Medrogestone

Medrogestone
Clinical data
Trade namesColprone, others
Other namesMetrogestone; Medrogesterone; AY-62022, NSC-123018, R-13615; 6,17α-Dimethyl-6-dehydroprogesterone; 6,17α-Dimethyl-4,6-pregnadiene-3,20-dione
Pregnancy
category
  • X
Routes of
administration		By mouth
Drug classProgestogen; Progestin
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
BioavailabilityNearly 100%[1][2]
Protein binding95%: Albumin (90%), CBGTooltip corticosteroid-binding globulin (3%), SHBGTooltip sex hormone-binding globulin (2%)[2]
MetabolismHepatic (hydroxylation)[1]
Elimination half-life35–36 hours[3][4][5]
Identifiers
  • (8R,9S,10R,13S,14S,17S)-17-acetyl-6,10,13,17-tetramethyl-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-3-one
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.012.323 Edit this at Wikidata
Chemical and physical data
FormulaC23H32O2
Molar mass340.507 g·mol−1
3D model (JSmol)
  • O=C4\C=C3\C(=C/[C@@H]1[C@H](CC[C@@]2([C@@](C(=O)C)(CC[C@@H]12)C)C)[C@@]3(C)CC4)C
  • InChI=1S/C23H32O2/c1-14-12-17-18(21(3)9-6-16(25)13-20(14)21)7-11-23(5)19(17)8-10-22(23,4)15(2)24/h12-13,17-19H,6-11H2,1-5H3/t17-,18+,19+,21-,22-,23+/m1/s1
  • Key:HCFSGRMEEXUOSS-JXEXPEPMSA-N

Medrogestone, sold under the brand name Colprone among others, is a progestin medication which has been used in menopausal hormone therapy and in the treatment of gynecological disorders.[6][2] It is available both alone and in combination with an estrogen.[7] It is taken by mouth.[2][8]

Medrogestone is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone.[2] It has weak antiandrogenic, glucocorticoid, and antimineralocorticoid activity and no other important hormonal activity.[2][1][9][10] Due to its progestogenic activity, medrogestone has antigonadotropic effects.[1][2]

Medrogestone was described as early as 1963 and was introduced for medical use by at least 1966.[11][12][9] It has mostly been discontinued and remains available only in a few countries.[13][7]

  1. ^ a b c d Schindler AE, Campagnoli C, Druckmann R, Huber J, Pasqualini JR, Schweppe KW, Thijssen JH (December 2003). "Classification and pharmacology of progestins" (PDF). Maturitas. 46 (Suppl 1): S7–S16. doi:10.1016/j.maturitas.2003.09.014. PMID 14670641.[permanent dead link]
  2. ^ a b c d e f g Kuhl H (2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric. 8 (Suppl 1): 3–63. doi:10.1080/13697130500148875. PMID 16112947. S2CID 24616324.
  3. ^ Stanczyk FZ (2002). "Pharmacokinetics and potency of progestins used for hormone replacement therapy and contraception". Reviews in Endocrine & Metabolic Disorders. 3 (3): 211–24. doi:10.1023/A:1020072325818. PMID 12215716. S2CID 27018468. Medrogestone The pharmacokinetics of medrogestone (5 mg dose) was studied in 12 Chinese young males who received a single oral dose of this drug [20]. The mean ± standard deviation Cmax was 8.21 ± 2.78 ng/ml and Tmax was 2.57 ± 1.02; the half-life of elimination was 34.9 ± 17.0 hours.
  4. ^ Lobo R, Crosignani P, Paoletti R, Bruschi F (6 December 2012). Women's Health and Menopause: New Strategies — Improved Quality of Life. Springer Science & Business Media. pp. 142–. ISBN 978-1-4615-1061-1.
  5. ^ Stanczyk FZ, Hapgood JP, Winer S, Mishell DR (April 2013). "Progestogens used in postmenopausal hormone therapy: differences in their pharmacological properties, intracellular actions, and clinical effects". Endocrine Reviews. 34 (2): 171–208. doi:10.1210/er.2012-1008. PMC 3610676. PMID 23238854.
  6. ^ Cite error: The named reference MortonHall1999 was invoked but never defined (see the help page).
  7. ^ a b Cite error: The named reference Drugs.com was invoked but never defined (see the help page).
  8. ^ Cutler WB, Garcia CR (1993). Menopause: A Guide for Women and Those who Love Them. Norton. pp. 134–. ISBN 978-0-393-30995-9.
  9. ^ a b Cite error: The named reference ReveszChappel1966 was invoked but never defined (see the help page).
  10. ^ Cite error: The named reference pmid4105445 was invoked but never defined (see the help page).
  11. ^ Cite error: The named reference Elks2014 was invoked but never defined (see the help page).
  12. ^ Cite error: The named reference DeghenghiLefebvre1963 was invoked but never defined (see the help page).
  13. ^ Cite error: The named reference IndexNominum2000 was invoked but never defined (see the help page).