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%
Protein binding95%: Albumin (90%), CBGTooltip corticosteroid-binding globulin (3%), SHBGTooltip sex hormone-binding globulin (2%)
MetabolismHepatic (hydroxylation)
Elimination half-life35–36 hours
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
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. It is available both alone and in combination with an estrogen. It is taken by mouth.

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

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