Quinestrol is aprodrug ofethinylestradiol (EE), with no estrogenic activity of its own.[3][9][10] It is takenorally and has prolonged activity following a single dose,[9][10] with a very longbiological half-life of more than 120 hours (5 days) due to enhancedlipophilicity and storage infat.[3][1] Because of its much longer half-life, quinestrol is two to three times as potent as EE.[3] Also because of its long half-life, quinestrol can be taken once a week or once a month.[3][4][5][6][7]
Following administration, quinestrol is absorbed via thelymphatic system, is stored inadipose tissue, and is gradually released from adipose tissue.[11]
Quinestrol is thegeneric name of the drug and itsINNTooltip International Nonproprietary Name,USANTooltip United States Adopted Name, andBANTooltip British Approved Name.[31][32][34][35] It is also known by its former developmental code nameW-3566.[31][32][34][35]
Quinestrol has been marketed under brand names including Agalacto-Quilea, Basaquines, Eston, Estrovis, Estrovister, Plestrovis, Qui-Lea, Soluna, and Yueketing, among others.[31][32][34][35]
One tablet form available in China consists of 6 mg levonorgestrel and 3 mg quinestrol; it is used as a prescription "long-term" oral contraceptive, with one dose taken each month.[35][36] It is sold under various brand names including Yuèkětíng (Chinese:悦可婷) and Àiyuè (Chinese:艾悦). A version with the racemicnorgestrel in place of levonorgestrel also appears to be available.[35]
The Chinese levonorgestrel/quinestrol 2:1 formula is known as EP-1 in veterinary practice. It is known to have some organ-specific effects on theMongolian gerbil as measured by receptor mRNA expression.[37] Incorporated into baits at a concentration of 50 ppm, EP-1 has been used to control wild Mongolian gerbil populations with some success.[38]
^abcHorsky (6 December 2012)."Contraception". In Horsky J, Presl J (eds.).Ovarian Function and its Disorders: Diagnosis and Therapy. Springer Science & Business Media. pp. 85, 358, 367.ISBN978-94-009-8195-9.
^abEpstein JA (1967). "Prolonged menstrual response of patients with gonadal failure following quinestrol administration".International Journal of Fertility.12 (2):181–186.PMID6033895.
^abGiannina T, Meli A (April 1969). "Prolonged oestrogenic activity in rats after single oral administration of ethinyloestradiol-3-cyclopentyl ether".The Journal of Pharmacy and Pharmacology.21 (4):271–272.doi:10.1111/j.2042-7158.1969.tb08247.x.PMID4390151.S2CID19407816.
^Hammond CB, Maxson WS (January 1982). "Current status of estrogen therapy for the menopause".Fertility and Sterility.37 (1):5–25.doi:10.1016/S0015-0282(16)45970-4.PMID6277697.
^Lauritzen C (June 1977). "[Estrogen thearpy in practice. 3. Estrogen preparations and combination preparations]" [Estrogen therapy in practice. 3. Estrogen preparations and combination preparations].Fortschritte Der Medizin (in German).95 (21):1388–92.PMID559617.
^Lauritzen CH (January 1976). "The female climacteric syndrome: significance, problems, treatment".Acta Obstetricia Et Gynecologica Scandinavica. Supplement.51:47–61.doi:10.3109/00016347509156433.PMID779393.
^Lauritzen C (1975). "The Female Climacteric Syndrome: Significance, Problems, Treatment".Acta Obstetricia et Gynecologica Scandinavica.54 (s51):48–61.doi:10.3109/00016347509156433.ISSN0001-6349.
^Ryden AB (1950). "Natural and synthetic oestrogenic substances; their relative effectiveness when administered orally".Acta Endocrinologica.4 (2):121–39.doi:10.1530/acta.0.0040121.PMID15432047.
^Ryden AB (1951). "The effectiveness of natural and synthetic oestrogenic substances in women".Acta Endocrinologica.8 (2):175–91.doi:10.1530/acta.0.0080175.PMID14902290.
^Kottmeier HL (1947). "Ueber blutungen in der menopause: Speziell der klinischen bedeutung eines endometriums mit zeichen hormonaler beeinflussung: Part I".Acta Obstetricia et Gynecologica Scandinavica.27 (s6):1–121.doi:10.3109/00016344709154486.ISSN0001-6349.There is no doubt that the conversion of the endometrium with injections of both synthetic and native estrogenic hormone preparations succeeds, but the opinion whether native, orally administered preparations can produce a proliferation mucosa changes with different authors. PEDERSEN-BJERGAARD (1939) was able to show that 90% of the folliculin taken up in the blood of the vena portae is inactivated in the liver. Neither KAUFMANN (1933, 1935), RAUSCHER (1939, 1942) nor HERRNBERGER (1941) succeeded in bringing a castration endometrium into proliferation using large doses of orally administered preparations of estrone or estradiol. Other results are reported by NEUSTAEDTER (1939), LAUTERWEIN (1940) and FERIN (1941); they succeeded in converting an atrophic castration endometrium into an unambiguous proliferation mucosa with 120–300 oestradiol or with 380 oestrone.
^Martinez-Manautou J, Rudel HW (1966). "Antiovulatory Activity of Several Synthetic and Natural Estrogens". In Robert Benjamin Greenblatt (ed.).Ovulation: Stimulation, Suppression, and Detection. Lippincott. pp. 243–253.
^Herr F, Revesz C, Manson AJ, Jewell JB (1970). "Biological Properties of Estrogen Sulfates".Chemical and Biological Aspects of Steroid Conjugation. pp. 368–408.doi:10.1007/978-3-642-49793-3_8.ISBN978-3-642-49506-9.
^Medical Gynaecology and Sociology. Medical and Scientific Services Limited. 1967.[...] J. Fertil., 1967, 12, 2) contains 23 papers presented at a symposium on QUINESTROL. Quinestrol is a newly-developed synthetic steroid, and is the cyclo-pentyl ether of a ethinyl oestradiol.
^"悦可婷 左炔诺孕酮炔雌醚片 6片/盒" [Yueketing Levonorgestrel Ethinylestradiol Tablets 6 Pieces/Box].Tmall (in Chinese). Archived fromthe original on 2018-07-16. Retrieved2018-07-16.When taking the medicine for the first time, take the medicine once after lunch on the fifth day counting from the day of menstrual cramps, and take the second medicine at an interval of 20 days. Afterwards, take the second medicine taking day as the monthly medicine taking date, and take one tablet every month. When changing from short-acting oral contraceptives to long-acting contraceptives, you can take one long-acting contraceptive the next day after taking 22 tablets, and then take one tablet every month on the same day you started taking long-acting contraceptives.
^Lv X, Shi D (January 2012). "Combined effects of levonorgestrel and quinestrol on reproductive hormone levels and receptor expression in females of the Mongolian gerbil (Meriones unguiculatus)".Zoological Science.29 (1):37–42.doi:10.2108/zsj.29.37.PMID22233494.S2CID22347486.
^Fu H, Zhang J, Shi D, Wu X (September 2013). "Effects of levonorgestrel-quinestrol (EP-1) treatment on Mongolian gerbil wild populations: a case study".Integrative Zoology.8 (3):277–284.doi:10.1111/1749-4877.12018.PMID24020466.
