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Details

Stereochemistry ABSOLUTE
Molecular Formula C22H30O2
Molecular Weight 326.4724
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PROMEGESTONE

SMILES

[H][C@@]12CC[C@](C)(C(=O)CC)[C@@]1(C)CCC3=C4CCC(=O)C=C4CC[C@@]23[H]

InChI

InChIKey=QFFCYTLOTYIJMR-XMGTWHOFSA-N
InChI=1S/C22H30O2/c1-4-20(24)22(3)12-10-19-18-7-5-14-13-15(23)6-8-16(14)17(18)9-11-21(19,22)2/h13,18-19H,4-12H2,1-3H3/t18-,19+,21+,22-/m1/s1

HIDE SMILES / InChI

Description

Promegestone (R 5020) is a potent progestin devoid of androgenic side-effects and has marked anti-estrogenic activity. Promegestone is an AChR noncompetitive antagonist that may alter AChR function by interactions at the lipid-protein interface. Promegestone is used in the treatment of gynecological disorders due to luteal insufficiency.

Approval Year

PubMed

Sample Use Guides

In Vivo Use Guide
The daily dosage in luteal insufficiency is usually 0.125 mg to 0.500 mg daily in a single dose from the 16th to the 25th day of the cycle. In the replacement therapy for menopause, isolated estrogen therapy is not recommended (risk of endometrial hyperplasia). In this case, the promégestone must be prescribed for the last 12 days of each therapeutic sequence, followed by an interruption of any replacement treatment lasting approximately one week, during which it is usual to observe a withdrawal haemorrhage. The effective dosage varies from one subject to another. It is usually 0.250 mg to 0.500 mg / day in a single dose. It should be adjusted individually according to the clinical presentation, the dose of estrogen used and the patient's response.
Route of Administration: Oral