Routes ofadministration Oral Metabolism Formula C22H30O3 Bioavailability 100% | ATC code G03FA16 (WHO) Biological half-life 13.8 hours Molar mass 342.472 g/mol Route Oral administration | |
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Trade names Ondeva, Totelle Sekvens Legal status In general: ℞ (Prescription only) | ||
Trimegestone how to pronounce it
Trimegestone (INN) (brand names Ondeva, Totelle Sekvens (both in combination with estrogen)) is a steroidal progestin of the 19-norprogesterone group related to promegestone which is marketed in Europe as a hormonal contraceptive and for use in hormonal replacement therapy for postmenopausal symptoms.
Contents
- Trimegestone how to pronounce it
- How to pronounce trimegestone
- Pharmacology
- Pharmacokinetics
- Chemistry
- History
- Brand names
- Availability
- References
How to pronounce trimegestone
Pharmacology
Trimegestone has very high affinity for the progesterone receptor, only weak affinity for the mineralocorticoid receptor, and little or no affinity for other steroid hormone receptors. In accordance, it is described as a very potent and pure progestogen, in fact the most potent progestin of the 19-norprogesterone group (clinically effective in endometriosis at only 0.1 mg/day), and possesses weak antimineralocorticoid activity and no androgenic, antiandrogenic, estrogenic, or glucocorticoid activity. Unlike progesterone, trimegestone does not metabolize into neurosteroids and hence does not influence GABAA receptor signaling or produce sedative side effects.
Pharmacokinetics
The oral bioavailability of trimegestone is 100%. Its elimination half-life is 13.8 hours. It is metabolized mainly via hydroxylation.
Chemistry
Trimegestone is a 19-norpregnane steroid and a derivative of 19-norprogesterone (19-norpregn-4-ene-3,20-dione) and 17α-methylprogesterone. It is also known as 21(S)-hydroxy-17α,21-dimethyl-9-dehydro-19-norprogesterone? or 21(S)-hydroxy-17α,21-dimethyl-19-norpregna-4,9-dien-3,20-dione?, as well as 17β-(S)-lactoyl-17α-methylestra-4,9-dien-3-one or 17β-((S)-2-hydroxypropanoyl)-17α-methylestra-4,9-dien-3-one.
Trimegestone is closely related structurally to the 19-norprogesterone and 17α-methylprogesterone derivatives demegestone and promegestone and is also known as 21-hydroxypromegestone. It is also related to the 19-norprogesterone derivatives gestonorone caproate, nomegestrol acetate, norgestomet, and segesterone acetate and to the 17α-methylprogesterone derivative medrogestone.
History
Trimegestone was first introduced in 2001.
Brand names
Trimegestone is marketed in combination with an estrogen under the brand names Ondeva and Totelle Sekvens.
Availability
Trimegestone is marketed in France and Sweden and possibly also in other European countries. It is not available in the United States.