Journal ArticleDOI
Pharmacology of estrogens and progestogens: influence of different routes of administration.
TLDR
This review comprises the pharmacokinetics and pharmacodynamics of natural and synthetic estrogens and progestogens used in contraception and therapy, with special consideration of hormone replacement therapy.Abstract:
This review comprises the pharmacokinetics and pharmacodynamics of natural and synthetic estrogens and progestogens used in contraception and therapy, with special consideration of hormone replacement therapy. The paper describes the mechanisms of action, the relation between structure and hormonal activity, differences in hormonal pattern and potency, peculiarities in the properties of certain steroids, tissue-specific effects, and the metabolism of the available estrogens and progestogens. The influence of the route of administration on pharmacokinetics, hormonal activity and metabolism is presented, and the effects of oral and transdermal treatment with estrogens on tissues, clinical and serum parameters are compared. The effects of oral, transdermal (patch and gel), intranasal, sublingual, buccal, vaginal, subcutaneous and intramuscular administration of estrogens, as well as of oral, vaginal, transdermal, intranasal, buccal, intramuscular and intrauterine application of progestogens are discussed. The various types of progestogens, their receptor interaction, hormonal pattern and the hormonal activity of certain metabolites are described in detail. The structural formulae, serum concentrations, binding affinities to steroid receptors and serum binding globulins, and the relative potencies of the available estrogens and progestins are presented. Differences in the tissue-specific effects of the various compounds and regimens and their potential implications with the risks and benefits of hormone replacement therapy are discussed.read more
Citations
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Journal ArticleDOI
Guidelines for the Primary Prevention of Stroke A Guideline for Healthcare Professionals From the American Heart Association/American Stroke Association
Larry B. Goldstein,Cheryl Bushnell,Robert J. Adams,Lawrence J. Appel,Lynne T. Braun,Seemant Chaturvedi,Mark A. Creager,Antonio Culebras,Robert H. Eckel,Robert G. Hart,Judith A. Hinchey,Virginia J. Howard,Edward C. Jauch,Steven R. Levine,James F. Meschia,Wesley S. Moore,J.V. (Ian) Nixon,Thomas A. Pearson +17 more
TL;DR: Evidence-based recommendations are included for the control of risk factors, interventional approaches to atherosclerotic disease of the cervicocephalic circulation, and antithrombotic treatments for preventing thrombosis and thromboembolic stroke.
Journal ArticleDOI
The 2017 hormone therapy position statement of The North American Menopause Society.
JoAnn V. Pinkerton,Fernando Sánchez Aguirre,Jennifer Blake,Felicia Cosman,Howard N. Hodis,Susan Hoffstetter,Andrew M. Kaunitz,Sheryl A. Kingsberg,Pauline M. Maki,JoAnn E. Manson,Polly Marchbanks,Michael R. McClung,Lila E. Nachtigall,Lawrence M. Nelson,Diane Todd Pace,Robert L. Reid,Phillip M. Sarrel,Jan L. Shifren,Cynthia A. Stuenkel,Wulf H. Utian +19 more
TL;DR: Hormone therapy (HT) remains the most effective treatment for vasomotor symptoms and the genitourinary syndrome of menopause (GSM) and has been shown to prevent bone loss and fracture.
Journal ArticleDOI
Guidelines for the Prevention of Stroke in Women A Statement for Healthcare Professionals From the American Heart Association/American Stroke Association
Cheryl Bushnell,Louise D. McCullough,Issam A. Awad,Monique V. Chireau,Wende N. Fedder,Karen L. Furie,Virginia J. Howard,Judith H. Lichtman,Lynda D. Lisabeth,Ileana L. Piña,Mathew J. Reeves,Kathryn M. Rexrode,Gustavo Saposnik,Vineeta Singh,Amytis Towfighi,Viola Vaccarino,Matthew Walters +16 more
TL;DR: This guideline focuses on the risk factors unique to women, such as reproductive factors, and those that are more common in women, including migraine with aura, obesity, metabolic syndrome, and atrial fibrillation, which believe a female-specific stroke risk score is warranted.
Journal ArticleDOI
Hormone Therapy and Venous Thromboembolism Among Postmenopausal Women Impact of the Route of Estrogen Administration and Progestogens: The ESTHER Study
Marianne Canonico,Emmanuel Oger,Geneviève Plu-Bureau,Jacqueline Conard,Guy Meyer,Hervé Lévesque,Nathalie Trillot,Marie-Thérèse Barrellier,Denis Wahl,Joseph Emmerich,Pierre-Yves Scarabin +10 more
TL;DR: Oral but not transdermal estrogen is associated with an increased VTE risk, and data suggest that norpregnane derivatives may be thrombogenic, whereas micronized progesterone and pregnane derivatives appear safe with respect toThrombotic risk.
Journal ArticleDOI
Effect of hormone replacement therapy on cardiovascular events in recently postmenopausal women: randomised trial
Louise Lind Schierbeck,Lars Rejnmark,Charlotte Landbo Tofteng,Lis Stilgren,Pia Eiken,Leif Mosekilde,Lars Køber,Jens-Erik Beck Jensen +7 more
TL;DR: After 10 years of randomised treatment, women receiving hormone replacement therapy early after menopause had a significantly reduced risk of mortality, heart failure, or myocardial infarction, without any apparent increase in risk of cancer, venous thromboembolism, or stroke.
References
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Journal ArticleDOI
Risks and benefits of estrogen plus progestin in healthy postmenopausal women: Principal results from the Women's Health Initiative randomized controlled trial
Jacques E. Rossouw,Garnet L. Anderson,Ross L. Prentice,Andrea Z. LaCroix,Charles Kooperberg,Marcia L. Stefanick,Rebecca D. Jackson,Shirley A.A. Beresford,Barbara V. Howard,Karen C. Johnson,Jane Morley Kotchen,Judith K. Ockene +11 more
TL;DR: Overall health risks exceeded benefits from use of combined estrogen plus progestin for an average 5.2-year follow-up among healthy postmenopausal US women, and the results indicate that this regimen should not be initiated or continued for primary prevention of CHD.
Journal ArticleDOI
Randomized Trial of Estrogen Plus Progestin for Secondary Prevention of Coronary Heart Disease in Postmenopausal Women
Stephen B. Hulley,Deborah Grady,Trudy L. Bush,Curt D Furberg,David M. Herrington,Betty Riggs,Eric Vittinghoff +6 more
TL;DR: Treatment with oral conjugated equine estrogen plus medroxyprogesterone acetate did not reduce the overall rate of CHD events in postmenopausal women with established coronary disease and the treatment did increase the rate of thromboembolic events and gallbladder disease.
Journal ArticleDOI
Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta
George G.J.M. Kuiper,Bo Carlsson,Kaj Grandien,Eva Enmark,Johan Häggblad,Stefan K. Nilsson,Jan-Åke Gustafsson +6 more
TL;DR: The messenger RNA expression of both ER subtypes in rat tissues by RT-PCR is investigated and the ligand binding specificity of the ER sub types is compared, revealing a single binding component for 16β-estradiol with high affinity.
Journal ArticleDOI
Effects of conjugated equine estrogen in postmenopausal women with hysterectomy: the Women's Health Initiative randomized controlled trial
Garnet L. Anderson,Marian C. Limacher,Annlouise R. Assaf,Tamsen Bassford,Shirley A.A. Beresford,Henry R. Black,Denise E. Bonds,Robert L. Brunner,Robert G. Brzyski,Bette J. Caan,Rowan T. Chlebowski,J. David Curb,Margery Gass,Jennifer Hays,Gerardo Heiss,Susan L. Hendrix,Barbara V. Howard,Judith Hsia,F. Allan Hubbell,Rebecca D. Jackson,Karen C. Johnson,Howard L. Judd,Jane Morley Kotchen,Lewis H. Kuller,Andrea Z. LaCroix,Dorothy S. Lane,Robert Langer,Norman L. Lasser,Cora E. Lewis,JoAnn E. Manson,Karen L. Margolis,Judith K. Ockene,Mary Jo O'Sullivan,Lawrence S. Phillips,Ross L. Prentice,Cheryl Ritenbaugh,John A Robbins,Jacques E. Rossouw,Gloria E. Sarto,Marcia L. Stefanick,Linda Van Horn,Jean Wactawski-Wende,Robert B. Wallace,Sylvia Wassertheil-Smoller +43 more
TL;DR: The use of conjugated equine estrogen (CEE) increases the risk of stroke, decreases therisk of hip fracture, and does not affect CHD incidence in postmenopausal women with prior hysterectomy over an average of 6.8 years, indicating no overall benefit.
Journal ArticleDOI
Effects of Estrogen or Estrogen/ Progestin Regimens on Heart Disease Risk Factors in Postmenopausal Women: The Postmenopausal Estrogen/Progestin Interventions (PEPI) Trial
Valery T. Miller,John C. LaRosa,Vanessa M. Barnabei,Craig M. Kessler,Ginny Levin,Ann Smith-Roth,Margaret Griffin,Diane B. Stoy,Trudy L. Bush,Howard A. Zacur,David A. Foster,Jean Anderson,Alice McKenzie,Susan C. Miller,Peter D. Wood,Marcia L. Stefanick,Robert Marcus,Allison Akana,W. Leroy Heinrichs,Charlene Kirchner,Katherine A. O'Hanlan,Melissa Ruyle,Mary A. Sheehan,Howard L. Judd,Gail A. Greendale,Richard Bayalos,Kathy Lozano,Kathy Kawakami,Elizabeth Barrett-Connor,Robert Langer,Donna Kritz-Silverstein,Mary Lou Carrion-Petersen,Carmela Cavero,Helmut G. Schrott,Susan R. Johnson,Deborah A. Feddersen,Denise L. Krutzfeldt,Jo Ann Benda,Carl J. Pauerstein,Jose Trabal,Robert S. Schenken,Michael P. Stern,Mercedes Rodriguez-Sifuentes,Carann Easton,H B Wells,Mark A. Espeland,George Howard,Robert Byington,Claudine Legault,Sally A. Shumaker,Patricia E. Hogan,Don Hire,Carol Wasilauskas,Margaret K. James,Kathy Lane,Tim Terrell,Stephanie Reece,June J Pierce,Mary Snow,Susan Anthony,Irma Mebane-Sims,Paula T. Einhorn,Sally Hunsberger,Myron A. Waclawiw,Ken Lippel,Diane L. Lucas,Joel Verter,Sherry Jackson,Joseph Kelaghan,Jeffrey M. Perlman,Pam Wolf,Joan McGowan,Stephen Gordon,Stephen Heyse,Judith E. Fradkin,Sherry Sherman,Lot B. Page,Ann Sorenson,Barbara S. Hulka,Baruch A. Brody,Ronald T. Burkman,Robert P. Heaney,Ronald M. Krauss,Harold Roberts,Janet Wittes,Lawrence Riggs,Richard Moss,John J. Albers,Santica M. Marcovina,S. Edwin Fineberg,Russell P. Tracy,Maria J. Merino,Robert E. Scully,Virginia A. LiVolsi,Gerald Kessler +94 more
TL;DR: Estrogen alone or in combination with a progestin improves lipoproteins and lowers fibrinogen levels without detectable effects on postchallenge insulin or blood pressure and in women with a uterus, CEE with cyclic MP has the most favorable effect on HDL-C and no excess risk of endometrial hyperplasia.
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Effects of conjugated equine estrogen in postmenopausal women with hysterectomy: the Women's Health Initiative randomized controlled trial
Garnet L. Anderson,Marian C. Limacher,Annlouise R. Assaf,Tamsen Bassford,Shirley A.A. Beresford,Henry R. Black,Denise E. Bonds,Robert L. Brunner,Robert G. Brzyski,Bette J. Caan,Rowan T. Chlebowski,J. David Curb,Margery Gass,Jennifer Hays,Gerardo Heiss,Susan L. Hendrix,Barbara V. Howard,Judith Hsia,F. Allan Hubbell,Rebecca D. Jackson,Karen C. Johnson,Howard L. Judd,Jane Morley Kotchen,Lewis H. Kuller,Andrea Z. LaCroix,Dorothy S. Lane,Robert Langer,Norman L. Lasser,Cora E. Lewis,JoAnn E. Manson,Karen L. Margolis,Judith K. Ockene,Mary Jo O'Sullivan,Lawrence S. Phillips,Ross L. Prentice,Cheryl Ritenbaugh,John A Robbins,Jacques E. Rossouw,Gloria E. Sarto,Marcia L. Stefanick,Linda Van Horn,Jean Wactawski-Wende,Robert B. Wallace,Sylvia Wassertheil-Smoller +43 more