Combination drug
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]
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
^
a
b
c
d
e
f
g
h
i 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 .
^
a
b
c
d
e
f 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 .
^
a
b
c
d
e
f
g
h
i
j 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 .
^
a
b
"MESIGYNA Solución Inyectable" . www.farmaciasahumada.cl . Archived from
the original on 18 November 2018. Retrieved 15 January 2022 .
^
a
b
c
d
e 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 .
^
a
b
c
"Norethisterone" .
^
a
b
c 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 .
^
a
b
c
"Micromedex Products: Please Login" .
^
a
b
c
d Valle Alvarez Dd (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.
^
a
b
c 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 .
^ d'Arcangues C (1993). "Once-a-month injectable contraceptives". World Health Forum . 14 (4): 439–40.
PMID
8185807 .
^ 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 .
^
a
b 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 . Archived from
the original (PDF) on 28 August 2021. Retrieved 17 September 2018 .
^
a
b Pramilla Senanayake, Malcolm Potts (14 April 2008).
Atlas of Contraception, Second Edition . CRC Press. pp. 50–.
ISBN
978-0-203-34732-4 .
^
a
b 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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