Inhibition of ovulation by intranasal nafarelin, a new superactive agonist of GnRH

Contraception. 1984 Aug;30(2):107-14. doi: 10.1016/0010-7824(84)90094-5.

Abstract

Thirty healthy female volunteers used a new superactive stimulatory analog of the hypothalamic gonadotropin-releasing hormone (GnRH) for inhibition of ovulation and contraception during 3 months. The potent GnRH agonist nafarelin (D-Nal(2)6-GnRH) was administered intranasally in a daily dose of 125 micrograms to 15 women and 250 micrograms to 15 women. The treatment inhibited ovulation in all women during the 89 months of therapy. No pregnancies occurred during 59 treatment months in which no additional contraceptives were used. The mean estradiol concentration decreased during the 3-month treatment within the normal range for the early to mid-follicular phase of the menstrual cycle. The results suggest that the GnRH agonist nafarelin has a potential for contraception by inhibition of ovulation in women.

PIP: 30 healthy female volunteers used a new superactive stimulatory anaog of the hypothalamic gonadotropin-releasing hormone (GnRH) for inhibition of ovulation and contraception over a 3 month period. The potent GnRH agonist nafarelin (D-Nal(2)6GnRH) was administered intranasally in a daily dose of 125 mcg to 15 women and 250 mcg to 15 women. The treatment inhibited ovulation in all women during the 89 months of therapy. No pregnancies occurred during 59 treatment months in which no additional contraceptives were used. The mean estradiol concentration decreased during the 3 months treatment within the normal range for the early to midfollicular phase of the menstrual cycle. Results suggest that the GnRH agonist nafarelin has potential for contraception because of its inhibition of ovulation in women.

MeSH terms

  • Administration, Intranasal
  • Adult
  • Contraceptives, Oral / therapeutic use*
  • Contraceptives, Oral, Synthetic / therapeutic use*
  • Dose-Response Relationship, Drug
  • Estradiol / blood
  • Female
  • Gonadotropin-Releasing Hormone / analogs & derivatives*
  • Gonadotropin-Releasing Hormone / therapeutic use
  • Humans
  • Menstruation / drug effects
  • Nafarelin
  • Ovulation / drug effects*
  • Pituitary Hormone-Releasing Hormones / therapeutic use*
  • Progesterone / blood

Substances

  • Contraceptives, Oral
  • Contraceptives, Oral, Synthetic
  • Pituitary Hormone-Releasing Hormones
  • Nafarelin
  • Gonadotropin-Releasing Hormone
  • Progesterone
  • Estradiol