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Why taper? SERT transporter occupancy studies show importance of gradual change in plasma concentration

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ChessieCat

That link goes to a log in page.  I am not able to view the pie chart.

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carefulprayerful

Login is required to the website (Medscape).  I have a saved copy of the image, but it is over 40 kB so I can't attach it in this message. 

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ChessieCat

You shouldn't post it anyway as it would be copyrighted.

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JayUT

 

On 11/3/2017 at 8:09 AM, ZK2015 said:

Hi Krasiyan, the equation for Paroxetine will be  Occupancy% = 102*dose/(5.2+dose)

so yes at 5mg you will be at 50% occupancy, however it is really a matter of trial and error you can try different percentages till you find the one that you can tolerate and start calculating your doses based on it.

also as Gridley mentioned you can cut your pills or make liquid from them, personally I found it easier to measure doses from liquid solution.

 

This SERT Occupancy graphs makes such a difference in my understanding of why a slow taper is so important. Especially towards the end of the taper.

 

What would be the occupancy equation for Sertraline? 

 

I am giving this taper another go after being on the sidelines for 3 years. Three years ago, I had somewhat manageable withdrawal problems from 50 mg to 37.5 mg to 25 mg to 12.5 mg, but failed miserably when I CT'd at 12.5 mg. I reinstated and held at 12.5 mg for the past 3 years. It looks like 12.5 mg Sertraline is still around 55% occupancy.

 

In Nov 2018, I decided to drop from 12.5 mg to 6.25 mg. I had some withdrawal, but it appeared to be manageable. Held 6.25 mg for 2 months. Then 6.25 mg to 0 mg was a fail. 6.25 mg is still appears to be around 40% SERT occupancy. I have reinstated at 5 mg 1 week ago and waiting to stabilize.

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Sebas
On 4/24/2014 at 10:04 PM, Mario said:

nice article !

the shapes of the curves also support the idea that the reduction speed should be reduced at lower dosages of SSRI,

like it is suggested in the turtle protocol (http://ssrigr.altervista.org)

 

Hi, read your history below.

What does the turtle protocol mean? I'm currently at approximately 5,6 ml paroxetine and wondering if i should stop tapering at 5,0 ml.

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ChessieCat
1 hour ago, Sebas said:

 

Hi, read your history below.

What does the turtle protocol mean? I'm currently at approximately 5,6 ml paroxetine and wondering if i should stop tapering at 5,0 ml. 

 

I will respond in your Intro topic.

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ChessieCat

I've added this simple explanation to Post #1 of this topic:

 

46 minutes ago, brassmonkey said:

 

Most psych drugs work by changing the levels of a specific neurotransmitter in the body. They usually increase the amount of the neurotransmitter by shutting down the receptor that absorbs it. This is called "down regulating" and a receptor that is down regulated is referred to as being "occupied".  These charts show the percentage of receptors in the body that are "occupied"  at a give dosage of the medication.  The percentage is on the left scale and the dose is across the bottom. Both charts are showing the same thing but the one on the left show the affects of the listed strength of the dose while the one on the right shows the affects of how much of the drug ends up in the blood from taking that dose.

 

If you trace a line up from the 10mg mark on the bottom of the left chaft to where it hits the curve and then over to the left it shows that at a 10mg dose 55% of the receptors in the body have been down regulated (shut off).  Do this again for 20mg and you will see that 75% of the receptors have been shut off.  As you can see the higher the dose the more receptors are shut off, but because of the curve of the line the more you take the less affect it has.

 

The curve tells us several things.  For one thing it shows that the larger the dose the less cumulative affect it has, so in reality a very high dose is not much more effective than a lower one.  But more importantly it shows that at the lower doses (10mg and below) a very small change in dose will result in a very large change in occupancy. A large decrease in occupancy means that there is a lot of healing to be done and a large increase in symptoms is most likely.  The curve also shows why it is so important to go slowly at the lower doses as a very small change in dose causes a very large change in occupancy.

 

These charts are one of the bases from which we worked out the 10% taper rule.  The curve line for a 10% taper very closely matches the curve for occupancy.  By removing the occupancy in a controlled manner we can allow the body to heal itself while the drug is still having an affect and keeping WD symptoms at a minimum. It's like playing Jenga and only removing blocks from the top of the stack.

 

 

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Lakelander82

So if low doses have the vast majority of receptors locked down, why bother tapering at a reduction of 10percent down from 50mg of Sertraline when you could just go straight from 50mg to 12mg in one step and then conduct a 10 percent taper from 12mg to 0.00.

 

 

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Lakelander82

Or indeed, if you wanted to be more cautious, went from 50mg to 25mg directly and then conducted a 10percent taper from 25mg because I can’t really see a great deal of difference in the occupancy between 50mg and 25mg. Basically what I’m saying is far too much time spent tapering needlessly at the higher doses when the graphs don’t really back it up. 

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Altostrata

It's likely that many people are taking dosages with excess capacity, i.e., they could reduce by 25% and still maintain full SERT saturation, then taper by 10% from there.

 

HOWEVER, we don't know what your individual curve looks like. It could be that a quarter of your dosage saturates your SERT receptors, or it could be that you need 90% for saturation, and a 25% reduction might throw you into acute withdrawal.

 

Admittedly -- we make this clear -- an initial 10% reduction is very cautious. But being that we only offer peer support over the Internet, we can't rescue you should you reduce by 25% and panic because you have severe symptoms. So we advise everyone to go the more cautious route of 10%, where if you do get withdrawal symptoms from tapering, they are less likely to be severe.

 

 

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Lakelander82

Realistically though, measuring out  such minuscule doses accurately, especially using your own homemade suspension is next to near impossible. Even if you carry out everything the same every time, you could be getting 12mg one day, 8mg the next, 14mg the next day, 5 mg the day after that. Your dose could be all over the place each day. When I got down to 12mg (theoretically) it looked like I was taking water with a few granules of powder in it, there could have been 2mgs in it for all i know. Everything is just guess work. 

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Altostrata

Many people have successfully tapered with homemade liquids. If you're trying to rationalize making a big decrease in dosage because of difficulty measuring, you're wrong.

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Lakelander82

I’m not trying to rationalise any big decrease, I’m merely saying that there is most likely significant disparities in dosages by making up your own suspension everyday...no matter how careful you are. 

 

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Altostrata

Making your own liquid suspension is not ideal. A liquid compounded by a pharmacy would be preferable, but many people can't afford it or don't have access to a reliable compounding pharmacy.

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