T Nation

Tamoxifen Citrate (Nolva) Frontload

This is for Bill. Others feel free to chime in.

Hey Bill,

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:

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"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."

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I would like to respond to the person. What is the appropriate response?

Thanks in advance…

Seems that forum member has his nolva and clomid potential sides mixed up.

[quote]chillain wrote:
Seems that forum member has his nolva and clomid potential sides mixed up.
[/quote]

Not true.

The only reason you notice bad sides with clomid is because it needs to be dosed so high to be effective.

Dose clomid or any other SERM high enough and youll get the same floaties and other side effects so commonly associated with clomid.

Hey Bill. How was the wedding?

Bump

I agree… i always was under the impression tamox had negative actions on lipid prfiles, carcinogens, and many other nasties… i personally would never take 140mg.

Brook

Have some patience buddy! :wink:

Just trying to keep the thread visible. I know BR is away for a bit.

What exactly are you asking Dynamo?
Nolvadex HAS been shown to cause change in the part of the eye known as the cornea.
It can affect visual acuity, or cause blood clots in the eye. I don’t believe that they are very likely, but it can happen.

[quote] Brook wrote:
I agree… i always was under the impression tamox had negative actions on lipid prfiles, carcinogens, and many other nasties… i personally would never take 140mg.

Brook[/quote]

Hmmm, carcinogenic;yes

But I believe it was actually shown to have a positive effect on the lipid profiles.

Although this effect was less than the effect in women.

Tamoxifen has estrogenic effects in the liver, it is after all an estrogen.

[quote]egnatiosj wrote:
What exactly are you asking Dynamo?
Nolvadex HAS been shown to cause change in the part of the eye known as the cornea.
It can affect visual acuity, or cause blood clots in the eye. I don’t believe that they are very likely, but it can happen. [/quote]

I am asking if the argument against frontloading Tamoxifen Citrate at 140mgs on day 1 of a 4 week PCT dosed at 20mg/d after day 1 is valid or not. The argument being that “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.”

In other words is that 40 ng/mL average peak plasma concentration that occured 5 hours after dosing the desired level or some step on the way to the desired level? Because if the desired level is achieved that quickly after dosing 20mg, why would there be any need to frontload?

Bill has stated that it takes 6 days for blood levels to reach the desired level when not frontloading. This fellow from the other board disputed that with this argument. I would like to know if that holds water?

bump (Bill will have a lot of catch up to do so I am lifting this thread to an easy access location).

Did this ever get answered?

Bill is MIA. Anyone know what’s up?

He is a busy man, and is not here all the time.

I am sure you could find out the answer yourself.

I personally would not use that amount - or even frontload the drug, it works just fine taken normally for me.

I think that the dose 140mg would cause little issue in the majority of the population if used once. I am certain of that if that is the peak blood level after 6 days of 40mg/day.
I would quickly assume that the guy who disagreed was thinking (mistakenly in this case) about prolonged dosing at that level.

Brook

Bump.

[quote]Dynamo Hum wrote:
This is for Bill. Others feel free to chime in.

Hey Bill,

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.

Other errors:

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.

DrSkeptix,

So in your opinion there is no advantage in frontloading Tamoxifen Citrate (Nolva) for a SERM PCT or gyno flareup.

[quote]Dynamo Hum wrote:
DrSkeptix,

So in your opinion there is no advantage in frontloading Tamoxifen Citrate (Nolva) for a SERM PCT or gyno flareup.[/quote]

I will correct myself, with your permission, on one item. An interested reader pm’ed me with more questions on corneal changes.
There are 12 articles since 1979 in which corneal changes or deposits are mentioned. One is of interest: in a Turkish prospective study of only 22 women, 72% of them had microscopic deposits in the corneal layers (I do not know if this temporary or permanent). But having a microscopic change does not merit worry if there is no clinical disease or disability associated with it. I guarantee to you that 72% of women taking tamoxifen do not report visual side effects. More like none.

To answer your question, DH, I do not know–Bill Roberts will have a better answer for you. No one does studies of this and guys won’t participate in them.
But let’s guess. First, a big bolus of tamoxifen may not be handled the same as a reasonable dose (i.e., pharmacology is not uniform and scalable). But if one cycles an aromatisable androgen over weeks, then the kinetics of tamoxifen (daily 20 mg)would match its adverse effects, over weeks. Maybe.

I forgot to mention that the front load was recommended to be split throughout the first day so as to maximize absorption.

Thanks for the reply and data.