Gestrinone

Gestrinone Uses, Dosage, Side Effects, Food Interaction and all others data.

Gestrinone, also known as ethylnorgestrienone, is a synthetic steroid of the 19-nortestosterone group that is marketed in Europe, Australia, and Latin America, though not the United States or Canada, and is used primarily in the treatment of endometriosis.

Gestrinone was developed in the early 1970s and was tested clinically as a weekly oral contraceptive in Europe and North America. Without significant advantages over other oral contraceptives and with its high cost, gestrinone was no longer used after the Stage II clinical trials. However, from 1982 this drug attracted increased interest due to significant therapeutic effects in the treatment endometriosis. Under different endocrine conditions, gestrinone possesses estrogenic, progestational, androgenic, antiestrogenic and antiprogesterone actions .

Gestrinone is a synthetic steroidal hormone which has androgenic, anti-estrogenic and anti-progestogenic properties . The findings of several studies suggest that gestrinone is as effective as danazol in the treatment of infertility associated with endometriosis and is better tolerated, in terms of adverse effects .

Gestrinone
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Gestrinone
Generic	Gestrinone
Gestrinone Other Names	Ethylnorgestrienone, Gestrinona, Gestrinone, Gestrinonum
Type
Formula	C₂₁H₂₄O₂
Weight	Average: 308.4141 Monoisotopic: 308.177630012
Groups	Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Endometriosis with or without accompanying sterility. Treatment is limited to a single course of 6 months duration per lifetime .

How Gestrinone works

Gestrinone has weak agonist activity on progesterone receptors in the rabbit endometrium and progesterone antagonist activity in various other pharmacological test systems. In addition, it has moderate agonist activity on prostatic androgen receptors in vitro. In several in vivo experiments, this activity was found to be low .

The primary action of gestrinone is on the hypothalamic-pituitary axis where it inhibits gonadotrophin release with a weak inhibitory effect on its synthesis. It also possesses anti-estrogen activity. The suppression of the ovular gonadotrophin peak is observed after the first month of treatment; the resulting decline in ovarian hormone secretion rapidly leads to endometrial atrophy. Aside from its central action, gestrinone also has anti-progesterone activity on cell receptors in both endometrium and extra-uterine ectopic implants. Gestrinone has no direct estrogen and/or uterotrophic effects .

A study was done to examine the efficacy of gestrinone in emergency contraception. The data from the study suggest that the mechanism of action of gestrinone used for the purposes of emergency contraception is likely the inhibition of implantation by acting on the endometrium as opposed to the inhibition of ovulation .

Toxicity

Many of gestrinone's adverse effects occur due to its androgenic activity. These effects include acne, seborrhea, hirsutism, weight gain and deepening of the voice. Most patients develop at least one adverse event while taking this drug. This is because the drug is embryotoxic in some animals and may also cause masculinization of a female fetus. Gestrinone significantly reduces HDL concentrations .

It is advisable to monitor liver transaminases and cholesterol levels in hyperlipidemic patients, as well as glucose in diabetic patients. Gestrinone has shown to decrease in the concentration of thyroid-binding globulin. Therefore, a decrease in serum total thyroxine levels is commonly observed. This is without clinical significance as free thyroxine levels and thyroid-stimulating hormone levels remain within the normal reference range .