Pharmacokinetics and biotransformation of orally administered oestrone sulphate and oestradiol valerate in post-menopausal women

Maturitas
A R AedoE Diczfalusy

Abstract

The pharmacokinetic properties and biotransformation of two orally active oestrogens, piperazine oestrone sulphate (PE1S, 2.5 mg/day) and oestradiol valerate (E2V, 2.0 mg/day), given alone or in combination with levonorgestrel (LNG, 250 micrograms/day) were compared in 8 post-menopausal women, using a randomized cross-over design. The end points measured in peripheral plasma included oestrone (E1), oestradiol (E2), oestriol (E3), oestrone sulphate (E1S), oestradiol sulphate (E2S) and oestriol sulphate (E3S). In addition, LNG and sex-hormone-binding globulin SHBG concentrations were also assessed. The plasma levels of E3 were invariably below the detection limit (220 pmol/l). The levels of all the other oestrogens analyzed were consistently higher and the area under the curve significantly greater (except in the case of E3S) following PE1S administration than those recorded after E2V ingestion. The terminal half-lives of the circulating oestrogens measured after PE1S administration did not differ from those found after E2V administration. After 21 days of PE1S administration (in combination with LNG for the last 10 days), the maximum levels of all the oestrogens (except those of E2) were significantly higher than those seen afte...Continue Reading

References

Jan 1, 1977·Acta Obstetricia Et Gynecologica Scandinavica. Supplement·J Spona, W H Schneider
Jan 1, 1977·Acta Obstetricia Et Gynecologica Scandinavica. Supplement·D E Englund, E D Johansson
Nov 1, 1976·Contraception·E WeinerE D Johansson
Mar 1, 1987·The Journal of Clinical Endocrinology and Metabolism·C LongcopeC C Johnston
Apr 1, 1988·Contraception·Y E ShiK Fotherby
Jul 1, 1967·British Journal of Preventive & Social Medicine·T Khosla, C R Lowe
Dec 1, 1982·Contraception·E WangE Diczfalusy
Jan 1, 1982·Clinical Pharmacokinetics·M Eichelbaum

❮ Previous
Next ❯

Citations

Oct 31, 2003·Maturitas·M HossainPatricia Ibarra de Palacios
May 17, 2001·Menopause : the Journal of the North American Menopause Society·C C SlaterF Z Stanczyk
Sep 29, 1998·The Journal of Pharmacy and Pharmacology·T B Vree, C J Timmer
Dec 15, 2015·Climacteric : the Journal of the International Menopause Society·L RazV M Miller
Aug 23, 2005·Climacteric : the Journal of the International Menopause Society·H Kuhl
Mar 29, 2002·Journal of Pharmaceutical Sciences·Uwe D Rohr, Katrin Saeger-Lorenz
Dec 15, 2016·Critical Reviews in Clinical Laboratory Sciences·Atoosa Rezvanpour, Andrew C Don-Wauchope
Aug 27, 2005·International Journal of Gynaecology and Obstetrics : the Official Organ of the International Federation of Gynaecology and Obstetrics·S PongsathaN Morakote
Mar 9, 2005·British Journal of Clinical Pharmacology·Marta ValleDavide Verotta
May 14, 2021·Expert Opinion on Pharmacotherapy·Andrea R GenazzaniTommaso Simoncini
Jul 29, 2021·Nature Reviews. Endocrinology·Michelle M Mielke, Virginia M Miller
Aug 26, 2021·Human Reproduction Update·Andrea R GenazzaniTommaso Simoncini

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.