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Estradiol

Estrogens
CATEGORIES

Estrogens, Contraceptive Agents, Anti-menopausal Agents


ALIASES

Activelle, Aerodiol, Agofollin, Alpicort, Alora, Angeliq, Angemin, Armonil, Betatabs, Calidiol, Cetura, Clifemme, Climaston, Climara, Climen, Climodien, Cliovellan, Cliovelle, Cyclabil, Cyclo-Progynova, Delestrogen, Dermestril, Divigel, Divina, Duogestan, Duova, Epheilia, Epiestrol, Eptausa, Esclima, Estalis, Estraderm, Estradiolo, Estradot, Estradurin, Estrahexal, Estreva, Estring, Estrimax, Estroclim, Estrodose, Estrofem, Estrogel, Eviana, Evopad, Evorel, Fematab, Femsete Combi, FemSeven, Femanest®, Femanor®, Femasekvens®, Feminova, Femoston, Femphascyl, FemSeven, Femostonconti, Folivirin, Gelestra, Ginaikos, Gracial, Gynodian, Indivina, IOA, Juvinelle, Klaira, Kliane, Klimodien, Klimonorm, Kliogest, Lafamme, Lenzetto, Levelyn, Linoladiol, Lyrelle, Menorest, Merimono, Montadiol, Naemis, Neofolin, Noresmea, Novofem, Oesclim, Oestraclin, Oestring, Oestrodose, Oestrogel, Olaira, Pausogest, Prapanol, Progynon, Progynova, Provames, Qlaira, Sandrena, Sequidot, Sibilla, Sprediol, Systen, Thais, Theralgan, Totelle Sekvens, Triaklim, Trisekvens, Trisequense, Trivina, Tulita, Vagifem, Velbienne, Vivelle, Zerella, Zoely, Zumenon


SUBSTANCES

estradiol, estradiol 3-acetate, estradiol hemihydrate, estradiol valerate


ENVIRONMENTAL CONCERN: HIGH
Generally refers to the 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Various isomers can be synthesized. [PubChem]

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HIGH
Estradiol is on the EU list of substances whose concentrations in surface waters should be monitored in the Member States for environmental reasons. In addition to e.g. ethinyl estradiol and endogenous estrogen, estradiol contributes to the amount of estrogens in the environment. See also ethinyl estradiol.

Estradiol is included in the Stockholm County Council's table of pharmaceuticals with a negative environmental impact according to the environmental programme 2017-2021.

Estradiol is more easily degraded than ethinyl estradiol in the body, in the wastwater treatment plant, in the environment and is less potent in fish. An oral dose of 1.5 mg estradiol gives an excreeted dose in the urine of only 100 micrograms. Therefore, the risk is probably lower with estradiol despite the often higher dosage. 

Is recommended in The Wise List. Environmental classification of pharmaceuticals is taken into consideration, sometimes with other environmental aspects, when selecting pharmaceuticals for the Wise List. When comparable pharmaceuticals are equivalent to medical effects, safety and pharmaceutical efficacy, environmental impact and price are considered.

Suggestions on how to reduce the release of estradiol
Concrete proposals on how to work to reduce emissions of environmentally harmful pharmaceuticals on the list have been developed in close cooperation with the Stockholm Drug and Therapeutics Committee's expert advice. The action proposals were developed from an environmental perspective. The patient's best always goes first and several pharmaceuticals on the list are also included in the Wise List. However, for such pharmaceuticals, there may be measures that could reduce the environmental impact.

Concrete proposal for estradiol:
• Estradiol is recommended in the Wise List.
• Individual adaptation of contraceptives as well as pharmaceuticals for treatment of menopausal symptoms and symptomatic vaginal atrophy is important in order to optimize treatment and avoid side effects.
• For topical application of patches with estradiol (Estradot, recommended in the Wise List) for menopausal symptoms, the amount of pharmaceutical administered to an individual is significantly lower than the dose required to give the corresponding effect with estradiol tablets.
• Ensure that you, in your own business, discard leftover pharmaceuticals and used patches and vaginal inserts correctly, http://www.janusinfo.se/Rutiner/Hantering-av-lakemedel/ 
• Inform the patient about the importance of discarding leftover pharmaceuticals, as well as used patches and vaginal inserts, correctly. Order the folder for patients "Protect the Environment – Throw in the Right Way" http://janusinfo.se/Beslutsstod/Miljo-och-lakemedel/Dokument/Informationsmaterial/

The risk classification moderate, according to Fass.se, is based on total sold amount (kg) of the substance in Sweden during the year 2011 and the toxicity of the substance.

REFERENCES

  1. Tan, B. L. L., D. W. Hawker, J. F. Mueller, F. D. L. Leusch, L. A. Tremblay and H. F. Chapman (2007). Comprehensive study of endocrine disrupting compounds using grab and passive sampling at selected wastewater treatment plants in South East Queensland, Australia. Environ Int 33, 654-669.
  2. Braga, O., G. A. Smythe, A. I. Schafer and A. J. Feitz (2005). Fate of steroid estrogens in Australian inland and coastal wastewater treatment plants. Environ Sci Technol 39, 3351-3358.
  3. Servos, M. R., D. T. Bennie, B. K. Burnison, A. Jurkovic, R. McInnis, T. Neheli, A. Schnell, P. Seto, S. A. Smythand T. A. Ternes (2005). Distribution of estrogens, 17 beta-estradiol and estrone, in Canadian municipal wastewater treatment plants. Sci Total Environ 336, 155-170.
  4. Zorita, S., L. Mårtensson and L. Mathiasson (2009). Occurrence and removal of pharmaceuticals in a municipal sewage treatment system in the south of Sweden. Sci Total Environ 407, 2760-2770.
  5. Fernandez, M. P., M. G. Ikonomou and I. Buchanan (2007). An assessment of estrogenic organic contaminants in Canadian wastewaters. Sci Total Environ 373, 250-269.
  6. Martín, J., D. Camacho-Muñoz, J. L. Santos, I. Aparicio and E. Alonso (2012). Occurrence of pharmaceutical compounds in wastewater and sludge from wastewater treatment plants: Removal and ecotoxicological impact of wastewater discharges and sludge disposal. J Hazard Mater. 239–240, 40-47.
  7. Bhandari, R., Deem, S., Holliday, D., Jandegian, C., Kassotis, C., Nagel, S., Tillitt, D., vom Saal, F., Rosenfeld, C., (2015), Effects of the environmental estrogenic contaminants bisphenol A and 17α-ethinyl estradiol on sexual development and adult behaviors in aquatic wildlife species, Gen Comp Endocrinol. Volume 214,195-219,
  8. Dammann, A., Shappell, N., Bartell, S., Schoenfuss, H., (2011), Comparing biological effects and potencies of estrone and 17β-estradiol in mature fathead minnows, Pimephales promelas, Aquat Toxicol. Volume 105, 559-568.
  9. Seki, M. , Fujishima, S. , Nozaka, T. , Maeda, M. and Kobayashi, K. (2006), Comparison of response to 17β‐estradiol and 17β‐trenbolone among three small fish species. Environ Toxicol Chem 25, 2742-2752.
  10. Seki, M. , Yokota, H. , Maeda, M. and Kobayashi, K. (2005), Fish full life‐cycle testing for 17β‐estradiol on medaka (Oryzias latipes). Environ Toxicol Chem, 24: 1259-1266.
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  12. Goodpoint. Prioritering av läkemedel med miljörisk inom SLL. Stockholm: Goodpoint; 2016. Rapport LS 2016–0634.
  13. Metcalfe CD, Metcalfe TL, Kiparissis Y, Koenig BG, Khan C, Hughes RJ et al. Estrogenic potency of chemicals detected in sewage treatment plant effluents as determined by in vivo assays with Japanese medaka (Oryzias latipes). Environ Toxicol Chem. 2001;20:297-308.
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  15. D.G.J Larsson, M Adolfsson-Erici, J Parkkonen, M Pettersson, A.H Berg, P.-E Olsson et al. Ethinyloestradiol — an undesired fish contraceptive? Aquatic Toxicology 1999; 45 (2-3): 91-97.
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  17. Friel PN, Hinchcliffe C, Wright JV. Hormone replacement with estradiol: conventional oral doses result in excessive exposure to estrone. Altern Med Rev. 2005;10:36-41.
  18. Stockholms läns landsting. Förteckning över miljöbelastande läkemedel med åtgärdsförslag framtagen inom ramen för SLL:s miljöprogram 2017–2021.
  19. Stockholms läns landsting. Kloka Listan 2018.
  20. Stockholm County Council. The Wise List 2015.
  21. Socialstyrelsen. Statistikdatabas för läkemedel.
  22. Stockholms läns landsting. Janusinfo: Läkemedelsuppföljning