The Pharmacokinetic Profile of Elestrin
Elestrin has the following pharmacokinetic (PK) profilea:
- Half-life is 54.8 hours with the 1-pump (0.52 mg/day of estradiol) dose and 75.2 hours for the 2-pump (1.04 mg/day of estradiol) dose2
- Steady-state serum concentrations of estradiol are achieved in approximately 3 days following daily application of Elestrin to the upper arm
- Tmax is reached within 18 hours with the 1-pump (0.52 mg/day of estradiol) dose; 4 hours with the 2-pump (1.04 mg/day of estradiol) dose.b,
With the 1-pump (0.52 mg/day of estradiol) dose, Tmax was 18 hours and significantly reduced, versus placebo, the frequency of hot flushes as early as week 5. The 2-pump (1.04 mg/day of estradiol) dose has a Tmax of 4 hours and significantly reduced, versus placebo, the frequency of hot flushes as early as week 3.3 Steady-state serum concentrations were achieved in approximately 3 days.
No significant estradiol transfer with Elestrin
Two and 8 hours after women applied 2.6 g Elestrin to one arm (12 women per time point), they engaged in direct arm-to-arm contact with a male partner for 5 minutes. No significant changes in estradiol PK parameters were observed in the male partners after contact.2 Still, if someone else is exposed to Elestrin by direct contact with the gel, that person should wash the area of contact with soap and water as soon as possible. The longer the gel is in contact with the skin before washing, the greater is the chance that the other person will absorb some of the estrogen hormone. This is especially important for men and children. Keep Elestrin out of the reach of children.
a All PK parameters except half-life are unadjusted for baseline concentrations and were measured after 14 days of dosing. Half-life is adjusted for baseline concentrations after multiple doses to upper arm and was measured after the last daily application.
b Shown as median.