Combination drug
Estradiol benzoate/hydroxyprogesterone caproate (EB/OHPC ), sold under the brand name Primosiston among others, is a combined estrogen and progestogen medication which is used to treat gynecological disorders and habitual abortion .[1] [2] [3] [4] [5] It contains estradiol benzoate (EB), an estrogen, and hydroxyprogesterone caproate (OHPC), a progestin .[1] [2] [3] [4] [5] The medication is given by injection into muscle .[1] [2] [3] [4] [5]
Medical uses [ edit ] EB/OHPC is used in the treatment of gynecological disorders such as menstrual disorders (e.g., amenorrhea , dysfunctional uterine bleeding ) and premenstrual syndrome , habitual abortion (threatened miscarriage), and for other indications.[1] [2] [3] [4]
Available forms [ edit ] EB/OHPC is available in the form of ampoules of oil solutions containing 10 mg estradiol benzoate (EB) and 125 to 250 mg hydroxyprogesterone caproate (OHPC).[1] [2] [3] [4] [5]
History [ edit ] EB/OHPC was first introduced for medical use in 1955.[6]
Society and culture [ edit ] Brand names [ edit ] EB/OHPC has been marketed under brand names including Dos Dias N, Lutes, Ostrolut, Primosiston (or Primosiston Inj. / Injection), Primosiston Fuerte, and Syngynon.[7] [8] [9]
Availability [ edit ] EB/OHPC has been mostly discontinued and hence is mostly no longer available.[7] [8] [9] It remains marketed under the brand names Primosiston in Ecuador and Peru , Dos Dias N in Argentina , and Lutes in Japan .[7] [8] [9] It was previously marketed under the brand names Ostrolut in Austria ; Primosiston (or Primosiston Inj. / Injection) (Schering )[1] [2] [4] in Argentina, Germany , Mexico , Switzerland , and Venezuela ; Primosiston Fuerte in Spain; and Syngynon in Germany, but these formulations have all been discontinued and hence are no longer available in these countries.[7] [8] [9]
See also [ edit ] References [ edit ] ^ a b c d e f Leidenberger FA (17 April 2013). Klinische Endokrinologie für Frauenärzte . Springer-Verlag. pp. 533–. ISBN 978-3-662-08110-5 . ^ a b c d e f Knörr K, Beller FK, Lauritzen C (17 April 2013). Lehrbuch der Gynäkologie . Springer-Verlag. pp. 255–. ISBN 978-3-662-00942-0 . ^ a b c d e Kahr H (8 March 2013). Konservative Therapie der Frauenkrankheiten: Anzeigen, Grenzen und Methoden Einschliesslich der Rezeptur . Springer-Verlag. pp. 22–. ISBN 978-3-7091-5694-0 . ^ a b c d e f Kern W, Auterhoff H, Neuwald F, Schmid W (9 March 2013). Hagers Handbuch der Pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Drogisten, Ärzte und Medizinalbeamte . Springer-Verlag. pp. 1163–. ISBN 978-3-642-49759-9 . ^ a b c d Die Gestagene . Springer-Verlag. 27 November 2013. pp. 1045–. ISBN 978-3-642-99941-3 . ^ Kaiser R (2008). "Gestagen-Östrogen-Kombinationen in der Gynäkologie. Zur Geschichte, Dosierung und Anwendung eines Hormonprinzips" [Progestogen-Estrogen Combinations in Gynecology. History, Dosage, and Use of a Hormone Principle]. Geburtshilfe und Frauenheilkunde . 53 (7): 503–513. doi :10.1055/s-2007-1022924 . ISSN 0016-5751 . PMID 8370495 . Zur kombinierten Anwendung von Gestagen en und Östrogenen stand en zunächst ölgelöstes Östradiolbenzoat und Progesteron zur Verfügung. Das erste derartige Mischpräparat kam in Deutschland 1950 auf den Mark t. Dem Wunsch nach verlän gerter Wirkungsdauer entsprach en dann Kristallmischsuspension en verschiedener Korngröße aus Östradiolmonobenzoat + Progesteron, deren Anwendung sich auf klinische Untersuchungen besch ränkte (83). Ölgelöste Depotpräparate mit Östradiolbenzoat oder -valerat + 17-hydroxyprogesteroncaproat wurden ab 1955 in die Therapie eingeführt (45.46). ^ a b c d "Hydroxyprogesterone" . Drugs.com . Retrieved May 27, 2019 . ^ a b c d Sweetman SC, ed. (2009). "Sex hormones and their modulators". Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. p. 2082. ISBN 978-0-85369-840-1 . ^ a b c d "Micromedex Products: Please Login" . www.micromedexsolutions.com . Retrieved May 27, 2019 .
Estrogens
ER Tooltip Estrogen receptor agonists Steroidal: Alfatradiol Certain androgens /anabolic steroids (e.g., testosterone , testosterone esters , methyltestosterone , metandienone , nandrolone esters ) (via estrogenic metabolites) Certain progestins (e.g., norethisterone , noretynodrel , etynodiol diacetate , tibolone ) Clomestrone Cloxestradiol acetate Conjugated estriol Conjugated estrogens Epiestriol Epimestrol Esterified estrogens Estetrol † Estradiol Estradiol esters (e.g., estradiol acetate , estradiol benzoate , estradiol cypionate , estradiol enanthate , estradiol undecylate , estradiol valerate , polyestradiol phosphate , estradiol ester mixtures (Climacteron )) Estramustine phosphate Estriol Estriol esters (e.g., estriol succinate , polyestriol phosphate ) Estrogenic substances Estrone Estrone esters Ethinylestradiol # Hydroxyestrone diacetate Mestranol Methylestradiol Moxestrol Nilestriol Prasterone (dehydroepiandrosterone; DHEA) Promestriene Quinestradol Quinestrol Progonadotropins
Antiestrogens
ER Tooltip Estrogen receptor antagonists (incl. SERMs Tooltip selective estrogen receptor modulators /SERDs Tooltip selective estrogen receptor downregulators )Aromatase inhibitors Antigonadotropins Androgens /anabolic steroids (e.g., testosterone , testosterone esters , nandrolone esters , oxandrolone , fluoxymesterone ) D2 receptor antagonists (prolactin releasers) (e.g., domperidone , metoclopramide , risperidone , haloperidol , chlorpromazine , sulpiride ) GnRH agonists (e.g., leuprorelin , goserelin ) GnRH antagonists (e.g., cetrorelix , elagolix ) Progestogens (e.g., chlormadinone acetate , cyproterone acetate , gestonorone caproate , hydroxyprogesterone caproate , medroxyprogesterone acetate , megestrol acetate ) Others
ER Tooltip Estrogen receptor
Agonists Steroidal: 2-Hydroxyestradiol 2-Hydroxyestrone 3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol 3α-Androstanediol 3α,5α-Dihydrolevonorgestrel 3β,5α-Dihydrolevonorgestrel 3α-Hydroxytibolone 3β-Hydroxytibolone 3β-Androstanediol 4-Androstenediol 4-Androstenedione 4-Fluoroestradiol 4-Hydroxyestradiol 4-Hydroxyestrone 4-Methoxyestradiol 4-Methoxyestrone 5-Androstenediol 7-Oxo-DHEA 7α-Hydroxy-DHEA 7α-Methylestradiol 7β-Hydroxyepiandrosterone 8,9-Dehydroestradiol 8,9-Dehydroestrone 8β-VE2 10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED) 11β-Chloromethylestradiol 11β-Methoxyestradiol 15α-Hydroxyestradiol 16-Ketoestradiol 16-Ketoestrone 16α-Fluoroestradiol 16α-Hydroxy-DHEA 16α-Hydroxyestrone 16α-Iodoestradiol 16α-LE2 16β-Hydroxyestrone 16β,17α-Epiestriol (16β-hydroxy-17α-estradiol) 17α-Estradiol (alfatradiol ) 17α-Dihydroequilenin 17α-Dihydroequilin 17α-Epiestriol (16α-hydroxy-17α-estradiol) 17α-Ethynyl-3α-androstanediol 17α-Ethynyl-3β-androstanediol 17β-Dihydroequilenin 17β-Dihydroequilin 17β-Methyl-17α-dihydroequilenin Abiraterone Abiraterone acetate Alestramustine Almestrone Anabolic steroids (e.g., testosterone and esters , methyltestosterone , metandienone (methandrostenolone) , nandrolone and esters , many others; via estrogenic metabolites) Atrimustine Bolandiol Bolandiol dipropionate Butolame Clomestrone Cloxestradiol Conjugated estriol Conjugated estrogens Cyclodiol Cyclotriol DHEA DHEA-S ent -Estradiol Epiestriol (16β-epiestriol, 16β-hydroxy-17β-estradiol) Epimestrol Equilenin Equilin ERA-63 (ORG-37663) Esterified estrogens Estetrol Estradiol Estramustine Estramustine phosphate Estrapronicate Estrazinol Estriol Estrofurate Estrogenic substances Estromustine Estrone Etamestrol (eptamestrol) Ethinylandrostenediol Ethinylestradiol Ethinylestriol Ethylestradiol Etynodiol Etynodiol diacetate Hexolame Hippulin Hydroxyestrone diacetate Lynestrenol Lynestrenol phenylpropionate Mestranol Methylestradiol Moxestrol Mytatrienediol Nilestriol Norethisterone Noretynodrel Orestrate Pentolame Prodiame Prolame Promestriene RU-16117 Quinestradol Quinestrol Tibolone Xenoestrogens: Anise -related (e.g., anethole , anol , dianethole , dianol , photoanethole ) Chalconoids (e.g., isoliquiritigenin , phloretin , phlorizin (phloridzin) , wedelolactone ) Coumestans (e.g., coumestrol , psoralidin ) Flavonoids (incl. 7,8-DHF , 8-prenylnaringenin , apigenin , baicalein , baicalin , biochanin A , calycosin , catechin , daidzein , daidzin , ECG , EGCG , epicatechin , equol , formononetin , glabrene , glabridin , genistein , genistin , glycitein , kaempferol , liquiritigenin , mirificin , myricetin , naringenin , penduletin , pinocembrin , prunetin , puerarin , quercetin , tectoridin , tectorigenin ) Lavender oil Lignans (e.g., enterodiol , enterolactone , nyasol (cis -hinokiresinol) ) Metalloestrogens (e.g., cadmium ) Pesticides (e.g., alternariol , dieldrin , endosulfan , fenarimol , HPTE , methiocarb , methoxychlor , triclocarban , triclosan ) Phytosteroids (e.g., digitoxin (digitalis ), diosgenin , guggulsterone ) Phytosterols (e.g., β-sitosterol , campesterol , stigmasterol ) Resorcylic acid lactones (e.g., zearalanone , α-zearalenol , β-zearalenol , zearalenone , zeranol (α-zearalanol) , taleranol (teranol, β-zearalanol) ) Steroid -like (e.g., deoxymiroestrol , miroestrol ) Stilbenoids (e.g., resveratrol , rhaponticin ) Synthetic xenoestrogens (e.g., alkylphenols , bisphenols (e.g., BPA , BPF , BPS ), DDT , parabens , PBBs , PHBA , phthalates , PCBs ) Others (e.g., agnuside , rotundifuran ) Mixed (SERMs Tooltip Selective estrogen receptor modulators ) Antagonists Coregulator-binding modulators: ERX-11
GPER Tooltip G protein-coupled estrogen receptor
Agonists Antagonists Unknown
PR Tooltip Progesterone receptor
Agonists Testosterone derivatives: Progestins: 6,6-Difluoronorethisterone 6,6-Difluoronorethisterone acetate 17α-Allyl-19-nortestosterone Allylestrenol Altrenogest Chloroethynylnorgestrel Cingestol Danazol Desogestrel Dienogest Ethinylandrostenediol Ethisterone Ethynerone Etonogestrel Etynodiol Etynodiol diacetate Gestodene Gestrinone Levonorgestrel Levonorgestrel esters (e.g., levonorgestrel butanoate ) Lynestrenol Lynestrenol phenylpropionate Metynodiol Metynodiol diacetate Norelgestromin Norethisterone (norethindrone) Norethisterone esters (e.g., norethisterone acetate , norethisterone enanthate ) Noretynodrel Norgesterone Norgestimate Norgestrel Norgestrienone Norvinisterone Oxendolone Quingestanol Quingestanol acetate Tibolone Tigestol Tosagestin ; Anabolic–androgenic steroids: 11β-Methyl-19-nortestosterone 11β-Methyl-19-nortestosterone dodecylcarbonate 19-Nor-5-androstenediol 19-Nor-5-androstenedione 19-Nordehydroepiandrosterone Bolandiol Bolandiol dipropionate Bolandione Dimethisterone Dienedione Dienolone Dimethandrolone Dimethandrolone buciclate Dimethandrolone dodecylcarbonate Dimethandrolone undecanoate Dimethyldienolone Dimethyltrienolone Ethyldienolone Ethylestrenol (ethylnandrol) Methyldienolone Metribolone (R-1881) Methoxydienone (methoxygonadiene) Mibolerone Nandrolone Nandrolone esters (e.g., nandrolone decanoate , nandrolone phenylpropionate ) Norethandrolone Normethandrone (methylestrenolone, normethandrolone, normethisterone) RU-2309 Tetrahydrogestrinone Trenbolone (trienolone) Trenbolone esters (e.g., trenbolone acetate , trenbolone enanthate ) Trendione Trestolone Trestolone acetate Mixed (SPRMs Tooltip Selective progesterone receptor modulators ) Antagonists
mPR Tooltip Membrane progesterone receptor (PAQR Tooltip Progestin and adipoQ receptor )