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Worrying stats about Diazepam and protein binding


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Hi guys,

This is just an excerpt from Google I was interested in.

It shows the percentage of protein binding, which occurs with a drug like Diazepam.

The results are quite shocking.

It is 98% binding

No wonder we suffer crazy withdrawals.

Protein binding percentage of Diazepam

 

Dave.

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Most drugs bind protein (albumin). It doesn't mean anything and has nothing to do with withdrawals.

?

I thought protein binding related to the affinity of the drug in the system.

As well as upregulation of GABA-a receptors, doesn't the body need to rid the toxins of the benzo stored as fat in withdrawal?

Dave.

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No, protein binding is not related to the affinity of the drug in the system. Affinity means how strongly the drug binds to its receptor. However, protein can "store" some of the drug. But most importantly, it's not the protein binding that causes withdrawals.

 

The body does need to get rid of benzos for GABA receptor upregulation. Although it's not clear if GABA receptors actually downregulate or something else happens to them that prevents them from functioning.

 

Fat in the body can also "store" benzos.

 

However, the important thing is the half-life of the benzos, no matter where they are stored. The half-life for most benzos is well known and you can find it in many places (e.g., Ashton manual).

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No, protein binding is not related to the affinity of the drug in the system. Affinity means how strongly the drug binds to its receptor. However, protein can "store" some of the drug. But most importantly, it's not the protein binding that causes withdrawals.

 

The body does need to get rid of benzos for GABA receptor upregulation. Although it's not clear if GABA receptors actually downregulate or something else happens to them that prevents them from functioning.

 

Fat in the body can also "store" benzos.

 

However, the important thing is the half-life of the benzos, no matter where they are stored. The half-life for most benzos is well known and you can find it in many places (e.g., Ashton manual).

Hey Maugham1,

Thanks for clearing this up.

So protein binding has little or nothing to do with the severity of benzo withdrawals? Phew...

Dave.

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