Global InformationPharmacokinetics of progesterone information
 | |
| Clinical data | |
|---|---|
| Routes of administration | • By mouth (capsule) • Sublingual (tablet) • Transdermal (cream, gel) • Vaginal (capsule, tablet, gel, suppository, ring) • Rectal (suppository) • IM injection (oil solution) • SC injection (aq. soln.) • Intrauterine (IUD) |
| Drug class | Progestogen; Antimineralocorticoid; Neurosteroid |
| Pharmacokinetic data | |
| Bioavailability | Oral: <2.4%[1] Vaginal (micronized insert): 4–8%[2][3][4] |
| Protein binding | 98–99%:[5][6] • Albumin: 80% • CBG: 18% • SHBG: <1% • Free: 1–2% |
| Metabolism | Mainly liver: • 5α- and 5β-reductase • 3α- and 3β-HSD • 20α- and 20β-HSD • Conjugation • 17α-Hydroxylase • 21-Hydroxylase • CYPs (e.g., CYP3A4) |
| Metabolites | • Dihydroprogesterones • Pregnanolones • Pregnanediols • 20α-Hydroxyprogesterone • 17α-Hydroxyprogesterone • Pregnanetriols • 11-Deoxycorticosterone (And glucuronide/sulfate conjugates) |
| Elimination half-life | • Oral: 5–10 hours (with food)[7][8] • Sublingual: 6–7 hours[9] • Vaginal: 14–50 hours[9][10] • Transdermal: 30–40 hours[11] • IM: 20–28 hours[10][12][13] • SC: 13–18 hours[13] • IV: 3–90 minutes[14] |
| Excretion | Bile and urine[15][16] |
The pharmacokinetics of progesterone, concerns the pharmacodynamics, pharmacokinetics, and various routes of administration of progesterone.[17][18]
Progesterone is a naturally occurring and bioidentical progestogen, or an agonist of the progesterone receptor, the biological target of progestogens like endogenous progesterone.[17] Progesterone also has antimineralocorticoid and inhibitory neurosteroid activity, whereas it appears to have little or no glucocorticoid or antiandrogenic activity and has no androgenic activity.[17] Because of its progestogenic activity, progesterone has functional antiestrogenic effects in certain tissues such as the uterus, cervix, and vagina.[17] In addition, progesterone has antigonadotropic effects due to its progestogenic activity and can inhibit fertility and suppress sex hormone production.[17] Progesterone differs from progestins (synthetic progestogens) like medroxyprogesterone acetate and norethisterone, with implications for pharmacodynamics and pharmacokinetics as well as efficacy, tolerability, and safety.[17]
Progesterone can be taken by mouth, in through the vagina, and by injection into muscle or fat, among other routes.[17] A progesterone vaginal ring and progesterone intrauterine device are also available as pharmaceutical products.[19][20]
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pmid24606090was invoked but never defined (see the help page). - ^ Fritz MA, Speroff L (28 March 2012). Clinical Gynecologic Endocrinology and Infertility. Lippincott Williams & Wilkins. pp. 44–. ISBN 978-1-4511-4847-3.
- ^ Marshall WJ, Bangert SK (2008). Clinical Chemistry. Elsevier Health Sciences. pp. 192–. ISBN 978-0-7234-3455-9.
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ХомякМамчур2014was invoked but never defined (see the help page). - ^ a b "Crinone® 4% and Crinone® 8% (progesterone gel)" (PDF). Watson Pharma, Inc. U.S. Food and Drug Administration. August 2013.
- ^ Mircioiu C, Perju A, Griu E, Calin G, Neagu A, Enachescu D, Miron DS (1998). "Pharmacokinetics of progesterone in postmenopausal women: 2. Pharmacokinetics following percutaneous administration". European Journal of Drug Metabolism and Pharmacokinetics. 23 (3): 397–402. doi:10.1007/bf03192300. PMID 9842983. S2CID 32772029.
- ^ Simon JA, Robinson DE, Andrews MC, Hildebrand JR, Rocci ML, Blake RE, Hodgen GD (July 1993). "The absorption of oral micronized progesterone: the effect of food, dose proportionality, and comparison with intramuscular progesterone". Fertility and Sterility. 60 (1): 26–33. doi:10.1016/S0015-0282(16)56031-2. PMID 8513955.
- ^ a b Cite error: The named reference
pmid26342177was invoked but never defined (see the help page). - ^ Aufrère MB, Benson H (June 1976). "Progesterone: an overview and recent advances". Journal of Pharmaceutical Sciences. 65 (6): 783–800. doi:10.1002/jps.2600650602. PMID 945344.
- ^ "PROMETRIUM (progesterone, USP)" (PDF). Solvay Pharmaceuticals, Inc. U.S. Food and Drug Administration. 1998.
- ^ "Progesterone injection" (PDF). Watson Laboratories, Inc. U.S. Food and Drug Administration. January 2007.
- ^ a b c d e f g Kuhl H (August 2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration" (PDF). Climacteric. 8 (Suppl 1): 3–63. doi:10.1080/13697130500148875. PMID 16112947. S2CID 24616324.
- ^ Unfer V, di Renzo GC, Gerli S, Casini ML (2006). "The Use of Progesterone in Clinical Practice: Evaluation of its Efficacy in Diverse Indications Using Different Routes of Administration". Current Drug Therapy. 1 (2): 211–219. doi:10.2174/157488506776930923.
- ^ Whitaker A, Gilliam M (2014). Contraception for Adolescent and Young Adult Women. Springer. p. 98. ISBN 9781461465799.
- ^ Chaudhuri SK (2007). Practice Of Fertility Control: A Comprehensive Manual (7th ed.). Elsevier India. p. 153. ISBN 978-81-312-1150-2.