Norgestrienone, sold under the brand names Ogyline, Planor, and Miniplanor, is a progestin medication which has been used in birth control pills, sometimes in combination with ethinylestradiol.[1][2][3][4][5] It was developed by Roussel Uclaf and has been registered for use only in France.[4][5][6] Under the brand name Planor, it has been marketed in France as 2 mg norgestrienone and 50 μg ethinylestradiol tablets.[7] It is taken by mouth.[5]
Norgestrienone was first described in the literature in 1965.[10] It is sometimes referred to as a "second-generation" progestin.[13] Norgestrienone is no longer available.[citation needed]
Notes: Values are percentages (%). Reference ligands (100%) were progesterone for the PRTooltip progesterone receptor, testosterone for the ARTooltip androgen receptor, E2 for the ERTooltip estrogen receptor, DEXATooltip dexamethasone for the GRTooltip glucocorticoid receptor, aldosterone for the MRTooltip mineralocorticoid receptor, DHTTooltip dihydrotestosterone for SHBGTooltip sex hormone-binding globulin, and cortisol for CBGTooltip Corticosteroid-binding globulin. Sources:[14][15][16][17]
Pharmacokineticsedit
The metabolism of norgestrienone in humans has been studied.[18]
Norgestrienone was first described in the literature in 1965.[10] It is sometimes referred to as a "second-generation" progestin based on its time of introduction.[13]
Society and cultureedit
Generic namesedit
Norgestrienone is the generic name of the drug and its INNTooltip International Nonproprietary Name.[1][2][4] It is also known by its developmental code names RU-2010 and A-301.[1][2][4]
Brand namesedit
Norgestrienone has been marketed under the brand names Ogyline, Planor, and Miniplanor.[1][2][4]
Availabilityedit
Norgestrienone is no longer marketed and hence is no longer available in any country.[citation needed] It was previously used in France.[4] The medication was never marketed in the United States.[21]
^ abcdefElks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 887–. ISBN 978-1-4757-2085-3.
^ abcdeMorton IK, Hall JM (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 202–. ISBN 978-94-011-4439-1.
^Diaz S, Pavez M, Quinteros E, Diaz J, Robertson DN, Croxatto HB (October 1978). "Clinical trial with subdermal implants containing norgestrienone". Contraception. 18 (4): 429–440. doi:10.1016/0010-7824(78)90027-6. PMID 720075.
^ abcdefghIndex Nominum 2000: International Drug Directory. Taylor & Francis. January 2000. pp. 751–. ISBN 978-3-88763-075-1.
^ abcdSweetman SC, ed. (2009). "Sex hormones and their modulators". Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. p. 2122. ISBN 978-0-85369-840-1. Norgestrienone is a progestogen structurally related to norethisterone that has been used as an oral contraceptive. Typical doses have been 2 mg daily with an oestrogen, and 350 micrograms daily when used alone.
^McGuire JL (2000). Pharmaceuticals, 4 Volume Set. Wiley. p. 1580,1599. ISBN 978-3-527-29874-7.
^ abIARC Working Group on the Evaluation of Carcinogenic Risks to Humans; World Health Organization; International Agency for Research on Cancer (2007). Combined Estrogen-progestogen Contraceptives and Combined Estrogen-progestogen Menopausal Therapy. World Health Organization. pp. 455–. ISBN 978-92-832-1291-1.
^ abLoughney DA, Schwender CF (December 1992). "A comparison of progestin and androgen receptor binding using the CoMFA technique". Journal of Computer-Aided Molecular Design. 6 (6): 569–581. Bibcode:1992JCAMD...6..569L. doi:10.1007/bf00126215. PMID 1291626. S2CID 22004130.
^ abAxelrod J (1 January 1982). Biochemical Actions of Hormones. Academic Press. ISBN 978-0-12-452809-3.
^ abcdLauritzen C, Studd JW (22 June 2005). Current Management of the Menopause. CRC Press. pp. 45–. ISBN 978-0-203-48612-2.
^ abDi Giulio RT, Monosson E (6 December 2012). Interconnections Between Human and Ecosystem Health. Springer Science & Business Media. pp. 60–. ISBN 978-94-009-1523-7.
^ abcdRozenbaum H (March 1982). "Relationships between chemical structure and biological properties of progestogens". American Journal of Obstetrics and Gynecology. 142 (6 Pt 2): 719–724. doi:10.1016/S0002-9378(16)32477-2. PMID 7065053.
^ abWeiss G (February 1999). "Risk of venous thromboembolism with third-generation oral contraceptives: A review". American Journal of Obstetrics and Gynecology. 180 (2 Pt 2): 295–301. doi:10.1016/S0002-9378(99)70721-0. PMID 9988833.
^ abRaynaud JP, Bouton MM, Moguilewsky M, Ojasoo T, Philibert D, Beck G, et al. (January 1980). "Steroid hormone receptors and pharmacology". Journal of Steroid Biochemistry. 12: 143–157. doi:10.1016/0022-4731(80)90264-2. PMID 7421203.
^ abOjasoo T, Raynaud JP, Doé JC (January 1994). "Affiliations among steroid receptors as revealed by multivariate analysis of steroid binding data". The Journal of Steroid Biochemistry and Molecular Biology. 48 (1): 31–46. doi:10.1016/0960-0760(94)90248-8. PMID 8136304. S2CID 21336380.
^ abRaynaud J, Ojasoo T, Bouton M, Philibert D (1979). "Receptor Binding as a Tool in the Development of New Bioactive Steroids". Drug Design. Medicinal Chemistry: A Series of Monographs. Vol. 11. Academic Press. pp. 169–214. doi:10.1016/B978-0-12-060308-4.50010-X. ISBN 9781483216102.
^Raynaud JP (1970). "Metabolism of contraceptive steroids in man". Excerpta Medica International Congress Series. 219: 915–922. Archived from the original on 29 March 2018.
^Lavery JP, Sanfilippo JS (6 December 2012). Pediatric and Adolescent Obstetrics and Gynecology. Springer Science & Business Media. pp. 236–. ISBN 978-1-4612-5064-7.
^Gomel V, Brill A (27 September 2010). Reconstructive and Reproductive Surgery in Gynecology. CRC Press. pp. 90–. ISBN 978-1-84184-757-3.
^Lednicer D (4 March 2009). Strategies for Organic Drug Synthesis and Design. John Wiley & Sons. pp. 134–. ISBN 978-0-470-39959-0.
^Schearer SD (1978). The use of progestins and androgens as a male contraceptive. Hormonal control of male fertility. DHEW Publication No.(NIH). (Report). pp. 78–1097. Archived from the original on 29 March 2018.