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Home , Estrapronicate, Estriol succinate

2274 Sex Hormones and their Modulators

Oestrogens are metabolised in the liver. A variety of vat; Estring; Estrofem N; Femoston mono; Oestrogel; menet; Climodien; Cyclocurt; Estalis Sequit; Estalist; Estan­ sulfate and glucuronide conjugates are formed, and these Progynova; Sandrenat; Systen; Vagifem; Zumenont; Thai.: CH­ dron Prolongatumt; Estracombt; Eviana; Fern 7 Sequit; are excreted in the urine and the bile. Those excreted in the mara; Divigel; Ediol; Estrofem; Oestrogel; Postmenop; Progy­ Femoston Continu; Femoston; Femphascyl Continu; Femphas­ bile undergo enterohepatic recycling or are excreted in the nont; Progynova; Vagifemt; Turk.: Aerodiol; Akrofolline; CH­ cyl; loa; Kliogest; Lafarnme; Naemist; Novofem; Qlaira; faeces. mara; Estraderm; Estramon; Estrava; Estrofem; Fern 7; Femijel; Trisequens; Zoely; Norw.: Activelle; Climodient; Cliovelle; UK: References to the pharmacokinetics of estradioFA and Vagifem; Bedol; CHmaval; Elleste-Solo; Estraderm; Estra­ Estalis Sekvenst; Estalis; Eviana; Indivina; Kliogestt; Novofem; dot; Estring: Evorel; Fematrixt; FemSeven; Oestrogel; Qlaira; Sequidot; Trisekvens; Zoely; NZ: Clianet; Fernoston; other oestrogens. 5•6 Progynova; Sandrena; Vagifem; Zumenon; Ukr. : Divigel Kliogest; Kliovance; Nuvelle; Trisequens; Philipp.: Angeliq; Cli­ I. Kuhnz W, et a!. Pharmacokinetics of free and total , in (.UnsnrenL); Estramon (3CTpaMoH); Oestrogel (3crpo}KeJIL); men 28; Femostont; Kliogest; Pol. : Activelle; Alpicort E; Angel­ young women following single intravenous and oral administration of 17 -estradioL Armeimittelfo rschung 1993; 43: 966-73. Progynova (ITporHHOBa); USA: Alora; Climara; Delestrogen; iq; Climen; Cliovelle; Cyclo-Progynova; Divina; Diviseq; Estalis f3 depGynogen; Depogen; Divigel; Elestrin; Esclimt; Estrace; Sequit; Estalis; Estracomb; Fern 7 Combi; Femoston Conti; 2. Schubert W, et al. Pharmacokinetic evaluation of oral 17 J3 -oestradiol and two different fat soluble analogues in ovariectomized women. Eur J Estraderm; Estrasorb; Estring; Estrogel; Evamist; FemPatch; Femoston Mini; Femoston; Gynodian Depott; Indivina; Klima­ Clin Pharmacal 1993; 44: 563-8. Femring; Femtrace; Gynodiol; Menostar; Minivelle; Vagifem; norm; Kliogest; Novofem; Qlaira; Systen Conti; Systen Sequi; 3. Baker VL Alternatives to oral replacement: transdermal Valergen; Vivelle; Venez.: Aerodiol; Climadenn; Estradot; Estro­ Trisequens; Port.: Activelle; Allurene; Angeliq; Avadene; Cli­ patches, percutaneous gels, vaginal creams and rings, implants, other gel; FemSeven; Progynova. men; Climodien; Dilena; Estalis Sequi; Estalis; Estracombt; methods of delivery. Obstet Gynecol Clin North Am 1994; 21: 271-9. l/5; 4. Price TM, et al. Single-dose pharmacokinetics of sublingual versus oral Femoston Femoston; Femsete Combi; Femsete Eva; Klio­ 89: Multi-ingredient Preparations. Arg. : Activelle; Angeliq; Atrimon; gest; Lafamme; Naemis; Novofem; Nuvelle; Progyluton; Qlaira; administration of micronized 17 S -estradiol. Obstet Gynecol 1997; 340-5. Ciclocur; Climene; Cristerona; Cydofem; Disequens; Dos Dias Trisequens; Rus.: Angeliq (AH)f(eJIMK); Climen (KrrHMeH); Climo­ 5. Stumpf PG. Pharmacokinetics of estrogen. Obstet Gynecol 1990; 75 N; Eos; Equifem; Estalis Sequit; Estalist; Estracombt; Estragest; dien (K.JrnMO.UlieH); Cyclo-Progynova (I.Vumo-nporHHOBa); Divina (suppl}: 9S-14S. Evorel Conti; Evorel Sequi; Farludiol Ciclo; Farludiol; Fempack; ()l;nBnHa); Diviseq ()l;HBMCeK); Divitren (,UnBnTPeH)f; Femoston 6. O'Connell MB. Pharmacokinetk and pharmacologic variation between Gadofem; Gynodian Depot; Hosterona; Kliogest; Lubriderm; ('i); Femoston (:Jf,.il[);Lunella (fl�); Evorel Sequi; Femapakt; Femoston Conti; Femoston; FemSe­ max; Estrofem; Linoladiol N; Neofollin; Octodiolt; Oestrogel; Novofem; Trisequens (t!\'�W);Yi Wei Xian (�MHIU);Cz.: Acti­ ven Conti; FemSeven Sequi; Hormonin; Indivina; Kliofem; Riselle; Systen; Vagifem; Denm.: Climarat; Divigel; Estrevat; velle; Alpicon F; Angeliq; Climen; Divina; Diviseq; Estalis Kliovance; Novofem; Nuvelle Continuous; Nuvellet; Qlaira; Estring; Estrofem; Estrogel; Evorel; Femanest; Progynon; Systen Sequit; Estalist; Femoston Conti; Femoston Mini; Femoston; Tridestra; Trisequens; Zoely; Ukr.: Angeliq (AH)f(eJIHK); Climen Conti; Vagifem; Vivelle Dot; Fin.: Climara; Dermestrilt; Divigel; Folivirin; Gynodian Depot; Gynovel; Indivina; Kliane; Klimo­ (I0mMeH); Divina (,UHBHHa)t; Femoston (

All cross-references refer to entries in Volume A 2275

Ph. Eur. 8: (Estriol). A white or almost white crystalline Estrone (BAN. rtNNJ powder. Practically insoluble in water; sparingly soluble in Adverse Effects and Precautions - - alcohol. E�tro�:_- tst��ha; ",ESt(oni; _ Estrr;m t..trn; -Foil'cuHna;- FoJHcvJar­ As for oestrogens in general (see Estradiol, p. 2273.2). See Hormone; Foll culiD; Ketohydroxyoestrin: also under Hormone Replacement Therapy, p. 2246.3. USP 36: (Estriol). A white or practically white, odourless, i crystalline powder. Insoluble in water; sparingly soluble in 3crpoH. alcohol; soluble in acetone, in chloroform, in dioxan, in $-Hydroxye>tra'1,3,5(10)-trien-1 7-one, ether, and in vegetable oils. Store in airtight containers. C$H2202�270.4 See under Hormone Replacement Therapy, p. 2251.1. CAS -. 53 · liP Estriol Sodium Succinate (BAN, rtNNMI !\TC�. GOJ0\01. P epa a ons r r ti ...... ATC \fet +- OGO,l0\07, QGGEC(04. .. . E?triol, Succinate Sodique d'; . Estriol, sucdr\ato sodiC() de; ProprietaryPreparations (details are given in Volume B) . Uil/11 � 2019HA706A. Natrii Succinas; O<:strio!,Sodiuf\) Sucdnate;.Succinato Estrioli Austral.: Genoral; Ogent; s6dico ..de es riol; Pharmacopoeias. In US. Single-ingredient Preparations. 3CTp!4o/la.Harpvm CyKUI&I�T. · t . Canad. : Ogen; Indon.: Ogent; S.Afr. : Ortho-Est; UK: Oisodium.. . 3-hydroxyestra-1 ,3,5(10Hrie""-16.q.1 7f3-diyl USP 36: (Estrone). Odourless, small white crystals or white · Harmogent; USA: Ogen. uccinate. to creamy-white crystalline powder. Practically insoluble in water; soluble 1 in 250 of alcohol and 1 in 110 of chloroform PharmacopoeialPreparations C2r,H)0Na20,=S325 BP 2014: at 15 degrees; soluble 1 in 50 of boiling alcohol, I in 33 of Tablets; C4S- 113.22"4. USP 36: Estropipate Tablets; Estropipate Vaginal Cream. ATC �. Gb3CA04. boiling acetone, 1 in 145 of boiling benzene, and 1 in 80 of I Vet ""':' OGOJ0\04. boiling chloroform; soluble in 50 of acetone at 50 degrees; ATC soluble in dioxan and in vegetable oils; slightly soluble in U/VI/ .�.64ll00CU6.5. solutions of fixed alkali hydroxides. Store in airtight containers at a temperature of 25 degrees, excursions !BAN, rtNNI permitted between 15 degrees and 30 degrees. Protect from light. Estriol. Su.:cinat<:: d'; Estnol,. succir;ato de; EstrioH SucCir\i!S; Estrio!isuksinaatti; Estriolsuccinat; Oestriol S.uccinate( S.ucci­ es\(lol; 3tTP>' na · Profile hato de I) CyKL(HHar. . 3-Hydroxyestra71;3,5(1 O) ·t�iene�l.6'a,17p-diyl Estrone is a naturally occurring oestrogen with actions and SUCciflate). uses similar to those described for estradiol (see p. 2271.1). t,c!-tJz0�; ;188;5 For menopausal HRT (see p. 2244. 1) estrone has been CAS .�. 514-68'.1' given orally at a dose of 1.4 to 2.8 mg daily in a cyclical or continuous regimen, as a combination product with ATe- G()3(:AQ4 ATC Vet -' 0GiJ.KA04. estradiol and estriol (see p. 2274.3). Estrone bas also been UN!/ +-. AS!JK2DY03. given by intramuscular injection in oily solutions and aqueous suspensions. When used specifically for meno­ pausal , estrone has been given vaginally. NOTE. Compounded preparations of may be Profile If used in women with a , estrone by any route should represented by the following names: Co-cyprindiol (BAN)-ethinylestradiol 35 parts and Estriol is a naturally occurring oestrogen with actions and be given with a progestogen. • 2000 parts (w/w). uses similar to those described for estradiol (p. 2271.1). It is used for menopausal HRT (p. 2244. 1). When P..r�P.?.r?_ti?.n.� Pharmacopoeias. In Chin., Bur. (see p. vii), Int., Jpn, and US. oestrogens are given to women with a uterus, a progestogen Ph. Eur. 8: (Ethinylestradiol). A white to slightly yellowish­ (details are given in Volume B) is required, particularly if used long term. Oral doses of Proprietary Preparations white, crystalline powder. It shows polymorphism. estriol 4 to 8 mg daily may be used initially, followed by a Single-ingredient Preparations. Canad. : Estragyn; USA: Practically insoluble in water; freely soluble in alcohol; gradual reduction to the lowest effective dose. Estriol has trone. dissolves in dilute alkaline solutions. Protect from light. also been given with other natural oestrogens such as Hong Kong: Hormonint; Mon.: USP 36: (Ethinyl Estradiol). A white to creamy white, estradiol and estrone (see below); usual doses of estriol have Multi-ingredient Preparations. Synergon; Port.: Gretalvite; Spain: Cicatral; Grietalgen; Thai.: odour!ess, crystalline powder. Insoluble in water; soluble in ranged from about 0.25 to 2 mg daily. Estriol may be used Metharmon-Ft; Turk.: Synergon; UK: Hormonin. alcohol, in chloroform, in ether, in vegetable oils, and in intravaginally for the short-term treatment of menopausal solutions of fixed alkali hydroxides. Store in nonmetallic atrophic vaginitis and kraurosis vulvae. A dose of Pharmacopoeial Preparations airtight containers. Protect from light. 500micrograms may be given as a 0.01% or 0.1% cream USP 36: Estrone Injectable Suspension. or as a pessary; initial treatment may be given once daily, then reduced to twice each week. Uses and Administration Estriol has also been given orally for infertility Estropipate !BANI Ethinylestradiol is a synthetic oestrogen with actions similar (p. 2253.1) caused by poor cervical penetration, in a dose to those of estradiol (see p. 2271.2). of 1 to 2 mg daily on days 6 to 15 of the menstrual cycle. The Estropipato; Piperazl�e • ; Piperazine Oestrone It is frequently used as the oestrogenic component of dose may be increased if necessary each month, until an Sulphat;o: 3

The symbol t denotes a preparation no longer actively marketed