Estradiol cypionate/medroxyprogesterone acetate explained

Estradiol cypionate/medroxyprogesterone acetate (EC/MPA), sold under the brand name Cyclofem among others, is a form of combined injectable birth control. It contains estradiol cypionate (EC), an estrogen, and medroxyprogesterone acetate (MPA), a progestin.[1] It is recommended for short-term use and is given once a month by injection into a muscle.[2]

Common side effects of EC/MPA include irregular menstrual periods which typically improves with time.[2] Other side effects include blood clots, headache, hair loss, depression, nausea, and breast pain.[2] [3] Use during pregnancy is not recommended.[1] Use during breastfeeding is likely safe.[4] It works mainly by preventing ovulation.[1]

EC/MPA came into medical use in 1993 with approval in the United States in 2000.[1] It is on the World Health Organization's List of Essential Medicines.[5] [6] The medication is approved for use in 18 countries.[7] It is used in Mexico, Thailand, and Indonesia, among other countries.[8] It is no longer commercially available in the United States.[1]

Medical uses

EC/MPA is used as a once-monthly combined injectable contraceptive to prevent pregnancy in women.

Available forms

EC/MPA is available in the form of a microcrystalline aqueous suspension of 5 mg EC and 25 mg MPA given in a 0.5 mL aqueous solution for intramuscular injection once per month. It is provided in the form of single-dose vials and ampoules. The particle sizes of the formulation are 93% within a range of 5 to 16 μm.[9]

History

Depot MPA (DMPA) and EC/MPA were developed by Upjohn in the 1960s.[10] [11] DMPA (brand name Depo-Provera) was introduced for use as a progestogen-only injectable contraceptive for the first time outside of the United States in 1969 and was subsequently approved for use in birth control in the United States in 1992.[12] [13] A variety of preliminary studies on EC/MPA as a contraceptive were published between 1968 and 1978.[14] [15] In the late 1970s, the World Health Organization (WHO) began an initiative known as the Special Programme of Research, Development and Research Training in Human Reproduction (WHO/HRP) to develop combined injectable contraceptives as part of its efforts to increase the availability and choices of birth control for women and men throughout the world. They sought to remedy the side effect of menstrual irregularity that is the major reason for discontinuation of progestogen-only injectable contraceptives like DMPA via incorporation of an estrogen.[16] Funding for the initiative was provided by the United Nations Development Programme (UNDP), United Nations Population Fund (UNFPA), and World Bank.

In 1980, the WHO conducted a pharmacokinetic study of estradiol cypionate, estradiol valerate, and estradiol benzoate to determine which ester(s) would be most suitable for use in combined injectable contraceptives.[17] Following the initial development of the medication by Upjohn under the code name Cyclo-Provera previously, EC/MPA was developed as a combined injectable contraceptive by the World Health Organization under the code name HRP-112 in the 1980s and early 1990s. The WHO also developed estradiol valerate/norethisterone enantate (code name HRP-102) as a combined injectable contraceptive. Development of EC/MPA was completed by the early 1990s and the medication was licensed to the WHO/HRP-established Concept Foundation as well as several pharmaceutical companies. EC/MPA was introduced for use as a combined injectable contraceptive under the brand name Cyclofem and others in Mexico, Thailand, and Indonesia in 1993.[18] It was available in 18 countries, mostly in Latin America and Asia, by 1998. In late 2000, EC/MPA was introduced for use as a combined injectable contraceptive by Upjohn under the brand name Lunelle in the United States. However, the formulation was discontinued in the United States in late 2003.[19]

Society and culture

Generic names

EC/MPA was originally known as Cyclo-Provera (or Cycloprovera), and is also known by its former developmental code name HRP-112.[20]

Brand names

Brand names of EC/MPA include Ciclofem, Ciclofemina, Cyclofem, Cyclofemina, Cyclogeston, Femelin, Femydrol, Gestin, Harmonis, Lunella, Lunelle, and Novafem.[21] [22]

Availability

EC/MPA has been approved for use in at least 18 countries. It is or has been used in Bolivia, Brazil, Chile, China, Colombia, Costa Rica, the Dominican Republic, Ecuador, El Salvador, Guatemala, Hong Kong, Indonesia, Malaysia, Mexico, Panama, Peru, Thailand, the United States, and Zimbabwe, among other countries.[23] [24] [25] [8] [26] [27] The medication is no longer available in the United States.[1]

See also

Notes and References

  1. Web site: Estradiol and medroxyprogesterone Intramuscular Advanced Patient Information - Drugs.com. www.drugs.com. 1 January 2017. live. https://web.archive.org/web/20170101232611/https://www.drugs.com/cons/estradiol-and-medroxyprogesterone-intramuscular.html. 1 January 2017.
  2. Book: WHO Model Formulary 2008 . 2009 . 9789241547659 . ((World Health Organization)) . Stuart MC, Kouimtzi M, Hill SR . 10665/44053 . World Health Organization . World Health Organization . free . 368–370 .
  3. Web site: Estradiol/medroxyprogesterone Side Effects in Detail - Drugs.com. www.drugs.com. 1 January 2017. live. https://web.archive.org/web/20170101232100/https://www.drugs.com/sfx/estradiol-medroxyprogesterone-side-effects.html. 1 January 2017.
  4. Web site: Estradiol / medroxyprogesterone (Lunelle) Use During Pregnancy. www.drugs.com. 1 January 2017. live. https://web.archive.org/web/20170101231526/https://www.drugs.com/pregnancy/estradiol-medroxyprogesterone.html. 1 January 2017.
  5. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 21st list 2019 . 2019 . 10665/325771 . World Health Organization . World Health Organization . Geneva . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO . free .
  6. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 22nd list (2021) . 2021 . 10665/345533 . World Health Organization . World Health Organization . Geneva . WHO/MHP/HPS/EML/2021.02 . free .
  7. 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 . 2018-08-02 . https://web.archive.org/web/20170810000242/http://www.wjpps.com/download/article/1412071798.pdf . 2017-08-10 . dead .
  8. Book: Senanayake P, Potts M . Hormonal Contraception . Atlas of Contraception . Second . 2008 . CRC Press . 9780203347324. 51 . https://books.google.com/books?id=7dDKBQAAQBAJ&pg=PA51. en. live. https://web.archive.org/web/20170102080305/https://books.google.ca/books?id=7dDKBQAAQBAJ&pg=PA51. 2017-01-02.
  9. Sang GW . Pharmacodynamic effects of once-a-month combined injectable contraceptives . Contraception . 49 . 4 . 361–385 . April 1994 . 8013220 . 10.1016/0010-7824(94)90033-7 . The exact formulation and the size of the microcrystals is most important for duration of action. The smaller particles are more rapidly dissolved than larger ones and, hence, MPA appears more rapidly in the circulation, with more rapid elimination from the body. This is also true for the once-a-month formulation, Cyclofem. From our laboratory’s data, the distribution of particle size of Cyclofem is showed in Table 2. [...] TABLE 2. Distribution of particle size of crystalline steroids in Cyclofem (aqueous suspension). Size of particle (μm): ≤4: 0.3%. 5–6: 7.3%. 6–8: 16.7%. 8–10: 29.0%. 10–13: 29.7%. 13–16: 9.9%. 16–20: 0.5%. >20: 0.1%. .
  10. Kaunitz AM . Injectable contraception. New and existing options . Obstetrics and Gynecology Clinics of North America . 27 . 4 . 741–780 . December 2000 . 11091987 . 10.1016/S0889-8545(05)70171-6 .
  11. Kaunitz AM . Injectable long-acting contraceptives . Clinical Obstetrics and Gynecology . 44 . 1 . 73–91 . March 2001 . 11219248 . 10.1097/00003081-200103000-00011 . 30793138 . free .
  12. Book: Nadakavukaren A . Our Global Environment: A Health Perspective . Seventh . 28 February 2011. Waveland Press. 978-1-4786-0976-6. 63–.
  13. Book: Levitt, Jeremy I. . vanc . Black Women and International Law: Deliberate Interactions, Movements and Actions . 30 April 2015. Cambridge University Press. 978-1-316-29840-4. 230–231.
  14. Hall PE . New once-a-month injectable contraceptives, with particular reference to Cyclofem/Cyclo-Provera . International Journal of Gynaecology and Obstetrics . 62 . Suppl 1 . S43–S56 . August 1998 . 9806239 . 10.1016/S0020-7292(98)00090-3 . 2826689 .
  15. Coutinho EM, Carlos de Souza J . Conception control by monthly injections of medroxyprogesterone suspension and long-acting oestrogen . Journal of Reproduction and Fertility . 15 . 2 . 209–214 . March 1968 . 5643482 . 10.1530/jrf.0.0150209 . 37979625 .
  16. Newton JR, D'arcangues C, Hall PE . A review of "once-a-month" combined injectable contraceptives . Journal of Obstetrics and Gynaecology . 4 . Suppl 1 . S1-34 . 1994 . 12290848 . 10.3109/01443619409027641 .
  17. Oriowo MA, Landgren BM, Stenström B, Diczfalusy E . A comparison of the pharmacokinetic properties of three estradiol esters . Contraception . 21 . 4 . 415–424 . April 1980 . 7389356 . 10.1016/S0010-7824(80)80018-7 .
  18. d'Arcangues C . Once-a-month injectable contraceptives . World Health Forum . 14 . 4 . 439–440 . 1993 . 8185807 .
  19. Book: Nagrath Arun. Malhotra Narendra. Seth Shikha. Progress in Obstetrics and Gynecology--3. 15 December 2012. Jaypee Brothers Medical Publishers Pvt. Ltd.. 978-93-5090-575-3. 416–.
  20. Koetsawang S . Once-a-month injectable contraceptives: efficacy and reasons for discontinuation . Contraception . 49 . 4 . 387–398 . April 1994 . 8013221 . 10.1016/0010-7824(94)90034-5 .
  21. Web site: Estradiol: Uses, Dosage & Side Effects . drugs.com .
  22. Web site: Medroxyprogesterone Uses, Dosage & Side Effects . drugs.com .
  23. Book: Sweetman SC . Sex hormones and their modulators . Martindale: The Complete Drug Reference . 36th . 2009 . 2082 . Pharmaceutical Press . London. 978-0-85369-840-1.
  24. Web site: Micromedex Products: Please Login.
  25. 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.
  26. 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–.
  27. Klitsch M . Still waiting for the contraceptive revolution . Family Planning Perspectives . 27 . 6 . 246–253 . 1995 . 8666089 . 10.2307/2136177 . 2136177 .

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