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Pharmacokinetics of progestogens
Progestogen Class Dosea Bioavailability Half-lifeTooltip Elimination half-life Refs
Allylestrenol Estrane NA ? Prodrug
Chlormadinone acetate Pregnane 2 mg ~100% 80 hours
Cyproterone acetate Pregnane 2 mg ~100% 54–79 hours
Desogestrel Gonane 0.15 mg 63% Prodrug
Dienogest Gonane 4 mg 96% 11–12 hours
Drospirenone Spirolactone 3 mg 66% 31–33 hours
Dydrogesterone Pregnane 10 mg 28% 14–17 hours
Etynodiol diacetate Estrane NA ? Prodrug
Gestodene Gonane 0.075 mg 88–99% 12–14 hours
Hydroxyprogesterone caproate Pregnane ND – 8 daysb [1]
Levonorgestrel Gonane 0.15–0.25 mg 90% 10–13 hours
Lynestrenol Estrane NA ? Prodrug
Medrogestone Pregnane 5 mg ~100% 35 hours
Medroxyprogesterone acetate Pregnane 10 mg ~100% 24 hours
Megestrol acetate Pregnane 160 mg ~100% 22 hours
Nomegestrol acetate Pregnane 2.5 mg 60% 50 hours [2][3]
Norethisterone Estrane 1 mg 64% 8 hours
Norethisterone acetate Estrane NA ? Prodrug
Noretynodrel Estrane NA ? Prodrug
Norgestimate Gonane NA ? Prodrug
Progesterone (micronized) Pregnane 100–200 mg <2.4% 5 hours [4][5]
Promegestone Pregnane NA ? Prodrug
Tibolone Estrane NA ? Prodrug
Trimegestone Pregnane 0.5 mg ~100% 15 hours
Notes: All by oral administration, unless otherwise noted. Footnotes: a = For the listed pharmacokinetic values. b = By intramuscular injection. Sources: [6][7][8][9][10]

References

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  1. ^ April Hazard Vallerand; Cynthia A Sanoski (4 June 2014). Davis's Canadian Drug Guide for Nurses®. F.A. Davis. pp. 658–. ISBN 978-0-8036-4086-3.
  2. ^ Lello, Stefano (2010). "Nomegestrol Acetate". Drugs. 70 (5): 541–559. doi:10.2165/11532130-000000000-00000. ISSN 0012-6667. PMID 20329803.
  3. ^ Ruan, Xiangyan; Seeger, Harald; Mueck, Alfred O. (2012). "The pharmacology of nomegestrol acetate". Maturitas. 71 (4): 345–353. doi:10.1016/j.maturitas.2012.01.007. ISSN 0378-5122.
  4. ^ Levine H, Watson N (March 2000). "Comparison of the pharmacokinetics of Crinone 8% administered vaginally versus Prometrium administered orally in postmenopausal women(3)". Fertil. Steril. 73 (3): 516–21. doi:10.1016/S0015-0282(99)00553-1. PMID 10689005.
  5. ^ Pickar JH, Bon C, Amadio JM, Mirkin S, Bernick B (December 2015). "Pharmacokinetics of the first combination 17β-estradiol/progesterone capsule in clinical development for menopausal hormone therapy". Menopause. 22 (12): 1308–16. doi:10.1097/GME.0000000000000467. PMC 4666011. PMID 25944519.
  6. ^ Schindler AE, Campagnoli C, Druckmann R, Huber J, Pasqualini JR, Schweppe KW, Thijssen JH (December 2003). "Classification and pharmacology of progestins". Maturitas. 46 Suppl 1: S7–S16. doi:10.1016/j.maturitas.2003.09.014. PMID 14670641.
  7. ^ Kuhl H (2011). "Pharmacology of Progestogens" (PDF). J Reproduktionsmed Endokrinol. 8 (1): 157–177.
  8. ^ Marc A. Fritz; Leon Speroff (28 March 2012). Clinical Gynecologic Endocrinology and Infertility. Lippincott Williams & Wilkins. pp. 761–. ISBN 978-1-4511-4847-3.
  9. ^ Lauritzen C (September 1990). "Clinical use of oestrogens and progestogens". Maturitas. 12 (3): 199–214. doi:10.1016/0378-5122(90)90004-P. PMID 2215269.
  10. ^ Kuhl H (September 1990). "Pharmacokinetics of oestrogens and progestogens". Maturitas. 12 (3): 171–97. doi:10.1016/0378-5122(90)90003-o. PMID 2170822.
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