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
↑ 1.0 1.1 1.2 "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.
↑ 2.0 2.1 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.
↑ 4.0 4.1 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 . {{cite book }}
: CS1 maint: unrecognized language (link )
↑ 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
Nonsteroidal: Benzestrol
Bifluranol
Chlorotrianisene
Dienestrol
Diethylstilbestrol (stilbestrol)
Diethylstilbestrol esters/ethers
Doisynoestrol (fenocycline)
Hexestrol
Methallenestril
Methestrol (promethestrol)
Paroxypropione
Quadrosilan
Triphenylbromoethylene
Triphenylchloroethylene
Zeranol
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 )
AR Tooltip Androgen receptor agonists
Testosterone derivatives: Androstenediol dipropionate
Boldenone undecylenate
Clostebol
Clostebol acetate
Clostebol caproate
Clostebol propionate
Cloxotestosterone acetate
Prasterone (dehydroepiandrosterone, DHEA)
Prasterone enanthate (DHEA enanthate)
Prasterone sulfate (DHEA sulfate)
Quinbolone
Testosterone #
Testosterone esters (e.g., testosterone cypionate , testosterone enanthate , testosterone propionate , testosterone undecanoate , testosterone ester mixtures (Deposterona , Omnadren , Sustanon , Testoviron Depot ))
Dihydrotestosterone derivatives: Androstanolone (stanolone, dihydrotestosterone, DHT)
Androstanolone esters
Bolazine capronate
Drostanolone propionate (dromostanolone propionate)
Epitiostanol
Mepitiostane
Mesterolone
Metenolone acetate (methenolone acetate)
Metenolone enanthate (methenolone enanthate)
Stenbolone acetate
19-Nortestosterone derivatives: Bolandiol dipropionate
Nandrolone esters (e.g., nandrolone decanoate , nandrolone phenylpropionate )
Norclostebol
Norclostebol acetate
Oxabolone cipionate (oxabolone cypionate)
Trenbolone acetate
Trenbolone hexahydrobenzylcarbonate (trenbolone cyclohexylmethylcarbonate)
17α-Alkylated testosterone derivatives: Bolasterone
Calusterone
Chlorodehydromethyltestosterone (CDMT)
Fluoxymesterone
Formebolone
Metandienone (methandienone, methandrostenolone)
Methandriol (methylandrostenediol)
Methandriol bisenanthoyl acetate
Methandriol dipropionate
Methandriol propionate
Methyltestosterone
Methyltestosterone 3-hexyl ether
Oxymesterone
Penmesterol
Tiomesterone (thiomesterone)
17α-Alkylated dihydrotestosterone derivatives: Androisoxazole
Furazabol
Mebolazine (dimethazine)
Mestanolone
Oxandrolone
Oxymetholone
Stanozolol
17α-Alkylated 19-nortestosterone derivatives: Ethylestrenol
Mibolerone
Norethandrolone
Normethandrone (methylestrenolone, normethisterone)
Propetandrol (propethandrol)
17α-Vinyltestosterone derivatives: Norvinisterone (vinylnortestosterone)
17α-Ethynyltestosterone derivatives: Danazol
Gestrinone
Progestins (e.g., ethisterone (ethynyltestosterone) , levonorgestrel , norgestrel , norethisterone (norethindrone) , lynestrenol , norgestrienone )
Tibolone
Progesterone derivatives: Medroxyprogesterone acetate
Progonadotropins
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
Nonsteroidal: (R,R)-THC
(S,S)-THC
2,8-DHHHC
β-LGND1
β-LGND2 (GTx-878)
AC-186
Allenestrol
Allenolic acid
Benzestrol
Bifluranol
Bisdehydrodoisynolic acid
Butestrol
Carbestrol
D-15414
DCW234
Diarylpropionitrile
Dienestrol
Diethylstilbestrol
Dimestrol (dianisylhexene)
Dimethylstilbestrol
Doisynoestrol (fenocycline)
Doisynolic acid
Efavirenz
Elacestrant
ERB-196 (WAY-202196)
Erteberel (SERBA-1, LY-500307)
Estrobin (DBE)
Fenestrel
FERb 033
Fosfestrol (diethylstilbestrol diphosphate)
Furostilbestrol (diethylstilbestrol difuroate)
GTx-758
Hexestrol
ICI-85966 (Stilbostat)
M2613
meso -Butestrol
meso -Hexestrol
Mestilbol
Methallenestril
Methestrol
Methestrol dipropionate
Paroxypropione
Pentafluranol
Phenestrol
Prinaberel (ERB-041, WAY-202041)
Propylpyrazoletriol
Quadrosilan
SC-3296
SC-4289
SERBA-2
SKF-82,958
Terfluranol
Triphenylbromoethylene
Triphenylchloroethylene
Triphenyliodoethylene
Triphenylmethylethylene (triphenylpropene)
WAY-166818
WAY-169916
WAY-200070
WAY-204688 (SIM-688)
WAY-214156
Unknown/unsorted: ERB-26
ERA-45
ERB-79
ZK-283197
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
GPER Tooltip G protein-coupled estrogen receptor
Agonists Antagonists Unknown
AR Tooltip Androgen receptor
Agonists
Testosterone derivatives: 4-Androstenediol
4-Dehydroepiandrosterone (4-DHEA)
4-Hydroxytestosterone
4,17α-Dimethyltestosterone
5-Androstenedione
11-Ketotestosterone
11β-Hydroxyandrostenedione
Adrenosterone (11-ketoandrostenedione, 11-oxoandrostenedione)
Androstenediol (5-androstenediol)
Androstenedione (4-androstenedione)
Atamestane
Boldenone
Boldione (1,4-androstadienedione)
Clostebol
Cloxotestosterone
Dehydroandrosterone
DHEA (androstenolone, prasterone; 5-DHEA)
Exemestane
Formestane
Plomestane
Quinbolone
Silandrone
Testosterone # (+dutasteride )
5α-Dihydrotestosterone derivatives: 1-Androstenediol
1-Androstenedione
1-Androsterone (1-andro, 1-DHEA)
1-Testosterone
3α-Androstanediol
5α-Androst-2-en-17-one
7β-Hydroxyepiandrosterone
11-Ketodihydrotestosterone
Androsterone
Bolazine
Dihydroethyltestosterone
Dihydrofluoxymesterone
Dihydromethylandrostenediol
Dihydrotestosterone (DHT) (androstanolone, stanolone )
Drostanolone
Epiandrosterone
Epitiostanol
Mepitiostane
Mesabolone
Mesterolone
Methyldiazinol
Nisterime
Prostanozol
Stenbolone
Testifenon (testiphenon, testiphenone)
19-Nortestosterone derivatives: 7α-Methyl-19-norandrostenedione (MENT dione, trestione)
11β-Methyl-19-nortestosterone
19-Nor-5-androstenediol
19-Nor-5-androstenedione
19-Nordehydroepiandrosterone
Bolandiol
Bolandione (19-nor-4-androstenedione)
Bolmantalate (nandrolone adamantoate)
Dienedione
Dienolone
Dimethandrolone
LS-1727 (nandrolone 17β-N -(2-chloroethyl)-N -nitrosocarbamate)
Methoxydienone (methoxygonadiene)
Nandrolone
Norclostebol
Normethandrone (methylestrenolone, normethisterone)
Oxabolone
Trenbolone
Trendione
Trestolone (MENT)
5α-Dihydro-19-nortestosterone derivatives: 5α-Dihydronandrolone
5α-Dihydrotrestolone
19-Norandrosterone
17α-Alkylated testosterone derivatives: Bolasterone
Calusterone
Chlorodehydromethylandrostenediol (CDMA)
Chlorodehydromethyltestosterone (CDMT)
Chloromethylandrostenediol (CMA)
Enestebol
Ethyltestosterone
Fluoxymesterone
Formebolone
Hydroxystenozole
Metandienone (methandrostenolone)
Methandriol (methylandrostenediol)
Methylclostebol (chloromethyltestosterone)
Methyltestosterone (+esterified estrogens )
Oxymesterone
Penmesterol
Tiomesterone
17α-Alkylated 5α-dihydrotestosterone derivatives: Androisoxazole
Desoxymethyltestosterone
Furazabol
Mebolazine (dimethazine)
Mestanolone
Metenolone
Methasterone
Methyl-1-testosterone
Methylepitiostanol
Methylstenbolone
Oxandrolone
Oxymetholone
Stanozolol
17α-Alkylated 19-nortestosterone derivatives: Bolenol
Dimethyldienolone
Dimethyltrienolone
Ethyldienolone
Ethylestrenol
Methyldienolone
Methylhydroxynandrolone (MOHN, MHN)
Metribolone
Mibolerone
Norboletone
Norethandrolone
Propetandrol
RU-2309
Tetrahydrogestrinone
17α-Alkylated 5α-dihydro-19-nortestosterone derivatives: 5α-Dihydronorethandrolone
5α-Dihydronormethandrone
17α-Vinyltestosterone derivatives: Norvinisterone (vinylnortestosterone)
17α-Vinyl-19-nortestosterone derivatives: Vinyltestosterone
17α-Ethynyltestosterone derivatives: Danazol
Ethinylandrostenediol
Ethisterone (ethynyltestosterone)
5α-Dihydro-17α-ethynyltestosterone derivatives: 17α-Ethynyl-3α-androstanediol
17α-Ethynyl-3β-androstanediol
Dihydroethisterone
17α-Ethynyl-19-nortestosterone derivatives: Δ4 -Tibolone
Desogestrel
Etonogestrel
Etynodiol
Gestodene
Gestrinone
Levonorgestrel
Levonorgestrel esters (e.g., levonorgestrel butanoate )
Lynestrenol
Norethisterone
Norethisterone esters (e.g., norethisterone acetate , norethisterone enanthate )
Norgestrel
Norgestrienone
Quingestanol
Tibolone
5α-Dihydro-17α-ethynyl-19-nortestosterone derivatives: 5α-Dihydrolevonorgestrel
5α-Dihydronorethisterone
Progesterone derivatives: 6α-Methylprogesterone
Medroxyprogesterone acetate
Megestrol acetate
Others/unsorted: 3-Keto-5α-abiraterone
5α-Androstane
Alternariol
Cl-4AS-1
Drupanol
Trilostane
ZM-182345
SARMs Tooltip Selective androgen receptor modulator Antagonists
GPRC6A