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Etonogestrel


Drug Approvals

(British Approved Name, US Adopted Name, rINN)

Synonyms: 3-keto-Desogestrel; Etonogestreeli; Etonogestrel; Etonogestrelum; Org-3236
BAN: Etonogestrel
USAN: Etonogestrel
INN: Etonogestrel [rINN (en)]
INN: Etonogestrel [rINN (es)]
INN: Étonogestrel [rINN (fr)]
INN: Etonogestrelum [rINN (la)]
INN: Етоногестрел [rINN (ru)]
Chemical name: 13-Ethyl-17-hydroxy-11-methylene-18,19-dinor-17α-pregn-4-en-20-yn-3-one; 17β-Hydroxy-11-methylene-18-homo-19-nor-17α-pregn-4-en-20-yn-3-one
Molecular formula: C22H28O2 =324.5
CAS: 54048-10-1
ATC code: G03AC08
Read code: y0CwW

Adverse Effects and Precautions

As for progestogens in general (see Progesterone). See also under Hormonal Contraceptives.

Breast feed ing. Etonogestrel was found in the breast milk of 42 women given a contraceptive etonogestrel implant. Over the 4-month study, compared with a group who used an intra-uterine non-hormonal device, etonogestrel did not affect the volume or composition of breast milk, or the growth of the breast-fed infants. At 3 years of age there was no difference in growth between these 2 groups of children.

Vaginal bleeding. Prolonged vaginal bleeding, lasting from 2 to 26 weeks, has been reported with the use of etonogestrel sub-dermal implants. Blood transfusion was needed in the management of one patient. Heavy bleeding has been described in 2 women after the implant had broken while in place.

Interactions

As for progestogens in general (see Progesterone). See also under Hormonal Contraceptives.

Pharmacokinetics

Etonogestrel is highly bound to plasma proteins about 32% is bound to sex hormone binding globulin and 66% to albumin. It is metabolised by the cytochrome P450 isoenzyme CYP3A4, and both metabolites and unchanged drug are excreted in the urine and faeces. The elimination half-life is about 25 to 30 hours. Etonogestrel is distributed into breast milk.

Uses and Administration

Etonogestrel, the active metabolite of desogestrel, is used as a hormonal contraceptive. A subdermal implant containing 68 mg of etonogestrel is used as a progestogenonly contraceptive that is effective for 3 years. Etonogestrel is also used as the progestogen component of a combined contraceptive delivered via a vaginal ring device. The ring releases an average of 120 micrograms daily of etonogestrel and 15 micrograms daily of ethinylestradiol and remains in the vagina for 3 weeks it is then removed for a one-week break after which a new ring is inserted.

Etonogestrel is under investigation as a male contraceptive, given orally or by implant, with testosterone implants or injections.

Preparations

Proprietary Preparations

Argentina: lmplanon

Australia:: Implanon

Austria: Implanon

Belgium: Implanon

Brazil: Implanon

Chile: Implanon

Czech Republic: Implanon

Denmark: Implanon

Finland: Implanon

France: Implanon

Germany: Implanon

Greece: Implanon

Hungary: Implanon

Indonesia: Implanon

Italy: Implanon

Malaysia: Implanon

Mexico: Implanon

Norway: Implanon

Portugal: Implanon

Singapore: Implanon

Spain: Implanon

Sweden: Implanon

Switzerland: Implanon

Thailand: Implanon

Turkey: Implanon

UK: Implanon

USA: Implanon

Venezuela: Implanon

Multi-ingredient

Australia: NuvaRing

Austria: NuvaRing

Belgium: NuvaRing

Brazil: NuvaRing

Canada: NuvaRing

Chile: NuvaRing

Czech Republic: NuvaRing

Denmark: NuvaRing

Finland: NuvaRing

France: NuvaRing

Germany: NuvaRing

Greece: NuvaRing

Hungary: NuvaRing

Italy: NuvaRing

Mexico: NuvaRing

The Netherlands: NuvaRing

Norway: NuvaRing

Portugal: NuvaRing

Russia: NuvaRing

Spain: NuvaRing

Sweden: NuvaRing

Switzerland: NuvaRing

USA: NuvaRing

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