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Pharmacokinetics of progesterone
From Wikipedia, the free encyclopedia
The pharmacokinetics of progesterone, concerns the pharmacodynamics, pharmacokinetics, and various routes of administration of progesterone.[17][18]
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Clinical data | |
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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.Tooltip aqueous solution) • Intrauterine (IUDTooltip intrauterine device) |
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% • CBGTooltip Corticosteroid-binding globulin: 18% • SHBGTooltip Sex hormone-binding globulin: <1% • Free: 1–2% |
Metabolism | Mainly liver: • 5α- and 5β-reductase • 3α-Tooltip 3α-Hydroxysteroid dehydrogenase and 3β-HSDTooltip 3β-Hydroxysteroid dehydrogenase • 20α-Tooltip 20α-Hydroxysteroid dehydrogenase and 20β-HSDTooltip 20β-Hydroxysteroid dehydrogenase • Conjugation • 17α-Hydroxylase • 21-Hydroxylase • CYPsTooltip CYP (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] • IVTooltip Intravenous injection: 3–90 minutes[14] |
Excretion | Bile and urine[15][16] |
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]