Birth control pill formulations
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Birth control pills come in a variety of formulations. The main division is between combined oral contraceptive pills, containing both estrogens and synthetic progestogens (progestins), and progestogen only pills. Combined oral contraceptive pills also come in varying types, including varying doses of estrogen, and whether the dose of estrogen or progestogen changes from week to week.
Mechanism of action
[edit]Combination pills usually work by preventing the ovaries from releasing eggs (ovulation). They also thicken the cervical mucus, which keeps sperm from penetrating into the uterus and joining with an egg. The hormones in combination and progestogen-only pills also thin the lining of the uterus. This could prevent pregnancy by interfering with implantation of a blastocyst.
Main action in typical use is prevention of ovulation.
Combined oral contraceptive pills
[edit]All contain an estrogen, ethinylestradiol or mestranol,[1][2] in varying amounts, and one of a number of different progestogens. (Regarding the estrogen, the inactive 3-methyl ether of ethinylestradiol, which must be metabolized by the liver into the active ethinylestradiol; 50
Monophasic
[edit]These are typically given as 21 tablets of estrogen and progestogen, followed by seven tablets of placebo or an iron supplement,[3][4] although some newer formulations contain more active tablets and fewer placebos. Everyday regimens (Microgynon 30 ED, Femodene ED, Logynon ED), which include seven inactive placebo pills, are rarely used in UK practice.[5] Different formulations contain different amounts of estrogen and progestogen:
- 15
μ g ethinylestradiol - 20
μ g ethinylestradiol- 1000
μ g norethisterone acetate (UK: Loestrin 20, Galen; US: Loestrin 1/20, Duramed; Microgestin 1/20, Watson Pharmaceuticals; Junel 1/20, Barr) - 1000
μ g norethisterone acetate: 24 days + 4 days ferrous fumarate only (US: Loestrin 24 Fe, Warner Chilcott) - 90
μ g levonorgestrel: continuous: 365 days/year, no placebo (US: Amethyst, Watson) - 100
μ g levonorgestrel: extended cycle: 84 days + 7 days 10μ g ethinylestradiol only (US: LoSeasonique, Teva; CamreseLo, Teva) - 100
μ g levonorgestrel (US: Alesse, Wyeth; Aviane, Barr; Lessina, Barr; Lutera, Watson; Sronyx, Watson) - 150
μ g desogestrel (UK: Mercilon, Organon; HU: Novynette, Richter Gedeon) - 75
μ g gestodene (UK: Femodette, Bayer; RU: Logest, Bayer; Brazil: Femiane, Bayer[7]) - 3000
μ g drospirenone: 24 days + 4 days placebo (US, EU, RU: Yaz; Bayer Schering Pharma AG. Cleonita); 21 days + 7 days placebo (US, EU: Yasminelle, Bayer); 24 days + 4 days placebo and levomefolate calcium (US: Beyaz; Bayer)
- 1000
- 30
μ g ethinylestradiol- 1500
μ g norethisterone acetate (UK: Loestrin 30, Galen; US: Loestrin 1.5/30, Duramed; Microgestin 1.5/30, Watson; Junel 1.5/30, Barr) - 300
μ g norgestrel (US: Lo/Ovral, Wyeth; Low-Ogestrel, Watson; Cryselle, Barr) - 150
μ g levonorgestrel (UK: Ovranette, Wyeth; Microgynon 30, Microgynon 30 ED, Bayer; US: Nordette, Duramed, Levora, Watson, Portia, Barr) - 150
μ g levonorgestrel: 21 day cycle + 7 days no pills (Canada: Min-Ovral 21; EU: Ovoplex 150/30; Sweden: Neovletta, Prionelle) - 150
μ g levonorgestrel: 21 day cycle + 7 days placebo (Canada: Min-Ovral 28; Sweden: Prionelle 28; RU: Rigevidon 21+7, Richter Gedeon) - 150
μ g levonorgestrel: extended cycle: 84 days + 7 days placebo (US: Seasonale, Duramed; Quasense, Watson; Jolessa, Barr, Introvale) - 150
μ g levonorgestrel: extended cycle: 84 days + 7 days 10μ g ethinylestradiol only (US: Seasonique, Duramed; Camrese, Teva; Amethia, Watson) - 75
μ g gestodene (UK: Femodene, Femodene ED, Bayer; Minulet, Wyeth; RU: Femoden, Jenapharm) - 150
μ g desogestrel (AU , EU, RU, UK: Marvelon, BR: Microdiol, US: Desogen, MSD; US: Ortho-Cept, Ortho-McNeil; RU: Regulon, Richter Gedeon) - 3000
μ g drospirenone (AU , EU, US: Yasmin, FR: Jasmine, RU: Yarina, Bayer Schering Pharma AG); with levomefolate calcium (US: Safyral, Bayer Schering Pharma AG) - 2000
μ g chlormadinone acetate (EU: Belara, Benelux: Bellina; Gedeon Richter) - 2000
μ g dienogest (AU , EU: Valette, RU: Jeanine, Bayer Schering Pharma AG; RU: Siluet, Gedeon Richter)
- 1500
- 35
μ g ethinylestradiol- 400
μ g norethisterone: chewable, spearmint flavor (US: Femcon Fe, Warner Chilcott) - 400
μ g norethisterone (US: Ovcon 35, Warner Chilcott; Balziva, Barr) - 500
μ g norethisterone (UK: Ovysmen, Janssen-Cilag; Brevinor, Pfizer; US: Modicon, Ortho-McNeil; Brevicon, Watson; Nortrel 0.5/35, Barr) - 1000
μ g norethisterone (AU , CAN: Synphasic, Pfizer; UK: Norimin, Pfizer; US: Ortho-Novum 1/35, Ortho-McNeil; Norinyl 1/35, Watson; Necon, Watson; Nortrel 1/35, Barr) - 1000
μ g etynodiol diacetate (US: Demulen 1/35, Pfizer; Zovia 1/35, Watson; Kelnor, Barr) - 250
μ g norgestimate (UK: Cilest, Janssen-Cilag; US: Ortho Cyclen, Ortho-McNeil; MonoNessa, Watson; Sprintec, Barr; Sweden: Amorest[8]) - 2000
μ g cyproterone acetate: only approved for severe acne or severe hirsutism in the UK (AU , RU: Diane-35, UK: Dianette, Bayer)
- 400
- 50
μ g mestranol (equivalent to 35μ g ethinylestradiol)- 1000
μ g norethisterone (UK: Norinyl-1, Pfizer; US: Ortho-Novum 1/50; Ortho-McNeil; Norinyl 1/50, Watson; Necon 1/50, Watson)
- 1000
- 50
μ g ethinylestradiol- 1000
μ g norethisterone (US: Ovcon 50, Warner Chilcott) - 1000
μ g etynodiol diacetate (US: Demulen 1/50, Pfizer; Zovia 1/50, Watson) - 500
μ g norgestrel (US: Ogestrel, Watson) - 250
μ g levonorgestrel (US: Nordiol, Wyeth)
- 1000
- 1.5 mg estradiol (as hemihydrate)
- 2.5 mg nomegestrol acetate: 24-day cycle + 4 placebo pills (
AU , EU, RU: Zoely, MSD)
- 2.5 mg nomegestrol acetate: 24-day cycle + 4 placebo pills (
- 15 mg estetrol monohydrate (equivalent to 14.2 mg estetrol)
- 3 mg drospirenone: 24-day cycle + 4 inactive pills (US, CAN: Nexstellis, Mayne, EU: Drovelis, Gedeon Richter Plc., EU: Lydisilka, Estetra SRL)
Multiphasic
[edit]- 25
μ g ethinylestradiol: triphasic- ethinylestradiol/norgestimate combination with 7 tablets 25
μ g/180μ g, 7 tablets 25μ g/215μ g, 7 tablets 25μ g/250μ g followed by 7 placebos (Ortho Tri-Cyclen Lo from Ortho-McNeil, Tri-Lo Sprintec back from Teva, Tri-Lo Marzia from Lupin, and norgestimate/ethinylestradiol from Mylan)[9] - ethinylestradiol/desogestrel combination with 7 tablets 25
μ g/100μ g, 7 tablets 25μ g/125μ g, 7 tablets 25μ g/150μ g, followed by 7 tablets of ferric oxide (US: Cyclessa, Organon; Velivet, Barr)
- ethinylestradiol/norgestimate combination with 7 tablets 25
- 20/30/35
μ g ethinylestradiol: estrophasic- ethinylestradiol/norethisterone acetate combination with 5 tablets 20
μ g/1000μ g, 7 tablets 30μ g/1000μ g, 9 tablets 35μ g/1000μ g, followed by 7 tablets of ferrous fumarate 75 mg (US: Estrostep Fe, Warner Chilcott)
- ethinylestradiol/norethisterone acetate combination with 5 tablets 20
- 35/30/30
μ g ethinylestradiol: triphasic- ethinylestradiol/desogestrel combination with 7 tablets 35
μ g/50μ g, 7 tablets 30μ g/100μ g, 7 tablets 30μ g/150μ g (RU: Tri-Merci, Organon)
- ethinylestradiol/desogestrel combination with 7 tablets 35
- 30/40/30
μ g ethinylestradiol: triphasic- ethinylestradiol/levonorgestrel combination with 6 tablets 30
μ g/50μ g, 5 tablets 40μ g/75μ g, 10 tablets 30μ g/125μ g (UK: Trinordiol, Wyeth; Logynon, Logynon ED, Bayer; US: Triphasil, Wyeth; Trivora, Watson; Enpresse, Barr) - ethinylestradiol/gestodene combination with 6 tablets 30
μ g/50μ g, 5 tablets 40μ g/70μ g, 10 tablets 30μ g/100μ g (UK: Triadene, Bayer; Tri-Minulet, Wyeth)
- ethinylestradiol/levonorgestrel combination with 6 tablets 30
- 35
μ g ethinylestradiol: triphasic- ethinylestradiol/norethisterone combination with 7 tablets 35
μ g/500μ g, 9 tablets 35μ g/1000μ g, 5 tablets 35μ g/500μ g (UK: Synphase, Pfizer; US: Tri-Norinyl, Watson; Leena, Watson) - ethinylestradiol/norethisterone combination with 7 tablets 35
μ g/500μ g, 7 tablets 35μ g/750μ g, 7 tablets 35μ g/1000μ g (UK: TriNovum, Janssen-Cilag; US: Ortho-Novum 7/7/7, Ortho-McNeil; Necon 7/7/7, Watson; Nortrel 7/7/7, Barr) - ethinylestradiol/norgestimate combination with 7 tablets 35
μ g/180μ g, 7 tablets 35μ g/215μ g, 7 tablets 35μ g/250μ g followed by 7 placebos (Ortho Tri-Cyclen, Ortho-McNeil; TriNessa, Watson; Tri-Sprintec, Barr)
- ethinylestradiol/norethisterone combination with 7 tablets 35
- 35
μ g ethinylestradiol: biphasic- ethinylestradiol/norethisterone combination with 10 tablets 35
μ g/500μ g, 11 tablets 35μ g/1000μ g, followed by 7 placebos (US: Ortho-Novum 10/11, Ortho-McNeil; Necon 10/11, Watson) - ethinylestradiol/norethisterone combination with 7 tablets 35
μ g/500μ g, 14 tablets 35μ g/1000μ g (UK: BiNovum, Janssen-Cilag)
- ethinylestradiol/norethisterone combination with 10 tablets 35
- 3/2/1 mg estradiol valerate: estrophasic
Progestogen-only pills
[edit]Progestogen-only pills (POPs) use a progestogen alone with doses taken continuously and no or a short gap between packs taken. People who use them may experience irregular light bleeds, and whilst irregular in the first few months of taking, usually settles to a regular pattern in time.
The following progestogens are used:
- 350
μ g norethisterone (norethindrone) (UK: Micronor, Janssen-Cilag; Noriday, Pfizer; US: Micronor, Ortho-McNeil; Nor-QD, Watson; Nora-BE, Watson; Jolivette, Watson; Camila, Barr; Errin, Barr; Heather, Glenmark; RU: Primolut-Nor, Bayer; Norkolut, Richter Gedeon) - 4 mg drospirenone (Slynd)
- 75
μ g desogestrel (UK: Cerazette, Loestrin; RU: Cerazette, Organon; Lactinette, Richter Gedeon; SE: Gestrina) - 30
μ g levonorgestrel (UK: Norgeston, Bayer; AUS, RU: Microlut, Bayer) - 500
μ g etynodiol diacetate (UK: Femulen, Pfizer) - 500
μ g lynestrenol (RU: Exluton, Organon) - 75
μ g norgestrel (US: Opill, Perrigo)
Contraindications
[edit]Generally oral contraceptives should not be used in people who currently have the following conditions:
- Thrombophlebitis or thromboembolic disorders
- A history of deep vein thrombophlebitis or thromboembolic disorders
- Cerebrovascular or coronary artery disease (current or history)
- Valvular heart disease with thrombogenic complications
- Severe hypertension
- Diabetes with vascular involvement
- Headaches with focal neurological symptoms
- Major surgery with prolonged immobilization
- Known or suspected carcinoma of the breast or personal history of breast cancer
- Carcinoma of the endometrium or other known or suspected estrogen-dependent neoplasia
- Undiagnosed abnormal genital bleeding
- Cholestatic jaundice of pregnancy or jaundice with prior pill use
- Hepatic adenomas or carcinomas, or active liver disease
- Known or suspected pregnancy
- Hypersensitivity to any component of the product
More comprehensive guidelines that include analysis of risks and benefits can be found in the World Health Organization Medical Eligibility for Contraceptive Use Guidelines[12] which are reflected in the CDC Medical Eligibility for Contraceptive Use Guidelines.[13]
See also
[edit]- Mestranol/noretynodrel (Enovid)—the first oral contraceptive
- List of progestogens available in the United States
- List of estrogens available in the United States
References
[edit]- ^ Hatcher, Robert A.; Nelson, Anita (2004). "Combined Hormonal Contraceptive Methods". In Hatcher; Robert A. (eds.). Contraceptive Technology (18th rev. ed.). New York: Ardent Media. pp. 391–460. ISBN 0-9664902-5-8.
- ^ Speroff, Leon; Darney, Philip D. (2005). "Oral Contraception". A Clinical Guide for Contraception (4th ed.). Philadelphia: Lippincott Williams & Wilkins. pp. 21–138. ISBN 0-7817-6488-2.
- ^ "US Patent:Oral contraceptive:Patent 6451778 Issued on September 17, 2002 Estimated Expiration Date: July 2, 2017". PatentStorm LLC. Archived from the original on June 13, 2011. Retrieved 2010-11-19.
- ^ Serge Herceberg; Paul Preziosi; Pilar Galan. "Iron deficiency in Europe" (PDF). Public Health Nutrition: 4(2B). pp. 537–545. Archived from the original (PDF) on 2011-07-26. Retrieved 2010-11-19.
- ^ FFPRHC (2007). "Clinical Guidance: First Prescription of Combined Oral Contraception" (PDF). Archived from the original (PDF) on 2007-07-04. Retrieved 2007-07-07.
- ^ "Archived copy" (PDF). Archived from the original (PDF) on 2011-07-22. Retrieved 2011-04-20.
{{cite web}}
: CS1 maint: archived copy as title (link) - ^ "Archived copy" (PDF). Archived from the original (PDF) on 2015-05-03. Retrieved 2014-11-29.
{{cite web}}
: CS1 maint: archived copy as title (link) - ^ "Amorest 28". FASS.se. Retrieved 2019-08-08.
- ^ "GoodRx - Error". Retrieved 31 August 2016.
- ^ "Natazia Prescribing Information" (PDF). Archived from the original (PDF) on 2011-10-05. Retrieved 2011-12-01.
- ^ "Summary of Product Characteristics for Qlaira". Archived from the original on 2009-12-26. Retrieved 2009-12-29.
- ^ "Medical eligibility criteria for contraceptive use". World Health Organization. Retrieved 2016-03-11.
- ^ "United States Medical Eligibility Criteria (USMEC) for Contraceptive Use | Unintended Pregnancy | Reproductive Health | CDC". www.cdc.gov. Retrieved 2016-03-11.