Ethinyl Estradiol And Etonogestrel

Ethinyl Estradiol And Etonogestrel Uses, Dosage, Side Effects, Food Interaction and all others data.

Etonogestrel molecule is a 3-ketodesogestrel or 19-nortestosterone which is a synthetic biologically active metabolite of progestin desogestrel. The first product including etonogestrel was developed by the Merck subsidiary Organon and FDA approved in 2001.

Etonogestrel attains its therapeutic effect inhibiting fertility by impairing the release of the luteinizing hormone which is one of the most important reproductive hormones for ovulation. As well, etonogestrel is known to increase the viscosity of the cervical mucus hindering the passage of the spermatozoa and altering the lining in the uterus to prevent the implantation of the fertilized eggs in the endometrium.

In clinical trials, etonogestrel was implanted and reported to avoid 100% of pregnancies over a three year period. When the implant was removed, normal periods were reinstalled within 90 days in 91% of the individuals. Fertility was established quickly with 20 reported pregnancies within 3 months of implant removal.

Ethinyl Estradiol And Etonogestrel
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	Ethinyl Estradiol And Etonogestrel
Generic	Ethinyl estradiol + etonogestrel
Weight	0.015mg + 0.12mg/24hours,
Type	Vaginal Ring, Vaginal
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Etonogestrel is a long-acting synthetic derived progestin contraceptive used in various devices such as contraceptive rings and intradermal implants.

Etonogestrel is administered in subdermal implants as long-acting reversible contraception. It is known to be effective in postpartum insertion including breastfeeding women.

Etonogestrel is part of the long-acting contraceptive implants that prevent pregnancy. The implant's effect can remain for 5 years.

Ethinyl Estradiol And Etonogestrel is also used to associated treatment for these conditions: Contraception, Contraceptive implant therapy

How Ethinyl Estradiol And Etonogestrel works

Etonogestrel binds with high affinity to the progesterone and estrogen receptors in the target organs. From the target organs, they include the female reproductive tract, mammary gland, hypothalamus, and pituitary. Once bound, this drug changes the synthesis of different proteins which in order decreases the level of gonadotropin-releasing hormone and the luteinizing hormone.

Toxicity

The reported LD50 of oral etonogestrel in the rat is reported to be higher than 2000 mg/kg. Overdosage can only happen when more than one implant is inserted. In cases of overdose, removal of the implant is recommended.

There aren't reports relating etonogestrel with carcinogenesis, mutagenesis or impaired fertility.

Volume of Distribution

The apparent volume of distribution of etonogestrel is of around 201 L.

Elimination Route

Vaginal administration of etonogestrel is known to be significantly absorbed through the vaginal epithelium but it does not increase the levels of etonogestrel in the urine. On the other hand, oral administration is absorbed in the GI tract and it goes through the first-pass metabolism.

When etonogestrel is administered subdermally it is absorbed rapidly into the bloodstream and it presents a bioavailability of 82%. It is reported that the implant releases around 60 mcg per day in the first 3 months and then decreases steady reaching a concentration of 30 mcg at the end of year 2.