[quote]Dynamo Hum wrote:
This is for Bill. Others feel free to chime in.
I was extolling the virtues of frontloading Nolva 140mg on day 1 of a 4 week SERM PCT (followed by 20mg/d) and a forum member (another board) rebutted with the following:
"Do your eyes and retinas a favor and don’t megadose nolvadex.
From AstraZeneca’s package insert for Nolvadex:
Absorption and Distribution
Following a single oral dose of 20 mg tamoxifen, an average peak plasma concentration of 40 ng/mL (range 35 to 45 ng/mL) occurred approximately 5 hours after dosing. The decline in plasma concentrations of tamoxifen is biphasic with a terminal elimination half-life of about 5 to 7 days."
I would like to respond to the person. What is the appropriate response?
Thanks in advance…[/quote]
Why anyone would do something like this is beyond me.
Tamoxifen itself is not a very strong anti-estrogen; it is a prodrug for 2 metabolites which are 10 to 1000 times more potent inhibitors of the estrogen receptor action.
So the tamoxifen half-life in serum is irrelevant. What matters is the status of the individual’s 2D6 enzyme. The time of elimination of the metabolites is measured in days and weeks.
The cornea is not effected by tamoxifen. Posterior capsular cataracts (lens) occur at an excess rate of 3 per 10,000 over 5 years of use (mostly in older women.)
Retinal changes and liver changes were reported in earlier Scandinavian studies when the dose was presumed to be 30 mg per day,over 2 or 3 years of use.
Tamoxifen actually is a fairly good antilipemic agent in men, and even in peri- and post-menopausal women.