Progesterone Use in Gynaecology
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Classification and Pharmacology of Progestins
Maturitas 46S1 (2003) S7–S16 Classification and pharmacology of progestins Adolf E. Schindler a,∗, Carlo Campagnoli b, René Druckmann c, Johannes Huber d, Jorge R. Pasqualini e, Karl W. Schweppe f, Jos H. H. Thijssen g a Institut für Medizinische Forschung und Fortbildung, Universitätsklinikum, Hufelandstr. 55, Essen 45147, Germany b Ospedale Ginecologico St. Anna, Corso Spezia 60, 10126 Torino, Italy c Ameno-Menopause-Center, 12, Rue de France, 06000 Nice, France d Abt. für Gynäkologische Endokrinologie, AKH Wien, Währingergürtel 18-20, 1090 Wien, Austria e Institute de Puériculture26, Boulevard Brune, 75014 Paris, France f Abt. für Gynäkologie und Geburtshilfe, Ammerland Klinik, Langestr.38, 26622 Westerstede, Germany g Department of Endocrinology, Universitair Medisch Centrum Utrecht, P.O. Box 85090, 3508 AB Utrecht, The Netherlands Abstract Besides the natural progestin, progesterone, there are different classes of progestins, such as retroprogesterone (i.e. dydroges- terone), progesterone derivatives (i.e. medrogestone) 17␣-hydroxyprogesterone derivatives (i.e. chlormadinone acetate, cypro- terone acetate, medroxyprogesterone acetate, megestrol acetate), 19-norprogesterone derivatives (i.e. nomegestrol, promege- stone, trimegestone, nesterone), 19-nortestosterone derivatives norethisterone (NET), lynestrenol, levonorgestrel, desogestrel, gestodene, norgestimate, dienogest) and spironolactone derivatives (i.e. drospirenone). Some of the synthetic progestins are prodrugs, which need to be metabolized to become active compounds. Besides -
2011/097571 A2
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau „ (10) International Publication Number (43) International Publication Date \i\ 11 August 2011 (11.08.2011) 2011/097571 A2 (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 38/22 (2006.01) A61P 11/06 (2006.01) kind of national protection available): AE, AG, AL, AM, A61K 31/573 (2006.01) A61P 11/00 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, A61P 29/00 (2006.01) A61P 37/00 (2006.01) CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (21) International Application Number: HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, PCT/US201 1/023917 KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, (22) International Filing Date: ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, 7 February 201 1 (07.02.201 1) NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, (25) Filing Language: English TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every (30) Priority Data: kind of regional protection available): ARIPO (BW, GH, 61/302,325 8 February 2010 (08.02.2010) US GM, KE, LR, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, 13/021,950 7 February 201 1 (07.02.201 1) US ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (71) Applicant (for all designated States except US): EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, PRAIRIE PHARMACEUTICALS, LLC [US/US]; LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, 1041 1 Motor City Drive, Suite 750, Bethesda, MD 20817 SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, (US). -
Combined Estrogen–Progestogen Menopausal Therapy
COMBINED ESTROGEN–PROGESTOGEN MENOPAUSAL THERAPY Combined estrogen–progestogen menopausal therapy was considered by previous IARC Working Groups in 1998 and 2005 (IARC, 1999, 2007). Since that time, new data have become available, these have been incorporated into the Monograph, and taken into consideration in the present evaluation. 1. Exposure Data 1.1.2 Progestogens (a) Chlormadinone acetate Combined estrogen–progestogen meno- Chem. Abstr. Serv. Reg. No.: 302-22-7 pausal therapy involves the co-administration Chem. Abstr. Name: 17-(Acetyloxy)-6-chlo- of an estrogen and a progestogen to peri- or ropregna-4,6-diene-3,20-dione menopausal women. The use of estrogens with IUPAC Systematic Name: 6-Chloro-17-hy- progestogens has been recommended to prevent droxypregna-4,6-diene-3,20-dione, acetate the estrogen-associated risk of endometrial Synonyms: 17α-Acetoxy-6-chloro-4,6- cancer. Evidence from the Women’s Health pregnadiene-3,20-dione; 6-chloro-Δ6-17- Initiative (WHI) of adverse effects from the use acetoxyprogesterone; 6-chloro-Δ6-[17α] of a continuous combined estrogen–progestogen acetoxyprogesterone has affected prescribing. Patterns of exposure Structural and molecular formulae, and relative are also changing rapidly as the use of hormonal molecular mass therapy declines, the indications are restricted, O CH and the duration of the therapy is reduced (IARC, 3 C 2007). CH3 CH3 O C 1.1 Identification of the agents CH3 H O 1.1.1 Estrogens HH For Estrogens, see the Monograph on O Estrogen-only Menopausal Therapy in this Cl volume. C23H29ClO4 Relative molecular mass: 404.9 249 IARC MONOGRAPHS – 100A (b) Cyproterone acetate Structural and molecular formulae, and relative Chem. -
Annex 2 Composition of Oral and Injectable Estrogen–Progestogen Contraceptives
ANNEX 2 COMPOSITION OF ORAL AND INJECTABLE ESTROGEN–PROGESTOGEN CONTRACEPTIVES Annex 2 lists the composition of brands of estrogen–progestogen preparations used in combined injectables (Table 1), combined oral (Table 2) and phasic oral (Table 3) contraceptives. The countries in which these formulations are used are noted. Are listed only those brands for which availability was reported. The source of these tables is the International Planned Parenthood Foundation (IPPF). Data have been taken from the IPPF 2002 website [http://contraceptive.ippf.org] at the time of the monograph meeting (June 2005). This online site is regularly updated. Table 1. Combined injectables Brand name Composition Countries of availability Acefil Dihydroxyprogesterone acetophenide 150 mg Paraguay + estradiol enanthate 10 mg Agurin Dihydroxyprogesterone acetophenide 150 mg Chile + estradiol enanthate 10 mg Anafertin Dihydroxyprogesterone acetophenide 75 mg El Salvador, Mexico + estradiol enanthate 5 mg Ciclofem Medroxyprogesterone acetate 25 mg Guatemala + estradiol cypionate 5 mg Ciclofemina Medroxyprogesterone acetate 25 mg El Salvador + estradiol cypionate 5 mg Ciclomes Dihydroxyprogesterone acetophenide 150 mg Paraguay + estradiol enanthate 10 mg Ciclovular Dihydroxyprogesterone acetophenide 150 mg Brazil + estradiol enanthate 10 mg Clinomin Dihydroxyprogesterone acetophenide 150 mg Paraguay + estradiol enanthate 10 mg Cyclofem Medroxyprogesterone acetate 25 mg Chile, Indonesia, Malaysia, Mexico, + estradiol cypionate 5 mg Panama, Zimbabwe Cyclofemina Medroxyprogesterone -
Combined Estrogen–Progestogen Menopausal Therapy
PHARMACEUTICALS volume 100 A A review of humAn cArcinogens This publication represents the views and expert opinions of an IARC Working Group on the Evaluation of Carcinogenic Risks to Humans, which met in Lyon, 14-21 October 2008 LYON, FRANCE - 2012 iArc monogrAphs on the evAluAtion of cArcinogenic risks to humAns COMBINED ESTROGEN–PROGESTOGEN MENOPAUSAL THERAPY Combined estrogen–progestogen menopausal therapy was considered by previous IARC Working Groups in 1998 and 2005 (IARC, 1999, 2007). Since that time, new data have become available, these have been incorporated into the Monograph, and taken into consideration in the present evaluation. 1. Exposure Data 1.1.2 Progestogens (a) Chlormadinone acetate Combined estrogen–progestogen meno- Chem. Abstr. Serv. Reg. No.: 302-22-7 pausal therapy involves the co-administration Chem. Abstr. Name: 17-(Acetyloxy)-6-chlo- of an estrogen and a progestogen to peri- or ropregna-4,6-diene-3,20-dione menopausal women. The use of estrogens with IUPAC Systematic Name: 6-Chloro-17-hy- progestogens has been recommended to prevent droxypregna-4,6-diene-3,20-dione, acetate the estrogen-associated risk of endometrial Synonyms: 17α-Acetoxy-6-chloro-4,6- cancer. Evidence from the Women’s Health pregnadiene-3,20-dione; 6-chloro-Δ6-17- Initiative (WHI) of adverse effects from the use acetoxyprogesterone; 6-chloro-Δ6-[17α] of a continuous combined estrogen–progestogen acetoxyprogesterone has affected prescribing. Patterns of exposure Structural and molecular formulae, and relative are also changing rapidly as the use of hormonal molecular mass therapy declines, the indications are restricted, O CH and the duration of the therapy is reduced (IARC, 3 C 2007). -
The Treatment of Monophasic Cycles with the Retroprogesterone Ro 4-8347
The treatment of monophasic cycles with the retroprogesterone Ro 4-8347 Autor(en): Taubert, H.-D. / Jürgensen, O. Objekttyp: Article Zeitschrift: Bulletin der Schweizerischen Akademie der Medizinischen Wissenschaften = Bulletin de l'Académie Suisse des Sciences Medicales = Bollettino dell' Accademia Svizzera delle Scienze Mediche Band (Jahr): 25 (1969) PDF erstellt am: 25.09.2021 Persistenter Link: http://doi.org/10.5169/seals-307794 Nutzungsbedingungen Die ETH-Bibliothek ist Anbieterin der digitalisierten Zeitschriften. Sie besitzt keine Urheberrechte an den Inhalten der Zeitschriften. Die Rechte liegen in der Regel bei den Herausgebern. Die auf der Plattform e-periodica veröffentlichten Dokumente stehen für nicht-kommerzielle Zwecke in Lehre und Forschung sowie für die private Nutzung frei zur Verfügung. Einzelne Dateien oder Ausdrucke aus diesem Angebot können zusammen mit diesen Nutzungsbedingungen und den korrekten Herkunftsbezeichnungen weitergegeben werden. Das Veröffentlichen von Bildern in Print- und Online-Publikationen ist nur mit vorheriger Genehmigung der Rechteinhaber erlaubt. Die systematische Speicherung von Teilen des elektronischen Angebots auf anderen Servern bedarf ebenfalls des schriftlichen Einverständnisses der Rechteinhaber. Haftungsausschluss Alle Angaben erfolgen ohne Gewähr für Vollständigkeit oder Richtigkeit. Es wird keine Haftung übernommen für Schäden durch die Verwendung von Informationen aus diesem Online-Angebot oder durch das Fehlen von Informationen. Dies gilt auch für Inhalte Dritter, die über dieses Angebot zugänglich sind. Ein Dienst der ETH-Bibliothek ETH Zürich, Rämistrasse 101, 8092 Zürich, Schweiz, www.library.ethz.ch http://www.e-periodica.ch Abteilung fiir gynäkologische Endokrinologie (Leiter: Prof. TT.-T). Taubert) der Universitälsfraueiiklinik, Frankfurt/Main (Direktor; Prof. 0. Käser) The Treatment of Monophasic Cycles with the Retroprogesterone Ro 4-8347 H.-l). -
BMJ Open Is Committed to Open Peer Review. As Part of This Commitment We Make the Peer Review History of Every Article We Publish Publicly Available
BMJ Open is committed to open peer review. As part of this commitment we make the peer review history of every article we publish publicly available. When an article is published we post the peer reviewers’ comments and the authors’ responses online. We also post the versions of the paper that were used during peer review. These are the versions that the peer review comments apply to. The versions of the paper that follow are the versions that were submitted during the peer review process. They are not the versions of record or the final published versions. They should not be cited or distributed as the published version of this manuscript. BMJ Open is an open access journal and the full, final, typeset and author-corrected version of record of the manuscript is available on our site with no access controls, subscription charges or pay-per-view fees (http://bmjopen.bmj.com). If you have any questions on BMJ Open’s open peer review process please email [email protected] BMJ Open Pediatric drug utilization in the Western Pacific region: Australia, Japan, South Korea, Hong Kong and Taiwan Journal: BMJ Open ManuscriptFor ID peerbmjopen-2019-032426 review only Article Type: Research Date Submitted by the 27-Jun-2019 Author: Complete List of Authors: Brauer, Ruth; University College London, Research Department of Practice and Policy, School of Pharmacy Wong, Ian; University College London, Research Department of Practice and Policy, School of Pharmacy; University of Hong Kong, Centre for Safe Medication Practice and Research, Department -
Literature Review of Organic Chemicals of Emerging Environmental Concern in Use in Auckland December TR 2008/028
Literature Review of Organic Chemicals of Emerging Environmental Concern in Use in Auckland December TR 2008/028 Auckland Regional Council Technical Report No.028 December 2008 ISSN 1179-0504 (Print) ISSN 1179-0512 (Online) ISBN 978-1-877483-69-1 Technical Report, first edition Reviewed by: Approved for ARC publication by: Name: Judy-Ann Ansen Name: Paul Metcalf Position: Team Leader Position: Group Manager Stormwater Action Team Environmental Programmes Organisation: Auckland Regional Council Organisation: Auckland Regional Council Date: 1 November 2008 Date: 1 October 2009 Recommended Citation: AHERNS, M., 2008. Review of Organic Chemicals of Potential Environmental Concern in Use in Auckland. Prepared by NIWA for Auckland Regional Council. Auckland Regional Council Technical Report 2008/028. © 2008 Auckland Regional Council This publication is provided strictly subject to Auckland Regional Council's (ARC) copyright and other intellectual property rights (if any) in the publication. Users of the publication may only access, reproduce and use the publication, in a secure digital medium or hard copy, for responsible genuine non-commercial purposes relating to personal, public service or educational purposes, provided that the publication is only ever accurately reproduced and proper attribution of its source, publication date and authorship is attached to any use or reproduction. This publication must not be used in any way for any commercial purpose without the prior written consent of ARC. ARC does not give any warranty whatsoever, including without limitation, as to the availability, accuracy, completeness, currency or reliability of the information or data (including third party data) made available via the publication and expressly disclaim (to the maximum extent permitted in law) all liability for any damage or loss resulting from your use of, or reliance on the publication or the information and data provided via the publication. -
Progestagens for Human Use. Exposure and Hazard Assessment for the Aquatic Environment J.P
Progestagens for human use. Exposure and hazard assessment for the aquatic environment J.P. Besse, J. Garric To cite this version: J.P. Besse, J. Garric. Progestagens for human use. Exposure and hazard assessment for the aquatic environment. Environmental Pollution, Elsevier, 2009, 157 (12), p. 3485 - p. 3494. 10.1016/j.envpol.2009.06.012. hal-00455636 HAL Id: hal-00455636 https://hal.archives-ouvertes.fr/hal-00455636 Submitted on 10 Feb 2010 HAL is a multi-disciplinary open access L’archive ouverte pluridisciplinaire HAL, est archive for the deposit and dissemination of sci- destinée au dépôt et à la diffusion de documents entific research documents, whether they are pub- scientifiques de niveau recherche, publiés ou non, lished or not. The documents may come from émanant des établissements d’enseignement et de teaching and research institutions in France or recherche français ou étrangers, des laboratoires abroad, or from public or private research centers. publics ou privés. Environmental Pollution, vol. 157, n° 12, doi : 10.1016/j.envpol.2009.06.012 1 Progestagens for human use, exposure and hazard assessment for 2 the aquatic environment 3 4 5 6 Reviewed version of manuscript ENVPOL-D-09-00080R1. 7 The abstract of this paper was evaluated and approved by Dr Wiegand. 8 9 10 Authors 11 12 Jean-Philippe BESSE a* 13 Jeanne GARRIC a** 14 15 a Unité Biologie des écosystèmes aquatiques. Laboratoire d’écotoxicologie, 16 Cemagref, 3bis quai Chauveau CP 220 69336 Lyon cedex 09, France 17 Tel.: +33 472208902 18 19 * first author 20 ** corresponding author. E-mail address: [email protected] 21 22 23 Capsule: 24 Gestagens exposure and hazard assessment for the aquatic environment. -
Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0 -
PRODUCT INFORMATION Dydrogesterone Item No
PRODUCT INFORMATION Dydrogesterone Item No. 20514 CAS Registry No.: 152-62-5 Formal Name: (9β,10α)-pregna-4,6-diene-3,20-dione O Synonym: NSC 92336 MF: C21H28O2 FW: 312.5 Purity: ≥98% H UV/Vis.: λmax: 287 nm H H Supplied as: A crystalline solid Storage: -20°C O Stability: ≥2 years Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures Dydrogesterone is supplied as a crystalline solid. A stock solution may be made by dissolving the dydrogesterone in the solvent of choice. Dydrogesterone is soluble in organic solvents such as ethanol, acetonitrile, and methanol, which should be purged with an inert gas. The solubility of dydrogesterone in these solvents is approximately 1 mg/ml. Description Dydrogesterone is a synthetic progestogen that has no estrogenic, androgenic, glucocorticoid, or anabolic effects, although it is an agonist of progesterone receptors (EC50 = 12.3 nM) and an antagonist of 1,2 androgen, mineralocorticoid, and glucocorticoid receptors (IC50s = 28.6, 82.7, and 363 nM, respectively). Dydrogesterone protects against sound stress-induced abortion in mice when administered at a dose of 1.25 mg per animal prior to the stressor on day five of pregnancy.3 Formulations containing dydrogesterone have been used in hormone replacement therapy, in the treatment of menstrual disorders, and to prevent miscarriage. References 1. Coelingh Bennink, H.J. and Boerrigter, P.J. Use of dydrogesterone as a progestogen for oral contraception. Steroids 68(10-13), 927-929 (2003). 2. Rižner, T.L., Brožič, P., Doucette, C., et al. Selectivity and potency of the retroprogesterone dydrogesterone in vitro. -
(12) Patent Application Publication (10) Pub. No.: US 2007/0082876 A1 Messinger Et Al
US 20070082876A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2007/0082876 A1 Messinger et al. (43) Pub. Date: Apr. 12, 2007 (54) NOVEL C18 MODIFIED RETROSTEROIDS Publication Classification AS PROGESTERONE RECEPTOR MODULATOR COMPOUNDS (51) Int. Cl. A6II 3/58 (2006.01) (75) Inventors: Joseph Messinger, Sehnde (DE); A 6LX 3/57 (2006.01) Heinrich-Hubert Thole, Hannover C07 43/00 (2006.01) (DE); Bettina Husen, Hannover (DE); C07J 5/00 (2006.01) Christiane Boecker, Hannover (DE); (52) U.S. Cl. ......................... 514/176; 514/177: 540/107; Maria Hinaje, Nancy (FR); Monika 552/574 Buchholz, Langenfeld (DE); Christoph Mark, Worms (DE); Vibhuti (57) ABSTRACT Klingler-Dabral, Griesheim (DE) Retrosteroidal compounds of formula I which act as proges Correspondence Address: terone receptor modulators, a method for their production, CROWELL & MORING LLP and pharmaceutical preparations containing these com INTELLECTUAL PROPERTY GROUP pounds. These compounds are preferably used for the treat P.O. BOX 143OO ment of benign gynecological disorders such as endometrio WASHINGTON, DC 20044-4300 (US) sis and uterine fibroids, as well as for female birth control (73) Assignee: Solvay Pharmaceuticals GmbH, Han and for hormone replacement therapy (HRT). nover (DE) (21) Appl. No.: 11/529,628 (22) Filed: Sep. 29, 2006 Related U.S. Application Data (60) Provisional application No. 60/722,689, filed on Sep. 30, 2005. (30) Foreign Application Priority Data Jul. 28, 2006 (EP)........................................ O6118O34.5 Antiluteolytic activity in guinea pigs 10 11 12 13 14 15 16 17 18 day post ovulationem - O - dydrogesterone - example 2 - Ar mifepristone -v- example 5 -- example 13 Patent Application Publication Apr.