Etonogestrel

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.

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	Etonogestrel
Availability	Prescription only
Generic	Etonogestrel
Etonogestrel Other Names	3-Ketodesogestrel, 3-Oxodesogestrel, Etonogestrel, étonogestrel, Etonogestrelum
Related Drugs	norethindrone, levonorgestrel, medroxyprogesterone, Depo-Provera, Mirena, Nexplanon
Weight	68mg
Type	Intradermal, Subcutaneous Implant, Implant
Formula	C₂₂H₂₈O₂
Weight	Average: 324.4565 Monoisotopic: 324.20893014
Protein binding	Etonogestrel is highly bound to plasma proteins being mainly albumin followed by sex-hormone binding globulin. The protein bound form of the etonogestrel represents around 96-99% of the administered dose.
Groups	Approved, Investigational
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.

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

How 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.

Food Interaction

Administer vitamin supplements.
Avoid alcohol.
Limit caffeine intake.
Take at the same time every day.
Take with food.

[Moderate] MONITOR: Grapefruit juice may increase the plasma concentrations of orally administered drugs that are substrates of the CYP450 3A4 isoenzyme.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

Because grapefruit juice inhibits primarily intestinal rather than hepatic CYP450 3A4, the magnitude of interaction is greatest for those drugs that undergo significant presystemic metabolism by CYP450 3A4 (i.e., drugs with low oral bioavailability).

In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands.

Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.

Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict.

MANAGEMENT: Patients who regularly consume grapefruit or grapefruit juice should be monitored for adverse effects and altered plasma concentrations of drugs that undergo significant presystemic metabolism by CYP450 3A4.

Grapefruit and grapefruit juice should be avoided if an interaction is suspected.

Orange juice is not expected to interact with these drugs.

Etonogestrel Hypertension interaction

[Moderate] Estrogens and progestogens may cause fluid retention, particularly when given in high dosages or for prolonged periods.

Therapy with these agents should be administered cautiously in patients who have preexisting problems with excess fluid.

In addition, patients with conditions that may be adversely affected by fluid accumulation, such as asthma, epilepsy, migraine, and cardiovascular or renal dysfunction, should be observed for exacerbation of their condition during estrogen and

Etonogestrel Disease Interaction

Major: abnormal genital bleeding, hepatic neoplasms, breast malignancy, liver disease, thromboembolismModerate: depression, fluid retention, retinal thrombosis, gallbladder disease

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.