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PubMed1995

[Vaginal and intrauterine contraception].

Vaginal contraception (condom, diaphragm and spermicide in pessary, tablet, jelly, cream, or sponge form) have been little used in France and generally in Europe since the advent of modern contraception with "the pill" and the intrauterine contraceptive device. The former methods, when properly used, are nevertheless both effective and useful, at least as interim measures. In addition, the protection they afford against sexually transmitted diseases and, for the condom, against HIV, is not negligible. Finally, the "barrier" methods of contraception such as the diaphragm and the condom afford significant protection against cancer of the cervix. The intrauterine contraceptive device (IUCD), used in France by 14% of women between 15 and 49 years of age and by 90 million women throughout the world for whom it is the main reversible means of contraception, have a mechanism of action that is still not fully understood. Most IUCD now used are made of copper. There are also diffusion IUCD based on progesterone or a synthetic progestational hormone which are useful in case of anaemia, menorrhagia or dysmenorrhea.

Administration, Intravaginal↗
PubMed1984

Role of ovarian steroid hormones in the regulation of adenylate cyclase during early progestation.

The hormonal regulation of uterine adenylate cyclase (AC) was measured in the rat by radiochemical analysis. Animals made pseudopregnant by cervical stimulation were ovariectomized on Day 1 (the first appearance of leukocytes in the vaginal smear) and injected for 6 days with sesame oil, 0.1-10.0 micrograms estrone, 2.0 mg progesterone, or 1.0 microgram estrone + 2.0 mg progesterone. AC activity in ovariectomized controls remained at basal levels (2.8-3.3 pmol cAMP formed/min X mg protein). The injection of progesterone did not alter AC activity significantly, but estrone increased AC activity during Days 3-5, and the response (5-17 pmol) was dose dependent. The action of estrone was not inhibited by progesterone. The present experiments revealed: a) AC from estrone-treated rats was activated 2- to 4-fold by 10 mM NaF; b) following treatment with estrone + progesterone, AC was activated 2- to 3-fold by a trauma to the uterus; c) unlike the response to fluoride, the effect of trauma was temporally limited to Day 4; and d) when AC was activated by trauma, no further increase was elicited by NaF. The data indicated that the transient sensitivity of AC to activation by trauma on Day 4 in E+P-treated rats was identical to that in intact rats and paralleled the normal timing of uterine sensitivity to decidual induction.

Adenylyl Cyclases↗
PubMed1990

Evidence for "memory" of cervical stimulation for the promotion of pregnancy in rats.

Successful pregnancy in the female rat depends upon two sets of physiological events: (1) transport of gametes (sperm and egg) through the reproductive tract so that fertilization can be effected and (2) establishment of an appropriate hormonal environment (progestational state) so that the fertilized egg can implant in the uterus and be maintained during subsequent gestation. This study highlights the independence of the mechanisms controlling the gametic and hormonal aspects of pregnancy by temporally separating the introduction of sperm into the female from the stimulation that triggers the progestational hormonal response. The progestational state was initiated by electrical stimulation of the cervix, and sperm was introduced directly into the uterus by artificial insemination. Although these two events were separated by up to 3 days, pregnancy could ensue. Cervical stimulation, normally a consequence of male intromission behavior, establishes a condition in the central nervous system, a "memory" that signals the probable induction of pregnancy. Without this "memory," animals with a short estrous cycle would continue to cycle after mating, thereby producing a hormonal environment incompatible with implantation. The "memory" is manifested by daily surges of prolactin irrespective of fertilization. This is the first physiological demonstration that a "memory" of cervical stimulation can be called upon to support a viable pregnancy.

Animals↗
PubMed1976

Systems approach to vaginal delivery of drugs III: Simulation studies interfacing steroid release from silicone matrix and vaginal absorption in rabbits.

A composite physical model involving the simultaneous receding boundary release of drug from a drug suspension-silicone polymer matrix system, diffusion across the aqueous layer, and passive transport across the vaginal membrane consisting of parallel lipoidal and aqueous pore pathways is described. Simulation studies with progesterone and hydrocortisone illustrate matrix release-limiting, membrane absorption, and aqueous diffusion layer-limiting cases when the cylindrical silicone delivery device is interfaced with the vaginal membrane of the rabbit.

Cell Membrane↗
PubMed1975

The absolute configuration of the enantiomers of glutethimide and aminoglutethimide.

Aminoglutethimide (Elipten¿ CIBA) was resolved into the optical antipodes I and II. The endocrinological properties and the absolute configuration of both enantiomers I and II were determined. Most of the steroidal synthesis inhibition was found in the (+) enantiomer II. On the basis of circular dichroism, the R-configuration was assigned to the (+) enantiomer II.

Adrenal Glands↗
PubMed1985

Plasma levonorgestrel and progesterone levels in women treated with silastic covered rods containing levonorgestrel.

Levonorgestrel and progesterone plasma levels were measured in women bearing levonorgestrel subdermal implants. Two groups using four or six levonorgestrel covered rods and one group of non-hormonal contraceptors were compared. Blood samples were drawn twice a week for six consecutive weeks at different intervals after treatment administration. The mean levonorgestrel levels (mean +/- S.D.) observed in the four rods group was .49 +/- .13 ng/ml in the first year and decreased to .34 +/- .06 in the fifth year of treatment. The mean values observed in the six rods group were .70 +/- .15 ng/ml in the second year and .43 +/- .11 in the sixth year. The levonorgestrel plasma levels were slightly above those found with Norplantr implants in the four rods group and well above it in the six rod group. The highest plasma progesterone value found in each sampling period was above 9 nmol/l in 7 (14%) out of 50 subjects in the four rods group, in 2 (4.3%) out of 47 subjects in the six rods group and in all the 49 control women. In 4 out of the 7 subjects from the 4 rods group and in the two subjects from the 6 rods group, the highest progesterone value was preceded and followed by values lower than 6 nmol/l. It was concluded that the progesterone levels were seldom compatible with the occurrence of ovulation in women treated with four or six levonorgestrel covered rods which release an estimated daily dose of 70 and 105 micrograms, respectively.

Adolescent↗
PubMed1988

Termination of early pregnancy by a single dose of mifepristone (RU 486), a progesterone antagonist.

Mifepristone (RU 486) is a new steroid which is a progesterone antagonist and which is able to interrupt early pregnancy without any major side-effects. The purpose of our study was to evaluate the clinical effect of a single oral dose of 600 mg on early pregnancy. The study included 150 healthy women applying for a legal abortion with an amenorrhea of no more than 42 days. Pregnancy was confirmed by clinical and ultrasound examination and plasma HCG assessment. Success was assumed by repeating these exams on the eighth day. 131 patients had a complete abortion (87.3%), with a very few side-effects. Only two patients needed curettage for heavy bleeding. Mifepristone is able to terminate early pregnancy by an easy ambulatory method under medical supervision.

Abortifacient Agents↗
PubMed1988

Antiprogestins.

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Abortifacient Agents↗