Medrogestone

Medrogestone
Clinical data

Trade names	Colprone, others
Pregnancy category	X
Routes of administration	By mouth
ATC code	G03DB03 (WHO) G03FB07 (WHO) (with estrogen)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	Nearly 100%
Protein binding	95%: Albumin (90%), CBG (3%), SHBG (2%)
Metabolism	Hepatic (hydroxylation)
Biological half-life	35–36 hours
Identifiers
IUPAC name (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
Synonyms	Metrogestone; Medrogesterone; AY-62022, NSC-123018, R-13615; 6,17α-Dimethyl-6-dehydroprogesterone; 6,17α-Dimethyl-4,6-pregnadiene-3,20-dione
CAS Number	977-79-7
PubChem CID	9949848
DrugBank	DB09124
ChemSpider	8125459
UNII	077DN93G5B
KEGG	D04885
ECHA InfoCard	100.012.323
Chemical and physical data
Formula	C₂₃H₃₂O₂
Molar mass	340.5 g/mol
3D model (Jmol)	Interactive image
SMILES 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 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:StdInChI

Medrogestone (INN, USAN, BAN) (brand name Colprone) is a steroidal progestin related to progesterone that is used in hormone replacement therapy for menopausal symptoms and in the treatment of gynecological disorders.

In the past, medrogestone was used in the treatment of endometrial cancer and in some regimens for breast cancer, and, in men, for benign prostatic hyperplasia. It still finds use in the treatment of amenorrhea and as the progestin component in certain forms of menopausal hormone replacement therapy.

Cyclic treatment with low-dose (10 mg/day) medrogestone has been found to be effective in the treatment of fibrocystic breast changes and associated mastodynia (breast pain).

Intrahepatic cholestasis of pregnancy (acute or in history), vaginal bleeding of unknown origin, and severe diseases of the liver such as tumors are absolute contraindications for medrogestone, as are thrombotic events such as thrombophlebitis or stroke. Relative contraindications include a history of jaundice or itching in pregnancy or gestational pemphigoid.

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Wikipedia