This was originally published here, in French (link).
We provide this translation for your convenience. Practical aspects may differ where you live.
Isentress HD®: 10 times the dose!
By Charles-Edouard!Isentress HD®, programmed overmedication: 10 times the dose!
With a 1/2 pill strategy, the patient reduces by 2 and is amazed! Instead of a massive dose, she takes a 1/2 dose... massive! How can we judge a reduction without knowing how much we have been cheated? The phase 2 studies should enlighten us... Not at all. Sometimes not published (ex. Efavirenz), they are systematically ignored by the manufacturer and the 'authorities': the maximum dose is always retainedI don't know of any exception. That's how we have 600 mg of EFV, 600 of ABC or 50 of DTG: the tests show that it's too much, but they sit on it! What is the use of testing!!! What is the use of 'authorities' if not as a registration chamber.
The first overmedication is theAbusive Indication Extension; we will come back to this... Another is not to differentiate between attack and maintenance. Let us mentionICCARRoPhobia, MonoPhobia or DemiPhobia.
The arrival of Isentress HD ® will reveal a spectacular increase in dose for the sole benefit of a commercial strategy. We say 10 times the dose, and we will demonstrate it.
Before the marketing of Isentress HD at 1200 mg(sic), we anticipated a drop of the dose.
Marketing will take advantage of a possible drop to twice a day to increase the dose tenfold in order to make it a once a day dose. The reformulation of Raltegravir into r-RAL shows a tripling (at least) of the dose; the too discreet pharmacokinetic tests show that the dose is at least 5 times higher. Finally, the methodological error, a la Levothirox®, shows that this factor, of at least 5, will be 10, in practice. And everyone will see nothing but fire. Your liver will pay for it!
r-RAL: proof by Dutrebis®.
Merck simply demonstrates better bioavailability. No clinical trial, too expensive: the collection of data where Dutrebis® has been distributed may be enough for the manufacturer.
Lamivudine is free, the RAL dose is reduced by 25%, so logically, its marketing would have been a loss of profit for Merck. Merck does not market it and the patients' associations, under perfusion, do not even ask for it!
r-RAL: the reformulated RALTEGRAVIR, better, not marketed...
The dose officially reduced, we will substitute 3TC with r-RAL, and make do with r-RAL alone.
The opportunity is very good: since we can reduce the dose, ensure a better bioavailability, bring everything down to a once-daily dose (QD), we hope to defend our position on the market, and, to do so, we are going to... raise the dose!
r-RAL: the pharmacokinetic proof
On paper, 1600 mg is indigestible... But here, since we can do with r-RAL (300 mg) what was done with RAL (400 mg), only 1200 mg are necessary. It's yucky... But in 2 tablets of 600 mg, it becomes feasible. By taking 1200 mg you don't realize what it's like to take 1600 mg of the previous formula.
Obviously at 1200 mg of r-RAL, the patient gets a nasty boost: the peak concentration will be 4 times higher! 4 times! Four times? No, Charles-Edouard, you are forgetting that we have improved the bioavailability by 25%, so your peak will not be 4 times higher but 5!
Oh the ugly calculation! Let's go see in vivo. Merck published it: multi-dose study of Raltegravir formulations.
At first sight, the peak with r-RAL seems slightly higher than with RAL. Beware! This is a LOG scale! So the pic r-RAL is 5 times that of RAL!!!
r-RAL: 5 times the peak!? No... at least 10!
Imagine if we multiplied by 5 the Efavirenz peak... It's a guaranteed depression/suicide: an overmortality that would be visible(and yet... it would be well hidden...). Well... If we increased the peak of EFV, we would have the usual morons telling us, what they already do, that we have to take it on an empty stomach, or in the evening, or 2 hours before going to bed, or changing creamery, etc...
At 5 times the peak, we understood the topo! But 10 times?! Where does that come from? Where do you get that from? 5, I see... but not 10...
Be patient, my little rabbit... 5 is what you will have seen... Because it has been cleverly made up to you like this... You have seen, but not all of it....
To see it clearly, let's follow closely the Levothyrox® scandal(Merck, again), which the manufacturer, clinicians and 'authorities' (and the 'minister' Buzyn) will have denied en bloc. Some are clever, others gullible
In the news
- Abusive Extension of Indication: Hypothyroidism: some people treated wrongly. 3 millions take Levothyrox®: an absolute aberration... We are only surprised now ???
- Foolish practice of medicine, homeopathy: new complaints. The defense of these charlatans? Suing for non-confraternity. Let us finally decide on the merits!
- Abacavir cleared by its opponents, in spite of themselves. They advanced in camouflage, armed with smoke and mirrors, and the maneuver was foiled. For the French patient, there is no excess cardiovascular risk and the hypothesis of a mechanism of action is taking on a life of its own. We will come back to this...
The French genius
It seems that French research is making fundamental discoveries:
- Descourt / Benkirane and their reservoir marker: CD32a is a marker of a CD4 T-cell HIV reservoir
- Delelis with his 3'PPT mutation
- Estaquier, interviewed here, and his published work: Anti-caspase Q-VD-OPH prevents progression to AIDS in macaques
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Have a good weekend, good stuffing and not too many meds ... Huh?
