Literature DB >> 27542520

Clarification of contraceptive drug pharmacokinetics in obesity.

William J Jusko1.   

Abstract

Related to concerns about the role of obesity in the efficacy of contraceptive drugs, a review of the literature was carried out in regard to the pharmacokinetics of ethinyl estradiol and various progestins given by various routes of administration. Most studies show that obese women exhibit modestly lower plasma concentrations of these drugs (circa 30%) when given the same doses as normal-weight women. While the mechanism is uncertain, precedence in the literature suggests that this is due to body weight-related differences in metabolism rates. Confusing in some of the literature is that a few studies have reported erroneously calculated pharmacokinetic parameters after multiple dosing of oral contraceptives. A demonstration of appropriate pharmacokinetic methodology is provided. Copyright Â
© 2016 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Clearance; Contraceptive drugs; Model-fitting; Obesity; Pharmacokinetics; Volume of distribution

Mesh:

Substances:

Year:  2016        PMID: 27542520      PMCID: PMC5422994          DOI: 10.1016/j.contraception.2016.08.003

Source DB:  PubMed          Journal:  Contraception        ISSN: 0010-7824            Impact factor:   3.375


  41 in total

1.  Quantitative levonorgestrel plasma level measurements in patients with regular and prolonged use of the levonorgestrel-releasing intrauterine system.

Authors:  Beata Seeber; Stephanie C Ziehr; Andreas Gschlieβer; Aandrea Gschliesser; Christina Moser; Verena Mattle; Christoph Seger; Andrea Griesmacher; Nicole Concin; Hans Concin; Ludwig Wildt
Journal:  Contraception       Date:  2012-03-06       Impact factor: 3.375

Review 2.  The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery.

Authors:  Dennis A Smith; Li Di; Edward H Kerns
Journal:  Nat Rev Drug Discov       Date:  2010-12       Impact factor: 84.694

3.  Pharmacokinetics of a combined oral contraceptive in obese and normal-weight women.

Authors:  Carolyn L Westhoff; Anupama H Torgal; Elizabeth R Mayeda; Malcolm C Pike; Frank Z Stanczyk
Journal:  Contraception       Date:  2010-02-20       Impact factor: 3.375

Review 4.  The free hormone hypothesis: a physiologically based mathematical model.

Authors:  C M Mendel
Journal:  Endocr Rev       Date:  1989-08       Impact factor: 19.871

5.  Role of endocytosis in cellular uptake of sex steroids.

Authors:  Annette Hammes; Thomas K Andreassen; Robert Spoelgen; Jens Raila; Norbert Hubner; Herbert Schulz; Jochen Metzger; Florian J Schweigert; Peter B Luppa; Anders Nykjaer; Thomas E Willnow
Journal:  Cell       Date:  2005-09-09       Impact factor: 41.582

Review 6.  Metabolism and pharmacokinetics of contraceptive steroids in obese women: a review.

Authors:  Alison B Edelman; Ganesh Cherala; Frank Z Stanczyk
Journal:  Contraception       Date:  2010-05-26       Impact factor: 3.375

7.  Prolonged monitoring of ethinyl estradiol and levonorgestrel levels confirms an altered pharmacokinetic profile in obese oral contraceptives users.

Authors:  Alison B Edelman; Ganesh Cherala; Myrna Y Munar; Barent Dubois; Martha McInnis; Frank Z Stanczyk; Jeffrey T Jensen
Journal:  Contraception       Date:  2012-11-12       Impact factor: 3.375

Review 8.  Interactions of sex hormone-binding globulin with target cells.

Authors:  William Rosner; Daniel J Hryb; Scott M Kahn; Atif M Nakhla; Nicholas A Romas
Journal:  Mol Cell Endocrinol       Date:  2009-08-19       Impact factor: 4.102

9.  Pharmacokinetics of levonorgestrel and ethinylestradiol in 9 women who received a low-dose oral contraceptive over a treatment period of 3 months and, after a wash-out phase, a single oral administration of the same contraceptive formulation.

Authors:  W Kuhnz; G al-Yacoub; A Fuhrmeister
Journal:  Contraception       Date:  1992-11       Impact factor: 3.375

10.  Adiposity and sex hormones across the menstrual cycle: the BioCycle Study.

Authors:  E H Yeung; C Zhang; P S Albert; S L Mumford; A Ye; N J Perkins; J Wactawski-Wende; E F Schisterman
Journal:  Int J Obes (Lond)       Date:  2012-02-07       Impact factor: 5.095

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  3 in total

1.  Pharmacokinetics of the 1.5 mg levonorgestrel emergency contraceptive in women with normal, obese and extremely obese body mass index.

Authors:  Melissa Natavio; Frank Z Stanczyk; Emilie A G Molins; Anita Nelson; William J Jusko
Journal:  Contraception       Date:  2019-01-28       Impact factor: 3.051

2.  Atogepant Has No Clinically Relevant Effects on the Pharmacokinetics of an Ethinyl Estradiol/Levonorgestrel Oral Contraceptive in Healthy Female Participants.

Authors:  Wendy Ankrom; Jialin Xu; Marie-Helene Vallee; Marissa F Dockendorf; Danielle Armas; Ramesh Boinpally; K Chris Min
Journal:  J Clin Pharmacol       Date:  2020-04-16       Impact factor: 3.126

3.  Quantitative Assessment of Levonorgestrel Binding Partner Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling.

Authors:  Brian Cicali; Karthik Lingineni; Rodrigo Cristofoletti; Thomas Wendl; Joachim Hoechel; Herbert Wiesinger; Ayyappa Chaturvedula; Valvanera Vozmediano; Stephan Schmidt
Journal:  CPT Pharmacometrics Syst Pharmacol       Date:  2020-12-13
  3 in total

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