Estradiol valerate/norethisterone enantate

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][3][4] It contains estradiol valerate (EV), an estrogen, and norethisterone enantate (NETE), a progestin.[1][2][3] The medication is given once a month by injection into muscle.[1][2][3]

Estradiol valerate /
norethisterone enantate
Estradiol valerate (top) and
norethisterone enantate (bottom)
Combination of
Estradiol valerateEstrogen
Norethisterone enantateProgestogen
Clinical data
Trade namesMesigyna, others
Other namesEV/NETE; HRP-102
Routes of
administration		Intramuscular injection
Identifiers
CAS Number
PubChem CID
UNII

EV/NETE is approved for use in at least 36 countries, and is the most widely used combined injectable contraceptive.[5][3] It is available widely throughout Latin America, in a few Asian and African countries, and in Turkey.[6][7][8]

Medical uses

EV/NETE is used as a combined injectable contraceptive to prevent pregnancy in women.[1][2][3] It is given by intramuscular injection once a month.[1][2][3]

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).[5][1][2][3]

Pharmacology

Pharmacodynamics
Hormone levels following a single intramuscular injection of EV/NETE (5 mg/50 mg) in healthy young men.[9] Testosterone levels were maximally suppressed by about 94%, to ~30 ng/dL, when measured at day 7.[9]

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.[9] 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.[9]

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.[4][1]

History

EV/NETE, along with estradiol cypionate/medroxyprogesterone acetate (EC/MPA; code name HRP-112), was developed by the World Health Organization.[5][10] Both EV/NETE and EC/MPA became available in 1993.[11]

Society and culture

Generic names

EV/NETE is also known by its former developmental code name HRP-102.[12]

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.[6][7][8][13][3][14][10][1][15]

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.[6][7][8][13][3][14][10][1][15] At least 15 of the countries in which EV/NETE is registered are Caribbean states.[5] EV/NETE is the most widely used combined injectable contraceptive.[5][3]

See also

References
  1. Garza-Flores J (April 1994). "Pharmacokinetics of once-a-month injectable contraceptives". Contraception. 49 (4): 347–59. doi:10.1016/0010-7824(94)90032-9. PMID 8013219.
  2. Sang GW (April 1994). "Pharmacodynamic effects of once-a-month combined injectable contraceptives". Contraception. 49 (4): 361–85. doi:10.1016/0010-7824(94)90033-7. PMID 8013220.
  3. Bagade O, Pawar V, Patel R, Patel B, Awasarkar V, Diwate S (2014). "Increasing use of long-acting reversible contraception: safe, reliable, and cost-effective birth control" (PDF). World J Pharm Pharm Sci. 3 (10): 364–392. ISSN 2278-4357.
  4. "MESIGYNA Solución Inyectable". www.farmaciasahumada.cl. Archived from the original on 18 November 2018. Retrieved 15 January 2022.
  5. Hall PE (August 1998). "New once-a-month injectable contraceptives, with particular reference to Cyclofem/Cyclo-Provera". Int J Gynaecol Obstet. 62 Suppl 1: S43–56. doi:10.1016/S0020-7292(98)00090-3. PMID 9806239. S2CID 2826689.
  6. "Norethisterone".
  7. Sweetman, Sean C., ed. (2009). "Sex hormones and their modulators". Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. p. 2082. ISBN 978-0-85369-840-1.
  8. "Micromedex Products: Please Login".
  9. Valle Alvarez, Doris del Cisne (11 May 2011). 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] (MSc). National Polytechnic Institute of Mexico.
  10. Newton JR, D'arcangues C, Hall PE (1994). "A review of "once-a-month" combined injectable contraceptives". J Obstet Gynaecol (Lahore). 4 Suppl 1: S1–34. doi:10.3109/01443619409027641. PMID 12290848.
  11. d'Arcangues C (1993). "Once-a-month injectable contraceptives". World Health Forum. 14 (4): 439–40. PMID 8185807.
  12. Koetsawang S (April 1994). "Once-a-month injectable contraceptives: efficacy and reasons for discontinuation". Contraception. 49 (4): 387–98. doi:10.1016/0010-7824(94)90034-5. PMID 8013221.
  13. IARC Working Group on the Evaluation of Carcinogenic Risks to Humans; International Agency for Research on Cancer (1 January 1999). Hormonal Contraception and Post-menopausal Hormonal Therapy (PDF). IARC. p. 65. ISBN 978-92-832-1272-0.
  14. Pramilla Senanayake; Malcolm Potts (14 April 2008). Atlas of Contraception, Second Edition. CRC Press. pp. 50–. ISBN 978-0-203-34732-4.
  15. IARC Working Group on the Evaluation of Carcinogenic Risks to Humans; World Health Organization; International Agency for Research on Cancer (2007). Combined Estrogen-progestogen Contraceptives and Combined Estrogen-progestogen Menopausal Therapy. World Health Organization. pp. 431–. ISBN 978-92-832-1291-1.
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