Estradiol valerate/norethisterone enantate explained

Estradiol valerate/norethisterone enantate (EV/NETE), sold under the brand name Mesigyna among others, is a form of combined injectable birth control which is used to prevent pregnancy in women.[1] [2] It contains estradiol valerate (EV), an estrogen, and norethisterone enantate (NETE), a progestin. The medication is given once a month by injection into muscle.

EV/NETE is approved for use in at least 36 countries, and is the most widely used combined injectable contraceptive. It is available widely throughout Latin America, in a few Asian and African countries, and in Turkey.

Medical uses

EV/NETE is used as a combined injectable contraceptive to prevent pregnancy in women. It is given by intramuscular injection once a month.

Available forms

EV/NETE is available in the form of an oil solution containing 5 mg estradiol valerate (EV) and 50 mg norethisterone enantate (NETE).

Pharmacology

Pharmacodynamics

EV/NETE is a combination of EV, an estrogen, and NETE, a progestogen with weak androgenic activity.

Through its progestogenic activity, NETE has potent antigonadotropic effects and can inhibit fertility and suppress sex hormone levels. A single intramuscular injection of EV/NETE has been found to strongly suppress testosterone levels in men.[3] Levels of testosterone decreased from ~503 ng/dL at baseline to ~30 ng/dL at the lowest point (–94%) which occurred at day 7 post-injection.

Pharmacokinetics

Peak levels of estradiol after an intramuscular injection of EV/NETE (5 mg/50 mg) are reached within 2 days and range from 232 to 428 pg/mL.

History

EV/NETE, along with estradiol cypionate/medroxyprogesterone acetate (EC/MPA; code name HRP-112), was developed by the World Health Organization.[4] Both EV/NETE and EC/MPA became available in 1993.[5]

Society and culture

Generic names

EV/NETE is also known by its former developmental code name HRP-102.[6]

Brand names

EV/NETE has been marketed under a variety of brand names including Chinese Injectable No. 3, Effectimes, Ginediol, Mesigyna, Mesilar, Meslart, Mesocept, Mesygest, Nofertyl, Nofertyl Lafrancol, Noregyna, Norestrin, Norifam, Norigynon, Nostidyn, Sexseg, and Solouna.

Availability

EV/NETE has been marketed in at least 36 countries, including Argentina, the Bahamas, Barbados, Bolivia, Brazil, Chile, Colombia, Costa Rica, the Dominican Republic, Ecuador, Egypt, El Salvador, Ghana, Grenada, Guatemala, Guyana, Haiti, Honduras, Jamaica, Kenya, Mexico, Nicaragua, Panama, Paraguay, Peru, St. Lucia, Turkey, Uruguay, Venezuela, and Zimbabwe.[7] [8] [9] [10] [11] [12] [13] [14] [15] At least 15 of the countries in which EV/NETE is registered are Caribbean states. EV/NETE is the most widely used combined injectable contraceptive.

See also

Notes and References

  1. Sang GW . Pharmacodynamic effects of once-a-month combined injectable contraceptives . Contraception . 49 . 4 . 361–85 . April 1994 . 8013220 . 10.1016/0010-7824(94)90033-7 .
  2. Web site: MESIGYNA Solución Inyectable . www.farmaciasahumada.cl . 15 January 2022 . https://web.archive.org/web/20181118165202/https://www.farmaciasahumada.cl/fasa/MFT/PRODUCTO/P7747.HTM . 18 November 2018 . dead.
  3. MSc . Valle Alvarez . Doris del Cisne . Efecto de una Dosis de 50 mg de Enantato de Noretisterona y 5 mg de Valerato de Estradiol en los Niveles de Testosterona Total en Hombres Mexicanos Sanos . Effect of a Dose of 50 mg of Norethisterone Enanthate and 5 mg of Estradiol Valerate on Total Testosterone Levels in Healthy Mexican Men . 11 May 2011 . National Polytechnic Institute of Mexico .
  4. Hall PE . New once-a-month injectable contraceptives, with particular reference to Cyclofem/Cyclo-Provera . Int J Gynaecol Obstet . 62 . S43–56 . August 1998 . Suppl 1 . 9806239 . 10.1016/S0020-7292(98)00090-3 . 2826689 .
  5. d'Arcangues C . Once-a-month injectable contraceptives . World Health Forum . 14 . 4 . 439–40 . 1993 . 8185807 .
  6. Koetsawang S . Once-a-month injectable contraceptives: efficacy and reasons for discontinuation . Contraception . 49 . 4 . 387–98 . April 1994 . 8013221 . 10.1016/0010-7824(94)90034-5 .
  7. Web site: Norethisterone.
  8. Book: Sweetman, Sean C. . Sex hormones and their modulators . Martindale: The Complete Drug Reference . 36th . 2009 . 2082 . Pharmaceutical Press . London. 978-0-85369-840-1.
  9. Web site: Micromedex Products: Please Login.
  10. Book: IARC Working Group on the Evaluation of Carcinogenic Risks to Humans. International Agency for Research on Cancer. Hormonal Contraception and Post-menopausal Hormonal Therapy. 1 January 1999. IARC. 978-92-832-1272-0. 65. 17 September 2018. 28 August 2021. https://web.archive.org/web/20210828080855/https://monographs.iarc.who.int/wp-content/uploads/2018/06/mono72.pdf. dead.
  11. Bagade O, Pawar V, Patel R, Patel B, Awasarkar V, Diwate S . Increasing use of long-acting reversible contraception: safe, reliable, and cost-effective birth control . World J Pharm Pharm Sci . 3 . 10 . 364–392 . 2014 . 2278-4357 .
  12. Book: Pramilla Senanayake. Malcolm Potts. Atlas of Contraception, Second Edition. 14 April 2008. CRC Press. 978-0-203-34732-4. 50–.
  13. Newton JR, D'arcangues C, Hall PE . A review of "once-a-month" combined injectable contraceptives . J Obstet Gynaecol (Lahore) . 4 . S1–34 . 1994 . Suppl 1 . 12290848 . 10.3109/01443619409027641.
  14. Garza-Flores J . Pharmacokinetics of once-a-month injectable contraceptives . Contraception . 49 . 4 . 347–59 . April 1994 . 8013219 . 10.1016/0010-7824(94)90032-9 .
  15. Book: IARC Working Group on the Evaluation of Carcinogenic Risks to Humans. World Health Organization. International Agency for Research on Cancer. Combined Estrogen-progestogen Contraceptives and Combined Estrogen-progestogen Menopausal Therapy. 2007. World Health Organization. 978-92-832-1291-1. 431–.

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