Antiprogestins: Mechanism of action and contraceptive potential

Irving M. Spitz, Horacio B. Croxatto, Ann Robbins

Resultado de la investigación: Review article

69 Citas (Scopus)

Resumen

Antiprogestins are characterized by substitutions at the 11β and 17α positions of the steroid ring system and bind strongly to both progesterone and glucocorticoid receptors. Although they function predominantly as antiprogestins and antiglucocorticoids, on occasion they display progestin agonistic and even anti-estrogenic properties. The most common clinical use of the antiprogestin mifepristone is to induce a medical abortion in the early stages of pregnancy. Progesterone maintains the endometrium, transforming it from a proliferative to a secretory state. It also facilitates the luteinizing hormone surge, which initiates ovulation. As a consequence, antiprogestins may also have contraceptive potential. Although antiprogestins do delay ovulation, this effect is inconsistent unless high doses are given, and under these circumstances, the antiprogestin effect is associated with unopposed estrogen action on the endometrium. Very low doses of antiprogestins do not affect hormonal secretion or ovulation or alter bleeding patterns, but they do have contraceptive potential by inducing profound alterations in endometrial morphology. Mifepristone is also a very effective and safe postcoital agent. This new class of pharmacological agents has numerous other gynecological and obstetrical indications, such as endometriosis, uterine myoma, and expulsion of the fetus in the case of fetal death in utero. Antiprogestins may also be used in the treatment of steroid-dependent tumors. There are also therapeutic implications consequent to their antiglucocorticoid properties.

Idioma originalEnglish
Páginas (desde-hasta)47-81
Número de páginas35
PublicaciónAnnual Review of Pharmacology and Toxicology
Volumen36
EstadoPublished - 1996

Huella dactilar

Mifepristone
Contraceptive Agents
Ovulation
Action Potentials
Steroids
Endometrium
Glucocorticoid Receptors
Progestins
Progesterone Receptors
Luteinizing Hormone
Progesterone
Tumors
Myoma
Estrogens
Substitution reactions
Fetal Death
Endometriosis
Fetus
Pharmacology
Hemorrhage

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology

Citar esto

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Antiprogestins : Mechanism of action and contraceptive potential. / Spitz, Irving M.; Croxatto, Horacio B.; Robbins, Ann.

En: Annual Review of Pharmacology and Toxicology, Vol. 36, 1996, p. 47-81.

Resultado de la investigación: Review article

TY - JOUR

T1 - Antiprogestins

T2 - Mechanism of action and contraceptive potential

AU - Spitz, Irving M.

AU - Croxatto, Horacio B.

AU - Robbins, Ann

PY - 1996

Y1 - 1996

N2 - Antiprogestins are characterized by substitutions at the 11β and 17α positions of the steroid ring system and bind strongly to both progesterone and glucocorticoid receptors. Although they function predominantly as antiprogestins and antiglucocorticoids, on occasion they display progestin agonistic and even anti-estrogenic properties. The most common clinical use of the antiprogestin mifepristone is to induce a medical abortion in the early stages of pregnancy. Progesterone maintains the endometrium, transforming it from a proliferative to a secretory state. It also facilitates the luteinizing hormone surge, which initiates ovulation. As a consequence, antiprogestins may also have contraceptive potential. Although antiprogestins do delay ovulation, this effect is inconsistent unless high doses are given, and under these circumstances, the antiprogestin effect is associated with unopposed estrogen action on the endometrium. Very low doses of antiprogestins do not affect hormonal secretion or ovulation or alter bleeding patterns, but they do have contraceptive potential by inducing profound alterations in endometrial morphology. Mifepristone is also a very effective and safe postcoital agent. This new class of pharmacological agents has numerous other gynecological and obstetrical indications, such as endometriosis, uterine myoma, and expulsion of the fetus in the case of fetal death in utero. Antiprogestins may also be used in the treatment of steroid-dependent tumors. There are also therapeutic implications consequent to their antiglucocorticoid properties.

AB - Antiprogestins are characterized by substitutions at the 11β and 17α positions of the steroid ring system and bind strongly to both progesterone and glucocorticoid receptors. Although they function predominantly as antiprogestins and antiglucocorticoids, on occasion they display progestin agonistic and even anti-estrogenic properties. The most common clinical use of the antiprogestin mifepristone is to induce a medical abortion in the early stages of pregnancy. Progesterone maintains the endometrium, transforming it from a proliferative to a secretory state. It also facilitates the luteinizing hormone surge, which initiates ovulation. As a consequence, antiprogestins may also have contraceptive potential. Although antiprogestins do delay ovulation, this effect is inconsistent unless high doses are given, and under these circumstances, the antiprogestin effect is associated with unopposed estrogen action on the endometrium. Very low doses of antiprogestins do not affect hormonal secretion or ovulation or alter bleeding patterns, but they do have contraceptive potential by inducing profound alterations in endometrial morphology. Mifepristone is also a very effective and safe postcoital agent. This new class of pharmacological agents has numerous other gynecological and obstetrical indications, such as endometriosis, uterine myoma, and expulsion of the fetus in the case of fetal death in utero. Antiprogestins may also be used in the treatment of steroid-dependent tumors. There are also therapeutic implications consequent to their antiglucocorticoid properties.

KW - estradiol

KW - mifepristone

KW - onapristone

KW - progesterone

KW - receptors

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