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Please use this identifier to cite or link to this item: http://hdl.handle.net/1843/54691
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dc.creatorGiovanni Grandipt_BR
dc.creatorMaria Chiara Del Saviopt_BR
dc.creatorAgnaldo Lopes da Silva Filhopt_BR
dc.creatorFabio Facchinettipt_BR
dc.date.accessioned2023-06-07T23:04:11Z-
dc.date.available2023-06-07T23:04:11Z-
dc.date.issued2020-04-07-
dc.citation.volume13pt_BR
dc.citation.issue4pt_BR
dc.citation.spage327pt_BR
dc.citation.epage330pt_BR
dc.identifier.doihttps://doi.org/10.1080/17512433.2020.1750365pt_BR
dc.identifier.issn1751-2441pt_BR
dc.identifier.urihttp://hdl.handle.net/1843/54691-
dc.description.resumoEstetrol (E4) is a natural fetal estrogenic steroid discovered in 1965 at the Karolinska Institutet in Stockholm (Sweden). It was studied for a period of 20 years originally as a biomarker of fetal wellbeing during pregnancy [2] before being abandoned as a weak estrogen: research into the potential physiological effects and applications of E4 resumed in 2001. E4 is a steroid hormone with four -OH groups, two more than estradiol (E2), the estrogen physiologically produced by the granulosa cells of human ovaries (Figure 1). The fetal liver is the exclusive site responsible for 15α- and 16α-hydroxylation: for this reason, E4 is only present during pregnancy from 9 weeks of gestation until only shortly after birth but its physiological role is still unknown. The two additional -OH groups have a crucial impact on the oral pharmacokinetics: the half-life of E4 is 20–28 hours, compared with only 10–20 minutes for estriol (E3), 1–2 hours for natural E2 and 10–12 hours formicronized E2. E4 is minimally, if at all,metabolized and not reconverted to E3 or E2. Receptor binding and target interaction studies showed E4 to have high selectivity for the estrogen receptors (ER), indicating a potential for low risk of side effects. No specific toxicity for E4 has been observed to date. The estrogen dose in COCs has gone from micrograms (50 to 15) in the age of EE, to a few milligrams (1.5–3) in the E2 era, to several milligrams (15) in the age of E4, as the estrogenic component became weaker and weaker: during evolution the emphasis has shifted from the crude mass of steroids administered to their real biological activity. In terms of safety, mainly the lowest E4 doses seems to be associated to a favorable hemostatic profile and impact on lipids, low drug-drug interaction and a limited stimulation of breast tissue. The 10 mg E4 dose potency at endometrial level seems similar to that of the 2 mg E2 V dose: for this reason it seems that at the highest doses of E4 used and studied (≥ 15mg), E4 COCs can guarantee more satisfactory cycle control in comparison to E2-based COCs (i.e. lowrate of unscheduled bleeding and/or spotting and the absence of withdrawal bleeding). Unfortunately, at these E4 doses (≥ 15 mg) the hemostatic and metabolic effects of this combination have not been deeply studied and it has not been clearly demonstrated to be weaker than during traditional EE-based COCs. However, this third estrogenic generation of COCs could provide additional benefits to women’s health and in the coming years will be a topic for great interest and further personalization in hormonal contraception technology.pt_BR
dc.format.mimetypepdfpt_BR
dc.languageengpt_BR
dc.publisherUniversidade Federal de Minas Geraispt_BR
dc.publisher.countryBrasilpt_BR
dc.publisher.departmentMED - DEPARTAMENTO DE GINECOLOGIA OBSTETRÍCIApt_BR
dc.publisher.initialsUFMGpt_BR
dc.relation.ispartofExpert Review of Clinical Pharmacology-
dc.rightsAcesso Abertopt_BR
dc.subjectHormonal contraceptionpt_BR
dc.subjectCombined hormonal contraceptivespt_BR
dc.subjectEthinyl-estradiolpt_BR
dc.subjectEstradiolpt_BR
dc.subjectEstetrolpt_BR
dc.subjectDrospirenonept_BR
dc.subjectEvonorgestrelpt_BR
dc.subjectHemostasispt_BR
dc.subjectMetabolismpt_BR
dc.subjectVenous thromboembolic eventspt_BR
dc.subjectCardiovascular riskspt_BR
dc.subject.otherContracepção hormonalpt_BR
dc.subject.otherEstetrolpt_BR
dc.subject.otherMetabolismopt_BR
dc.subject.otherHemostasiapt_BR
dc.subject.otherFatores de risco de doenças cardíacaspt_BR
dc.subject.otherHormôniospt_BR
dc.subject.otherEsteroidespt_BR
dc.titleEstetrol (E4): the new estrogenic component of combined oral contraceptivespt_BR
dc.typeArtigo de Periódicopt_BR
dc.url.externahttps://www.tandfonline.com/doi/full/10.1080/17512433.2020.1750365pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-8486-7861pt_BR
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