrations, formation, and metabolism and assay complexity, the pharmacokinetics of estrogens are difficult to study. Oral estrogens have minimal systemic bioavailability (2% to 10%) due to gut and liver (first‐pass) metabolism. High concentrations of estrone are achieved with oral administration, whereas higher concentrations of estradiol are generally achieved after percutaneous absorption. Although vaginal products (such as… 

Pharmacokinetics of estrogen and progesterone in chronic kidney disease.

These studies suggest that women with CKD should receive a least a 50% reduction in oral estradiol doses, and knowledge of the concentration effect relationship for the treatment of symptoms of menopause, as well as prevention of osteoporosis, will benefit all postmenopausal women.

The pharmacokinetics and efficacy of different estrogens are not equivalent.

  • R. Ansbacher
  • Medicine, Biology
    American journal of obstetrics and gynecology
  • 2001
The studies comparing estrogen formulations are summarized, the differential effects of various estrogen products that promote postmenopausal health are discussed, and the dosage and route of administration are discussed.

Evaluation of Single‐ and Multiple‐Dose Pharmacokinetics of Synthetic Conjugated Estrogens, A (Cenestin®) Tablets: A Slow‐Release Estrogen Replacement Product

A multiple‐dose, placebo‐controlled, randomized pharmacokinetic study was performed in 15 early (i.e., 1–3 years) postmenopausal women to evaluate the single and steady‐state pharmacokinetics of

Are all estrogens created equal? A review of oral vs. transdermal therapy.

  • M. Goodman
  • Medicine, Biology
    Journal of women's health
  • 2012
Significant differences appear to exist between oral and transdermal estrogens in terms of hormonal bioavailability and metabolism, with implications for clinical efficacy, potential side effects, and risk profile of different hormone therapy options, but neither results nor study designs are uniform.

Pharmacokinetics and systemic endocrine effects of the phyto-oestrogen 8-prenylnaringenin after single oral doses to postmenopausal women.

The decrease in LH serum concentrations found after the highest dose demonstrates the ability of 8-PN to exert systemic endocrine effects in postmenopausal women.

Hormone replacement therapy in menopausal women: Past problems and future possibilities

There is evidence that estriol, by binding preferentially to estrogen receptor-β, may inhibit some of the unwanted effects of estradiol, which is an increasingly popular alternative hormone therapy used for menopausal symptoms.

Estradiol pharmacokinetics after transdermal application of patches to postmenopausal women: matrix versus reservoir patches

Objective A new matrix 17β-estradiol transdermal patch incorporating lauric acid to improve estradiol skin absorption has been designed for hormone replacement therapy. Estradiol pharmacokinetics

Rationale for low-dose systemic hormone replacement therapy and review of estradiol 0.5 mg/NETA 0.1 mg

Estradiol 0.5 mg/norethisterone acetate 0.1 mg, despite being a lower dose than conventional hormones, is a compound, among a few other low-dose options, that can be used in hormone replacement therapy, and has demonstrated its effectiveness, with high tolerability and, apparently, no safety concerns, in a 6-month study.

Evaluation and Optimization of Pharmacokinetic Models for in Vitro to in Vivo Extrapolation of Estrogenic Activity for Environmental Chemicals

Three pharmacokinetic models with varying complexities to extrapolate in vitro to in vivo dosimetry for a group of 29 ER agonists were evaluated, finding the simplest had the best overall performance for predicting both oral and injection LELs from guideline uterotrophic studies, and can be parameterized entirely using freely available in silico tools.



Pharmacokinetics of estrogen

  • PG Stumpf
  • Medicine, Biology
    Obstetrics and gynecology
  • 1990

Biologic effects of transdermal estradiol.

Pharmacokinetics of estradiol, free and total estrone, in young women following single intravenous and oral administration of 17 beta-estradiol.

The purpose of the study was to determine the absolute bioavailability of orally administered E2 in a larger group of women and to assess the inter- and intraindividual variability of basic pharmacokinetic parameters of E2 and metabolically derived E1.

Interactions with oral contraceptives

  • K. Fotherby
  • Medicine, Biology
    American journal of obstetrics and gynecology
  • 1990

Antipyrine Pharmacokinetics in Women Receiving Conjugated Estrogens

Although antipyrine clearance is significantly impaired by oral contraceptives, there is no evidence of altered antipyrines pharmacokinetics from treatment with conjugated estrogens.

Effects of oral contraceptive steroids on acetaminophen metabolism and elimination

The data suggest that the increased clearance of acetaminophen from plasma in women taking OC steroids results from increased glucuronidation of the drug, although the mechanism is not known.

Transport of equine estrogens: binding of conjugated and unconjugated equine estrogens with human serum proteins.

The results indicate that the equine estrogens bind to SHBG and albumin in a manner similar to that of E1 and E2, and that the low MCR of EqS reported previously may be due to its binding to albumin.