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7-Keto-DHEA (also known as 7-Keto, 7-ketodehydroepiandrosterone, or 7-oxodehydroepiandrosterone) is a steroid produced by metabolism of the prohormone It is often used as the acetate ester prodrug 7-Keto-DHEA acetate.
7-Keto is unique among other derivatives of DHEA because of its oxygenated 7-position. This molecular configuration imparts different characteristics to the molecule, and research reveals that 7-Keto DHEA has multiple distinct effects in the body.Such as, Increased metabolism/weight loss, Age-related immune enhancement
Similar to DHEA, 7-keto-DHEA is rapidly sulfated to 7-keto-DHEA sulfate in the body. An analytical method was developed for quantification of 7-keto-DHEA sulfate in human plasma. This was an HPLC method, which utilized calibration curves for 7-keto-DHEA sulfate in the range of 10 to 500 ng/ml.
Trough levels were measured after each escalating dose sequence; 0, 50, 100 and 200 mg per day. Trough plasma concentrations increased proportionally to the daily dose. Mean trough levels (15.8 ng/ml) after 1 week of dosing at 200 mg/day were similar to those determined after 4 weeks of dosing (16.3 ng/ml). This indicated that the ratio of the formation rate of this metabolite to its elimination clearance is constant during multiple dosing and does not accumulate.
After a twelve-hour washout period, all 22 subjects were given a single dose of 7-keto-DHEA at 100 mg and plasma levels were obtained at 0.25, 0.50, 1.0, 2.0, 4.0, 6.0 and 12.0 hrs after the dose. The mean plasma concentrations as measured in the study demonstrated a peak plasma level of 158 ng/ml, which occurred at 2.2 hours after the dose. The average elimination half-life was determined to be 2.17 hours. Based on the data, the dosing regime of twice per day was recommended as the ideal dosing schedule with steady state blood levels being the goal.
A one-compartment model was assumed with first order absorption and no lag phase. The results of these simulations using this pharmacokinetic model showed that there was good agreement between: a) the simulated and measured means of the trough plasma levels, and b) the plasma concentrations of a single 100 mg oral dose.
The pharmacokinetic analysis revealed that 7-keto-DHEA is rapidly absorbed and converted to its sulfate derivative, it reaches peak plasma concentrations in 2.2 hours, and it has a half-life of 2.17 hours. There is no accumulation with repeated dosing and, with twice daily dosing, should reach a steady state plasma level in 11 hours.
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