Estradiol butyrylacetate/testosterone ketolaurate/reserpine Combination drug
Pharmaceutical compound
Estradiol butyrylacetate/testosterone ketolaurate/reserpine (EBA/TKL/R ), sold under the brand name Klimanosid R-Depot , is an injectable combination medication of estradiol butyrylacetate (EBA), an estrogen , testosterone ketolaurate (TKL; testosterone caprinoylacetate), an androgen /anabolic steroid , and reserpine , an antipsychotic , which was previously used in menopausal hormone therapy for women, particularly in those with pronounced neurovegetative symptoms .[ 1] [ 2] [ 3] [ 4] [ 5] [ 6] It contains 2 mg EBA, 50 mg TKL, and 0.4 mg reserpine in oil solution in each 1 mL ampoule and is administered by intramuscular injection at regular intervals.[ 1] [ 4] The medication was marketed in 1957.[ 1]
EBA/TKL reportedly has a duration of about 21 days.[ 7]
Oral tablet products with the same brand names of Klimanosid and Klimanosid R, containing methylestradiol and methyltestosterone , with and without reserpine, were marketed around the same time as Klimanosid-R Depot, and should not be confused with the injectable formulation.[ 8] [ 2] [ 9]
See also
References
^ a b c "Neue Spezialitäten". Klinische Wochenschrift . 35 (13): 692. 1957. doi :10.1007/BF01481278 . ISSN 0023-2173 . S2CID 40387087 . Klimanosid "R"-Depot enthält je Ampulle: Testosteron als Caprinoytacetat 50,0 mg, Oestradiol als Butyrylacetat 2,0 mg und Reserpin "Boehringer" 0,4 mg (Klimakterische und präklimaterische Ausfallserscheinungen einsehließlich ausgeprägter emotioneller Störungen). Hersteller: C.F. Boehringer & Soehne GmbH, Mannheim.
^ a b Schirren C (14 March 2013). "Die Sexualhormone" . In Kimmig J (ed.). Therapie der Haut- und Geschlechtskrankheiten . Springer-Verlag. pp. 508–. ISBN 978-3-642-94850-3 .
^ Kaiser R (1962). Die hormonale Behandlung von Zyklusstörungen: ein Leitfaden für die Praxis . Thieme. p. 86.
^ a b Gehe & Co (1969). Gehes Codex der pharmazeutischen u. Organotherapeutischen Spezialpräparate(einschl. Der Sera, Impfstoffe, Kosmetica, Reinigungs-, Desinfektions- u. Schädlingsbekämpfungsmittel) umfassend deutsche und zahlreiche ausländische Erzeugnisse . Schwarzeck-Verlag G.m.b.H. KlimanosidDepot-Ampullen (f üher Klimanosid-„R"-Depot-Ampullen) Z : 1 Ampulle zu 1 ml zur i.m. Injektion enthält: 50 mg Testosteron (in Form des Caprinoylacetatsä sowie 2 mg Oestradiol (in Form des Butyrylacetats). I: Klimakterische und [...]
^ Wenner R, Hauser GA (1959). "[Neurovegetative studies and results of therapy in climacteric women]". Archiv für Gynäkologie . 193 (1): 58– 69. doi :10.1007/BF00837146 . PMID 13843987 . S2CID 42511052 .
^ Knörr K, Lauritzen C, Beller FK (1972). "Empfängnisregelung — Empfängnisverhütung". Lehrbuch der Gynäkologie . Springer. pp. 227– 257. doi :10.1007/978-3-662-00942-0_20 . ISBN 978-3-540-05593-8 .
^ Ufer J (1 January 1978). Hormontherapie in der Frauenheilkunde: Grundlagen und Praxis [Hormone Therapy in Gynecology: Principles and Practice ] (in German) (5th ed.). de Gruyter. p. 276. ISBN 978-3110066647 . OCLC 924728827 .
^ Hager HH, Kern W, List PH, Roth HJ (29 July 2013). Hagers Handbuch der Pharmazeutischen Praxis: Für Apotheker, Arzneimittelhersteller, Ärzte und Medizinalbeamte: Wirkstoffgruppen II Chemikalien und Drogen (A-AL) . Springer-Verlag. pp. 157, 160, 185. ISBN 978-3-662-25655-8 .
^ Kahr H, Müller HA (1956). "Behandlung der Menstruationsstörungen". Konservative Therapie der Frauenkrankheiten . Springer. pp. 1– 85. doi :10.1007/978-3-7091-5694-0_1 . ISBN 978-3-7091-5696-4 . [Not to be confused with the oral tablet version:] Klimanosid: Tabl. 0,005 mg Methyloestradiol + 3,0 mg Methyltestosteron.
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
Androgens (incl. AAS Tooltip anabolic–androgenic steroid )
Antiandrogens
AR Tooltip Androgen receptor antagonists Steroidogenesis inhibitors
Antigonadotropins
D2 receptor antagonists (prolactin releasers ) (e.g., domperidone , metoclopramide , risperidone , haloperidol , chlorpromazine , sulpiride )
Estrogens (e.g., bifluranol , diethylstilbestrol , estradiol , estradiol esters , ethinylestradiol , ethinylestradiol sulfonate , paroxypropione )
GnRH agonists (e.g., leuprorelin )
GnRH antagonists (e.g., cetrorelix )
Progestogens (incl., chlormadinone acetate , cyproterone acetate , hydroxyprogesterone caproate , gestonorone 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
AR Tooltip Androgen receptor
Agonists SARMs Tooltip Selective androgen receptor modulator Antagonists
GPRC6A