Klonopin vs. diazepam

It's quite possible I've posted this before, in that case I'm simply repeating myself.

 

This is an old file I stored somewhere on my computer, probably from one of those no longer existing benzo withdrawal forums. I know, bad not to mention a source.

 

The question of diazepam vs. clonazepam comes up so now and then. I've seen different versions, but here it goes:

 

'A Brief Explanation in Favor of Tapering Directly from Klonopin vs. Valium Substitution

 

The power of suggestion is very strong. If we read consistent biased material and don't fully educate ourselves, we are inclined to believe a certain way. The best we can do is to become informed with as much unbiased, educational material and form our own opinions. This is why we have a Resource Center.

 

Here is some information I've compiled regarding benzos due to studying over the years.

 

Valium is 98% bound to plasma proteins. It rapidly crosses the blood-brain barrier and peaks within 2 hours following administration. Following the peak, the initial distribution phase in the brain is one hour. Since Valium is highly bound to plasma proteins, the drug is rapidly redistributed to adipose (fat) tissue. It is stored there, and slowly eliminated over a period of 4 days (or one month for prolonged use). Given that it is redistributed throughout the body, the duration of action following a single dose is 6-8 hours (average 6). The actual half-life of the drug (which is 30-100 hours) means very little.

 

Additionally, the so called "active metabolites" (Oxazepam and Temazepam) are glucuronidated during the metabolic process and are excreted rapidly via the kidneys. So, they are not "active", and they do not count as part of Valium's overall pharmacological effect. Valium's active metabolite is Desmethyldiazepam. This is what exerts an effect. The concept of several active metabolites is praised often with regard to Valium's half life, but what it really means is that the drug is "dirty", i.e. deposits in adipose tissue, hanging around in the body longer than its actual intended use and action. Librium was Sternbach's first creation, and was even dirtier. Then Valium followed. Today, we now have been given the creation of Tranxene (pure Desmethyldiazepam), which is the cleanest Diazepam variant.

 

By comparison, Klonopin is 86% bound to plasma proteins. Therefore, it is less lipophilic (attracted to fats) than Valium, Librium or Tranxene. It also takes longer to peak (2-4 hours). The initial distribution phase is the same as Valium, however, Klonopin is not redistributed to fat tissue like Valium. For this reason, the duration of action is prolonged to 12-18 hours. Klonopin is the longest-acting benzodiazepine that is currently marketed. The half-life ranges from 18-50 hours (mean 34 hours). Klonopin has both a long half-life and very prolonged duration of action. It is also the drug of choice for tapering off of higher-potency benzodiazepines, such as Ativan and Xanax. Valium has little to no affinity for alpha subunits 2 and 3 (which Ativan, Klonopin and Xanax bind to), therefore Valium is more problematic to substitute in place of them. Valium is less selective and binds to alpha subunits 1 and 5, as do all of the low-potency benzodiazepines.

 

The original argument for tapering other benzodiazepines with Valium was because of the ability to taper in smaller amounts due to the fact that Valium is supplied in doses low enough to allow small reductions with the dry taper method.

 

Now that we have better ways, i.e. water/liquid titration and the ability to procure compounded medication, there is less urgency to see Valium substitution as the only viable option for a successful benzodiazepine taper.'

 

As a further reference: https://wiki.tripsit.me/wiki/GABA_Receptors_and_Subunits_Info

Thanks for this info. My psych refuses to switch me over to Valium from Clonazepam, this gives me hope, as I have to do a self-taper.