Concentration-dependent mechanisms of ovulation inhibition by the progestin ST-1435. 1985

P L Lähteenmäki, and P Lähteenmäki

We summarize the hormonal profiles of women at different stages of inhibition of ovarian function during sustained-release subcutaneous treatment with a progestin, ST-1435. In the highest release group of ST-1435, a decrease in the luteinizing hormone (LH)follicle-stimulating hormone (FSH) ratio was found; and in spite of follicular phase levels of plasma FSH, inhibition of folliculogenesis, as judged by plasma estradiol (E2) concentrations below 60 pg/ml, occurred during the entire treatment period of 230 days. This may be indicative of a direct action of ST-1435 on the ovaries. When the average plasma concentration of ST-1435 decreased below 100 pg/ml, follicle development had started in most of the study subjects. At that time, the LH/FSH ratio had normalized to that found during the follicular phase of the normal menstrual cycle. In spite of the E2 rise during follicular development, no midcycle gonadotropin surges or subsequent elevations in plasma progesterone concentrations were found, thus indicating that the positive feedback action of E2 on gonadotropins was blocked by this progestin. We infer that the mechanism of inhibition of ovulation by sustained parenteral treatment with the progestin ST-1435 is concentration dependent, in such a manner that lower plasma concentrations of ST-1435 act on the hypothalamus and/or pituitary, whereas at higher plasma concentrations of ST-1435, a direct effect on the ovaries is also achieved.

UI MeSH Term Description Entries
D007986 Luteinizing Hormone A major gonadotropin secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR). Luteinizing hormone regulates steroid production by the interstitial cells of the TESTIS and the OVARY. The preovulatory LUTEINIZING HORMONE surge in females induces OVULATION, and subsequent LUTEINIZATION of the follicle. LUTEINIZING HORMONE consists of two noncovalently linked subunits, alpha and beta. Within a species, the alpha subunit is common in the three pituitary glycoprotein hormones (TSH, LH and FSH), but the beta subunit is unique and confers its biological specificity. ICSH (Interstitial Cell Stimulating Hormone),Interstitial Cell-Stimulating Hormone,LH (Luteinizing Hormone),Lutropin,Luteoziman,Luteozyman,Hormone, Interstitial Cell-Stimulating,Hormone, Luteinizing,Interstitial Cell Stimulating Hormone
D009652 Norpregnenes Pregnenes with one double bond or more than three double bonds which have undergone ring contractions or are lacking carbon-18 or carbon-19..
D009653 Norprogesterones Progesterones which have undergone ring contraction or which are lacking carbon 18 or 19.
D010060 Ovulation The discharge of an OVUM from a rupturing follicle in the OVARY. Ovulations
D011374 Progesterone The major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production. Progesterone, converted from PREGNENOLONE, also serves as an intermediate in the biosynthesis of GONADAL STEROID HORMONES and adrenal CORTICOSTEROIDS. Pregnenedione,Progesterone, (13 alpha,17 alpha)-(+-)-Isomer,Progesterone, (17 alpha)-Isomer,Progesterone, (9 beta,10 alpha)-Isomer
D011863 Radioimmunoassay Classic quantitative assay for detection of antigen-antibody reactions using a radioactively labeled substance (radioligand) either directly or indirectly to measure the binding of the unlabeled substance to a specific antibody or other receptor system. Non-immunogenic substances (e.g., haptens) can be measured if coupled to larger carrier proteins (e.g., bovine gamma-globulin or human serum albumin) capable of inducing antibody formation. Radioimmunoassays
D003271 Contraceptive Agents, Female Chemical substances or agents with contraceptive activity in females. Use for female contraceptive agents in general or for which there is no specific heading. Contraceptives, Female,Agents, Female Contraceptive,Female Contraceptive Agents,Female Contraceptives
D003692 Delayed-Action Preparations Dosage forms of a drug that act over a period of time by controlled-release processes or technology. Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004343 Drug Implants Small containers or pellets of a solid drug implanted in the body to achieve sustained release of the drug. Drug Implant,Drug Pellet,Pellets, Drug,Drug Pellets,Implant, Drug,Implants, Drug,Pellet, Drug

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