Class | Examples | RE complex retention | Pharmacodynamic profile | Uterine effects |
---|---|---|---|---|
Short-acting (a.k.a. "weak" or "impeded") |
Estriol • 16-Epiestriol • 17α-Estradiol • ent-Estradiol • 16-Ketoestradiol • Dimethylstilbestrol • meso-Butestrol | Short (1–4 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 (6–24 hours) | Single or once-daily injections: full agonist | Early and late responses |
B. Clomifene • Nafoxidine • Nitromifene • Tamoxifen | Long (>24–48 hours) | Single injection: agonist Repeated injections: antagonist |
Early and late responses | |
Footnotes: a = Early responses occur after 0–6 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 6–48 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] |
Class | Examples | RE complex retention | Pharmacodynamic profile | Uterine effects |
---|---|---|---|---|
Short-acting (a.k.a. "weak" or "impeded") |
Estriol • 16-Epiestriol • 17α-Estradiol • ent-Estradiol • 16-Ketoestradiol • Dimethylstilbestrol • meso-Butestrol | Short (1–4 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 (6–24 hours) | Single or once-daily injections: full agonist | Early and late responses |
B. Clomifene • Nafoxidine • Nitromifene • Tamoxifen | Long (>24–48 hours) | Single injection: agonist Repeated injections: antagonist |
Early and late responses | |
Footnotes: a = Early responses occur after 0–6 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 6–48 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] |