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Birth control pill formulations

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Ingredients of oral contraceptives
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Birth control pills come in a variety of formulations. The main division is betweencombined oral contraceptive pills, containing bothestrogens andsyntheticprogestogens (progestins), andprogestogen 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

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Combination pills usually work by preventing theovaries from releasing eggs (ovulation). They also thicken thecervical mucus, which keepssperm from penetrating into the uterus and joining with anegg. The hormones in combination and progestogen-only pills also thin the lining of theuterus. This could preventpregnancy by interfering with implantation of ablastocyst.

Main action in typical use is prevention of ovulation.

Combined oral contraceptive pills

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All contain an estrogen,ethinylestradiol ormestranol,[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 μg of mestranol is equivalent to only 35 μg of ethinylestradiol and should not be used when high-dose [50 μg ethinylestradiol] estrogen pills are needed; mestranol was the estrogen used in the first oral contraceptive,Enovid). They are usually taken for 21 days with then a seven-day gap during which a withdrawal bleed (often, but incorrectly, referred to as amenstrual period) occurs. These differ in the amount of estrogen given, and whether they are monophasic (the same dose of estrogen and progestogen during each of the 21 days) or multiphasic (varying doses). The introduction ofextended-cycle monophasic pills (i.e. Seasonale) has shown that the withdrawal bleeding intervals can be decreased.

In 2023, the combination ethinylestradiol/norgestrel was the 282nd most commonly prescribed medication in the United States, with more than 700,000 prescriptions.[3][4]

Monophasic

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These are typically given as 21 tablets of estrogen and progestogen, followed by seven tablets of placebo or aniron supplement,[5][6] 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.[7] Different formulations contain different amounts of estrogen and progestogen:

  • 15 μg ethinylestradiol
    • 60 μggestodene: 24 days + 4 days placebo (Spain: Melodene-15; Israel: Minesse)[8]
  • 20 μg ethinylestradiol
    • 1000 μgnorethisterone acetate (UK: Loestrin 20, Galen; US: Loestrin 1/20,Duramed; Microgestin 1/20,Watson Pharmaceuticals; Junel 1/20,Barr)
    • 1000 μg norethisterone acetate: 24 days + 4 daysferrous fumarate only (US: Loestrin 24 Fe,Warner Chilcott)
    • 90 μglevonorgestrel:continuous: 365 days/year, no placebo (US: Amethyst,Watson)
    • 100 μg levonorgestrel: extended cycle: 84 days + 7 days 10 μg ethinylestradiol only (US: LoSeasonique, Teva; CamreseLo, Teva)
    • 100 μg levonorgestrel (US: Alesse, Wyeth; Aviane, Barr; Lessina, Barr; Lutera, Watson; Sronyx, Watson)
    • 150 μgdesogestrel (UK: Mercilon,Organon; HU: Novynette,Richter Gedeon)
    • 75 μggestodene (UK: Femodette,Bayer; RU: Logest, Bayer; Brazil: Femiane, Bayer[9])
    • 3000 μgdrospirenone: 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 (RU: Yaz Plus, US:Beyaz; Bayer)
  • 30 μg ethinylestradiol
    • 1500 μg norethisterone acetate (UK: Loestrin 30, Galen; US: Loestrin 1.5/30, Duramed; Microgestin 1.5/30, Watson;Junel 1.5/30, Barr)
    • 300 μgnorgestrel (US: Lo/Ovral, Wyeth; Low-Ogestrel, Watson; Cryselle, Barr)
    • 150 μg levonorgestrel (UK: Ovranette, Wyeth; Microgynon 30, Microgynon 30 ED, Bayer; US: Nordette, Duramed, Levora, Watson, Portia, Barr)
    • 150 μg levonorgestrel: 21 day cycle + 7 days no pills (Canada: Min-Ovral 21; EU: Ovoplex 150/30; Sweden:Neovletta,Prionelle)
    • 150 μg levonorgestrel: 21 day cycle + 7 days placebo (Canada: Min-Ovral 28; Sweden:Prionelle 28; RU: Rigevidon 21+7, Richter Gedeon)
    • 150 μg levonorgestrel:extended cycle: 84 days + 7 days placebo (US: Seasonale, Duramed; Quasense, Watson; Jolessa, Barr, Introvale)
    • 150 μg levonorgestrel: extended cycle: 84 days + 7 days 10 μg ethinylestradiol only (US: Seasonique, Duramed; Camrese, Teva; Amethia, Watson)
    • 75 μg gestodene (UK: Femodene, Femodene ED, Bayer; Minulet, Wyeth; RU: Femoden,Jenapharm)
    • 150 μg desogestrel(AU, EU, RU, UK: Marvelon, BR: Microdiol, US: Desogen,MSD; US: Ortho-Cept,Ortho-McNeil; RU: Regulon, Richter Gedeon)
    • 3000 μgdrospirenone (AU, EU, US: Yasmin, FR: Jasmine, RU: Yarina, Bayer Schering Pharma AG); with levomefolate calcium (US: Safyral, Bayer Schering Pharma AG)
    • 2000 μgchlormadinone acetate (EU: Belara,Benelux: Bellina; Gedeon Richter)
    • 2000 μgdienogest (AU, EU: Valette, RU: Jeanine, Bayer Schering Pharma AG; RU: Siluet, Gedeon Richter)
  • 35 μg ethinylestradiol
    • 400 μgnorethisterone: chewable,spearmint flavor (US: Femcon Fe, Warner Chilcott)
    • 400 μg norethisterone (US: Ovcon 35, Warner Chilcott; Balziva, Barr)
    • 500 μg norethisterone (UK: Ovysmen,Janssen-Cilag; Brevinor,Pfizer; US: Modicon, Ortho-McNeil; Brevicon, Watson; Nortrel 0.5/35, Barr)
    • 1000 μg 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 μgetynodiol diacetate (US: Demulen 1/35, Pfizer; Zovia 1/35, Watson; Kelnor, Barr)
    • 250 μgnorgestimate (UK: Cilest, Janssen-Cilag; US: Ortho Cyclen, Ortho-McNeil; MonoNessa, Watson; Sprintec, Barr; Sweden:Amorest[10])
    • 2000 μgcyproterone acetate: only approved for severeacne or severehirsutism in the UK (AU, RU: Diane-35, UK: Dianette,Bayer)
  • 50 μg mestranol (equivalent to 35 μg ethinylestradiol)
    • 1000 μg norethisterone (UK: Norinyl-1, Pfizer; US: Ortho-Novum 1/50; Ortho-McNeil; Norinyl 1/50, Watson; Necon 1/50, Watson)
  • 50 μg ethinylestradiol
    • 1000 μg norethisterone (US: Ovcon 50, Warner Chilcott)
    • 1000 μg etynodiol diacetate (US: Demulen 1/50, Pfizer; Zovia 1/50, Watson)
    • 500 μg norgestrel (US: Ogestrel, Watson)
    • 250 μg levonorgestrel (US: Nordiol, Wyeth)
  • 1.5 mg estradiol (as hemihydrate)
  • 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

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  • 25 μg ethinylestradiol: triphasic
    • ethinylestradiol/norgestimate combination with 7 tablets 25 μg/180 μg, 7 tablets 25 μg/215 μg, 7 tablets 25 μg/250 μg 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)[11]
    • ethinylestradiol/desogestrel combination with 7 tablets 25 μg/100 μg, 7 tablets 25 μg/125 μg, 7 tablets 25 μg/150 μg, followed by 7 tablets offerric oxide (US: Cyclessa, Organon; Velivet, Barr)
  • 20/30/35 μg ethinylestradiol: estrophasic
    • ethinylestradiol/norethisterone acetate combination with 5 tablets 20 μg/1000 μg, 7 tablets 30 μg/1000 μg, 9 tablets 35 μg/1000 μg, followed by 7 tablets of ferrous fumarate 75 mg (US:Estrostep Fe, Warner Chilcott)
  • 35/30/30 μg ethinylestradiol: triphasic
    • ethinylestradiol/desogestrel combination with 7 tablets 35 μg/50 μg, 7 tablets 30 μg/100 μg, 7 tablets 30 μg/150 μg (RU: Tri-Merci, Organon)
  • 30/40/30 μg ethinylestradiol: triphasic
    • ethinylestradiol/levonorgestrel combination with 6 tablets 30 μg/50 μg, 5 tablets 40 μg/75 μg, 10 tablets 30 μg/125 μg (UK: Trinordiol, Wyeth; Logynon, Logynon ED, Bayer; US: Triphasil, Wyeth; Trivora, Watson; Enpresse, Barr)
    • ethinylestradiol/gestodene combination with 6 tablets 30 μg/50 μg, 5 tablets 40 μg/70 μg, 10 tablets 30 μg/100 μg (UK: Triadene, Bayer; Tri-Minulet, Wyeth)
  • 35 μg ethinylestradiol: triphasic
    • ethinylestradiol/norethisterone combination with 7 tablets 35 μg/500 μg, 9 tablets 35 μg/1000 μg, 5 tablets 35 μg/500 μg (UK: Synphase, Pfizer; US: Tri-Norinyl, Watson; Leena, Watson)
    • ethinylestradiol/norethisterone combination with 7 tablets 35 μg/500 μg, 7 tablets 35 μg/750 μg, 7 tablets 35 μg/1000 μg (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 μg/180 μg, 7 tablets 35 μg/215 μg, 7 tablets 35 μg/250 μg followed by 7 placebos (Ortho Tri-Cyclen, Ortho-McNeil; TriNessa, Watson; Tri-Sprintec, Barr)
  • 35 μg ethinylestradiol: biphasic
    • ethinylestradiol/norethisterone combination with 10 tablets 35 μg/500 μg, 11 tablets 35 μg/1000 μg, followed by 7 placebos (US: Ortho-Novum 10/11, Ortho-McNeil; Necon 10/11, Watson)
    • ethinylestradiol/norethisterone combination with 7 tablets 35 μg/500 μg, 14 tablets 35 μg/1000 μg (UK: BiNovum, Janssen-Cilag)

  • 3/2/1 mgestradiol valerate: estrophasic
    • estradiol valerate/dienogest combination with 2 tablets 3 mg/0 mg, followed by 5 tablets 2 mg/2 mg, 17 tablets 2 mg/3 mg, 2 tablets 1 mg/0 mg, and 2 placebos. (AU, EU, RU: Qlaira, US: Natazia,Bayer)[12][13]

Progestogen-only pills

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Progestogen-only pills (POPs) use aprogestogen 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 μgnorethisterone (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 mgdrospirenone (Slynd)
  • 75 μgdesogestrel (UK: Cerazette, Loestrin; RU: Cerazette, Organon; Lactinette, Richter Gedeon; SE: Gestrina)
  • 30 μglevonorgestrel (UK: Norgeston, Bayer; AUS, RU: Microlut, Bayer)
  • 500 μgetynodiol diacetate (UK: Femulen, Pfizer)
  • 500 μglynestrenol (RU: Exluton, Organon)
  • 75 μgnorgestrel (US: Opill, Perrigo)

Contraindications

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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[14] which are reflected in theCDC Medical Eligibility for Contraceptive Use Guidelines.[15]

See also

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References

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  1. ^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.
  2. ^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.
  3. ^"The Top 300 of 2023".ClinCalc.Archived from the original on 17 August 2025. Retrieved17 August 2025.
  4. ^"Ethinyl Estradiol; Norgestrel Drug Usage Statistics, United States, 2014 - 2023".ClinCalc. Retrieved17 August 2025.
  5. ^"US Patent:Oral contraceptive:Patent 6451778 Issued on September 17, 2002 Estimated Expiration Date: July 2, 2017".PatentStorm LLC. Archived fromthe original on 13 June 2011. Retrieved19 November 2010.
  6. ^Serge Herceberg, Paul Preziosi, Pilar Galan."Iron deficiency in Europe"(PDF). Public Health Nutrition: 4(2B). pp. 537–545. Archived fromthe original(PDF) on 26 July 2011. Retrieved19 November 2010.
  7. ^FFPRHC (2007)."Clinical Guidance: First Prescription of Combined Oral Contraception"(PDF). Archived fromthe original(PDF) on 4 July 2007. Retrieved7 July 2007.
  8. ^"Archived copy"(PDF). Archived fromthe original(PDF) on 22 July 2011. Retrieved20 April 2011.{{cite web}}: CS1 maint: archived copy as title (link)
  9. ^"Archived copy"(PDF). Archived fromthe original(PDF) on 3 May 2015. Retrieved29 November 2014.{{cite web}}: CS1 maint: archived copy as title (link)
  10. ^"Amorest 28".FASS.se. Retrieved8 August 2019.
  11. ^"GoodRx - Error". Retrieved31 August 2016.
  12. ^"Natazia Prescribing Information"(PDF). Archived fromthe original(PDF) on 5 October 2011. Retrieved1 December 2011.
  13. ^"Summary of Product Characteristics for Qlaira". Archived fromthe original on 26 December 2009. Retrieved29 December 2009.
  14. ^"Medical eligibility criteria for contraceptive use".World Health Organization. Retrieved11 March 2016.
  15. ^"United States Medical Eligibility Criteria (USMEC) for Contraceptive Use | Unintended Pregnancy | Reproductive Health | CDC".www.cdc.gov. Retrieved11 March 2016.
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