Temazepam: Routes of Administration

[pharmapsyche]

I just want some input from my fellow "drug forumers".

Would sublingual administration increase blood concentrations?
What about an aqueous solution of temazepam? Would that hit harder, last longer and increase blood concentrations as opposed to oral administration?

My big question is rectal administration. Would it be better to rectally administer an aqueous solution of temazepam? I mean, better as in higher blood concentration, stronger effects, etc? Imput would be great.

[Jatelka]

Temazepam is not very water soluble (like most benzos).

Generally speaking: An aqueous solution would hit faster, but taken orally would not increase maximum plasma concentrations, nor would it last longer (duration of action is duration of action after all).

Rectal administration generally means you need a lower dose overall to reach the same plasma concentration, for most drugs (although SWIM does not know this for certain for Temazepam) about a third less. Onset of action is slightly quicker than oral. Temazepam is metabolised in the liver so by administering rectally you could conceivably achieve higher plasma concentrations (by avoiding first pass metabolism).

Have you seen this thread? http://www.drugs-forum.com/forum/showthread.php?t=15884

Sublingual administration will certainly reduce time of onset but SWIM cannot see that plasma concentrations would increase.

Hope this helps.

Look forward to seeing the "Plugged Benzo Trip Report"!

(edited in light of CD-Rose and MickleMouses comments)

[pharmapsyche]

Thanks Jatelka for the info. You are certainly one of my favorite members on this fourm due to your direct answers and careful research. I am going to try rectal administration, I think.. although I'm nervous that it might be a waste of a good 60mgs of temazepam, you know? I'll let you know how it goes. Again, thanks for being.. well, you!

[C.D.rose]

Temazepam is highly water soluble (unlike most benzos). An aqueous solution would hit faster, but taken orally would not increase maximum plasma concentrations, nor would it last longer (duration of action is duration of action after all).
hey jatelka..

how sure are you about the water solubility of temazepam?
SWIM wasn't sure about it but he thought he'd remember differently, and he looked up his bookmarks..

http://www.inchem.org/documents/pims/pharm/pim683.htm
Point 3.3.3

on the other hand, he found a value for water solubility of temazepam via google : 164mg/L - this is not much indeed, but if you had pure temazepam powder, you might well prepare half or 3/4 of a liter...

concerning the discussion, he can't report from experience, but he doubts you'd regret trying it rectally. just try it out..

bye..

[Jatelka]

Edited in view of CD-Rose and MickelMouse's comments: You're exactly right guys and I was mistaken.

See this is what I love about this forum.

[Micklemouse]

Looked around and 164mg/l rings true...

http://redpoll.pharmacy.ualberta.ca/drugbank/cgi-bin/getCard.cgi?CARD=APRD00676.txt

Also found this interesting little article...

http://www.aapspharmscitech.org/view.asp?art=pt070104

If I read this right, then the solubility refers to the parent drug itself.