Estradiol cypionate/medroxyprogesterone acetate

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Estradiol cypionate /
medroxyprogesterone acetate
Estradiol 17 beta-cypionate.svg
Medroxyprogesterone acetate.svg
Estradiol cypionate (top) and medroxy-
progesterone acetate (bottom)
Combination of
Estradiol cypionate Estrogen
Medroxyprogesterone acetate Progestogen
Clinical data
Trade names Cyclofem, Lunelle, others [1]
Other namesEC/MPA; Cyclo-Provera; HRP-112
AHFS/Drugs.com Micromedex Detailed Consumer Information
Pregnancy
category
  • X
Routes of
administration 		Intramuscular injection
ATC code
Legal status
Legal status
  • US:Withdrawn
Identifiers
CAS Number
PubChem CID
UNII

Estradiol cypionate/medroxyprogesterone acetate (EC/MPA), sold under the brand name Cyclofem among others, is a form of combined injectable birth control. [2] It contains estradiol cypionate (EC), an estrogen, and medroxyprogesterone acetate (MPA), a progestin. [2] It is recommended for short-term use and is given once a month by injection into a muscle. [3]

Contents

Common side effects of EC/MPA include irregular menstrual periods which typically improves with time. [3] Other side effects include blood clots, headache, hair loss, depression, nausea, and breast pain. [3] [4] Use during pregnancy is not recommended. [2] Use during breastfeeding is likely safe. [5] It works mainly by preventing ovulation. [2]

EC/MPA came into medical use in 1993 with approval in the United States in 2000. [6] [2] It is on the World Health Organization's List of Essential Medicines. [7] [8] The medication is approved for use in 18 countries. [9] It is used in Mexico, Thailand, and Indonesia, among other countries. [6] It is no longer commercially available in the United States. [2]

Medical uses

EC/MPA is used as a once-monthly combined injectable contraceptive to prevent pregnancy in women. [10]

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. [10] It is provided in the form of single-dose vials and ampoules. [10] The particle sizes of the formulation are 93% within a range of 5 to 16 μm. [11]

History

Depot MPA (DMPA) and EC/MPA were developed by Upjohn in the 1960s. [12] [13] 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. [14] [15] [13] A variety of preliminary studies on EC/MPA as a contraceptive were published between 1968 and 1978. [10] [16] [17] 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. [16] 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. [10] Funding for the initiative was provided by the United Nations Development Programme (UNDP), United Nations Population Fund (UNFPA), and World Bank. [16]

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. [10] [16] [18] 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. [16] [10] The WHO also developed estradiol valerate/norethisterone enantate (code name HRP-102) as a combined injectable contraceptive. [16] [10] 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. [16] 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. [6] [10] [19] It was available in 18 countries, mostly in Latin America and Asia, by 1998. [16] 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. [16] [12] However, the formulation was discontinued in the United States in late 2003. [20]

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. [21]

Brand names

Brand names of EC/MPA include Ciclofem, Ciclofemina, Cyclofem, Cyclofemina, Cyclogeston, Femelin, Femydrol, Gestin, Harmonis, Lunella, Lunelle, and Novafem. [22] [23]

Availability

EC/MPA has been approved for use in at least 18 countries. [9] 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. [22] [23] [24] [25] [26] [9] [6] [27] [28] The medication is no longer available in the United States. [2]

See also

Related Research Articles

<span class="mw-page-title-main">Progestogen (medication)</span> Medication producing effects similar to progesterone

A progestogen, also referred to as a progestagen, gestagen, or gestogen, is a type of medication which produces effects similar to those of the natural female sex hormone progesterone in the body. A progestin is a synthetic progestogen. Progestogens are used most commonly in hormonal birth control and menopausal hormone therapy. They can also be used in the treatment of gynecological conditions, to support fertility and pregnancy, to lower sex hormone levels for various purposes, and for other indications. Progestogens are used alone or in combination with estrogens. They are available in a wide variety of formulations and for use by many different routes of administration. Examples of progestogens include natural or bioidentical progesterone as well as progestins such as medroxyprogesterone acetate and norethisterone.

<span class="mw-page-title-main">Hormonal contraception</span> Birth control methods that act on the endocrine system

Hormonal contraception refers to birth control methods that act on the endocrine system. Almost all methods are composed of steroid hormones, although in India one selective estrogen receptor modulator is marketed as a contraceptive. The original hormonal method—the combined oral contraceptive pill—was first marketed as a contraceptive in 1960. In the ensuing decades, many other delivery methods have been developed, although the oral and injectable methods are by far the most popular. Hormonal contraception is highly effective: when taken on the prescribed schedule, users of steroid hormone methods experience pregnancy rates of less than 1% per year. Perfect-use pregnancy rates for most hormonal contraceptives are usually around the 0.3% rate or less. Currently available methods can only be used by women; the development of a male hormonal contraceptive is an active research area.

<span class="mw-page-title-main">Concept Foundation</span>

The Concept Foundation is a non-profit foundation which was established by the UNDP/UNFPA/WHO/WB Special program in Reproductive Health (WHO/HRP), PATH, the World Bank in 1989 in Bangkok, Thailand, "as a mechanism through which WHO’s rights associated with an injectable contraceptive, Cyclofem, could be licensed to potential producers in developing countries". Estradiol cypionate/medroxyprogesterone acetate, is a once-a-month combined injectable contraceptive which contains 25 mg of medroxyprogesterone acetate—the same ingredient in Depo Provera—and 5 mg of estradiol cypionate.

Combined injectable contraceptives (CICs) are a form of hormonal birth control for women. They consist of monthly injections of combined formulations containing an estrogen and a progestin to prevent pregnancy.

<span class="mw-page-title-main">Algestone acetophenide</span> Chemical compound

Algestone acetophenide, also known more commonly as dihydroxyprogesterone acetophenide (DHPA) and sold under the brand names Perlutal and Topasel among others, is a progestin medication which is used in combination with an estrogen as a form of long-lasting injectable birth control. It has also been used alone, but is no longer available as a standalone medication. DHPA is not active by mouth and is given once a month by injection into muscle.

<span class="mw-page-title-main">Medroxyprogesterone acetate</span> Injectable form of birth control

Medroxyprogesterone acetate (MPA), also known as depot medroxyprogesterone acetate (DMPA) in injectable form and sold under the brand name Depo-Provera among others, is a hormonal medication of the progestin type. It is used as a method of birth control and as a part of menopausal hormone therapy. It is also used to treat endometriosis, abnormal uterine bleeding, paraphilia, and certain types of cancer. The medication is available both alone and in combination with an estrogen. It is taken by mouth, used under the tongue, or by injection into a muscle or fat.

<span class="mw-page-title-main">Estradiol cypionate</span> Chemical compound

Estradiol cypionate (EC), sold under the brand name Depo-Estradiol among others, is an estrogen medication which is used in hormone therapy for menopausal symptoms and low estrogen levels in women, in hormone therapy for trans women, and in hormonal birth control for women. It is given by injection into muscle once every 1 to 4 weeks.

<span class="mw-page-title-main">Norethisterone enanthate</span> Chemical compound

Norethisterone enanthate (NETE), also known as norethindrone enanthate, is a form of hormonal birth control which is used to prevent pregnancy in women. It is used both as a form of progestogen-only injectable birth control and in combined injectable birth control formulations. It may be used following childbirth, miscarriage, or abortion. The failure rate per year in preventing pregnancy for the progestogen-only formulation is 2 per 100 women. Each dose of this form lasts two months with only up to two doses typically recommended.

<span class="mw-page-title-main">Estradiol enantate</span> Chemical compound

Estradiol enantate, also spelled estradiol enanthate and sold under the brand names Perlutal and Topasel among others, is an estrogen medication which is used in hormonal birth control for women. It is formulated in combination with dihydroxyprogesterone acetophenide, a progestin, and is used specifically as a combined injectable contraceptive. Estradiol enantate is not available for medical use alone. The medication, in combination with DHPA, is given by injection into muscle once a month.

<span class="mw-page-title-main">Estradiol hexahydrobenzoate</span> Chemical compound

Estradiol hexahydrobenzoate (EHHB), sold under a number of brand names including Benzo-Ginoestril A.P., BenzoGynoestryl Retard, Ginestryl-15-Depot, Menodin, and Tardoginestryl, is an estrogen medication which was previously used for indications such as menopausal hormone therapy and gynecological disorders. EHHB is given by injection into muscle at regular intervals, for instance once every few weeks.

Combined birth control pills that contain natural estradiol or an estradiol ester include:

Progestogen-only injectable contraceptives (POICs) are a form of hormonal contraception and progestogen-only contraception that are administered by injection and providing long-lasting birth control. As opposed to combined injectable contraceptives, they contain only a progestogen without an estrogen, and include two progestin preparations:

<span class="mw-page-title-main">Estradiol benzoate butyrate</span> Chemical compound

Estradiol benzoate butyrate (EBB), sold under the brand names Neolutin N, Redimen, Soluna, and Unijab and formerly known under the developmental code name Unimens, is an estrogen medication which is used in hormonal birth control for women. It is formulated in combination with dihydroxyprogesterone acetophenide, a progestin, and is used specifically as a combined injectable contraceptive. EBB is not available for medical use alone. The medication, in combination with DHPA, is given by injection into muscle once a month.

Conjugated estrogens/medroxyprogesterone acetate (CEs/MPA), sold under the brand names Prempro and Premphase, is a combination product of conjugated equine estrogens (Premarin), an estrogen collected from horse urine, and medroxyprogesterone acetate (Provera), a progestogen, which is used in menopausal hormone therapy for the treatment of menopausal symptoms.

<span class="mw-page-title-main">Estradiol valerate/norethisterone enantate</span> 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. It contains estradiol valerate (EV), an estrogen, and norethisterone enantate (NETE), a progestin. The medication is given once a month by injection into muscle.

<span class="mw-page-title-main">Estradiol valerate/hydroxyprogesterone caproate</span> Pharmaceutical combination

Estradiol valerate/hydroxyprogesterone caproate (EV/OHPC), sold under the brand names Gravibinon and Injectable No. 1 among others, is a combined estrogen and progestogen medication which is used in the treatment of threatened miscarriage and other indications and as a form of combined injectable birth control to prevent pregnancy. It contains estradiol valerate (EV), an estrogen, and hydroxyprogesterone caproate (OHPC), a progestin. The medication is given by injection into muscle once a day to once a month depending on the indication.

<span class="mw-page-title-main">Estradiol enantate/algestone acetophenide</span> Pharmaceutical combination

Estradiol enantate/algestone acetophenide, also known as estradiol enantate/dihydroxyprogesterone acetophenide (E2-EN/DHPA) and sold under the brand names Perlutal and Topasel among others, is a form of combined injectable birth control which is used to prevent pregnancy. It contains estradiol enantate (E2-EN), an estrogen, and algestone acetophenide, a progestin. The medication is given once a month by injection into muscle.

<span class="mw-page-title-main">Estradiol benzoate butyrate/algestone acetophenide</span> Combination drug

Estradiol benzoate butyrate/algestone acetophenide, also known as estradiol benzoate butyrate/dihydroxyprogesterone acetophenide (EBB/DHPA) and sold under the brand names Neolutin N, Redimen, Soluna, and Unijab, is a form of combined injectable birth control which is used in Peru and Singapore. It contains estradiol benzoate butyrate (EBB), an estrogen, and algestone acetophenide, a progestin. The medication is given once per month by injection into muscle.

Menstrual suppression refers to the practice of using hormonal management to stop or reduce menstrual bleeding. In contrast to surgical options for this purpose, such as hysterectomy or endometrial ablation, hormonal methods to manipulate menstruation are reversible.

References

  1. ↑ 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. p. 431. ISBN   9789283212911. Archived from the original on 2017-01-02.
  2. 1 2 3 4 5 6 7 "Estradiol and medroxyprogesterone Intramuscular Advanced Patient Information - Drugs.com". www.drugs.com. Archived from the original on 1 January 2017. Retrieved 1 January 2017.
  3. 1 2 3 World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. pp. 368–370. hdl: 10665/44053 . ISBN   9789241547659.
  4. ↑ "Estradiol/medroxyprogesterone Side Effects in Detail - Drugs.com". www.drugs.com. Archived from the original on 1 January 2017. Retrieved 1 January 2017.
  5. ↑ "Estradiol / medroxyprogesterone (Lunelle) Use During Pregnancy". www.drugs.com. Archived from the original on 1 January 2017. Retrieved 1 January 2017.
  6. 1 2 3 4 Senanayake P, Potts M (2008). "Hormonal Contraception". Atlas of Contraception (Second ed.). CRC Press. p. 51. ISBN   9780203347324. Archived from the original on 2017-01-02.
  7. ↑ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl: 10665/325771 . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  8. ↑ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl: 10665/345533 . WHO/MHP/HPS/EML/2021.02.
  9. 1 2 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. Archived from the original (PDF) on 2017-08-10. Retrieved 2018-08-02.
  10. 1 2 3 4 5 6 7 8 9 Newton JR, D'arcangues C, Hall PE (1994). "A review of "once-a-month" combined injectable contraceptives". Journal of Obstetrics and Gynaecology. 4 (Suppl 1): S1-34. doi:10.3109/01443619409027641. PMID   12290848.
  11. ↑ Sang GW (April 1994). "Pharmacodynamic effects of once-a-month combined injectable contraceptives". Contraception. 49 (4): 361–385. doi:10.1016/0010-7824(94)90033-7. PMID   8013220. 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%.
  12. 1 2 Kaunitz AM (December 2000). "Injectable contraception. New and existing options". Obstetrics and Gynecology Clinics of North America. 27 (4): 741–780. doi:10.1016/S0889-8545(05)70171-6. PMID   11091987.
  13. 1 2 Kaunitz AM (March 2001). "Injectable long-acting contraceptives". Clinical Obstetrics and Gynecology. 44 (1): 73–91. doi: 10.1097/00003081-200103000-00011 . PMID   11219248. S2CID   30793138.
  14. ↑ Nadakavukaren A (28 February 2011). Our Global Environment: A Health Perspective (Seventh ed.). Waveland Press. pp. 63–. ISBN   978-1-4786-0976-6.
  15. ↑ Levitt JI (30 April 2015). Black Women and International Law: Deliberate Interactions, Movements and Actions. Cambridge University Press. pp. 230–231. ISBN   978-1-316-29840-4.
  16. 1 2 3 4 5 6 7 8 9 Hall PE (August 1998). "New once-a-month injectable contraceptives, with particular reference to Cyclofem/Cyclo-Provera". International Journal of Gynaecology and Obstetrics. 62 (Suppl 1): S43–S56. doi:10.1016/S0020-7292(98)00090-3. PMID   9806239. S2CID   2826689.
  17. ↑ Coutinho EM, Carlos de Souza J (March 1968). "Conception control by monthly injections of medroxyprogesterone suspension and long-acting oestrogen". Journal of Reproduction and Fertility. 15 (2): 209–214. doi:10.1530/jrf.0.0150209. PMID   5643482. S2CID   37979625.
  18. ↑ Oriowo MA, Landgren BM, Stenström B, Diczfalusy E (April 1980). "A comparison of the pharmacokinetic properties of three estradiol esters". Contraception. 21 (4): 415–424. doi:10.1016/S0010-7824(80)80018-7. PMID   7389356.
  19. ↑ d'Arcangues C (1993). "Once-a-month injectable contraceptives". World Health Forum. 14 (4): 439–440. PMID   8185807.
  20. ↑ Nagrath Arun; Malhotra Narendra; Seth Shikha (15 December 2012). Progress in Obstetrics and Gynecology--3. Jaypee Brothers Medical Publishers Pvt. Ltd. pp. 416–. ISBN   978-93-5090-575-3.
  21. ↑ Koetsawang S (April 1994). "Once-a-month injectable contraceptives: efficacy and reasons for discontinuation". Contraception. 49 (4): 387–398. doi:10.1016/0010-7824(94)90034-5. PMID   8013221.
  22. 1 2 "Estradiol: Uses, Dosage & Side Effects". drugs.com.
  23. 1 2 "Medroxyprogesterone Uses, Dosage & Side Effects". drugs.com.
  24. ↑ Sweetman SC, 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.
  25. ↑ "Micromedex Products: Please Login".
  26. ↑ 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.
  27. ↑ 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.
  28. ↑ Klitsch M (1995). "Still waiting for the contraceptive revolution". Family Planning Perspectives. 27 (6): 246–253. doi:10.2307/2136177. JSTOR   2136177. PMID   8666089.
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