Gestrinona
Revisão de evidência científica
Dr. Leonardo Jacobsen · 2026
Gestrinona/Apêndice/Referências

Referências

84 referênciasordenadas por autorcom PubMed e DOI

Bibliografia consolidada de toda a obra. Cada entrada liga ao registro no PubMed e, quando disponível, ao DOI. Referências de tetra-hidrogestrinona (THG) referem-se ao análogo de dopagem, não à gestrinona (ver o capítulo sobre a THG).

  • Alvarez F, et al. (1978). Comparative clinical trial of the progestins R-2323 and levonorgestrel administered by subdermal implants. Contraception. 18(2):151–162. PubMed·DOI
  • Arakawa S, et al. (1989). Inhibition of rat ovarian 3β-hydroxysteroid dehydrogenase, 17α-hydroxylase and 17,20 lyase by progestins and danazol. Endocrinol Jpn. 36(3):387–394. PubMed·DOI
  • Brown J, Kives S, Akhtar M. (2012). Progestagens and anti-progestagens for pain associated with endometriosis. Cochrane Database Syst Rev. (3):CD002122. PubMed·DOI
  • Catlin DH, Sekera MH, Ahrens BD, Starcevic B, Chang YC, Hatton CK. (2004). Tetrahydrogestrinone: discovery, synthesis, and detection in urine. Rapid Commun Mass Spectrom. 18(12):1245–1249. PubMed·DOI
  • Ciou HH, et al. (2022). Repurposing gestrinone for tumor suppressor through P21 reduction regulated by JNK in gynecological cancer. Transl Res. 243:21–32. PubMed·DOI
  • Clébicar Barbosa C, Moreira Braz A, Demolinari Coelho C, et al. (2026). Implante de gestrinona para fins estéticos: perfil, percepção e efeitos adversos autorrelatados em mulheres adultas. Ciência et Praxis. 22(37):51–60. DOI
  • Coutinho EM. (1981). Conservative treatment of uterine leiomyoma with the antiestrogen antiprogesterone R-2323. Int J Gynaecol Obstet. 19(5):357–360. PubMed·DOI
  • Coutinho EM. (1982). Treatment of endometriosis with gestrinone (R-2323), a synthetic antiestrogen, antiprogesterone. Am J Obstet Gynecol. 144(8):895–898. PubMed·DOI
  • Coutinho EM, Azadian-Boulanger G. (1984). Treatment of fibrocystic disease of the breast with gestrinone, a new trienic synthetic steroid with anti-estrogen, anti-progesterone properties. Int J Gynaecol Obstet. 22(5):363–366. PubMed·DOI
  • Coutinho EM, Azadian-Boulanger G, Gonçalves MT. (1986). Regression of uterine leiomyomas after treatment with gestrinone, an antiestrogen, antiprogesterone. Am J Obstet Gynecol. 155(4):761–767. PubMed·DOI
  • Coutinho EM, Gonçalves MT, Azadian-Boulanger G, Silva AR. (1987). Endometriosis therapy with gestrinone by oral, vaginal or parenteral administration. Contrib Gynecol Obstet. 16:227–235. PubMed
  • Coutinho EM, Azadian-Boulanger G. (1988). Treatment of endometriosis by vaginal administration of gestrinone. Fertil Steril. 49(3):418–422. PubMed
  • Coutinho EM. (1989a). Gestrinone in the treatment of myomas. Acta Obstet Gynecol Scand Suppl. 150:39–46. PubMed·DOI
  • Coutinho EM, Gonçalves MT. (1989b). Long-term treatment of leiomyomas with gestrinone. Fertil Steril. 51(6):939–946. PubMed·DOI
  • Coutinho EM. (1990). Treatment of large fibroids with high doses of gestrinone. Gynecol Obstet Invest. 30(1):44–47. PubMed
  • David SS, Huggins GR, Garcia CR, Busacca C. (1979). A synthetic steroid (R2323) as a once-a-week oral contraceptive. Fertil Steril. 31(3):278–281. PubMed
  • Dawood MY, Obasiolu CW, Ramos J, Khan-Dawood FS. (1997). Clinical, endocrine, and metabolic effects of two doses of gestrinone in treatment of pelvic endometriosis. Am J Obstet Gynecol. 176(2):387–394. PubMed
  • De Leo V, Morgante G, La Marca A, et al. (2002). A benefit-risk assessment of medical treatment for uterine leiomyomas. Drug Saf. 25(11):759–779. PubMed·DOI
  • Devogelaer JP, Nagant de Deuxchaisnes C, Donnez J. (1993). Endometriosis [letter]. Lancet. 341(8840):312–313. PubMed·DOI
  • Dhar R, Stout CW, Link MS, Homoud MK, Weinstock J, Estes NA III. (2005). Cardiovascular toxicities of performance-enhancing substances in sports. Mayo Clin Proc. 80(10):1307–1315. PubMed·DOI
  • Dowsett M, Forbes KL, Rose GL, Mudge JE, Jeffcoate SL. (1986). A comparison of the effects of danazol and gestrinone on testosterone binding to sex hormone binding globulin in vitro and in vivo. Clin Endocrinol (Oxf). 24(5):555–563. PubMed·DOI
  • Becker CM, Bokor A, Heikinheimo O, et al; ESHRE Endometriosis Guideline Development Group. (2022). ESHRE guideline: endometriosis. Hum Reprod Open. 2022(2):hoac009. PubMed·DOI
  • Ezzat L. (2017). Medical treatment of endometriosis: an update. Int J Reprod Contracept Obstet Gynecol. 6(10):4187–4192. DOI
  • Fagundes VL, et al. (2025). Safety profile of gestrinone: a systematic review. Pharmaceutics. 17(5):638. PubMed·DOI
  • Fedele L, Bianchi S, Viezzoli T, Arcaini L, Candiani GB. (1989). Gestrinone versus danazol in the treatment of endometriosis. Fertil Steril. 51(5):781–785. PubMed·DOI
  • Fedele L, Marchini M, Baglioni A, Dell'Antonio G, Motta T. (1990). Evaluation of histological and ultrastructural aspects of endometrium during treatment with gestrinone in women with amenorrhea or spotting. Acta Obstet Gynecol Scand. 69(2):143–146. PubMed·DOI
  • Fedele L, Marchini M, Bianchi S, Di Nola G. (1995). Histological impact of medical therapy — clinical implications. Br J Obstet Gynaecol. 102(Suppl 12):8–11. PubMed·DOI
  • Forbes KL, Thomas FJ. (1993). Tissue and endocrine responses to gestrinone and danazol in the treatment of endometriosis. Reprod Fertil Dev. 5(1):103–109. PubMed·DOI
  • Foster ZJ, Housner JA. (2004). Anabolic-androgenic steroids and testosterone precursors: ergogenic aids and sport. Curr Sports Med Rep. 3(4):234–241. PubMed·DOI
  • Fu J, Song H, Zhou M, Zhu H, Wang Y, Chen H, Huang W. (2017). Progesterone receptor modulators for endometriosis. Cochrane Database Syst Rev. (7):CD009881. PubMed·DOI
  • Gao X, Wu E, Chen G. (2007). Mechanism of emergency contraception with gestrinone: a preliminary investigation. Contraception. 76(3):221–227. PubMed·DOI
  • Halbe HW, Nakamura MS, da Silveira GPG, Carvalho WPC. (1995). Updating the clinical experience in endometriosis — the Brazilian perspective. Br J Obstet Gynaecol. 102(Suppl 12):17–21. PubMed·DOI
  • Hornstein MD, Gleason RE, Barbieri RL. (1990). A randomized double-blind prospective trial of two doses of gestrinone in the treatment of endometriosis. Fertil Steril. 53(2):237–241. PubMed
  • The Gestrinone Italian Study Group. (1996). Gestrinone versus a gonadotropin-releasing hormone agonist for the treatment of pelvic pain associated with endometriosis: a multicenter, randomized, double-blind study. Fertil Steril. 66(6):911–919. PubMed·DOI
  • Jeng CJ, Chuang L, Shen J. (2014). A comparison of progestogens or oral contraceptives and gonadotropin-releasing hormone agonists for the treatment of endometriosis: a systematic review. Expert Opin Pharmacother. 15(6):767–773. PubMed·DOI
  • Kauppila A, Isomaa V, Rönnberg L, Vierikko P, Vihko R. (1985). Effect of gestrinone in endometriosis tissue and endometrium. Fertil Steril. 44(4):466–470. PubMed·DOI
  • Kauppila A. (1993). Changing concepts of medical treatment of endometriosis. Acta Obstet Gynecol Scand. 72(5):324–336. PubMed·DOI
  • Kim Y, et al. (2000). Determination and excretion study of gestrinone in human urine by high performance liquid chromatography and gas chromatography/mass spectrometry. Rapid Commun Mass Spectrom. 14(14):1293–1300. PubMed
  • Kim Y, et al. (2000b). Determination of the metabolites of gestrinone in human urine by high performance liquid chromatography, liquid chromatography/mass spectrometry and gas chromatography/mass spectrometry. Rapid Commun Mass Spectrom. 14(18):1717–1726. PubMed·DOI
  • Kou L, Huang C, Xiao D, Liao S, Li Y, Wang Q. (2025). Pharmacologic interventions for endometriosis-related pain: a systematic review and network meta-analysis. Obstet Gynecol. (online). PubMed·DOI
  • Kuuranne T, et al. (2008). Screening of in vitro synthesised metabolites of 4,9,11-trien-3-one steroids by liquid chromatography-mass spectrometry. Eur J Mass Spectrom (Chichester). 14(3):181–189. PubMed·DOI
  • Labrie F, Luu-The V, Martel C, Chernomoretz A, Calvo E, Morissette J, Labrie C. (2006). Dehydroepiandrosterone (DHEA) is an anabolic steroid like dihydrotestosterone (DHT), the most potent natural androgen, and tetrahydrogestrinone (THG). J Steroid Biochem Mol Biol. 100(1–3):52–58. PubMed·DOI
  • Lévesque JF, Templeton E, Trimble L, Berthelette C, Chauret N. (2005). Discovery, biosynthesis, and structure elucidation of metabolites of a doping agent and a direct analogue, tetrahydrogestrinone and gestrinone, using human hepatocytes. Anal Chem. 77(10):3164–3172. PubMed·DOI
  • Lobo VLR, et al. (2008). Does gestrinone antagonize the effects of estrogen on endometrial implants upon the peritoneum of rats? Clinics (Sao Paulo). 63(4):525–530. PubMed·DOI
  • Machnik M, Gerlach M, Kietzmann M, Niedorf F, Thevis M, Schenk I, Guddat S, Düe M, Schänzer W. (2009). Detection and pharmacokinetics of tetrahydrogestrinone in horses. J Vet Pharmacol Ther. 32(2):197–202. PubMed·DOI
  • Maia H Jr, Haddad C, Moura Hirsch MC, Saback W, Casoy J. (2014). Treatment of refractory endometriosis-related pain with vaginal gestrinone in Pentravan associated with Pinus pinaster extract and resveratrol: a preliminary study. Gynecol Obstet (Sunnyvale). 4(9):246. DOI
  • Malavasi A, et al. (2025). Rationale and design of the GLADE study: a randomized, multicenter, double-blind, placebo-controlled trial evaluating the safety and efficacy of gestrinone subdermal bioabsorbable pellet in endometriosis-related pelvic pain. Ann Med. 57(1):2527352. PubMed·DOI
  • Marchini M, Fedele L, Bianchi S, Di Nola G, Nava S, Vercellini P. (1992). Endometrial patterns during therapy with danazol or gestrinone for endometriosis: structural and ultrastructural study. Hum Pathol. 23(1):51–56. PubMed·DOI
  • Mizutani T, et al. (1992). No inhibitory effects of gestrinone and medroxyprogesterone acetate on the estrogen production by ovaries of hypophysectomized rats stimulated by gonadotropins. Endocrinol Jpn. 39(6):615–621. PubMed·DOI
  • Niaraki MA, Moghissi KS, Borin K. (1981). The effect of a synthetic progestogen, ethylnorgestrienone, on hypothalamic-pituitary-ovarian function, cervical mucus, vaginal cytology, and endometrial morphology. Fertil Steril. 35(3):284–288. PubMed·DOI
  • Nieto A, et al. (1997). Evaluation of gestrinone after surgery in treatment of endometriosis. Gynecol Obstet Invest. 43(3):192–194. PubMed·DOI
  • Ohno Y, et al. (1991). Antiestrogenic effect of gestrinone as an inhibitor of [3H]-estradiol binding to nuclear type II sites. Gynecol Obstet Invest. 31(2):97–101. PubMed·DOI
  • Orlando R, et al. (2007). Nanomolar concentrations of anabolic-androgenic steroids amplify excitotoxic neuronal death in mixed mouse cortical cultures. Brain Res. 1165:21–29. PubMed·DOI
  • Pereira HMG, Padilha MC, Radler de Aquino Neto F. (2009). Tetrahydrogestrinone analysis and designer steroids revisited. Bioanalysis. 1(8):1475–1489. PubMed·DOI
  • Peters F. (1992). Multicentre study of gestrinone in cyclical breast pain. Lancet. 339(8787):205–208. PubMed·DOI
  • de Souza Pinto LP, Ferrari G, dos Santos IK, de Mello Roesler CR, de Mello Gindri I. (2023). Evaluation of safety and effectiveness of gestrinone in the treatment of endometriosis: a systematic review and meta-analysis. Arch Gynecol Obstet. 307(1):21–37. PubMed·DOI
  • Raynaud JP, Ojasoo T. (1986). The design and use of sex-steroid antagonists. J Steroid Biochem. 25(5B):811–833. PubMed·DOI
  • Renke G, Antunes M, Sakata R, Tostes F. (2024). Effects, doses, and applicability of gestrinone in estrogen-dependent conditions and post-menopausal women. Pharmaceuticals (Basel). 17(9):1248. PubMed·DOI
  • Rose GL, et al. (1988). The inhibitory effects of danazol, danazol metabolites, gestrinone, and testosterone on the growth of human endometrial cells in vitro. Fertil Steril. 49(2):224–228. PubMed·DOI
  • Roy SN, Bhattacharya S. (2004). Benefits and risks of pharmacological agents used for the treatment of menorrhagia. Drug Saf. 27(2):75–90. PubMed·DOI
  • Sagsveen M, Farmer JE, Prentice A, Breeze A. (2003). Gonadotrophin-releasing hormone analogues for endometriosis: bone mineral density. Cochrane Database Syst Rev. (4):CD001297. PubMed·DOI
  • Shaw RW. (1994). A risk benefit assessment of drugs used in the treatment of endometriosis. Drug Saf. 11(2):104–113. PubMed·DOI
  • Snyder BW, Beecham GD, Winneker RC. (1989). Studies on the mechanism of action of danazol and gestrinone (R2323) in the rat: evidence for a masked estrogen component. Fertil Steril. 51(4):705–710. PubMed·DOI
  • Spellacy WN, Mahan CS, Buhi WC, Dumbaugh VA, Birk SA. (1978). Blood glucose, insulin, cholesterol and triglyceride levels in women treated for six months with the weekly oral contraceptive R2323. Contraception. 18(2):121–126. PubMed·DOI
  • Sun F, Qi Y, Zhuang L, Huang Y. (2026). Thermal ablation and thermal ablation combined with medical therapy for adenomyosis: a systematic review and network meta-analysis. Ultrasound Med Biol. 52(6):993–1001. PubMed·DOI
  • Tamaya T, et al. (1991). Rationale for frequency and dose of administration in gestrinone therapy for pelvic endometriosis in the experimental model of rabbit uterus. Gen Pharmacol. 22(3):505–510. PubMed·DOI
  • Thomas EJ, Cooke ID. (1987). Impact of gestrinone on the course of asymptomatic endometriosis. Br Med J (Clin Res Ed). 294(6567):272–274. PubMed
  • Triolo O, De Vivo A, Benedetto V, Falcone S, Antico F. (2006). Gestrinone versus danazol as preoperative treatment for hysteroscopic surgery: a prospective, randomized evaluation. Fertil Steril. 85(4):1027–1031. PubMed·DOI
  • Turnbull AC, Rees MCP. (1990). Gestrinone in the treatment of menorrhagia. Br J Obstet Gynaecol. 97(8):713–715. PubMed
  • Venturini PL, Bertolini S, Fasce V, et al. (1989). Endocrine, metabolic, and clinical effects of gestrinone in women with endometriosis. Fertil Steril. 52(4):589–595. PubMed
  • Verma U, Laumas KR. (1981). Screening of anti-progestins using in vitro human uterine progesterone receptor assay system. J Steroid Biochem. 14(8):733–740. PubMed·DOI
  • Veth VB, van de Kar MMA, Duffy JMN, van Wely M, Mijatovic V, Maas JWM. (2023). Gonadotropin-releasing hormone analogues for endometriosis. Cochrane Database Syst Rev. 6(6):CD014788. PubMed·DOI
  • Pinto da Costa Viana D, Jacobsen L, Padovesi I, et al. (2025). Tolerability and shared decision-making in the hormonal management of endometriosis-associated pain. Biomedicines. 13(9):2294. PubMed·DOI
  • Viganò P, et al. (1994). Gestrinone inhibits macrophage function and mitogen-stimulated lymphocyte proliferation in vitro. J Reprod Immunol. 27(1):63–71. PubMed·DOI
  • Wang Q, et al. (2000). Determination of gestrinone in human serum by liquid chromatography-electrospray tandem mass spectrometry. J Chromatogr B Biomed Sci Appl. 746(2):151–159. PubMed·DOI
  • Worthington M, Lees B, Irvine LM, Shaw RW, Crook D, Stevenson JC. (1993). A randomized comparative study of the metabolic effects of two regimens of gestrinone in the treatment of endometriosis. Fertil Steril. 59(3):522–526. PubMed·DOI
  • Wu S, Dong J, Cong J, Wang C, VonHertzen H, Godfrey EM. (2010). Gestrinone compared with mifepristone for emergency contraception: a randomized controlled trial. Obstet Gynecol. 115(4):740–744. PubMed·DOI
  • Wu L, Wu Q, Liu L. (2013). Oral contraceptive pills for endometriosis after conservative surgery: a systematic review and meta-analysis. Gynecol Endocrinol. 29(10):883–890. PubMed·DOI
  • Xiong Y, Huang W, Wang C, et al. (2026). Effectiveness and safety of postoperative medical treatments following fertility-preserving surgery for endometriosis: a network meta-analysis. BJOG. 133(2):253–262. PubMed·DOI
  • Yang TS, Tsan SH, Chen CR, Chang SP, Ng HT. (1996). The efficacy and safety of a 19 nor-steroid in the treatment of endometriosis. Chin Med J (Taipei). 58(2):89–96. PubMed
  • Zheng Y, Ma R, Xu H, Wang L, Zhang L, Mao H, Zhao R. (2023). Efficacy and safety of different subsequent therapies after fertility preserving surgery for endometriosis: a systematic review and network meta-analysis. Medicine (Baltimore). 102(31):e34496. PubMed·DOI
  • Zhu Y, Qiu XY, Wang L, et al. (2007). Effects of gestrinone on uterine leiomyoma and expression of c-Src in a guinea pig model. Acta Pharmacol Sin. 28(5):685–694. PubMed·DOI
  • Zhu Y, Zhang T, Xie S, et al. (2012). Gestrinone inhibits growth of human uterine leiomyoma may relate to activity regulation of ERα, Src and P38 MAPK. Biomed Pharmacother. 66(8):569–577. PubMed·DOI
  • Zierau O, Lehmann S, Vollmer G, Schänzer W, Diel P. (2008). Detection of anabolic steroid abuse using a yeast transactivation system. Steroids. 73(11):1143–1147. PubMed·DOI
Nota
Lista compilada automaticamente a partir das referências citadas nos onze capítulos, deduplicadas por identificador PubMed. Revisão pessoal de evidência — não é publicação revisada por pares.