Trimegestone
Progestin | |
| ATC code | |
|---|---|
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | 100%[1] |
| Protein binding | 98% (to albumin)[2] |
| Metabolism | Mainly hydroxylation[2] |
| Elimination half-life | Range: 12–20 hours[3] Mean: 13.8–15.6 hours[2][4] |
| Identifiers | |
| |
JSmol) | |
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Trimegestone, sold under the brand names Ondeva and Totelle among others, is a
Trimegestone was first described in 1979 and was introduced for medical use in 2001.[9][10][11] It is sometimes described as a "fourth-generation" progestin.[12][13] The medication is marketed throughout Europe and Latin America.[14][6] It is not available in the United States or Canada.[15][14][6]
Medical uses
Trimegestone is used in
Available forms
Trimegestone is available both alone (as Ondeva) and in combination with estradiol (as Ginotex, Lovelle, Minique, Totelle), both of which are approved for the treatment of menopausal symptoms and prevention of postmenopausal osteoporosis.[7][17] Preparations of trimegestone are oral tablets and contain 0.1 to 0.5 mg of the medication.[18]
Side effects
The most common
Pharmacology
Pharmacodynamics
Trimegestone is a
In addition to its affinity for the PR, trimegestone has moderate affinity for the
The antiandrogenic potency of trimegestone in animals is about 30% of that of cyproterone acetate.[23]
Pharmacokinetics
The
Chemistry
Trimegestone, also known as 21(S)-hydroxy-17α,21-dimethyl-δ9-19-norprogesterone or as 21(S)-hydroxy-17α,21-dimethyl-19-norpregna-4,9-dien-3,20-dione, is a
History
Trimegestone was first described in 1979 and was introduced for medical use in 2001.
Society and culture
Generic names
Trimegestone is the
Brand names
Trimegestone under the brand names Ginotex, Lovelle, Lovelle Ciclico, Lovelle Continuo, Minique, Ondeva, Totelle, Totelle Ciclico, Totelle Ciclo, Totelle Continuo, Totelle Cycle, Totelle Cyclo, Totelle Secuencial, and Totelle Sekvens.[14][6][27][11][3][28] With the exception of Ondeva, which is formulated alone, all of these products are formulated in combination with estradiol.[14][6][27]
Availability
Trimegestone is or has been marketed in
Research
The oral combination of trimegestone and
References
- ^ ISBN 978-3-319-14385-9.
- ^ S2CID 24616324.
- ^ S2CID 27018468.
- ^ S2CID 39422122.
- ^ a b "Ethinylestradiol/trimegestone". AdisInsight. Springer Nature Switzerland AG.
- ^ a b c d e f g h i "Trimegestone".
- ^ a b c "Trimegestone". AdisInsight. Springer Nature Switzerland AG.
- ^ S2CID 20860088.
- ^ ISBN 9780444802033.
- ^ ISBN 978-0-12-397214-9.
- ^ ISBN 978-0-08-044514-4.
- S2CID 9543491.
- ISBN 978-1-107-43611-4.
- ^ a b c d e f "Micromedex Products: Please Login".
- ^ ISBN 978-1-60913-345-0.
- ^ ISBN 978-3-527-62330-3.
- ^ "Estradiol/trimegestone". AdisInsight. Springer Nature Switzerland AG.
- ISBN 978-0-203-49009-9.
- ^ S2CID 24893971.
- ^ PMID 10599548.
- ^ PMID 19434889.
- ^ a b c Kuhl H (2011). "Pharmacology of progestogens" (PDF). Journal für Reproduktionsmedizin und Endokrinologie-Journal of Reproductive Medicine and Endocrinology. 8 (Special Issue 1): 157–176.
- S2CID 23112620.
- ^ ISBN 978-0-412-46630-4.
- ISBN 978-0-323-15344-7.
- ^ ISBN 978-0-12-040537-4.
- ^ ISBN 978-0-85369-840-1.
- )
- ^ "Conjugated estrogens/trimegestone - Wyeth". AdisInsight. Springer Nature Switzerland AG.
- ^ "Estradiol/trimegestone transdermal patch - ProStrakan". AdisInsight. Springer Nature Switzerland AG.
Further reading
- Wahab M, Al-Azzawi F (September 2001). "Trimegestone: expanding therapeutic choices for the treatment of the menopause". Expert Opin Investig Drugs. 10 (9): 1737–44. S2CID 20860088.
- Winneker RC, Bitran D, Zhang Z (November 2003). "The preclinical biology of a new potent and selective progestin: trimegestone". Steroids. 68 (10–13): 915–20. S2CID 24893971.
- Grubb G, Spielmann D, Pickar J, Constantine G (November 2003). "Clinical experience with trimegestone as a new progestin in HRT". Steroids. 68 (10–13): 921–6. S2CID 40883746.
- Sitruk-Ware R, Bossemeyer R, Bouchard P (June 2007). "Preclinical and clinical properties of trimegestone: a potent and selective progestin". Gynecol. Endocrinol. 23 (6): 310–9. S2CID 39422122.