| Class | Examples | RE complex retention | Pharmacodynamic profile | Uterine effects |
|---|---|---|---|---|
| Short-acting (a.k.a. "weak" or "impeded") |
Estriol ⢠16-Epiestriol ⢠17Îą-Estradiol ⢠ent-Estradiol ⢠16-Ketoestradiol ⢠Dimethylstilbestrol ⢠meso-Butestrol | Short (1â4 hours) | Single or once-daily injections: partial agonist or antagonist | Early responsesa |
| Implant or multiple injections per day: full agonist | Early and late responsesb | |||
| Long-acting | A. Estradiol ⢠Estrone ⢠Ethinylestradiol ⢠Diethylstilbestrol ⢠Hexestrol | Intermediate (6â24 hours) | Single or once-daily injections: full agonist | Early and late responses |
| B. Clomifene ⢠Nafoxidine ⢠Nitromifene ⢠Tamoxifen | Long (>24â48 hours) | Single injection: agonist Repeated injections: antagonist |
Early and late responses | |
| Footnotes: a = Early responses occur after 0â6 hours and include water imbibition, hyperemia, amino acid and nucleotide uptake, activation of RNA polymerases I and II, and stimulation of induced protein, among others. b = Late responses occur after 6â48 hours and include cellular hypertrophy and hyperplasia and sustained RNA polymerase I and II activity, among others. Sources: [1] [2] [3] [4] [5] [6] [7] | ||||
Template documentationSee also
References
- ^ Clark JH, Paszko Z, Peck EJ (January 1977). "Nuclear binding and retention of the receptor estrogen complex: relation to the agonistic and antagonistic properties of estriol". Endocrinology. 100 (1): 91â96. doi: 10.1210/endo-100-1-91. PMID 830547.
- ^ Clark JH, Hardin JW, McCormack SA (1979). "Mechanism of action of estrogen agonists and antagonists". Journal of Animal Science. 49 Suppl 2: 46â65. doi: 10.1093/ansci/49.supplement_ii.46. PMID 400777.
- ^ Lunan CB, Klopper A (September 1975). "Antioestrogens. A review". Clinical Endocrinology. 4 (5): 551â572. doi: 10.1111/j.1365-2265.1975.tb01568.x. PMID 170029. S2CID 9628572.
- ^ Rabe T, Runnebaum B, Kellermeier-Wittlinger S (1994). "Hormontherapie" [Hormone Therapy]. In Runnebaum B, Rabe T (eds.). Gynäkologische Endokrinologie und Fortpflanzungsmedizin: Band 1: Gynäkologische Endokrinologie [Gynecological Endocrinology and Reproductive Medicine: Volume 1: Gynecological Endocrinology]. pp. 63â147. doi: 10.1007/978-3-662-07635-4_3. ISBN 978-3-662-07635-4.
- ^ Clark JH, Markaverich BM (1983). "The agonistic and antagonistic effects of short acting estrogens: a review". Pharmacology & Therapeutics. 21 (3): 429â453. doi: 10.1016/0163-7258(83)90063-3. PMID 6356176.
- ^ Clark JH, Markaverich BM (April 1984). "The agonistic and antagonistic actions of estriol". Journal of Steroid Biochemistry. 20 (4B): 1005â1013. doi: 10.1016/0022-4731(84)90011-6. PMID 6202959.
- ^ Terenius L, Ljungkvist I (1972). "Aspects on the mode of action of antiestrogens and antiprogestogens". Gynecologic Investigation. 3 (1): 96â107. doi: 10.1159/000301746. PMID 4347201.
| Class | Examples | RE complex retention | Pharmacodynamic profile | Uterine effects |
|---|---|---|---|---|
| Short-acting (a.k.a. "weak" or "impeded") |
Estriol ⢠16-Epiestriol ⢠17Îą-Estradiol ⢠ent-Estradiol ⢠16-Ketoestradiol ⢠Dimethylstilbestrol ⢠meso-Butestrol | Short (1â4 hours) | Single or once-daily injections: partial agonist or antagonist | Early responsesa |
| Implant or multiple injections per day: full agonist | Early and late responsesb | |||
| Long-acting | A. Estradiol ⢠Estrone ⢠Ethinylestradiol ⢠Diethylstilbestrol ⢠Hexestrol | Intermediate (6â24 hours) | Single or once-daily injections: full agonist | Early and late responses |
| B. Clomifene ⢠Nafoxidine ⢠Nitromifene ⢠Tamoxifen | Long (>24â48 hours) | Single injection: agonist Repeated injections: antagonist |
Early and late responses | |
| Footnotes: a = Early responses occur after 0â6 hours and include water imbibition, hyperemia, amino acid and nucleotide uptake, activation of RNA polymerases I and II, and stimulation of induced protein, among others. b = Late responses occur after 6â48 hours and include cellular hypertrophy and hyperplasia and sustained RNA polymerase I and II activity, among others. Sources: [1] [2] [3] [4] [5] [6] [7] | ||||
Template documentationSee also
References
- ^ Clark JH, Paszko Z, Peck EJ (January 1977). "Nuclear binding and retention of the receptor estrogen complex: relation to the agonistic and antagonistic properties of estriol". Endocrinology. 100 (1): 91â96. doi: 10.1210/endo-100-1-91. PMID 830547.
- ^ Clark JH, Hardin JW, McCormack SA (1979). "Mechanism of action of estrogen agonists and antagonists". Journal of Animal Science. 49 Suppl 2: 46â65. doi: 10.1093/ansci/49.supplement_ii.46. PMID 400777.
- ^ Lunan CB, Klopper A (September 1975). "Antioestrogens. A review". Clinical Endocrinology. 4 (5): 551â572. doi: 10.1111/j.1365-2265.1975.tb01568.x. PMID 170029. S2CID 9628572.
- ^ Rabe T, Runnebaum B, Kellermeier-Wittlinger S (1994). "Hormontherapie" [Hormone Therapy]. In Runnebaum B, Rabe T (eds.). Gynäkologische Endokrinologie und Fortpflanzungsmedizin: Band 1: Gynäkologische Endokrinologie [Gynecological Endocrinology and Reproductive Medicine: Volume 1: Gynecological Endocrinology]. pp. 63â147. doi: 10.1007/978-3-662-07635-4_3. ISBN 978-3-662-07635-4.
- ^ Clark JH, Markaverich BM (1983). "The agonistic and antagonistic effects of short acting estrogens: a review". Pharmacology & Therapeutics. 21 (3): 429â453. doi: 10.1016/0163-7258(83)90063-3. PMID 6356176.
- ^ Clark JH, Markaverich BM (April 1984). "The agonistic and antagonistic actions of estriol". Journal of Steroid Biochemistry. 20 (4B): 1005â1013. doi: 10.1016/0022-4731(84)90011-6. PMID 6202959.
- ^ Terenius L, Ljungkvist I (1972). "Aspects on the mode of action of antiestrogens and antiprogestogens". Gynecologic Investigation. 3 (1): 96â107. doi: 10.1159/000301746. PMID 4347201.