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MPA has been studied at "massive" dosages of up to 5,000 mg per day orally and 2,000 mg per day via intramuscular injection, without major tolerability or safety issues described. [ 122 ] [ 123 ] [ 124 ] Overdose is not described in the Food and Drug Administration (FDA) product labels for injected MPA (Depo-Provera or Depo-SubQ Provera 104).
Results of the Women's Health Initiative (WHI) menopausal hormone therapy randomized controlled trials; Clinical outcome Hypothesized effect on risk Estrogen and progestogen (CEs Tooltip conjugated estrogens 0.625 mg/day p.o. + MPA Tooltip medroxyprogesterone acetate 2.5 mg/day p.o.) (n = 16,608, with uterus, 5.2–5.6 years follow up) Estrogen ...
There is a case report of progesterone misuse with an oral dosage of 6,400 mg per day. [137] Administration of as much as 500 mg progesterone by intravenous infusion in humans was uneventful in terms of toxicity, but did induce deep sleep, though the individuals were still able to be awakened with sufficient stimulation. [119] [17] [120] [121]
Progesterone is used as part of hormone replacement therapy in people who have low progesterone levels, and for other reasons. For purposes of comparison with normal physiological circumstances, luteal phase levels of progesterone are 4 to 30 ng/mL, while follicular phase levels of progesterone are 0.02 to 0.9 ng/mL, menopausal levels are 0.03 to 0.3 ng/mL, and levels of progesterone in men ...
Two types of female oral contraceptive pill, taken once per day, are widely available: The combined oral contraceptive pill contains estrogen and a progestin; colloquially known as "the Pill". The progestogen-only pill, colloquially known as "minipill". For perfect use it is 99% effective and typical use is 91% effective.
Progesterone and some of its metabolites, such as 5β-dihydroprogesterone, are agonists of the pregnane X receptor (PXR), [30] albeit weakly so (EC 50 >10 μM). [31] In accordance, progesterone induces several hepatic cytochrome P450 enzymes, [32] such as CYP3A4, [33] [34] especially during pregnancy when concentrations are much higher than ...
In the sheep and human, progesterone is the major placental progestogen. The equine placenta produces a variety of progestogens, primarily 5α-dihydroprogesterone and 5α,20α-tetrahydroprogesterone, beginning on day 60. A complete luteo-placental shift occurs by day 120–150.
In terms of dosage equivalence, norethisterone and NETA are typically used at respective dosages of 0.35 mg/day and 0.6 mg/day as progestogen-only contraceptives, and at respective dosages of 0.5–1 mg/day and 1–1.5 mg/day in combination with ethinylestradiol in combined oral contraceptives. [8]