Birth control pill formulations

Source: Wikipedia, the free encyclopedia.

Birth control pills come in a variety of formulations. The main division is between

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

Combination pills usually work by preventing the

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

All contain an estrogen,

extended-cycle monophasic pills
(i.e. Seasonale) has shown that the withdrawal bleeding intervals can be decreased.

Monophasic

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:

Multiphasic

  • 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)[9]
    • 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 of
      ferric 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 mg estradiol 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)[10][11]

Progestogen-only pills

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 μg 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 μg desogestrel (UK: Cerazette, Loestrin; RU: Cerazette, Organon; Lactinette, Richter Gedeon; SE: Gestrina)
  • 30 μg levonorgestrel (UK: Norgeston, Bayer; AUS, RU: Microlut, Bayer)
  • 500 μg etynodiol diacetate (UK: Femulen, Pfizer)
  • 500 μg lynestrenol (RU: Exluton, Organon)

Contraindications

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

References

  1. ISBN 0-9664902-5-8
    .
  2. ISBN 0-7817-6488-2
    .
  3. ^ "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.
  4. ^ 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.
  5. ^ FFPRHC (2007). "Clinical Guidance: First Prescription of Combined Oral Contraception" (PDF). Archived from the original (PDF) on 2007-07-04. Retrieved 2007-07-07.
  6. ^ "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)
  7. ^ "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)
  8. FASS.se
    . Retrieved 2019-08-08.
  9. ^ "GoodRx - Error". Retrieved 31 August 2016.
  10. ^ "Natazia Prescribing Information" (PDF). Archived from the original (PDF) on 2011-10-05. Retrieved 2011-12-01.
  11. ^ "Summary of Product Characteristics for Qlaira". Archived from the original on 2009-12-26. Retrieved 2009-12-29.
  12. ^ "Medical eligibility criteria for contraceptive use". World Health Organization. Retrieved 2016-03-11.
  13. ^ "United States Medical Eligibility Criteria (USMEC) for Contraceptive Use | Unintended Pregnancy | Reproductive Health | CDC". www.cdc.gov. Retrieved 2016-03-11.
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