Gestrinonum

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

Gestrinonum, 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.

Gestrinonum 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 .

Gestrinonum 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 .

Trade Name Gestrinonum
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
Gestrinonum
Gestrinonum

Uses

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

How Gestrinonum works

Gestrinonum 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. Gestrinonum 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. Gestrinonum significantly reduces HDL concentrations .

It is advisable to monitor liver transaminases and cholesterol levels in hyperlipidemic patients, as well as glucose in diabetic patients. Gestrinonum 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 .

Volume of Distribution

67 L

Elimination Route

The oral absorption of gestrinone is 30% ±30 .

Half Life

Plasma half-life is 24 hr .

Clearance

Renal Excretion accounts for < 1 % .

Elimination Route

About 40-45% of a dose is excreted in the urine and 30-35% in the feces .

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